Dean R. Artis - Kensington CA Michael S. Dina - Daly City CA John A. Flygare - Burlingame CA Richard A. Goldsmith - Daly City CA Regina A. Munroe - San Mateo CA Alan G. Olivero - Half Moon Bay CA Richard Pastor - San Francisco CA Thomas E. Rawson - Mountain View CA Kirk D. Robarge - San Francisco CA Daniel P. Sutherlin - San Carlos CA Kenneth J. Weese - South San Francisco CA Aihe Zhou - San Jose CA Yan Zhu - Foster City CA
Compounds having the structure shown below wherein A, B, N , N , X, Y, Q, R , R and R are as defined herein 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.
Inhibitors of serine proteases are provided having formula (I) wherein X, R, R, R, Rand Rare as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.
Dean R. Artis - Kensington CA, US Michael S. Dina - Daly City CA, US John A. Flygare - Burlingame CA, US Richard A. Goldsmith - Daly City CA, US Regina A. Munroe - San Mateo CA, US Alan G. Olivero - Half Moon Bay CA, US Richard Pastor - San Francisco CA, US Thomas E. Rawson - Mountain View CA, US Kirk D. Robarge - San Francisco CA, US Daniel P. Sutherlin - San Carlos CA, US Kenneth J. Weese - South San Francisco CA, US Aihe Zhou - San Jose CA, US Yan Zhu - Foster City CA, US
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.
Zhenhong R. Cai - Foster City CA, US Salman Y. Jabri - San Francisco CA, US Haolun Jin - Foster City CA, US Rachael A. Lansdown - San Francisco CA, US Samuel E. Metobo - Newark CA, US Michael R. Mish - La Honda CA, US Richard M. Pastor - San Francisco CA, US
Bing-Yan Zhu - Palo Alto CA, US Michael Siu - Burlingame CA, US Steven R. Magnuson - Dublin CA, US Richard Pastor - San Francisco CA, US He Haiying - Shanghai, CN Xiao Yisong - Shanghai, CN Zheng Jifu - Shanghai, CN Xu Xing - Chengdu, CN Zhao Junping - Yanan, CN Christopher Hurley - Hertfordshire, GB Jun Liang - Palo Alto CA, US Wendy Liu - Foster City CA, US Joseph P. Lyssikatos - Piedmont CA, US
Assignee:
Genentech, Inc. - South San Francisco CA
International Classification:
A61K 31/437 C07D 471/02
US Classification:
514303, 546119
Abstract:
A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R, R, R, Rand Rare 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.
Pyrazolopyrimidine Jak Inhibitor Compounds And Methods
Jeffrey Blaney - Piedmont CA, US Paul A. Gibbons - San Francisco CA, US Emily Hanan - Redwood City CA, US Joseph P. Lyssikatos - Piedmont CA, US Steven R. Magnuson - Dublin CA, US Richard Pastor - San Francisco CA, US Thomas E. Rawson - Mountain View CA, US Aihe Zhou - San Jose CA, US Bing-Yan Zhu - Palo-Alto CA, US
Assignee:
Genentech, Inc. - South San Francisco CA
International Classification:
A01N 43/90 A61K 31/519 C07D 487/00
US Classification:
5142593, 544281
Abstract:
The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R, R, Rand 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.
Inhibitors of serine proteases are provided having formula (I) wherein X, R, R, R, Rand Rare as defined herein. In particular, the compounds bind to factor VIIa, tissue factor/factor Xa complex, thrombin, trypsin, plasmin and kallikrein and have anticoagulant activity. Pharmaceutical compositions comprising the compounds are useful for inhibiting the formation of veinous and/or arterial thrombi in vivo.
Dean Artis - Kensington CA, US Michael Dina - Daly City CA, US John Flygare - Burlingame CA, US Richard Goldsmith - Daly City CA, US Regina Munroe - San Mateo CA, US Alan Olivero - Half Moon Bay CA, US Richard Pastor - San Francisco CA, US Thomas Rawson - Mountain View CA, US Kirk Robarge - San Francisco CA, US Daniel Sutherlin - San Carlos CA, US Kenneth Weese - South San Francisco CA, US Aihe Zhou - San Jose CA, US Yan Zhu - Foster City CA, US
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.