公开(公告)号：US20230295170A1

公开(公告)日：2023-09-21

申请号：US18072505

申请日：2022-11-30

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. CZABANIUK ,  Timothy Hopper ,  Jonathan B. Houze ,  Jane Panteleev ,  Gwenaella Rescourio ,  Vincent Santora ,  Haoxuan Wang ,  Ryan D. White ,  Alice R. Wong ,  Yongwei Wu ,  Maxence Bos ,  John Mancuso ,  Ivan Franzoni

IPC: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”).




This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US20230295169A1

公开(公告)日：2023-09-21

申请号：US18072501

申请日：2022-11-30

Applicant: AMGEN INC. ,  Vigil Neuroscience, Inc.

Inventor： Lara C. CZABANIUK ,  Timothy HOPPER ,  Jonathan B. HOUZE ,  Jane PANTELEEV ,  Gwenaella RESCOURIO ,  Vincent SANTORA ,  Haoxuan WANG ,  Ryan D. WHITE ,  Alice R. WONG ,  Yongwei WU ,  Maxence BOS ,  John MANCUSO ,  Ivan FRANZONI

IPC: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61P25/28 ,  C07D413/14 ,  C07D471/04

Abstract: The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2”).




This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.

公开(公告)号：US20230295122A1

公开(公告)日：2023-09-21

申请号：US18041719

申请日：2021-08-18

Applicant: BRISTOL-MYERS SQUIBB COMPANY

Inventor： David S. Yoon ,  Alicia Regueiro-Ren ,  Michael Mandler ,  Shoshana L. Posy ,  Chunjian Liu

IPC: C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D235/18 ,  C07D519/00 ,  C07D405/12 ,  C07D401/10 ,  C07D487/10 ,  C07D487/04 ,  C07D403/10 ,  C07D401/12 ,  C07D451/02

CPC classification number: C07D401/14 ,  C07D451/04 ,  C07D471/04 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D235/18 ,  C07D519/00 ,  C07D405/12 ,  C07D401/10 ,  C07D487/10 ,  C07D487/04 ,  C07D403/10 ,  C07D401/12 ,  C07D451/02

Abstract: The present invention relates to 1H-benzo[d]imidazole derivatives of formula (I) or a salt thereof. The present compounds are inhibitors of TLR9 and useful in treating preventing, or slowing fibrotic diseases, such as e.g. liver fibrosis, renal fibrosis, biliary fibrosis or pancreatic fibrosis, non-alcoholic steatohepatitis (NASH), non-alcoholic fatty liver disease (NAFLD), chronic kidney disease, diabetic kidney disease, primary sclerosing cholangitis (PSC) or primary biliary cirrhosis (PBC), or idiopathic pulmonary fibrosis (IPF).

公开(公告)号：US20230295114A1

公开(公告)日：2023-09-21

申请号：US17923837

申请日：2021-05-07

Applicant: Georgiamune LLC

Inventor： Samir KHLEIF ,  Mikayel MKRTICHYAN ,  Malcolm MACCOSS

IPC: C07D401/12 ,  C07D213/74 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D401/12 ,  C07D213/74 ,  C07D401/14 ,  C07D413/14

Abstract: Compounds of Formula la, lb, or Ic,, are described, where the various substituents are defined herein. The compounds can modulate a property or effect of Akt3 in vitro or in vivo, and can also be used, individually or in combination with other agents, in the prevention or treatment of a variety of conditions. Methods for synthesizing the compounds are described. Pharmaceutical compositions and methods of using these compounds or compositions, individually or in combination with other agents or compositions, in the prevention or treatment of a variety of conditions are also described.

公开(公告)号：US11760753B2

公开(公告)日：2023-09-19

申请号：US17075583

申请日：2020-10-20

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Emily Hanan ,  Steven T. Staben ,  Robert Andrew Heald ,  Calum MacLeod ,  Richard Elliott

IPC: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04 ,  A61P11/00 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  A61K45/06 ,  C07B43/06

CPC classification number: C07D413/14 ,  A61K31/553 ,  C07D267/08 ,  C07D498/04

Abstract: Described herein are benzoxazepin oxazolidinone compounds with phosphoinositide-3 kinase (PI3K) modulation activity or function having the Formula I structure:






or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such PI3K modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon PI3K dysregulation.

公开(公告)号：US20230286997A1

公开(公告)日：2023-09-14

申请号：US17976267

申请日：2022-10-28

Applicant: SHY Therapeutics LLC

Inventor： Yaron R. Hadari ,  Luca Carta ,  Michael Schmertzler ,  Theresa M. Williams ,  Charles H. Reynolds

IPC: C07D495/04 ,  C07D473/30 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D221/04 ,  C07D401/12 ,  C07D407/14 ,  C07D409/14 ,  C07D239/94 ,  C07D417/14 ,  C07D487/04 ,  C07D265/30 ,  C07D271/06 ,  C07D495/14

CPC classification number: C07D495/04 ,  C07D473/30 ,  C07D401/04 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D221/04 ,  C07D401/12 ,  C07D407/14 ,  C07D409/14 ,  C07D239/94 ,  C07D417/14 ,  C07D487/04 ,  C07D265/30 ,  C07D271/06 ,  C07D495/14

Abstract: Provided herein are compounds that inhibit the phosphorylation of MAPK and thus are useful in compositions and methods for treating cancer and inflammatory disease.

公开(公告)号：US20230286965A1

公开(公告)日：2023-09-14

申请号：US18122780

申请日：2023-03-17

Applicant: SK BIOPHARMACEUTICALS CO., LTD.

Inventor： Yong Je SHIN ,  Jin Hee KIM ,  Jun LEE ,  Sook Kyung PARK ,  Ho Yeon LEE ,  Hyun Suk CHOI ,  Se Hyuk KIM ,  Eun Ji KANG ,  Ho Youl LEE ,  Soo Yeon JUNG

IPC: C07D413/06 ,  C07D401/06 ,  C07D413/14 ,  C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D491/08 ,  C07D487/04 ,  A61P35/00

CPC classification number: C07D413/06 ,  A61P35/00 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/08 ,  C07D491/107

Abstract: The present disclosure relates to a compound derivative containing a 6-7 bicyclic ring and use thereof. The compound according to the present disclosure can be effectively used in the prevention or treatment of diseases caused by PRMT5 by acting as a PRMT5 inhibitor.

公开(公告)号：US20230286945A1

公开(公告)日：2023-09-14

申请号：US17990133

申请日：2022-11-18

Applicant: Biosplice Therapeutics, Inc.

Inventor： Sunil Kumar KC ,  Chi Ching Mak ,  Brian Walter Eastman ,  Jianguo Cao ,  Venkataiah Bollu ,  Gopi Kumar Mittapalli ,  Chandramouli Chiruta

IPC: C07D401/14 ,  C07D471/10 ,  C07D417/04 ,  C07D413/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/08 ,  C07D401/04 ,  C07D491/048 ,  C07D417/14 ,  C07D487/04 ,  C07D471/08

CPC classification number: C07D401/14 ,  C07D471/10 ,  C07D417/04 ,  C07D413/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/08 ,  C07D401/04 ,  C07D491/048 ,  C07D417/14 ,  C07D487/04 ,  C07D471/08

Abstract: Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.

公开(公告)号：US20230285378A1

公开(公告)日：2023-09-14

申请号：US17941090

申请日：2022-09-09

Applicant: AbbVie Inc.

Inventor： Mary E. Bellizzi ,  David A. Betebenner ,  Jean-Christophe C. Califano ,  William A. Carroll ,  Daniel D. Caspi ,  David A. DeGoey ,  Pamela L. Donner ,  Charles A. Flentge ,  Yi Gao ,  Charles W. Hutchins ,  Douglas K. Hutchinson ,  Warren M. Kati ,  Tammie K. Jinkerson ,  Ryan G. Keddy ,  Allan C. Krueger ,  Wenke Li ,  Dachun Liu ,  Clarence J. Maring ,  Mark A. Matulenko ,  Christopher E. Motter ,  Lissa T. Nelson ,  Sachin V. Patel ,  John K. Pratt ,  John T. Randolph ,  Todd W. Rockway ,  Kathy Sarris ,  Michael D. Tufano ,  Seble H. Wagaw ,  Rolf Wagner ,  Kevin R. Woller

IPC: A61K31/454 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D453/00 ,  C07D491/113 ,  C07D403/14 ,  C07F7/02 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/4355 ,  A61K31/438 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  A61K31/435

CPC classification number: A61K31/454 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D453/00 ,  C07D491/113 ,  C07D403/14 ,  C07F7/02 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/422 ,  A61K31/4355 ,  A61K31/438 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/695 ,  A61K45/06 ,  A61K31/435 ,  Y02P20/582

Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

公开(公告)号：US11753373B2

公开(公告)日：2023-09-12

申请号：US17830185

申请日：2022-06-01

Applicant: ACEA Therapeutics, Inc.

Inventor： Long Mao ,  Xiao Xu ,  Namir Shaabani ,  Can Jin

IPC: C07D401/12 ,  C07D403/12 ,  C07D207/26 ,  C07D207/416 ,  C07D401/14 ,  C07D403/14 ,  C07D413/14

CPC classification number: C07D207/26 ,  C07D207/416 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14

Abstract: Provided herein, inter alia, are compounds, pharmaceutical compositions and methods related to the treatment of viral infections caused by coronavirus or enterovirus. Provided herein are compounds of Formula (I), (II) and (III)




and methods of using the compounds for therapy. These compounds are peptidomimetics that inhibit protease 3CL of a coronavirus, and are useful for treating conditions caused by viral infections, including COVID-19.