公开(公告)号：US20230348421A1

公开(公告)日：2023-11-02

申请号：US18005952

申请日：2021-07-22

申请人： GENEORA PHARMA (SHIJIAZHUANG) CO., LTD.

发明人： Rui ZHANG ,  Liang YE ,  Mingxu MA ,  Wenyan WANG ,  Yusen DAI ,  Jingwei TIAN

IPC分类号： C07D401/12 ,  C07D409/12 ,  C07D401/06 ,  C07D405/14 ,  C07D405/12 ,  C07D211/58 ,  C07D487/08 ,  C07C275/26

CPC分类号： C07D401/12 ,  C07D409/12 ,  C07D401/06 ,  C07D405/14 ,  C07D405/12 ,  C07D211/58 ,  C07D487/08 ,  C07C275/26

摘要： The present invention relates to a novel compound as a 5-HT2A receptor inhibitor or inverse agonist, a preparation method therefor, and a pharmaceutical composition thereof. The present invention also relates to an application of the compound or the pharmaceutical composition in the preparation of a drug for treating 5-HT2A receptor-related diseases, the diseases comprising: non-motor symptoms caused by Parkinson's disease: delusion, illusion, depression, anxiety, cognitive disorder, and sleep disorder; dementia-related mental diseases; major depressive disorder; or negative symptoms of schizophrenia, etc.

公开(公告)号：US20230348369A1

公开(公告)日：2023-11-02

申请号：US17923167

申请日：2021-05-05

申请人： Cytokinetics, Inc.

发明人： Antonio ROMERO ,  Aroop CHANDRA ,  Christopher EVANS ,  Minxing SHEN

IPC分类号： C07C275/26 ,  C07D401/12 ,  C07D211/58 ,  C07D213/40 ,  C07D231/12 ,  C07D261/08 ,  C07D211/26 ,  C07D413/12 ,  C07D213/74 ,  C07D221/20 ,  C07D213/38 ,  C07C275/18 ,  C07D205/12 ,  C07D207/06 ,  C07D205/04 ,  C07D401/04 ,  C07D295/16 ,  C07D215/08 ,  C07D217/04 ,  C07D209/44 ,  C07D209/08 ,  C07D307/22 ,  C07D209/54 ,  C07D265/36 ,  C07D471/04 ,  C07D305/08 ,  C07C311/13 ,  C07C311/20 ,  C07D241/04 ,  C07D215/06 ,  C07D403/12 ,  C07D231/56 ,  C07D401/06 ,  C07D403/04 ,  C07D403/10 ,  C07D213/82 ,  C07D213/81 ,  C07C317/32 ,  C07D213/87 ,  C07D295/182 ,  C07D207/08 ,  C07D241/08 ,  C07D207/267 ,  C07D249/06 ,  C07D335/02 ,  C07D231/14 ,  C07D309/08 ,  C07D211/78 ,  C07D213/75 ,  C07D213/56 ,  C07D405/06 ,  C07D413/06 ,  C07D271/10 ,  C07D263/56 ,  C07D241/12 ,  C07D249/08 ,  C07D239/26 ,  C07D213/68 ,  C07D213/65 ,  C07C317/30 ,  C07D213/71 ,  C07D401/14

CPC分类号： C07C275/26 ,  C07D401/12 ,  C07D211/58 ,  C07D213/40 ,  C07D231/12 ,  C07D261/08 ,  C07D211/26 ,  C07D413/12 ,  C07D213/74 ,  C07D221/20 ,  C07D213/38 ,  C07C275/18 ,  C07D205/12 ,  C07D207/06 ,  C07D205/04 ,  C07D401/04 ,  C07D295/16 ,  C07D215/08 ,  C07D217/04 ,  C07D209/44 ,  C07D209/08 ,  C07D307/22 ,  C07D209/54 ,  C07D265/36 ,  C07D471/04 ,  C07D305/08 ,  C07C311/13 ,  C07C311/20 ,  C07D241/04 ,  C07D215/06 ,  C07D403/12 ,  C07D231/56 ,  C07D401/06 ,  C07D403/04 ,  C07D403/10 ,  C07D213/82 ,  C07D213/81 ,  C07C317/32 ,  C07D213/87 ,  C07D295/182 ,  C07D207/08 ,  C07D241/08 ,  C07D207/267 ,  C07D249/06 ,  C07D335/02 ,  C07D231/14 ,  C07D309/08 ,  C07D211/78 ,  C07D213/75 ,  C07D213/56 ,  C07D405/06 ,  C07D413/06 ,  C07D271/10 ,  C07D263/56 ,  C07D241/12 ,  C07D249/08 ,  C07D239/26 ,  C07D213/68 ,  C07D213/65 ,  C07C317/30 ,  C07D213/71 ,  C07D401/14 ,  C07C2602/50 ,  C07C2601/14 ,  C07C2601/04 ,  C07C2601/02 ,  C07C2602/08 ,  C07C2602/10 ,  C07B2200/05

摘要： Provided are compounds of Formula (II): or a pharmaceutically acceptable salt thereof, wherein R1, n, and Y1 are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula (II), or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula (II), or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20230303486A1

公开(公告)日：2023-09-28

申请号：US18003226

申请日：2021-06-24

申请人： Idorsia Pharmaceuticals Ltd

发明人： Olivier BEZENCON ,  Caroline DEYMIER ,  Jens-Uwe PETERS ,  Romain SIEGRIST ,  Jean-Philippe SURIVET

IPC分类号： C07C275/26 ,  C07D213/40 ,  C07D239/26 ,  A61P25/08

CPC分类号： C07C275/26 ,  A61P25/08 ,  C07D213/40 ,  C07D239/26 ,  C07C2601/04

摘要： The invention relates to compounds of Formula (I)





wherein X1, X2, X3, L, RX4, R1, R2A, R2B, R3, R4, R5, and R6 are as described in the description; to their preparation, to pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing one or more compounds of Formula (I), and to the use of such compounds as medicaments, especially as Kv7 openers.

公开(公告)号：US20230136562A1

公开(公告)日：2023-05-04

申请号：US17997483

申请日：2021-04-27

申请人： Idorsia Pharmaceuticals Ltd

发明人： Olivier BEZENCON ,  Caroline DEYMIER ,  Jens-Uwe PETERS ,  Romain SIEGRIST ,  Jean-Philippe SURIVET

IPC分类号： C07C275/26 ,  C07D213/16 ,  C07D217/26 ,  C07D239/26 ,  C07D257/04 ,  C07D255/02 ,  C07C317/28

摘要： The invention relates to compounds of Formula (I) wherein X1, X2, X3, Y, R1, R2A, R2B, R3, and R4 are as described in the description; to their preparation, to pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing one or more compounds of Formula (I), and to the use of such compounds as medicaments, especially as Kv7 openers.

公开(公告)号：US11484525B2

公开(公告)日：2022-11-01

申请号：US16921843

申请日：2020-07-06

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  FRIEDRICH-ALEXANDER-UNIVERSITÄT ERLANGEN-NÜRNBERG ,  THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY ,  THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

发明人： Brian K. Shoichet ,  Henry Lin ,  Peter Gmeiner ,  Aashish Manglik ,  Brian Kobilka ,  Bryan L. Roth ,  Daniela Gisela Dengler

IPC分类号： A61K31/381 ,  C07C275/26 ,  C07D401/12 ,  C07C275/24 ,  C07D207/452 ,  C07D233/16 ,  C07D498/18 ,  C07D333/16 ,  C07D249/04 ,  C07D409/12 ,  C07D471/04 ,  C07D333/20 ,  C07D295/125 ,  C07D333/58 ,  C07D495/04 ,  A61P25/36 ,  A61K31/165 ,  A61K31/17

摘要： Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.

公开(公告)号：US20220331346A1

公开(公告)日：2022-10-20

申请号：US17307138

申请日：2021-05-04

申请人： BRISTOL-MYERS SQUIBB COMPANY

发明人： Alaric J. DYCKMAN ,  T.G. Murali Dhar ,  Hai-Yun Xiao ,  John L. Gilmore ,  Michael G. Yang ,  Zili Xiao ,  David Marcoux

IPC分类号： A61K31/695 ,  C07F7/08 ,  A61K31/135 ,  C07D215/14 ,  C07D241/04 ,  C07C323/29 ,  C07C251/38 ,  C07C251/42 ,  C07C251/44 ,  C07D209/46 ,  C07D213/38 ,  C07C275/26 ,  C07C217/74 ,  C07C323/25 ,  C07C235/46 ,  C07F9/54 ,  C07F9/572 ,  C07F9/09 ,  C07C215/42 ,  C07C217/52 ,  C07C217/58 ,  C07C219/24 ,  C07C233/41 ,  C07C233/65 ,  C07C251/50 ,  C07C251/52 ,  C07C251/54 ,  C07C271/34 ,  C07C317/28 ,  C07C317/32 ,  C07C321/16 ,  C07C321/22 ,  C07C321/28 ,  C07D213/32 ,  C07D213/69 ,  C07D213/70 ,  C07D215/12 ,  C07D217/24 ,  C07D231/12 ,  C07D231/20 ,  C07D239/26 ,  C07D241/12 ,  C07D277/24 ,  C07D305/08 ,  C07D309/06 ,  C07D309/12 ,  C07D311/58 ,  C07D311/76 ,  C07D319/20 ,  C07D333/16 ,  C07F9/117 ,  C07F9/62 ,  C07F9/6503 ,  C07F9/6509 ,  C07F9/655 ,  C07F9/6553 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/166 ,  A61K31/17 ,  A61K31/222 ,  A61K31/24 ,  A61K31/27 ,  A61K31/337 ,  A61K31/351 ,  A61K31/352 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4174 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/4965 ,  A61K31/505 ,  A61K31/661

摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R1 is —OH or —OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

公开(公告)号：US20210387986A1

公开(公告)日：2021-12-16

申请号：US16979096

申请日：2019-03-13

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA

发明人： Dean Sheppard ,  Aparna Sundaram ,  William F. DeGrado ,  Hyunil Jo

IPC分类号： C07D471/08 ,  C07D213/81 ,  C07C275/26 ,  C07C275/24 ,  C07D207/48 ,  C07D277/06

摘要： Disclosed herein, inter alia, are inhibitors of integrin alpha 2 beta 1 and methods of using the same.

公开(公告)号：US20210379055A1

公开(公告)日：2021-12-09

申请号：US16962941

申请日：2019-01-17

申请人： Aurigene Discovery Technologies Limited

发明人： Dinesh Chikkanna ,  Vinayak V. Khairnar ,  Muralidhara Ramachandra ,  Leena Khare Satyam

IPC分类号： A61K31/496 ,  A61K45/06 ,  C07D295/215 ,  C07D205/04 ,  C07D231/56 ,  C07D211/58 ,  C07D333/28 ,  C07C275/26 ,  C07C311/11 ,  C07D211/72 ,  C07D471/08 ,  C07D401/04 ,  C07D207/16 ,  C07C237/24 ,  C07D261/04 ,  A61P35/00 ,  A61K31/495 ,  A61K31/17 ,  A61K31/4468 ,  A61K31/439 ,  A61K31/454

摘要： The present invention relates to substituted alkynylene compounds represented by the compounds of formula (I), pharmaceutically acceptable salts and stereoisomers thereof. The present invention further provides the therapeutic uses of the compounds of formula (I) as anti-cancer agents.

公开(公告)号：US11091430B2

公开(公告)日：2021-08-17

申请号：US16786429

申请日：2020-02-10

申请人： REATA PHARMACEUTICALS, INC.

发明人： Eric Anderson ,  Xin Jiang ,  Melean Visnick

IPC分类号： C07C255/47 ,  C07J63/00 ,  C07C275/34 ,  C07C271/24 ,  C07C275/26 ,  C07C311/09 ,  C07D261/08 ,  C07D307/20 ,  C07D487/08 ,  C07C311/07 ,  C07D209/56 ,  C07D211/44 ,  C07D231/12 ,  C07D295/195

摘要： This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

公开(公告)号：US20210221781A1

公开(公告)日：2021-07-22

申请号：US17055550

申请日：2019-05-15

申请人： LIN BIOSCIENCE PTY LTD.

发明人： Yu-Hsin Tom LIN ,  Cheng-Chi Irene WANG ,  Jason OLEJNICZAK

IPC分类号： C07D295/215 ,  A61K31/573 ,  A61K38/13 ,  A61K31/4725 ,  A61K9/00 ,  A61P27/04 ,  C07D211/38 ,  C07D213/40 ,  C07C275/26 ,  C07C275/30 ,  C07D257/04 ,  C07C311/32 ,  C07D249/06 ,  C07D309/14 ,  C07D487/04 ,  C07D211/48 ,  C07D237/20

摘要： Provided herein are compounds, pharmaceutical compositions, and methods of treatment for various diseases or conditions, such as cancer. In one aspect, the method comprises the treatment of metastatic cancers. Compounds and methods provided herein are also used for the treatment of diseases such as inflammatory disease, cardiovascular disease, autoimmune disease, and dry eye syndrome. Further provided herein are dietary supplement formulations and methods for supporting a healthy lifestyle.