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1. 发明申请

WO2019215341A1 FURIN INHIBITORS 审中-公开
公开(公告)号：WO2019215341A1
公开(公告)日：2019-11-14
申请号：PCT/EP2019/062098
申请日：2019-05-10
申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人： AXTEN, Jeffrey Michael , CHEUNG, Mui , DEMARTINO, Michael P. , GUAN, Huiping Amy , HU, Yan , MILLER, Aaron Bayne , QIN, Donghui , WU, Chengde , ZHANG, Zhiliu , LIN, Xiaojuan
IPC分类号： C07D401/14 , A61K31/44 , A61K31/4427 , C07D213/76 , C07D401/04 , C07D413/12
摘要： This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.

2. 发明申请

WO2019021208A1 INDAZOLE DERIVATIVES USEFUL AS PERK INHIBITORS 审中-公开
公开(公告)号：WO2019021208A1
公开(公告)日：2019-01-31
申请号：PCT/IB2018/055548
申请日：2018-07-25
申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人： AXTEN, Jeffrey Michael , KRISTAM, Rajendra , VENKATESHAPPA, Chandregowda
IPC分类号： A61K31/519 , C07D487/04 , A61P25/28
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , A61P25/28
摘要： The invention is directed to substituted indazole derivatives and uses thereof. Specifically, the invention is directed to compounds according to Formula I and the use of compounds of Formula (I) in treating disease states (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , are as defined herein; or a salt thereof including a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, spinal cord injury, traumatic brain injury, ischemic stroke, stroke, Parkinson disease, diabetes, metabolic syndrome, metabolic disorders, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, fatal familial insomnia, Gerstmann-Straussler-Scheinker syndrome, and related prion diseases, amyotrophic lateral sclerosis, progressive supranuclear palsy, myocardial infarction, cardiovascular disease, inflammation, organ fibrosis, chronic and acute diseases of the liver, fatty liver disease, liver steatosis, liver fibrosis, chronic and acute diseases of the lung, lung fibrosis, chronic and acute diseases of the kidney, kidney fibrosis, chronic traumatic encephalopathy (CTE), neurodegeneration, dementias, frontotemporal dementias, tauopathies, Pick's disease, Neimann-Pick's disease, amyloidosis, cognitive impairment, atherosclerosis, ocular diseases, neurological disorders, pain, arrhythmias, in organ transplantation and in the transportation of organs for transplantation. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

3. 发明申请

WO2018225093A1 CHEMICAL COMPOUNDS AS ATF4 PATHWAY INHIBITORS 审中-公开
公开(公告)号：WO2018225093A1
公开(公告)日：2018-12-13
申请号：PCT/IN2018/050375
申请日：2018-06-07
申请人： GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
发明人： AXTEN, Jeffrey Michael , DEMARTINO, Michael P. , EVANS, Karen Anderson , RALPH, Jeffrey M , KALITA, Biswajit
IPC分类号： C07D233/36 , C07C233/41 , C07D305/08 , C07D213/65 , A61K31/4166 , A61K31/337 , A61K31/44 , A61K31/165 , A61P35/00 , A61P25/00 , A61P9/00 , A61P3/00 , A61P27/00 , A61P29/00 , C07D311/58
CPC分类号： C07D213/65 , A61K31/4015 , A61K31/4412 , A61K31/4439 , A61K45/06 , A61P3/00 , A61P9/00 , A61P25/00 , A61P27/00 , A61P29/00 , A61P35/00 , C07C233/41 , C07C235/22 , C07C235/40 , C07C237/10 , C07C2601/02 , C07C2602/06 , C07C2602/10 , C07C2602/38 , C07C2602/40 , C07C2602/44 , C07D205/04 , C07D207/12 , C07D207/273 , C07D209/44 , C07D211/14 , C07D211/46 , C07D233/36 , C07D241/08 , C07D295/135 , C07D305/08 , C07D307/85 , C07D311/58 , C07D401/12 , A61K2300/00
摘要： The invention is directed to substituted bridged cycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula (IIIQ): wherein X 6' , a, b, C 8' , D 8' , L 82' , L 83' , R 81' , R 82' , R 83' , R 84' , R 85' , R 86' , z 82' , z 84' , z 85' , and z 86' are as defined herein; or salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway. Accordingly, invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting the ATF4 pathway and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

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