公开(公告)号：WO2003029224A1

公开(公告)日：2003-04-10

申请号：PCT/US2002/031784

申请日：2002-10-03

Applicant: PHARMACIA CORPORATION ,  SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J. ,  ZENG, Qingping ,  ABBAS, Zaheer ,  FENTON, Ricky, L. ,  KUSTURIN, Carrie, L. ,  HAYAT, Rahman, K. ,  SAMPLE, Kirby, R. ,  SCHWEITZER, Barbara, A. ,  WOOD, Rhonda, S. ,  SZALONY, Jim ,  SULEYMANOV, Osman, D. ,  SALYERS, Anita ,  NICHOLSON, Nancy, S.

Inventor： SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J. ,  ZENG, Qingping ,  ABBAS, Zaheer ,  FENTON, Ricky, L. ,  KUSTURIN, Carrie, L. ,  HAYAT, Rahman, K. ,  SAMPLE, Kirby, R. ,  SCHWEITZER, Barbara, A. ,  WOOD, Rhonda, S. ,  SZALONY, Jim ,  SULEYMANOV, Osman, D. ,  SALYERS, Anita ,  NICHOLSON, Nancy, S.

IPC: C07D239/47

CPC classification number: C07D231/38 ,  C07C257/18 ,  C07C2601/04 ,  C07C2601/10 ,  C07D207/32 ,  C07D211/56 ,  C07D211/98 ,  C07D213/74 ,  C07D231/48 ,  C07D237/04 ,  C07D239/10 ,  C07D239/22 ,  C07D241/04 ,  C07D241/20 ,  C07D249/14 ,  C07D253/06 ,  C07D253/075 ,  C07D263/48 ,  C07D265/02 ,  C07D277/42 ,  C07D307/22 ,  C07D333/36 ,  C07D401/12 ,  C07D403/10 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: The present invention relates to compounds, and prodrugs thereof, composition and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Abstract translation: 本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。 本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

公开(公告)号：WO2003093242A2

公开(公告)日：2003-11-13

申请号：PCT/US2002/031770

申请日：2002-10-03

Applicant: PHARMACIA CORPORATION ,  SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J.

Inventor： SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J.

IPC: C07D231/00

CPC classification number: C07D213/74 ,  C07C257/18 ,  C07C2601/04 ,  C07C2601/10 ,  C07D207/32 ,  C07D207/46 ,  C07D211/56 ,  C07D211/98 ,  C07D231/38 ,  C07D231/48 ,  C07D237/04 ,  C07D239/10 ,  C07D239/22 ,  C07D241/04 ,  C07D241/20 ,  C07D249/14 ,  C07D253/06 ,  C07D253/075 ,  C07D263/48 ,  C07D265/02 ,  C07D277/42 ,  C07D307/22 ,  C07D333/36 ,  C07D401/12 ,  C07D403/10 ,  C07D413/12 ,  C07D471/04

Abstract: The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Abstract translation: 本发明涉及化合物及其前药，可用于预防和治疗哺乳动物血栓形成病症的组合物和方法。 本发明的化合物及其前药选择性地抑制凝血级联的某些蛋白酶。

公开(公告)号：WO2003093242A3

公开(公告)日：2003-11-13

申请号：PCT/US2002/031770

申请日：2002-10-03

Applicant: PHARMACIA CORPORATION ,  SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J.

Inventor： SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J.

IPC: C07D231/48

Abstract: The present invention relates to substituted 5-membered polycyclic compounds and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

公开(公告)号：WO2003028729A3

公开(公告)日：2003-04-10

申请号：PCT/US2002/031468

申请日：2002-10-03

Applicant: PHARMACIA CORPORATION ,  SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J. ,  ZENG, Qingping

Inventor： SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J. ,  ZENG, Qingping

IPC: A61K31/4965

Abstract: The present invention relates to prodrug compounds, comprising a 5- or 6- membered heterocyclic or aromatic ring substituted with a derivatized amidine, as well as compositions and methods useful for preventing and treating thrombotic conditions in mammals. The prodrug compounds of the present invention selectively inhibit certain proteases of the coagulation cascade.

公开(公告)号：WO2003028729A2

公开(公告)日：2003-04-10

申请号：PCT/US2002/031468

申请日：2002-10-03

Applicant: PHARMACIA CORPORATION ,  SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J. ,  ZENG, Qingping

Inventor： SOUTH, Michael, S. ,  WEBBER, Ronald, K. ,  HUANG, Horng-Chih ,  TOTH, Mihaly, V. ,  MOORMANN, Alan, E. ,  SNYDER, Jeffrey, S. ,  SCHOLTEN, Jeffrey, A. ,  GARLAND, Danny, J. ,  RUEPPEL, Melvin, L. ,  NEUMANN, William, L. ,  LONG, Scott ,  WEI, Huang ,  TRUJILLO, John ,  PARLOW, John, J. ,  JONES, Darin, E. ,  CASE, Brenda ,  HAYES, Michael, J. ,  ZENG, Qingping

IPC: A61K31/4965

CPC classification number: C07D213/74 ,  C07C257/18 ,  C07C2601/04 ,  C07C2601/10 ,  C07D207/32 ,  C07D211/56 ,  C07D211/98 ,  C07D231/38 ,  C07D231/48 ,  C07D237/04 ,  C07D239/10 ,  C07D239/22 ,  C07D241/04 ,  C07D241/20 ,  C07D249/14 ,  C07D253/06 ,  C07D253/075 ,  C07D263/48 ,  C07D265/02 ,  C07D277/42 ,  C07D307/22 ,  C07D333/36 ,  C07D401/12 ,  C07D403/10 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: The present invention relates to prodrug compounds, comprising a 5- or 6- membered heterocyclic or aromatic ring substituted with a derivatized amidine, as well as compositions and methods useful for preventing and treating thrombotic conditions in mammals. The prodrug compounds of the present invention selectively inhibit certain proteases of the coagulation cascade.

Abstract translation: 本发明涉及包含被衍生的脒取代的5-或6-元杂环或芳环的前药化合物，以及可用于预防和治疗哺乳动物血栓形成状况的组合物和方法。 本发明的前药化合物选择性地抑制凝血级联的某些蛋白酶。