公开(公告)号：US20240360104A1

公开(公告)日：2024-10-31

申请号：US18553988

申请日：2022-04-26

申请人： Dana-Farber Cancer Institute, Inc.

发明人： Nathanael S. Gray ,  Tinghu Zhang ,  Mengyang Fan ,  Jianwei Che ,  Wenchao Lu ,  Sirano Dhe-Paganon ,  Nicholas Paul Kwiatkowski

IPC分类号： C07D403/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D495/04

CPC分类号： C07D403/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D495/04

摘要： Provided herein are compounds of Formula (I′), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), or Formula (VIII) and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, or prodrugs thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.

公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

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

发明人： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC分类号： C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

摘要： The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

公开(公告)号：US20240350468A1

公开(公告)日：2024-10-24

申请号：US18751439

申请日：2024-06-24

申请人： AICURIS GMBH & CO. KG

发明人： Yogeshwar BACHHAV ,  Wilfried SCHWAB ,  Alexander BIRKMANN ,  Susanne BONSMANN ,  Thomas GOLDNER

IPC分类号： A61K31/4439 ,  A61K9/00 ,  A61K45/06 ,  C07D417/12

CPC分类号： A61K31/4439 ,  A61K9/0014 ,  A61K45/06 ,  C07D417/12

摘要： The present invention relates to the field of anti-viral active agents, particularly to salts, more particularly to a maleate salt of the free base of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]-acetamide, to pharmaceutical formulations thereof as well as to methods for the production of these salts. The present invention also relates to the use of theses salts and of respective pharmaceutical formulations thereof in methods of treatment and/or prevention of human herpes simplex virus infections, particularly infections caused by HSV-1 and HSV-2.

公开(公告)号：US12121511B2

公开(公告)日：2024-10-22

申请号：US17159485

申请日：2021-01-27

申请人： Gilead Sciences, Inc.

发明人： Stephen E. Ammann ,  Gediminas J. Brizgys ,  James S. Cassidy ,  Elbert Chin ,  Chienhung Chou ,  Jeromy J. Cottell ,  Chao-I Hung ,  Kavoos Kolahdouzan ,  Daniel G. Shore ,  Suzanne M. Szewczyk ,  James G. Taylor ,  Rhiannon Thomas-Tran ,  Nathan E. Wright ,  Zheng-Yu Yang

IPC分类号： A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D471/04 ,  C07D493/04 ,  C07D493/10 ,  C07D498/04

CPC分类号： A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D471/04 ,  C07D493/04 ,  C07D493/10 ,  C07D498/04

摘要： The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition.

公开(公告)号：US20240342176A1

公开(公告)日：2024-10-17

申请号：US18292362

申请日：2022-07-27

申请人： GUANGZHOU JOYO PHARMATECH CO., LTD ,  SHANGHAI JIA TAN PHARMATECH CO., LTD.

发明人： Yongguo Li ,  Wei Wei ,  Wei Ye

IPC分类号： A61K31/519 ,  A61K31/4439 ,  A61K39/00 ,  A61P35/00

CPC分类号： A61K31/519 ,  A61K31/4439 ,  A61P35/00 ,  A61K2039/505

摘要： A pharmaceutical combination and an application thereof. The pharmaceutical combination comprises a PI3K inhibitor and an immune checkpoint inhibitor, wherein the PI3K inhibitor is selected from a compound represented by formula (I), linperlisib, samotolisib, copanlisib, SHC014748M, pilaralisib, buparlisib, taselisib, YZJ-0673, gedatolisib, omipalisib, bimiralisib, voxtalisib, AL58805, and HEC68498, and pharmaceutically acceptable salts thereof, and the immune checkpoint inhibitor is a PD-1/PD-L1 inhibitor. The compound represented by formula (Ia) has a high inhibitory effect on PI3Kδ and PI3Kγ kinases, and the pharmaceutical combination uses a PI3K inhibitor and a PD-1 inhibitor in combination, thereby effectively improving the inhibitory effect on tumors, and solving the problem of drug resistance of PD-1/PD-L1 inhibitors.

公开(公告)号：US12110263B2

公开(公告)日：2024-10-08

申请号：US17740260

申请日：2022-05-09

申请人： CORTEXYME, INC.

发明人： Andrei W. Konradi ,  Robert A. Galemmo, Jr. ,  Stephen S. Dominy ,  Casey C. Lynch ,  Leslie J. Holsinger

IPC分类号： C07C233/62 ,  A61K31/165 ,  A61K31/167 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/655 ,  A61K45/06 ,  A61P25/00 ,  A61P31/04 ,  C07B59/00 ,  C07C233/78 ,  C07C235/10 ,  C07C235/50 ,  C07C237/42 ,  C07C245/08 ,  C07C247/16 ,  C07C247/18 ,  C07C317/28 ,  C07C323/40 ,  C07C323/42 ,  C07C381/00 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D257/04 ,  C07D261/12 ,  C07D401/12 ,  C07D413/12 ,  C07F5/02

CPC分类号： C07C233/62 ,  A61K31/165 ,  A61K31/167 ,  A61K31/41 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4439 ,  A61K31/505 ,  A61K31/513 ,  A61K31/655 ,  A61K45/06 ,  A61P25/00 ,  A61P31/04 ,  C07B59/001 ,  C07C233/78 ,  C07C235/10 ,  C07C235/50 ,  C07C237/42 ,  C07C245/08 ,  C07C247/16 ,  C07C247/18 ,  C07C317/28 ,  C07C323/40 ,  C07C323/42 ,  C07C381/00 ,  C07D213/65 ,  C07D213/68 ,  C07D213/70 ,  C07D213/81 ,  C07D213/82 ,  C07D239/34 ,  C07D239/36 ,  C07D239/38 ,  C07D257/04 ,  C07D261/12 ,  C07D401/12 ,  C07D413/12 ,  C07F5/02 ,  C07C2601/08

摘要： The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.

公开(公告)号：US20240327427A1

公开(公告)日：2024-10-03

申请号：US18249829

申请日：2021-10-22

申请人： Icahn School of Medicine at Mount Sinai

发明人： Bin Zhang ,  Jian Jin ,  Husnu Umit Kaniskan ,  Lihuai Qin ,  Minghui Wang ,  Aiqun Li ,  Kristen J. Brennand ,  Eric E. Schadt ,  Vahram Haroutunian ,  Lap Ho ,  Xianxiao Zhou ,  Zhenyu Yue

IPC分类号： C07D513/04 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61P25/28 ,  C07D277/46 ,  C07D277/82 ,  C07D417/04

CPC分类号： C07D513/04 ,  A61K31/426 ,  A61K31/427 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61P25/28 ,  C07D277/46 ,  C07D277/82 ,  C07D417/04

摘要： Disclosed herein are novel drugs useful in treating Alzheimer's Disease and methods of use.

公开(公告)号：US20240327354A1

公开(公告)日：2024-10-03

申请号：US18579953

申请日：2022-07-22

申请人： INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE ,  INSTITUT PASTEUR DE LILLE ,  UNIVERSITÉ DE LILLE ,  CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE ,  CHRU DE LILLE ,  JOHANN WOLFGANG GOETHE-UNIVERSITÄT FRANKFURT AM MAIN

发明人： Anaïs VIEIRA DA CRUZ ,  Coline PLÉ ,  Marion FLIPO ,  Nina COMPAGNE ,  Nicolas WILLAND ,  Heng-Keat TAM ,  Juan Carlos JIMÉNEZ CASTELLANOS ,  Klaas Martinus POS ,  Ruben Christiaan HARTKOORN ,  Reinke Tobias MÜLLER

IPC分类号： C07D213/74 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D213/80 ,  C07D215/38 ,  C07D217/22 ,  C07D241/44 ,  C07D295/073 ,  C07D401/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

CPC分类号： C07D213/74 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/496 ,  A61K31/498 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D213/80 ,  C07D215/38 ,  C07D217/22 ,  C07D241/44 ,  C07D295/073 ,  C07D401/04 ,  C07D413/04 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

摘要： The present invention concerns novel Gram-negative bacteria efflux pump inhibitors. It further relates to the use of Gram-negative bacteria efflux pump inhibitors to prevent and/or treat antibiotic resistance by potentiating the activity of antibiotics. Infections by multidrug resistant (MDR) Gram-negative bacteria are a major threat to global healthcare. The inventors have discovered a novel class of Resistance Nodulation cell Division-efflux pump inhibitors. The inventors tested the effects of these inhibitors on growth inhibition of different bacteria as well as their impact on the boosting of antibiotic activity in different bacteria. Particularly, the inventors tested the effects of these inhibitors on E. coli, A. baumamnii, K. pneumoniae and P. aeruginosa.

公开(公告)号：US20240325487A1

公开(公告)日：2024-10-03

申请号：US18381799

申请日：2023-10-19

申请人： Ardelyx, Inc.

发明人： Dominique Charmot ,  Jason G. Lewis ,  Jeffrey W. Jacobs ,  Ingrid Langsetmo ,  Christopher Carreras

IPC分类号： A61K38/10 ,  A61K31/00 ,  A61K31/195 ,  A61K31/27 ,  A61K31/352 ,  A61K31/353 ,  A61K31/382 ,  A61K31/4045 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/475 ,  A61K31/506 ,  A61K31/7072 ,  A61K33/26 ,  A61K38/16 ,  A61K45/06 ,  G01N33/50 ,  G01N33/84

CPC分类号： A61K38/10 ,  A61K31/00 ,  A61K31/195 ,  A61K31/27 ,  A61K31/352 ,  A61K31/353 ,  A61K31/382 ,  A61K31/4045 ,  A61K31/421 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/475 ,  A61K31/506 ,  A61K31/7072 ,  A61K33/26 ,  A61K38/16 ,  A61K45/06 ,  G01N33/5038 ,  G01N33/5044 ,  G01N33/84

摘要： Provided are non-NHE3-binding agents having activity as phosphate transport/uptake inhibitors in the gastrointestinal tract, including in the small intestine, methods for their use as therapeutic or prophylactic agents, and related methods of drug discovery.

公开(公告)号：US20240325364A1

公开(公告)日：2024-10-03

申请号：US18578659

申请日：2022-07-08

申请人： Nottingham Trent University

发明人： Mark Duncan Turner ,  Alun Christopher Garner

IPC分类号： A61K31/4439 ,  A61K31/4174 ,  A61K31/42 ,  A61K31/443 ,  A61P3/04

CPC分类号： A61K31/4439 ,  A61K31/4174 ,  A61K31/42 ,  A61K31/443 ,  A61P3/04

摘要： The invention provides a compound of Formula (I) or a tautomer, isomer, prodrug, metal complex, or pharmaceutically acceptable salt thereof for use in the treatment of a metabolic disorder or for inducing weight loss: wherein R1 is: H; a straight or branched alkyl; a straight or branched alkyl substituted with at least one moiety selected from the group comprising: halogen, hydroxy, alkoxy, NH2, mono- or disubstituted amino, thiol, and phosphine; aryl; aralkyl; hydroxy; alkoxy; aryloxy; arylalkoxy; NH2; mono- or disubstituted amino; or halogen; X is: CH or N; L is absent or present, and when present is: an optionally substituted straight or branched C1-C10 alkyl, optionally containing one or more rings, and/or optionally containing one or more double bonds; and Ar is: an optionally substituted 5-membered unsaturated heterocyclic ring.