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LIPIDOMIC BIOMARKERS FOR THE PREDICTION OF CARDIOVASCULAR OUTCOMES IN CORONARY ARTERY DISEASE PATIENTS NOT UNDERGOING STATIN TREATMENT

Thu, 03 Nov 2016 08:00:00 EDT

The present invention inter alia provides a method, and use thereof, of predicting severe CVD complications such as AMI or CVD death by detecting the lipid concentrations or lipid ratios of a biological sample and comparing it to a control and has identified specific lipid markers that are more specific and sensitive in predicting these CVD complications than currently utilized clinical markers. Also provided are antibodies towards said lipids, and the use thereof for predicting, diagnosing, preventing and/or treating CVD complications. The invention additionally relates to kits comprising lipids and/or an antibody thereto, for use in the prediction and/or diagnosis of CVD complications.



METHODS AND KITS FOR DETERMINING RISK FOR DEVELOPING ALZHEIMER'S DISEASE AND PREVENTION OR TREATMENT THEREOF

Thu, 03 Nov 2016 08:00:00 EDT

Methods are disclosed for determining a patient's risk for developing Alzheimer's disease and preventing or treating Alzheimer's disease. Kits for assessing a patient's risk of developing Alzheimer's are also provided.



BIOMARKERS AND METHODS FOR PROGRESSION PREDICTION FOR CHRONIC KIDNEY DISEASE

Thu, 03 Nov 2016 08:00:00 EDT

Subject of the present invention are biomarkers and methods for the identification of an increased risk of the progression of chronic kidney disease (CKD), or for monitoring chronic kidney disease therapy, comprising the detecting the level of one or more of NTpro BNP, EGF, Apo H, GDF-15, and albumin-to-creatinine ratio.



HIGH-AFFINITY SMALL MOLECULE FORMYLPEPTIDE RECEPTOR LIGANDS FROM SCREENING OF COMBINATORIAL MIXTURE-BASED LIBRARIES

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides novel methods and assays for high-throughput screening of combinatorial libraries to identify FPR1 and/or FPR2 ligands (e.g., agonists and/or antagonists), preferably FPR1 agonists and/or FPR2 antagonists, by positional scanning deconvolution. The invention also provides novel FPR1 and FPR2 ligands (e.g, agonists and antagonists), related pharmaceutical compositions and methods of treating FPR1 and FPR2-related disorders.



USE OF BUBR1 AS A BIOMARKER OF DRUG RESPONSE TO FURAZANOBENZIMIDAZOLES

Thu, 03 Nov 2016 08:00:00 EDT

Use of BUBR1 as a biomarker for predicting the response to a compound, preferably resistance of a disease such as cancer in a subject, wherein the compound is a compound of general formula I wherein R represents phenyl, thienyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents a group C═Y, wherein Y stands for oxygen or nitrogen substituted by hydroxy or lower alkoxy; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R2, R3 and R6 represent hydrogen; R4 and R5, independently of each other, represent hydrogen, lower alkyl or lower alkoxy; or R4 and R5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof; or wherein R represents phenyl or pyridinyl wherein phenyl is optionally substituted by one or two substituents independently selected from alkyl, halo-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, acyloxy-lower alkyl, phenyl, hydroxy, lower alkoxy, hydroxy-lower alkoxy, lower alkoxy-lower alkoxy, phenyl-lower alkoxy, lower alkylcarbonyloxy, amino, monoalkylamino, dialkylamino, lower alkoxycarbonylamino, lower alkylcarbonylamino, substituted amino wherein the two substituents on nitrogen form together with the nitrogen heterocyclyl, lower alkylcarbonyl, carboxy, lower alkoxycarbonyl, formyl, cyano, halogen, and nitro; and wherein two adjacent substituents are methylenedioxy; and wherein pyridinyl is optionally substituted by lower alkoxy, amino or halogen; X represents oxygen; R1 represents hydrogen, lower alkylcarbonyl, hydroxy-lower alkyl or cyano-lower alkyl; R2, R3 and R6 represent hydrogen; R4 and R5, independently of each other, represent hydrogen, lower alkyl or lower alkoxy; or R4 and R5 together represent methylenedioxy; and pharmaceutically acceptable derivatives thereof. Methods of treatment of neoplastic and autoimmune diseases with these compounds are also disclosed.



METHOD AND APPARATUS FOR PREDICTING EFFECTIVE DOSE OR SENSITIVITY OF 5-HYDROXY-1H-IMIDAZOLE-4-CARBOXAMIDE, METHOD FOR DETERMINING AMOUNT OF XANTHOSINE MONOPHOSPHATE, AND TREATMENT AGENT AND METHOD FOR TREATING MYELODYSPLASTIC SYNDROME

Thu, 03 Nov 2016 08:00:00 EDT

An object of the present invention is to provide a method and apparatus for predicting an effective dose of or the sensitivity to 5-hydroxy-1H-imidazole-4-carboxamide, which are capable of performing a determination in a simple operation and a short time, a method for determining amounts of xanthosine monophosphate, and a treatment agent and treatment method for treating myelodysplastic syndrome. According to the present invention, provided are a method for predicting an effective dose of or the sensitivity to 5-hydroxy-1H-imidazole-4-carboxamide, including determining amounts of xanthosine monophosphate in blood and a prediction apparatus, a method for determining amounts of xanthosine monophosphate, including determining xanthosine monophosphate in blood in two different determining conditions by mass spectrometry, and a treatment agent and treatment method for treating myelodysplastic syndrome.



Pathogenesis Quantification Systems and Treatment Methods for Citrus Greening Blight

Thu, 03 Nov 2016 08:00:00 EDT

The invention relates to a novel pathogenesis model, method, or kit for detecting pathogenesis in a subject. In particular, the invention provides a pathogen index derived from a ratio of the amount of dual pathogen targets relative to the amount of host quantitative measures. The pathogen index is used in diagnosis, prognosis, and/or treatment strategy of any disease, including citrus greening diseases (HLB). Research tools and methods for screening drugs for treating or preventing citrus greening diseases, as well as treatment or prevention methods for citrus greening diseases are also provided.



METHODS AND COMPOSITIONS FOR IDENTIFICATION OF PROSTATE CANCER MARKERS

Thu, 03 Nov 2016 08:00:00 EDT

A method for diagnosing and treating prostate cancer in a human subject is provided, the method comprises: a. providing a sample of prostate tissue, blood, or urine from the subject; b. determining the level of expression of SEQ ID NO: 1 and the expression of SEQ ID NO: 5 in the sample, wherein an increased level of expression of SEQ ID NO:1 and a reduced level of expression of SEQ ID NO: 5 in the sample is indicative of a diagnosis that the subject has prostate cancer; and c. administering a therapeutically effective prostate cancer treatment selected from the group consisting of an androgen receptor (AR)-targeted therapy, an antimicrotubule agent, an alkylating agent and an anthracenedione to the subject to treat the prostate cancer in the human subject diagnosed with prostate cancer.



TET2 AS A DIAGNOSTIC AND PRONOSTIC MARKER IN HEMATOPOIETIC NEOPLASMS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention concerns an in vitro method for diagnosing a myeloid tumour or a lymphoid tumour in a subject, which comprises the step of analyzing a biological sample from said subject by (i) detecting the presence of a mutation in the Ten Eleven Translocation protein family member 2 gene (TET2) coding for the polypeptide having the sequence SEQ ID NO: 2, and/or (ii) analyzing the expression of the TET2 gene; wherein the detection of such a TET2 mutation, of the absence of expression of TET2 or of the expression of a truncated TET2 is indicative of a subject developing or predisposed to develop a myeloid tumour or a lymphoid tumour.



DDX3 AS A BIOMARKER FOR CANCER AND METHODS RELATED THERETO

Thu, 03 Nov 2016 08:00:00 EDT

The invention encompasses methods for treating or preventing diseases and disorders associated abnormal cell growth, for example, treating or preventing cancer or tumor growth, by administering to a subject in need thereof a composition comprising a therapeutically or prophylactically effective amount of a compound that downregulates DDX3, for example a fused diimidazodiazepine ring compound or a pharmaceutically acceptable salt thereof. The invention also encompasses the use of DDX3 as a biomarker for diagnostic and treatment purposes, for example, to identify a hyperproliferative disorder susceptible to treatment by down regulation of DDX3.



Method for Detecting Chromosomal Rearrangements

Thu, 03 Nov 2016 08:00:00 EDT

An object of the invention is an in vitro method for detecting chromosomal rearrangements between at least two specific chromosomal regions in a biological sample of a human subject, which comprises the steps of: a) isolating deoxyribonucleic acid (DNA) molecules comprising said specific chromosomal regions from said biological sample, wherein said DNA molecules have an average length of X base pairs; b)amplifying the DNA molecules of step a) by a multiplex polymerase chain reaction assay, said assay comprising at least two sets of primers, wherein each set of primers is capable of hybridizing with a specific reference chromosomal region, and each set of primer comprises a plurality of primers, said primers being capable of hybridizing to a nucleic acid strand of one of the said specific chromosomal regions at sites regularly spaced of less than X/2 base pairs; and hybridizing the product of the amplification of step b) with at least one set of nucleic probes.



PREDICTING THERAPEUTIC RESPONSE IN PARKINSON'S DISEASE

Thu, 03 Nov 2016 08:00:00 EDT

Provided herein are methods and compositions for determining the susceptibility of Parkinson's disease patients to optimized drug therapy (ODT) and or deep brain stimulation (DBS) therapy.



AP5B1 AS A NEW MARKER FOR MODERATE TO SEVERE ACNE

Thu, 03 Nov 2016 08:00:00 EDT

The invention relates to the identification of Adaptor-Related Protein Complex 5, subunit 1 (AP5B1) as a biomarker of moderate to severe acne. The invention also relates to products and methods for detecting, diagnosing, staging, treating or monitoring the course of acne in a human subject.



GENETIC VARIANTS AS MARKERS FOR USE IN DIAGNOSIS, PROGNOSIS AND TREATMENT OF EOSINOPHILIA, ASTHMA AND MYOCARDIAL INFARCTION

Thu, 03 Nov 2016 08:00:00 EDT

Polymorphic variants (e.g., certain alleles of polymorphic markers) that have been found to be associated with high blood eosinophil counts, conditions causative of eosinophilia (e.g., asthma, myocardial infarction), and/or hypertension are provided herein. Such polymorphic markers are useful for diagnostic purposes, such as in methods of determining a susceptility, and for prognostic purposes, including methods of predicting prognosis and methods of assessing an individual for probability of a response to a therapeutic agent, as further described herein. Further applications utilize the polymorphic markers of the invention include, screening methods and genotyping methods. The invention furthermore provides related kits, computer-readable medium, and apparatus.



NON-CODING RNA OF SALMONELLA AND IDENTIFICATION AND USE THEREOF

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides Salmonella non-coding RNA and the identification and application thereof. In particular, the present invention proves through experiments that a Salmonella bacterium delivers non-coding RNAs (ncRNAs) encoded by the bacterium itself into a host cell, generates milRNAs similar to microRNAs by means of a microRNA splicing system in the cell, regulates the immune system with the milRNAs, and further protects the Salmonella bacterium from being cleared by the host. Adsorbing milRNAs using milRNA inhibitors can effectively inhibit the survival ability of the bacterium in the cell, leading to a reduced vitality of the bacterium. The present invention further provides relevant reagents and methods for effective detection of, treatment to and study on Salmonella bacteria or Salmonella infectious diseases.



MODULATORS OF GLYCEROPHOSPHODIESTER PHOSPHODIESTERASE PROTEINS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to glycerophosphodiester phosphodiesterase (GDE) proteins. More specifically, the present invention relates to targeting GDE proteins to modulate its glycosylphosphatidylinositol (GPI)-cleaving activity. In a specific embodiment, the present invention provides a GDE modulator that modulates the surface GPI anchor cleavage activity of GDE.



SYNTHESIS METHOD FOR L-CYCLIC ALKYL AMINO ACID AND PHARMACEUTICAL COMPOSITION HAVING THEREOF

Thu, 03 Nov 2016 08:00:00 EDT

A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD+, and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is where n1≧1, m1≧0 and the M1 is H or a monovalent cation; the Structural Formula (II) is where n2≧0, m2≧0, the M2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.



ADENO-ASSOCIATED VIRAL (AAV) VECTORS USEFUL FOR TRASDUCING ADIPOSE TISSUE

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to adeno-associated viral vector useful for transducing adipose tissue. The invention also relates to polynucleotides, plasmids, vectors and methods for the production of such adeno-associated viral vector. The invention also relates to gene therapy methods useful for the treatment of a disease that requires the regulation of the expression levels of a gene.



Use of miR-494 to Modulate TRAIL-induced Apoptosis through BIM Down-regulation

Thu, 03 Nov 2016 08:00:00 EDT

Methods and compositions for inhibiting tumorigenicity both in vitro and in vivo in a subject in need thereof, comprising administering an effective amount of an anti-miR-494 nucleic acid construct sufficient to target one or more tumor suppressor genes (TSGs) are described. Activation of the ERK1/2 pathway is a major determinant of diverse cellular processes and cancer development and is responsible for the transcription of several important miRNAs. Described herein is a link between the ERK1/2 pathway and BIM expression through miR-494. This ERK1/2 pathway regulates apoptosis and cell proliferation through miR-494 and mechanisms responsible for TRAIL resistance. Materials and methods related to the study and treatment of cancer are described.



METHODS AND COMPOSITIONS FOR TREATING CANCER USING PEPTIDE NUCLIEC ACID-BASED AGENTS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides compositions and methods for treating cancer with peptide nucleic acid agents. In some embodiments, the present invention provides methods and compositions relating to peptide nucleic acid agents that target oncogenes. For example, the present invention provides compositions, including pharmaceutical compositions, comprising agents specific for BRAF V600E inhibition, or fragments or characteristic portions thereof. The present invention further provides various therapeutic and/or diagnostic methods of using BRAF V600E specific peptide nucleic acid agents and/or compositions.



METHODS FOR TREATMENT OF ALPORT SYNDROME

Thu, 03 Nov 2016 08:00:00 EDT

Provided herein are methods for the treatment of Alport Syndrome, using modified oligonucleotides targeted to miR-21. In certain embodiments, a modified oligonucleotide targeted to miR-21 improves kidney function and/or reduces fibrosis in subjects having Alport Syndrome. In certain embodiments, administration of a modified oligonucleotide targeted to miR-21 delays the onset of end-stage renal disease in a subject having Alport Syndrome. In certain embodiments, a modified oligonucleotide targeted to miR-21 delays the need for dialysis or kidney transplant in a subject having Alport Syndrome.



ARTIFICIAL MATCH-TYPE miRNA FOR CONTROLLING GENE EXPRESSION AND USE THEREFOR

Thu, 03 Nov 2016 08:00:00 EDT

The invention provides an artificial match-type miRNA utilizing miRNA. A In particular, the invention provides a single strand nucleic acid containing an X region and a Y region, wherein the 3′-terminal of the X region and the 5′-terminal of the Y region are linked via a linker region of a non-nucleotide structure, the X region contains a guide strand sequence of a mature miRNA, and the Y region contains a sequence completely complementary to the X region is an artificial match-type miRNA. The artificial match-type miRNA can suppress expression of the target gene.



SEQUENCE-SPECIFIC INHIBITION OF SMALL RNA FUNCTION

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to the discovery of a method for inhibiting RNA silencing in a target sequence-specific manner. RNA silencing requires a set of conserved cellular factors to suppress expression of gene-encoded polypeptide. The invention provides compositions for sequence-specific inactivation of the RISC component of the RNA silencing pathway, and methods of use thereof. The RISC inactivators of the present invention enable a variety of methods for identifying and characterizing miRNAs and siRNAs, RISC-associated factors, and agents capable of modulating RNA silencing. Therapeutic methods and compositions incorporating RISC inactivators and therapeutic agents identified through use of RISC inactivators are also featured.



FULLY STABILIZED ASYMMETRIC SIRNA

Thu, 03 Nov 2016 08:00:00 EDT

Provided herein are self-delivering oligonucleotides that are characterized by efficient RISC entry, minimum immune response and off-target effects, efficient cellular uptake without formulation, and efficient and specific tissue distribution.



Novel non-coding RNA, cancer target and compounds for cancer treatment

Thu, 03 Nov 2016 08:00:00 EDT

The invention relates to the novel long non-coding BARD1 RNA molecule BARD1 9′L, siRNAs for therapeutic use and methods for the detection of BARD1 9′L as well as a promoters driving the expression of BARD1 9′L.



NOVEL FUSION GENES AS FACTORS RESPONSIBLE FOR GASTRIC CANCER

Thu, 03 Nov 2016 08:00:00 EDT

To identify mutations that can serve as indicators for predicting the effectiveness of drug treatments in cancers such as gastric cancer; to provide a means for detecting said mutations; and to provide a means for identifying, based on said mutations, patients with cancer or subjects with a risk of cancer, in whom drugs targeting genes having said mutations or proteins encoded by said genes show a therapeutic effect. A method for detecting a gene fusion serving as a responsible mutation (driver mutation) for cancer, the method comprising the step of detecting any one of an ATG3-EPHB1 fusion polynucleotide, a TNIK-RNF123 fusion polynucleotide, or an SLC12A2-NRG2 fusion polynucleotide, or a polypeptide encoded thereby, in an isolated sample from a subject.



METHODS FOR DEPYROGENATION OF PROTEINS

Thu, 03 Nov 2016 08:00:00 EDT

Methods relating to depyrogenaton of proteins including vapor hydrogen peroxide treatment, gaseous chloride dioxide treatment or dehydrothermal treatment are described.



Compounds Suitable for Treatment of Haemophilia

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to VWF compounds as well as compositions suitable for treatment of blood clotting diseases.



PROTEASE RESISTANT PEPTIDES

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides protease-resistant peptides, methods of making such peptides, as well as compositions comprising protease-resistant peptides and method of treatment utilizing such peptides. Incorporation of alpha-methyl-functionalized amino acids directly into the main chain during standard peptide synthesis via the methodologies described herein has been determined to produce protease-resistant peptides.



Melanocortin Receptor-Specific Peptides

Thu, 03 Nov 2016 08:00:00 EDT

Melanocortin receptor-specific cyclic peptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and z are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.



BETA-HAIRPIN PEPTIDOMIMETICS AS SELECTIVE ELASTASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

β-Hairpin peptidomimetics of the general formula cyclo(-Xaa1-Xaa2-Thr3-Xaa4-Ser5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-) and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa4, Xaa6, Xaa7, Xaa8, Xaa9, Xaa10, Xaa11, Xaa12 and Xaa13 being amino acid residues which are defined in the description and the claims, have elastase inhibitory properties, especially against human neutrophil elastase, and can be used for preventing infections or diseases related to such infections in healthy individuals or for slowing infections in infected patients. The compounds of the invention can further be used where cancer, or immunological diseases, or pulmonary diseases, or cardiovascular diseases, or neurodegenerative diseases, or inflammation, or diseases related to inflammation, are mediated or resulting from elastase activity. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.



METHOD FOR PROMOTING EXPRESSION OF CALRETICULIN, AND SYNTHETIC PEPTIDE FOR USE IN METHOD FOR PROMOTING EXPRESSION OF CALRETICULIN

Thu, 03 Nov 2016 08:00:00 EDT

A method for promoting expression of calreticulin in at least one kind of eukaryotic cell, and a synthetic peptide useful in this method are provided. In the method provided by the present invention, a culture of target cells is prepared, and a calreticulin expression-promoting peptide having calreticulin expression-promoting activity is supplied at least once to that culture.



COMPOSITIONS AND METHODS FOR INCREASING TELOMERASE ACTIVITY

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to methods and compositions for increasing telomerase activity in cells. Such compositions include pharmaceutical formulations. The methods and compositions are useful for treating diseases subject to treatment by an increase in telomerase activity in cells or tissue of a patient. They are also useful for enhancing replicative capacity of cells in culture, as in ex vivo cell therapy and for enhancing proliferation of stem and progenitor cells.



NOVEL 7-DEAZAPURINE NUCLEOSIDES FOR THERAPEUTIC USES

Thu, 03 Nov 2016 08:00:00 EDT

The invention provides compounds of formula I: wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.



URIDINE DIPHOSPHATE DERIVATIVES, COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISORDERS

Thu, 03 Nov 2016 08:00:00 EDT

This disclosure relates to uridine di phosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.



NOVEL FERROCENYL COMPOUNDS

Thu, 03 Nov 2016 08:00:00 EDT

A ferrocenyl compound having the general formula (I): (I) Het is a substituted or unsubstituted heterocyclic moiety. L1, L2 and L3 are each a linker independently selected from alkylene, alkyleneoxy, alkyleneoxyalkylene, alkylenecarbonyl, alkyleneoxycarbonyl, alkyleneamido, alkyleneoxyamido, alkenylene, alkenyleneoxy, alkenylenecarbonyl, alkenyleneamido, alkynylene, alkynyleneoxy, alkynylenecarbonyl and alkynyleneamido, all of which may be straight chain or branched, substituted or unsubstituted. R1 and R2 are each independently selected from H, substituted or unsubstituted alkyl carbonyl, substituted or unsubstituted aryl carbonyl, substituted or unsubstituted phosphate, substituted or unsubstituted phosphonate and substituted or unsubstituted phosphoramidate. M and n are each 0 or 1 and m+n≠0.1



COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF CANCERS

Thu, 03 Nov 2016 08:00:00 EDT

The present teachings relate to compounds and compositions for treatment of cancers. In some embodiments, the composition comprises a platinum (IV) complex having at least one polar moiety as a ligand.



UREA DERIVATIVES USEFUL AS KINASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

There are provided compounds of formula I, wherein R1, R1A, R1C to R1E, Ra, Rb, X1, E and G have meanings given in the description, which compounds have antiinflammatory activity (e.g., through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.



1H-PYRAZOLO[3,4-B]PYRIDINES AND THERAPEUTIC USES THEREOF

Thu, 03 Nov 2016 08:00:00 EDT

Provided herein are compounds according to Formulas (I) or (II) and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, osteoarthritis, idiopathic pulmonary fibrosis and neurological conditions/disorders/diseases.



Selective BACE1 Inhibitors

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof.



5-ARYL-1-IMINO-1-OXO-[1,2,4]THIADIAZINES

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides a compound of formula I′ having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.



Tetrahydro[1,8]naphthyridine Sulfonamide And Related Compounds for Use as Agonists of RORy and the Treatment of Disease

Thu, 03 Nov 2016 08:00:00 EDT

The invention provides tetrahydro[1,8]naphthyridine and related compounds, pharmaceutical compositions, methods of promoting RORγ activity, increasing the amount of IL-17 in a subject, and treating cancer using such tetrahydro[1,8]naphthyridine and related compounds.



FUSED BICYCLIC ISOXAZOLINES AS INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN

Thu, 03 Nov 2016 08:00:00 EDT

Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is (CH2) or O, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:



Compounds Inhibiting Eukaryotic Elongation Factor 2 Kinase Activity

Thu, 03 Nov 2016 08:00:00 EDT

Eukaryotic elongation factor 2 kinase inhibitors of the formula where R1, R2, R3a, R3b, R4a, R4b, R5a, R5b, R6a, R6b, R7 and x are as defined in the specification, pharmaceutical compositions and formulations including compounds of the foregoing formula, and methods of preventing, ameliorating or treating indications, conditions, disorders or syndromes associated with elongation factor 2 phosphorylation.



PHARMACOLOGICALLY ACTIVE COMPOUNDS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to compounds of formula I shown below: wherein Q is as defined herein. The compounds of formula I act as selective positive allosteric modulators of strychnine-sensitive alpha 1-glycine receptors. The present invention further relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of diseases or conditions in which strychnine-sensitive alpha 1-glycine receptor activity is implicated (such as, for example, chronic pain. The present invention also relates to processes for the preparation of these compounds and to pharmaceutical compositions comprising them.



ALCOHOL-, DIOL-, AND CARBOHYDRATE-SUBSTITUTED INDENOISOQUINOLINES AS TOPOISOMERASE I INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

The invention described herein pertains to substituted indenoisoquinoline compounds as described herein, wherein RA, RD, W, X and Y are defined herein, pharmaceutical compositions and formulations comprising the indenoisoquinoline compounds, their synthesis, and methods for their use in the treatment and/or prevention of cancer.



PIPERIDINYLOXY LACTONE OREXIN RECEPTOR ANTAGONISTS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention is directed to piperidinyloxy lactone compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the piperidinyloxy lactone compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.



IMIDAZOLE DERIVATIVE USED AS ANTIVIRAL AGENT AND USE THEROF IN PREPARATION OF MEDICAMENT

Thu, 03 Nov 2016 08:00:00 EDT

Disclosed are an antiviral compound and a use thereof in the preparation of a medicament for the treatment of virus infections. Specifically, the present invention relates an imidazole derivative for treating respiratory syncytial virus infection.



TETRAHYDRO-PYRIMIDOAZEPINES AS MODULATORS OF TRPV1

Thu, 03 Nov 2016 08:00:00 EDT

Certain tetrahydro-pyrimidoazepine compounds are described, which are useful as TRPV1 modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by TRPV1. Thus, the compounds may be administered to treat, e.g., pain, itch, cough, asthma, or inflammatory bowel disease.



SOLID FORMS OF 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL)PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO[2,3-b]PYRAZIN-2(1H)-ONE, COMPOSITIONS THEREOF AND METHODS OF THEIR USE

Thu, 03 Nov 2016 08:00:00 EDT

Provided herein are formulations, processes, solid forms and methods of use relating to 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one.



Imidazopyrazinones as PDE1 Inhibitors

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides imidazopyrazinones as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.



CRYSTALS (2) OF PYRAZINO[2,1-c][1,2,4]TRIAZINE COMPOUND

Thu, 03 Nov 2016 08:00:00 EDT

Provided are a crystal of a hydrate of compound 1, showing diffraction peaks at diffraction angles (2θ±0.2°) of 10.7°, 10.9°, 14.4°, 19.1° and 22.8°, in powder X-ray diffraction, a crystal of compound 1 or hydrate thereof, showing diffraction peaks at diffraction angles (2θ±0.2°) of 7.2°, 8.9°, 13.2°, 16.4° and 22.4°, in powder X-ray diffraction, a crystal of an anhydride of compound 1, showing diffraction peaks at diffraction angles (2θ±0.2°) of 10.3°, 14.2°, 14.6°, 16.1° and 22.1°, in powder X-ray diffraction, and a crystal of compound 1 or hydrate thereof, showing diffraction peaks at diffraction angles (2θ±0.2°) of 7.3°, 10.7°, 16.3°, 19.8° and 23.8°, in powder X-ray diffraction.



PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL COMPOUNDS

Thu, 03 Nov 2016 08:00:00 EDT

A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.



PYRIMIDOPYRIMIDINONES USEFUL AS WEE-1 KINASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.



BIARYL BRUTON'S TYROSINE KINASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.



2-METHYLSULPHANYL-6-NITRO-7-OXO-1, 2, 4-TRIAZOLO [5, 1-C] [1, 2, 4] TRIAZINIDE L-ARGININE DIHYDRATE ACTIVE TOWARD WEST NILE VIRUS

Thu, 03 Nov 2016 08:00:00 EDT

The claimed invention relates to the field of biologically active compounds and concerns 2-methylsulphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-arginine dihydrate, which exhibits an antiviral effect and is intended for the treatment and prophylaxis of human and animal viral diseases, primarily West Nile Virus, and can be used in the chemical and pharmaceutical industry, in scientific research laboratories and medical facilities, and also in veterinary science. The claimed invention is directed toward achieving the technical result of creating a novel effective drug of the azoloazine variety which exhibits antiviral activity toward a group of RNA-containing viruses, and reducing the dependence of the active compound on cell metabolism. This technical result is achieved in the creation of the novel drug 2-methylsulphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-arginine dihydrate, which exhibits an aniviral effect and has the formula (I). This technical result is achieved in that a method for producing 2-methylsylphanyl-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide L-arginine dihydrate includes mixing arginine, dissolved in water, and 2-methylthio-6-nitro-7-oxo-1,2,4-triazolo[5,1-c][1,2,4]triazinide sodium dihydrate, dissolved in a (1:1) water-ethanol mixture, whereupon the resultant mixture is boiled then cooled, and the precipitate is filtered off and dried.



FUSED PYRAZOLE DERIVATIVE

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides a cyclic aminomethyl pyrimidine derivative including a pharmaceutically acceptable salt thereof with high selectivity for dopamine D4 receptor, which is useful for treating a disease such as attention deficit hyperactivity disorder. Specifically, the present invention relates no a compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein n and m are independently 1 or 2; W1, W3, and W4 are independently single bond or optionally-substituted C1-4 alkylene group; W2 is optionally-substituted C1-4 alkylene group; R1 and R2 are independently hydrogen atom, etc.; R3 is hydrogen atom, halogen atom, etc.; X1 and X2 are independently single bond, oxygen atom, etc.; ring Q1 is optionally-substituted 5- to 10-membered heteroaryl group, etc.; ring Q2 is optionally-substituted 6-membered heteroaryl group, etc.



PYRIDONE-SULFONE MORPHINAN ANALOGS AS OPIOID RECEPTOR LIGANDS

Thu, 03 Nov 2016 08:00:00 EDT

The application is directed to Pyridone-sulfone morphinan analogs compounds of Formula I: or pharmaceutically acceptable salts and solvates thereof, wherein ==, R1, R2, R3, R4 and Z are as defined as set forth in the specification. The invention is also directed to use of the compounds of Formula I or the pharmaceutically acceptable salts and solvates thereof to treat disorders responsive to the odulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.



MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.



METHOD FOR TREATING PAIN SYNDROME AND OTHER DISORDERS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides the use of certain compounds to treat peripheral or central pain syndrome and other disorders associated with the T-type calcium ion channels.



PYRAZOLO[1,5-A]PYRIDINE DERIVATIVES AND METHODS OF THEIR USE

Thu, 03 Nov 2016 08:00:00 EDT

The invention is directed to pyrazolo[1,5-a]pyridine derivatives and their use as AXL and c-MET kinase inhibitors.



TRICYCLIC COMPOUNDS AS ANTICANCER AGENTS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention is directed to tricyclic compounds (I), pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.



P2X3 AND/OR P2X2/3 COMPOUNDS AND METHODS

Thu, 03 Nov 2016 08:00:00 EDT

The present application provides novel compounds and methods for preparing and using these compounds. In one embodiment, the compounds are of the structure of formula (I), wherein R1-R4 are defined herein. In a further embodiment, these compounds are useful in method for regulating one or both of the P2X3 or P2X2/3 receptors. In another embodiment, these compounds are useful for treating pain in patients by administering one or more of the compounds to a patient.



MALEIMIDE DERIVATIVES AS MODULATORS OF WNT PATHWAY

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein R1 represents optionally substituted alkyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkoxy); optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or -alkylaryl; R2 represents H; or alkyl; R3 represents H; or alkyl; U, V and W represent —(CH2)—; or U and V together represent —CH═CH— and W represents C═O; Y represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl); and Z represents aryl; heteroaryl; optionally substituted carbocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6alkoxy, C1-6haloalkyl, C1-6haloalkoxy and halo); or optionally substituted heterocyclyl (wherein optional substituents include one or more substituents each independently selected from C1-6alkyl, C1-6 alkoxy, —C(O)OC1-6alkyl, —C(O)C1-6alkyl and —C(O)NHC1-6alkyl).



IMIDAZO [1,2-a]PYRIDINE COMPOUNDS, SYNTHESIS THEREOF, AND METHODS OF USING SAME

Thu, 03 Nov 2016 08:00:00 EDT

Embodiments relate to the field of chemistry and biochemistry, and, more specifically, to imidazopyridine compounds, synthesis thereof, and methods of using same. Disclosed herein are various imidazo[1,2-a]pyhdine compounds and methods of using the novel compounds to treat or prevent tuberculosis in a subject or to inhibit fungal growth on plant species. Other embodiments include methods of synthesizing imidazo[1,2-a]pyridine compounds, such as the disclosed imidazo[1,2-a]pyridine compounds.



DIAZEPANE OREXIN RECEPTOR ANTAGONISTS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention is directed to diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the diazepane compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.



APOPTOSIS SIGNAL-REGULATING KINASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

The present application relates to compounds having the inhibitory activity to apoptosis signal-regulating kinase (ASK1), thus are thus useful in treating ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.



NOVEL GLUTAMINASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

The present disclosure provides compounds of formula (I) to (III) as glutaminase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders involving glutamine.



TRPV1 ANTAGONISTS INCLUDING DIHYDROXY SUBSTITUENT AND USES THEREOF

Thu, 03 Nov 2016 08:00:00 EDT

The disclosure relates to Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein Ar1, Ar2, L1, L2, X, R3, R22, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I), and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I).



OXIME-SUBSTITUTED AMIDE COMPOUND AND PEST CONTROL AGENT

Thu, 03 Nov 2016 08:00:00 EDT

To provide a novel pesticide, especially a fungicide and a nematocide. An oxime-substituted amide compound represented by the formula (I) or its salt, and a pesticide containing it: wherein G1 is a structure represented by G1-1 or the like, G2 is a structure represented by G2-2 or the like: W is an oxygen atom or the like, X1 is a halogen atom, methyl, trifluoromethyl or the like, each of X2, X3, X4 and X5 is independently a hydrogen atom, a halogen atom or the like, each of Y1 and Y3 is independently a halogen atom, cyano, methyl, trifluoromethyl, C2-C6 alkynyl or the like, each of Y2 and Y4 is independently a hydrogen atom, a halogen atom or the like, R1 is C1-C6 alkyl, C1-C4 haloalkyl, (C1-C4)alkyl substituted with R18, C3-C6 cycloalkyl, C3-C6 alkenyl or the like, each of R2 and R3 is independently a hydrogen atom, methyl or the like, R4 is a hydrogen atom or the like, R18 is C3-C6 cycloalkyl, phenyl, phenyl substituted with (Z)m or the like, Z is a halogen atom or the like, and m is an integer of 1, 2 or 3.



SMALL MOLECULE MODIFIERS OF THE HEC1-NEK2 INTERACTION IN G2/M

Thu, 03 Nov 2016 08:00:00 EDT

Certain embodiments of the present invention provide selected compounds having a molecular structure according to Formula 1: In Formula 1, Z is —CO—, —SO—, or —SO2—; Ar is phenyl, heteroaryl, or heterocycloalkyl; Het is heteroaryl; R is R″, X, or NR1R2; R′ is R3, or OR3; R″ is R4, or OR4; R1 and R2 are each independently H, alkyl, or acyl; R3 is H, heteroaryl, or alkyl; R4 is H, heteroaryl, or CnH2n+1 (n>2); and X is F, Br, I, CN, or NO2. In some embodiments, compounds having a molecular structure according to Formula 1 have the property of inhibiting a growth of a cell line selected from HeLa and MB468 with a sub-micromolar IC50.



NRF2 REGULATORS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.



NITROGEN-CONTAINING SIX-MEMBERED CYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

Thu, 03 Nov 2016 08:00:00 EDT

A compound represented by formula (I): wherein Z1 is C(R2) or N; Z3 is CH or N; Z2 is C(R3) or N; provided that Z1 is C(R2) and Z3 is CH when Z2 is N; Ring A is a substituted or unsubstituted aromatic carbocycle, or the like; R1 is substituted or unsubstituted alkyl, or the like; R2 is a hydrogen atom, halogen, or the like; R3 is a hydrogen atom, halogen, or the like; or a pharmaceutically acceptable salt thereof.



SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE

Thu, 03 Nov 2016 08:00:00 EDT

The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.



SUBSTITUTED AMINOPYRIMIDINE COMPOUNDS AND METHODS OF USE

Thu, 03 Nov 2016 08:00:00 EDT

The invention relates to the preparation and use of new aminopyrimidine derivatives as drug candidates in free form or in pharmaceutically acceptable salt form and formulations thereof for the modulation of a disorder or disease which is mediated by the activity of the PI3K enzymes. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of disorders or diseases, such as disorders of immunity and inflammation in which PI3K enzymes play a role in leukocyte function, and hyperproliferative disorders associated with PI3K activity, including but not restricted to leukemias and solid tumors, in mammals, especially humans.



A Novel Compound for the Treatment of Hepatitis C

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides (R)-5-(3-((2-(1,2,4-oxadiazol-3-yl)propan-2-yl)carbamoyl)phenyl)-6-(sec-butyl)-2-(4-fluorophenyl)-N-methylbenzofuran-3-carboxamide (formula I), including pharmaceutically acceptable salts, as well as compositions and methods of using the compound. The compound has activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.



1-HETEROARYL-INDOLINE-4-CARBOXAMIDES AS MODULATORS OF GPR52 USEFUL FOR THE TREATMENT OR PREVENTION OF DISORDERS RELATED THERETO

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g., posttraumatic stress disorder (PTSD)); a disruptive, impulse-control, or conduct disorder; a sleep-wake disorder; a substance-related disorder; an addictive disorder; a behavioral disorder; hypofrontality; an abnormality in the tuberoinfundibular, mesolimbic, mesocortical, or nigrostriatal pathway; decreased activity in the striatum; cortical dysfunction; neurocognitive dysfunction; and conditions related thereto



Quinazolin-THF-Amines as PDE1 Inhibitors

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides Quinazolin-THF-amines as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.



KINASE INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

There are provided compounds of formula I, wherein: Y represents NR2R3; one of R2 and R3 represents —[C2-4 alkylene-O]1-12—[C2-4 alkylene]-R2a and the other of R2 and R3 has a meaning given in the description; and R, R1, R2a, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.



NOVEL IMIDAZOLIDINE-2,4-DIONE DERIVATIVES

Thu, 03 Nov 2016 08:00:00 EDT

Imidazolidine-2,4-dione derivatives of formula (I): These compounds have anti-proliferative activity and are useful for treating pathological states and diseases linked to an abnormal cell proliferation, such as cancer.



INHIBITORS OF BRUTON'S TYROSINE KINASE

Thu, 03 Nov 2016 08:00:00 EDT

This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.



Novel benzimidazole derivatives as EP4 ligands

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to novel benzimidazole derivatives of the general formula (I), to processes for their preparation and to their use for preparing pharmaceutical compositions for the treatment of disorders and indications associated with the EP4 receptor.



SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS AS FACTOR XIA INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.



THERAPEUTICALLY ACTIVE COMPOSITIONS AND THEIR METHODS OF USE

Thu, 03 Nov 2016 08:00:00 EDT

Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.



NOVEL IMIDAZOLIDINE-2,4-DIONE DERIVATIVES

Thu, 03 Nov 2016 08:00:00 EDT

Imidazolidine-2,4-dione derivatives of formula (I): The compounds have anti-proliferative activity and are useful for treating pathological states and diseases linked to an abnormal cell proliferation such as cancer.



SUBSTITUTED PIPERIDINYL-TETRAHYDROQUINOLINES

Thu, 03 Nov 2016 08:00:00 EDT

The present application relates to novel substituted piperidinyltetrahydroquinolines, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of diabetic microangiopathies, diabetic ulcers on the extremities, in particular for promoting wound healing of diabetic foot ulcers, diabetic heart failure, diabetic coronary microvascular heart disorders, peripheral and cardial vascular disorders, thromboembolic disorders and ischaemias, peripheral circulatory disturbances, Raynaud's phenomenon, CREST syndrome, microcirculatory disturbances, intermittent claudication, and peripheral and autonomous neuropathies.



2-AMINO-3-ESTER-PYRIDYL OREXIN RECEPTOR ANTAGONISTS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention is directed to 2-amino-3-ester pyridyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2-amino-3-ester pyridyl compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.



THIOETHER-PIPERIDINYL OREXIN RECEPTOR ANTAGONISTS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention is directed to thioether-piperidinyl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the thioether-piperidinyl compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.



NOVEL PIPERIDINE CARBOXAMIDE COMPOUND, PREPARATION METHOD, AND USAGE THEREOF

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides a compound of a general formula I, a stereomeride, pharmaceutically acceptable salt or a solvate thereof, a preparation method thereof, and usages in preparing medicines for preventing and/or treating diseases or symptoms caused by drug-resistant tumors or drug-resistant bacteria and in preparing medicines for preventing and/or treating diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection. Preferably, the diseases or symptoms related to tumors, neurodegenerative diseases, allogeneic transplantation rejection, and infection are diseases or symptoms caused by a heat shock protein 70 (Hsp70). The compound in the present invention is used for overcoming a difficult problem of drug resistance of tumors, improves the effect of tumor treatment, and provides a new medical strategy for clinical tumor treatment.



Inhibitors of 17Beta-Hydroxysteroid Dehydrogenases Type 1 and Type 2

Thu, 03 Nov 2016 08:00:00 EDT

Provided herein are non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 and type 2 (17β-HSD1 and 17β-HSD2) inhibitors, their production and use, especially for the treatment and for prophylaxis of hormone-related diseases.



Sulfamate Derivative Compounds for Use in Treating or Alleviating Pain

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to sulfamate derivative compounds and a composition for treating and/or alleviating pain containing the sulfamate derivative compounds or a pharmaceutically acceptable salt thereof as an active ingredient. More specifically, the present invention relates to a pharmaceutical composition for treating or alleviating pain containing a sulfamate derivative compound and/or a pharmaceutically acceptable salt thereof as an active ingredient. Furthermore, the present invention relates to a method for treatment or alleviation of pain comprising administering a sulfamate derivative compound in a pharmaceutically effective amount to a subject in need of treatment or alleviation of pain; and a use of the sulfamate derivative compound or the pharmaceutically acceptable salt thereof in treating and/or alleviating pain, are provided.



TONABERSAT PRODRUGS

Thu, 03 Nov 2016 08:00:00 EDT

The invention relates to pharmaceutically active compounds having improved pharmacokinetic properties and being useful for the treatment or prevention of a range of conditions including migraine, epilepsy, non-epileptic seizures, brain injury (including stroke, intracranial haemorrhage and trauma induced) or cardiovascular diseases including myocardial infarction, coronary revascularization or angina. The compounds of the invention form a novel group of related prodrugs of formula (II), where Ar is a 3-chloro-4-fluorophenyl ring, a 3-chlorophenyl ring or a 4-fluorophenyl ring; and R is a hydrolysable group comprising an amino group or an acidic group.



NOVEL KINASE MODULATORS

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.



CRYSTALLINE FORM OF CABAZITAXEL AND PROCESS FOR PREPARING THE SAME

Thu, 03 Nov 2016 08:00:00 EDT

The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β, 10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same.



AMIDOPHENOXYPROPANOLAMINES

Thu, 03 Nov 2016 08:00:00 EDT

The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.



Novel Compound, Organic Cation Transporter 3 Detection Agent, And Organic Cation Transporter 3 Activity Inhibitor

Thu, 03 Nov 2016 08:00:00 EDT

[Problem] The present invention addresses the problem of providing a novel compound. The present invention also addresses the problem of providing an OCT3 detection agent or an OCT3 activity inhibitor, which comprises the novel compound. [Solution] A compound represented by formula (A), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. R1-R2-R3-R4 (A)



GAMMA-AMINOBUTYRIC ACID (GABA) ANALOGUES FOR THE TREATMENT OF PAIN AND OTHER DISORDERS

Thu, 03 Nov 2016 08:00:00 EDT

A compound of Formula (1) wherein R1 represents hydrogen, halo, a C1-C4 alkyl group, a C1-C4 alkylhalide group, a C1-C4 alkoxy-C2-C4 alkyl group, a C2-C4 alkenyl group, a C2-C4 alkynyl group or a C3-C7 cyclo alkyl group; R2 represents Formula (1)′ or Formula (1)″ a tautomer thereof; and R3 represents hydrogen, a C1-C4 alkyl group, a C1-C4 alkoxy-C2-C4 alkyl group or a C7 cyclo alkyl group; or a pharmaceutically acceptable salt or solvate thereof. Processes to prepare said compounds and novel intermediates are also claimed. Such compound finds utility in treating neuropathic pain and disorders of the central nervous system.



3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL) PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

A compound of formula (I) or a salt thereof are provided: wherein R1, X and R3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.



TRIAZOLES AS KV3 INHIBITORS

Thu, 03 Nov 2016 08:00:00 EDT

Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.



METHODS TO TREAT LYMPHOPLASMACYTIC LYMPHOMA

Thu, 03 Nov 2016 08:00:00 EDT

The present invention provides compounds of any one of Formulae (A), (I-11), (II), and (V) (e.g., compounds of Formula (A-1)-(A-18)), and methods for treating Waldenström's macroglobulinemia (WM) and other B cell neoplasm in a subject using the compounds. The methods comprise administering to a subject in need thereof an effective amount of the compounds. Also provided are methods to treat B cell neoplasms using the compounds in combination with inhibitors of Bruton's tyrosine kinase (BTK), interleukin-1 receptor-associated kinase 1 (IRAK1), interleukin-1 receptor-associated kinase 4 (IRAK4), bone marrow on X chromosome kinase (BMX), phosphoinositide 3-kinase (PI3K), transforming growth factor b-activated kinase-1 (TAK1), and/or a Src family kinase.