Class / Patent application number | Description | Number of patent applications / Date published |
514309000 | Chalcogen attached directly to the six-membered hetero ring by nonionic bonding | 77 |
20080207685 | Heterocyclic Compounds As Modulators Of Peroxisome Proliferator Activated Receptors, Useful For The Treatment And/Or Prevention Of Disorders Modulated By A Ppar - The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases. | 08-28-2008 |
20080242699 | Cyclohexylamin isoquinolone derivatives - The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) | 10-02-2008 |
20080249128 | Substituted Sulfonamide Compounds - Substituted sulfonamide compounds with bradykinin receptor (B1R) modulating activity; processes for the preparation thereof, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or inhibit pain and/or other disorders and/or disease states. | 10-09-2008 |
20080293763 | NOVEL NITROGEN-CONTAINING HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. | 11-27-2008 |
20090093518 | Piperidinyl-substituted isoquinolone derivatives - The invention relates to 6-piperidinyl-substituted isoquinolone derivatives of the formula (I) | 04-09-2009 |
20090131473 | 2-(ARYLOXY) ACETAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS - The present invention relates generally to novel 2-(aryloxy)acetamides of Formula (I): | 05-21-2009 |
20090163542 | 5-ht7 receptor antagonists - The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some tetrahydroisoquinoline substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders. | 06-25-2009 |
20090221634 | Compositions and Methods for Disruption of BRCA2-Rad51 Interaction - Contemplated compounds disrupt interaction between BRCA2 and RAD51, likely by binding to RAD51. Based on the crucial role of the BRCA2-RAD51 complex formation in DNA repair and the role of RAD51 in the control of entry into S-phase from G1, numerous compositions and methods are presented. Among other advantageous uses, contemplated compounds may be employed as protective agents for non-neoplastic cells in chemotherapy before exposure of the cells to a chemotherapeutic drug, and/or as DNA-damage sensitizer for neoplastic cells. | 09-03-2009 |
20090298871 | SULFONYL-PHENYL-2H-[1,2,4]OXADIAZOL-5-ONE DERIVATIVES , PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS - The invention relates to sulfonyl-phenyl-oxadiazolones and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARgamma agonist activity. | 12-03-2009 |
20100056568 | Cycloalkylamine substituted isoquinolone and isoquinolinone derivatives - The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) | 03-04-2010 |
20100076016 | ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds. | 03-25-2010 |
20100105725 | ANTIDIABETIC BICYCLIC COMPOUNDS - Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders. | 04-29-2010 |
20100137359 | CASPASE INHIBITORS AND USES THEREOF - The present invention provides a compound of formula I: | 06-03-2010 |
20100184802 | Bicycloheteroaryl Compounds as P2X7 Modulators and Uses Thereof - Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others. | 07-22-2010 |
20100197725 | 1-OXO-ISOINDOLINE-4-CARBOXAMIDE AND 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLINE-5-CARBOXAMIDE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof. | 08-05-2010 |
20100240698 | MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS - Inhibitors of HCV of formula al | 09-23-2010 |
20100267767 | NUCLEAR RECEPTOR BINDING AGENTS - The present invention relates to methods for prevention and/or treatment of metabolic disorders, post-menopausal obesity and conditions associated with high fat diet consumption including, obesity, body weight gain, fat mass formation, bone mineral content reduction, white adipose tissue weight gain, increased cholesterol levels, increased leptin levels, insulin resistance, type II diabetes, increased blood glucose levels, inflammatory diseases, cardiovascular diseases, fatty liver condition (accumulation of fat in the liver), decreased uncoupling protein-1 (UCP-1) levels and increased lipogenesis. | 10-21-2010 |
20100280067 | INHIBITORS OF ACETYL-COA CARBOXYLASE - The present invention relates to compounds that act as acetyl-CoA carboxylase (ACC) inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds. | 11-04-2010 |
20100317691 | ISOQUINOLONE COMPOUNDS AS SUBTYPE-SELECTIVE AGONISTS FOR MELATONIN RECEPTORS MT1 AND MT2 - A method of treating, preventing, or ameliorating a pathological condition associated with a melatonin receptor in a mammal by using a pharmaceutical composition containing a compound of formula (I) as a ligand interacting with the melatonin receptor, | 12-16-2010 |
20100331362 | Treatment method for anemia - The present invention relates to improved methods for treating anemia. Methods and compounds useful for treating anemia, wherein the anemia treatment is associated with a lower risk of thrombosis or hypertension compared to that observed with rhEPO therapy, are provided. | 12-30-2010 |
20110015223 | Compounds and methods for treatment of cancer-related anemia - The invention relates to methods and compounds for treating anemia of cancer. In particular, methods for treating anemia of cancer in a subject having cancer, and methods for increasing reticulocytes, increasing hemoglobin, increasing hematocrit, and increasing red blood cell count in subjects having anemia of cancer, wherein such subjects are refractory to treatment with recombinant human erythropoietin (EPO) are encompassed herein. | 01-20-2011 |
20110034507 | FARNESOID X RECEPTOR AGONISTS - The present invention relates to farnesoid X receptors (FXR, NR1H4). FXR is a member of the nuclear receptor class of ligand-activate transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same. Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome. | 02-10-2011 |
20110039886 | Enhanced erythropoiesis and iron metabolism - The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease. | 02-17-2011 |
20110053975 | CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES - The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly. | 03-03-2011 |
20110130419 | NOVEL SALT OF ISOQUINOLINE COMPOUND AND CRYSTAL THEREOF - The invention provides a salt of (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one and a crystal thereof. (R)-3-[2-(2-Hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one monophosphate is a compound which is chemically stable, has high solubility, and shows less weight change due to humidity as compared to a free form and monohydrochloride dihydrate, and is superior as a bulk drug for pharmaceutical products. | 06-02-2011 |
20110130420 | ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - Isoquinolone derivatives of the general formula Ik″ are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia. | 06-02-2011 |
20110166178 | Methods for treating anemia using inhibitors of hypoxia-inducible factor (HIF) hydroxylase - The present invention relates to methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included. Compounds for use in these methods are provided, as are methods of identifying such compounds. | 07-07-2011 |
20110190339 | 6-SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES - The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds. | 08-04-2011 |
20110190340 | BI- AND POLYCYCLIC SUBSTITUTED ISOQUINOLINE AND ISOQUINOLINONE DERIVATIVES - The invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of the formula (I) wherein R | 08-04-2011 |
20110190341 | SUBSTITUTED ISOQUINOLINES AND ISOQUINOLINONES AS RHO KINASE INHIBITORS - The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds. | 08-04-2011 |
20110237621 | Macrocyclic Inhibitors of Hepatitis C Virus - Inhibitors of HCV replication of formula (I) | 09-29-2011 |
20110263642 | METHODS FOR TREATMENT OF MULTIPLE SCLEROSIS - The present invention relates to methods and compounds useful for treating multiple sclerosis. | 10-27-2011 |
20110263643 | 2,3-Disubstituted Piperidine Orexin Receptor Antagonists - The present invention is directed to 2,3-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved. | 10-27-2011 |
20110263644 | Compounds and Methods for Treatment of Stroke - The present invention relates to methods and agents useful for the treatment of stroke, including ischemic stroke and hemorrhagic stroke. In particular, methods and agents for treating stroke in a subject are provided, wherein the agent is administered prior to diagnosis of the stroke as an ischemic stroke or a hemorrhagic stroke. | 10-27-2011 |
20110288120 | ISOQUINOLINONE DERIVATIVES AS NK3 ANTAGONISTS - Isoquinolone derivatives of the general formula (I) are NK3 antagonists. | 11-24-2011 |
20120029011 | NOVEL NITROGEN-CONTAINING HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. | 02-02-2012 |
20120071503 | POSITIVE ALLOSTERIC MODULATORS OF GROUP II MGLURS - The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like. | 03-22-2012 |
20120088790 | PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY - The present invention relates to phenalkylamine derivatives of the formula (I) or (II) | 04-12-2012 |
20120208842 | Novel 1-(1-OXO-1,2,3,4-TETRAHYDROISOQUINOLIN-7-YL)Urea Derivatives As N-FORMYL Peptide Receptor Like-1 (FPRL-1) Receptor Modulators - The present invention relates to novel 1-(1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. | 08-16-2012 |
20120238601 | TREATMENT OF CANCER - The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions. | 09-20-2012 |
20120309786 | 3-AMINO-PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - Compounds represented by the general formula (I): | 12-06-2012 |
20120316198 | HYDRAZONE AND DIACYL HYDRAZINE COMPOUNDS AND METHODS OF USE - Disclosed herein are novel hydrazone and diacyl hydrazine derivatives that are inhibitors of the endoplasmic reticulum-associated protein degradation (ERAD) pathway. Also disclosed are hydrazone and diacyl hydrazine derivatives as potent and selective inhibitors of the p97 ATPase. These agents provide useful tools for the study of protein degradation and other processes involving p97. Methods of treating diseases or disorders for which p97 inhibition and/or ER stress induction is an effective treatment with certain hydrazone and diacyl hydrazine derivatives are also disclosed. | 12-13-2012 |
20130040988 | 3-AMINO-PYRIDINE DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - Compounds represented by the general formula (1): | 02-14-2013 |
20130065919 | SUBSTITUTED N-ALKYL AND N-ACYL TETRAHYDRO-ISOQUINOLINE DERIVATIVES, PREPARATION AND THERAPEUTIC USE THEREOF - The present disclosure relates to a series of substituted N-alkyl and N-acyl tetrahydro-isoquinoline derivatives of formula (I). | 03-14-2013 |
20130109715 | 6-Substituted isoquinolines and isoquinolinones | 05-02-2013 |
20130116277 | ALDO-KETO REDUCTASE SUBFAMILY 1C3 (AKR1C3) INHIBITORS - The present invention relates to a novel class of AKR1C3 inhibitors, to compositions containing them, to methods for their preparation, and to methods of use thereof. The AKR1C3 inhibitors may be useful in the treatment of, for example, prostate cancer, benign prostate hyperplasia (BPH), lung cancer, acne, seborrhea, hirsuitism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, uterine cancer, uterine fibroids, endometriosis, myeloma and leiomyoma. | 05-09-2013 |
20130116278 | ANTIMICROBIAL AGENTS - The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein R | 05-09-2013 |
20130131105 | HCV PROTEASE INHIBITORS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 05-23-2013 |
20130150403 | NUCLEAR RECEPTOR BINDING AGENTS - The present application relates to methods of treating, preventing, delaying the onset of, reducing the incidence of, or reducing the severity of hypertension and of a condition associated with cardiovascular disease | 06-13-2013 |
20130203805 | Methods for treating anemia using inhibitors of hypoxia-inducible factor (HIF) hydroxylase - The present invention relates to methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included. Compounds for use in these methods are provided, as are methods of identifying such compounds. | 08-08-2013 |
20130253005 | SMALL MOLECULE INHIBITORS OF USP1 DEUBIQUITINATING ENZYME ACTIVITY - Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents. | 09-26-2013 |
20130274286 | NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NMPRTase) INHIBITOR FOR GLIOMA THERAPY - The present invention relates to identification of a compound which inhibits the enzyme NMPRTase and glioma cancer cell growth and further used for glioma therapy. Pre-B-cell colony enhancing factor 1 gene (PBEF1) encodes nicotinamide phosphoribosyltransferase (NMPRTase), which catalyses the rate limiting step in the salvage pathway of NAD metabolism in mammalian cells. PBEF1 transcript and protein levels have been shown to be elevated in glioblastoma and a chemical inhibitor of NMPRTase has been shown to specifically inhibit cancer cells. Here a structure based drug discovery approach has been reported with an aim to develop novel inhibitors for glioblastoma therapy. Present invention relates to virtual screening using docking of ligands from a large library of 13,000 compounds against NMPRTase as the macromolecular target resulting in short listing of 34 possible ligands, of which six were tested experimentally, using the NMPRTase enzyme inhibition assay and further with the glioma cell viability assays. Of these, two compounds were found to be significantly efficacious in inhibiting the conversion of nicotinamide to NAD, and out of which one compound, 3-amino-2-benzyl-7-nitro-4-(2-quinolyl-)-1,2-dihydroisoquinolin-1-one, was found to inhibit the growth of a PBEF1 over expressing glioma derived cell line U87 also. | 10-17-2013 |
20130296363 | QUINOLINE AND ISOQUINOLINE DERIVATIVES FOR USE AS JAK MODULATORS - Provided herein are compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 11-07-2013 |
20130338187 | Novel 1-(1-OXO-1,2,3,4-TETRAHYDROISOQUINOLIN-7-YL)Urea Derivatives As N-FORMYL Peptide Receptor Like-1 (FPRL-1) Receptor Modulators - The present invention relates to novel 1-(1-Oxo-1,2,3,4-tetrahydroisoquinolin-7-yl)urea derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor. | 12-19-2013 |
20140024675 | CRYSTALLINE FORMS OF A PROLYL HYDROXYLASE INHIBITOR - The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof. | 01-23-2014 |
20140024676 | CRYSTALLINE FORMS OF A PROLYL HYDROXYLASE INHIBITOR - The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof. | 01-23-2014 |
20140057941 | Methods For Increasing Mean Corpuscular Volume - The invention relates to methods and compounds useful for treating deficiencies in hemoglobin production. Methods and compounds useful for increasing mean corpuscular volume are provided. Methods and compounds for treating microcytosis and methods and compounds for treating microcytic anemia are also provided. | 02-27-2014 |
20140142136 | Enhanced Erythropoiesis and Iron Metabolism - The present invention relates to methods and compounds for regulating or enhancing erythropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease. | 05-22-2014 |
20140148480 | USE OF COUMARIN DERIVATIVES FOR THE PREPARATION OF DRUGS FOR TREATING SKIN DISEASES - A compound of formula (I-1) | 05-29-2014 |
20140171465 | Methods For Increasing Reticulocyte Hemoglobin Content - The invention relates to methods and compounds useful for treating deficiencies in hemoglobin production. Methods and compounds useful for increasing reticulocyte hemoglobin content are provided. | 06-19-2014 |
20140275158 | CYCLOHEXYL ISOQUINOLINONE COMPOUNDS - The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof. | 09-18-2014 |
20140275159 | SUBSTITUTED 2-AZA-BICYCLO[2.2.2]OCTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C - This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 | 09-18-2014 |
20140275160 | COMBINATION THERAPY - Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt. | 09-18-2014 |
20140275161 | COMBINATION THERAPY - Described herein are compounds and compositions for treating glaucoma and/or reducing intraocular pressure. Compositions may comprise an isoquinoline compound and a prostaglandin or a prostaglandin analog. Compounds described herein include those in which an isoquinoline compound is covalently linked to a prostaglandin or a prostaglandin analog, and those in which an isoquinoline compound and a prostaglandin free acid together form a salt. | 09-18-2014 |
20140303202 | CRYSTALLINE FORMS OF A PROLYL HYDROXYLASE INHIBITOR - The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof. | 10-09-2014 |
20140309256 | Therapeutic Method - The present invention provides a method of treatment for anemia, or of increasing the hemoglobin level, in a subject without significantly increasing the platelet count during the course of treatment, by administering a compound that inhibits HIF prolyl hydroxylase. | 10-16-2014 |
20140323519 | HETEROCYCLIC COMPOUNDS AS B-RAF INHIBITORS FOR TREATMENT OF CANCER - This invention relates to novel heterocyclic compounds that are useful for treating cancer and other cellular proliferative diseases and/or disorders associated with B-Raf activity. The compounds of the invention may be illustrated by the Formula (I). (Formula (I)) | 10-30-2014 |
20140343094 | NOVEL NITROGEN-CONTAINING HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. | 11-20-2014 |
20150031721 | POLYMORPHIC FORMS OF COMPOUNDS AS PROLYL HYDROXYLASE INHIBITOR, AND USES THEREOF - The present invention relates to the polymorphic forms of the compound of Formula (I), preparation thereof including the preparation of intermediates and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder or a condition, or in the manufacturing of a medicament for the treatment of a disease, a disorder or a condition. | 01-29-2015 |
20150038528 | 4 -HYDROXY- ISOQUINOLINE COMPOUNDS AS HIF HYDROXYLASE INHIBITORS - The present invention relates to novel compounds of formula (I), and compositions capable of inhibiting PHD1 enzyme activity selectively over other isoforms, for example, PHD2 and/or PHD3 enzymes. The invention also relates to compounds of formula (I) for use in disorders such as muscle degeneration, colitis, IBD, and certain ischemias. | 02-05-2015 |
20150038529 | CRYSTALLINE FORMS OF A PROLYL HYDROXYLASE INHIBITOR - The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof. | 02-05-2015 |
20150353493 | OXIDISABLE PYRIDINE DERIVATIVES, THEIR PREPARATION AND USE AS ANTI-ALZHEIMER AGENTS - A compound of formula (I) in which the dotted lines indicate the presence of at least one double bond; n=0 to 4; R | 12-10-2015 |
20150359787 | TETRAHYDROISOQUINOLIN-1-ONE DERIVATIVE OR SALT THEREOF - To provide a pharmaceutical, in particular a compound which can be used as a therapeutic agent for irritable bowel syndrome (IBS). It was found that a tetrahydroisoquinolin-1-one derivative having an amide group at the 4-position or a pharmaceutically acceptable salt thereof has an excellent bombesin 2 (BB2) receptor antagonistic action. It is also found that the tetrahydroisoquinolin-1-one derivative is highly effective on bowel movement disorders. From the above, the tetrahydroisoquinolin-1-one derivative of the present invention is useful as a therapeutic agent for diseases associated with a BB2 receptor, in particular IBS. | 12-17-2015 |
20160002170 | CRYSTALLINE FORMS OF -ACETIC ACID - The present disclosure relates to crystalline forms of {[1-cyano-5-(4-chlorophenoxy)-4-hydroxy-isoquinoline-3-carbonyl]-amino}-acetic acid (Compound A), the process of preparing crystalline forms of Compound A, the pharmaceutical compositions containing them, and the methods of use thereof. | 01-07-2016 |
20160009653 | CYANOISOQUINOLINE COMPOUNDS AND METHODS OF USE THEREOF | 01-14-2016 |
20160090639 | Method for selection of hDIS3 PIN domain inhibitors and use of hDIS3 PIN domain inhibitors for cancer treatment - The present invention relates to a method for selection or screening of hDIS3 PIN domain inhibitors, yeast strain and cell line used in such methods It also relates to new therapeutic agents selected hDIS3 PIN domain inhibitors and uses thereof in the treatment of cancers having mutations inhDIS3 RNB domain, especially multiple myeloma. The invention also relates to composition comprising new therapeutic agent hDIS3 PIN domain inhibitor and method for inducing synthetic lethality in a cancer cell. | 03-31-2016 |
20160166519 | CHEMICAL MOLECULES THAT INHIBIT THE SLICING MECHANISM FOR TREATING DISEASES RESULTING FROM SPLICING ANOMALIES | 06-16-2016 |