公开(公告)号：US20240299360A1

公开(公告)日：2024-09-12

申请号：US17760169

申请日：2021-02-03

Applicant: Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Inventor： Dong Liu ,  Peng Zhao ,  Jian Liu ,  Linghang Zhuang ,  Fengqi Zhang ,  Xinzhu Zhang ,  Chunying Song ,  Suxing Liu ,  Jing Li

IPC: A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/55 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

CPC classification number: A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/55 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: Compounds of formula (I) useful as inhibitors of ADAMTS-5 and/or ADAMTS-4, pharmaceutical compositions thereof, and use of them as therapeutic agents for the treatment of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis, are disclosed.

公开(公告)号：US12083107B2

公开(公告)日：2024-09-10

申请号：US18049652

申请日：2022-10-26

Applicant: Bjoern Colin Kahrs

Inventor： Bjoern Colin Kahrs

IPC: A61K31/05 ,  A61K9/00 ,  A61K31/12 ,  A61K31/16 ,  A61K31/19 ,  A61K31/216 ,  A61K31/225 ,  A61K31/26 ,  A61K31/385 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/47 ,  A61P1/04 ,  A61P5/48 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P17/14 ,  A61P19/02 ,  A61P21/02 ,  A61P21/04 ,  A61P25/00 ,  A61P25/14 ,  A61P25/16 ,  A61P25/28 ,  A61P29/00 ,  A61P37/06 ,  A61P43/00

CPC classification number: A61K31/4439 ,  A61K9/0053 ,  A61K31/05 ,  A61K31/12 ,  A61K31/16 ,  A61K31/19 ,  A61K31/216 ,  A61K31/225 ,  A61K31/26 ,  A61K31/385 ,  A61K31/426 ,  A61K31/47 ,  Y02A50/30 ,  A61K31/05 ,  A61K2300/00 ,  A61K31/12 ,  A61K2300/00 ,  A61K31/16 ,  A61K2300/00 ,  A61K31/19 ,  A61K2300/00 ,  A61K31/216 ,  A61K2300/00 ,  A61K31/26 ,  A61K2300/00 ,  A61K31/385 ,  A61K2300/00 ,  A61K31/4439 ,  A61K2300/00 ,  A61K31/47 ,  A61K2300/00

Abstract: The invention relates to pharmaceutical compositions comprising PPAR agonists and Nrf2 activators and methods of using combinations of PPAR agonists and Nrf2 activators for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis.

公开(公告)号：US12083101B2

公开(公告)日：2024-09-10

申请号：US17201268

申请日：2021-03-15

Applicant: Novartis AG

Inventor： Vincent Bordas ,  Cara Brocklehurst ,  Patrick Chene ,  Pascal Furet ,  Vito Guagnano ,  Patricia Imbach-Weese ,  Joerg Kallen ,  Mickael Le Douget ,  Edwige Liliane Jeanne Lorthiois ,  Joseph McKenna ,  Bahaa Salem ,  Tobias Schmelzle ,  Holger Sellner ,  Nicolas Soldermann ,  Markus Voegtle ,  Markus Wartmann

IPC: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/404 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D413/04 ,  C07D417/04 ,  C07D491/04

CPC classification number: A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D417/04

Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof;






a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US20240294508A1

公开(公告)日：2024-09-05

申请号：US18561308

申请日：2022-05-16

Applicant: SIRONAX LTD.

Inventor： Zhaolan ZHANG ,  Zhiyuan ZHANG ,  Yaning SU ,  Yanping XU

IPC: C07D403/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D403/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: Provided herein are compounds of Formula Ia and Ib, compositions comprising the same, and methods of using the same, including use in treating various diseases and conditions, including those mediated by receptor-interacting protein 1 (RIP1) signaling

公开(公告)号：US20240287080A1

公开(公告)日：2024-08-29

申请号：US18567687

申请日：2022-06-09

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

Inventor： Paul A. BARSANTI ,  Kevin J. DUFFY ,  Brian G. LAWHORN ,  Firoz Ali JAIPURI ,  Daneil Lee SEVERANCE ,  Chenbo WANG ,  Nicholas David ADAMS ,  Janos BOTYANSZKI ,  Michael G. DARCY ,  Terence J. KIESOW ,  John J. MCATEE ,  Cuthbert MARTYR ,  Alexander BUTTRAGO SANTANILLA ,  Xinrong TIAN

IPC: C07D487/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/519 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/519 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D493/04 ,  C07D498/04

Abstract: Disclosed herein are certain thiadiazolyl derivatives 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：US20240287053A1

公开(公告)日：2024-08-29

申请号：US18566804

申请日：2022-06-21

Applicant: Alchemedicine, Inc.

Inventor： Keigo TANAKA ,  Tomohisa NINOMIYA ,  Yoshihide TOMATA

IPC: C07D413/14 ,  A61K31/4439 ,  A61K31/497 ,  A61P9/12 ,  C07D405/14

CPC classification number: C07D413/14 ,  A61K31/4439 ,  A61K31/497 ,  A61P9/12 ,  C07D405/14

Abstract: An object of the present invention is to provide a compound having an ETA receptor antagonistic effect, etc. The object can be attained by a compound represented by the following formula (1):




wherein variables are as described herein, or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240279338A1

公开(公告)日：2024-08-22

申请号：US18567216

申请日：2022-06-07

Applicant: Ares Trading S.A. ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 4) LTD.

Inventor： Rinat Zaynagetdinov ,  Kalyan Chakravarthy Nallaparaju ,  Natalya Belousova ,  Yan Lan

IPC: C07K16/28 ,  A61K31/4439 ,  A61K38/00 ,  A61K39/395 ,  A61P35/00 ,  C07K14/71 ,  C07K16/22

CPC classification number: C07K16/2827 ,  A61K31/4439 ,  A61K39/3955 ,  A61P35/00 ,  C07K14/71 ,  C07K16/22 ,  A61K38/00 ,  C07K2319/30

Abstract: The present invention relates to combination therapies useful for the treatment of cancer. In particular, the invention relates to the combined use of a PD-1 inhibitor, a TGFβ inhibitor, and an adenosine inhibitor to treat cancer.

公开(公告)号：US20240277658A1

公开(公告)日：2024-08-22

申请号：US18030875

申请日：2021-10-15

Applicant: ALBERT-LUDWIGS-UNIVERSITÄT FREIBURG

Inventor： Olaf GROSS ,  Emilia NEUWIRT ,  Manfred JUNG

IPC: A61K31/397 ,  A61K31/17 ,  A61K31/277 ,  A61K31/341 ,  A61K31/351 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5375 ,  A61P37/04

CPC classification number: A61K31/397 ,  A61K31/17 ,  A61K31/277 ,  A61K31/341 ,  A61K31/351 ,  A61K31/402 ,  A61K31/404 ,  A61K31/4178 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/433 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/5375 ,  A61P37/04

Abstract: The present invention relates to a compound or pharmaceutically acceptable salts thereof, that modulates NLRP3 in that the NLRP3 inflammasome is activated. This invention further relates to the compounds and/or compositions for use in the prevention and treatment of a condition, disease or a disorder by activating the NLRP3 inflammasome, wherein the disease is selected from a group comprising infectious diseases, or cancer. Moreover, the invention relates to the use of the present compounds for analyzing a the activity of NLRP3 activation.

公开(公告)号：US12065459B2

公开(公告)日：2024-08-20

申请号：US16672114

申请日：2019-11-01

Applicant: Achillion Pharmaceuticals, Inc.

Inventor： Jason Allan Wiles ,  Venkat Rao Gadhachanda ,  Qiuping Wang ,  Godwin Pais ,  Akihiro Hashimoto ,  Dawei Chen ,  Xiangzhu Wang ,  Atul Agarwal ,  Milind Deshpande ,  Avinash S. Phadke

IPC: C07F9/572 ,  A61K9/00 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/00 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/02 ,  C07F7/08 ,  C07F9/6558 ,  C07F9/6561

CPC classification number: C07F9/5728 ,  A61K9/0014 ,  A61K9/0019 ,  A61K9/0048 ,  A61K9/0053 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/407 ,  A61K31/4162 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/549 ,  A61K31/55 ,  A61K31/675 ,  A61K31/683 ,  C07B59/002 ,  C07D209/12 ,  C07D209/14 ,  C07D209/30 ,  C07D209/40 ,  C07D209/42 ,  C07D209/44 ,  C07D209/88 ,  C07D401/14 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/06 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/14 ,  C07D491/113 ,  C07D495/04 ,  C07D513/04 ,  C07F5/025 ,  C07F5/027 ,  C07F7/0812 ,  C07F9/65583 ,  C07F9/6561 ,  C07F9/65616 ,  C07B2200/05

Abstract: Compounds, methods of use, and processes for making inhibitors of complement factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an aryl, heteroaryl or heterocycle (R32) are provided. The inhibitors described herein target factor D and inhibit or regulate the complement cascade at an early and essential point in the alternative complement pathway, and reduce factor D's ability to modulate the classical and lectin complement pathways. The inhibitors of factor D described herein are capable of reducing the excessive activation of complement, which has been linked to certain autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

公开(公告)号：US12059420B2

公开(公告)日：2024-08-13

申请号：US17261954

申请日：2019-07-22

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： James Aaron Balog ,  Jay A. Markwalder ,  Weifang Shan ,  David K. Williams ,  Susheel Jethanand Nara ,  Saumya Roy ,  Soodamani Thangavel ,  Srinivas Cheruku ,  Ramesh Kumar Sistla

IPC: A61K31/506 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/395 ,  C07D213/74 ,  C07D213/75 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D487/04

CPC classification number: A61K31/506 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K39/3955 ,  C07D213/74 ,  C07D213/75 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention provides compounds of formula (I): wherein all of the variables are as defined herein. These compounds are inhibitors of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases.