公开(公告)号：US20240336601A1

公开(公告)日：2024-10-10

申请号：US18259408

申请日：2021-12-30

申请人： Chulalongkorn University

发明人： Jakapun SOPONPONG ,  Tanachote RUENGSATRA ,  Nonthaneth NALINRATANA ,  Udomsak UDOMNILOBOL ,  Supanan AMPAWA ,  Nopparat THAVORNSIN ,  Jakkrit SRISA ,  Eakkaphon RATTANANGKOOL ,  Chayan CHAROENPAKDEE ,  Pongkorn CHAIYAKUNVAT ,  Sirikan DEESIRI ,  Songkiat SONGTHAMMANUPHAP ,  Wilasinee DUNKOKSUNG ,  Tirayut VILAIVAN ,  Supranee BURANAPRADITKUN ,  Trairak PISITKUN ,  Nattiya HIRANKARN ,  Thomayant PRUEKSARITANONT

IPC分类号： C07D405/10 ,  A61K31/397 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/546 ,  A61P35/00 ,  C07D209/08 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04 ,  C07D519/00

CPC分类号： C07D405/10 ,  A61K31/397 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/546 ,  A61P35/00 ,  C07D209/08 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/10 ,  C07D513/04 ,  C07D519/00

摘要： The present disclosure relates to compounds of Formula (I):




and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating PD-1 activity, PD-L1 activity, and/or the PD-1/PD-L1 interaction and may be used in the treatment of disorders in which PD-1 activity, PD-L1 activity, and/or PD-1/PD-L1 interaction is implicated, such as cancer.

公开(公告)号：US20240294465A1

公开(公告)日：2024-09-05

申请号：US18567733

申请日：2022-06-09

申请人： HELMHOLTZ ZENTRUM MUNCHEN - DEUTSCHES FORSCHUNGSZENTRUM FUR GESUNDHEIT UND UMWELT

发明人： Gerald BURGSTALLER ,  Michael GERCKENS ,  Oliver PLETTENBURG ,  Ali YILDIRIM ,  Ma HUILONG

IPC分类号： C07C235/38 ,  A61K31/167 ,  A61K31/245 ,  A61K31/343 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/37 ,  A61K31/396 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/4402 ,  C07C317/32 ,  C07C325/02 ,  C07D209/08 ,  C07D213/643 ,  C07D213/75 ,  C07D229/02 ,  C07D231/20 ,  C07D235/08 ,  C07D249/04 ,  C07D271/12 ,  C07D307/81 ,  C07D307/87 ,  C07D311/20 ,  C07D311/58 ,  C07D317/60 ,  C07D319/18 ,  G01N33/50 ,  G01N33/58

CPC分类号： C07C235/38 ,  A61K31/167 ,  A61K31/245 ,  A61K31/343 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/37 ,  A61K31/396 ,  A61K31/404 ,  A61K31/415 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/4402 ,  C07C317/32 ,  C07C325/02 ,  C07D209/08 ,  C07D213/643 ,  C07D213/75 ,  C07D229/02 ,  C07D231/20 ,  C07D235/08 ,  C07D249/04 ,  C07D271/12 ,  C07D307/81 ,  C07D307/87 ,  C07D311/20 ,  C07D311/58 ,  C07D317/60 ,  C07D319/18 ,  G01N33/5044 ,  G01N33/582 ,  C07C2601/02

摘要： The present invention relates to new cinnamic add amides which may be used for treatment of fibrosis and neoplasia and to cinnamic acid amides for use in the treatment of fibrosis, neoplasia, arthrolithiasis, familiar mediterranean fever and pericarditis. Further, the invention relates to a pharmaceutical composition comprising said cinnamic acid amides and to a screening essay for identifying compounds suitable for the treatment of fibrosis.

公开(公告)号：US12065405B2

公开(公告)日：2024-08-20

申请号：US18299347

申请日：2023-04-12

申请人： ATAI Therapeutics, Inc.

发明人： Robert B. Perni ,  Glenn Short ,  Srinivas G. Rao ,  Tanweer A. Khan

IPC分类号： C07D209/16 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D401/06 ,  C07D403/06 ,  C07F9/572

CPC分类号： C07D209/16 ,  C07D209/08 ,  C07D209/12 ,  C07D209/14 ,  C07D401/06 ,  C07D403/06 ,  C07F9/5728

摘要： Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.

公开(公告)号：US20240166598A1

公开(公告)日：2024-05-23

申请号：US18264109

申请日：2022-02-02

申请人： Arizona Board of Regents on Behalf of the University of Arizona ,  The Board of Trustees of the University of Illinois

发明人： Gregory R. Thatcher ,  Zhengnan Shen ,  Rui Xiong ,  Kiira Ratia ,  Lijun Rong ,  Laura Cooper

IPC分类号： C07D205/04 ,  A61K39/215 ,  A61K39/39 ,  A61K45/06 ,  A61P31/14 ,  C07C211/49 ,  C07C237/30 ,  C07D209/08 ,  C07D209/14 ,  C07D211/58 ,  C07D211/62 ,  C07D213/81 ,  C07D215/12 ,  C07D333/20 ,  C07D333/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07H19/067

CPC分类号： C07D205/04 ,  A61K39/215 ,  A61K39/39 ,  A61K45/06 ,  A61P31/14 ,  C07C211/49 ,  C07C237/30 ,  C07D209/08 ,  C07D209/14 ,  C07D211/58 ,  C07D211/62 ,  C07D213/81 ,  C07D215/12 ,  C07D333/20 ,  C07D333/58 ,  C07D401/12 ,  C07D403/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07H19/067

摘要： Provided herein are PLpro inhibitors and methods of treating and/or preventing an infection caused by a coronavirus by administration of one or more of said PLpro inhibitors to a subject in need thereof, as well as pharmaceutical formulations and kits for use in these methods.

公开(公告)号：US11952346B2

公开(公告)日：2024-04-09

申请号：US17545494

申请日：2021-12-08

申请人： Escient Pharmaceuticals, Inc.

发明人： Marion Lanier ,  Marcus Boehm ,  Liming Huang ,  Esther Martinborough ,  Marcos Sainz ,  Brandon Selfridge ,  Adam Yeager

IPC分类号： C07D209/08 ,  C07C255/60 ,  C07D213/73 ,  C07D231/14 ,  C07D239/48 ,  C07D239/94 ,  C07D277/56 ,  C07D277/62 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D471/04

CPC分类号： C07D213/73 ,  C07C255/60 ,  C07D209/08 ,  C07D231/14 ,  C07D239/48 ,  C07D239/94 ,  C07D277/56 ,  C07D277/62 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D471/04

摘要： Methods are provided for modulating MRGPRX2 generally, or for treating a MRGPRX2 dependent condition more specifically, by contacting the MRGPRX2 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I):




or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein D, W, Z, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20240101529A1

公开(公告)日：2024-03-28

申请号：US18319846

申请日：2023-05-18

申请人： Gilead Sciences, Inc.

发明人： Aesop Cho ,  Katherine De La Fuente ,  Thomas P. Stratton ,  Peiyuan Wang ,  William J. Watkins ,  Jie Xu ,  Kin S. Yang

IPC分类号： C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D413/10 ,  C07D405/14 ,  C07D209/08 ,  C07D405/06 ,  A61P31/22

CPC分类号： C07D401/10 ,  C07D403/10 ,  C07D417/10 ,  C07D413/10 ,  C07D405/14 ,  C07D209/08 ,  C07D405/06 ,  A61P31/22

摘要： The present disclosure relates to indolinyl compounds. The present disclosure further relates to compounds that inhibit viral helicase-primase. The present disclosure further relates to the use of the compounds for the preparation a medicament for the treatment of diseases and/or condition through inhibiting viral helicase-primase. The present disclosure also relates to use of those compounds in the treatment of viral infections. The present disclosure further relates to intermediates for its preparation and to pharmaceutical compositions containing those compounds.

公开(公告)号：US11912659B2

公开(公告)日：2024-02-27

申请号：US17232511

申请日：2021-04-16

申请人： The Wistar Institute of Anatomy and Biology

发明人： Troy E. Messick ,  Garry R. Smith ,  Allen B. Reitz ,  Paul M. Lieberman ,  Mark E. McDonnell ,  Yan Zhang ,  Marianne Carlsen ,  Shuai Chen

IPC分类号： C07D209/08 ,  C07D403/12 ,  C07D405/14 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D487/08 ,  C07D471/08 ,  C07D417/12 ,  A61P35/00 ,  A61P31/20 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D277/62 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107

CPC分类号： C07D209/08 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4155 ,  A61K31/422 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  A61P31/20 ,  A61P35/00 ,  C07D277/62 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/10 ,  C07D417/10 ,  C07D417/12 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

摘要： The present invention provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by EBNA1 activity, such as, but not limited to, cancer, infectious mononucleosis, chronic fatigue syndrome, multiple sclerosis, systemic lupus erythematosus and/or rheumatoid arthritis. The present invention further provides EBNA1 inhibitors, and/or pharmaceutical compositions comprising the same, that are useful for the treatment of diseases caused by latent Epstein-Barr Virus (EBV) infection and/or lytic EBV infection.

公开(公告)号：US20240018113A1

公开(公告)日：2024-01-18

申请号：US18372771

申请日：2023-09-26

申请人： Astellas Pharma, Inc. ,  Mitobridge, Inc.

发明人： Junko Maeda ,  Ikumi Kuriwaki ,  Kai Kitamura ,  Yumi Yamashita ,  Kenichi Kakefuda ,  Akio Kamikawa ,  Kenji Negoro ,  Wataru Hamaguchi ,  Ryushi Seo ,  Jeffrey Ciavarri

IPC分类号： C07D295/16 ,  C07D213/56 ,  C07D231/12 ,  C07D205/04 ,  C07D307/22 ,  C07D207/273 ,  C07D305/08 ,  C07D333/48 ,  C07D405/10 ,  C07D207/16 ,  C07D211/48 ,  C07C237/42 ,  C07C311/46 ,  C07C311/13 ,  C07D207/12 ,  C07D211/62 ,  C07C233/22 ,  C07D295/195 ,  C07C233/69 ,  C07C235/42 ,  C07D309/14 ,  C07D213/75 ,  C07D231/40 ,  C07D403/06 ,  C07C233/81 ,  C07D209/08 ,  C07D295/155 ,  C07D487/10 ,  C07D403/10 ,  C07D401/06 ,  C07D279/12 ,  C07D239/26

CPC分类号： C07D295/16 ,  C07D213/56 ,  C07D231/12 ,  C07D205/04 ,  C07D307/22 ,  C07D207/273 ,  C07D305/08 ,  C07D333/48 ,  C07D405/10 ,  C07D207/16 ,  C07D211/48 ,  C07C237/42 ,  C07C311/46 ,  C07C311/13 ,  C07D207/12 ,  C07D211/62 ,  C07C233/22 ,  C07D295/195 ,  C07C233/69 ,  C07C235/42 ,  C07D309/14 ,  C07D213/75 ,  C07D231/40 ,  C07D403/06 ,  C07C233/81 ,  C07D209/08 ,  C07D295/155 ,  C07D487/10 ,  C07D403/10 ,  C07D401/06 ,  C07D279/12 ,  C07D239/26

摘要： [Problem] A compound which is useful as a STING inhibitor is provided.
[Means for Solution] The present inventors have found aryl alkynamide derivatives having an inhibitory action on STING. The aryl alkynamide derivatives of the present invention have an inhibitory action on STING and can be used as an agent for treating an autoimmune disease, a neurodegenerative disease, a type I interferonopathy and/or other STING-mediated disease.

公开(公告)号：US20240009169A9

公开(公告)日：2024-01-11

申请号：US17478235

申请日：2021-09-17

申请人： University of Florida Research Foundation, Incorporated ,  University of Toledo

发明人： Patrick R. Griffin ,  Theodore Kamenecka ,  Beata Lecka-Czernik

IPC分类号： A61K31/404 ,  A61K31/4045 ,  C07D209/08 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/5377 ,  C07D209/18

CPC分类号： A61K31/404 ,  A61K31/4045 ,  C07D209/08 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/5377 ,  C07D209/18

摘要： The invention provides methods of treatment of a progressive bone disease, such as osteoporosis, Paget's Disease, multiple myeloma, or hyperparathyroidism, comprising administration of an effective amount of a non-agonist PPARG modulator to a patient afflicted with the disease.

公开(公告)号：US20240000792A1

公开(公告)日：2024-01-04

申请号：US18463183

申请日：2023-09-07

申请人： Calico Life Sciences LLC ,  AbbVie Inc.

发明人： Kathleen Ann Martin ,  Carmela Sidrauski ,  Jennifer M. Frost ,  Yunsong Tong ,  Xiangdong Xu ,  SeungWon Chung ,  Qingwei Zhang ,  Lei Shi ,  Kathleen J. Murauski ,  Michael J. Dart ,  John T. Randolph

IPC分类号： A61K31/538 ,  A61K31/343 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/472 ,  A61K45/06 ,  C07C235/22 ,  C07D209/08 ,  C07D209/42 ,  C07D217/16 ,  C07D265/36 ,  C07D307/85 ,  C07D311/66 ,  C07D317/46 ,  C07D319/20 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D493/04

CPC分类号： A61K31/538 ,  A61K31/343 ,  A61K31/353 ,  A61K31/357 ,  A61K31/36 ,  A61K31/404 ,  A61K31/4045 ,  A61K31/472 ,  A61K45/06 ,  C07C235/22 ,  C07D209/08 ,  C07D209/42 ,  C07D217/16 ,  C07D265/36 ,  C07D307/85 ,  C07D311/66 ,  C07D317/46 ,  C07D319/20 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D493/04

摘要： Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.