-
1.Substituted polycyclic aryl and heteroaryl pyridones useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译: 用于选择性抑制凝血级联的取代的多环芳基和杂芳基吡啶酮公开(公告)号:US20050165062A1
公开(公告)日:2005-07-28
申请号:US11009787
申请日:2004-12-10
申请人: Michael South , Qingping Zeng , Ashton Hamme , Melvin Rueppel
发明人: Michael South , Qingping Zeng , Ashton Hamme , Melvin Rueppel
IPC分类号: C07D213/74 , C07D213/75 , C07D213/77 , C07D215/38 , C07D401/12 , C07D417/12 , C07D521/00 , A61K31/4439 , A61K31/4415 , C07D211/84 , C07D41/02
CPC分类号: C07D213/74 , C07D213/75 , C07D213/77 , C07D215/38 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D417/12
摘要: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
摘要翻译: 本发明涉及用作凝血级联丝氨酸蛋白酶抑制剂的取代多环芳基和杂芳基吡啶酮化合物,以及用于治疗和预防各种血栓形成病症(包括冠状动脉和脑血管疾病)的抗凝血治疗的化合物,组合物和方法。
-
2.(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效
标题翻译: (R) - 用于抑制胆固醇酯转移蛋白活性的卤代取代稠合杂环氨基化合物公开(公告)号:US20050043294A1
公开(公告)日:2005-02-24
申请号:US10929013
申请日:2004-08-27
申请人: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
发明人: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC分类号: C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07D213/65 , C07D251/42 , C07D307/42 , C07D333/20 , A61K31/55 , A61K31/137 , A61K31/47
CPC分类号: C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
摘要翻译: 本发明涉及可用作胆固醇酯转移蛋白(CETP;血浆脂质转移蛋白-1)的抑制剂的取代的芳基和杂芳基(R) - 手性卤代1-取代氨基 - (n + 1) - 阿尔卡醇化合物,化合物,组合物和方法 用于治疗动脉粥样硬化和其他冠状动脉疾病。 描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。
-
3.Substituted polycyclic aryl and heteroaryl pyridines useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译: 用于选择性抑制凝血级联的取代的多环芳基和杂芳基吡啶公开(公告)号:US20050153965A1
公开(公告)日:2005-07-14
申请号:US11004437
申请日:2004-12-03
申请人: Michael South , Brenda Case , Danny Garland , Michael Hayes , Horng-Chih Huang , Wei Huang , Darin Jones , William Neumann , John Parlow , David Reitz , Melvin Rueppel , Ronald Webber
发明人: Michael South , Brenda Case , Danny Garland , Michael Hayes , Horng-Chih Huang , Wei Huang , Darin Jones , William Neumann , John Parlow , David Reitz , Melvin Rueppel , Ronald Webber
IPC分类号: A61K31/44 , A61K31/4418 , A61K31/4436 , A61K31/4439 , A61K45/00 , A61P7/02 , A61P9/10 , A61P11/00 , A61P35/00 , A61P43/00 , C07D213/74 , C07D213/89 , C07D401/10 , C07D409/04 , C07D43/02 , A61K31/444 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , C07D41/02
CPC分类号: C07D213/74 , C07D213/89
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。
-
4.(R)-Chiral Halogenated Substituted Fused Heterocyclic Amino Compounds Useful for Inhibiting Cholesterol Ester Transfer Protein Activity 审中-公开
标题翻译: (R) - 用于抑制胆固醇酯转移蛋白活性的手性卤代取代的稠合杂环氨基化合物公开(公告)号:US20070219274A1
公开(公告)日:2007-09-20
申请号:US11693161
申请日:2007-03-29
申请人: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michelle Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
发明人: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michelle Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC分类号: A61K31/135 , C07C211/43
CPC分类号: C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
摘要翻译: 本发明涉及可用作胆固醇酯转移蛋白(CETP;血浆脂质转移蛋白-1)的抑制剂的取代的芳基和杂芳基(R) - 手性卤代1-取代氨基 - (n + 1) - 阿尔卡醇化合物,化合物,组合物和方法 用于治疗动脉粥样硬化和其他冠状动脉疾病。 描述了从手性和非手性中间体制备手性取代的烷醇化合物的新型高产率立体选择性方法。
-
5.6-Membered heterocyclic compounds useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译: 可用于选择性抑制凝血级联的6-元杂环化合物公开(公告)号:US20050267123A1
公开(公告)日:2005-12-01
申请号:US11159877
申请日:2005-06-23
申请人: Michael South , Ronald Webber , Horng-Chih Huang , Mihaly Toth , Alan Moormann , Jeffery Snyder , Jeffrey Scholten , Danny Garland , Melvin Rueppel , William Neumann , Scott Long , Wei Huang , John Trujillo , John Parlow , Darin Jones , Brenda Case , Michael Hayes
发明人: Michael South , Ronald Webber , Horng-Chih Huang , Mihaly Toth , Alan Moormann , Jeffery Snyder , Jeffrey Scholten , Danny Garland , Melvin Rueppel , William Neumann , Scott Long , Wei Huang , John Trujillo , John Parlow , Darin Jones , Brenda Case , Michael Hayes
IPC分类号: C07D249/12 , A61K31/451 , A61K31/495 , A61K31/50 , A61K31/513 , A61K31/53 , A61K31/535 , A61K45/00 , A61P7/02 , A61P9/10 , A61P43/00 , C07C257/18 , C07D207/32 , C07D211/56 , C07D211/98 , C07D213/74 , 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 , C07D43/02
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。
-
公开(公告)号:US20060229304A1
公开(公告)日:2006-10-12
申请号:US11373770
申请日:2006-03-09
申请人: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
发明人: James Sikorski , Richard Durley , Margaret Grapperhaus , Mark Massa , Emily Reinhard , Yvette Fobian , Michael Tollefson , Lijuan Wang , Brian Hickory , Monica Norton , William Vernier , Deborah Mischke , Michele Promo , Ashton Hamme , Dale Spangler , Melvin Rueppel
IPC分类号: A61K31/538 , C07D265/36 , A61K31/138
CPC分类号: C07D307/42 , A61K31/138 , A61K31/538 , C07B2200/07 , C07C217/84 , C07C217/86 , C07C217/88 , C07C217/90 , C07C239/20 , C07C323/19 , C07C323/20 , C07C323/32 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D251/42 , C07D333/20
摘要: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.
-
7.Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译: 用于选择性抑制凝血级联的5元多环化合物公开(公告)号:US20050239860A1
公开(公告)日:2005-10-27
申请号:US11159684
申请日:2005-06-23
申请人: Michael South , Ronald Webber , Horng-Chih Huang , Mihaly Toth , Alan Moormann , Jeffery Snyder , Jeffrey Scholten , Danny Garland , Melvin Rueppel , William Neumann , Scott Long , Wei Huang , John Trujillo , John Parlow , Darin Jones , Brenda Case , Michael Hayes
发明人: Michael South , Ronald Webber , Horng-Chih Huang , Mihaly Toth , Alan Moormann , Jeffery Snyder , Jeffrey Scholten , Danny Garland , Melvin Rueppel , William Neumann , Scott Long , Wei Huang , John Trujillo , John Parlow , Darin Jones , Brenda Case , Michael Hayes
IPC分类号: A61K31/166 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4152 , A61K31/4168 , A61K31/4196 , A61K31/421 , A61K31/426 , A61P7/02 , A61P9/00 , A61P11/00 , A61P35/00 , A61P43/00 , C07C257/18 , C07D207/14 , C07D207/32 , C07D207/34 , C07D207/46 , C07D211/56 , C07D211/98 , C07D213/74 , C07D231/12 , C07D231/38 , C07D231/46 , C07D231/48 , C07D233/88 , C07D237/04 , C07D239/10 , C07D239/22 , C07D241/04 , C07D241/20 , C07D249/08 , C07D249/14 , C07D253/06 , C07D253/075 , C07D263/48 , C07D265/02 , C07D277/20 , C07D277/42 , C07D307/22 , C07D333/36 , C07D401/12 , C07D403/10 , C07D413/12 , C07D471/04 , C07D231/44
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.Substituted polycyclic aryl and heteroaryl pyrimidinones useful for selective inhibition of the coagulation cascade 审中-公开
标题翻译: 用于选择性抑制凝血级联的取代的多环芳基和杂芳基嘧啶酮公开(公告)号:US20050054643A1
公开(公告)日:2005-03-10
申请号:US10680873
申请日:2003-10-07
申请人: Michael South , Ashton Hamme , William Neumann , Darin Jones , Melvin Rueppel
发明人: Michael South , Ashton Hamme , William Neumann , Darin Jones , Melvin Rueppel
IPC分类号: C07D239/46 , C07D239/47 , C07D253/07 , C07D401/04 , C07D417/12 , A61K31/53
CPC分类号: C07D239/47 , C07D253/07 , C07D401/04 , C07D417/12
摘要: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
摘要翻译: 本发明涉及可用作凝血级联丝氨酸蛋白酶抑制剂的取代的多环芳基和杂芳基嘧啶酮化合物,以及用于治疗和预防各种血栓形成疾病(包括冠状动脉和脑血管疾病)的抗凝血治疗的化合物,组合物和方法。
-
9.
公开(公告)号:US20050043313A1
公开(公告)日:2005-02-24
申请号:US10940693
申请日:2004-09-14
申请人: Michael South , Brenda Case , Thomas Dice , Ricky Fenton , Gary Franklin , Michael Hayes , Horng-Chih Huang , Wei Huang , Darin Jones , Carrie Kusturin , Richard Lindmark , Scott Long , William Neumann , David Reitz , John Trujillo , Ching-Cheng Wang , Rhonda Wood , Qingping Zeng , Matthew Mahoney , John Parlow , Melvin Rueppel
发明人: Michael South , Brenda Case , Thomas Dice , Ricky Fenton , Gary Franklin , Michael Hayes , Horng-Chih Huang , Wei Huang , Darin Jones , Carrie Kusturin , Richard Lindmark , Scott Long , William Neumann , David Reitz , John Trujillo , Ching-Cheng Wang , Rhonda Wood , Qingping Zeng , Matthew Mahoney , John Parlow , Melvin Rueppel
IPC分类号: A61K38/00 , C07D241/20 , C07D401/12 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/06 , C07K5/078 , A61K31/4965 , A61K31/497 , C07D43/02
CPC分类号: C07D401/12 , A61K38/00 , C04B35/632 , C07D241/20 , C07D403/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/06139 , C07K5/06191
摘要: The invention relates to substituted polycyclic aryl and heteroaryl pyrazinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.
-
-
-
-
-
-
-
-