公开(公告)号：US12128028B2

公开(公告)日：2024-10-29

申请号：US17258273

申请日：2019-07-05

申请人： METRION BIOSCIENCES LIMITED

发明人： Marc Rogers ,  Robert Kirby ,  Gakujun Shomi ,  Takuya Matsuo ,  Satoru Kobayashi ,  Junichiro Kanazawa ,  Nobutaka Yamaoka ,  Makoto Torizuka ,  Koichi Suzawa

IPC分类号： A61K31/4164 ,  A61K31/4178 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/46 ,  A61K31/5377 ,  A61K31/55 ,  C07D233/28 ,  C07D235/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/08 ,  C07D491/107

CPC分类号： A61K31/4164 ,  A61K31/4178 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/46 ,  A61K31/5377 ,  A61K31/55 ,  C07D233/28 ,  C07D235/02 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D471/08 ,  C07D491/107

摘要： The invention relates to heterocyclic sulfonamide derivatives and their use in the treatment and prophylaxis of autoimmune, inflammatory, cardiovascular, neuronal, auditory, renal and metabolic mediated diseases, and to compositions containing said derivatives and processes for their preparation.

公开(公告)号：US20240351999A1

公开(公告)日：2024-10-24

申请号：US18569148

申请日：2022-06-10

申请人： INSTITUTE OF MATERIA MEDICA ,CHINESE ACADEMY OF MEDICAL SCIENCES

发明人： Song WU ,  Wenxuan ZHANG ,  Xintong ZHAO ,  Qingyun YANG ,  Jing FENG ,  Jie ZHANG ,  Chi ZHANG ,  Zunsheng HAN ,  Tianlei LI ,  Jie XIA ,  Kun ZHANG ,  Bo LIU ,  Huihui SHAO ,  Yue WANG ,  Yuhua HU ,  Xinyu LUO ,  Hanyilan ZHANG ,  Xu LIAN ,  Zihao ZHU

IPC分类号： C07D401/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61P31/04 ,  C07D413/14 ,  C07D417/14

CPC分类号： C07D401/14 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K45/06 ,  A61P31/04 ,  C07D413/14 ,  C07D417/14

摘要： The present invention belongs to the technical field of antibacterial drugs, and discloses a pyrrolylacylpiperidylamine compound and use thereof. The present invention in particular relates to a pyrrolylacylpiperidylamine compound and a pharmaceutically acceptable salt thereof, and use thereof in the preparation of a medicament for resisting infections with bacteria, mycoplasma or chlamydia. The compound has a structure shown in the following general formula:

公开(公告)号：US20240350505A1

公开(公告)日：2024-10-24

申请号：US18537061

申请日：2023-12-12

申请人： Repare Therapeutics Inc.

发明人： Michal Zimmermann ,  Anne Roulston ,  Maria Koehler

IPC分类号： A61K31/5377 ,  A61K9/00 ,  A61K31/454 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/541 ,  A61K31/55 ,  A61P35/00

CPC分类号： A61K31/5377 ,  A61K9/0053 ,  A61K31/454 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/541 ,  A61K31/55 ,  A61P35/00

摘要： Disclosed are methods of treating a cancer in a subject using an ATR inhibitor and PARP inhibitor. wherein the cancer has been previously identified as a cancer having a loss of function of ATM, BRCA2, RNAse H2A, RNAse H2B, CDK12, or a combination thereof, or as an ALT+ cancer. Also disclosed are methods of inducing cell death in an aberrant cancer cell having a loss of function of ATM, BRCA2, RNAse H2A, RNAse H2B, CDK12, or a combination thereof, or an ALT+ cancer cell, by contacting the cell with an effective amount of an ATR inhibitor and PARP inhibitor.

公开(公告)号：US20240342185A1

公开(公告)日：2024-10-17

申请号：US18578875

申请日：2022-07-13

申请人： THE SCRIPPS RESEARCH INSTITUTE ,  SHANGPHARMA INNOVATION INC.

发明人： Luke L. LAIRSON ,  Emily CHIN ,  Brett BOOKSER ,  David LAPOINTE

IPC分类号： A61K31/5377 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

CPC分类号： A61K31/5377 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14

摘要： Provided herein are compounds of Formula (I), their pharmaceutically acceptable salts, and their pharmaceutical compositions: (I) wherein R1, R2, R3, L, X, and Ar are defined in the present disclosure. The compounds are inhibitors of cyclic gmp-amp synthase (cGAS) or CGAS-related cGAMP production, and they are useful in treating or preventing inflammatory diseases or conditions in a subject.

公开(公告)号：US20240336604A1

公开(公告)日：2024-10-10

申请号：US18294663

申请日：2022-08-03

申请人： THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPT. OF HEALTH AND HUMAN SERVICES ,  THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL

发明人： Disha GANDHI ,  Kevin FRANKOWSKI ,  Marc FERRER ,  R. Benjamin FREE ,  David R. SIBLEY ,  Amy E. MORITZ ,  Noel Terrence SOUTHALL ,  Xin HU ,  Amber KELLEY

IPC分类号： C07D413/06 ,  A61K31/4025 ,  A61K31/424 ,  A61K31/426 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/416 ,  C07D277/14 ,  C07D401/06 ,  C07D403/06 ,  C07D498/10

CPC分类号： C07D413/06 ,  A61K31/4025 ,  A61K31/424 ,  A61K31/426 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D207/416 ,  C07D277/14 ,  C07D401/06 ,  C07D403/06 ,  C07D498/10

摘要： Compounds of Formula I, Formula II, and Formula III and the pharmaceutically acceptable salts thereof are disclosed. The variables R1-10 are disclosed herein. The compounds are useful for treating central nervous system disorders, especially those involving substance use disorder and/or withdrawal syndrome. Pharmaceutical compositions containing compounds of Formula I or Formula II or Formula III and methods of treatment comprising administering compounds of Formula I or Formula II or Formula III are also disclosed.

公开(公告)号：US20240327393A1

公开(公告)日：2024-10-03

申请号：US18574309

申请日：2022-07-08

申请人： SIRONAX LTD.

发明人： Jianguang HAN ,  Zhiyuan ZHANG ,  Weijie HOU ,  Yimin JIANG ,  Yanping XU

IPC分类号： C07D413/12 ,  A61K31/366 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5415 ,  A61K31/5513 ,  A61K31/553 ,  C07D209/46 ,  C07D217/04 ,  C07D217/06 ,  C07D263/58 ,  C07D277/82 ,  C07D279/16 ,  C07D311/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/08

CPC分类号： C07D413/12 ,  A61K31/366 ,  A61K31/4035 ,  A61K31/416 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/472 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5355 ,  A61K31/536 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5415 ,  A61K31/5513 ,  A61K31/553 ,  C07D209/46 ,  C07D217/04 ,  C07D217/06 ,  C07D263/58 ,  C07D277/82 ,  C07D279/16 ,  C07D311/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/04 ,  C07D498/08

摘要： Provided are compounds of Formula I, compositions comprising the same, and methods of using the same, including use in treating various diseases and conditions, e.g., those involving ferroptosis.

公开(公告)号：US20240325369A1

公开(公告)日：2024-10-03

申请号：US18580583

申请日：2022-07-18

申请人： Janssen Pharmaceutica NV

发明人： Peter Francis ,  Angela Mennicke LOPEZ-GITLITZ ,  Natalie A NUTNICK ,  Gary Edward MASON ,  Xin ZHAO ,  Michael P GORMLEY ,  Yuangen ZHU ,  Karen Ann URTISHAK ,  Shibu THOMAS ,  Adam A Del Corral

IPC分类号： A61K31/454 ,  A61K9/00 ,  A61P35/00

CPC分类号： A61K31/454 ,  A61K9/0053 ,  A61P35/00

摘要： The present invention relates to a method of improving the efficacy of treatment of line 2+ metastatic castration-resistant prostate cancer (mCRPC) with biallelic DNA-repair anomalies in a male human, wherein said biallelic DNA-repair anomalies are selected from: i) BRCA (BRCA1, BRCA2, or a combination thereof), ii) non-BRCA (ATM, FANCA, PALB2, CHEK2, BRIP1, HDAC2, or any combination thereof): or iii) any combination thereof; wherein the male human has received prior taxane-based chemotherapy and androgen receptor (AR)-targeted therapy; said method of improving the efficacy of treatment comprising administering to said male human a once-daily oral dosing of 300 mg niraparib.

公开(公告)号：US20240317729A1

公开(公告)日：2024-09-26

申请号：US18667078

申请日：2024-05-17

申请人： YALE UNIVERSITY ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  CAMBRIDGE ENTERPRISE LIMITED

发明人： CRAIG M. CREWS ,  DENNIS BUCKLEY ,  ALESSIO CIULLI ,  WILLIAM L. JORGENSEN ,  PETER C. GAREISS ,  INGE VAN MOLLE ,  JEFFREY GUSTAFSON ,  HYUN-SEOP TAE ,  JULIEN MICHEL ,  DENTON WADE HOYER ,  ANKE G. ROTH ,  JOHN DAVID HARLING ,  IAN EDWARD DAVID SMITH ,  AFJAL HUSSAIN MIAH ,  SEBASTIEN ANDRE CAMPOS ,  JOELLE LE

IPC分类号： C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/00 ,  C12N9/00

CPC分类号： C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/003 ,  C12N9/93

摘要： The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. 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 a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

公开(公告)号：US20240316025A1

公开(公告)日：2024-09-26

申请号：US18732162

申请日：2024-06-03

申请人： Terns Pharmaceuticals, Inc.

发明人： Martijn FENAUX ,  Kevin KLUCHER ,  Christopher T. JONES ,  Thorsten A. KIRSCHBERG

IPC分类号： A61K31/454 ,  A61K31/4439 ,  A61K31/4748 ,  A61K31/53 ,  A61K31/575 ,  A61P1/16

CPC分类号： A61K31/454 ,  A61K31/4439 ,  A61K31/4748 ,  A61K31/53 ,  A61K31/575 ,  A61P1/16

摘要： Provided herein are methods for treating liver disorders, including non-alcoholic steatohepatitis, and symptoms and manifestations thereof, in a patient which utilize, among others, a combination treatment of an FXR agonist and a THRβ agonist.

公开(公告)号：US20240307375A1

公开(公告)日：2024-09-19

申请号：US18574883

申请日：2022-06-22

申请人： OSAKA UNIVERSITY ,  KYOTO UNIVERSITY

发明人： Ryu NAGATA ,  Yoshitaka ISAKA ,  Takeshi YAMAMOTO ,  Hiroaki YONISHI ,  Tamotsu YOSHIMORI ,  Maho HAMASAKI ,  Yasuo MORI

IPC分类号： A61K31/496 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4995

CPC分类号： A61K31/496 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4995

摘要： An object of this invention is to provide a pharmaceutical composition for preventing and/or treating acute kidney injury, and an autophagy activator. The invention relates to, for example, a pharmaceutical composition for preventing and/or treating acute kidney injury, comprising a compound represented by formula (1), a salt thereof, or a prodrug thereof:






wherein
A is an optionally substituted benzene ring;
B is an optionally substituted aryl or an optionally substituted heteroaryl;
X is an oxygen atom or a sulfur atom; Y is a nitrogen atom or a carbon atom;
of is a single or double bond when Y is a carbon atom, or
of is a single bond when Y is a nitrogen atom;
each R1 independently represents lower alkyl, or
two R1s may be bound to each other to form a spiro ring or a crosslinked structure, or
two R1s may be bound to each other to form a saturated fused heterocycle together with nitrogen and carbon atoms constituting a ring containing Y;
p is 0, 1, or 2; or
(R1)p is oxo.