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公开(公告)号：US11773078B2
公开(公告)日：2023-10-03
申请号：US17054491
申请日：2019-05-10
Inventor： Jeffrey Michael Axten , Mui Cheung , Michael P. Demartino , Huiping Amy Guan , Yan Hu , Aaron Bayne Miller , Donghui Qin , Chengde Wu , Zhiliu Zhang , Xiaojuan Lin
IPC: C07D401/12 , C07D401/14 , A61P11/00 , C07D211/26 , C07D487/08
CPC classification number: C07D401/14 , A61P11/00 , C07D211/26 , C07D401/12 , C07D487/08
Abstract: 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.
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公开(公告)号：US11547704B2
公开(公告)日：2023-01-10
申请号：US16898667
申请日：2020-06-11
Inventor： Jeffrey Michael Axten , Mui Cheung , Michael P. Demartino , Hilary Schenck Eidam , Raghava Reddy Kethiri , Biswajit Kalita
IPC: A61K31/4468 , A61K31/438 , A61K31/439 , A61K31/445 , A61K31/454 , C07D211/32 , C07D211/58 , C07D211/66 , C07D403/12 , C07D417/12 , C07D471/08 , C07D498/10 , C07D211/26 , C07D211/60 , C07D401/04 , C07D211/56 , C07D211/62 , C07D401/12 , C07D209/52 , C07D405/12 , C07D451/04
Abstract: The invention is directed to substituted piperidine derivatives. Specifically, the invention is directed to compounds according to Formula IIII: wherein A, B, X, Y, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, z2, z4, z5, and z6 are as defined herein, and salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway 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, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, 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 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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公开(公告)号：US20220315556A1
公开(公告)日：2022-10-06
申请号：US17054491
申请日：2019-05-10
Inventor： Jeffrey Michael Axten , Mui Cheung , Michael P. Demartino , Huiping Amy Guan , Yan Hu , Aaron Bayne Miller , Donghui Qin , Chengde Wu , Zhiliu Zhang , Xiaojuan Lin
IPC: C07D401/14 , A61P11/00 , C07D401/12 , C07D211/26 , C07D487/08
Abstract: 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.
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公开(公告)号：US10851053B2
公开(公告)日：2020-12-01
申请号：US16307513
申请日：2017-06-07
Inventor： Jeffrey Michael Axten , Mui Cheung , Anthony William Dean , Michael P. DeMartino , Hilary Schenck Eidam , Biswajit Kalita , Raghava Reddy Kethiri , Rajendra Kristam
IPC: A61K31/403 , A61K31/4025 , A61K31/4015 , A61K31/44 , A61K31/4439 , C07D209/52 , C07D207/26 , C07D207/09 , C07D401/06 , C07D401/12 , C07D401/14 , A61P25/28 , A61P25/00 , A61P35/00 , C07D487/10 , C07D405/06 , C07D405/12 , C07D487/04
Abstract: The invention is directed to substituted pyrrolidine derivatives. Specifically, the invention is directed to compounds according to Formula III: wherein A, B, L1, L2, L3, R1, R2, R3, R4, R5, R6, R9, R10, R30, Y1, Y2, z2, z4, z5, and z6 are as defined herein, and salts thereof. The compounds of the invention are inhibitors of the ATF4 pathway 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, diabetes, Parkinson disease, Huntington's disease, Creutzfeldt-Jakob Disease, and related prion diseases, progressive supranuclear palsy, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, inflammation, fibrosis, chronic and acute diseases of the liver, chronic and acute diseases of the lung, chronic and acute diseases of the kidney, chronic traumatic encephalopathy (CTE), neurodegeneration, dementia, cognitive impairment, atherosclerosis, ocular diseases, 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 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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