公开(公告)号：US20240317767A1

公开(公告)日：2024-09-26

申请号：US18670264

申请日：2024-05-21

申请人： AstraZeneca AB

发明人： Johan Olof BRODDEFALK ,  Hans Fredrik EMTENÂS ,  Kenneth Lars GRANBERG ,  Malin Anita LEMURELL ,  Daniel Tor PETTERSEN ,  Alleyn Thomas PLOWRIGHT ,  Lars Johan Andreas ULANDER

IPC分类号： C07D487/04 ,  A61K31/4155 ,  A61K31/4985 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  C07D231/40 ,  C07D231/44 ,  C07D231/50 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04

CPC分类号： C07D487/04 ,  A61K31/4155 ,  A61K31/4985 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  C07D231/40 ,  C07D231/44 ,  C07D231/50 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04

摘要： The present application relates to novel compounds of formula (I)




to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.

公开(公告)号：US20240018113A1

公开(公告)日：2024-01-18

申请号：US18372771

申请日：2023-09-26

申请人： Astellas Pharma, Inc. ,  Mitobridge, Inc.

发明人： Junko Maeda ,  Ikumi Kuriwaki ,  Kai Kitamura ,  Yumi Yamashita ,  Kenichi Kakefuda ,  Akio Kamikawa ,  Kenji Negoro ,  Wataru Hamaguchi ,  Ryushi Seo ,  Jeffrey Ciavarri

IPC分类号： C07D295/16 ,  C07D213/56 ,  C07D231/12 ,  C07D205/04 ,  C07D307/22 ,  C07D207/273 ,  C07D305/08 ,  C07D333/48 ,  C07D405/10 ,  C07D207/16 ,  C07D211/48 ,  C07C237/42 ,  C07C311/46 ,  C07C311/13 ,  C07D207/12 ,  C07D211/62 ,  C07C233/22 ,  C07D295/195 ,  C07C233/69 ,  C07C235/42 ,  C07D309/14 ,  C07D213/75 ,  C07D231/40 ,  C07D403/06 ,  C07C233/81 ,  C07D209/08 ,  C07D295/155 ,  C07D487/10 ,  C07D403/10 ,  C07D401/06 ,  C07D279/12 ,  C07D239/26

CPC分类号： C07D295/16 ,  C07D213/56 ,  C07D231/12 ,  C07D205/04 ,  C07D307/22 ,  C07D207/273 ,  C07D305/08 ,  C07D333/48 ,  C07D405/10 ,  C07D207/16 ,  C07D211/48 ,  C07C237/42 ,  C07C311/46 ,  C07C311/13 ,  C07D207/12 ,  C07D211/62 ,  C07C233/22 ,  C07D295/195 ,  C07C233/69 ,  C07C235/42 ,  C07D309/14 ,  C07D213/75 ,  C07D231/40 ,  C07D403/06 ,  C07C233/81 ,  C07D209/08 ,  C07D295/155 ,  C07D487/10 ,  C07D403/10 ,  C07D401/06 ,  C07D279/12 ,  C07D239/26

摘要： [Problem] A compound which is useful as a STING inhibitor is provided.
[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

公开(公告)号：US11787766B2

公开(公告)日：2023-10-17

申请号：US16639949

申请日：2018-08-17

申请人： SHANGHAI ENNOVABIO PHARMACEUTICALS CO., LTD.

发明人： Lei Jiang ,  Jianwen Deng ,  Xiaoli Lu ,  Ke Shang ,  Jianyong Shou ,  Bing Wang ,  Danyi Wu ,  Xueli Xu ,  Yuan Xu ,  Yi Zhang ,  Mingwei Zheng

IPC分类号： C07D213/69 ,  C07D213/73 ,  C07D213/84 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D519/00 ,  A61K31/137 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4545 ,  A61K39/12 ,  A61K39/245 ,  A61K39/29 ,  A61K45/06 ,  C07C211/03 ,  C07C223/02 ,  C07D231/40

CPC分类号： C07D213/69 ,  A61K31/137 ,  A61K31/165 ,  A61K31/4155 ,  A61K31/437 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4545 ,  A61K39/12 ,  A61K39/245 ,  A61K39/29 ,  A61K45/06 ,  C07C211/03 ,  C07C223/02 ,  C07D213/73 ,  C07D213/84 ,  C07D231/40 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D519/00

摘要： Provided are a compound for the prevention and treatment of diseases associated with PD-L1, a preparation method therefor and use thereof. Specifically, provided are the compound of formula I, the stereoisomer and the racemate thereof, or pharmaceutically acceptable salts thereof, and also provided is an application thereof in the preparation of a drug for the prevention and treatment of diseases associated with PD-L1.

公开(公告)号：US20230242548A1

公开(公告)日：2023-08-03

申请号：US18058655

申请日：2022-11-23

申请人： The Regents of the University of California

发明人： Jonathan Ostrem ,  Ulf Peters ,  Kevan M. Shokat

IPC分类号： C07D495/04 ,  A61K38/17 ,  C07D231/40 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/10 ,  C07D207/14 ,  C07D211/62 ,  C07D295/185 ,  C07D295/26 ,  C07D211/58 ,  C07D487/04 ,  C12N9/14 ,  C07C235/20 ,  C07C317/08 ,  C12Q1/6886

CPC分类号： C07D495/04 ,  A61K38/1709 ,  C07C235/20 ,  C07C317/08 ,  C07D207/14 ,  C07D211/58 ,  C07D211/62 ,  C07D231/40 ,  C07D295/26 ,  C07D295/185 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/12 ,  C07D417/12 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C12N9/14 ,  C12Q1/6886 ,  C12Q2600/156 ,  C12Q2600/158 ,  C12Y306/05002 ,  G01N2500/04

摘要： K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.

公开(公告)号：US11667648B2

公开(公告)日：2023-06-06

申请号：US16813295

申请日：2020-03-09

申请人： Promega Corporation

发明人： Sergiy Levin ,  Rachel Friedman Ohana ,  Thomas Kirkland ,  Keith V. Wood

IPC分类号： C07D491/22 ,  C07D231/40 ,  C07D487/04

CPC分类号： C07D491/22 ,  C07D231/40 ,  C07D487/04

摘要： Provided herein are cell-permeable, cell-compatible, and chemoselectively-cleavable linkers for tethering (e.g., covalently) functional elements (e.g., a cellular interaction element and a capture element), and methods of use (e.g., intracellular capture and extracellular release of cellular targets) therewith.

公开(公告)号：US20180305319A1

公开(公告)日：2018-10-25

申请号：US15738016

申请日：2016-06-28

申请人： SANDOZ AG

发明人： Olga SCHÖNE ,  Hans-Peter Spitzenstätter ,  Marius KAUFMANN

IPC分类号： C07D231/40

CPC分类号： C07D231/40 ,  C07D501/46

摘要： The present invention relates to a process for the preparation of carbamoylamino pyrazole derivatives using diacetoxyiodobenzene (PhI(OAc)2) in combination with a non-nucleophilic base.

公开(公告)号：US20180282285A1

公开(公告)日：2018-10-04

申请号：US15973655

申请日：2018-05-08

申请人： Dow AgroSciences LLC

发明人： Qiang YANG ,  Beth LORSBACH ,  Gregory WHITEKER ,  Gary ROTH ,  Carl DeAMICIS ,  Thomas CLARK ,  Kaitlyn GRAY ,  Belgin CANTURK ,  Elisabeth J. KANE ,  Yu ZHANG ,  Joseck M. MUHUHI

IPC分类号： C07D231/38 ,  C07C321/16 ,  C07D401/04 ,  A01N43/56 ,  C07D231/40 ,  C07C321/14

CPC分类号： C07D231/38 ,  A01N43/56 ,  C07C321/14 ,  C07C321/16 ,  C07C2601/02 ,  C07D231/40 ,  C07D401/04

摘要： The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.

公开(公告)号：US20180251431A1

公开(公告)日：2018-09-06

申请号：US15836406

申请日：2017-12-08

申请人： VERTEX PHARMACEUTICALS INCORPORATED

发明人： Paul S. Charifson ,  Jon H. Come ,  John J. Court ,  Zachary Gale-Day ,  Wenxin Gu ,  Katrina L. Jackson ,  Sanjay Shivayogi Magavi ,  Suganthini S. Nanthakumar ,  Steven Michael Ronkin ,  Rebecca Jane Swett ,  Qing Tang

IPC分类号： C07D231/40 ,  C07D401/04 ,  C07D409/12 ,  C07D403/04 ,  C07D401/12 ,  C07D417/04 ,  C07D405/04 ,  C07D405/14 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D417/12 ,  C07D413/04

CPC分类号： C07D231/40 ,  A61P25/00 ,  A61P25/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： Disclosed are chemical entities which are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Formula (I) has the structure, R1a, R1b, R2, R3, R4a, R4b and Y are as defined herein. These chemical entities are useful for reduction of very long chain fatty acid levels. These chemical entities and pharmaceutically acceptable compositions comprising such chemical entities can be useful for treating various diseases, disorders and conditions, such as adrenoleukodystrophy (ALD).

公开(公告)号：US20180194757A1

公开(公告)日：2018-07-12

申请号：US15791713

申请日：2017-10-24

申请人： THERAVANCE BIOPHARMA R&D IP, LLC

发明人： Roland Gendron ,  Adam D. Hughes

IPC分类号： C07D413/06 ,  C07D413/04 ,  A61K31/415 ,  C07D405/04 ,  C07D403/12 ,  C07D403/06 ,  C07D403/04 ,  C07D401/06 ,  C07D401/04 ,  C07D231/40 ,  C07D231/14 ,  A61K45/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/422 ,  A61K31/4178 ,  A61K31/4155 ,  C07D405/12

CPC分类号： C07D413/06 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D231/14 ,  C07D231/40 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04

摘要： In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

公开(公告)号：US20180186807A1

公开(公告)日：2018-07-05

申请号：US15680794

申请日：2017-08-18

申请人： Global Blood Therapeutics, Inc.

发明人： Calvin W. Yee ,  Zhe Li

IPC分类号： C07D493/08 ,  C07D487/08 ,  C07D401/04 ,  C07C235/24 ,  C07D231/40 ,  C07D213/75 ,  C07D309/14

CPC分类号： C07D493/08 ,  C07C235/24 ,  C07D213/75 ,  C07D231/40 ,  C07D309/14 ,  C07D401/04 ,  C07D487/08

摘要： Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.