公开(公告)号：US20250059176A1

公开(公告)日：2025-02-20

申请号：US18938776

申请日：2024-11-06

Applicant: GUANGZHOU INNOCARE PHARMA TECH CO., LTD.

Inventor： Xiangyang CHEN ,  Yingxiang GAO ,  Chong LIU ,  Haihong NI

IPC: C07D417/04 ,  A61K31/444 ,  A61P35/00 ,  C07D211/34 ,  C07D213/82 ,  C07D231/14 ,  C07D277/56 ,  C07D295/185 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

Abstract: Compounds of Formula I, as shown below and defined herein: and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).

公开(公告)号：US12220401B2

公开(公告)日：2025-02-11

申请号：US18362249

申请日：2023-07-31

Applicant: Loxo Oncology, Inc.

Inventor： Nicolas Guisot

IPC: A61K31/415 ,  A61K31/4155 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  A61P37/02 ,  C07D231/14 ,  C07D231/38 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  C07D405/08 ,  C07D405/14 ,  C07D413/06 ,  C07D417/04

Abstract: This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases.

公开(公告)号：US20250042843A1

公开(公告)日：2025-02-06

申请号：US18597537

申请日：2024-03-06

Applicant: Tetraphase Pharmaceuticals, Inc.

Inventor： Jingye Zhou ,  Xiao-Yi Xiao ,  Louis Plamondon ,  Diana K. Hunt ,  Roger B. Clark ,  Robert Zahler

IPC: C07C233/57 ,  A61K31/65 ,  A61K45/06 ,  C07C311/08 ,  C07C311/21 ,  C07D205/04 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D207/10 ,  C07D207/12 ,  C07D207/14 ,  C07D207/16 ,  C07D207/34 ,  C07D209/94 ,  C07D211/60 ,  C07D211/76 ,  C07D213/74 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D231/56 ,  C07D233/61 ,  C07D239/42 ,  C07D249/04 ,  C07D257/04 ,  C07D261/18 ,  C07D261/20 ,  C07D277/56 ,  C07D295/088 ,  C07D295/12 ,  C07D295/15 ,  C07D295/26 ,  C07D311/08 ,  C07D333/34 ,  C07D333/38 ,  C07D413/12

Abstract: The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.

公开(公告)号：US12077507B2

公开(公告)日：2024-09-03

申请号：US18194410

申请日：2023-03-31

Applicant: The Regents of the University of California

Inventor： Kevan M. Shokat ,  Daniel Gentile ,  Steven Moss

IPC: C07D231/14 ,  C12N9/14 ,  C12N9/96 ,  G01N33/68

CPC classification number: C07D231/14 ,  C12N9/14 ,  C12N9/96 ,  C12Y306/05002 ,  G01N33/68

Abstract: Disclosed herein, inter alia, are compositions and methods for modulating Ras and treating cancer.

公开(公告)号：US20240182427A1

公开(公告)日：2024-06-06

申请号：US18516315

申请日：2023-11-21

Applicant: Rezolute, Inc.

Inventor： Michael Burke ,  Jeffrey Breit ,  Randy Wald ,  William Steinhauff

IPC: C07D231/14 ,  A61K9/20

CPC classification number: C07D231/14 ,  A61K9/2009 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/0053 ,  C07B2200/13

Abstract: Described herein are high loading, stable solid dosage forms of a plasma kallikrein inhibitor, 1-benzyl-1H-pyrazole-4-carboxylic acid 4-carbamimidoylbenzylamide (Compound 1) or a pharmaceutically acceptable salt thereof. Methods of treatment of patients that will benefit from the effects of a plasma kallikrein inhibitor are also disclosed.

公开(公告)号：US11999699B2

公开(公告)日：2024-06-04

申请号：US17840712

申请日：2022-06-15

Applicant: GRUENENTHAL GMBH

Inventor： Sebastian Krueger ,  Sebastian Peil ,  Clemens Dialer ,  Marcel Muelbaier ,  Markus Wagener ,  Ingo Konetzki ,  Nikolay Sitnikov ,  Jo Alen ,  Martin Pettersson

IPC: C07D231/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/14 ,  C07D413/12

CPC classification number: C07D231/14 ,  C07D401/12 ,  C07D403/12 ,  C07D405/06 ,  C07D405/14 ,  C07D413/12

Abstract: The present invention relates to compounds according to general formula (I)




which act as inhibitors of NaV1.8 and can be used in the treatment of pain.

公开(公告)号：US20240101545A1

公开(公告)日：2024-03-28

申请号：US18496692

申请日：2023-10-27

Applicant: GUANGZHOU INNOCARE PHARMA TECH CO., LTD.

Inventor： Xiangyang CHEN ,  Yingxiang GAO ,  Chong LIU ,  Haihong NI

IPC: C07D417/04 ,  A61K31/444 ,  A61P35/00 ,  C07D211/34 ,  C07D213/82 ,  C07D231/14 ,  C07D277/56 ,  C07D295/185 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

CPC classification number: C07D417/04 ,  A61K31/444 ,  A61P35/00 ,  C07D211/34 ,  C07D213/82 ,  C07D231/14 ,  C07D277/56 ,  C07D295/185 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

Abstract: Compounds of Formula I, as shown below and defined herein:




and pharmaceutically acceptable salts, syntheses, intermediates, formulations, and methods of treating diseases including cancer, inflammation, and autoimmune disease mediated at least in part by Bruton's Tyrosine Kinase (BTK).

公开(公告)号：US20240083852A1

公开(公告)日：2024-03-14

申请号：US18234629

申请日：2023-08-16

Applicant: Shaoxing Shangyu Xin Yinbang Biochemical Co., Ltd.

Inventor： Shengxue LIU ,  Yintao SHI ,  Qiang GONG ,  Sufang ZHONG ,  Jianjiang ZHANG ,  Xiaoyuan QIAN ,  Fang GUO ,  Rujun CHEN ,  Xiaoying JIAN

IPC: C07D231/14 ,  C07D409/12

CPC classification number: C07D231/14 ,  C07D409/12

Abstract: The present application relates to a synthesis method for N-methyl-3-substituted methyl-4-pyrazolamide derivative and N-methyl-3-substituted methyl-4-pyrazolic acid, including the following steps: step S1: synthesis of intermediate E; step S2: synthesis of intermediate D; step S3: synthesis of intermediate C; step S4: synthesis of N-methyl-3-substituted methyl-4-pyrazolamide derivative; and synthesis of N-methyl-3- substituted methyl-4-pyrazolic acid by decomposition of N-methyl-3-substituted methyl-4-pyrazolamide derivative.

公开(公告)号：US11839617B2

公开(公告)日：2023-12-12

申请号：US17857492

申请日：2022-07-05

Applicant: HMI Medical Innovations, LLC

Inventor： Gerard M. Housey

IPC: A61K31/5377 ,  C07D213/81 ,  C07D213/87 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/84 ,  C07D253/065 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/574 ,  C07D239/48 ,  C07C243/38 ,  C07D213/77 ,  C07D213/86 ,  C07D215/38 ,  C07D253/075 ,  C07D403/12 ,  G01N33/573 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  G01N33/50 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/495 ,  A61K31/517

CPC classification number: A61K31/5377 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/444 ,  A61K31/4436 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  C07C243/38 ,  C07D213/77 ,  C07D213/81 ,  C07D213/86 ,  C07D213/87 ,  C07D215/38 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/48 ,  C07D239/84 ,  C07D253/065 ,  C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/502 ,  G01N33/5011 ,  G01N33/5041 ,  G01N33/573 ,  G01N33/574 ,  G01N2500/00 ,  G01N2500/10

Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

公开(公告)号：US11795162B2

公开(公告)日：2023-10-24

申请号：US16639807

申请日：2018-08-17

Applicant: Saint Louis University

Inventor： Thomas Burris ,  John K. Walker ,  Carissa S. Hampton ,  Keith McCormick Haynes ,  Kristine Griffett ,  Cyrielle Billon ,  Sadichha Sitaula

IPC: C07D209/42 ,  C07D413/04 ,  C07D231/14 ,  C07D277/56 ,  C07D277/82 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07F5/02

CPC classification number: C07D413/04 ,  C07D209/42 ,  C07D231/14 ,  C07D277/56 ,  C07D277/82 ,  C07D307/68 ,  C07D333/38 ,  C07D401/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07F5/027

Abstract: In one aspect, the present disclosure describes new estrogen receptor-related orphan receptor (EER) inverse agonist compounds. Also described are pharmaceutical formulations, methods of synthesis and uses thereof.