公开(公告)号：US20180179159A1

公开(公告)日：2018-06-28

申请号：US15903150

申请日：2018-02-23

Applicant: Cephalon, Inc.

Inventor： Nadine C. Becknell ,  Reddeppa Reddy Dandu ,  Bruce D. Dorsey ,  Dimitar B. Gotchev ,  Robert L. Hudkins ,  Linda Weinberg ,  Craig A. Zificsak ,  Allison L. Zulli

IPC: C07D211/44 ,  C07D495/04 ,  C07D401/14 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04 ,  C07D495/02 ,  C07D491/048 ,  C07D471/08 ,  C07D471/04 ,  C07D471/02 ,  C07D417/14 ,  C07D417/12 ,  C07D409/14 ,  C07D405/12 ,  C07D405/06 ,  C07D401/12 ,  C07D413/14 ,  C07D405/14 ,  C07D409/12

CPC classification number: C07D211/44 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/08 ,  C07D491/048 ,  C07D495/02 ,  C07D495/04

Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses

公开(公告)号：US09475766B2

公开(公告)日：2016-10-25

申请号：US13975483

申请日：2013-08-26

Applicant: Cephalon, Inc. ,  University of Hawaii ,  University of Utah Research Foundation

Inventor： Bruce D. Dorsey ,  Scott K. Kuwada ,  Jay P. Theroff ,  Craig A. Zificsak

IPC: A61K31/66 ,  A61K31/275 ,  A61K31/18 ,  A61K31/10 ,  C07C317/32 ,  C07C317/14 ,  C07C317/44 ,  C07D213/40 ,  C07D213/57 ,  C07D213/70 ,  C07D215/36 ,  C07D217/06 ,  C07D223/10 ,  C07D231/12 ,  C07D235/16 ,  C07D263/32 ,  C07D263/56 ,  C07D271/07 ,  C07D271/10 ,  C07D295/18 ,  C07D309/08 ,  C07D309/14 ,  C07D333/20 ,  C07D333/24 ,  C07D295/192

CPC classification number: C07C317/32 ,  C07C317/14 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/57 ,  C07D213/70 ,  C07D213/71 ,  C07D215/36 ,  C07D217/06 ,  C07D223/10 ,  C07D223/12 ,  C07D231/12 ,  C07D235/06 ,  C07D235/16 ,  C07D263/32 ,  C07D263/56 ,  C07D263/57 ,  C07D271/07 ,  C07D271/10 ,  C07D295/18 ,  C07D295/185 ,  C07D295/192 ,  C07D309/08 ,  C07D309/14 ,  C07D333/20 ,  C07D333/24

Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.

Abstract translation: 其中D，n，Ra，Rb和Rc如本文所定义，以及使用式II化合物治疗或降低患者腹膜癌病变风险的药物组合物和方法。

公开(公告)号：US20140113882A1

公开(公告)日：2014-04-24

申请号：US14038915

申请日：2013-09-27

Applicant: Cancer Research Technology Limited ,  Cephalon, Inc.

Inventor： Henry J. Breslin ,  Bruce D. Dorsey ,  Benjamin J. Dugan ,  Katherine M. Fowler ,  Robert L. Hudkins ,  Eugen F. Mesaros ,  Nathaniel J.T. Monck ,  Emma L. Morris ,  Ikeoluwa Olowoye ,  Gregory R. Ott ,  Gregoire A. Pave ,  Jonathan R. Roffey ,  Christelle N. Soudy ,  Ming Tao ,  Craig A. Zificsak ,  Allison L. Zulli

IPC: C07D471/04 ,  C07F9/6584 ,  C07D498/04 ,  C07D493/08

CPC classification number: C07D471/04 ,  C07D493/08 ,  C07D498/04 ,  C07D519/00 ,  C07F9/6584

Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.

Abstract translation: 本申请提供式（I）化合物或其盐，其中R 7，R 8，R 9，G和X如本文所定义。 本申请进一步描述了包含该组合物的组合物。 式（I）化合物及其盐具有PKC抑制活性，可用于治疗增殖性疾病。

公开(公告)号：US20140005175A1

公开(公告)日：2014-01-02

申请号：US13975483

申请日：2013-08-26

Applicant: Cephalon, Inc. ,  University of Utah Research Foundation ,  University of Hawaii

Inventor： Bruce D. Dorsey ,  Scott K. Kuwada ,  Jay P. Theroff ,  Craig A. Zificsak

IPC: C07C317/32 ,  C07D213/40 ,  C07D223/10 ,  C07D295/192

CPC classification number: C07C317/32 ,  C07C317/14 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/57 ,  C07D213/70 ,  C07D213/71 ,  C07D215/36 ,  C07D217/06 ,  C07D223/10 ,  C07D223/12 ,  C07D231/12 ,  C07D235/06 ,  C07D235/16 ,  C07D263/32 ,  C07D263/56 ,  C07D263/57 ,  C07D271/07 ,  C07D271/10 ,  C07D295/18 ,  C07D295/185 ,  C07D295/192 ,  C07D309/08 ,  C07D309/14 ,  C07D333/20 ,  C07D333/24

Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.

Abstract translation: 描述了式II化合物：其中D，n，Ra，Rb和Rc如本文所定义，以及使用式II化合物治疗或降低患者腹膜癌病风险的药物组合物和方法。

公开(公告)号：US09902696B2

公开(公告)日：2018-02-27

申请号：US15185710

申请日：2016-06-17

Applicant: Cephalon, Inc.

Inventor： Nadine C. Becknell ,  Reddeppa Reddy Dandu ,  Bruce D. Dorsey ,  Dimitar B. Gotchev ,  Robert L. Hudkins ,  Linda Weinberg ,  Craig A. Zificsak ,  Allison L. Zulli

IPC: C07D211/44 ,  C07D495/04 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04 ,  C07D409/12 ,  C07D409/14 ,  C07D495/02 ,  C07D471/08 ,  C07D471/04 ,  C07D401/14 ,  C07D417/14 ,  C07D417/12 ,  C07D491/048 ,  C07D405/12 ,  C07D405/06 ,  C07D401/12 ,  C07D413/14 ,  C07D405/14 ,  C07D471/02

CPC classification number: C07D211/44 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/08 ,  C07D491/048 ,  C07D495/02 ,  C07D495/04

Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

公开(公告)号：US20170029367A1

公开(公告)日：2017-02-02

申请号：US15294420

申请日：2016-10-14

Applicant: Cephalon, Inc. ,  University of Hawaii ,  University of Utah Research Foundation

Inventor： Bruce D. Dorsey ,  Scott K. Kuwada ,  Jay P. Theroff ,  Craig A. Zificsak

IPC: C07C317/32 ,  C07C317/44 ,  C07D295/185 ,  C07D213/40 ,  C07D333/20 ,  C07D217/06 ,  C07D231/12 ,  C07D271/10 ,  C07D235/06 ,  C07D263/57 ,  C07D263/32 ,  C07C317/14 ,  C07D309/08 ,  C07D213/71 ,  C07D309/14 ,  C07D223/12

CPC classification number: C07C317/32 ,  C07C317/14 ,  C07C317/44 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/14 ,  C07D213/40 ,  C07D213/57 ,  C07D213/70 ,  C07D213/71 ,  C07D215/36 ,  C07D217/06 ,  C07D223/10 ,  C07D223/12 ,  C07D231/12 ,  C07D235/06 ,  C07D235/16 ,  C07D263/32 ,  C07D263/56 ,  C07D263/57 ,  C07D271/07 ,  C07D271/10 ,  C07D295/18 ,  C07D295/185 ,  C07D295/192 ,  C07D309/08 ,  C07D309/14 ,  C07D333/20 ,  C07D333/24

Abstract: Compounds of formula II are described: wherein D, n, Ra, Rb, and Rc are as herein defined, along with pharmaceutical compositions and methods of using compounds of formula II for treating or reducing the risk of peritoneal carcinomatosis in a patient.

Abstract translation: 其中D，n，Ra，Rb和Rc如本文所定义，以及使用式II化合物治疗或降低患者腹膜癌病变风险的药物组合物和方法。

公开(公告)号：US20160368874A1

公开(公告)日：2016-12-22

申请号：US15185710

申请日：2016-06-17

Applicant: Cephalon, Inc.

Inventor： Nadine C. Becknell ,  Reddeppa Reddy Dandu ,  Bruce D. Dorsey ,  Dimitar B. Gotchev ,  Robert L. Hudkins ,  Linda Weinberg ,  Craig A. Zificsak ,  Allison L. Zulli

IPC: C07D211/44 ,  C07D405/12 ,  C07D471/04 ,  C07D405/14 ,  C07D491/048 ,  C07D413/14 ,  C07D409/14 ,  C07D417/14 ,  C07D401/14 ,  C07D409/12 ,  C07D495/04 ,  C07D417/12 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04

CPC classification number: C07D211/44 ,  C07D211/54 ,  C07D211/58 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/02 ,  C07D471/04 ,  C07D471/08 ,  C07D491/048 ,  C07D495/02 ,  C07D495/04

Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

Abstract translation: 本文描述了具有作为脂肪酸合成酶抑制剂的活性的根据式（I）的1,4-取代的哌啶化合物。 本文还描述了含有所述1,4-取代的哌啶化合物的药物组合物，以及通过施用本文所述的一种或多种化合物或药物制剂来治疗由脂肪酸合酶介导的疾病的方法。 本文还描述了合成所述化合物的方法，包括所述1,4-取代的哌啶化合物和用于那些合成的合成中间体。