公开(公告)号：US12234244B2

公开(公告)日：2025-02-25

申请号：US17716707

申请日：2022-04-08

Applicant: Araxes Pharma LLC

Inventor： Liansheng Li ,  Jun Feng ,  Tao Wu ,  Pingda Ren ,  Yi Liu ,  Yuan Liu ,  Yun Oliver Long

IPC: A61K31/517 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04 ,  C07D495/04

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds, or a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, have the following structure: wherein A, L1, L2, Q, R1, R2a, R3a, R3b, R4a, R4b, R9, R10, Y, and Z are as exemplified herein. Pharmaceutical compositions comprising such compounds, methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, and methods associated with preparation of such compounds are also provided.

公开(公告)号：US12017996B2

公开(公告)日：2024-06-25

申请号：US17740364

申请日：2022-05-10

Applicant: JIANGSU MEDOLUTION LTD

Inventor： Dawei Zhang

IPC: C07D215/54 ,  C07D401/04

CPC classification number: C07D215/54 ,  C07D401/04

Abstract: The present disclosure is directed to formulations of novel quinolines and their pharmaceutically acceptable salts, which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this disclosure have a general Formula I






wherein R10 to R14 and X are defined herein.

公开(公告)号：US11999698B2

公开(公告)日：2024-06-04

申请号：US17470980

申请日：2021-09-09

Applicant: InflaRx GmbH

Inventor： Yong Li ,  Renfeng Guo ,  Niels Christoph Riedemann

IPC: C07D215/54 ,  C07D405/12

CPC classification number: C07D215/54 ,  C07D405/12

Abstract: The present invention relates to fused piperidinyl bicyclic, meta-substituted piperidinyl and their related compounds that modulate activities of mammalian C5a receptor by directly binding to the C5a receptor. The invention also relates to pharmaceutical compositions containing such compounds and their use in the treatment of a disease or a disorder involving pathogenic activation of C5a receptors.

公开(公告)号：US20230303586A1

公开(公告)日：2023-09-28

申请号：US18178452

申请日：2023-03-03

Applicant: Araxes Pharma LLC

Inventor： Liansheng LI ,  Jun FENG ,  Tao WU ,  Pingda REN ,  Yi LIU ,  Yuan Liu ,  Yun Oliver Long

IPC: C07D495/04 ,  C07D239/94 ,  C07D401/12 ,  C07D217/22 ,  C07D215/46 ,  C07D215/54 ,  C07D239/84 ,  C07D487/04 ,  C07D239/95 ,  C07D403/04 ,  C07D241/44 ,  C07D401/04 ,  C07D409/04

CPC classification number: C07D495/04 ,  C07D215/46 ,  C07D215/54 ,  C07D217/22 ,  C07D239/84 ,  C07D239/94 ,  C07D239/95 ,  C07D241/44 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D409/04 ,  C07D487/04

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I):





or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

公开(公告)号：US11713324B2

公开(公告)日：2023-08-01

申请号：US17126581

申请日：2020-12-18

Applicant: Neurocrine Biosciences, Inc.

Inventor： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Willy Moree ,  Martin Rowbottom ,  Warren Wade ,  Liren Zhao ,  Richard Lowe ,  Nicole Smith ,  Neil Ashweek ,  Yun-Fei Zhu

IPC: C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D239/36 ,  C07D213/58

CPC classification number: C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/58 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure:




wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

公开(公告)号：US11591313B2

公开(公告)日：2023-02-28

申请号：US17168109

申请日：2021-02-04

Applicant: Stingray Therapeutics, Inc.

Inventor： Srinivas Rao Kasibhatla ,  Raman Kumar Kalakuntla ,  Alexis Weston ,  Trason Thode ,  Sunil Sharma ,  Mohan R. Kaadige

IPC: C07D403/04 ,  A61P35/00 ,  C07D239/88 ,  C07D239/94 ,  C07D239/74 ,  C07D403/14 ,  C07D487/08 ,  C07D401/14 ,  C07D401/04 ,  C07D215/54

Abstract: Compounds and methods for their preparation and use as therapeutic or prophylactic agents, for example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1).

公开(公告)号：US20220371999A1

公开(公告)日：2022-11-24

申请号：US17740364

申请日：2022-05-10

Applicant: JIANGSU MEDOLUTION LTD

Inventor： Dawei Zhang

IPC: C07D215/54 ,  C07D401/04

Abstract: The present disclosure is directed to formulations of novel quinolines and their pharmaceutically acceptable salts, which are useful for the treatment of protein kinases mediated diseases and conditions. The compounds of this disclosure have a general Formula I wherein R10 to R14 and X are defined herein.

公开(公告)号：US11034656B2

公开(公告)日：2021-06-15

申请号：US16765473

申请日：2018-11-20

Applicant: TELIGENE LTD

Inventor： Dawei Zhang

IPC: C07D215/54

Abstract: The present application relates to maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)aniline]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, crystalline forms thereof, to processes for its preparation, to pharmaceutical compositions comprising it and to its use in the control of disorders.

公开(公告)号：US20200290969A1

公开(公告)日：2020-09-17

申请号：US16784951

申请日：2020-02-07

Applicant: InflaRx GmbH

Inventor： YONG LI ,  RENFENG GUO ,  NIELS CHRISTOPH RIEDEMANN

IPC: C07D215/54 ,  C07D405/12

Abstract: The present invention relates to fused piperidinyl bicyclic, meta-substituted piperidinyl and their related compounds that modulate activities of mammalian C5a receptor by directly binding to the C5a receptor. The invention also relates to pharmaceutical compositions containing such compounds and their use in the treatment of a disease or a disorder involving pathogenic activation of C5a receptors.

公开(公告)号：US20200283397A1

公开(公告)日：2020-09-10

申请号：US16672083

申请日：2019-11-01

Applicant: Imago Biosciences, Inc.

Inventor： Hugh Y. RIENHOFF, JR. ,  John M. MCCALL ,  Michael CLARE ,  Cassandra CELATKA ,  Amy E. TAPPER

IPC: C07D249/06 ,  C07C309/30 ,  A61K9/00 ,  A61K31/496 ,  C07D239/26 ,  A61K31/506 ,  C07D295/192 ,  A61K31/495 ,  C07D279/12 ,  A61K31/54 ,  C07D205/04 ,  A61K31/397 ,  C07D295/26 ,  C07D215/54 ,  C07C53/18 ,  C07D231/12 ,  C07D263/32 ,  A61K31/541 ,  C07B59/00 ,  C07D403/12 ,  A61K31/4192 ,  C07D401/12 ,  A61K31/454 ,  C07D249/08 ,  A61K31/4196 ,  C07D211/66 ,  A61K31/445 ,  C07D239/42 ,  C07D491/107 ,  C07D413/12 ,  A61K31/5377 ,  C07D498/08 ,  A61K31/5383 ,  C07D471/10 ,  A61K31/435 ,  C07D401/04 ,  A61K31/41 ,  C07D487/04 ,  A61K31/4162 ,  C07D487/08 ,  A61K31/4995 ,  A61K31/551 ,  C07D237/08 ,  A61K31/501 ,  A61K9/16 ,  A61K9/48 ,  A61K45/06 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00

Abstract: Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.