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：US20130296312A1

公开(公告)日：2013-11-07

申请号：US13920153

申请日：2013-06-18

Applicant: Cephalon, Inc.

Inventor： Matthew A. Curry ,  Bruce D. Dorsey ,  Benjamin J. Dugan ,  Diane E. Gingrich ,  Eugen F. Mesaros ,  Karen L. Milkiewicz

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: This application relates, in part, to compounds of the general Formula I and/or salts thereof, wherein X, R1A, R1B, R2, R3, R4, and R5 are as defined herein. The application also relates to compositions and methods of inhibiting at least JAK2 in subjects in recognized need thereof for the treatment of diseases or disorders for which inhibition of at least JAK2 is indicated.

Abstract translation: 本申请部分涉及通式I和/或其盐的化合物，其中X，R 1A，R 1B，R 2，R 3，R 4和R 5如本文所定义。 本申请还涉及在认可需要的受试者中至少抑制JAK2以治疗至少表达JAK2的抑制的疾病或病症的组合物和方法。

公开(公告)号：US20170027948A1

公开(公告)日：2017-02-02

申请号：US15292468

申请日：2016-10-13

Applicant: Cephalon, Inc.

Inventor： Henry J. Breslin ,  Bruce D. Dorsey ,  Gregory R. Ott

IPC: A61K31/529 ,  A61K31/5377

CPC classification number: A61K31/529 ,  A61K31/5377 ,  C07D487/08 ,  C07D487/18

Abstract: The present invention provides compounds of Formula I or a pharmaceutically acceptable salt forms thereof, wherein R1, R2, R3, R4, R5, A and X are as defined herein, methods of treatment and uses thereof.

Abstract translation: 或其药学上可接受的盐形式，其中R 1，R 2，R 3，R 4，R 5，A和X如本文所定义，其处理方法及其用途。

公开(公告)号：US20140323435A1

公开(公告)日：2014-10-30

申请号：US14285007

申请日：2014-05-22

Applicant: Cancer Research Technology Limited ,  Cephalon, Inc.

Inventor： Bruce D. Dorsey ,  Keith S. Learn ,  Emma L. Morris ,  Gregory R. Ott ,  Jonathan R.A. Roffey ,  Christelle N. Soudy ,  Jason C. Wagner

IPC: C07D495/04 ,  C07D495/20 ,  C07F7/08 ,  C07D495/14

CPC classification number: C07D495/04 ,  C07D495/14 ,  C07D495/20 ,  C07D519/00 ,  C07F7/0812

Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its 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 1，R 2，R 3，R 4，R 5，R 6，A，G，M，Q和X如本文所定义。 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：US20140031351A1

公开(公告)日：2014-01-30

申请号：US14025986

申请日：2013-09-13

Applicant: Cephalon, Inc.

Inventor： Henry J. Breslin ,  Bruce D. Dorsey ,  Gregory R. Ott

IPC: C07D487/08

CPC classification number: A61K31/529 ,  A61K31/5377 ,  C07D487/08 ,  C07D487/18

Abstract: The present invention provides compounds of Formula I or a pharmaceutically acceptable salt forms thereof, wherein R1, R2, R3, R4, R5, A and X are as defined herein, methods of treatment and uses thereof.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐形式，其中R 1，R 2，R 3，R 4，R 5，A和X如本文所定义，其处理方法及其用途。

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。