公开(公告)号：US20240300892A1

公开(公告)日：2024-09-12

申请号：US18484675

申请日：2023-10-11

申请人： Amgen Inc.

发明人： Michael D. Bartberger ,  Ana Gonzalez Buenrostro ,  Hilary Plake Beck ,  Xiaoqi Chen ,  Richard Victor Connors ,  Jeffrey Deignan ,  Jason A. Duquette, I ,  John Eksterowicz ,  Benjamin Fisher ,  Brian M. Fox ,  Jiasheng Fu ,  Zice Fu ,  Felix Gonzalez Lopez De Turiso ,  Michael W. Gribble ,  Darin J. Gustin ,  Julie A. Heath ,  Xin Huang ,  XianYun Jiao ,  Michael G. Johnson ,  Frank Kayser ,  David John Kopecky ,  SuJen Lai ,  Yihong Li ,  Zhihong Li ,  Jiwen Liu ,  Jonathan D. Low ,  Brian S. Lucas ,  Zhihua MA ,  Lawrence R. McGee ,  Joel McIntosh ,  Dustin L. McMinn ,  Julio C. Medina ,  Jeffrey Thomas Mihalic ,  Steven H. Olson ,  Yossup Rew ,  Philip M. Roveto ,  Daqing Sun ,  Xiaodong Wang ,  Yingcai Wang ,  Xuelei Yan ,  Ming Yu ,  Jiang Zhu

IPC分类号： C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

CPC分类号： C07D211/76 ,  C07D221/20 ,  C07D279/02 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D407/04 ,  C07D407/06 ,  C07D409/04 ,  C07D409/12 ,  C07D413/06 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/10 ,  C07D491/08 ,  C07D491/153 ,  C07D498/08 ,  C07D498/14 ,  C07D498/20

摘要： The present invention provides MDM2 inhibitor compounds of Formula I,






wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.

公开(公告)号：US20240246931A1

公开(公告)日：2024-07-25

申请号：US18556846

申请日：2022-04-22

申请人： JUBILANT PRODEL LLC

发明人： Naveen SADHU ,  Dhanalakshmi SIVANANDHAN ,  Zainuddin MOHD ,  Sridharan RAJAGOPAL

IPC分类号： C07D401/12 ,  A61K45/06 ,  C07D205/04 ,  C07D207/08 ,  C07D211/22 ,  C07D221/20 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

CPC分类号： C07D401/12 ,  A61K45/06 ,  C07D205/04 ,  C07D207/08 ,  C07D211/22 ,  C07D221/20 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04

摘要： The present invention relates in general, to the field of pharmaceutical compounds, more particularly to the compounds of Formula (I) which acts as inhibitors for PD1/PD-L1 interaction. The present invention further relates to a method of preparation of compounds of Formula (I). The present invention also relates to a composition of compounds of Formula (I).

公开(公告)号：US12024498B2

公开(公告)日：2024-07-02

申请号：US17986325

申请日：2022-11-14

申请人： OHIO STATE INNOVATION FOUNDATION

发明人： Daniel W. Conroy ,  Christopher P. Jaroniec

IPC分类号： C07D401/12 ,  C07D211/94 ,  C07D221/20 ,  C07D491/20 ,  G01N24/12 ,  G01R33/62

CPC分类号： C07D401/12 ,  C07D211/94 ,  C07D221/20 ,  C07D491/20 ,  G01N24/12 ,  G01R33/62

摘要： Disclosed are methods for performing dynamic nuclear polarization using the polarizing agents described herein. In general, the methods involve (a) providing a frozen sample in a magnetic field, wherein the frozen sample includes a polarizing agent described herein and an analyte with at least one spin half nucleus; (b) polarizing the at least one spin half nucleus of the analyte by irradiating the frozen sample with radiation having a frequency that excites electron spin transitions in the polarizing agent; (c) optionally melting the sample to produce a molten sample; and (d) detecting nuclear spin transitions in the at least one spin half nucleus of the analyte in the frozen or molten sample. In certain embodiments, the polarizing agents can be peptide-based. In these embodiments, the polarizing agents can be readily prepared by solid-phase peptide synthesis.

公开(公告)号：US20240140919A1

公开(公告)日：2024-05-02

申请号：US18526983

申请日：2023-12-01

申请人： Denali Therapeutics Inc.

发明人： Robert A. Craig II, II ,  Javier de Vicente Fidalgo ,  Anthony A. Estrada ,  Jianwen A. Feng ,  Brian M. Fox ,  Katrina W. Lexa ,  Maksim Osipov ,  Zachary K. Sweeney ,  Arun Tottumkara

IPC分类号： C07D271/07 ,  C07C235/22 ,  C07C255/46 ,  C07D205/04 ,  C07D205/12 ,  C07D209/52 ,  C07D211/58 ,  C07D221/20 ,  C07D233/32 ,  C07D401/04 ,  C07D413/04

CPC分类号： C07D271/07 ,  C07C235/22 ,  C07C255/46 ,  C07D205/04 ,  C07D205/12 ,  C07D209/52 ,  C07D211/58 ,  C07D221/20 ,  C07D233/32 ,  C07D401/04 ,  C07D413/04

摘要： The present disclosure relates generally to eukaryotic initiation factor 2B modulators of formula A, or a pharmaceutically acceptable salt, stereoisomer, or mixture of stereoisomers thereof and methods of making and using thereof.

公开(公告)号：US11952347B2

公开(公告)日：2024-04-09

申请号：US17539679

申请日：2021-12-01

申请人： Arvinas Operations, Inc.

发明人： Andrew P. Crew ,  Lawrence B. Snyder ,  Jing Wang

IPC分类号： C07D401/14 ,  A61K31/02 ,  A61K31/166 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D233/42 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04

CPC分类号： C07D233/42 ,  A61K31/02 ,  A61K31/166 ,  A61K31/277 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61K47/10 ,  C07D205/04 ,  C07D209/48 ,  C07D211/76 ,  C07D213/72 ,  C07D221/20 ,  C07D231/12 ,  C07D237/08 ,  C07D239/24 ,  C07D241/04 ,  C07D401/04 ,  C07D401/14

摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 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 disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US20230414585A1

公开(公告)日：2023-12-28

申请号：US18215887

申请日：2023-06-29

申请人： Valo Health, Inc.

发明人： Xiaozhang Zheng ,  Pui Yee Ng ,  Mary-Margaret Zablocki

IPC分类号： A61K31/438 ,  C07D401/04 ,  C07D221/20 ,  C07D401/06 ,  C07D209/54

CPC分类号： A61K31/438 ,  C07D401/04 ,  C07D221/20 ,  C07D401/06 ,  C07D209/54 ,  A61P25/14

摘要： The present invention is directed to inhibitors of histone deacetylases (HDACs) such as HDAC6, and their use in the treatment of diseases such as cell proliferative diseases (e.g., cancer), neurological (e.g., neurodegenerative disease or neurodevelopmental disease), inflammatory or autoimmune disease, infection, metabolic disease, hematologic disease, or cardiovascular disease.

公开(公告)号：US20230331681A1

公开(公告)日：2023-10-19

申请号：US18213055

申请日：2023-06-22

申请人： Arvinas Operations, Inc.

发明人： Michael BERLIN ,  Andrew P. CREW ,  Craig M. CREWS ,  Hanqing DONG ,  Keith R. HORNBERGER ,  Lawrence B. SNYDER ,  Jing WANG ,  Kurt ZIMMERMANN

IPC分类号： C07D233/42 ,  A61K31/166 ,  C07D211/76 ,  C07D241/04 ,  C07D231/12 ,  C07D213/72 ,  C07D205/04 ,  C07D237/08 ,  C07D239/24 ,  C07D221/20 ,  A61K31/277 ,  A61K47/10 ,  A61K31/02 ,  A61K31/497 ,  C07D209/48 ,  C07D401/14 ,  A61K45/06 ,  A61K31/506 ,  A61K31/496 ,  A61K31/501 ,  C07D401/04

CPC分类号： C07D233/42 ,  A61K31/166 ,  C07D211/76 ,  C07D241/04 ,  C07D231/12 ,  C07D213/72 ,  C07D205/04 ,  C07D237/08 ,  C07D239/24 ,  C07D221/20 ,  A61K31/277 ,  A61K47/10 ,  A61K31/02 ,  A61K31/497 ,  C07D209/48 ,  C07D401/14 ,  A61K45/06 ,  A61K31/506 ,  A61K31/496 ,  A61K31/501 ,  C07D401/04

摘要： The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 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 disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.

公开(公告)号：US20230234958A1

公开(公告)日：2023-07-27

申请号：US18066551

申请日：2022-12-15

申请人： Relay Therapeutics, Inc. ,  D. E. Shaw Research, LLC.

发明人： Alexander M. Taylor ,  Andre Lescarbbeau ,  Elizabeth H. Kelley ,  Kelley C. Shortsleeves ,  W. Patrick Walters ,  Mark Andrew Murcko ,  Thomas H. McLean ,  Hakan Gunaydin ,  Fabrizio Giordanetto ,  Eric Therrien

IPC分类号： C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00 ,  C07D221/20 ,  C07D401/12 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04

CPC分类号： C07D487/04 ,  C07D401/04 ,  C07D401/14 ,  C07D519/00 ,  C07D221/20 ,  C07D401/12 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107 ,  C07D513/04

摘要： The present disclosure relates to novel compounds including formula (X) and pharmaceutical compositions thereof, and methods for inhibiting the activity of SHP2 phosphatase with the compounds and compositions of the disclosure. The present disclosure further relates to, but is not limited to, methods for treating disorders associated with SHP2 deregulation with the compounds and compositions of the disclosure.

公开(公告)号：US20230102879A1

公开(公告)日：2023-03-30

申请号：US17573405

申请日：2022-01-11

申请人： President and Fellows of Harvard College

发明人： Daniel E. Kahne ,  Vadim Baidin

IPC分类号： C07F5/02 ,  A61P31/04 ,  C07C211/27 ,  C07C211/40 ,  C07C215/28 ,  C07D209/04 ,  C07D213/38 ,  C07D213/643 ,  C07D215/06 ,  C07D215/12 ,  C07D221/04 ,  C07D221/20 ,  C07D231/12 ,  C07D231/56 ,  C07D239/26 ,  C07D239/34 ,  C07D261/08 ,  C07D267/10 ,  C07D295/13 ,  C07D307/14 ,  C07D307/79 ,  C07D307/87 ,  C07D309/04 ,  C07D311/74 ,  C07D317/58 ,  C07D319/08 ,  C07D327/06 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08 ,  C07D495/04 ,  C07D498/08

摘要： Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.

公开(公告)号：US20220380314A1

公开(公告)日：2022-12-01

申请号：US17760878

申请日：2020-09-17

申请人： Bial - R&D Investments, S.A. ,  Fondazione Istituto Italiano di Tecnologia

发明人： Renato T. Skerlj ,  Elyse Marie Josee Bourque ,  Soumya Ray ,  Rita Scarpelli ,  Vincenzo Cilibrasi

IPC分类号： C07D217/06 ,  C07D401/10 ,  C07D215/08 ,  C07D241/38 ,  C07D471/04 ,  C07D265/36 ,  C07D498/10 ,  C07D215/233 ,  C07D211/16 ,  C07D211/28 ,  C07D211/48 ,  C07D401/04 ,  C07D405/10 ,  C07D265/30 ,  C07D207/06 ,  C07D221/20 ,  C07D209/54 ,  C07D265/34 ,  C07D211/70 ,  C07C275/26 ,  C07D471/08 ,  C07D405/12 ,  C07D241/20 ,  C07D265/32 ,  C07C271/16 ,  C07D451/06

摘要： The invention provides substituted, saturated and unsaturated N-heterocyclic carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.