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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.
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2.发明申请(R)-Chiral Halogenated Substituted Fused Heterocyclic Amino Compounds Useful for Inhibiting Cholesterol Ester Transfer Protein Activity 审中-公开（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。
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3.发明申请(R)-chiral halogenated substituted fused heterocyclic amino compounds useful for inhibiting cholesterol ester transfer protein activity 失效（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。
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公开(公告)号：US20070088033A1
公开(公告)日：2007-04-19
申请号：US11531492
申请日：2006-09-13
申请人： Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
发明人： Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
IPC分类号： A61K31/53 , A61K31/506 , A61K31/497 , A61K31/4439 , A61K31/4545 , A61K31/4709 , C07D417/02 , C07D403/02 , C07D401/02
CPC分类号： C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
摘要： Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
摘要翻译： 公开了式I化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， >和R 5＆gt;在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物，制备化合物的方法和使用该化合物的治疗方法。
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公开(公告)号：US20060211694A1
公开(公告)日：2006-09-21
申请号：US11226556
申请日：2005-09-14
申请人： Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
发明人： Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
IPC分类号： A61K31/53 , A61K31/506 , A61K31/498 , A61K31/497 , A61K31/501 , A61K31/4439 , A61K31/4747 , A61K31/4709 , A61K31/4412
CPC分类号： C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
摘要： Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
摘要翻译： 公开了式I化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， >和R 5＆gt;在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物，制备化合物的方法和使用该化合物的治疗方法。
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公开(公告)号：US20050176775A1
公开(公告)日：2005-08-11
申请号：US10918826
申请日：2004-08-13
申请人： Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marrufo , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
发明人： Balekudru Devadas , John Walker , Shaun Selness , Terri Boehm , Richard Durley , Rajesh Devraj , Brian Hickory , Paul Rucker , Kevin Jerome , Heather Madsen , Edgardo Alvira , Michele Promo , Radhika Blevis-Bal , Laura Marrufo , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey Shieh , Aruna Sambandam , Shuang Liu , Ian Scott , Kevin McGee
IPC分类号： A61K20060101 , A61K31/4412 , A61K31/4415 , A61K31/4439 , A61P29/00 , C07D211/86 , C07D213/64 , C07D213/69 , C07D213/70 , C07D213/73 , C07D213/74 , C07D213/75 , C07D213/80 , C07D213/84 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D417/04 , C07D41/02
CPC分类号： C07D213/69 , C04B35/632 , C07D213/64 , C07D213/70 , C07D213/73 , C07D213/80 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/10 , C07D417/04
摘要： Disclosed are compounds of Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
摘要翻译： 公开了式I的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4， SUB＆gt;和R 5＆gt;在本文中定义。 这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。 还公开了含有化合物的药物组合物，制备化合物的方法和使用该化合物的治疗方法。
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公开(公告)号：US20050165106A1
公开(公告)日：2005-07-28
申请号：US11032650
申请日：2005-01-10
申请人： Ronald Webber , Richard Durley , Alok Awasthi , Arijia Bergmanis , Kam Fok , Scott Ganser , Timothy Hagen , E. Hallinan , Donald Hansen , Brian Hickory , Pamela Manning , Michael Mao , Alan Moormann , Barnett Pitzele , Michelle Promo , Richard Schartman , Jeffrey Scholten , Jeffrey Snyder , Mihaly Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Tjoeng
发明人： Ronald Webber , Richard Durley , Alok Awasthi , Arijia Bergmanis , Kam Fok , Scott Ganser , Timothy Hagen , E. Hallinan , Donald Hansen , Brian Hickory , Pamela Manning , Michael Mao , Alan Moormann , Barnett Pitzele , Michelle Promo , Richard Schartman , Jeffrey Scholten , Jeffrey Snyder , Mihaly Toth , Mahima Trivedi , Sofya Tsymbalov , Foe Tjoeng
IPC分类号： A61P1/00 , A61K31/198 , A61K31/4166 , A61K31/4245 , A61P1/02 , A61P1/04 , A61P1/16 , A61P3/00 , A61P3/08 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/02 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/06 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/10 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/34 , A61P25/36 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P39/02 , A61P43/00 , C07C317/48 , C07C317/50 , C07C323/58 , C07C323/59 , C07D233/76 , C07D271/06 , C07D271/07 , C07D277/56
CPC分类号： C07D271/07 , C07C317/48 , C07C323/58 , C07C323/59 , C07D233/76 , C07D277/56
摘要： The present invention relates to amidino compounds and salts and prodrugs thereof. In another embodiment the present invention also provides a use of the present compounds in therapy, particular as nitric oxide synthase inhibitors. In a further embodiment, the present invention provides methods of making the amidino compounds.
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