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METHODS AND MATERIALS FOR CHARACTERIZING INTESTINAL BARRIER FUNCTION

Thu, 23 Feb 2017 08:00:00 EST

The present invention the present invention provides methods and materials related to the characterization of intestinal barrier function, and related methods for preventing and/or treating intestinal barrier dysfunction. In particular, the present invention provides methods and materials for characterizing intestinal barrier function within mammals (e.g., humans) through determining the level, presence, and/or frequency of biomarkers for intestinal function (e.g., functional enterocyte mass, enterocyte integrity, paracellular tight junction function, gut inflammation) within a biological sample.



Methods for Diagnosing and Treating Iron Dysregulation

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to methods for diagnosing and treating iron overload and iron deficiency.



BIOMARKERS FOR RESPONSE TO PI3K INHIBITORS

Thu, 23 Feb 2017 08:00:00 EST

The presently disclosed subject matter relates to the use of one or more biomarkers to evaluate whether a PI3Kα inhibitor would produce an anti-cancer effect in a subject during the course of treatment with a PI3Kα inhibitor. It is based, at least in part, on the discovery that certain nucleotides can be isolated from the serum of patients undergoing cancer treatment and can be used as a biomarker to indicate the effectiveness of PI3K treatment on cancer growth. Accordingly, in a non-limiting embodiment, a method for determining whether an anti-cancer effect is likely being produced in a cancer by a PI3Kα inhibitor, comprises determining the presence and/or level of one or more PIK3CA biomarkers in one or more samples serially obtained during PI3Kα inhibitor treatment, where if the presence and/or level of a PIK3CA biomarker is increased, it is less likely that the PI3Kα inhibitor is having an anti-cancer effect on the cancer.



METHODS OF TREATING CANCER PATIENTS WITH FARNESYLTRANSFERASE INHIBITORS

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to the field of molecular biology and cancer biology. Specifically, the present invention relates to methods of treating a subject with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on genotyping and expression profiling of certain immunological genes and RAS mutation status in the subject.



DIAGNOSIS OF COWDEN AND COWDEN-LIKE SYNDROME BY DETECTION OF DECREASED KILLIN EXPRESSION

Thu, 23 Feb 2017 08:00:00 EST

A method of diagnosing Cowden syndrome (CS) and Cowden-like Syndrome (CLS) is described. The method includes diagnosing CS and CLS in a subject by identifying a decrease in expression of the KILLIN gene, or by identifying hypermethylation of the KILLIN promoter region. Kits for diagnosing CS and CLS by identifying subjects having KILLIN promoter region hypermethylation and primers specific for a methylated KILLIN promoter region are also described.



Cationic Polymer Based Wired Enzyme Formulations for Use in Analyte Sensors

Thu, 23 Feb 2017 08:00:00 EST

Embodiments of the invention include analyte-responsive compositions and electrochemical analyte sensors having a sensing layer that includes an analyte-responsive enzyme and a cationic polymer. Also provided are systems and methods of making the sensors and using the electrochemical analyte sensors in analyte monitoring.



RNAi-Mediated Inhibition of Phosphodiesterase Type 4 for Treatment of CAMP-Related Ocular Disorders

Thu, 23 Feb 2017 08:00:00 EST

RNA interference is provided for inhibition of phosphodiesterase type 4 mRNA expression for treating patients with a cAMP-related ocular disorder. Phosphodiesterase type 4 mRNA targets include mRNA for 4A, 4B, 4C, and 4D phosphodiesterase isoforms.



METHODS FOR TREATMENT OF DISORDERS IN THE FRONT OF THE EYE UTILIZING NUCLEIC ACID MOLECULES

Thu, 23 Feb 2017 08:00:00 EST

Aspects of the invention relate to methods for treating an ocular disorder associated with the front of the eye, comprising administering to the eye of a subject in need thereof a therapeutic RNA molecule, in an effective amount to treat an ocular disorder associated with the front of the eye.



COMPOSITION FOR ENHANCING RADIATION SENSITIVITY COMPRISING PI4K ISOZYME INHIBITOR

Thu, 23 Feb 2017 08:00:00 EST

The present disclosure relates to a composition for enhancing radiation sensitivity including a PI4K isozyme inhibitor as an active ingredient. As the PI4K isozyme inhibitor, a PI4K isozyme-specific siRNA or antiviral agent according to the present disclosure has an excellent effect of enhancing radiation sensitivity such as reducing viability of the cancer cells and radiation resistance during in radiation irradiation and suppressing and delaying DNA damage repair induced by the radiation by inhibiting the PI4K isozyme to be used as a radiation sensitivity adjuvant and an anticancer treatment assisting agent.



METHODS FOR TREATING CANCER USING NUCLEIC ACIDS TARGETING MDM2 OR MYCN

Thu, 23 Feb 2017 08:00:00 EST

Aspects of the invention relate to methods for treating cancer by administering to a subject in need thereof a therapeutically effective amount of a nucleic acid molecule that is directed against a gene encoding mouse double minute 1 homolog (MDM1), mouse double minute 2 homolog (MDM2), mouse double minute 3 homolog (MDM3), mouse double minute 4 homolog (MDM4) or V-myc myelocytomatosis viral related oncogene (MYCN) for treating cancer. Further aspects of the invention relate to nucleic acid molecules and compositions comprising nucleic acid molecules.



USE OF TELOMERASE INHIBITORS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISORDERS AND MYELOPROLIFERATIVE NEOPLASMS

Thu, 23 Feb 2017 08:00:00 EST

Provided herein are methods for reducing neoplastic progenitor cell proliferation and alleviating symptoms associated in individuals diagnosed with or thought to have Essential Thrombocythemia (ET). Also provided herein are methods for using telomerase inhibitors for maintaining blood platelet counts at relatively normal ranges in the blood of individuals diagnosed with or suspected of having ET.



METHODS AND MODIFICATIONS THAT PRODUCE ssRNAi COMPOUNDS WITH ENHANCED ACTIVITY, POTENCY AND DURATION OF EFFECT

Thu, 23 Feb 2017 08:00:00 EST

Compositions and methods for down modulating expression of target nucleic acids using a single strand oligoribonucleotide siRNA compound are disclosed.



Manipulating MicroRNA for the Management of Neurological Diseases or Conditions and Compositions Related Thereto

Thu, 23 Feb 2017 08:00:00 EST

This disclosure relates to manipulating microRNA for the management of neurological disorders and compositions related thereto. In certain embodiments, the disclosure contemplates inhibition of miR324 or miR324-5p, e.g., the use of nucleobase polymers for antisense disruptions or RNA interference of miR-324 expression or for miR324-5p binding in order to increase Kv4.2 expression. In certain embodiments, the disclosure relates to methods of treating or preventing a neurological disease or condition comprising administering an effective amount of an inhibitor to a subject in need thereto.



RNA INTERFERENCE FOR THE TREATMENT OF GAIN-OF-FUNCTION DISORDERS

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to the discovery of an effective treatment for a variety of gain-of-function diseases, in particular, Huntington's disease (HD). The present invention utilizes RNA Interference technology (RNAi) against polymorphic regions in the genes encoding various gain-of-function mutant proteins resulting in an effective treatment for the gain-of-function disease.



EXTRACELLULAR VESICLE METHODS AND COMPOSITIONS

Thu, 23 Feb 2017 08:00:00 EST

Disclosed herein are methods and compositions for treating cancers.



METHOD AND COMPOSITION FOR DIAGNOSIS OR TREATMENT OF AGGRESSIVE PROSTATE CANCER

Thu, 23 Feb 2017 08:00:00 EST

Methods, pharmaceutical formulations and medicaments for treating prostate cancer or preventing the progression of a nonaggressive form of prostate cancer to an aggressive form, in a mammal, include a therapeutically effective amount of one or more active agents that reduce the expression or biological activity of both Forkhead box protein M1 (FOXM1) and Centromere protein F (CENPF) or biologically active fragments thereof or biologically active fragments thereof selected from the group consisting of an isolated shRNA, siRNA, antisense RNA, antisense DNA, Chimeric Antisense DNA/RNA, microRNA, and ribozymes that are sufficiently complementary to either a gene or an mRNA encoding either FOXM1 or CENPF proteins. A method is also presented for discovering synergistic master regulators of other phenotype transitions, wherein the master regulators are conserved among different species.



METHODS AND COMPOSITIONS FOR INHIBITING RETINOPATHY OF PREMATURITY

Thu, 23 Feb 2017 08:00:00 EST

Disclosed are vectors and compositions comprising a pol II promoter and an shRNA wherein the shRNA has a sense RNA strand and an antisense RNA strand, wherein the sense and the antisense RNA strands form an RNA duplex, and wherein the sense RNA strand comprises a nucleotide sequence identical to a target sequence in STAT3, VEGFR, or EPOR. Also disclosed are methods of treating retinopathy of prematurity (ROP), methods of inhibiting expression of STAT3, VEGFR, and EPOR, and methods of regulating signaling events associated with intravitreal neovascularization (IVNV).



VASCULAR RE-MODELLING

Thu, 23 Feb 2017 08:00:00 EST

The present invention is based on the finding that microRNA from the microRNA gene cluster located on the human chromosomal at locus 14q32 play an important role in vascular development and re-modelling. Modulators of any of the 14q32 microRNA may be exploited as a means to modulate vascular re-modelling processes and/or in the treatment and/or prevention of vascular disorders or disease.



METHODS FOR TREATING PROGEROID LAMINOPATHIES USING OLIGONUCLEOTIDE ANALOGUES TARGETING HUMAN LMNA

Thu, 23 Feb 2017 08:00:00 EST

Provided are methods of treatment in subjects having progeroid diseases and related conditions which rely upon LMNA-targeted antisense oligonucleotides for reducing expression of one or more aberrantly spliced LMNA mRNA isoforms that encode progerin.



ANTISENSE OLIGOMERS AND METHODS FOR TREATING SMN-RELATED PATHOLOGIES

Thu, 23 Feb 2017 08:00:00 EST

An antisense oligonucleotide of 10 to 50 nucleotides comprising a targeting sequence complementary to a region near or within intron 6, intron 7, or exon 8 of the Survival Motor Neuron 2 (SMN2) gene pre-mRNA.



AZOARYLS AS REVERSIBLY MODULATABLE TUBULIN INHIBITORS

Thu, 23 Feb 2017 08:00:00 EST

The invention concerns a new class of tubulin polymerisation inhibitors and their applications in research and medicine, notably in chemotherapy. The invention proposes new azoaryl derivatives of formula (I): as defined in Claim 1, which may be fully reversibly interconverted between non-tubulin-binding trans and tubulin-binding as isomeric forms, either by irradiation or spontaneously. The invention also concerns compounds with a azoaryl structure for use in studying the cytoskeleton and/or its associated processes, or in the treatment of a disease for which a tubulin polymerisation inhibition activity has a beneficial effect, wherein the compound is administered to the cell, organism or patient in need of such treatment in the trans form of the diazenyl bond, and where this trans form is inactive as regards a tubulin polymerisation inhibition effect, and where after photoisomerisation in vitro, in cellulo or in vivo to an azoaryl compound in its cis isomeric form of the diazenyl bond by the application of light, optionally with modification in vitro, in cellulo or in vivo of one or more substituents, the resultant cis form is active as regards a tubulin polymerisation inhibition effect.



BIODEGRADABLE POLYESTERAMIDE COPOLYMERS FOR DRUG DELIVERY

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to a poly (ester amide) (PEA) having a chemical formula described by structural formula (IV), wherein m+p varies from 0.9-0.1 and q varies from 0.1 to 0.9m+p+q=1 whereby m or p could be 0n is about 5 to about 300; (pref. 50-200)R1 is independently selected from the group consisting of (C2-C20) alkylene, (C2-C20) alkenylene, —(R9—CO—O—R10—O—CO—R9)—, —CHR11—O—CO—R12—COOCR11— and combinations thereof;R3 and R4 in a single backbone unit m or p, respectively, are independently selected from the group consisting of hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C6-C10)aryl, (C1-C6)alkyl, —(CH2)SH, —(CH2)2S(CH3), —CH2OH, —CH(OH)CH3, —(CH2)4NH3+, —(CH2)3NHC(═NH2+)NH2, —CH2COOH, —(CH2)COOH, —CH2—CO—NH2, —CH2CH2—CO—NH2, —CH2CH2COOH, CH3—CH2—CH(CH3)—, (CH3)2—CH—CH2—, H2N—(CH2)4—, Ph-CH2—, CH═C—CH2—, HO-p-Ph-CH2—, (CH3)2—CH—, Ph-NH—, NH—(CH2)3—C—, NH—CH═N—CH═C—CH2—.R5 is selected from the group consisting of (C2-C20)alkylene, (C2-C20)alkenylene, alkyloxy or oligoethyleneglycolR6 is selected from bicyclic-fragments of 1,4:3,6-dianhydrohexitols of structural formula (III); R7 is selected from the group consisting of (C6-C10)aryl (C1-C6)alkylR8 is —(CH2)4-;R9 or R10 are independently selected from C2-C12 alkylene or C2-C12 alkenylene.R11 or R12 are independently selected from H, methyl, C2-C12 alkylene or C2-C12 alkenylene whereby a is at least 0.05 and b is at least 0.05 and a+b=1.



FACTOR VIII B CELL EPITOPE VARIANTS HAVING REDUCED IMMUNOGENICITY

Thu, 23 Feb 2017 08:00:00 EST

Provided herein are methods and compositions for preventing or reducing an initial immune response to factor VIII in patients suffering from hemophilia A and for reducing the intensity of the immune response in patients having pre-formed inhibitor antibodies against factor VIII.



CCR2 ANTAGONIST PEPTIDES

Thu, 23 Feb 2017 08:00:00 EST

The invention relates to a peptide comprising the following amino acid sequence Thr-Phe-Leu-Lys or Thr-Phe-Leu-Lys-Cys, useful as a CCR2 non competitive antagonist peptide.



Novel Glucagon Analogues

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to novel peptide compounds which have a protracted profile of action and improved solubility and stability, to the use of the compounds in therapy, to methods of treatment comprising administration of the compounds to patients in need thereof, and to the use of the compounds in the manufacture of medicaments. The compounds of the invention are of particular interest in relation to the treatment of hyperglycemia, diabetes and obesity, as well as a variety of diseases or conditions associated with hyperglycemia, diabetes and obesity.



Variants of C-Type Natriuretic Peptide

Thu, 23 Feb 2017 08:00:00 EST

The present disclosure provides variants of C-type natriuretic peptide (CNP), pharmaceutical compositions comprising CNP variants, and methods of making CNP variants. The CNP variants are useful as therapeutic agents for the treatment of diseases responsive to CNP, including but not limited to bone-related disorders, such as skeletal dysplasias (e.g., achondroplasia), and vascular smooth muscle disorders (e.g., restenosis and arteriosclerosis).



ISLET AMYLOID POLYPEPTIDES WITH IMPROVED SOLUBILITY

Thu, 23 Feb 2017 08:00:00 EST

The present disclosure provides for isolated non-naturally occurring, mutant-human IAPP polypeptides. These polypeptides can be formulated or co-formulated at physiological pH, which enable the polypeptides of the instant disclosure to be delivered to a subject having an amyloid-based disease in a single injection with an insulin agent. The present disclosure also provides methods and compositions for treating amyloid-based disease in a subject in need thereof, comprising administering an effective amount of an isolated, mutant-hIAPP polypeptide, including formulations or co-formulations thereof.



INTEGRIN-BLOCKING POLYPEPTIDES AND USES THEREOF

Thu, 23 Feb 2017 08:00:00 EST

A series of integrin blockers that present strong angiogenesis inhibiting performance, high integrin affinity and integrin-bonding capacity is provided. This series of integrin blockers can be adopted in treatment of solid tumors and rheumatoid arthritis. Specifically, said series of integrin blockers include polypeptide I, polypeptide II and polypeptide III (see SEQ ID NO: 1, SEQ ID NO: 2 and SEQ ID NO: 3) that can be adopted in treatment of solid tumors and rheumatoid arthritis. This invention also relates to application of these three integrin-blocking polypeptides in preparation of anti-tumor drugs, wherein the tumors that can be treated include those primary or secondary cancers originated from head and neck region or other organs such as brain, thyroid, esophagus, pancreas, lung, liver, stomach, breast, kidney, gallbladder, colon, rectum, ovary, cervix, uterus, prostate, bladder and testicle, as well as melanoma and sarcomas.



ANTI-INFLAMMATORY NANOFIBERS

Thu, 23 Feb 2017 08:00:00 EST

Provided herein are anti-inflammatory nanofibers and methods of use thereof. In particular methods are provided for the use of anti-inflammatory nanofibers in the promotion of tissue (e.g., urinary bladder tissue) regeneration.



PEPTIDE HAVING EFFICACY FOR REMEDYING HYPOPIGMENTATION AND INHIBITING ADIPOGENESIS, AND USE OF SAME

Thu, 23 Feb 2017 08:00:00 EST

A peptide formed from the amino acid sequence of SEQ ID NO: 1 or SEQ ID NO: 2, according to the present invention, shows a melanogenesis increment activity and an adipogenesis inhibitory activity. A peptide of the present invention, by increasing phosphorylation of MITF, which is a transcription factor for increasing a tyrosinase expression, and CREB for increasing an MITF expression, consequently increases a tyrosinase expression and ultimately increases melanin synthesis. A peptide of the present invention, by reducing the amount of fat accumulated inside a cell and reducing expressions of perilipin and PPARγ, which contribute to adipogenic mechanism, ultimately inhibits adipogenesis. The present invention provides a composition for remedying or treating melanin hypopigmentation, the composition comprising the peptide, and provides pharmaceutical composition for treating or preventing obesity.



HEPCIDIN MIMETIC PEPTIDES AND USES THEREOF

Thu, 23 Feb 2017 08:00:00 EST

Compounds and methods are described herein that can be used to treat subjects for conditions related to hepcidin activity, such as but not limited diseases of iron metabolism, beta thalassemia, hemochromatosis, iron-loading anemias, alcoholic liver disease, or chronic hepatitis C.



INHIBITORS OF NF KAPPA-B ACTIVITY FOR TREATMENT OF DISEASES AND DISORDERS

Thu, 23 Feb 2017 08:00:00 EST

Peptides and methods of use thereof, are disclosed for use in treating various disease and disorders, including inflammation, pain, oral mucositis, oral lesions, and cancer. The peptides modulate the activity of the transcription factor NF κB.



ANDROSTANE AND PREGNANE STEROIDS WITH POTENT ALLOSTERIC GABA RECEPTOR CHLORIDE IONOPHORE MODULATING PROPERTIES

Thu, 23 Feb 2017 08:00:00 EST

This invention describes compounds of Structures 1, 2, and 3 and their use as allosteric modulators of the GABA receptor chloride ionophore complex to alleviate stress, anxiety, mood disorders, seizures, depression, treatment of drug and alcohol abuse, memory, premenstrual disorders, and neural system damage.



C-TERMINAL HSP90 INHIBITORS

Thu, 23 Feb 2017 08:00:00 EST

Hsp90 C-terminal inhibitors and pharmaceutical compositions containing such compounds are provided. The compounds of the disclosure are useful for the treatment and/or prevention of neurodegenerative disorders such as diabetic peripheral neuropathy.



HETERODINUCLEAR PLATINUM-RUTHENIUM COMPLEXES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF

Thu, 23 Feb 2017 08:00:00 EST

A novel class of heterodinuclear Pt—Ru complexes are provided, and the methods for preparing the complexes are described. The inhibitory activities of the heterodinuclear Pt—Ru complexes against cancer/tumor cell growth, including cancer/tumor cells having a resistance to cisplatin, are further demonstrated.



Substituted 4-Phenyl Pyridines

Thu, 23 Feb 2017 08:00:00 EST

Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK1) receptor. The compounds have the general formula (I):



NOVEL ANNELATED PHENOXYACETAMIDES

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to compounds of formula (I) wherein R1, R2, R3, and Z− have one of the meanings as indicated in the specification or a pharmaceutically acceptable salt thereof, to the use of compounds of formula (I) as a medicament, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I).



PYRIMIDINONES AS PI3K INHIBITORS

Thu, 23 Feb 2017 08:00:00 EST

The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.



HISTONE DEACETYLASE INHIBITORS

Thu, 23 Feb 2017 08:00:00 EST

This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).



NEW CRYSTALLINE FORM OF CEFAMANDOLE SODIUM COMPOUND, FORMULATION AND PREPARATION METHOD THEREOF

Thu, 23 Feb 2017 08:00:00 EST

A novel crystalline form is defined by diffraction angle 2θ° of X-ray powder diffraction pattern and characteristic peak of differential scanning calorimetry (DSC). The novel crystalline form of Cefamandole Nafate is prepared as follows: adding Cefamandole Nafate in solid state to an organic solvent to form a suspension with a concentration of 0.04˜0.3 g/ml, stirring the suspension at 40˜50° C. for a period of time, and then cooling to 5˜15° C. at certain cooling rate, continuing to stir for a period of time, then suction filtrating the obtained suspension, the resulting filer cake is Cefamandole Nafate as wet product, which is dried to constant weight to provide the novel crystalline form of Cefamandole Nafate as final product.



OXADIAZINE COMPOUNDS AND METHODS OF USE THEREOF

Thu, 23 Feb 2017 08:00:00 EST

The present disclosure relates to oxadiazine compounds, pharmaceutical compositions comprising an effective amount of an oxadiazine compound and methods for using an oxadiazine compound in the treatment of a neurodegenerative disease, comprising administering to a subject in need thereof an effective amount of an oxadiazine compound.



SMALL MOLECULE INHIBITORS OF G PROTEIN COUPLED RECEPTOR 6 KINASES POLYPEPTIDES

Thu, 23 Feb 2017 08:00:00 EST

This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.



Monocyclic, Thieno, Pyrido, and Pyrrolo Pyrimidine Compounds and Methods of Use and Manufacture of the Same

Thu, 23 Feb 2017 08:00:00 EST

The present invention provides a compound of Formula I: wherein R is H, a methyl group, an ethyl group, a n-propyl group, an iso-propyl group, or a n-butyl group; and R1 is H, a 4′-methyl group, a 4′-OH, a 4′-OMe group, a 2′,3′-C2H4 group, a; 3′,4′-C2H4 group, a 3′,4′-diF, a 3′,4′,5′-triF, or a 4′-OCF3; and optionally including a salt or a hydrate of said compound, and further provides a pharmaceutical composition comprising the compound of Formula I and one or more acceptable pharmaceutical carriers. A method of treating a patient having cancer comprising administering a therapeutically effective amount of a compound of Formula I, or a pharmaceutical composition comprising a compound of Formula I and one or more acceptable pharmaceutical carriers to the patient is disclosed.



TETRANDRINE FAMILY PHARMACEUTICAL FORMULATIONS AND METHOD

Thu, 23 Feb 2017 08:00:00 EST

Drug formulations, methods and their use in treatment of diseases using formulations of pure di-acid salts of tetrandrine family members, especially d-tetrandrine di-hydrochloride, combined with a pharmaceutical diluent or carrier.



TETRANDRINE FAMILY PHARMACEUTICAL FORMULATIONS AND METHOD

Thu, 23 Feb 2017 08:00:00 EST

Drug formulations, methods and their use in treatment of diseases using formulations of pure di-acid salts of tetrandrine family members, especially d-tetrandrine di-hydrochloride, combined with a pharmaceutical diluent or carrier.



HETEROCYCLIC COMPOUND

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to compound (I) or a salt thereof which has a RORγt inhibitory action. wherein each symbol is as defined in the specification.



TETRAHYDROOXEPINOPYRIDINE COMPOUND

Thu, 23 Feb 2017 08:00:00 EST

[Problem] Provided is a compound having a positive allosteric modulating activity (PAM activity) on an α7 nicotinic acetylcholine receptor (α7 nACh receptor). [Means for Solution] The present inventors have studied on a PAM activity on an α7 nACh receptor, and they have found that a tetrahydrooxepinopyridine compound has a PAM activity on an α7 nACh receptor, thereby completing the present invention. The tetrahydrooxepinopyridine compound of the present invention has a PAM activity on an α7 nACh receptor and can be expected as an agent for preventing or treating dementia, cognitive impairment, schizophrenia, Alzheimer's disease, CIAS, negative symptoms of schizophrenia, inflammatory diseases, or pain.



PYRROLOBENZODIAZEPINE COMPOUNDS

Thu, 23 Feb 2017 08:00:00 EST

The invention relates to pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) of formula (I) and in particular to PBD dimers linked through the C1 position, and PBD monomers linked through the C1 position to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents. (I) and salts or solvates thereof, wherein: the dotted lines indicates the optional presence of a double bond between C1 and C2 or C2 and C3; R2-R7 are independently selected substituent groups; and either: (i) R8 and R9 together form a double bond; (ii) R8 is H and R9 is OH; or (iii) R8 is H and R9 is ORA and RA is C1-6 alkyl; where R1 has the formula: —X-L-X′-D-X-L-X′— is a linker group and D has the formula (II) or (III): or where the compound is a dimer with each monomer being the same or different and being of formula (I) where the R1 of the first monomer and R′1 or R′6 of the second monomer, or R6 of the first monomer and R′1 of the second monomer, form together a bridge having the formula —X-L-X′— linking the monomers.



INHIBITORS OF BRUTON'S TYROSINE KINASE

Thu, 23 Feb 2017 08:00:00 EST

Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.



BROMODOMAIN INHIBITOR

Thu, 23 Feb 2017 08:00:00 EST

The present invention relates to substituted heterocyclic derivative compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition of acetyl lysine regions of proteins, such as histones. Said compositions and methods are useful for the treatment of cancer and neoplastic disease.