公开(公告)号：US11926625B2

公开(公告)日：2024-03-12

申请号：US17653540

申请日：2022-03-04

Applicant: Nimbus Saturn, Inc.

Inventor： Neelu Kaila ,  Ian Linney ,  Stuart Ward ,  Grant Wishart ,  Benjamin Whittaker ,  William Sinko ,  Shawn Watts ,  Mark Anthony Ashwell ,  Byron Scott Delabarre

IPC: C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107

CPC classification number: C07D471/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

公开(公告)号：US11926617B2

公开(公告)日：2024-03-12

申请号：US17835098

申请日：2022-06-08

Applicant: Achillion Pharmaceuticals, Inc.

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

IPC: C07D405/14 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D413/14 ,  C07F9/6558 ,  C07D417/14 ,  C07D487/04 ,  C07D519/00 ,  C07D403/12 ,  C07D407/14 ,  C07D409/14 ,  C07D403/10 ,  C07D513/04 ,  C07D487/22 ,  A61P37/00 ,  A61P1/16 ,  A61P29/00 ,  C07D493/04

CPC classification number: C07D403/04 ,  A61P1/16 ,  A61P29/00 ,  A61P37/00 ,  C07D401/14 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D407/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/22 ,  C07D493/04 ,  C07D513/04 ,  C07D519/00 ,  C07F9/65583

Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I″ and I′″ or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

公开(公告)号：US20240076295A1

公开(公告)日：2024-03-07

申请号：US18108045

申请日：2023-02-10

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Andrew P. Crew ,  Jing Wang ,  Michael Berlin ,  Peter Dragovich ,  Huifen Chen ,  Leanna Staben

IPC: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/54 ,  A61P35/00 ,  C07D413/14

CPC classification number: C07D417/14 ,  A61K47/10 ,  A61K47/18 ,  A61K47/22 ,  A61K47/545 ,  A61P35/00 ,  C07D413/14

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US11919890B2

公开(公告)日：2024-03-05

申请号：US17210261

申请日：2021-03-23

Applicant: Rigel Pharmaceuticals, Inc.

Inventor： Vanessa Taylor ,  Jiaxin Yu ,  Esteban Masuda ,  Ihab Darwish ,  Yan Chen

IPC: C07D413/12 ,  A61K31/553 ,  A61P29/00 ,  A61P37/02 ,  C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

CPC classification number: C07D413/14 ,  C07D471/10 ,  C07D487/08 ,  C07D491/107

Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.

公开(公告)号：US20240067657A1

公开(公告)日：2024-02-29

申请号：US18258903

申请日：2021-12-21

Applicant: Kira A. ARMACOST ,  Richard Thaddeus BERGER ,  Andrew J. COOKE ,  Christopher Douglas COX ,  Brendan M. CROWLEY ,  Marc LABROLI ,  Michael Aaron PLOTKIN ,  Izzat Tiedje RAHEEM ,  Anthony W. SHAW ,  Kelly-Ann S. SCHLEGEL ,  Jason W. SKUDLAREK ,  Ling TONG ,  Merck Sharp & Dohme LLC

Inventor： Kira A. Armacost ,  Richard Thaddeus Berger, Jr. ,  Andrew J. Cooke ,  Christopher Douglas Cox ,  Brendan M. Crowley ,  Marc Labroli ,  Michael Aaron Plotkin ,  Izzat Tiedje Raheem ,  Anthony W. Shaw ,  Kelly-Ann S. Schlegel ,  Jason W. Skudlarek ,  Ling Tong

IPC: C07D498/04 ,  A61K31/517 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D498/04 ,  A61K31/517 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D519/00

Abstract: The present invention relates to novel Amido-Substituted Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R7, and R8 are as defined herein. The present invention also relates to compositions comprising at least one Amido-Substituted Heterocycle Compound, and methods of using the Amido-Substituted Heterocycle Compounds for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US20240059693A1

公开(公告)日：2024-02-22

申请号：US18256997

申请日：2021-12-14

Applicant: Merck Sharp & Dohme LLC

Inventor： Ronald K. Chang ,  Andrew J. Cooke, JR. ,  Christopher Douglas Cox ,  Marc Labroli ,  Izzat Tiedje Raheem ,  Jack D. Scott ,  Jeffrey W. Schubert ,  Jason W. Skudlarek ,  Zheng Tan ,  Ling Tong

IPC: C07D487/04 ,  C07D519/00 ,  C07D403/14 ,  C07D403/06 ,  C07D413/14 ,  A61K31/517 ,  A61P31/22

CPC classification number: C07D487/04 ,  C07D519/00 ,  C07D403/14 ,  C07D403/06 ,  C07D413/14 ,  A61K31/517 ,  A61P31/22

Abstract: The present invention relates to novel Fused Bicyclic Pyrazole Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are as defined herein. The present invention also relates to compositions comprising at least one Fused Bicyclic Pyrazole Derivative, and methods of using the Fused Bicyclic Pyrazole Derivatives for treating or preventing a herpesvirus infection in a patient.

公开(公告)号：US20240059686A1

公开(公告)日：2024-02-22

申请号：US18085500

申请日：2022-12-20

Applicant: Arvinas Operations, Inc.

Inventor： Andrew P. CREW ,  Hanqing DONG ,  Jing WANG ,  Xin CHEN ,  Yimin QIAN ,  Craig M. CREWS ,  Michael BERLIN ,  Meizhong JIN

IPC: C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  C07D233/86 ,  C07D401/04 ,  C07D491/107 ,  C07D471/10 ,  A61K45/06 ,  C07K5/078 ,  A61P35/00 ,  A61P25/28

CPC classification number: C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12 ,  C07D233/86 ,  A61P25/28 ,  C07D491/107 ,  C07D471/10 ,  A61K45/06 ,  C07K5/06165 ,  A61P35/00 ,  C07D401/04

Abstract: The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US20240059681A1

公开(公告)日：2024-02-22

申请号：US18369069

申请日：2023-09-15

Applicant: HAISCO PHARMACEUTICALS PTE. LTD.

Inventor： Yao Li ,  Zongjun Shi ,  Guobiao ZHANG ,  Lei Chen ,  Wenjing Wang ,  Xiaobo Zhang ,  Dengyu Zheng ,  Bo Xu ,  Xin Liu ,  Yajun Wang ,  Fei Ye ,  Pingming Tang ,  Jia Ni ,  Chen Zhang ,  Pangke Yan

IPC: C07D413/12 ,  C07D267/10 ,  C07D413/14 ,  C07D417/12 ,  C07F9/6527

CPC classification number: C07D413/12 ,  C07D267/10 ,  C07D413/14 ,  C07D417/12 ,  C07F9/6527

Abstract: Disclosed is a nitrile derivative compound represented by formula (I), a stereoisomer, a deuterated product, a co-crystal, a solvate or a pharmaceutically acceptable salt thereof, wherein each group is as defined in the description. The compound has dipeptidyl peptidase 1 inhibitory activity and can be used to prepare a drug for treating diseases including obstructive airway diseases, bronchiectasis, cystic fibrosis, asthma, emphysema, and chronic obstructive pulmonary diseases.

公开(公告)号：US11905299B2

公开(公告)日：2024-02-20

申请号：US17317041

申请日：2021-05-11

Applicant: Gilead Sciences, Inc.

Inventor： Elizabeth M. Bacon ,  Gayatri Balan ,  Chien-Hung Chou ,  Christopher T. Clark ,  Jeromy J. Cottell ,  Musong Kim ,  Thorsten A. Kirschberg ,  John O. Link ,  Gary Phillips ,  Scott D. Schroeder ,  Neil H. Squires ,  Kirk L. Stevens ,  James G. Taylor ,  William J. Watkins ,  Nathan E. Wright ,  Sheila M. Zipfel

IPC: C07D401/12 ,  C07D498/04 ,  C07D405/14 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07D401/14 ,  C07B59/00

CPC classification number: C07D498/04 ,  C07B59/002 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D495/04 ,  C07B2200/05

Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.

公开(公告)号：US11897875B2

公开(公告)日：2024-02-13

申请号：US17883734

申请日：2022-08-09

Applicant: UNIVERSITY OF MARYLAND, BALTIMORE ,  THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

Inventor： Scott Thompson ,  Adam Van Dyke ,  Craig Thomas ,  Patrick Morris

IPC: C07D417/14 ,  A61P25/24 ,  C07D261/08 ,  C07D413/12 ,  C07D413/14 ,  A61K9/19 ,  A61K45/06

CPC classification number: C07D417/14 ,  A61P25/24 ,  C07D261/08 ,  C07D413/12 ,  C07D413/14 ,  A61K9/19 ,  A61K45/06 ,  C07B2200/05

Abstract: The present invention relates to novel alpha5 subunit-selective negative allosteric modulators of GABAA receptors that have been deuterated to improve their medicinal properties by prolonging their half-lives, rendering them useful as fast-acting pharmaceutical treatments for depression related disorders.