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Buccal Cell Diagnosis of Arrhythmogenic Cardiomyopathy (ACM)

Thu, 06 Apr 2017 08:00:00 EDT

Described herein are, inter alia, methods for diagnosing and treating arrhythmogenic cardiomyopathy (ACM) by detecting cardiac intercalated disk proteins, e.g., desmosomal proteins, mechanical and gap junction proteins, in buccal cells. Exemplary desmosomal and gap junction proteins that can be evaluated in the methods described herein include plakoglobin, plakophilin 1, desmoplakin, and Cx43. The methods can also include selecting and/or administering a treatment for ACM to the subject.



METHODS FOR TREATING INFLAMMATORY AND OTHER DISEASES AND THE USE OF BIOMARKERS AS PREDICTORS OF CLINICAL SENSITIVITY TO TREATMENT WITH APREMILAST

Thu, 06 Apr 2017 08:00:00 EDT

Provided herein are methods for predicting the clinical sensitivity of an inflammatory disease (e.g., ankylosing spondylitis) and a subject's response to treatment with apremilast using the level of a biomarker (e.g., MCP1). Also provided herein are methods for treating an inflammatory disease.



EARLY DETECTION OF PREECLAMPSIA

Thu, 06 Apr 2017 08:00:00 EDT

The invention provides non-invasive assays to reliably identify women who have or are predisposed to developing preeclampsia (PE). The method comprises measuring a level of annexin A2 (ANXA2) in a test sample obtained of a subject; and identifying the subject as having preeclampsia or at an increased risk of developing preeclampsia when the level of ANXA2 in the test sample is decreased in relation to a control sample. Methods to treat subject identified as having PE or at an increased risk of developing preeclampsia are also provided.



SCREEN FOR INHIBITORS OF FILOVIRUS AND USES THEREFOR

Thu, 06 Apr 2017 08:00:00 EDT

The invention provides methods to identify agents useful to prevent, inhibit or treat viral infections, e.g., filovirus infections, as well as compositions having one or more agents to prevent, inhibit or treat viral infection.



DETECTION OF CHROMOSOMAL ABNORMALITIES ASSOCIATED WITH PROGNOSIS OF NON SMALL CELL LUNG CANCER

Thu, 06 Apr 2017 08:00:00 EDT

The methods and compositions described herein address the need for a diagnostic method that can be provided to patients with early stage lung cancer, especially non-small cell lung cancer (NSCLC), to determine whether the patient is at increased risk of poor disease outcome. The methods and compositions thus allow for more informed treatment decisions for the early stage lung cancer patient.



METHODS FOR PREDICTING RESPONSE TO HDACI/DNMTI COMBINATION IN MULTIPLE MYELOMA

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to a method of testing whether a patient suffering from multiple myeloma will respond or not to a combination treatment consisting of at least one histone deacetylase inhibitor (HDACi) with at least one DNA methyltransferase inhibitors (DNMTi) comprising: i) determining the expression level (ELi) of several genes G1-Gn selected from table A in a biological sample obtained from said patient ii) comparing the expression level (ELi) determined at step i) with a predetermined reference level (ELRi) iii) calculating the HADMS score trough the following formula (I) wherein βi represent the regression β coefficient reference value for the gene Gi and Ci=1 if the expression of the gene Gi (ELi) is higher than the predetermined reference level (ELRi) or Ci=−1 if the expression of the gene (ELi) is lower than or equal to the predetermined reference level (ELRi) iv) comparing the score HADMS determined at step iii) with a predetermined reference value HADMSR v) and concluding that the patient will respond to the combination treatment when the HADMS score is higher than the predetermined reference value HADMSR or concluding that the patient will not respond to the combination treatment when the HADMS score is lower than the predetermined reference value HADMSR. HADMS=∑i=1nβi×Ci(I)



DIAGNOSTIC METHOD

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to a method of diagnosing a paroxysmal pain disorder, such as trigeminal neuralgia, in a human subject and also provides a method of identifying patients most likely to respond to therapy and to kits for use in said methods.



AAV VECTORS FOR VASCULAR GENE THERAPY IN CORONARY HEART DISEASE AND PERIPHERAL ISCHAEMIA

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to the provision of a gene therapy for coronary heart disease and peripheral ischemia in mammals. One embodiment is an adeno-associated viral vector (AAV vector) comprising a first gene encoding a myocardin-related transcription factor A (MRTF-A). The invention further also relates to a pharmaceutical composition comprising an AAV vector of the invention and a pharmaceutically acceptable carrier. Methods for preparing the vector of the invention are also disclosed.



MICRORNA INDUCTION OF CARDIAC REGENERATION

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to compostions and methods for promoting cellular proliferation and de-differentiation of cells into stem cells to foster tissue regeneration. Specifically, the invention relates to transiently administering a microRNA (miR) or its mimic for promoting cardiomyocyte proliferation and cardiac regeneration.



DNA APTAMERS SPECIFIC TO CD200R1 AND THEIR THERAPEUTIC USES

Thu, 06 Apr 2017 08:00:00 EDT

Disclosed are short DNA aptamers that selectively recognize CD200R1, a protein expressed on the surface of myeloid and lymphoid cells that delivers immune inhibitory signals to modulate inflammation when engaged with its ligand, CD200. Also disclosed is the use of said aptamers as therapeutic agents, for the purpose of decreasing inflammatory response; treatment of spinal cord injury; treatment of an immune related disease such as arthritis, allergy, infection; as a course of treatment during or after transplantation; or for treatment of an autoimmune disorders such as systemic lupus erythematosus, Parkinson's Disease, or multiple sclerosis.



DIAGNOSIS AND TREATMENT OF FRIEDREICH'S ATAXIA

Thu, 06 Apr 2017 08:00:00 EDT

The present invention is directed to oligonucleotides based on peptide nucleic acid oligonucleotide or an equivalent oligonucleotide analogue, such as morpholino or a locked nucleic acid sequences and the use of such oligonucleotides for the dissociation of higher order structures, including triplex-helix DNA structures, in repeated sequences of DNA in Friedreich's ataxia. The dissociation of such structures may be used in the diagnosis and/or treatment of Friedreich's ataxia. Consequently, the present invention is also directed to a method for diagnosing Friedreich's ataxia and the use of peptide nucleic acid oligonucleotide or an equivalent oligonucleotide analogue, such as morpholino or a locked nucleic acid sequences in the treatment of Friedreich's ataxia. Preferably, the oligonucleotides comprise a sequence selected from the group consisting of (GAA)n, (CTT)n, (JTT)n or a mixed (JTT/CTT)n sequence.



METHOD OF THERAPY AND DIAGNOSIS OF ENDOTHELIAL DYSFUNCTION

Thu, 06 Apr 2017 08:00:00 EDT

The invention discloses a method of therapy of endothelial dysfunction, by administering microRNA let-7g to a subject in need, wherein the microRNA let-7g inhibits SMAD2 transcription factor from activation and translocation into nucleus, thereby decreasing monocyte cell adhesion, inflammation and thrombosis and increasing angiogenesis.



Compositions and Methods for Inhibiting Gene Expression of LPA

Thu, 06 Apr 2017 08:00:00 EDT

RNA interference (RNAi) agents and RNAi agent conjugates for inhibiting the expression of the LPA (apo(a)) gene are described. Pharmaceutical compositions comprising one or more LPA RNAi agents optionally with one or more additional therapeutics are also described. Delivery of the described LPA RNAi agents to liver cells in vivo provides for inhibition of LPA gene expression and treatment of cardiovascular and cardiovascular-related diseases.



SPINAL MUSCULAR ATROPHY (SMA) TREATMENT VIA TARGETING OF SMN2 SPLICE SITE INHIBITORY SEQUENCES

Thu, 06 Apr 2017 08:00:00 EDT

The present invention is directed to methods and compositions capable of blocking the inhibitory effect of a newly-identified intronic inhibitory sequence element, named ISS-N1 (for “intronic splicing silencer”), located in the SMN2 gene. The compositions and methods of the instant invention include oligonucleotide reagents (e.g., oligoribonucleotides) that effectively target the SMN2 ISS-N1 site in the SMN2 pre-mRNA, thereby modulating the splicing of SMN2 pre-mRNA to include exon 7 in the processed transcript. The ISS-N1 blocking agents of the invention cause elevated expression of SMN protein, thus compensating for the loss of SMN protein expression commonly observed in subjects with spinal muscular atrophy (SMA).



siRNA Therapy for Transthyretin (TTR) Related Ocular Amyloidosis

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to a method of treating ocular amyloidosis by reducing TTR expression in a subject by administering a double-stranded ribonucleic acid (dsRNA) that targets a TTR gene to the retinal pigment epithelium of the subject.



ADMINISTERING ANTISENSE OLIGONUCLEOTIDES COMPLEMENTARY TO HUMAN APOLIPOPROTEIN B

Thu, 06 Apr 2017 08:00:00 EDT

Methods for long-term lowering of lipid levels in human subjects and for the treatment of conditions associated with elevated LDL-cholesterol and elevated ApoB are provided.



MULTIVALENT CATION FORMULATIONS OF PARTIALLY DESULFATED HEPARINS

Thu, 06 Apr 2017 08:00:00 EDT

Multivalent cation compositions of partially desulfated heparins are presented. Multivalent cation compositions of the disclosure can be formulated at high concentrations. The compositions, processes for making the compositions, unit dosage forms, kits, and methods of treatment are also disclosed.



DIBLOCK COPOLYMERS AND POLYNUCLEOTIDE COMPLEXES THEREOF FOR DELIVERY INTO CELLS

Thu, 06 Apr 2017 08:00:00 EDT

Described herein are copolymers, and methods of making and utilizing such copolymers. Such copolymers have at least two blocks: a first block that has at least one unit that is hydrophilic at physiologic pH, and a second block that has hydrophobic groups. This second block further has at least one unit with a group that is anionic at about physiologic pH. The described copolymers are disruptive of a cellular membrane, including an extracellular membrane, an intracellular membrane, a vesicle, an organelle, an endosome, a liposome, or a red blood cell. Preferably, in certain instances, the copolymer disrupts the membrane and enters the intracellular environment. In specific examples, the copolymer is endosomolytic.



Bi-Specific Therapeutic Proteins for Tissue Repair

Thu, 06 Apr 2017 08:00:00 EDT

Bi-specific fusion proteins with therapeutic uses are provided, as well as pharmaceutical compositions comprising such fusion proteins, and methods for using such fusion proteins to repair or regenerate damaged or diseased tissue.



FIBROBLAST GROWTH FACTOR MUTANTS HAVING IMPROVED FUNCTIONAL HALF-LIFE AND METHODS OF THEIR USE

Thu, 06 Apr 2017 08:00:00 EDT

Mutant fibroblast growth factor (FGF) proteins having a polypeptide sequence with a high sequence identity to proteins encoded by members of the Fgf-1 subfamily of genes from a mammalian species, such as human, and with a specific amino acid substitution of an alanine at a position corresponding to amino acid position 66 of human FGF-1 with a cysteine and/or a specific amino acid substitution of a phenylalanine at a position corresponding to amino acid position 132 of human FGF-1 with a tryptophan (based on the 140 amino acid numbering scheme of human FGF-1) are provided. Other amino acid mutations or substitutions may be combined. Polynucleotide sequences encoding the mutant FGF proteins and host cells containing such polynucleotide sequences are provided. Methods of administering a mutant FGF protein to an individual to treat an ischemic condition or disease or a wound or tissue injury are also provided.



FIBROBLAST GROWTH FACTOR MUTANTS HAVING IMPROVED FUNCTIONAL HALF-LIFE AND METHODS OF THEIR USE

Thu, 06 Apr 2017 08:00:00 EDT

Mutant fibroblast growth factor (FGF) proteins having a polypeptide sequence with a high sequence identity to proteins encoded by members of the Fgf-1 subfamily of genes from a mammalian species, such as human, and with a specific amino acid substitution of an alanine at a position corresponding to amino acid position 66 of human FGF-1 with a cysteine and/or a specific amino acid substitution of a phenylalanine at a position corresponding to amino acid position 132 of human FGF-1 with a tryptophan (based on the 140 amino acid numbering scheme of human FGF-1) are provided. Other amino acid mutations or substitutions may be combined. Polynucleotide sequences encoding the mutant FGF proteins and host cells containing such polynucleotide sequences are provided. Methods of administering a mutant FGF protein to an individual to treat an ischemic condition or disease or a wound or tissue injury are also provided.



CHIMERIC FGF21 PROTEINS WITH ENHANCED BINDING AFFINITY FOR BETA-KLOTHO FOR THE TREATMENT OF TYPE II DIABETES, OBESITY, AND RELATED METABOLIC DISORDERS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to chimeric proteins that include an N-terminus coupled to a C-terminus, where the N-terminus includes an N-terminal portion of fibroblast growth factor 21 (“FGF21”) and the C-terminus includes a C-terminal portion of fibroblast growth factor 19 (“FGF19”). The present invention also relates to pharmaceutical compositions including chimeric proteins according to the present invention, as well as methods for treating a subject suffering from diabetes, obesity, or metabolic syndrome, methods of treating a subject in need of increased FGF21-βKlotho-FGF receptor complex formation, methods of causing increased FGF21 receptor agonist-βKlotho-FGF receptor complex formation, and methods of screening for compounds with enhanced binding affinity for the βKlotho-FGF receptor complex involving the use of chimeric proteins of the present invention.



HTT REPRESSORS AND USES THEREOF

Thu, 06 Apr 2017 08:00:00 EDT

Disclosed herein are Htt repressors and methods and compositions for use of these Htt repressors.



ANTI-INFLAMMATORY COMPOUNDS AND METHODS OF USE

Thu, 06 Apr 2017 08:00:00 EDT

Disclosed herein are methods of treating or inhibiting inflammation in a subject by administering an anti-inflammatory protein to the subject. In some embodiments, the protein has at least 80% sequence identity to the amino acid sequence set forth as SEQ ID NO: 1 or fragments thereof. Also disclosed are methods of identifying anti-inflammatory compounds by determining the effect of test compounds on inflammation in zebrafish gut. In some embodiments, germ-free zebrafish or zebrafish inoculated with a single defined bacterial strain are contacted with one or more test compounds and a marker of inflammation in the gut is measured and compared to a control. Recombinant vectors including a nucleic acid encoding the anti-inflammatory protein (such as a nucleic acid encoding a protein with at least 80% sequence identity to SEQ ID NO: 1 or fragments thereof) operably linked to a heterologous promoter are also disclosed.



CYCLOHEPTAPEPTIDE AGENTS FOR TREATMENT OF CANCER AND OBESITY DISEASES

Thu, 06 Apr 2017 08:00:00 EDT

New anticancer and anti-obesity agents based on cyclic peptide compounds are isolated from the stem barks of Maytenus variabilis (Loes.) C. Y. Cheng (Celastraceae). The invention also includes its preparation and application method for treating cancer and obesity diseases.



TEMPLATE-FIXED PEPTIDOMIMETICS

Thu, 06 Apr 2017 08:00:00 EDT

The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity



Novel Tumor-Targeting Compounds

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to a novel compounds targeting human cancer cells, a method for synthesis of such compounds, and use of such compounds in treating cancer.



INHIBITION OF GLIADIN PEPTIDES

Thu, 06 Apr 2017 08:00:00 EDT

Novel compounds and methods for the inhibition of biological barrier permeability and for the inhibition of peptide translocation across biological barriers are identified. Assays for determining modulators of biological barrier permeability and for peptide translocation across biological barriers are provided. Methods for treating diseases relating to aberrant biological barrier permeability and peptide translocation across biological barriers are provided. Such diseases include celiac disease, necrotizing enterocolitis, diabetes, cancer, inflammatory bowel diseases, asthma, COPD, excessive or undesirable immune response, gluten sensitivity, gluten allergy, food allergy, rheumatoid arthritis, multiple sclerosis, immune-mediated or type 1 diabetes mellitus, systemic lupus erythematosus, psoriasis, scleroderma and autoimmune thyroid diseases.



Compositions and Methods Relating to Ionic Salts of Peptides

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to compounds of Formula I, compositions containing same, and methods of use.



Extended Triterpene Derivatives

Thu, 06 Apr 2017 08:00:00 EDT

The present invention concerns novel pharmaceutically active triterpene derivatives, pharmaceutical compositions containing the same, their use as medicaments, and the use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are derivatives of betulinic acid having substitutions at one or more of the C-3, C2-8 and C-19 positions as further described herein. The novel compounds are useful as antiretroviral agents. In particular, the novel compounds are useful for the treatment of Human Immunodeficiency Virus (HIV).



Crystalline Forms of Fosnetupitant

Thu, 06 Apr 2017 08:00:00 EDT

The present invention provides crystalline forms of the chloride monohydrochloride salt of fosnetupitant, methods of making the crystalline forms, and pharmaceutical dosage forms that make use of the crystalline forms.



PHOSPHONATES WITH REDUCED TOXICITY FOR TREATMENT OF VIRAL INFECTIONS

Thu, 06 Apr 2017 08:00:00 EDT

There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.



NOVEL ACTIVATORS OF GLUCOKINASE

Thu, 06 Apr 2017 08:00:00 EDT

The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.



MUSCARINIC RECEPTOR AGONISTS

Thu, 06 Apr 2017 08:00:00 EDT

This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.



COMPOUNDS FOR TREATMENT OF FLUOROQUINOLONE-RESISTANT BACTERIA

Thu, 06 Apr 2017 08:00:00 EDT

Compounds that specifically kill fluoroquinolone (FQ) resistant bacteria have been developed and are described herein. The FQs are the most commonly prescribed antibiotics to adults in the U.S. and thus are extremely important drugs. However, bacterial resistant to these drugs is now ubiquitous in some of the most common and deadly Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Indeed, FQs are no longer indicated for treatment of MRSA and VRE infections because of such resistance. The compounds have specific and potent activity versus MRSA and VRE.



SEPIAPTERIN REDUCTASE INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

Inhibitors of sepiapterin reductase and uses of sepiapterin reductase inhibitors in analgesia, treatment of acute and chronic pain, anti-inflammation, and immune cell regulation are disclosed.



DERIVATIZED CORROLES AND METALLOCORROLES AND THEIR USE AS IMAGING AND THERAPEUTIC AGENTS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention is directed to derivatized corroles, methods of making and using the same as imaging and therapeutic agents. In certain embodiments, the corroles are compounds having a Structure (I-H) and (I-M): where R1, R2, R3, and R4 are independently —F or —N(H)—(CH2)m—Y, provided that at least one of R1, R2, R3, and R4 is —N(H)—(CH2)m—Y, and m and Y are described herein.



HELQUATS WITH HETEROAROMATIC SUBSTITUENTS, PREPARATION THEREOF, AND USE THEREOF AS G-QUADRUPLEX STABILIZERS

Thu, 06 Apr 2017 08:00:00 EDT

Helquat derivatives of general formula I, in which substituents R1 and R2 are independently selected from a group comprising H and C1 to C4 alkyl, up to three of S1,2, S1′,2′, S3,4 and S3′,4′ are present, each of S1,2, S1′,2′, S3,4 and S3′,4′ independently represents a linker consisting of a bivalent hydrocarbon chain having 3-6 carbon atoms, preferably hydrocarbon chain having 4 carbon atoms, and one to four atoms selected from the carbon atoms with the descriptor 2, 4, 2′, and 4′ are substituted with a substituent R3 of general formula II, wherein R4 is substituted or unsubstituted heteroaryl, T1 and T2 are independent linkers that bridge atoms N5 with C8 and N5′ with C8′, wherein T1 and T2 independently represent a bivalent hydrocarbon chain having 2-5 carbon atoms, preferably 2 or 3 carbon atoms; and anions (X1)− and (X2)− independently represent anions of pharmaceutically acceptable salts.



(5,6-DIHYDRO)PYRIMIDO[4,5-E]INDOLIZINES

Thu, 06 Apr 2017 08:00:00 EDT

A compound of Formula I: wherein, R1 and R2 independently are selected from the group consisting of optionally substituted (6-10C)aryl and (1-5C)heteroaryl groups. The compounds can be used in pharmaceutical compositions, in particular in the treatment of cancer.



7-BENZYL-4-(2-METHYLBENZYL)-2,4,6,7,8,9-HEXAHYDROIMIDAZO [1,2-A]PYRIDO[3,4-E]PYRIMIDIN-5(1H)-ONE, ANALOGS THEREOF, AND SALTS THEREOF AND METHODS FOR THEIR USE IN THERAPY

Thu, 06 Apr 2017 08:00:00 EDT

This disclosure relates to methods of treatment using compound (1) or analogs thereof, and pharmaceutically acceptable salts thereof. Also disclosed are compounds of formula (10): as defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the same. Methods of treatment, such as for cancer, are provided that comprise administering the compounds and their salts to a subject in need of such treatment.



COMPOSITIONS AND METHODS FOR INHIBITING BETA-LACTAMASE

Thu, 06 Apr 2017 08:00:00 EDT

Substituted dihydroisoxazole derivatives useful as inhibitors of β-lactamases are provided. The invention further provides medical uses of substituted dihydroisoxazole derivatives, for example, as antibacterial agents.



MACROCYCLES WITH AROMATIC P2' GROUPS AS FACTOR XIA INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.



Novel Cyclopropabenzofuranyl Pyridopyrazinediones

Thu, 06 Apr 2017 08:00:00 EDT

Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I wherein X, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6, R7, R10, R11, and y are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.



FLUORINATED 3-(2-OXO-3-(3-ARYLPROPYL)IMIDAZOLIDIN-1-YL)-3-ARYLPROPANOIC ACID DERIVATIVES

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.



SUBSTITUTED PYRAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.



APOPTOSIS-INDUCING AGENTS FOR THE TREATMENT OF CANCER AND IMMUNE AND AUTOIMMUNE DISEASES

Thu, 06 Apr 2017 08:00:00 EDT

Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.



ANTAGONISTS ACTING AT MULTIPLE PROSTAGLANDIN RECEPTORS FOR THE TREATMENT OF INFLAMMATION

Thu, 06 Apr 2017 08:00:00 EDT

Compounds, processes for their preparation, pharmaceutical compositions containing such compounds and their use in treating therapeutic conditions, in particular conditions mediated by the action of ligands on the FP, DP, EP1, EP4, IP, DP1, FP and TP prostaglandin (PG) receptors thereby providing a general anti-inflammatory response.



HETEROCYCLIC COMPOUND

Thu, 06 Apr 2017 08:00:00 EDT

Provided is a compound having a superior PKC inhibitory action, and useful as a prophylactic or therapeutic agent for immune diseases, inflammatory diseases and the like, or a salt thereof. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a superior PKC inhibitory action, and is useful as a prophylactic or therapeutic agent for immune diseases, inflammatory diseases and the like.



Carboxamide Derivatives and Use Thereof

Thu, 06 Apr 2017 08:00:00 EDT

The present disclosure provides substituted pyridyl-, pyrimidinyl-, pyrazinyl-, pyridazinyl-, and triazinyl-based carboxamides of Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein Z, HET, R10, and E are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I-A to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.



OPTICALLY ACTIVE PDE10 INHIBITOR

Thu, 06 Apr 2017 08:00:00 EDT

The present invention is directed to a pure enantiomer of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, in particular, (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone. The present invention is also directed a crystal structure of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a pharmaceutical composition of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a method of inhibiting PDE10 with (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, and a process and particular individual intermediates used in the production of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone.



HETEROCYCLE-SUBSTITUTED PYRIDYL BENZOTHIOPHENES AS KINASE INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.



COMPOUNDS USEFUL AS MODULATORS OF TRPM8

Thu, 06 Apr 2017 08:00:00 EDT

The present disclosure relates to compounds which are useful as cooling sensation compounds.



Multicyclic Compounds And Methods Of Using Same

Thu, 06 Apr 2017 08:00:00 EDT

The invention generally relates to compounds represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders (e.g., PAK-mediated, for example, PAK4-mediated, diseases and disorders).



PYRAZOLE-SUBSTITUTED ARYLAMIDES AS P2X3 AND P2X2/3 ANTAGONISTS

Thu, 06 Apr 2017 08:00:00 EDT

Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.



BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.



PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS HDAC6 SELECTIVE INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.



HETEROCYCLIC COMPOUNDS USEFUL AS PIM KINASE INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

The present application is concerned with heterocyclic compounds that inhibit the activity of Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancers and other diseases.



Dual Inhibitor Compounds for Use in the Treatment of Neurodegenerative Disorders and Alzheimer's Disease

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to Compounds of Formula (I) and pharmaceutical compositions containing the same. It further relates to their use in the prevention or treatment of central nervous system diseases or disorders, in particular, cognitive, neurodegenerative or neuronal diseases or disorders.



NOVEL COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) inhibitory activity, isomers thereof, or pharmaceutically acceptable salts thereof, the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions comprising the same, a method of treating disease using the composition, and methods for preparing the novel compounds. The novel compounds according to the present invention have histone deacetylase 6 (HDAC6) inhibitory activity, and are effective for the prevention or treatment of HDAC6-associated diseases, including cancer, inflammatory diseases, autoimmune diseases, neurological diseases and neurodegenerative disorders.



DIAMINOPYRIMIDINES AS P2X3 AND P2X2/3 ANTAGONISTS

Thu, 06 Apr 2017 08:00:00 EDT

Compounds and methods for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I): or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein.



PYRIMIDINE HYDROXY AMIDE COMPOUNDS AS PROTEIN DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to novel pyrimidine hydroxy amide compounds, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.



IMIDAZOLE DERIVATIVES AS FORMYL PEPTIDE RECEPTOR MODULATORS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor.



ALKYNYL INDAZOLE DERIVATIVE AND USE THEREOF

Thu, 06 Apr 2017 08:00:00 EDT

The main object of the present invention is to provide a novel compound which has a VEGF receptor tyrosine kinase inhibitory activity and is useful as an active ingredient for the treatment of diseases accompanying angiogenesis or edema, for example, age-related macular degeneration or the like. The present invention includes, for example, an alkynyl indazole derivative represented by the following general formula (I), a pharmaceutical acceptable salt thereof, and a medicine containing thereof.



PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS

Thu, 06 Apr 2017 08:00:00 EDT

The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.



NON-HYGROSCOPIC SALTS OF 5-HT2C AGONISTS

Thu, 06 Apr 2017 08:00:00 EDT

Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management.



AROMATIC HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF

Thu, 06 Apr 2017 08:00:00 EDT

Provided herein are aromatic heterocyclic derivatives or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof used for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and use of such compounds or pharmaceutical compositions thereof for managing or treating 5-HT6 receptor-mediated diseases, especially in the manufacture of a medicament for managing or treating Alzheimer's disease.



NOVEL LACTAMS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to novel lactams of formulae (I) and (II). The present invention further relates to the use of these compounds in the treatment of microbial infections and microbial contamination of surfaces, particularly infections and surface contaminations characterised by biofilm formation. Further provided are compounds of formula (I) and (II) substituted with acrylate or methacrylate groups and their attachment to surfaces or polymers to inhibit microbial contamination.



Compositions And Methods Of Use Of Phorbol Esters For Treatment of Stroke

Thu, 06 Apr 2017 08:00:00 EDT

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment and prevention of stroke and the sequelae of stroke. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools to treat or prevent stroke and the long term effects of stroke in mammalian subjects.



TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF

Thu, 06 Apr 2017 08:00:00 EDT

Nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety, such as a somatostatin receptor binding moiety, via a linker have been designed. Such nanoparticles and microparticles can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.



GROWTH HORMONE POLYPEPTIDES AND METHODS OF MAKING AND USING SAME

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to compositions comprising growth hormone linked to extended recombinant polypeptide (XTEN), isolated nucleic acids encoding the compositions and vectors and host cells containing the same, and methods of making and using such compositions in treatment of growth hormone-related diseases, disorders, and conditions.



LOW-BURST POLYMERS AND METHODS TO PRODUCE POLYMERS

Thu, 06 Apr 2017 08:00:00 EDT

A PLG copolymer material, termed a PLG(p) copolymer material, adapted for use in a controlled release formulation for a bioactive material is provided, wherein the formulation exhibits a reduced “initial burst” effect when introduced into the tissue of a patient in need thereof. A method of preparation of the PLG copolymer material is also provided, as are methods of use.



ENGINEERED LIGHT-ACTIVATED ANION CHANNEL PROTEINS AND METHODS OF USE THEREOF

Thu, 06 Apr 2017 08:00:00 EDT

Aspects of the disclosure include compositions, devices, systems and methods for optogenetic modulation of action potentials in target cells. The subject devices include light-generating devices, control devices, and delivery devices for delivering light-responsive polypeptides, or nucleic acids encoding same, to target cells. The subject compositions and systems include light-activated polypeptides, nucleic acids comprising nucleotide sequences encoding these polypeptides, as well as expression systems that facilitate expression of these polypeptides in target cells. Also provided are methods of using the subject devices and systems to optogenetically manipulate action potentials in target cells, e.g., to treat a neurological or psychiatric condition in a human or animal subject.



SYSTEMIC GENE REPLACEMENT THERAPY FOR TREATMENT OF X-LINKED MYOTUBULAR MYOPATHY (XLMTM)

Thu, 06 Apr 2017 08:00:00 EDT

The present invention provides compositions and methods for treating a myopathy. In certain embodiments, the invention provides compositions and methods for treating, improving muscle function, and prolonging survival in a subject with X-linked myotubular myopathy (XLMTM). The present invention provides a method comprising systemic administration of a composition that induces the increased expression of myotubularin in the muscle of a subject. The invention provides sustained regional and global increases in muscle function.



USE OF LEPTIN FOR TREATING HUMAN LIPOATROPHY AND METHOD FOR DETERMINING PREDISPOSITION TO SAID TREATMENT

Thu, 06 Apr 2017 08:00:00 EDT

Leptin, leptin analogs, and leptin derivatives are used to treat patients with lipoatrophy. Leptin is effective against conditions of lipoatrophy for both genetic and acquired forms of the disease. A therapeutically effective amount of leptin can be administered in a variety of ways, including subcutaneously and using gene therapy methods. Methods of the present invention contemplate administration of leptin, leptin analogs, and leptin derivatives to patients having a leptin level of approximately 4 ng/ml or less before treatment.



FGF-9 Variants and Methods of Use Thereof

Thu, 06 Apr 2017 08:00:00 EDT

A method of treating an individual (i) having abnormal bone; or (ii) afflicted with a disease or disorder related to normal or abnormal FGF receptors or a skeletal disorder; or (iii) having dysplasic bone. The method includes administering to the individual a pharmaceutical composition comprising a therapeutically effective amount of a fibroblast growth factor 9 (FGF-9) variant comprising at least one amino acid substitution in the beta 8-beta 9 loop, wherein said FGF-9 variant incorporates one of the amino acid sequences set forth in SEQ ID NO: 11, 13, 14, 15, 16 or 17.



FIBROBLAST GROWTH FACTOR MUTANTS HAVING IMPROVED FUNCTIONAL HALF-LIFE AND METHODS OF THEIR USE

Thu, 06 Apr 2017 08:00:00 EDT

Mutant fibroblast growth factor (FGF) proteins having a polypeptide sequence with a high sequence identity to proteins encoded by members of the Fgf-1 subfamily of genes from a mammalian species, such as human, and with a specific amino acid substitution of an alanine at a position corresponding to amino acid position 66 of human FGF-1 with a cysteine and/or a specific amino acid substitution of a phenylalanine at a position corresponding to amino acid position 132 of human FGF-1 with a tryptophan (based on the 140 amino acid numbering scheme of human FGF-1) are provided. Other amino acid mutations or substitutions may be combined. Polynucleotide sequences encoding the mutant FGF proteins and host cells containing such polynucleotide sequences are provided. Methods of administering a mutant FGF protein to an individual to treat an ischemic condition or disease or a wound or tissue injury are also provided.



Treatment of Obesity and Obesity-Related Disorders by Pharmalogical Targeting of Kv 1.3 Potassium Channels

Thu, 06 Apr 2017 08:00:00 EDT

Activation of brown adipose tissue, treatment of obesity and/or treatment of obesity-related disorders in human or non-human animal subjects by administering to the subject a potassium channel inhibiting agent. The potassium channel inhibiting agent may comprise ShK toxin or a modified ShK toxin. Examples of modified ShK toxins include ShK-186.



ENDOMUCIN AS AN ANTI-INFLAMMATORY AGENT

Thu, 06 Apr 2017 08:00:00 EDT

The invention provides compositions and methods for utilizing endomucin as an anti-inflammatory agent.



USE OF CYCLIC PEPTIDES FROM FLAXSEED FOR IMPROVING ANIMAL AND HUMAN HEALTH

Thu, 06 Apr 2017 08:00:00 EDT

The present application includes a method for improving human and animal health comprising administering an effective amount of a linus cyclopeptide (LCP) extract from flaxseed to a subject in need thereof. Also included are feeds, foodstuffs, functional food compositions, natural product compositions nutraceuticals and food additive compositions comprising an LCP extract from flaxseed.



METHOD OF TREATING LOW BLOOD PRESSURE

Thu, 06 Apr 2017 08:00:00 EDT

A method for treating a patient suffering from one of septic shock, acute kidney injury, severe hypotension, cardiac arrest, and refractory hypotension, but not from myocardial infarction, is provided. The method includes administering a therapeutically effective dose of Angiotensin II, or Ang II, to the patient.



CONJUGATES AND PRODRUGS FOR TREATING OF CANCER AND INFLAMMATORY DISEASES

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to the field of cancer and inflammatory diseases. More particularly, it aims to provide, for these purposes, novel conjugated forms of active ingredients belonging to the dolastatin family and having the formula as follows: It is also directed towards prodrug forms of these conjugates.



WINTERIZED CRUDE CANNABIS EXTRACTS AND METHODS OF PREPARATION AND USE

Thu, 06 Apr 2017 08:00:00 EDT

The present technology relates to liquid compositions for use in a personal vaporizer. More particularly, the present technology relates to liquid compositions comprising winterized Cannabis extract, and to methods of administering vaporized, winterized Cannabis extract to a subject by inhalation.



INHIBITION OF ENDOSOMAL TOLL-LIKE RECEPTOR ACTIVATION

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates, in general, to pattern-recognition receptors (PRRs), including toll-like receptors (TLRs), and, in particular, to a method of inhibiting nucleic acid-induced activation of, for example, endosomal TLRs using an agent that binds to the nucleic acid (“nucleic acid binding agent”), preferably, in a manner that is independent of the nucleotide sequence, the chemistry (e.g., DNA or RNA, with or without base or sugar modifications) and/or the structure (e.g., double-stranded or single-stranded, complexed or uncomplexed with, for example protein) of the nucleic acid(s) responsible for inducing TLR activation. The invention also relates to methods of identifying nucleic acid binding agents suitable for use in such methods.



PHARMACEUTICAL COMPOSITIONS COMPOSED OF LOW MOLECULAR WEIGHT SULFATED HYALURONAN

Thu, 06 Apr 2017 08:00:00 EDT

Described herein are pharmaceutical compositions composed of low molecular weight sulfated hyaluronan.



COMBINATION FORMULATION OF TWO ANTIVIRAL COMPOUNDS

Thu, 06 Apr 2017 08:00:00 EDT

Disclosed are pharmaceutical compositions comprising Compound I, having the formula: and an effective amount of sofosbuvir wherein the sofosbuvir is substantially crystalline. Also disclosed are methods of use for the pharmaceutical composition.



FORMULATION COMPRISING A GEMCITABINE-PRODRUG

Thu, 06 Apr 2017 08:00:00 EDT

This invention relates to pharmaceutical formulations of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate, a monophosphate derivative of the well-known oncology drug gemcitabine. In particular, the invention relates to formulations which comprise a polar aprotic solvent, preferably dimethyl acetamide (DMA). Formulations comprising these solvent provide therapeutically effective treatments of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. The invention also relates to methods of using said formulations and kits comprising said formulations.



TRANSIENT INHIBITION OF ADENOSINE KINASE AS AN ANTI-EPILEPTOGENESIS TREATMENT

Thu, 06 Apr 2017 08:00:00 EDT

Methods of anti-epileptogenesis treatment in which adenosine kinase (ADK) activity or expression is inhibited only transiently to provide a long-term benefit to a non-epileptic or epileptic subject. In an exemplary method, a therapeutically effective amount of an ADK inhibitor may be administered to a human non-epileptic subject over a finite, predetermined treatment period having a duration of less than two months. The non-epileptic subject may have sustained a precipitating event with a known risk to trigger latent development of an acquired form of epilepsy. Administration of the ADK inhibitor to the subject may be stopped at the end of the treatment period for at least the longer of (i) six months and (ii) ten times the duration of the treatment period. The step of administering may reduce the chance of the subject having seizures caused by the acquired form of epilepsy for an extended period following the end of the treatment period.



GALACTOSIDE INHIBITORS FOR NEW USES

Thu, 06 Apr 2017 08:00:00 EDT

Provided is a method for treatment or prevention of α-synucleinopathies in a mammalian subject, the method comprising administering a therapeutically effective amount of at least one composition to the subject, wherein the composition comprises a molecule for pharmacological modulation of galectin activity in a mammalian brain.



Pharmaceutical Composition and Method for Neoangiogenesis/Revascularization Useful in Treating Ischemic Heart Disease

Thu, 06 Apr 2017 08:00:00 EDT

A pharmaceutical composition and a method of treating ischemic heart diseases by growing new blood vessels that supply oxygen and nutrients to infarcted heart tissues throughout the entire infarct zone and for preventing cardiomyocyte apoptosis in ischemic events. The pharmaceutical composition contains an active ingredient compound with a backbone structure of formula (I).



Process for the Extraction of Strawberry P-Coumaroyl Hexose and/or Polyphenols, Extract and Uses Thereof

Thu, 06 Apr 2017 08:00:00 EDT

A composition of purified and biologically active p-coumaroyl hexose and/or polyphenols is provided by separation from strawberry's pulp by a method of extraction and purification using a hydrophobic adsorbent using GRAS solvent. Also provided is the use of the composition.



NOVEL TLR4 INHIBITORS FOR THE TREATMENT OF HUMAN INFECTIOUS AND INFLAMMATORY DISORDERS

Thu, 06 Apr 2017 08:00:00 EDT

The present invention relates to methods of treating infectious, inflammatory and post-traumatic disorders by administering various compounds newly discovered to have TLR4 inhibitory activity. In addition to methods of treatment, the present invention further provides for pharmaceutical compositions comprising said compounds, together with a suitable pharmaceutical carrier. Because TLR4 is the most upstream receptor in the pro-inflammatory LPS signaling cascade, treatments of the invention, which inhibit or antagonize TLR4 action, may avoid the pitfalls associated with other cytokine inhibitors that act further down the pathway and accordingly play a less specific (and perhaps non-critical) role.



Synthetic composition for regulating satiety

Thu, 06 Apr 2017 08:00:00 EDT

The application relates to synthetic compositions containing one or more human milk oligosaccharides for regulating satiety or reducing propensity to obesity.



IMIDAZOPYRIDINES SYK INHIBITORS

Thu, 06 Apr 2017 08:00:00 EDT

Certain imidazopyridines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.



COMPOSITIONS FOR ORAL ADMINISTRATION OF ZOLEDRONIC ACID OR RELATED COMPOUNDS FOR TREATING COMPLEX REGIONAL PAIN SYNDROME

Thu, 06 Apr 2017 08:00:00 EDT

Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, such as zoledronic acid, can be used to treat or alleviate pain or related conditions.



Compositions for oral administration of zoledronic acid or related compounds for treating complex regional pain syndrome

Thu, 06 Apr 2017 08:00:00 EDT

Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, can be used to treat or alleviate pain or related conditions such as complex regional pain syndrome.



CO-ADMINISTRATION OF STEROIDS AND ZOLEDRONIC ACID TO PREVENT AND TREAT PAIN

Thu, 06 Apr 2017 08:00:00 EDT

Oral dosage forms of osteoclast inhibitors, such as nitrogen-containing bisphosphonates, such as zoledronic acid and neridronic acid in an acid or a salt form, or in a molecular complex can be used to treat or alleviate pain or related conditions, such as complex regional pain syndrome.



METHODS AND COMPOUNDS TO INHIBIT ENVELOPED VIRUS RELEASE

Thu, 06 Apr 2017 08:00:00 EDT

A compound having an antiviral activity for inhibiting release of an enveloped virus from a cell is disclosed, including methods of inhibiting release of an enveloped virus from a cell. The antiviral activity of the compound includes inhibiting formation of an associative complex or disrupting formation of an associative complex. The associative complex comprises an L-domain motif of the enveloped virus and at least one cellular polypeptide, or fragment thereof, capable of binding the L-domain motif of the enveloped virus.



DGAT1 INHIBITION FOR TREATMENT OF DEMYELINATING INFLAMMATORY DISEASE

Thu, 06 Apr 2017 08:00:00 EDT

Methods are provided for treating autoimmune disease in a subject by inhibiting the activity of DGAT1.



PHARMACEUTICAL COMBINATION COMPRISING A CLASS III RECEPTOR TYROSINE KINASE INHIBITOR AND THE ALKYLATING HISTONE-DEACETYLASE INHIBITOR FUSION MOLECULE EDO-S101 TOGETHER WITH ITS USE IN THE TREATMENT OF CANCER

Thu, 06 Apr 2017 08:00:00 EDT

The present invention is directed to a combination comprising a class III receptor tyrosine kinase inhibitor and a compound of formula I or a pharmaceutically acceptable salt thereof: to a pharmaceutical composition and to a kit both comprising said combination, to the combination, composition or kit for use in the treatment of cancer, and to a method of treatment of cancer in a patient in need thereof comprising administering to said patient an effective amount of said combination, composition or kit.



Compounds That Enhance ATOH1 Expression

Thu, 06 Apr 2017 08:00:00 EDT

This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.