Class / Patent application number | Description | Number of patent applications / Date published |
514228500 | Three or more ring hetero atoms in the polycyclo ring system | 89 |
20080207607 | Heterotricyclic metalloprotease inhibitors - The present invention relates generally to azatriocyclic containing pharmaceutical agents, and in particular, to azatricyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azatricyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors. | 08-28-2008 |
20080255106 | Novel 2-Phenyl-Imidazo[4,5-B]Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase for the Treatment of Dementia and Neurodegenerative Disorders - Compounds of formula I | 10-16-2008 |
20090099161 | Substituted Imidazoquinolines and Imidazonaphthyridines - Imidazoquinolines and imidazonaphthyridines with a substituent containing a functional group, e.g., an amide, sulfonamide, urea, or heterocyclyl group, at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed. | 04-16-2009 |
20090105233 | SERINE-THREONINE PROTEIN KINASE AND PARP MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules. | 04-23-2009 |
20090149452 | XANTHINE OXIDASE INHIBITOR - A compound represented by the following formula (I) is used as a xanthine oxidase inhibitor: in which R | 06-11-2009 |
20090239854 | Tetracyclic compounds - This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 09-24-2009 |
20090258867 | PYRAZOLO[1,5-A] PYRIMIDINE COMPOUNDS AS CB1 RECEPTOR ANTAGONIST - The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R | 10-15-2009 |
20090264423 | SERINE-THREONINE PROTEIN KINASE AND PARP MODULATORS - The invention relates in part to molecules having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. Molecules of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such molecules. | 10-22-2009 |
20090275569 | Benzotriazine Inhibitors of Kinases - The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases. | 11-05-2009 |
20090325945 | IMIDAZO[4, 5-B]PYRIDIN-2-ONE AND OXAZOLO[4, 5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS CANCER THERAPEUTIC COMPOUNDS - The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: wherein: J is independently —O— or —NR | 12-31-2009 |
20100022522 | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 01-28-2010 |
20100029627 | MTKI QUINAZOLINE DERIVATIVES - The present invention concerns the compounds of formula | 02-04-2010 |
20100048544 | PYRROLO (3, 2, 1-IJ) QUINOLINE-4-ONE-DERIVATIVES FOR TREATING TUBERCULOSIS - Tricyclic nitrogen-containing compounds of Formula (I) or pharmaceutically acceptable salts and/or N-oxides thereof: | 02-25-2010 |
20100063038 | Substituted 4-Amino-Pyrrolotriazine Derivatives Useful for Treating Hyper-Proliferative Disorders and Diseases Associated with Angiogenesis - This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients. | 03-11-2010 |
20100093714 | AMIDES OF THIENO[2,3-d]PYRIMIDINE AND THEIR USE AS ADENOSINE A2a RECEPTOR ANTAGONISTS - This invention relates to a novel thieno[2,3-d]pyrimidine, A, and its therapeutic and prophylactic uses, wherein R | 04-15-2010 |
20100113436 | DISPIRO TETRAOXANE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MALARIA AND/OR CANCER - A compound having the formula (I) wherein ring A represents a substituted or unsubstituted monocyclic or multicyclic ring; m=any positive integer; n=0-5; X=CH and Y=—C(O)NR | 05-06-2010 |
20100125068 | METHODS FOR INHIBITING PROTEIN KINASES - The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds. | 05-20-2010 |
20100152174 | MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI - The present invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C | 06-17-2010 |
20100197674 | OXOPYRAZINE DERIVATIVE AND HERBICIDE - The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. | 08-05-2010 |
20100249119 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocyclic compound having a strong Raf inhibitory activity, which is represented by the following formula | 09-30-2010 |
20100249120 | SUBSTITUTED PYRAZOLO-PYRROLO-PYRIDINE-DIONE COMPOUNDS - The present invention relates to substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted pyrazolo-pyrrolo-pyridine-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof. | 09-30-2010 |
20100273786 | TETRAHYDRO-IMIDAZ0[1,5-A]PYRAZINE DERIVATIVES, PREPARATION PROCESS AND MEDICINAL USE THEREOF - Tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I), their preparation methods, pharmaceutical compositions containing the derivatives and uses thereof as medicaments, especially as dipeptidyl peptidase IV inhibitors, wherein the substituents of formula (I) are defined as same as the description. | 10-28-2010 |
20100280021 | PYRIDOPYRIMIDINE PROTEIN TYROSINE PHOSPHATASE INHIBITORS - The present invention comprises pyridopyrimidinediamine compounds of the general formula I: | 11-04-2010 |
20100305113 | Substituted Imidazopyridazines as Lipid Kinase Inhibitors - The invention relates to novel compounds of the formula I, | 12-02-2010 |
20100305114 | Heterocyclic Aromatic Compounds Useful As Growth Hormone Secretagogues - Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I | 12-02-2010 |
20100331319 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. | 12-30-2010 |
20110021511 | SUBSTITUTED 5H-PYRIMIDO[5,4-B]INDOLES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF FOR TREATING NON-SOLID MALIGNANT TUMORS OF THE BLOOD-PRODUCING SYSTEM - The invention relates to compounds of general formula 1 | 01-27-2011 |
20110053920 | SUBSTITUTED BICYCLIC PYRIMIDINES - The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted heterobicyclic pyrimidines of Formula (I): | 03-03-2011 |
20110118246 | Novel Compounds - The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity. | 05-19-2011 |
20110124634 | BIOACTIVE COMPOUNDS FOR TREATMENT OF CANCER AND NEURODEGENERATIVE DISEASES - The invention provides bioactive compounds for the treatment of various malconditions such as cancer and neurodegenerative diseases including Alzheimer's disease. The chemical compounds as disclosed herein are found to show bioactivity in bioassays related to these conditions. Pharmaceutical compositions, combinations and methods of synthesis are provided, as are methods of using the compound, compositions and combinations in the treatment of the diseases. | 05-26-2011 |
20110152254 | SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 06-23-2011 |
20110172216 | PYRAZOLOPYRIMIDINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 07-14-2011 |
20110172217 | RING-FUSED MORPHOLINE DERIVATIVE HAVING PI3K-INHIBITING ACTIVITY - The present invention provides compounds or a pharmaceutically acceptable salt thereof which inhibit the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and are therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused morpholine compound shown in the present specification, or a pharmaceutically acceptable salt thereof. | 07-14-2011 |
20110190281 | SULFONE SUBSTITUTED 2,3-DIHYDROIMIDAZO [1,2-C] QUINAZOLINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES WITH ANGIOGENESIS - This invention relates to novel sulfone 2I3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients. | 08-04-2011 |
20110224199 | Heterocyclic Aromatic Compounds Useful As Growth Hormone Secretagogues - Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I | 09-15-2011 |
20110237574 | USE OF MODIFIED PYRIMIDINE COMPOUNDS TO PROMOTE STEM CELL MIGRATION AND PROLIFERATION - This invention provides cells and methods for stimulating proliferation and migration of endogenous and exogenous mammalian stem cells in vivo and in vitro. The invention provides reagents and methods for efficiently proliferating mammalian stem cells in an animal in need thereof and producing stem cells that can be re-introduced into an animal in need thereof to alleviate neurological and corporal disorders. | 09-29-2011 |
20110237575 | INHIBITORS OF FATTY ACID BINDING PROTEIN (FABP) - The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (“FABP”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the present invention is shown below: (I) | 09-29-2011 |
20110294796 | BENZOTRIAZINE INHIBITORS OF KINASES - The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases. | 12-01-2011 |
20120058997 | IMIDAZO[1,2-B]PYRIDAZINE AND PYRAZOLO[1,5-A]PYRIMIDINE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of the following structure (I) and (II): | 03-08-2012 |
20120094987 | SUBSTITUTED PYRIDO [3', 2': 4, 5] THIENO [3, 2-D] PYRIMIDINES AND PYRIDO [3', 2': 4, 5] FURO [3, 2-D] PYRIMIDINES USED AS INHIBITORS OF THE PDE-4 AND/OR THE RELEASE OF TNF-alpha - The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNFα-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes. | 04-19-2012 |
20120142678 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. | 06-07-2012 |
20120178744 | FUSED TRICYCLIC COMPOUNDS AS NOVEL mTOR INHIBITORS - The present invention provides Fused Tricyclic Compounds of the Formula (I) wherein Q, R | 07-12-2012 |
20120252799 | HETEROCYCLIC AROMATIC COMPOUNDS USEFUL AS GROWTH HORMONE SECRETAGOGUES - Novel heterocyclic aromatic compounds are provided that are useful in stimulating endogenous production or release of growth hormone, said compounds having the general structure of formula I | 10-04-2012 |
20120264747 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 10-18-2012 |
20120270866 | 8-ETHYL-6-(ARYL)PYRIDO[2,3-D]PYRIMIDIN-7(8H)-ONES FOR THE TREATMENT OF CNS DISORDERS - Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders. | 10-25-2012 |
20120289501 | Benzene-fused 6-membered oxygen-containing heterocyclic derivatives of bicyclic heteroaryls - The invention relates to new derivatives of formula I, wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a proliferative disease. | 11-15-2012 |
20130035332 | Substituted 1,3-Benzothiazol-2(3H)-Ones and [1,3]Thiazolo[5,4-B]Pyridin-2(IH)-Ones as Positive Allosteric Modulators of MGLUR2 - The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved. | 02-07-2013 |
20130053376 | NOVEL TYROSINE KINASE INHIBITORS - Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use. | 02-28-2013 |
20130131054 | TETRACYCLIC COMPOUNDS - This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 05-23-2013 |
20130137681 | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS - The present invention provides heteroaryl substituted pyrrolo[2,3-b]pyridines and heteroaryl substituted pyrrolo[2,3-b]pyrimidines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases. | 05-30-2013 |
20130150353 | Fused Tricyclic Inhibitors of Mammalian Target of Rapamycin - This invention relates to novel fused tricyclic compounds that are inhibitors of mammalian Target of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP, and are useful in the treatment of cellular proliferative diseases, for example cancer and other proliferative disorders. | 06-13-2013 |
20130190304 | TETRACYCLIC COMPOUNDS - This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-25-2013 |
20130203746 | TETRACYCLIC COMPOUNDS - This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 08-08-2013 |
20130210815 | SUBSTITUTED IMIDAZOPYRAZINES - The present invention relates to substituted imidazopyrazine compounds of general formula (I) in which A, R | 08-15-2013 |
20130210816 | FUSED-IMIDAZOYL COMPOUNDS USEFUL AS ANTIMICROBIAL AGENTS - The invention relates to fused-imidazoyl compounds of Formula (I): wherein ring A, R | 08-15-2013 |
20130237533 | CDK Inhibitors - Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. | 09-12-2013 |
20130237534 | CDK INHIBITORS - Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. | 09-12-2013 |
20130289028 | HETEROCYCLIC FUSED ANTHRAQUINONE DERIVATIVES, MANUFACTURING METHOD AND PHARMACEUTICAL COMPOSITION USING THEREOF - A heterocyclic fused anthraquinone derivatives, which is represented by a formula (I): | 10-31-2013 |
20130289029 | Fused Ring Compound For Use As Mineralocorticoid Receptor Antagonist - The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y | 10-31-2013 |
20130296312 | Preparation and Uses of 1,2,4-Triazolo [1,5a] Pyridine Derivatives - This application relates, in part, to compounds of the general Formula I | 11-07-2013 |
20130345209 | AMINOTRIAZOLOPYRIDINE FOR USE IN THE TREATMENT OF INFLAMMATION, AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to the compound according to Formula I, and to its use in medicine, in particular in the treatment of inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons. In particular, the compound inhibits JAK a family of tyrosine kinases, and more particularly JAK1. The present invention also provides pharmaceutical compositions comprising the compound, methods for the prophylaxis and/or treatment of diseases involving inflammatory conditions, autoimmune diseases, proliferative diseases, allergy, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons by administering the compound. | 12-26-2013 |
20140005183 | Novel 4-(Substituted Amino)-7H-Pyrrolo[2,3-d] Pyrimidines As LRRK2 Inhibitors | 01-02-2014 |
20140045829 | SUBSTITUTED 1,3-BENZOTHIAZOL-2(3H)-ONES AND [1,3]THIAZOLO[5,4-B]PYRIDIN-2(1H)-ONES AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 - The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved. | 02-13-2014 |
20140073635 | Substituted Imidazopyridinyl-Aminopyridine Compounds - The present invention relates to substituted imidazopyridinyl-aminopyridine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazopyridinyl-aminopyridine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 03-13-2014 |
20140100220 | NOVEL COMPOUND USEFUL FOR THE TREATMENT OF DEGENERATIVE AND INFLAMMATORY DISEASES - A novel compound able to inhibit JAK is disclosed, this compound may be prepared as a pharmaceutical composition, 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, inflammatory conditions, autoimmune diseases, proliferative diseases, transplantation rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6. | 04-10-2014 |
20140128382 | 5-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO- AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE - The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and uses, including Alzheimer's disease, are also disclosed. | 05-08-2014 |
20140194414 | TETRACYCLIC COMPOUNDS - This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. | 07-10-2014 |
20140200213 | 2-SPIRO-SUBSTITUTED IMINOTHIAZINES AND THEIR MONO-AND DIOXIDES AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE - In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): | 07-17-2014 |
20140256714 | MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI - The present invention concerns the compounds of formula | 09-11-2014 |
20140329807 | HETEROCYCLIC PROTEIN KINASE INHIBITORS - The present invention provides protein kinase having one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R | 11-06-2014 |
20140343047 | TETRANDRINE DERIVATIVES WITH SUBSTITUTED 5-CARBON, PREPARATION METHOD AND USE THEREOF - The present invention belongs to the field of natural medicine and pharmaceutical chemistry and specifically relates to novel 5-substituted tetrandrine derivatives of formula (I) and a pharmaceutically acceptable adduct, complex and salt thereof, to a process for the preparation of these compounds, pharmaceutical compositions containing such compounds and their use in preparing antineoplastic medicaments. | 11-20-2014 |
20140350002 | IMIDAZOPYRIDIN-2-ONE DERIVATIVES - The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR | 11-27-2014 |
20150011539 | NOVEL TYROSINE KINASE INHIBITORS - Provided are compounds of the formula (I): | 01-08-2015 |
20150025065 | NEW AZABENZIMIDAZOLE DERIVATIVES - The present invention relates to compounds of general formula I, | 01-22-2015 |
20150031689 | PERIPHERALLY RESTRICTED DIPHENYL PURINE DERIVATIVES - The invention provides compounds capable of acting as antagonists at cannabanoid receptors according to the following formula: Such compounds may be used to treat conditions for which the cannabinoid receptor system has been implicated, such as obesity, liver disease, diabetes, pain, and inflammation. | 01-29-2015 |
20150072979 | METHODS AND COMPOSITIONS FOR TREATING VIRAL INFECTIONS - The present invention provides compositions and methods for treating, preventing, and inhibiting viral replication, viral infections and viral diseases and disorders, comprising the use of artemisinin derivatives having anti-viral activity. | 03-12-2015 |
20150126500 | PIPERAZINYL PYRIMIDINE DERIVATIVES, PREPARATION METHOD AND USE THEREOF - Provided are piperazinyl pyrimidine derivatives of formula I having CCR | 05-07-2015 |
20150126501 | Fused Ring Compound For Use As Mineralocorticoid Receptor Antagonist - The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y | 05-07-2015 |
20150315207 | Novel Heterocyclic Compound Classes for Signaling Modulation - The invention relates to compounds of Formulas I-VII (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating cellular signaling pathways and biological processes associated therewith including inhibition of kinase activity such as PI-3 kinase or inhibition of bromodomain proteins or both at the same time as well as to therapeutic methods for treating a disease associated with aberrant PI3K and/or bromodomain proteins. | 11-05-2015 |
20160024089 | TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS - A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R | 01-28-2016 |
20160060258 | 2-AMINOPYRIDO[4,3-D]PYRIMIDIN-5-ONE DERIVATIVES AND THEIR USE AS WEE-1 INHIBITORS - The present invention relates to compounds of formula (I) that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer. | 03-03-2016 |
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