公开(公告)号：US20240360151A1

公开(公告)日：2024-10-31

申请号：US18602519

申请日：2024-03-12

申请人： SANOFI

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

IPC分类号： 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分类号： 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

摘要： 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：US20240352007A1

公开(公告)日：2024-10-24

申请号：US18390071

申请日：2023-12-20

申请人： Basilea Pharmaceutica International AG, Allschwil

发明人： Gregor WELTI ,  Markus HEUBES ,  David TAGLIAFERRI

IPC分类号： C07D413/04 ,  C07C269/06 ,  C07C271/06

CPC分类号： C07D413/04 ,  C07C269/06 ,  C07C271/06 ,  C07B2200/13

摘要： The present invention provides processes for preparing a compound of formula I and pharmaceutically acceptable salts thereof,




comprising deprotecting a compound of formula II




wherein each R3 independently represents a tertiary alkyl group, preferably wherein each R3 is tertiary butyl. The invention also provides intermediates useful for preparing compounds of formula I and processes for preparing these intermediates. Additionally the invention provides polymorphic forms of the dichloride salt of the compound of formula I and their use in the treatment of proliferative disorders.

公开(公告)号：US20240343716A1

公开(公告)日：2024-10-17

申请号：US18435619

申请日：2024-02-07

申请人： ABIVAX ,  CENTRE NATIONAL DE RECHERCHE SCIENTIFIQUE ,  INSTITUT CURIE ,  UNIVERSITE DE MONTPELLIER

发明人： Jamal TAZI ,  Florence MAHUTEAU ,  Pierre ROUX ,  Romain NAJMAN ,  Didier SCHERRER ,  Carsten BROCK ,  Nathalie CAHUZAC ,  Gilles GADEA ,  Noelie CAMPOS ,  Aude GARCEL ,  Julien SANTO

IPC分类号： C07D413/04 ,  A61K31/4709 ,  A61K31/4985 ,  C07D213/74 ,  C07D215/38 ,  C07D215/42 ,  C07D215/46 ,  C07D217/02 ,  C07D241/44 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D413/04 ,  A61K31/4709 ,  A61K31/4985 ,  C07D213/74 ,  C07D215/38 ,  C07D215/42 ,  C07D215/46 ,  C07D217/02 ,  C07D241/44 ,  C07D401/12 ,  C07D403/12

摘要： The manufacture and use of compounds of formula (Ia) or a pharmaceutically acceptable salt thereof for preventing, inhibiting or treating cancer, AIDS and/or premature aging. The compounds of formula (Ia) being:




where:



R independently represents a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —CN group, a hydroxyl group, a —COOR1 group, a (C1-C3)fluoroalkyl group, a —NO2 group, a —NR1R2 group, or a (C1-C3)alkoxy group;
R′ is a hydrogen atom, a halogen atom, a (C1-C3)alkyl group, a —NO2 group, a (C1-C3)alkoxy group, or a —NR1R2 group; and
R1 and R2 are a hydrogen atom or a (C1-C3)alkyl group.

公开(公告)号：US12110546B2

公开(公告)日：2024-10-08

申请号：US16805125

申请日：2020-02-28

申请人： Illumina Cambridge Limited

发明人： Nikolai Nikolaevich Romanov ,  Patrick McCauley ,  Niall Hynes

IPC分类号： C12Q1/6869 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07H19/06 ,  C07H19/16

CPC分类号： C12Q1/6869 ,  C07D405/04 ,  C07D413/04 ,  C07D417/04 ,  C07H19/06 ,  C07H19/16 ,  C12Q1/6869 ,  C12Q2535/101 ,  C12Q2563/107

摘要： The present application relates to tertiary amine substituted coumarin derivatives and their uses as fluorescent labels. These compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.

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：US20240317730A1

公开(公告)日：2024-09-26

申请号：US18731285

申请日：2024-06-01

申请人： Voronoi Inc.

发明人： Youn Ho Lee ,  Seon Ah Hwang ,  In Seob Shim ,  Hyeon Ho Jeon ,  Woo Mi Do ,  Hee Sun Ryu ,  Jung Beom Son ,  Nam Doo Kim ,  Sung Hwan Kim ,  Hong Ryul Jung ,  Young Yi Lee

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D498/04 ,  C07D498/08 ,  C07F9/6584

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10 ,  C07D498/04 ,  C07D498/08 ,  C07F9/6584

摘要： The present disclosure relates to a heteroaryl derivative and uses thereof. The heteroaryl derivative of the present disclosure exhibits excellent inhibitory activity against EGFR and/or HER2, and thus may be usefully employed as a therapeutic agent for EGFR- and/or HER2-related diseases.

公开(公告)号：US20240317726A1

公开(公告)日：2024-09-26

申请号：US18596586

申请日：2024-03-05

申请人： OrsoBio, Inc.

发明人： Christian GEGE ,  Olaf KINZEL ,  Eva HAMBRUCH ,  Manfred BIRKEL ,  Claus KREMOSER ,  Ulrich DEUSCHLE

IPC分类号： C07D409/14 ,  A61P1/16 ,  C07D209/18 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04

CPC分类号： C07D409/14 ,  A61P1/16 ,  C07D209/18 ,  C07D401/04 ,  C07D403/04 ,  C07D403/10 ,  C07D405/04 ,  C07D405/10 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04 ,  C07B2200/05

摘要： The present invention relates to bicyclic compounds (e.g. indoles) containing a sulfonyl moiety, which bind to the liver X receptor (LXRa and/or LXKJ3) and act preferably as inverse agonists of LXR.

公开(公告)号：US12098146B2

公开(公告)日：2024-09-24

申请号：US16751803

申请日：2020-01-24

申请人： JANSSEN PHARMACEUTICA NV

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

IPC分类号： 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分类号： C07D413/14 ,  A61P35/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/04 ,  C07D417/14 ,  A61K31/495

摘要： 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：US12083101B2

公开(公告)日：2024-09-10

申请号：US17201268

申请日：2021-03-15

申请人： Novartis AG

发明人： Vincent Bordas ,  Cara Brocklehurst ,  Patrick Chene ,  Pascal Furet ,  Vito Guagnano ,  Patricia Imbach-Weese ,  Joerg Kallen ,  Mickael Le Douget ,  Edwige Liliane Jeanne Lorthiois ,  Joseph McKenna ,  Bahaa Salem ,  Tobias Schmelzle ,  Holger Sellner ,  Nicolas Soldermann ,  Markus Voegtle ,  Markus Wartmann

IPC分类号： A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/404 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D401/14 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D413/04 ,  C07D417/04 ,  C07D491/04

CPC分类号： A61K31/4155 ,  A61K31/343 ,  A61K31/351 ,  A61K31/357 ,  A61K31/4025 ,  A61K31/403 ,  A61K31/41 ,  A61K31/426 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/4525 ,  A61K31/506 ,  A61P35/00 ,  C07D307/81 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D407/12 ,  C07D417/04

摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof;






a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

公开(公告)号：US20240287006A1

公开(公告)日：2024-08-29

申请号：US18570555

申请日：2022-06-16

申请人： The Regents of the University of California

发明人： Michael Rape ,  Julia Sabine Schaletzky ,  Edward Eric Wehri ,  Andrew Garrett Manford

IPC分类号： C07D263/58 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K45/06 ,  C07D215/26 ,  C07D413/04 ,  C07D471/04

CPC分类号： C07D263/58 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K45/06 ,  C07D215/26 ,  C07D413/04 ,  C07D471/04

摘要： The present disclosure provides pharmaceutical compositions and drug delivery devices comprising a compound of formula I, II, III, or IV. Methods are provided for inhibiting activity of an E3 ligase, involving contacting the E3 ligase with a compound of formula I, II, III, or IV. The present disclosure provides various treatment methods involving administration of such compounds.