公开(公告)号：US20240360122A1

公开(公告)日：2024-10-31

申请号：US18619638

申请日：2024-03-28

Applicant: Terns (Suzhou) Biotechnology Co., Ltd. ,  Terns Pharmaceuticals, Inc.

Inventor： Jianwei BIAN ,  Chunlong CAI ,  Lu A. CHOU

IPC: C07D417/14 ,  A61K31/4545

CPC classification number: C07D417/14 ,  A61K31/4545

Abstract: The disclosure relates to solid forms of 2-((4-(6-((4-cyano-2-fluorobenzyl)oxy)pyridin-2-yl)piperidin-1-yl)methyl)-1-(thiazol-5-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid (Compound 1), including solid forms of Compound 1, salts of Compound 1 and solid forms thereof, including crystalline forms of Compound 1 and salts thereof, as well as polymorphs of Compound 1 and salts of Compound 1.

公开(公告)号：US20240360100A1

公开(公告)日：2024-10-31

申请号：US18684645

申请日：2022-08-18

Applicant: The Board of Regents of The University of Texas System

Inventor： Jia Zhou ,  Kathryn A. Cunningham ,  Noelle C. Anastasio ,  Andrew A. Bolinger

IPC: C07D401/12 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D211/60 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D401/12 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  C07D211/60 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

Abstract: Disclosed herein are serotonin (5-hydroxytryptamine) 5-HT2A receptor and/or 5-HT2C receptor allosteric modulators, the preparation thereof and use thereof.

公开(公告)号：US20240358703A1

公开(公告)日：2024-10-31

申请号：US18418061

申请日：2024-01-19

Applicant: KURA ONCOLOGY, INC.

Inventor： Francis BURROWS ,  Linda V. KESSLER ,  Liansheng LI ,  Pingda REN ,  Yi WANG ,  Tao WU ,  Jingchuan ZHANG

IPC: A61K31/519 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/505 ,  A61K31/5377 ,  A61P35/02

CPC classification number: A61K31/519 ,  A61K31/44 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/453 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/505 ,  A61K31/5377 ,  A61P35/02

Abstract: The present disclosure provides methods for treating hematological malignancies and Ewing's sarcoma using menin inhibitors. Compositions for use in these methods are also provided.

公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

公开(公告)号：US12115154B2

公开(公告)日：2024-10-15

申请号：US17124357

申请日：2020-12-16

Applicant: SRX Cardio, LLC

Inventor： Simeon Bowers ,  Mark Karbarz ,  Jiang Zhu ,  Thomas E. Barta ,  Jonathan William Bourne ,  Anjali Pandey

IPC: C07D211/14 ,  A61K31/451 ,  A61K31/4545 ,  A61P3/06 ,  C07D401/04

CPC classification number: A61K31/451 ,  A61K31/4545 ,  A61P3/06 ,  C07D211/14 ,  C07D401/04

Abstract: The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

公开(公告)号：US20240336565A1

公开(公告)日：2024-10-10

申请号：US18574284

申请日：2022-07-01

Applicant: Acer Therapeutics, Inc.

Inventor： John KLOPP

IPC: C07D211/58 ,  A61K31/4545 ,  C07C309/04 ,  C07C309/30 ,  C07C309/35

CPC classification number: C07D211/58 ,  A61K31/4545 ,  C07C309/04 ,  C07C309/30 ,  C07C309/35

Abstract: Provided herein are solid forms of osanetant, including salts thereof, processes for making the solid forms, and their therapeutic methods of use. Also provided is a process for preparing osanetant, and intermediates for use in the same.

公开(公告)号：US20240335440A1

公开(公告)日：2024-10-10

申请号：US18715927

申请日：2022-12-05

Applicant: IDEAYA BIOSCIENCES, INC. ,  PFIZER INC.

Inventor： Matthew Anthony MAURER ,  Michael Gabriel O'QUIGLEY ,  Richard ZANG ,  Jaymes HOLLAND ,  Mai Hope LE ,  Sarah Shwu-Kuan JAW-TSAI

IPC: A61K31/497 ,  A61K31/4545 ,  A61P35/00

CPC classification number: A61K31/497 ,  A61K31/4545 ,  A61P35/00

Abstract: Provided herein is a combination therapy and methods of using such combination therapy to treat diseases or disorders associated with PKC and c-MET.

公开(公告)号：US20240327430A1

公开(公告)日：2024-10-03

申请号：US18600352

申请日：2024-03-08

Applicant: Breakpoint Therapeutics GmbH

Inventor： Andrea Guerrero Corella ,  Stuart Robert Flanagan ,  Jonathan Hollick ,  Julien Gilbert Jacques Malassis ,  Matthew Raymond Smith ,  Ian Andrew Yule ,  Jonathan Mark Bentley

IPC: C07D513/04 ,  A61K31/4545

CPC classification number: C07D513/04 ,  A61K31/4545

Abstract: The present invention relates to a compound of the Formula:




or a pharmaceutically acceptable salt thereof.
The compound of the present invention inhibits Polθ. This novel therapeutic compound is therefore useful for the treatment and/or prevention of diseases and conditions in which Polθ activity is implicated, such as, for example but not limited to, the treatment and/or prevention of cancer. The present invention also relates to pharmaceutical compositions comprising the novel therapeutic compound defined herein, to processes for synthesising the compound and to their use for the treatment of diseases and/or conditions in which Polθ activity is implicated.

公开(公告)号：US20240327399A1

公开(公告)日：2024-10-03

申请号：US18660829

申请日：2024-05-10

Applicant: GlaxoSmithKline Intellectual Property (No.4) Limited ,  IDEAYA Biosciences, Inc.

Inventor： Janos BOTYANSZKI ,  Kevin Duffy ,  Young Eun Choi ,  Claire L. Neilan ,  Marcus M. Fischer

IPC: C07D417/14 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/675 ,  A61P35/00 ,  C07F9/6558

CPC classification number: C07D417/14 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/675 ,  A61P35/00 ,  C07F9/65583

Abstract: Disclosed herein are compounds of Formula (I):




that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.

公开(公告)号：US20240327389A1

公开(公告)日：2024-10-03

申请号：US18499791

申请日：2022-05-04

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： TAO WANG ,  Zhongxing Zhang ,  Zhiwei Yin

IPC: C07D405/14 ,  A61K31/395 ,  A61K31/444 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/553 ,  C07D211/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14

CPC classification number: C07D405/14 ,  A61K31/444 ,  A61K31/4525 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/553 ,  A61K31/5545 ,  C07D211/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D413/14

Abstract: The present disclosure generally relates to lactone and lactam containing compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds. and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.