公开(公告)号：US11970463B2

公开(公告)日：2024-04-30

申请号：US17810367

申请日：2022-07-01

Applicant: ASTRAZENECA AB ,  Mitsubishi Tanabe Pharma Corporation

Inventor： Lars Anders Mikael Johansson ,  Giulia Bergonzini ,  Henrik Gradén ,  Hiroshi Sugama ,  Takehiko Matsumura

IPC: C07D237/28 ,  C07D237/34 ,  C07D471/04

CPC classification number: C07D237/28 ,  C07D471/04

Abstract: The specification generally relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where R1, R2A, R2B, R2C, R2D, W, X, Y, and Z have the meanings defined herein. Such compounds are useful in inhibiting NLRP3 inflammasome activity and may be useful as therapeutic agents. The specification also relates to the use of such compounds to treat or prevent diseases and conditions in which the NLRP3 inflammasome is implicated. The specification further relates to compositions comprising such compounds.

公开(公告)号：US20240116877A1

公开(公告)日：2024-04-11

申请号：US18073721

申请日：2022-12-02

Applicant: Deciphera Pharmaceuticals, LLC

Inventor： Yu Mi Ahn ,  Timothy Caldwell ,  Daniel L. Flynn ,  Bertrand LeBourdonnec

IPC: C07D239/94 ,  C07D237/28 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D487/08

CPC classification number: C07D239/94 ,  C07D237/28 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D487/08

Abstract: Described herein are compounds that are inhibitors of wild type and oncogenic mutant c-KIT kinase and their use in the treatment of disorders such as cancers.

公开(公告)号：US20240083903A1

公开(公告)日：2024-03-14

申请号：US18264468

申请日：2022-02-15

Applicant: Jongwon Lim ,  Vladimir Simov ,  Brandon A. Vara ,  Charles S. Yeung ,  Sebastian E. Schneider ,  Erin F. DiMauro ,  Merck Sharp& Dohme LLC

Inventor： Jongwon Lim ,  Vladimir Simov ,  Brandon A. Vara ,  Charles S. Yeung ,  Sebastian E. Schneider ,  Erin F. DiMauro

IPC: C07D487/04 ,  A61P35/00 ,  C07D209/34 ,  C07D215/20 ,  C07D217/04 ,  C07D231/56 ,  C07D235/24 ,  C07D235/26 ,  C07D237/28 ,  C07D239/84 ,  C07D263/57 ,  C07D265/36 ,  C07D277/66 ,  C07D317/56 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D487/04 ,  A61P35/00 ,  C07D209/34 ,  C07D215/20 ,  C07D217/04 ,  C07D231/56 ,  C07D235/24 ,  C07D235/26 ,  C07D237/28 ,  C07D239/84 ,  C07D263/57 ,  C07D265/36 ,  C07D277/66 ,  C07D317/56 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention is directed to a compound of Formula I: or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising them and methods of using such compounds or pharmaceutical salts thereof.

公开(公告)号：US20230250066A1

公开(公告)日：2023-08-10

申请号：US17999334

申请日：2021-05-14

Applicant: SYNGENTA CROP PROTECTION AG

Inventor： Suzanna Jane DALE ,  Zoe Jane ANDERSON ,  Vikas SIKERVAR

IPC: C07D237/28 ,  C07D405/12 ,  A01P13/00 ,  A01N43/58

CPC classification number: C07D237/28 ,  C07D405/12 ,  A01P13/00 ,  A01N43/58

Abstract: Compounds of the formula (I), wherein the substituents are as defined in claim 1. The invention further relates to herbicidal compositions which comprise a compound of Formula (I) and to the use of compounds of Formula (I) for controlling weeds, in particular in crops of useful plants.

公开(公告)号：US09815797B2

公开(公告)日：2017-11-14

申请号：US15101283

申请日：2014-12-08

Applicant: UCB BIOPHARMA SPRL

Inventor： Rikki Peter Alexander ,  Gregory Foulkes ,  Martin Clive Hutchings ,  Victoria Elizabeth Jackson ,  Boris Kroeplien ,  James Thomas Reuberson ,  Sarah Margaret Rook ,  Zhaoning Zhu

IPC: C07D239/74 ,  A61K31/47 ,  A61K31/472 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  C07D215/14 ,  C07D237/28 ,  A61K31/502 ,  C07D215/06 ,  C07D237/32 ,  C07D241/44 ,  A61K45/06 ,  C07D217/16 ,  C07D241/42 ,  C07D403/04

CPC classification number: C07D239/74 ,  A61K31/47 ,  A61K31/472 ,  A61K31/498 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K45/06 ,  C07D215/06 ,  C07D215/14 ,  C07D217/16 ,  C07D237/28 ,  C07D237/32 ,  C07D241/42 ,  C07D241/44 ,  C07D403/04 ,  A61K2300/00

Abstract: A series of substituted heteroaromatic compounds containing two fused six-membered rings, tivity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.

公开(公告)号：US09102687B2

公开(公告)日：2015-08-11

申请号：US13996989

申请日：2011-12-22

Applicant: Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg ,  Kristoffer Månsson ,  Per Vedsø ,  Thomas Vifian

Inventor： Gunnar Grue-Sørensen ,  Xifu Liang ,  Thomas Högberg ,  Kristoffer Månsson ,  Per Vedsø ,  Thomas Vifian

IPC: C07D405/06 ,  C07D513/04 ,  C07C271/34 ,  C07C271/36 ,  C07C271/38 ,  C07D249/06 ,  C07D261/18 ,  C07D277/32 ,  C07D295/21 ,  C07D309/08 ,  C07D333/38 ,  C07D401/04 ,  C07D471/04 ,  C07D495/04 ,  C07D265/36 ,  C07D271/08 ,  C07D277/587 ,  C07D295/205 ,  C07D307/00 ,  C07D307/94

CPC classification number: C07D261/18 ,  A61K31/365 ,  A61K31/381 ,  A61K31/404 ,  A61K31/415 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/472 ,  A61K31/502 ,  A61K31/5375 ,  A61K31/538 ,  C07C271/34 ,  C07C271/36 ,  C07C271/38 ,  C07C2603/86 ,  C07D209/08 ,  C07D209/42 ,  C07D213/79 ,  C07D215/50 ,  C07D217/26 ,  C07D231/14 ,  C07D231/56 ,  C07D233/90 ,  C07D237/28 ,  C07D239/28 ,  C07D249/04 ,  C07D249/06 ,  C07D261/20 ,  C07D263/34 ,  C07D265/36 ,  C07D271/08 ,  C07D277/32 ,  C07D277/56 ,  C07D277/587 ,  C07D295/182 ,  C07D295/205 ,  C07D295/21 ,  C07D307/00 ,  C07D307/68 ,  C07D307/94 ,  C07D309/08 ,  C07D333/38 ,  C07D333/40 ,  C07D401/04 ,  C07D405/06 ,  C07D471/04 ,  C07D493/08 ,  C07D495/04 ,  C07D513/04

Abstract: The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Abstract translation: 本发明涉及通式I的化合物，其中R是任选被R 7取代的杂芳基; 或R是任选被R 8取代的杂环烷基或杂环烯基; 或R为X，其中X为-NR 11 R 12; 其药学上可接受的盐，水合物或溶剂合物，用于单独或与一种或多种其它药学活性化合物组合用于治疗，用于预防，治疗或改善响应刺激的中性粒细胞氧化性突发的反应的疾病或病症 的角质形成细胞IL-8释放或响应于坏死的诱导。

公开(公告)号：US20140275093A1

公开(公告)日：2014-09-18

申请号：US14054970

申请日：2013-10-16

Applicant: Millennium Pharmaceuticals, Inc.

Inventor： Christopher Blackburn ,  Kenneth M. Gigstad ,  Sean J. Harrison ,  He Xu

IPC: C07C259/08 ,  C07D207/34 ,  C07D333/70 ,  C07D239/28 ,  C07D491/048 ,  C07D209/42 ,  C07D241/44 ,  C07D285/14 ,  C07D307/85 ,  C07C259/10

CPC classification number: C07C259/08 ,  A61K31/166 ,  A61K31/341 ,  A61K31/343 ,  A61K31/381 ,  A61K31/404 ,  A61K31/407 ,  A61K31/437 ,  A61K31/4965 ,  A61K31/498 ,  A61K31/502 ,  A61K31/505 ,  C07C259/10 ,  C07C275/26 ,  C07C275/28 ,  C07C275/34 ,  C07C311/06 ,  C07C311/19 ,  C07C2601/04 ,  C07C2601/06 ,  C07D207/34 ,  C07D209/42 ,  C07D211/62 ,  C07D231/14 ,  C07D233/84 ,  C07D237/28 ,  C07D239/28 ,  C07D241/44 ,  C07D277/56 ,  C07D277/64 ,  C07D285/14 ,  C07D307/84 ,  C07D307/85 ,  C07D311/14 ,  C07D333/68 ,  C07D333/70 ,  C07D417/04 ,  C07D491/04 ,  C07D491/048

Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract translation: 本发明提供式（I）化合物：其中环A，X 1，X 2，X 3，R 2，R 4 b，R 10和G具有如说明书中所述的值，可用作HDAC6的抑制剂。 本发明还提供包含本发明化合物的药物组合物，以及使用该组合物治疗增殖性，炎症性，感染性，神经性或心血管疾病或病症的方法。

公开(公告)号：US08410099B2

公开(公告)日：2013-04-02

申请号：US12987351

申请日：2011-01-10

Applicant: Claude Vernhet ,  Elodie Barbagallo ,  Murielle Rinaldi-Carmona ,  Pascale Roux

Inventor： Claude Vernhet ,  Elodie Barbagallo ,  Murielle Rinaldi-Carmona ,  Pascale Roux

IPC: A01N43/58 ,  A61K31/50

CPC classification number: C07D237/28 ,  C07D405/04 ,  C07D409/04

Abstract: The present invention is related to novel substituted 1-benzylcinnolin-4(1H)-one derivatives having affinity for cannabinoid CB2 receptors, their preparation and their therapeutic application.

Abstract translation: 本发明涉及对大麻素CB2受体具有亲和力的新型取代的1-苄基噌啉-4（1H） - 酮衍生物及其制备及其治疗应用。

公开(公告)号：US20130018075A1

公开(公告)日：2013-01-17

申请号：US13614711

申请日：2012-09-13

Applicant: Allison L. Marlow ,  Eli Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

Inventor： Allison L. Marlow ,  Eli Wallace ,  Jeongbeob Seo ,  Joseph P. Lyssikatos ,  Hong Woon Yang ,  James Blake

IPC: A61K31/4412 ,  A61P35/00

CPC classification number: C07D213/80 ,  A61K31/437 ,  A61K31/4412 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/5377 ,  A61K45/06 ,  C07D209/46 ,  C07D213/82 ,  C07D215/48 ,  C07D231/56 ,  C07D237/24 ,  C07D237/28 ,  C07D237/32 ,  C07D239/74 ,  C07D401/04 ,  C07D401/06 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  A61K2300/00

Abstract: Disclosed are methods of treating hyperproliferative disorders, method of treating inflammatory disorders, and methods of inhibiting MEK activity in a mammal, comprising administering an effective amount of one or more compounds of the Formula V or pharmaceutically acceptable salts thereof, wherein R1, R2, R7, R8, R9 and W are as defined in the specification.

Abstract translation: 公开了治疗过度增殖性疾病的方法，治疗炎性疾病的方法和抑制哺乳动物MEK活性的方法，包括施用有效量的一种或多种式V化合物或其药学上可接受的盐，其中R1，R2，R7 R8，R9和W如说明书中所定义。

公开(公告)号：US08119640B2

公开(公告)日：2012-02-21

申请号：US12866338

申请日：2009-02-12

Applicant: James K. Chen ,  Joel M. Hyman ,  Cory A. Ocasio

Inventor： James K. Chen ,  Joel M. Hyman ,  Cory A. Ocasio

IPC: A61K31/495

CPC classification number: C07D215/54 ,  A61K31/47 ,  A61K31/4709 ,  C07C257/14 ,  C07C311/16 ,  C07C311/21 ,  C07D215/42 ,  C07D231/14 ,  C07D237/28 ,  C07D239/90 ,  C07D239/95 ,  C07D285/135 ,  C07D333/14 ,  C07D405/04 ,  C07D409/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D455/02 ,  C07D471/14 ,  C07D513/04

Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.

Abstract translation: 本公开提供了用于抑制Hh途径的化合物，药物制剂，试剂盒和方法以及与Hh途径相关的癌症和发育障碍的缓解。