公开(公告)号：US12233062B2

公开(公告)日：2025-02-25

申请号：US18591753

申请日：2024-02-29

Applicant: Jacobio Pharmaceuticals Co., Ltd.

Inventor： Huifeng Han ,  Panliang Gao ,  Cunbo Ma ,  Di Kang

IPC: A61K31/497 ,  A61K31/438 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D417/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D495/10 ,  C07D513/04 ,  C07D513/10 ,  C07D519/00

Abstract: This invention provides a compound of formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention provides a pharmaceutical composition comprising the said compound.

公开(公告)号：US12202816B2

公开(公告)日：2025-01-21

申请号：US17278489

申请日：2019-09-27

Applicant: CALLIDITAS THERAPEUTICS SUISSE SA

Inventor： Peter Machin ,  Mark Chambers ,  Alastair Hodges ,  Andrew Sharpe ,  Grant Wishart ,  Benjamin Perry ,  Sylvain Celanire ,  Freddy Heitz

IPC: C07D401/14 ,  A61K45/06 ,  A61P1/16 ,  C07D405/14 ,  C07D417/14 ,  C07D491/107 ,  C07D491/20 ,  C07D498/04

Abstract: Disclosed herein are new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).

公开(公告)号：US20240425484A1

公开(公告)日：2024-12-26

申请号：US18732048

申请日：2024-06-03

Applicant: Atomwise Inc.

Inventor： Shahab Mortezaei

IPC: C07D401/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/675 ,  A61P17/06 ,  A61P37/06 ,  C07D239/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D491/107 ,  C07F9/6558

Abstract: In exemplary embodiments, inhibitors of Tyrosine Kinase 2 (TYK2), pharmaceutical formulations comprising these compounds, methods of using these compounds to inhibit TYK2, and treat diseases such as autoimmune and inflammatory diseases are provided.

公开(公告)号：US20240409548A1

公开(公告)日：2024-12-12

申请号：US18698867

申请日：2022-10-04

Applicant: Arena Pharmaceuticals, Inc.

Inventor： Anthony C. Blackburn

IPC: C07D491/107 ,  A61K31/4709 ,  C07C309/04

Abstract: Provided is a solvate that is 1-ethyl-3-((R)-3-((S)-2-hydroxy-3-(3-(methylsulfonyl)phenoxy)propylamino)-1-oxa-8-azaspiro[4.5]decan-8-ylsulfonyl)quinolin-4(1H)-one mesylate hemihydrate Form 2, and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor.

公开(公告)号：US20240400591A1

公开(公告)日：2024-12-05

申请号：US18682463

申请日：2022-08-09

Applicant: Jacobio Pharmaceuticals Co., Ltd.

Inventor： Sujing LI ,  Amin LI ,  Qian ZHENG ,  Chaojie DANG ,  Xinrui FAN ,  Wei LONG ,  Yanping WANG

IPC: C07F9/6558 ,  A61K31/397 ,  A61K31/403 ,  A61K31/438 ,  A61K31/439 ,  A61K31/4535 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/67 ,  A61K31/675 ,  C07D333/58 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  C07D495/04 ,  C07F9/6568 ,  C07F9/6584

Abstract: Provided are compounds of formula (I) which can bind to mutant p53 and restore the ability of the p53 mutant to bind DNA and activate downstream effectors involved in tumor suppression. Also provided are pharmaceutical compositions comprising the compounds, methods of preparing the compounds and the use in the manufacture of medicaments for preventing or treating a disease or condition related to p53 mutants.

公开(公告)号：US20240391877A1

公开(公告)日：2024-11-28

申请号：US18696975

申请日：2022-09-30

Applicant: WUHAN CREATERNA SCIENCE AND TECHNOLOGY CO.,LTD.

Inventor： Jun LOU ,  Jingkang WU ,  Li LIU ,  Youyou SUN ,  Yongkai CHEN ,  Yihan ZHANG ,  Xiaoqin LU ,  Feng ZHOU ,  Ying CHEN ,  Liqian ZHANG ,  Fan YANG ,  Chaodong WANG

IPC: C07D221/20 ,  A61K31/397 ,  A61K31/403 ,  A61K31/407 ,  A61K31/438 ,  A61K31/444 ,  A61K31/5386 ,  C07D205/12 ,  C07D209/54 ,  C07D221/22 ,  C07D265/34 ,  C07D401/10 ,  C07D471/10 ,  C07D491/107

Abstract: Disclosed are a compound as an inhibitor of complement factor D, and a pharmaceutical composition thereof and the use thereof. Specifically disclosed are a compound as represented by formula (I), a tautomer thereof, a stereoisomer thereof and a prodrug thereof, or a pharmaceutically acceptable salt of any one of the above-mentioned compounds, or a solvate of any one of the above-mentioned compounds. The compound has a good inhibitory activity on complement factor D, and has an excellent pharmacokinetic and pharmacodynamic activity. Formula (I)

公开(公告)号：US12145940B2

公开(公告)日：2024-11-19

申请号：US17568530

申请日：2022-01-04

Applicant: Hoffmann-La Roche Inc.

Inventor： Barbara Biemans ,  Georg Jaeschke ,  Antonio Ricci ,  Daniel Rueher ,  Fionn O'Hara

IPC: C07D401/10 ,  A61K31/527 ,  A61P25/16 ,  C07D487/10 ,  C07D491/107 ,  C07D491/20

Abstract: The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.

公开(公告)号：US20240376119A1

公开(公告)日：2024-11-14

申请号：US18516710

申请日：2022-05-20

Applicant: CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd.

Inventor： Guorui MI ,  Chuanwu ZHAO ,  Qian GUO ,  Jianan ZHANG ,  Chunna LI ,  Wenli WEI ,  Yanxia XU

IPC: C07D491/107 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61P35/00 ,  C07D401/14 ,  C07D413/14 ,  C07D519/00

Abstract: Provided in the present invention are a class of compounds as represented by formula (I), or a prodrug, a tautomer, a stereoisomer, a solvate, and an isotopic derivative thereof, or a pharmaceutically acceptable salt thereof. The compound has an SHP2 kinase inhibitory effect and can be used for treating and/or preventing diseases, disorders, and conditions mediated by SHP2 activity, such as tumors, cancers, cancer metastasis, cardiovascular diseases, immune disorders, visual disorders, etc.

公开(公告)号：US20240360151A1

公开(公告)日：2024-10-31

申请号：US18602519

申请日：2024-03-12

Applicant: SANOFI

Inventor： Jean-Philippe LETALLEC ,  Franck Marguet ,  Fréderic Petit ,  Baptiste Ronan ,  Corinne Terrier

IPC: C07D498/10 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/553 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

CPC classification number: C07D498/10 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/553 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

Abstract: The present invention relates to a compound of formula (I) wherein n is 1 or 2, R1 is halogen, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, ethynyl, propargyl, or (C3-C6)cycloalkyl, or two R1 form a cyclopentane ring fused to the phenol; R2 and R3 represent H, cyano, ethynyl, propargyl, (C1-C4)alkyl, hydroxy(C1-C4)alkyl or a halo(C1-C4)alkyl, or R2 and R3 form together with the atoms connecting them a (C5-C6)carbocyclic ring fused to the pyridazine ring; R4 and R5 form together with N to which they are attached an optionally substituted 3-7 membered monocyclic heterocycloalkyl ring, 8-11 membered bicyclic heterocycloalkyl ring or 7-12 membered bicyclic heterocyclic spiro ring. The present invention also relates to a medicament and a pharmaceutical composition comprising said compound of formula (I), as well as their therapeutic uses, in particular as inhibitor of NOD-like receptor protein 3 inflammasome for treating for example Parkinson's disease or frontotemporal Dementia.

公开(公告)号：US20240300939A1

公开(公告)日：2024-09-12

申请号：US18568899

申请日：2022-06-13

Applicant: Scorpion Therapeutics, Inc.

Inventor： David St. Jean, Jr. ,  Maxwell David Cummings

IPC: C07D417/12 ,  A61K31/343 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/427 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D307/81 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/10

CPC classification number: C07D417/12 ,  A61K31/343 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/427 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D307/81 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/10

Abstract: This disclosure provides compounds of Formula (I), Formula (II), and pharmaceutically acceptable salts thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Ka). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) PI3Ka activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.