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公开(公告)号:US11203632B2
公开(公告)日:2021-12-21
申请号:US15749210
申请日:2016-07-29
Inventor: Valeriu Damian , Austin Keith Doyle , Laura Maria Halo , Emma R. Harding , Xuan Hong , Alan Peter Lewis , Mark Uden
Abstract: The present invention relates to methods of selecting, screening, engineering, making and modifying antibodies that have improved bioavailability upon subcutaneous administration to a human. Antibodies and variant antibodies with improved bioavailability upon subcutaneous administration to a human are also described.
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公开(公告)号:US11197857B2
公开(公告)日:2021-12-14
申请号:US16464439
申请日:2017-11-30
Inventor: Olena I. Barbash , Andy Fedoriw , Sarah Gerhart , Ryan G. Kruger , Jenny Laraio , Helai Mohammad , Shane W. Obrien , Jacob Rubin , Niyant Shah , Ping Zhang
IPC: A61K31/415 , A61K31/506 , A61P35/04
Abstract: The present invention provides a combination of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and a Type II protein arginine methyltransferase (Type II PRMT) inhibitor. The present invention also provides methods for treating cancer in a human in need thereof, the methods comprising administering to the human a combination of a Type I PRMT inhibitor and a Type II PRMT inhibitor, together with at least one of: a pharmaceutically acceptable carrier and a pharmaceutically acceptable diluent, thereby treating the cancer in the human. The present invention further provide a pharmaceutical composition comprising a therapeutically effective amount of a Type I PRMT inhibitor and a second pharmaceutical composition comprising a therapeutically effective amount of a Type II PRMT inhibitor.
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公开(公告)号:US20210347902A1
公开(公告)日:2021-11-11
申请号:US17346974
申请日:2021-06-14
Inventor: Tejinder Kaur BHINDER , Chong DING , Xu FENG , Wenqing JIANG , Alan Peter LEWIS , Yingli MA , Guhan NAGAPPAN , Radha Shah PARMAR , Yangsheng QIU , Liuqing YANG , Qing ZHANG , Yanjiao ZHOU
Abstract: The present invention relates to TrkB binding agonists, and to the use of such agonists in the treatment of neurological disorders and other disorders. The present invention also relates to specific TrkB binding agonists comprising CDRs, variable regions, heavy and light chains, and variant sequences thereof.
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公开(公告)号:US11117905B2
公开(公告)日:2021-09-14
申请号:US16467193
申请日:2017-12-11
IPC: A61K8/00 , A61K9/00 , C07D243/08 , C07D281/02 , C07D291/08 , C07D513/04 , C07D515/04 , C07D285/36 , C07D409/14
Abstract: The present invention relates to bisaryl heterocycle compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to bisaryl heterocycles of Formula (I),
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公开(公告)号:US20210260033A1
公开(公告)日:2021-08-26
申请号:US17052817
申请日:2019-05-24
Inventor: Andrew Mark FEDORIW , Susan KORENCHUK , Helai MOHAMMAD , Christian S. SHERK
IPC: A61K31/415 , C07K16/28 , A61K39/395 , A61K9/00 , A61P35/00 , A61P35/02
Abstract: The present disclosure provides a method of treating cancer in a human in need thereof, the method comprising administering to the human a therapeutically effective amount of a Type I protein arginine methyltransferase (Type I PRMT) inhibitor and administering to the human a therapeutically effective amount of an ICOS (CD278), Inducible T-cell Costimulator) binding protein or antigen binding portion thereof.
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公开(公告)号:US20210253532A1
公开(公告)日:2021-08-19
申请号:US17156478
申请日:2021-01-22
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: C07D231/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D401/06 , 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:US20210253528A1
公开(公告)日:2021-08-19
申请号:US16973587
申请日:2019-07-08
Inventor: Michael P. DEMARTINO , Karen Anderson EVANS , Israil PENDRAK , Joseph E. PERO
IPC: C07D213/64 , C07C271/28 , C07C275/30 , C07C235/20 , C07D207/273 , A61K45/06 , A61K31/506
Abstract: The invention is directed to substituted carbon-linked bicycloalkane derivatives. Specifically, the invention is directed to compounds according to Formula (X): wherein C′, D′, L2′, L3′, R2′, R3′, R4′, R5′, R6′, R7′, R8′, z2′, z3′, z4′, z5′, z6′, X1, and X2 are as defined herein; or a salt thereof including a pharmaceutically acceptable salt 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, 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 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:US20210238162A1
公开(公告)日:2021-08-05
申请号:US16062223
申请日:2016-12-15
Inventor: Rodolfo CADILLA , David Norman DEATON , Ashley Paul HANCOCK , Heather HOBBS , Simon Teanby HODGSON , Andrew L. LARKIN , Joelle LE , Paul N. MORTENSON , Daniel J. PRICE , Gordon SAXTY , Lee T. SCHALLER , Christie SCHULTE , Ian Edward David SMITH , Stephen Andrew THOMSON , Joseph Wendell WILSON
IPC: C07D401/14 , C07D401/12 , C07D215/54 , C07D417/12 , C07D405/12 , C07D413/12 , C07D413/14 , C07D491/056 , C07D491/048 , A61P21/00 , A61P11/06
Abstract: The present invention relates to compounds of Formula (XI): wherein R1a, R2a, R3a, R4a, R5a, R6a, and Aa are as defined herein, and pharmaceutically acceptable salts thereof. The compounds of the present invention are inhibitors of hematopoietic prostaglandin D synthase (H-PGDS) inhibitors and can be useful in the treatment of Duchenne Muscular Dystrophy. 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 H-PGDS activity 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:US11078216B2
公开(公告)日:2021-08-03
申请号:US16467538
申请日:2017-12-11
Inventor: James Francis Callahan , Vincent J. Colandrea , Anthony William James Cooper , Nicole Cathleen Goodwin , Chelsea Ariane Huff , Joel Karpiak , Jeffrey K. Kerns , Hong Nie
IPC: A61K31/554 , A61K31/553 , A61P1/16 , A61P9/00 , A61P11/00 , A61P11/06 , A61P13/12 , A61P17/06 , A61P35/00 , C07D281/02 , C07D417/06 , C07D417/12 , C07D417/14 , C07D419/06 , C07D419/12 , C07D419/14 , C07D513/04 , C07D515/04 , C07D401/14
Abstract: The present invention relates to bisaryl amide analogs, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to bisaryl heterocycles of Formula (I),
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公开(公告)号:US11072591B2
公开(公告)日:2021-07-27
申请号:US16639163
申请日:2018-08-16
IPC: C07D257/04 , C07D403/06 , C07D401/06 , C07D405/06 , C07D249/06 , A61P31/06 , A61K45/06
Abstract: The invention relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by Mycobacterium, such as tuberculosis.
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