公开(公告)号：US20240174605A1

公开(公告)日：2024-05-30

申请号：US18279985

申请日：2022-03-01

申请人： RESEARCH TRIANGLE INSTITUTE

发明人： Yanan ZHANG ,  Dehui ZHANG

IPC分类号： C07C311/37 ,  A61K31/167 ,  A61K31/18 ,  A61K31/381 ,  A61K31/40 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/496 ,  A61P25/28 ,  C07C237/42 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D277/56 ,  C07D295/16 ,  C07D333/38 ,  C07D401/12 ,  C07D417/12

CPC分类号： C07C311/37 ,  A61K31/167 ,  A61K31/18 ,  A61K31/381 ,  A61K31/40 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/496 ,  A61P25/28 ,  C07C237/42 ,  C07D213/40 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D213/82 ,  C07D277/56 ,  C07D295/16 ,  C07D333/38 ,  C07D401/12 ,  C07D417/12 ,  C07C2601/02

摘要： The present disclosure provides novel arylsulfonamide compounds as embodiments of the present disclosure. The compounds are believed to be orexin receptor agonists, useful for the treatment of diseases and conditions caused by reduced activity of orexin.

公开(公告)号：US20230348373A1

公开(公告)日：2023-11-02

申请号：US17626061

申请日：2020-07-10

申请人： Rafael Pharmaceuticals, Inc.

发明人： Sol J. Barer ,  Yanchao Xin ,  Yaping Hong ,  Gang Zhou

IPC分类号： C07C323/52 ,  C07C323/41 ,  C07D295/16 ,  A61P35/00

CPC分类号： C07C323/52 ,  A61P35/00 ,  C07C323/41 ,  C07D295/16 ,  C07B2200/05

摘要： The invention provides new deuterated derivatives of 6,8-bis(benzylsulfanyl)octanoic acid, pharmaceutical compositions thereof, and methods for treating cancer with the new compositions.

公开(公告)号：US11465978B2

公开(公告)日：2022-10-11

申请号：US15021592

申请日：2014-09-11

申请人： THE ADMINISTRATORS OF THE TULANE EDUCATIONAL FUND ,  DUQUESNE UNIVERSITY OF THE HOLY GHOST

发明人： Suravi Chakrabarty ,  Patrick T. Flaherty ,  Darlene Monlish ,  Jane E. Cavanaugh ,  Matthew E. Burow ,  Steven Elliott ,  Van T. Hoang

IPC分类号： C07D295/192 ,  C07D295/16 ,  C07C229/58 ,  C07C237/30 ,  C07C237/32 ,  C07C237/34 ,  C07C237/36

摘要： Disclosed are anthranilic amide derivatives having the formula. Compositions are disclosed that include the anthranilic amide derivatives and the use of the anthranilic amide derivatives for the manufacture of a medicament. Further disclosed are methods of inhibiting or treating cancer, inhibiting or reversing an epithelial to mesenchymal cellular transition, and/or inhibiting MEK1/2 and/or MEK 5 enzymatic activity in a subject by administering to the subject an effective amount of a disclosed anthranilic amide derivative.

公开(公告)号：US10919850B2

公开(公告)日：2021-02-16

申请号：US16355258

申请日：2019-03-15

申请人： Araxes Pharma LLC

发明人： Pingda Ren ,  Yi Liu ,  Liansheng Li ,  Jun Feng ,  Tao Wu

IPC分类号： C07D205/04 ,  C07D487/10 ,  C07D211/62 ,  C07D213/64 ,  C07D487/04 ,  C07D295/16 ,  C07D401/04 ,  C07D285/14 ,  G01N33/58 ,  C07D213/74 ,  C07D231/40 ,  C07D401/12 ,  C07D403/04 ,  C07D237/04 ,  C07D403/06 ,  C07D405/06 ,  C07D419/12 ,  C07D471/04 ,  C07D285/16 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D403/12

摘要： Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.

公开(公告)号：US10344016B2

公开(公告)日：2019-07-09

申请号：US16207360

申请日：2018-12-03

申请人： AMGEN INC.

发明人： Paul John Dransfield ,  Zice Fu ,  Julie Anne Heath ,  Jeffrey T. Mihalic ,  Vatee Pattaropong

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D401/12 ,  C07D405/14 ,  C07D417/14 ,  A61K45/06 ,  C07B57/00 ,  C07B59/00 ,  C07D211/54 ,  C07D213/71 ,  C07D213/82 ,  C07D239/26 ,  C07D239/30 ,  C07D241/12 ,  C07D241/24 ,  C07D249/08 ,  C07D471/04 ,  C07D413/14 ,  C07D413/04 ,  C07D213/61 ,  C07D239/34 ,  C07D241/18 ,  C07F7/08 ,  C07D295/16 ,  C07C311/13 ,  A61K31/695 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/437

摘要： Bromotriazole intermediates are useful in the synthesis of agonists of the APH receptor. Such compounds include those selected from

公开(公告)号：US10273207B2

公开(公告)日：2019-04-30

申请号：US15891304

申请日：2018-02-07

申请人： Araxes Pharma LLC

发明人： Pingda Ren ,  Yi Liu ,  Liansheng Li ,  Jun Feng ,  Tao Wu

IPC分类号： C07D205/04 ,  C07D487/10 ,  C07D211/62 ,  C07D213/64 ,  C07D487/04 ,  C07D295/16 ,  C07D401/04 ,  C07D285/14 ,  G01N33/58 ,  C07D213/74 ,  C07D231/40 ,  C07D401/12 ,  C07D403/04 ,  C07D237/04 ,  C07D403/06 ,  C07D405/06 ,  C07D419/12 ,  C07D471/04 ,  C07D285/16 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D403/12

摘要： Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.

公开(公告)号：US10155725B2

公开(公告)日：2018-12-18

申请号：US14981847

申请日：2015-12-28

申请人： MERIAL, INC.

发明人： Charles Q. Meng ,  Alan Long ,  Scot Huber ,  Srinivas Reddy Gurrala ,  Douglas Edward Wilkinson ,  Gregory Pacofsky

IPC分类号： A61K31/497 ,  C07D215/38 ,  A61K31/167 ,  A61K31/4704 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4995 ,  A61K45/06 ,  C07D241/04 ,  C07D277/64 ,  C07D307/81 ,  C07D401/06 ,  C07D401/12 ,  C07D417/06 ,  C07D471/08 ,  C07D403/12 ,  C07D213/74 ,  C07D215/42 ,  C07D217/06 ,  C07D333/66 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D263/58 ,  C07D277/82 ,  C07D295/15 ,  C07D295/185 ,  C07D295/215 ,  C07D307/14 ,  C07D307/82 ,  C07C233/56 ,  C07C235/16 ,  A61K31/47 ,  A61K31/472 ,  C07D211/58 ,  C07D295/16 ,  C07D333/60

摘要： The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.

公开(公告)号：US20180327374A1

公开(公告)日：2018-11-15

申请号：US15774157

申请日：2016-11-07

申请人： Michael T. RUDD ,  Edward J. BRNARDIC ,  Yuntae KIM ,  Robert S. MEISSNER ,  Vanessa RADA ,  Shawn J. STACHEL ,  Celina V. ZERBINATTI ,  Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  Edward J. Brnardic ,  Yuntae Kim ,  Robert S. Meissner ,  Vanessa L. Rada ,  Shawn J. Stachel ,  Celina V. Zerbinatti

IPC分类号： C07D295/16 ,  C07D243/08 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D513/04 ,  A61P25/28 ,  A61P25/18 ,  A61P25/16 ,  A61P3/10

CPC分类号： C07D295/16 ,  A61K31/496 ,  A61P3/10 ,  A61P25/16 ,  A61P25/18 ,  A61P25/28 ,  C07D213/74 ,  C07D213/85 ,  C07D243/08 ,  C07D295/192 ,  C07D295/205 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/08 ,  C07D487/08 ,  C07D487/18 ,  C07D513/04 ,  C07D515/04

摘要： In its many embodiments, the present invention provides substituted cyanopyridine containing compounds of the Formula (I): and acceptable salts thereof, wherein R1, R2, R3, R4, R5, X, Y, Q, and the moiety are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.

公开(公告)号：US10106514B2

公开(公告)日：2018-10-23

申请号：US14811238

申请日：2015-07-28

申请人： Abraham Joy ,  John Swanson

发明人： Abraham Joy ,  John Swanson

IPC分类号： C08G63/685 ,  C07D295/16 ,  C07C235/08 ,  C07C235/14 ,  C08G73/02

摘要： A thermoresponsive polyester comprising units derived from an amide functional diol compound having a first amide group having a nitrogen atom and a carbonyl group; a second amide group tethered directly or indirectly through an organic group at the carbonyl group of the first amide group; and two organic groups terminated with a hydroxyl group attached to the nitrogen atom of the first amide group. The thermoresponsive polyesters exhibit a lower critical solution temperature at which they undergo a thermally induced reversible hydrophobicity change. This hydrophobicity change may involve the formation of coacervates of the thermoresponsive polyesters which can then coalesce into a precipitated polymer rich phase.

公开(公告)号：US20180162812A1

公开(公告)日：2018-06-14

申请号：US15891304

申请日：2018-02-07

申请人： Araxes Pharma LLC

发明人： Pingda Ren ,  Yi Liu ,  Liansheng Li ,  Jun Feng ,  Tao Wu

IPC分类号： C07D205/04 ,  G01N33/58 ,  C07D213/74 ,  C07D401/04 ,  C07D295/16 ,  C07D487/04 ,  C07D213/64 ,  C07D211/62 ,  C07D487/10 ,  C07D403/12 ,  C07D211/60 ,  C07D211/58 ,  C07D211/56 ,  C07D285/16 ,  C07D471/04 ,  C07D419/12 ,  C07D405/06 ,  C07D403/06 ,  C07D237/04 ,  C07D403/04 ,  C07D401/12 ,  C07D231/40 ,  C07D285/14

CPC分类号： C07D205/04 ,  C07D211/56 ,  C07D211/58 ,  C07D211/60 ,  C07D211/62 ,  C07D213/64 ,  C07D213/74 ,  C07D231/40 ,  C07D237/04 ,  C07D285/14 ,  C07D285/16 ,  C07D295/16 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/06 ,  C07D419/12 ,  C07D471/04 ,  C07D487/04 ,  C07D487/10 ,  G01N33/58

摘要： Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.