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：US12129241B1

公开(公告)日：2024-10-29

申请号：US18385790

申请日：2023-10-31

申请人： KING FAISAL UNIVERSITY

发明人： Hany Mohamed Abd El-Lateef Ahmed ,  Mai Mostafa Khalaf Ali ,  Antar Ahmed Abdelhamid Ahmed

IPC分类号： C07D401/04 ,  A61P31/04 ,  A61P31/10

CPC分类号： C07D401/04 ,  A61P31/04 ,  A61P31/10

摘要： An 9-(2-hydroxypyridin-3-yl)-10-(2-hydroxyethyl)-3,3,6,6-tetramethyl-3,4,6,7,9,10-hexahydroacridine1,8(2H,5H)-dione compound, its synthesis, and its use as an antimicrobial agent.

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：US12122750B2

公开(公告)日：2024-10-22

申请号：US18315533

申请日：2023-05-11

申请人： Eli Lilly and Company

发明人： Thomas James Beauchamp ,  Zhaogen Chen ,  Scott Eugene Conner ,  Jon Andre Erickson ,  Maria Cristina Garcia Paredes ,  Jayana Pankajkumar Lineswala ,  Emanuele Sher ,  Bishnu Thapa ,  Leonard Larry Winneroski

IPC分类号： C07D211/62 ,  C07D401/04 ,  C07D401/06 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04

CPC分类号： C07D211/62 ,  C07D401/04 ,  C07D401/06 ,  C07D405/12 ,  C07D405/14 ,  C07D471/04

摘要： This invention provides certain piperidine compounds as AT2R antagonists, e.g., compounds of formula (I):






or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and X are as defined herein, pharmaceutical compositions thereof, and methods of using the same to treat pain associated with AT2R activity.

公开(公告)号：US12115154B2

公开(公告)日：2024-10-15

申请号：US17124357

申请日：2020-12-16

申请人： SRX Cardio, LLC

发明人： Simeon Bowers ,  Mark Karbarz ,  Jiang Zhu ,  Thomas E. Barta ,  Jonathan William Bourne ,  Anjali Pandey

IPC分类号： C07D211/14 ,  A61K31/451 ,  A61K31/4545 ,  A61P3/06 ,  C07D401/04

CPC分类号： A61K31/451 ,  A61K31/4545 ,  A61P3/06 ,  C07D211/14 ,  C07D401/04

摘要： The present disclosure relates to novel compounds capable of binding to PCSK9, thereby modulating PCSK9 biological activity. Also provided are compositions comprising these compounds, methods of preparing the compounds, and methods for use of the compounds in the treatment of PCSK9-related conditions and diseases.

公开(公告)号：US20240336626A1

公开(公告)日：2024-10-10

申请号：US18738508

申请日：2024-06-10

申请人： Wuhan Tianma Microelectronics Co., Ltd. Shanghai Branch ,  Wuhan Tianma Microelectronics Co., Ltd.

发明人： Ying LIU ,  Yupei ZHANG ,  Dongyang DENG

IPC分类号： C07D498/04 ,  C07D401/04 ,  C09K11/02 ,  C09K11/06 ,  H10K85/60

CPC分类号： C07D498/04 ,  C07D401/04 ,  C09K11/02 ,  C09K11/06 ,  H10K85/622 ,  H10K85/631 ,  H10K85/654 ,  H10K85/6572

摘要： Provided are an organic compound and use thereof. Specifically, an organic compound, an OLED display panel, and an electronic device are provided. The organic compound has a structure shown in Formula (I); the OLED display panel comprises a first electrode, a second electrode, and an organic thin film layer provided between the first electrode and the second electrode; the organic thin film layer comprises a light-emitting layer; and a host material of the light-emitting layer comprises any one or a combination of at least two of the organic compounds; and the electronic device comprises the OLED display panel. The compound, when used as a host material of the light-emitting layer for the preparation of an OLED device, can reduce the driving voltage of the device, and improve the luminous efficacy and lifetime of the device.

公开(公告)号：US20240327377A1

公开(公告)日：2024-10-03

申请号：US18743634

申请日：2024-06-14

申请人： NIPPON SODA CO., LTD.

发明人： Keita SAKANISHI ,  Hikaru AOYAMA ,  Daisuke USHIJIMA ,  Takao IWASA ,  Norifumi SAKIYAMA ,  Maki MATSUI

IPC分类号： C07D401/04 ,  A01N43/50 ,  A01N43/54 ,  A01N43/653 ,  C07D233/64 ,  C07D401/14

CPC分类号： C07D401/04 ,  A01N43/50 ,  A01N43/54 ,  A01N43/653 ,  C07D233/64 ,  C07D401/14

摘要： An object of the present invention is to provide a heteroaryl azole compound that is excellent in pest control activity, particularly, insecticidal activity and/or miticidal activity, is excellent in safety, and may be industrially advantageously synthesized. The heteroaryl azole compound of the present invention is a compound of the following formula (II), an N-oxide compound, stereoisomer, tautomer or hydrate thereof, or a salt of any of these compounds. Here, in the formula (II), R1 represents a substituted or unsubstituted C1-6 alkylthio group or the like; B1 represents a nitrogen atom or CR2; R2 represents a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group or the like; R3 represents a hydrogen atom, a substituted or unsubstituted C1-6 alkyl group or the like; R represents a substituted or unsubstituted C1-6 alkyl group or the like; A represents a carbon atom or a nitrogen atom; X represents a substituted or unsubstituted C1-6 alkyl group or the like; n represents a number of chemically acceptable X, and is an integer of 0 to 2; and X is the same or different when n is 2.

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：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：US20240317706A1

公开(公告)日：2024-09-26

申请号：US18640987

申请日：2024-04-19

申请人： Monte Rosa Therapeutics, Inc.

发明人： Bernhard Fasching ,  Thomas Ryckmans ,  Andreas Ritzén ,  Vladimiras Oleinikovas

IPC分类号： C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D493/08

CPC分类号： C07D401/04 ,  A61K31/454 ,  A61K31/4545 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D493/08

摘要： Described herein, in part, are compounds that mediate the degradation of cyclin-dependent kinase 2 (CDK2), and are therefore useful in the treatment of various disorders, such as cancer.