公开(公告)号：WO2007022102A3

公开(公告)日：2007-02-22

申请号：PCT/US2006/031682

申请日：2006-08-14

Applicant: GENENTECH, INC. ,  HOFFMAN-LA ROCHE, INC. ,  F. HOFFMAN-LA ROCHE, AG ,  ZHOU, Aihe ,  RAWSON, Thomas, E. ,  SAFINA, Brian ,  DOTSON, Jennafer ,  ALIAGAS-MARTIN, Ignacio ,  HALLADAY, Jason ,  LIANG, Jun ,  RUETH, Matthias ,  ZHU, Bing-Yan ,  BROOKFIELD, Frederick ,  PRIME, Michael ,  ZHANG, Birong ,  LI, Jun, M.

Inventor： RAWSON, Thomas, E. ,  SAFINA, Brian ,  DOTSON, Jennafer ,  ALIAGAS-MARTIN, Ignacio ,  HALLADAY, Jason ,  LIANG, Jun ,  RUETH, Matthias ,  ZHU, Bing-Yan ,  BROOKFIELD, Frederick ,  PRIME, Michael ,  ZHANG, Birong ,  LI, Jun, M.

IPC: C07D487/04 ,  C07D491/04 ,  A61K31/4155 ,  A61P35/00

Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula: (I) wherein A, X, Y, Z, Ra, Rb, Rc, R 1 , R 2 , R 3 and m are defined herein.

公开(公告)号：WO2011003065A3

公开(公告)日：2011-05-19

申请号：PCT/US2010040906

申请日：2010-07-02

Applicant: GENENTECH INC ,  GIBBONS PAUL ,  HANAN EMILY ,  LIU WENDY ,  LYSSIKATOS JOSEPH P ,  MAGNUSON STEVEN R ,  MENDONCA ROHAN ,  PASTOR RICHARD ,  RAWSON THOMAS E ,  SIU MICHAEL ,  ZAK MARK E ,  ZHOU AIHE ,  ZHU BING-YAN

Inventor： GIBBONS PAUL ,  HANAN EMILY ,  LIU WENDY ,  LYSSIKATOS JOSEPH P ,  MAGNUSON STEVEN R ,  MENDONCA ROHAN ,  PASTOR RICHARD ,  RAWSON THOMAS E ,  SIU MICHAEL ,  ZAK MARK E ,  ZHOU AIHE ,  ZHU BING-YAN

IPC: C07D487/04 ,  A61K31/437 ,  A61P35/00 ,  C07D403/12

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，佐剂或载体的药物组合物，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：WO2004113278A2

公开(公告)日：2004-12-29

申请号：PCT/US2004/015915

申请日：2004-05-19

Applicant: GENENTECH, INC. ,  GAZZARD, Lewis J. ,  RAWSON, Thomas E.

Inventor： GAZZARD, Lewis J. ,  RAWSON, Thomas E.

IPC: C07C311/00

CPC classification number: C07D307/79 ,  C07C307/06 ,  C07C311/51 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/86

Abstract: Compounds having the general formula I are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties. These compounds may be used in methods of preventing and/or treating clotting disorders.

公开(公告)号：WO9426723A3

公开(公告)日：1995-02-02

申请号：PCT/US9405157

申请日：1994-05-10

Applicant: GENENTECH INC ,  UNIV TEXAS ,  MARSTERS JAMES C JR ,  BROWN MICHAEL S ,  CROWLEY CRAIG W ,  GOLDSTEIN JOSEPH L ,  JAMES GUY L ,  MCDOWELL ROBERT S ,  OARE DAVID ,  RAWSON THOMAS E ,  REYNOLDS MARK ,  SOMERS TODD G

Inventor： MARSTERS JAMES C JR ,  BROWN MICHAEL S ,  CROWLEY CRAIG W ,  GOLDSTEIN JOSEPH L ,  JAMES GUY L ,  MCDOWELL ROBERT S ,  OARE DAVID ,  RAWSON THOMAS E ,  REYNOLDS MARK ,  SOMERS TODD G

IPC: A61K31/55 ,  A61K31/551 ,  A61K38/00 ,  A61P31/04 ,  A61P35/00 ,  C07D223/16 ,  C07D243/10 ,  C07D243/14 ,  C07D243/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D409/06 ,  C07D409/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078 ,  C07K5/08 ,  C07K5/083 ,  C07K5/097 ,  C07K5/10 ,  C07K5/103 ,  C07K5/117

CPC classification number: C07D223/16 ,  A61K38/00 ,  C07D243/10 ,  C07D243/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D487/04 ,  C07D513/04 ,  C07K5/0207 ,  C07K5/0606 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/081 ,  C07K5/0821 ,  C07K5/0827 ,  C07K5/1013 ,  C07K5/1024 ,  C07K5/1027

Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

公开(公告)号：WO2011003065A2

公开(公告)日：2011-01-06

申请号：PCT/US2010/040906

申请日：2010-07-02

Applicant: GENENTECH, INC. ,  GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

Inventor： GIBBONS, Paul ,  HANAN, Emily ,  LIU, Wendy ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  MENDONCA, Rohan ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  SIU, Michael ,  ZAK, Mark E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC: C07D487/04 ,  C07D403/12 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R 1 , R 2 and R 3 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: 式I化合物，其对映异构体，非对映异构体，互变异构体或可药用盐，其中R 1， 3如本文所定义，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，以及治疗或减轻患者中抑制Janus激酶活性的疾病或病症的严重程度或减轻其严重程度的方法。 p>

公开(公告)号：WO2010051549A1

公开(公告)日：2010-05-06

申请号：PCT/US2009/063014

申请日：2009-11-02

Applicant: GENENTECH, INC. ,  BLANEY, Jeffrey ,  GIBBONS, Paul A. ,  HANAN, Emily ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

Inventor： BLANEY, Jeffrey ,  GIBBONS, Paul A. ,  HANAN, Emily ,  LYSSIKATOS, Joseph P. ,  MAGNUSON, Steven R. ,  PASTOR, Richard ,  RAWSON, Thomas E. ,  ZHOU, Aihe ,  ZHU, Bing-Yan

IPC: A01N43/90 ,  A61K31/519

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. Ia

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。 IA

公开(公告)号：WO0041531A3

公开(公告)日：2001-08-16

申请号：PCT/US0000673

申请日：2000-01-11

Applicant: GENENTECH INC ,  ALIAGAS MARTIN IGNACIO ,  ARTIS DEAN R ,  DINA MICHAEL S ,  FLYGARE JOHN A ,  GOLDSMITH RICHARD A ,  MUNROE REGINA A ,  OLIVERO ALAN G ,  PASTOR RICHARD ,  RAWSON THOMAS E ,  ROBARGE KIRK D ,  SUTHERLIN DANIEL P ,  WEESE KENNETH J ,  ZHOU AIHE ,  ZHU YAN

Inventor： ALIAGAS-MARTIN IGNACIO ,  ARTIS DEAN R ,  DINA MICHAEL S ,  FLYGARE JOHN A ,  GOLDSMITH RICHARD A ,  MUNROE REGINA A ,  OLIVERO ALAN G ,  PASTOR RICHARD ,  RAWSON THOMAS E ,  ROBARGE KIRK D ,  SUTHERLIN DANIEL P ,  WEESE KENNETH J ,  ZHOU AIHE ,  ZHU YAN

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 ,  C07C257/16 ,  C07C311/06 ,  C07C311/21

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

Abstract: Compounds having structure (A) 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.

Abstract translation: 具有结构（A）的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。 这些化合物可用于预防和/或治疗凝血障碍的方法。

公开(公告)号：WO2007120333A3

公开(公告)日：2007-10-25

申请号：PCT/US2006/062112

申请日：2006-12-14

Applicant: GENENTECH, INC. ,  SAFINA, Brian ,  RAWSON, Thomas E. ,  ZHU, Bing-Yan

Inventor： SAFINA, Brian ,  RAWSON, Thomas E. ,  ZHU, Bing-Yan

IPC: A61K31/4162 ,  C07D487/02

Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I): I wherein X, Y, Z, R 1 , R 2 , R 3, R a , R b , and n are as described herein.

公开(公告)号：WO2004113278A3

公开(公告)日：2004-12-29

申请号：PCT/US2004/015915

申请日：2004-05-19

Applicant: GENENTECH, INC. ,  GAZZARD, Lewis J. ,  RAWSON, Thomas E.

Inventor： GAZZARD, Lewis J. ,  RAWSON, Thomas E.

IPC: C07C307/06

Abstract: Compounds having the general formula (I) are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties. These compounds may be used in methods of preventing and/or treating clotting disorders.

公开(公告)号：WO1994026723A2

公开(公告)日：1994-11-24

申请号：PCT/US1994005157

申请日：1994-05-10

Applicant: GENENTECH, INC. ,  BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM ,  MARSTERS, James, C., Jr. ,  BROWN, Michael, S. ,  CROWLEY, Craig, W. ,  GOLDSTEIN, Joseph, L. ,  JAMES, Guy, L. ,  McDOWELL, Robert, S. ,  OARE, David ,  RAWSON, Thomas, E. ,  REYNOLDS, Mark ,  SOMERS, Todd, G.

Inventor： GENENTECH, INC. ,  BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

IPC: C07D243/14

CPC classification number: C07D223/16 ,  A61K38/00 ,  C07D243/10 ,  C07D243/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D409/14 ,  C07D487/04 ,  C07D513/04 ,  C07K5/0207 ,  C07K5/0606 ,  C07K5/06139 ,  C07K5/06191 ,  C07K5/081 ,  C07K5/0821 ,  C07K5/0827 ,  C07K5/1013 ,  C07K5/1024 ,  C07K5/1027

Abstract: Benzodiazepine derivatives are disclosed that act as potent inhibitors of ras farnesyl:protein transferase. Pharmaceutical compositions containing these benzodiazepines are provided for treatment of diseases for which inhibition of the ras farnesyl:protein transferase is indicated.

Abstract translation: 公开了苯并二氮杂衍生物，其作为法西尼酯：蛋白转移酶的有效抑制剂。 提供含有这些苯二氮卓类药物的药物组合物，用于治疗对法拉第法：蛋白转移酶的抑制作用的疾病的治疗。