公开(公告)号：US20160318929A1

公开(公告)日：2016-11-03

申请号：US15108400

申请日：2014-12-18

Applicant: CEPHALON, INC.

Inventor： Robert L Hudkins ,  Allison L. Zulli

IPC: C07D471/04

CPC classification number: C07D471/04 ,  A61P35/00

Abstract: The invention is directed to pyrazolo[1,5-a]pyridine derivatives and their use as AXL and c-MET kinase inhibitors.

Abstract translation: 本发明涉及吡唑并[1,5-a]吡啶衍生物及其作为AXL和c-MET激酶抑制剂的用途。

公开(公告)号：US20160243119A1

公开(公告)日：2016-08-25

申请号：US15146164

申请日：2016-05-04

Applicant: Cephalon, Inc.

Inventor： Shawn P. Allwein ,  Laurent Courvoisier (deceased) ,  Martin J. Jacobs ,  Gregory R. Ott

IPC: A61K31/506

CPC classification number: A61K31/506 ,  C07D403/04 ,  C07D403/12

Abstract: The present invention provides a compound of formula (I) or a salt form thereof. The compound of formula (I) has ALK and FAK inhibitory activity, and may be used to treat proliferative disorders.

Abstract translation: 本发明提供式（I）化合物或其盐形式。 式（I）化合物具有ALK和FAK抑制活性，可用于治疗增殖性疾病。

公开(公告)号：US09233115B2

公开(公告)日：2016-01-12

申请号：US13949346

申请日：2013-07-24

Applicant: Cephalon, Inc.

Inventor： Raffaella Bernardini ,  Alberto Bernareggi ,  Paolo G. Cassara ,  Sankar Chatterjee ,  Germano D'Arasmo ,  Sergio De Munari ,  Edmondo Ferretti ,  Mohamed Iqbal ,  Ernesto Menta ,  Patricia A. Messina McLaughlin ,  Ambrogio Oliva

IPC: A61K31/69 ,  A61K45/06 ,  C07F5/02

CPC classification number: A61K31/69 ,  A61K45/06 ,  C07F5/025

Abstract: The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

公开(公告)号：US08895756B2

公开(公告)日：2014-11-25

申请号：US13719409

申请日：2012-12-19

Applicant: Cephalon, Inc.

Inventor： Jason Edward Brittain ,  Joe Craig Franklin

IPC: C07D235/04 ,  A61K9/19 ,  A61K9/00 ,  A61K31/4184 ,  A61K47/10

CPC classification number: A61K31/4184 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/10

Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.

公开(公告)号：US08884014B2

公开(公告)日：2014-11-11

申请号：US13678886

申请日：2012-11-16

Applicant: Cephalon, Inc. ,  Cephalon France

Inventor： Shawn P. Allwein ,  Arnaud Grandeury ,  Guy Piacenza ,  Sebastien Rose

IPC: C07D403/00 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates a method for purifying a fused pyrrolocarbazole compound known as 11-isobutyl-2-methyl-8-(2-pyrimidinylamino)-2,5,6,11,12,13-hexahydro-4Hindazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one using an acid complex thereof. The present invention also relates to a crystalline form of the acid complex.

Abstract translation: 本发明涉及一种纯化称为11-异丁基-2-甲基-8-（2-嘧啶基氨基）-2,5,6,11,12,13-六氢-4H-吲唑并[5,4-噻唑并[ a]吡咯并[3,4-c]咔唑-4-酮。 本发明还涉及酸络合物的结晶形式。

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：US20140275102A1

公开(公告)日：2014-09-18

申请号：US14207465

申请日：2014-03-12

Applicant: Cephalon Inc.

Inventor： Stephen J. Bierlmaier ,  Laurent Courvoisier ,  Ralph C. Haltiwanger ,  Martin J. Jacobs

IPC: C07D403/12

CPC classification number: C07D403/12

Abstract: Solid state forms of the compound 6-[4-[3-((R)-2-methylpyrrolidine-1-yl)-propoxy]phenyl]2H-pyridazine-3-one hydrochloride (Compound 1), processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided. Compound 1 is a histamine H3 receptor antagonist/inverse agonist. Thus the provided solid state forms are useful, for example, for the manufacture of a medicament for the treatment of disorders mediated by the H3 receptor.

Abstract translation: 化合物6- [4- [3 - （（R）-2-甲基吡咯烷-1-基） - 丙氧基]苯基] -2H-哒嗪-3-酮盐酸盐（化合物1）的固体形式，制备固体的方法 状态及其药物组合物。 化合物1是组胺H3受体拮抗剂/反向激动剂。 因此，提供的固态形式可用于例如制备用于治疗由H3受体介导的病症的药物。

公开(公告)号：US08765810B2

公开(公告)日：2014-07-01

申请号：US13654765

申请日：2012-10-18

Applicant: The Trustees Of The University Of Pennsylvania ,  Cephalon, Inc.

Inventor： Mark I. Greene ,  Ramachandran Murali ,  Xin Cheng ,  Raphael Ottenbrite ,  Yingxin Xiaio

IPC: A61K31/15 ,  A61K31/352 ,  A61K31/365 ,  C07C251/86

CPC classification number: C07D493/10 ,  A61K31/15 ,  A61K31/352 ,  A61K31/365 ,  C07C251/86 ,  C07D311/82

Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-α mediated conditions.

Abstract translation: 本发明涉及作为肿瘤坏死因子受体I的变构抑制剂的化合物，包含这些化合物的组合物，以及使用这些化合物及其组合物治疗TNF-α介导的病症的方法。

公开(公告)号：US20140148490A1

公开(公告)日：2014-05-29

申请号：US14169961

申请日：2014-01-31

Applicant: Cephalon, Inc.

Inventor： Jason Edward Brittain ,  Joe Craig Franklin

IPC: A61K9/19 ,  A61K31/4184

CPC classification number: A61K31/4184 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/10

Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.

Abstract translation: 本发明提供了适用于药物用途的冻干苯达莫司汀的药物制剂。 本发明还提供了生产冻干的苯达莫司汀的方法。 药物制剂可用于任何对苯达莫司汀治疗敏感的疾病，如肿瘤疾病。

公开(公告)号：US20140128443A1

公开(公告)日：2014-05-08

申请号：US14151242

申请日：2014-01-09

Applicant: Cephalon, Inc.

Inventor： Anthony S. Drager ,  Rachel Y. LaBell ,  Piyush R. Patel

IPC: A61K9/08 ,  A61K31/4184

CPC classification number: A61K31/4184 ,  A61K9/0019 ,  A61K9/08 ,  A61K47/10 ,  A61K47/18 ,  A61K47/20 ,  A61K47/22 ,  A61K47/40

Abstract: Stable liquid formulations of bendamustine, and pharmaceutically acceptable salts thereof, and polar aprotic solvents, are described.

Abstract translation: 描述了苯达莫司汀及其药学上可接受的盐和极性非质子溶剂的稳定液体制剂。