公开(公告)号：US20240360151A1

公开(公告)日：2024-10-31

申请号：US18602519

申请日：2024-03-12

Applicant: SANOFI

Inventor： Jean-Philippe LETALLEC ,  Franck Marguet ,  Fréderic Petit ,  Baptiste Ronan ,  Corinne Terrier

IPC: C07D498/10 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/553 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

CPC classification number: C07D498/10 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/541 ,  A61K31/553 ,  C07D401/04 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/04

Abstract: The present invention relates to a compound of formula (I) wherein n is 1 or 2, R1 is halogen, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, ethynyl, propargyl, or (C3-C6)cycloalkyl, or two R1 form a cyclopentane ring fused to the phenol; R2 and R3 represent H, cyano, ethynyl, propargyl, (C1-C4)alkyl, hydroxy(C1-C4)alkyl or a halo(C1-C4)alkyl, or R2 and R3 form together with the atoms connecting them a (C5-C6)carbocyclic ring fused to the pyridazine ring; R4 and R5 form together with N to which they are attached an optionally substituted 3-7 membered monocyclic heterocycloalkyl ring, 8-11 membered bicyclic heterocycloalkyl ring or 7-12 membered bicyclic heterocyclic spiro ring. The present invention also relates to a medicament and a pharmaceutical composition comprising said compound of formula (I), as well as their therapeutic uses, in particular as inhibitor of NOD-like receptor protein 3 inflammasome for treating for example Parkinson's disease or frontotemporal Dementia.

公开(公告)号：US20240300939A1

公开(公告)日：2024-09-12

申请号：US18568899

申请日：2022-06-13

Applicant: Scorpion Therapeutics, Inc.

Inventor： David St. Jean, Jr. ,  Maxwell David Cummings

IPC: C07D417/12 ,  A61K31/343 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/427 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D307/81 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/10

CPC classification number: C07D417/12 ,  A61K31/343 ,  A61K31/381 ,  A61K31/382 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/427 ,  A61K31/437 ,  A61K31/443 ,  A61K31/4525 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  C07D307/81 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/10

Abstract: This disclosure provides compounds of Formula (I), Formula (II), and pharmaceutically acceptable salts thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Ka). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) PI3Ka activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

公开(公告)号：US12060367B2

公开(公告)日：2024-08-13

申请号：US18314445

申请日：2023-05-09

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： Joachim Broeker ,  Jason Abbott ,  Jianwen Cui ,  Stephen W. Fesik ,  Julian Fuchs ,  Andreas Gollner ,  Lorenz Herdeis ,  Tim Hodges ,  Andrew Little ,  Andreas Mantoulidis ,  Jason Phan ,  Juergen Ramharter ,  Dhruba Sarkar ,  Christian Alan Paul Smethurst ,  Kevin Sokol ,  Heinz Stadtmueller ,  Qi Sun ,  Matthias Treu ,  Alex Waterson ,  Birgit Wilding ,  Tobias Wunberg

IPC: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

Abstract: The present invention encompasses compounds of formula (I)






wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US12037324B2

公开(公告)日：2024-07-16

申请号：US17861809

申请日：2022-07-11

Applicant: Université de Montréal ,  Bristol-Myers Squibb Company

Inventor： Eldon Scott Priestley ,  Samuel Kaye Reznik ,  Edward H. Ruediger ,  James R. Gillard ,  Oz Scott Halpern ,  Wen Jiang ,  Jeremy Richter ,  Rejean Ruel ,  Sasmita Tripathy ,  Wu Yang ,  Xiaojun Zhang

IPC: C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

CPC classification number: C07D401/14 ,  A61K31/41 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/501 ,  A61P9/04 ,  C07D233/90 ,  C07D235/26 ,  C07D239/20 ,  C07D257/04 ,  C07D271/07 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D498/10

Abstract: The present invention provides compounds of Formula (I):




wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are biased agonists, or β-Arrestin agonists of the angiotensin II receptor, which may be used as medicaments.

公开(公告)号：US20240226114A1

公开(公告)日：2024-07-11

申请号：US18477240

申请日：2023-09-28

Applicant: Vividion Therapeutics, Inc.

Inventor： David WEINSTEIN ,  Jason GREEN ,  Shota KIKUCHI ,  Donald C ROGNESS ,  Philip ALIBI ,  Matthew PATRICELLI ,  Nilotpal ROY ,  I-Chung LO

IPC: A61K31/553 ,  A61K31/496 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61P35/00 ,  C07D241/04 ,  C07D265/30 ,  C07D265/34 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/10

CPC classification number: A61K31/553 ,  A61K31/496 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61P35/00 ,  C07D241/04 ,  C07D265/30 ,  C07D265/34 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D405/10 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/10

Abstract: Compounds and methods for inhibiting Nrf2 by activating KEAP1.

公开(公告)号：US20240190821A1

公开(公告)日：2024-06-13

申请号：US18275382

申请日：2022-02-01

Applicant: Triana Biomedicines, Inc.

Inventor： William J. Greenlee ,  Nicholas Calandra ,  Soumya Ray ,  Arthur F. Kluge

IPC: C07D209/40 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D471/18 ,  C07D487/04 ,  C07D487/10 ,  C07D498/10

CPC classification number: C07D209/40 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04 ,  C07D471/18 ,  C07D487/04 ,  C07D487/10 ,  C07D498/10

Abstract: The present application discloses novel compounds of formula (I), pharmaceutical compositions containing these compounds and methods of inducing degradation of a protein, comprising contacting the protein with an effective amount of a compound of the disclosure. Methods of treating disease and disorders that results from abnormal activity of a target protein in a subject, are also disclosed.

公开(公告)号：US11999694B2

公开(公告)日：2024-06-04

申请号：US17976150

申请日：2022-10-28

Applicant: Sensorium Therapeutics, Inc.

Inventor： Jacob M. Hooker ,  Michael S. Placzek

IPC: C07D209/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D475/04 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D519/00 ,  C07F7/18

CPC classification number: C07D209/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D475/04 ,  C07D491/113 ,  C07D491/20 ,  C07D495/04 ,  C07D495/10 ,  C07D497/10 ,  C07D498/10 ,  C07D519/00 ,  C07F7/1804

Abstract: Disclosed are prodrug compounds that can be converted to mesembrine under biologically relevant conditions, such as hydrolysis in vivo; and related methods of preparing and using these compounds. Stable preparations of isolated mesembrine stereoisomers are also provided.

公开(公告)号：US20240174690A1

公开(公告)日：2024-05-30

申请号：US18314445

申请日：2023-05-09

Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH ,  VANDERBILT UNIVERSITY

Inventor： Joachim BROEKER ,  Jason ABBOTT ,  Jianwen CUI ,  Stephen W. FESIK ,  Julian FUCHS ,  Andreas GOLLNER ,  Lorenz HERDEIS ,  Tim HODGES ,  Andrew LITTLE ,  Andreas MANTOULIDIS ,  Jason PHAN ,  Juergen RAMHARTER ,  Dhruba SARKAR ,  Christian Alan Paul SMETHURST ,  Kevin SOKOL ,  Heinz STADTMUELLER ,  Qi SUN ,  Matthias TREU ,  Alex WATERSON ,  Birgit WILDING ,  Tobias WUNBERG

IPC: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

CPC classification number: C07D498/10 ,  A61P1/00 ,  A61P1/18 ,  A61P11/00 ,  A61P17/00 ,  A61P35/00 ,  C07D519/00

Abstract: The present invention encompasses compounds of formula (I)




wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V and W have the meanings given in the claims and specification, their use as inhibitors of KRAS, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US11981683B2

公开(公告)日：2024-05-14

申请号：US17699082

申请日：2022-03-19

Applicant: Arvinas Operations, Inc.

Inventor： Erika Marina Vieira Araujo ,  Michael Berlin ,  Hanqing Dong ,  Steven M. Sparks ,  Jing Wang ,  Wei Zhang

IPC: C07D401/14 ,  A61K45/06 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D498/10

CPC classification number: C07D498/10 ,  A61K45/06 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10

Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20240131023A1

公开(公告)日：2024-04-25

申请号：US18460063

申请日：2023-09-01

Applicant: Arvinas Operations, Inc.

Inventor： LAWRENCE B. Snyder ,  Andrew P. Crew ,  Jing Wang ,  Hanqing Dong

IPC: A61K31/496 ,  A61K31/167 ,  A61K31/277 ,  A61K31/337 ,  A61K31/417 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/57 ,  A61K31/661 ,  A61K31/663 ,  A61K31/675 ,  A61K38/09 ,  A61K47/54 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/10

CPC classification number: A61K31/496 ,  A61K31/167 ,  A61K31/277 ,  A61K31/337 ,  A61K31/417 ,  A61K31/4523 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/57 ,  A61K31/661 ,  A61K31/663 ,  A61K31/675 ,  A61K38/09 ,  A61K47/545 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D498/10

Abstract: This disclosure pertains to compounds, the preparation thereof, and the use of these compounds in the treatment of prostate cancer, including metastatic and/or castrate-resistant prostate cancer, in subjects in need thereof.