公开(公告)号：US11981661B2

公开(公告)日：2024-05-14

申请号：US17465536

申请日：2021-09-02

Applicant: Hoffmann-La Roche Inc.

Inventor： Joerg Benz ,  Uwe Grether ,  Benoit Hornsperger ,  Carsten Kroll ,  Bernd Kuhn ,  Rainer E. Martin ,  Fionn O'Hara ,  Bernd Puellmann ,  Hans Richter ,  Martin Ritter

IPC: C07D401/14 ,  A61K9/00 ,  A61K9/20 ,  A61K9/48 ,  C07D403/06 ,  C07D413/06 ,  C07D413/14 ,  C07D487/04

CPC classification number: C07D403/06 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4866 ,  C07D401/14 ,  C07D413/06 ,  C07D413/14 ,  C07D487/04

Abstract: The invention provides new heterocyclic compounds having the general formula (I)




wherein B, C, L, X, Y, RL and R3 to R5 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

公开(公告)号：US20240150334A1

公开(公告)日：2024-05-09

申请号：US18482129

申请日：2023-10-06

Applicant: Pfizer Inc.

Inventor： Jan Antoinette Cusi Romero Adams ,  Bruce Michael Bechle ,  Jason Kenneth Dutra ,  Michelle Renee Garnsey ,  Xinjun Hou ,  Jisun Lee ,  Deane Milford Nason, II ,  Steven Victor O'Neil ,  Danica Antonia Rankic ,  Yang Wang ,  Ann Sorrentino Wright ,  Lei Zhang ,  Liying Zhang ,  David James Edmonds

IPC: C07D413/04 ,  C07D231/56 ,  C07D263/56 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D413/04 ,  C07D231/56 ,  C07D263/56 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D498/04 ,  C07D513/04

Abstract: Described herein are compounds of Formula I,




wherein the variables are defined herein, their use as HSD17B13 inhibitors and/or degraders, pharmaceutical compositions containing such compounds and their use to treat, for example, NAFLD and NASH.

公开(公告)号：US20240150333A1

公开(公告)日：2024-05-09

申请号：US17913033

申请日：2021-03-22

Applicant: H. LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE, INC.

Inventor： Ernst SCHONBRUNN ,  Justin LOPCHUK ,  Md Rezaul KARIM ,  Zachary SHULTZ

IPC: C07D413/04 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D413/04 ,  C07D413/14 ,  C07D471/04

Abstract: Disclosed are inhibitors for TAF1. The TAF1 inhibitors are compounds having a structure according to one of the Formula described herein. Methods of using the disclosed compounds to treat proliferative disorders are also disclosed.

公开(公告)号：US20240150320A1

公开(公告)日：2024-05-09

申请号：US18448696

申请日：2023-08-11

Applicant: Corcept Therapeutics Incorporated

Inventor： Hazel Hunt ,  Lorna DUFFY ,  Ian STRUTT ,  Morgan JOUANNEAU ,  Thomas HORNSBY ,  Mark MILLS ,  Andrew William PHILLIPS ,  Jon-Paul WARD

IPC: C07D401/14 ,  C07D231/56 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04

CPC classification number: C07D401/14 ,  C07D231/56 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04

Abstract: The present disclosure provides compounds of Formula I or II. Compounds of Formula I or II may be used in pharmaceutical formulations, and may be used for modulating glucocorticoid receptors.

公开(公告)号：US11975005B2

公开(公告)日：2024-05-07

申请号：US18087672

申请日：2022-12-22

Applicant: TIANLI BIOTECH PTY LTD

Inventor： Alastair Stewart ,  Christine Keenan ,  Trudi Harris

IPC: C07D403/04 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/519 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  A61P35/00 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04

CPC classification number: A61K31/519 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/573 ,  A61K31/58 ,  A61K45/06 ,  A61P35/00 ,  C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D487/04 ,  A61K31/58 ,  A61K2300/00 ,  A61K31/573 ,  A61K2300/00 ,  A61K31/4439 ,  A61K2300/00 ,  A61K31/444 ,  A61K2300/00 ,  A61K31/506 ,  A61K2300/00 ,  A61K31/519 ,  A61K2300/00

Abstract: The present invention relates to compositions, methods and kits for the treatment of respiratory disease. In particular, the compositions, methods and kits are particularly useful, but not limited to, the treatment or prevention of exacerbations of asthma and chronic obstructive pulmonary disease. The present invention provides a method of treating or preventing a respiratory disease in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an inhibitor of casein kinase 1, thereby treating or preventing a respiratory disease in a subject. The present invention also provides a method of treating or preventing a respiratory disease in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an inhibitor of ALK5, thereby treating or preventing a respiratory disease in a subject, wherein the inhibitor is administered directly to the airway and/or lungs. The present invention also provides a method of treating or preventing a condition of the airway or lung involving fibrosis in a subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of an inhibitor of casein kinase 1 or an inhibitor of ALK5, thereby treating or preventing a condition of the airway or lung involving fibrosis in a subject.

公开(公告)号：US11970483B2

公开(公告)日：2024-04-30

申请号：US17280633

申请日：2019-09-27

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Shinobu Sasaki ,  Yasutomi Asano ,  Kazuaki Takami ,  Masaki Seto ,  Haruhi Ando

IPC: C07D405/14 ,  A61P1/10 ,  C07D407/12 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D405/14 ,  A61P1/10 ,  C07D407/12 ,  C07D407/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the formula (I):




wherein R1 is a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, or an optionally substituted C1-6 alkoxy group; and ring A is an optionally further substituted ring, or a salt thereof.

公开(公告)号：US11970480B2

公开(公告)日：2024-04-30

申请号：US17663749

申请日：2022-05-17

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Adam Kenneth Charnley ,  Michael G. Darcy ,  Jason W. Dodson ,  Xiaoyang Dong ,  Terry V. Hughes ,  Jianxing Kang ,  Lara Kathryn Leister ,  Yiqian Lian ,  Yue Li ,  John F. Mehlmann ,  Neysa Nevins ,  Joshi M. Ramanjulu ,  Joseph J. Romano ,  Gren Z. Wang ,  Guosen Ye ,  Daohua Zhang

IPC: C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/22 ,  C07D493/10 ,  C07D498/18 ,  C07F9/6558

CPC classification number: C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D487/22 ,  C07D493/10 ,  C07D498/18 ,  C07F9/65583

Abstract: Disclosed are compounds having the formula:






wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, and R17, are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.

公开(公告)号：US20240132513A1

公开(公告)日：2024-04-25

申请号：US18235753

申请日：2023-08-18

Applicant: AGENEBIO, INC.

Inventor： Belew Mekonnen ,  John A. Butera ,  Jianxing Huang ,  Hemantbhai Patel

IPC: C07D487/14 ,  A61K45/06 ,  A61P25/28 ,  C07D413/14 ,  C07D487/04 ,  C07D498/14 ,  C07D519/00

CPC classification number: C07D487/14 ,  A61K45/06 ,  A61P25/28 ,  C07D413/14 ,  C07D487/04 ,  C07D498/14 ,  C07D519/00

Abstract: Benzazepine derivatives, compositions comprising therapeutically effective amounts of those benzazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders or associated with risk factors for cognitive impairment. In particular, it relates to the use of a α5-containing GABAA R agonist (e.g., a α5-containing GABAA R positive allosteric modulator) in treating cognitive impairment associated with central nervous system (CNS) disorders or having a risk factor associated with cognitive impairment in a subject in need or at risk thereof, including, without limitation, subjects having or at risk for age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI (aMCI), Age-Associated Memory Impairment (AAMI), Age Related Cognitive Decline (ARCD), dementia, Alzheimer's Disease (AD), prodromal AD, post-traumatic stress disorder (PTSD), schizophrenia, bipolar disorder, amyotrophic lateral sclerosis (ALS), cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease (PD), autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of a α5-containing GABAA R agonist (e.g., a α5-containing GABAA R positive allosteric modulator) as described herein in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

公开(公告)号：US20240132480A1

公开(公告)日：2024-04-25

申请号：US18270621

申请日：2022-01-07

Applicant: Cornell University ,  Tri-Institutional Therapeutics Discovery Institute, Inc.

Inventor： John Ginn ,  Shan SUN ,  Mayako Michino ,  Nigel Liverton ,  Rui Liang ,  Peter T. Meinke ,  David Huggins ,  Ruslana Bryk ,  Carl F. Nathan

IPC: C07D403/12 ,  A61P31/06 ,  C07D209/08 ,  C07D209/34 ,  C07D209/42 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D403/12 ,  A61P31/06 ,  C07D209/08 ,  C07D209/34 ,  C07D209/42 ,  C07D231/56 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

Abstract: Disclosed are compounds for inhibiting lipoamide dehydrogenase (Lpd), and methods of treating tuberculosis.

公开(公告)号：US20240132473A1

公开(公告)日：2024-04-25

申请号：US18545582

申请日：2023-12-19

Applicant: Shanghai Xunhe Pharmaceutical Technology Co. Ltd.

Inventor： Nongnong WEI ,  Hua JIN ,  Yongyong ZHENG ,  Feng ZHOU ,  Meihua HUANG

IPC: C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04

Abstract: The present invention relates to the technical field of biomedicine, in particular to a sulfoximide substituted indazole compound, an isomer thereof, or a pharmaceutically acceptable salt thereof. The structure of the sulfoximide substituted indazole compound is shown by formula I: