公开(公告)号：US20060116356A1

公开(公告)日：2006-06-01

申请号：US11106363

申请日：2005-04-14

Applicant: Zhenhong Cai ,  Xiaowu Chen ,  Maria Fardis ,  Salman Jabri ,  Haolun Jin ,  Choung Kim ,  Samuel Metobo ,  Michael Mish ,  Richard Pastor

Inventor： Zhenhong Cai ,  Xiaowu Chen ,  Maria Fardis ,  Salman Jabri ,  Haolun Jin ,  Choung Kim ,  Samuel Metobo ,  Michael Mish ,  Richard Pastor

IPC: A61K31/675 ,  C07F9/6544 ,  C07F9/6533

CPC classification number: A61K31/66 ,  A61K31/662 ,  A61K31/665 ,  A61K31/675 ,  A61K47/548 ,  C07D209/48 ,  C07D213/38 ,  C07D471/04 ,  C07D487/04 ,  C07F9/6561

Abstract: Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.

Abstract translation: 公开了具有至少一个膦酸酯基团的新型HIV整合酶抑制剂化合物，其受保护的中间体以及用于抑制HIV整合酶的方法。

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：US20050186198A1

公开(公告)日：2005-08-25

申请号：US11088511

申请日：2005-03-24

Applicant: Ignacio Aliagas-Martin ,  Dean Artis ,  Michael Dina ,  John Flygare ,  Richard Goldsmith ,  Regina Munroe ,  Alan Olivero ,  Richard Pastor ,  Thomas Rawson ,  Kirk Robarge ,  Daniel Sutherlin ,  Kenneth Weese ,  Aihe Zhou ,  Yan Zhu

Inventor： Ignacio Aliagas-Martin ,  Dean Artis ,  Michael Dina ,  John Flygare ,  Richard Goldsmith ,  Regina Munroe ,  Alan Olivero ,  Richard Pastor ,  Thomas Rawson ,  Kirk Robarge ,  Daniel Sutherlin ,  Kenneth Weese ,  Aihe Zhou ,  Yan Zhu

IPC: C07D333/34 ,  A61K31/18 ,  A61K31/196 ,  A61K31/216 ,  A61K31/381 ,  A61P7/02 ,  A61P9/10 ,  C07C257/18 ,  C07C311/05 ,  C07C311/08 ,  C07C311/13 ,  C07C311/18 ,  C07C311/29 ,  C07C311/51 ,  A61K38/48 ,  A61K31/445 ,  A61K31/54 ,  A61K31/60

CPC classification number: C07C257/18 ,  C07C311/05 ,  C07C311/08 ,  C07C311/13 ,  C07C311/18 ,  C07C311/29 ,  C07C311/51

Abstract: Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.

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：US08609687B2

公开(公告)日：2013-12-17

申请号：US13471269

申请日：2012-05-14

Applicant: Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: A61K31/437 ,  C07D471/02

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. 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 JAK kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2，R 3，R 4和R 5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JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。

公开(公告)号：US20120225855A1

公开(公告)日：2012-09-06

申请号：US13471269

申请日：2012-05-14

Applicant: Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

Inventor： Bing-Yan Zhu ,  Michael Siu ,  Steven R. Magnuson ,  Richard Pastor ,  He Haiying ,  Xiao Yisong ,  Zheng Jifu ,  Xu Xing ,  Zhao Junping ,  Christopher Hurley ,  Jun Liang ,  Wendy Liu ,  Joseph P. Lyssikatos

IPC: C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61P9/00 ,  A61P3/10 ,  A61P37/00 ,  A61P25/00 ,  A61P1/16 ,  A61P37/08 ,  A61P25/28 ,  A61P19/08 ,  A61P31/00 ,  A61P35/04 ,  A61P35/02 ,  A61P9/10 ,  A61P25/16 ,  A61P17/00 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. 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 JAK kinase activity in a patient are disclosed.

公开(公告)号：US08637526B2

公开(公告)日：2014-01-28

申请号：US13099179

申请日：2011-05-02

Applicant: Jeffrey Blaney ,  Paul A. Gibbons ,  Emily Hanan ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Richard Pastor ,  Thomas E. Rawson ,  Aihe Zhou ,  Bing-Yan Zhu

Inventor： Jeffrey Blaney ,  Paul A. Gibbons ,  Emily Hanan ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Richard Pastor ,  Thomas E. Rawson ,  Aihe Zhou ,  Bing-Yan Zhu

IPC: A01N43/90 ,  A61K31/519 ,  C07D487/00

CPC classification number: C07D487/04

Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia 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 JAK kinase activity in a patient.

Abstract translation: 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK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：US20120022043A1

公开(公告)日：2012-01-26

申请号：US13099179

申请日：2011-05-02

Applicant: Jeffrey Blaney ,  Paul A. Gibbons ,  Emily Hanan ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Richard Pastor ,  Thomas E. Rawson ,  Aihe Zhou ,  Bing-Yan Zhu

Inventor： Jeffrey Blaney ,  Paul A. Gibbons ,  Emily Hanan ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Richard Pastor ,  Thomas E. Rawson ,  Aihe Zhou ,  Bing-Yan Zhu

IPC: A61K31/519 ,  A61K31/5377 ,  A61P37/00 ,  A61P37/06 ,  A61P11/06 ,  A61P17/06 ,  A61P17/00 ,  A61P25/00 ,  C07D487/04 ,  A61P29/00

CPC classification number: C07D487/04

Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia 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 JAK kinase activity in a patient.

Abstract translation: 本发明提供了式Ia的JAK激酶抑制剂，其对映体，非对映异构体或其药学上可接受的盐，其中R1，R2，R7和Z在本文中定义，药物组合物包括式Ia化合物和药学上可接受的载体，佐剂或载体 以及对患者中JAK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：US20100035875A1

公开(公告)日：2010-02-11

申请号：US12488406

申请日：2009-06-19

Applicant: Bing-Yan ZHU ,  Michael SIU ,  Steven R. MAGNUSON ,  Richard PASTOR ,  He HAIYING ,  Xiao YISONG ,  Zheng JIFU ,  Xu XING ,  Zhao JUNPING ,  Wendy LIU

Inventor： Bing-Yan ZHU ,  Michael SIU ,  Steven R. MAGNUSON ,  Richard PASTOR ,  He HAIYING ,  Xiao YISONG ,  Zheng JIFU ,  Xu XING ,  Zhao JUNPING ,  Wendy LIU

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P9/00 ,  A61P37/00 ,  A61P29/00 ,  A61P19/00 ,  A61P25/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. 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 JAK kinase activity in a patient are disclosed.

Abstract translation: 其中R 1，R 2，R 3，R 4和R 5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JAK激酶抑制剂。 公开了包含式I化合物和药学上可接受的载体，佐剂或载体的药物组合物，以及治疗或减轻对患者中JAK激酶活性的抑制作用的疾病或病症的严重程度的方法。

公开(公告)号：US20080076738A1

公开(公告)日：2008-03-27

申请号：US11578649

申请日：2005-04-11

Applicant: Zhenhong Cai ,  Xiaowu Chen ,  Maria Fardis ,  Salman Jabri ,  Haolun Jin ,  Choung Kim ,  Samuel Metobo ,  Michael Mish ,  Richard Pastor

Inventor： Zhenhong Cai ,  Xiaowu Chen ,  Maria Fardis ,  Salman Jabri ,  Haolun Jin ,  Choung Kim ,  Samuel Metobo ,  Michael Mish ,  Richard Pastor

IPC: A61K31/675 ,  A61P31/18 ,  C07F9/02

CPC classification number: A61K31/66 ,  A61K31/662 ,  A61K31/665 ,  A61K31/675 ,  A61K47/548 ,  C07D209/48 ,  C07D213/38 ,  C07D471/04 ,  C07D487/04 ,  C07F9/6561

Abstract: Novel HIV integrase inhibitor compounds having at least one phosphonate group, protected intermediates thereof, and methods for inhibition of HIV-integrase are disclosed.

Abstract translation: 公开了具有至少一个膦酸酯基团的新型HIV整合酶抑制剂化合物，其受保护的中间体以及用于抑制HIV整合酶的方法。