公开(公告)号：US20240327427A1

公开(公告)日：2024-10-03

申请号：US18249829

申请日：2021-10-22

Applicant: Icahn School of Medicine at Mount Sinai

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

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

Abstract: 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

Applicant: 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

Inventor： 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: 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 classification number: 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

Abstract: 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

Applicant: Ardelyx, Inc.

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

IPC: 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 classification number: 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

Abstract: 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

Applicant: Nottingham Trent University

Inventor： Mark Duncan Turner ,  Alun Christopher Garner

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

CPC classification number: A61K31/4439 ,  A61K31/4174 ,  A61K31/42 ,  A61K31/443 ,  A61P3/04

Abstract: 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.

公开(公告)号：US12102625B2

公开(公告)日：2024-10-01

申请号：US18051471

申请日：2022-10-31

Applicant: Gilead Sciences, Inc.

Inventor： Derek M. Dalton ,  Peter C. Fung ,  Nolan Griggs ,  Jeffrey N. Hemenway ,  Olga V. Lapina ,  Matthew M. Logan ,  Sean T. Neville ,  Bryan J. Reynolds ,  Hui-Wen Shih ,  Anna M. Wagner

IPC: A61K31/4439 ,  C07D401/14 ,  C07D413/14

CPC classification number: A61K31/4439 ,  C07D401/14 ,  C07D413/14

Abstract: Disclosed herein are novel solid forms of FXR agonists. The disclosure also relates to pharmaceutical compositions containing one or more of the solid forms disclosed herein, as well as methods of using the solid forms in the treatment of conditions mediated by FXR. The disclosure also relates to methods for obtaining such solid forms.

公开(公告)号：US20240317708A1

公开(公告)日：2024-09-26

申请号：US18573802

申请日：2022-06-30

Applicant: ZEDIRA GMBH

Inventor： Ralf PASTERNACK ,  Christian BÜCHOLD ,  Martin HILS ,  Martin STIELER ,  Uwe GERLACH

IPC: C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

CPC classification number: C07D401/12 ,  A61K31/4375 ,  A61K31/44 ,  A61K31/443 ,  A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/4748 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  C07D213/75 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

Abstract: The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases, in particular transglutaminase 2.

公开(公告)号：US20240316021A1

公开(公告)日：2024-09-26

申请号：US18736166

申请日：2024-06-06

Applicant: Innovative Molecules GmbH

Inventor： Gerald KLEYMANN ,  Christian GEGE

IPC: A61K31/4439 ,  A61K31/426 ,  A61K45/06 ,  A61P31/22 ,  C07D277/46 ,  C07D417/12

CPC classification number: A61K31/4439 ,  A61K31/426 ,  A61K45/06 ,  A61P31/22 ,  C07D277/46 ,  C07D417/12

Abstract: The present invention relates to novel antiviral compounds with specific stereoconfiguration, especially to specific novel enantiomers, to a process for their preparation and to their use as medicaments, in particular as antiviral medicaments.

公开(公告)号：US20240316019A1

公开(公告)日：2024-09-26

申请号：US18612570

申请日：2024-03-21

Applicant: Bayer Aktiengesellschaft

Inventor： Hardi MUNDL ,  Bodo KIRSCH ,  Pablo COLORADO ,  Ashkan SHOAMANESH ,  Robert HART

IPC: A61K31/4439 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/616 ,  A61P9/10

CPC classification number: A61K31/4439 ,  A61K31/4365 ,  A61K31/519 ,  A61K31/616 ,  A61P9/10

Abstract: Provided herein are methods of preventing symptomatic ischemic stroke in humans who have suffered from an acute non-cardioembolic ischemic stroke or a high-risk transient ischemic attack.

公开(公告)号：US12098146B2

公开(公告)日：2024-09-24

申请号：US16751803

申请日：2020-01-24

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： Iwona Wrona ,  Kerem Ozboya ,  Matthew Lucas ,  Bhaumik Pandya ,  Bertrand Le Bourdonnec

IPC: C07D413/04 ,  A61K31/166 ,  A61K31/175 ,  A61K31/436 ,  A61K31/4439 ,  A61K31/453 ,  A61K31/4545 ,  A61K31/475 ,  A61K31/495 ,  A61K31/497 ,  A61K31/501 ,  A61K31/55 ,  A61K45/06 ,  A61P35/00 ,  A61P35/04 ,  C07D237/22 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14

CPC classification number: C07D413/14 ,  A61P35/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/04 ,  C07D417/14 ,  A61K31/495

Abstract: The present invention features compounds useful in the treatment of neurological disorders and primary brain cancer. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders and primary brain cancer.

公开(公告)号：US20240299370A1

公开(公告)日：2024-09-12

申请号：US18605099

申请日：2024-03-14

Applicant: DermBiont, Inc.

Inventor： Mark DE SOUZA ,  John KINCAID ,  Karl BEUTNER ,  Emma TAYLOR ,  Florencia Maria GUIDALI BONJOUR ,  Vanessa Alexandra COFRE URRUTIA ,  Charles Rodney GREENAWAY EVANS

IPC: A61K31/4439 ,  A61K9/00 ,  A61K47/10 ,  A61K47/38 ,  A61P17/08

CPC classification number: A61K31/4439 ,  A61K9/0014 ,  A61K47/10 ,  A61K47/38 ,  A61P17/08

Abstract: Provided herein is a composition including a compound having the structure:






a pharmaceutically acceptable salt(s) thereof, and one or more excipients selected from (a)-(g): a) C2-6 alcohol; b) an organic solvent and/or a penetration enhancer; c) an antioxidant; d) a preservative; e) water; f) a pH adjuster; and g) a gelling agent, wherein C2-6 alcohol, the organic solvent and/or a penetration enhancer, the antioxidant, the preservative, water, the pH adjuster, and the gelling agent are defined and described herein. Methods of treating a skin disease, condition or disorder, in particular seborrheic keratosis, with the compositions are also provided herein.