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公开(公告)号:US20210163472A1
公开(公告)日:2021-06-03
申请号:US16770673
申请日:2018-12-12
Inventor: Gianpaolo BRAVI , Heather HOBBS , Graham George Adam INGLIS , Simon NICOLLE , Simon PEACE
IPC: C07D471/04 , A61P11/00 , C07D519/00
Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, L and A are as defined in the description and claims, or pharmaceutically acceptable salts thereof having mTOR kinase inhibitor activity. The invention also relates to pharmaceutical compositions including a compound of formula (I) or a pharmaceutically acceptable salt thereof, and to the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an mTOR kinase inhibitor activity is indicated, and in particular the treatment of idiopathic pulmonary fibrosis.
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公开(公告)号:US20210130339A1
公开(公告)日:2021-05-06
申请号:US16480839
申请日:2018-01-19
Inventor: Feng REN , Yingxia SANG , Baowei ZHAO
IPC: C07D413/14 , C07D405/14
Abstract: Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).
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公开(公告)号:US20210108227A1
公开(公告)日:2021-04-15
申请号:US17047730
申请日:2019-04-16
Inventor: Christopher HERRING
IPC: C12N15/86 , C12N7/02 , C07K14/245
Abstract: Provided is a cell containing a nucleic acid sequence having a parvovirus terminal repeat sequence, wherein the cell overexpresses single strand binding protein compared to a cell of a wild-type (WT) strain of the same species. Also provided is a nucleic acid vector containing a nucleic acid sequence having a parvovirus terminal repeat sequence and a nucleic acid sequence encoding a single strand binding protein. Methods of using said nucleic acid vector to propagate and purify nucleic acid vectors involved in the production of parvovirus vector particle production are also described.
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公开(公告)号:US10975081B2
公开(公告)日:2021-04-13
申请号:US15746817
申请日:2016-07-22
Inventor: Xiao Ding , Yun Jin , Qian Liu , Feng Ren , Yingxia Sang , Luigi Piero Stasi , Zehong Wan , Hailong Wang , Weiqiang Xing , Yang Zhan , Baowei Zhao
IPC: C07D487/04 , A61P25/28 , A61P25/16 , A61K31/5377
Abstract: Disclosed are substituted fused pyrazoles, for example substituted indazoles, that inhibit LRRK2 kinase activity, pharmaceutical compositions containing them and their use in the treatment of Parkinson's disease.
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公开(公告)号:US20210047299A1
公开(公告)日:2021-02-18
申请号:US16963539
申请日:2019-01-23
IPC: C07D403/12 , A61P33/06
Abstract: The present invention relates to novel compounds or pharmaceutically acceptable salts thereof, corresponding compositions, and methods and/or uses in therapy, for example in the treatment of parasitic infections such as malaria, in particular infection by Plasmodium falciparum.
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公开(公告)号:US10906924B2
公开(公告)日:2021-02-02
申请号:US16618537
申请日:2018-06-27
Inventor: Martha Alicia De La Rosa , Hongfeng Deng , Ghotas Evindar , Wieslaw Mieczyslaw Kazmierski , John Franklin Miller , Vicente Samano , Yoshiaki Washio , Bing Xia
IPC: C07F9/6561 , C07D491/107 , C07D491/20
Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
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公开(公告)号:US10899716B2
公开(公告)日:2021-01-26
申请号:US16778206
申请日:2020-01-31
Inventor: Niall Andrew Anderson , Deepak Bandyopadhyay , Alain Claude-Marie Daugan , Frederic G. Donche , Patrick M. Eidam , Nicolas Eric Faucher , Nicolas S. George , Philip Anthony Harris , Jae U. Jeong , Bryan W. King , Clark A. Sehon , Gemma Victoria White , David Duff Wisnoski
IPC: A61K31/4439 , C07D401/06 , C07D231/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D405/04 , C07D405/06 , C07D409/14 , C07D417/14 , C07D403/04 , C07D487/04 , A61P21/00 , A61K31/415 , A61K31/422 , A61K31/454 , A61K31/4545 , A61K31/506 , A61K31/5377 , C07D403/06 , C07D409/06 , C07D413/04
Abstract: Disclosed are compounds having the formula: wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.
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公开(公告)号:US20210017212A1
公开(公告)日:2021-01-21
申请号:US17063947
申请日:2020-10-06
Inventor: Michael Joseph BISHOP , Vincent J. Colandrea , Yuehu Li , Eugene L. Stewart , Iulia Strambeanu , Katherine Louisa Widdowson , James Walter Janetka , Laurel Kathryn Mcgrane
IPC: C07H7/04
Abstract: Disclosed herein are new C-mannoside compounds and compositions and their application as pharmaceuticals for the treatment of human disease. Methods of inhibition of FimH activity in a human subject are also provided for the treatment diseases such as urinary tract infection.
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公开(公告)号:US10787509B2
公开(公告)日:2020-09-29
申请号:US15987942
申请日:2018-05-24
Inventor: Steven Grant , Martin Orecchia , Chika Akinseye , Laura Hook , Alan Lewis , Tejinder Bhinder
IPC: A61K39/395 , C07K16/24 , C07K14/54 , A61K39/00
Abstract: The present disclosure relates to compositions, for treating interleukin 5 (IL-5) mediated diseases, and related methods.
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公开(公告)号:US20200297710A1
公开(公告)日:2020-09-24
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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