公开(公告)号：US08999998B2

公开(公告)日：2015-04-07

申请号：US13382145

申请日：2010-07-02

Applicant: Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark Zak ,  Aihe Zhou ,  Bing-Yan Zhu

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark Zak ,  Aihe Zhou ,  Bing-Yan Zhu

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：US08461328B2

公开(公告)日：2013-06-11

申请号：US13004808

申请日：2011-01-11

Applicant: Srinivasan Babu ,  Phillippe Bergeron ,  Peter Dragovich ,  Hazel Joan Dyke ,  Paul Gibbons ,  Stefan Gradl ,  Emily Hanan ,  Christopher Hurley ,  Tony Johnson ,  Michael Koehler ,  Janusz Kulagowski ,  Sharada Labadie ,  Joseph Lyssikatos ,  Rohan Mendonca ,  Rebecca Pulk ,  Stuart Ward ,  Bohdan Waszkowycz ,  Mark Zak

Inventor： Srinivasan Babu ,  Phillippe Bergeron ,  Peter Dragovich ,  Hazel Joan Dyke ,  Paul Gibbons ,  Stefan Gradl ,  Emily Hanan ,  Christopher Hurley ,  Tony Johnson ,  Michael Koehler ,  Janusz Kulagowski ,  Sharada Labadie ,  Joseph Lyssikatos ,  Rohan Mendonca ,  Rebecca Pulk ,  Stuart Ward ,  Bohdan Waszkowycz ,  Mark Zak

IPC: A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P37/06 ,  C07D413/14 ,  C07D471/14

CPC classification number: C07D471/14 ,  C07D487/10

Abstract: The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.

Abstract translation: 本发明提供具有以下通式的新颖的式I化合物：其中R1，R2，R3，X和Y如本文所述。 因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。

公开(公告)号：US20120190665A1

公开(公告)日：2012-07-26

申请号：US13382145

申请日：2010-07-02

Applicant: Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark Zak ,  Aihe Zhou ,  Bing-Yan Zhu

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark Zak ,  Aihe Zhou ,  Bing-Yan Zhu

IPC: A61K31/519 ,  A61K31/5377 ,  A61P35/00 ,  A61P35/02 ,  A61P7/00 ,  A61P1/00 ,  A61P17/06 ,  A61P17/00 ,  A61P19/02 ,  C07D487/04 ,  A61P29/00

CPC classification number: C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2和R 3在本文中定义的式I化合物，对映异构体，非对映异构体，互变异构体或其药学上可接受的盐可用作一种或多种Janus激酶的抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或媒介物的药物组合物，以及对患者中Janus激酶活性的抑制作出反应的疾病或病症的严重程度的治疗或减轻的方法。

公开(公告)号：US20110201593A1

公开(公告)日：2011-08-18

申请号：US13004808

申请日：2011-01-11

Applicant: Srinivasan Babu ,  Phillippe Bergeron ,  Peter Dragovich ,  Hazel Joan Dyke ,  Paul Gibbons ,  Stefan Gradl ,  Emily Hanan ,  Christopher Hurley ,  Tony Johnson ,  Michael Koehler ,  Janusz Kulagowski ,  Sharada Labadie ,  Joseph Lyssikatos ,  Rohan Mendonca ,  Rebecca Pulk ,  Stuart Ward ,  Bohdan Waszkowycz ,  Mark Zak

Inventor： Srinivasan Babu ,  Phillippe Bergeron ,  Peter Dragovich ,  Hazel Joan Dyke ,  Paul Gibbons ,  Stefan Gradl ,  Emily Hanan ,  Christopher Hurley ,  Tony Johnson ,  Michael Koehler ,  Janusz Kulagowski ,  Sharada Labadie ,  Joseph Lyssikatos ,  Rohan Mendonca ,  Rebecca Pulk ,  Stuart Ward ,  Bohdan Waszkowycz ,  Mark Zak

IPC: A61K31/397 ,  C07D471/14 ,  A61K31/437 ,  C07D413/14 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/55 ,  A61K31/506 ,  A61P19/02 ,  A61P17/06 ,  A61P37/06 ,  A61P11/06

CPC classification number: C07D471/14 ,  C07D487/10

Abstract: The invention provides novel compounds of formula I having the general formula: wherein R1, R2, R3, X and Y are as described herein. Accordingly, the compounds may be provided in pharmaceutically acceptable compositions and used for the treatment of immunological or hyperproliferative disorders.

Abstract translation: 本发明提供具有以下通式的新颖的式I化合物：其中R1，R2，R3，X和Y如本文所述。 因此，化合物可以以药学上可接受的组合物提供，并用于治疗免疫学或过度增殖性疾病。