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.

公开(公告)号：USRE49594E1

公开(公告)日：2023-08-01

申请号：US16974363

申请日：2020-05-04

Applicant: Research Triangle Institute

Inventor： Scott P. Runyon ,  Rangan Maitra ,  Sanju Narayanan ,  James Barnwell Thomas ,  Kenneth S. Rehder ,  Srinivas Olepu

IPC: C07D491/107 ,  C07D403/12 ,  C07D231/14 ,  C07D403/06 ,  C07D407/12 ,  C07D413/12 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08

CPC classification number: C07D491/107 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4245 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D231/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08

Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

公开(公告)号：US20230227427A1

公开(公告)日：2023-07-20

申请号：US17926864

申请日：2021-05-25

Applicant: SANOFI

Inventor： Barrie Phillip MARTIN ,  Jan-Christoph WESTERMANN ,  Oliver Thomas KERN ,  Arthur Jonathan HOLMES ,  Bohdan WASZKOWYCZ ,  Angus MORRISON ,  Michael KICZUN ,  Mounir AL MASRI ,  Alasdair SMITH ,  Anthony HUXLEY

IPC: C07D401/12 ,  C07D471/04 ,  C07D231/14 ,  C07D403/12 ,  C07D487/04 ,  C07D413/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D401/12 ,  C07D471/04 ,  C07D231/14 ,  C07D403/12 ,  C07D487/04 ,  C07D413/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds that are IL-17A modulators. The compounds have the structural Formula I defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with modulation of IL-17A activity.

公开(公告)号：US20230192757A1

公开(公告)日：2023-06-22

申请号：US18169964

申请日：2023-02-16

Applicant: Sage Therapeutics, Inc.

Inventor： Gabriel Martinez Botella ,  Francesco G. Salituro ,  Albert Jean Robichaud ,  Boyd L. Harrison

IPC: C07J43/00 ,  C07D249/18 ,  C07D231/14 ,  C07D295/033 ,  C07D249/04 ,  A61P25/00 ,  C07J13/00 ,  C07J75/00 ,  A61K9/00 ,  A61K31/58

CPC classification number: C07J43/003 ,  C07D249/18 ,  C07D231/14 ,  C07D295/033 ,  C07D249/04 ,  A61P25/00 ,  C07J13/007 ,  C07J75/00 ,  A61K9/0019 ,  A61K9/0053 ,  A61K31/58

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R1, R2a, R2b, R3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.