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1. 发明申请

WO2003093242A3 SUBSTITUTED 5-MEMBERED POLYCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
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
申请人： 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.
发明人： 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分类号： C07D231/48
摘要： 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.

2. 发明申请

WO2002042272A3 SUBSTITUTED POLYCYCLIC ARYL AND HETEROARYL PYRIDINES USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
公开(公告)号：WO2002042272A3
公开(公告)日：2002-05-30
申请号：PCT/US2001/043280
申请日：2001-11-20
申请人： PHARMACIA CORPORATION , SOUTH, Michael, S. , CASE, Brenda , GARLAND, Danny, J. , HAYES, Michael, J. , HUANG, Horng-Chih , HUANG, Wei , JONES, Darin, E. , NEUMANN, William, L. , PARLOW, John, J. , REITZ, David, B. , RUEPPEL, Melvin, L. , WEBBER, Ronald, K.
发明人： SOUTH, Michael, S. , CASE, Brenda , GARLAND, Danny, J. , HAYES, Michael, J. , HUANG, Horng-Chih , HUANG, Wei , JONES, Darin, E. , NEUMANN, William, L. , PARLOW, John, J. , REITZ, David, B. , RUEPPEL, Melvin, L. , WEBBER, Ronald, K.
IPC分类号： A61K31/4418
摘要： 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.

3. 发明申请

WO0001687A9 BENZOTHIEPINES HAVING ACTIVITY AS INHIBITORS OF ILEAL BILE ACID TRANSPORT AND TAUROCHOLATE UPTAKE 审中-公开
标题翻译：具有作为ILEAL BILE ACID TRACSPORT和TAUROCHOLATE摄取的抑制剂的活性的BENZOTHIEPINES
公开(公告)号：WO0001687A9
公开(公告)日：2000-07-20
申请号：PCT/US9912828
申请日：1999-06-29
申请人： SEARLE & CO , LEE LEN F , BANERJEE SHYAMAL C , HUANG HORNG CHIH , LI JINGLIN J , MILLER RAYMOND E , REITZ DAVID B , TREMONT SAMUEL J
发明人： LEE LEN F , BANERJEE SHYAMAL C , HUANG HORNG-CHIH , LI JINGLIN J , MILLER RAYMOND E , REITZ DAVID B , TREMONT SAMUEL J
IPC分类号： A61K31/00 , A61K31/38 , A61K31/4035 , A61K31/41 , A61K31/4178 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/4995 , A61K31/662 , A61K31/67 , A61P1/16 , A61P3/06 , A61P9/10 , A61P43/00 , C07B53/00 , C07C319/14 , C07C323/12 , C07C323/18 , C07C323/19 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/653 , C07F9/6553 , C07K5/06 , C07K5/068 , C08G65/329
CPC分类号： A61K31/38 , C07C319/14 , C07D337/06 , C07D337/08 , C07D409/10 , C07D409/12 , C07D487/08 , C07D495/04 , C07D495/10 , C07F9/65539 , C07K5/06086 , C08G65/329 , C07C323/12 , C07C323/18
摘要： Novel benzothiepines, derivatives, and analogs thereof; methods of preparing such compounds; pharmaceutical compositions containing such compounds; and methods of using these compounds and compositions in the preparation of a medicament, particularly medicaments for use in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
摘要翻译：新的苯并噻庚因衍生物及其类似物; 制备这些化合物的方法; 含有这些化合物的药物组合物; 以及使用这些化合物和组合物制备药物，特别是用于预防和治疗哺乳动物中与高血脂症状相关的高脂血症或与高胆固醇血症有关的药物的方法。

4. 发明申请

WO9840375A2 COMBINATION THERAPY EMPLOYING ILEAL BILE ACID TRANSPORT INHIBITING BENZOTHIEPINES AND HMG Co-A REDUCTASE INHIBITORS 审中-公开
标题翻译：联合治疗使用ILEAL BILE ACID运输抑制苯扎硫酯和HMG联合还原酶抑制剂
公开(公告)号：WO9840375A2
公开(公告)日：1998-09-17
申请号：PCT/US9803792
申请日：1998-03-10
申请人： SEARLE & CO , REITZ DAVID B , LEE LEN F , LI JINGLIN J , HUANG HORNG CHIH , TREMONT SAMUEL J , MILLER RAYMOND E , BANERIEE SHYAMAL C , MANNING ROBERT E , GLENN KEVIN C , KELLER BRADLEY T
发明人： REITZ DAVID B , LEE LEN F , LI JINGLIN J , HUANG HORNG-CHIH , TREMONT SAMUEL J , MILLER RAYMOND E , BANERIEE SHYAMAL C , MANNING ROBERT E , GLENN KEVIN C , KELLER BRADLEY T
IPC分类号： C07D337/08 , A61K31/19 , A61K31/22 , A61K31/366 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/4025 , A61K31/4035 , A61K31/405 , A61K31/4178 , A61K31/437 , A61K31/4375 , A61K31/4436 , A61K31/4709 , A61K31/4725 , A61K31/473 , A61K31/496 , A61K31/498 , A61K31/4995 , A61K31/502 , A61K31/5377 , A61K31/55 , A61K31/67 , A61K45/06 , A61P3/06 , C07D409/04 , C07D409/10 , C07D409/12 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D337/00
CPC分类号： A61K45/06 , A61K31/22 , A61K31/366 , A61K31/405 , A61K2300/00
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。还提供了使用回肠胆汁酸转运抑制剂和HMG Co-A还原酶抑制剂联合治疗高脂血症的组合物和方法。

5. 发明申请

WO1997033882A1 NOVEL BENZOTHIEPINES HAVING ACTIVITY AS INHIBITORS OF ILEAL BILE ACID TRANSPORT AND TAUROCHOLATE UPTAKE 审中-公开
标题翻译：具有活性的新型胆碱酯酶作为ILEAL BILE ACID TRACSPORT和TAUROCHOLATE摄取的抑制剂
公开(公告)号：WO1997033882A1
公开(公告)日：1997-09-18
申请号：PCT/US1997004076
申请日：1997-03-11
申请人： G.D. SEARLE AND CO. , REITZ, David, B. , LEE, Len, F. , LI, Jinglin, J. , HUANG, Horng-Chih , TREMONT, Samuel, J. , MILLER, Raymond, E. , BANERJEE, Shyamal, C.
发明人： G.D. SEARLE AND CO.
IPC分类号： C07D337/08
CPC分类号： C08G65/329 , A61K31/38 , C07D337/08 , C07D409/10 , C07D495/04
摘要： Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.
摘要翻译：提供了新的苯并噻庚因，衍生物和类似物; 含有它们的药物组合物; 以及在医学中使用这些化合物和组合物的方法，特别是用于预防和治疗哺乳动物中高脂血症的疾病，例如与动脉粥样硬化或高胆固醇血症有关的那些。

6. 发明申请

WO1995030656A1 SUBSTITUTED CYCLOPENTADIENYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译：用于治疗炎症的替代环己二烯化合物
公开(公告)号：WO1995030656A1
公开(公告)日：1995-11-16
申请号：PCT/US1995004790
申请日：1995-04-26
申请人： G.D. SEARLE & CO. , HUANG, Horng-Chih , REITZ, David, R.
发明人： G.D. SEARLE & CO.
IPC分类号： C07D213/34
CPC分类号： C07C317/14 , C07C311/16 , C07C2601/10
摘要： A class of 2,3-substituted cyclopenta-2,4-dienyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein each of R and R is independently selected from hydrido, lower alkyl, lower hydroxyalkyl, halo, lower haloalkyl, lower alkoxycarbonyl and carboxyl; and wherein each of R rhrough R is independently selected from hydrido, halo, lower alkyl, lower alkylthio, cyano, hydroxyl, mercapto, lower haloalkyl, lower haloalkoxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkylsulfonyl, lower haloalkylsulfonyl and sulfamyl; provided R and R are not both hydrido or methoxy; or a pharmaceutically suitable salt or prodrug thereof. One of the two substituted phenyl groups can be replaced by a substituted pyridine group.
摘要翻译：描述了一类2,3-取代的环戊二烯-2,4-二烯基化合物用于治疗炎症和炎症相关疾病。特别感兴趣的化合物由式（II）定义，其中R 1和R 2各自独立地选自氢，低级烷基，低级羟烷基，卤素，低级卤代烷基，低级烷氧基羰基和羧基; R 3和R 4各自独立地选自氢，卤素，低级烷基，低级烷硫基，氰基，羟基，巯基，低级卤代烷基，低级卤代烷氧基，低级烷氧基，低级羟烷基，低级烷氧基烷基，低级烷基磺酰基，低级卤代烷基磺酰基和氨磺酰基; 条件是R 5和R 10都不是氢或甲氧基; 或其药学上合适的盐或前药。两个取代的苯基中的一个可以被取代的吡啶基取代。

7. 发明申请

WO2003093242A2 SUBSTITUTED 5-MEMBERED POLYCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
标题翻译：取代的5组分多环化合物可用于选择性抑制凝聚剂CASCADE
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
申请人： 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.
发明人： 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分类号： C07D231/00
CPC分类号： 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
摘要： 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.
摘要翻译：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。

8. 发明申请

WO2003029216A1 6-MEMBERED HETEROCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
标题翻译：用于选择性抑制凝聚剂CASCADE的6组分杂环化合物
公开(公告)号：WO2003029216A1
公开(公告)日：2003-04-10
申请号：PCT/US2002/031769
申请日：2002-10-03
申请人： PHARMACIA CORPORATION , SOUTH, Michael, S. , WEBBER, Ronald, K. , HUANG, Horng-Chih , TOTH, Mihaly, V. , MOORMANN, Alan, E. , SNYDER, Jeffery, 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.
发明人： SOUTH, Michael, S. , WEBBER, Ronald, K. , HUANG, Horng-Chih , TOTH, Mihaly, V. , MOORMANN, Alan, E. , SNYDER, Jeffery, 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分类号： C07D211/98
CPC分类号： 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 , C07D413/12 , C07D471/04
摘要： 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.
摘要翻译：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。

9. 发明申请

WO2011045702A1 PYRROLO[2,3-D] PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：吡咯并[2,3-D]吡嗪化合物
公开(公告)号：WO2011045702A1
公开(公告)日：2011-04-21
申请号：PCT/IB2010/054447
申请日：2010-10-01
申请人： PFIZER INC. , ACKER, Brad Alan , HARTMANN, Susan J. , HUANG, Horng-Chih , JACOBSEN, Eric Jon , PROMO, Michele Ann , WOLFSON, Sergey Gregory , XIE, Jin
发明人： ACKER, Brad Alan , HARTMANN, Susan J. , HUANG, Horng-Chih , JACOBSEN, Eric Jon , PROMO, Michele Ann , WOLFSON, Sergey Gregory , XIE, Jin
IPC分类号： C07D487/04 , A61K31/519 , A61P37/00
CPC分类号： C07D487/04
摘要： Described herein are pyrrolo[2,3-d]pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing these compounds, and methods for their preparation.
摘要翻译：本文描述的是吡咯并[2,3-d]嘧啶化合物，它们用作Janus Kinase（JAK）抑制剂，含有这些化合物的药物组合物及其制备方法。

10. 发明申请

WO2003029224A1 6-MEMBERED UNSATURATED HETEROCYCLIC COMPOUNDS USEFUL FOR SELECTIVE INHIBITION OF THE COAGULATION CASCADE 审中-公开
标题翻译： 6成员不饱和杂环化合物可用于选择性抑制凝聚剂CASCADE
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
申请人： 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.
发明人： 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分类号： C07D239/47
CPC分类号： 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
摘要： 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.
摘要翻译：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。

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