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公开(公告)号:US20060241157A1
公开(公告)日:2006-10-26
申请号:US10540341
申请日:2003-12-31
申请人: Scott Conner , Tianwei Ma , Nathan Mantlo , Daniel Mayhugh , Jeffrey Schkeryantz , Alan Warshawsky , Guoxin Zhu
发明人: Scott Conner , Tianwei Ma , Nathan Mantlo , Daniel Mayhugh , Jeffrey Schkeryantz , Alan Warshawsky , Guoxin Zhu
IPC分类号: A61K31/425 , A61K31/42 , A61K31/415 , C07D261/02 , C07D231/12
CPC分类号: C07D231/12 , C07D233/20 , C07D233/22 , C07D233/64 , C07D249/06 , C07D253/04 , C07D261/08
摘要: The present invention is directed to compounds represented by the following structural formula, Formula I: wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) E is C(R3)(R4)A or A and wherein (i) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsulfonamide; (e) Z1 and Z2 are each independently selected from the group consisting of N, O, and C with the proviso that at least one of Z1 and Z2 is N; (f) Z3 is selected from the group consisting of N, O, and C. (g) R8 is selected from the group consisting of hydrogen, C1-C6 alkyl, C1-C4 alkylenyl and halo; (h) R9 is selected from the group consisting of hydrogen, C1-C4 alkyl, C1-C4 alkylenyl, halo, aryl-C0-C4 alkyl, heteroaryl, C1-C6 allyl, and OR29.
摘要翻译: 本发明涉及由以下结构式(I)表示的化合物:其中:(a)X选自单键,O,S,S(O)2和N; (b)U是脂族连接体; (c)Y选自O,C,S,NH和单键; (d)E是C(R3)(R4)A或A,其中(i)A选自羧基,四唑,C 1 -C 6烷基腈,甲酰胺,磺酰胺和酰基磺酰胺; (e)Z1和Z2各自独立地选自N,O和C,条件是Z1和Z2中的至少一个是N; (f)Z 3选自N,O和C.(g)R 8选自氢,C 1 -C 6烷基,C 1 -C 4亚烷基和卤素; (h)R 9选自氢,C 1 -C 4烷基,C 1 -C 4亚烷基,卤素,芳基-C 0 -C 4烷基,杂芳基,C 1 -C 6烯丙基和OR 29。
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公开(公告)号:US20070112045A1
公开(公告)日:2007-05-17
申请号:US10580202
申请日:2004-12-21
申请人: Nathan Mantlo , Antonio Navarro , Ashraf Saeed , Douglas Gernert , Tianwei Ma , Lance Pfeifer
发明人: Nathan Mantlo , Antonio Navarro , Ashraf Saeed , Douglas Gernert , Tianwei Ma , Lance Pfeifer
IPC分类号: A61K31/433 , A61K31/4245 , A61K31/4196 , C07D285/12 , C07D271/10 , C07D249/08
CPC分类号: A61K31/4196 , A61K31/4245 , A61K31/433 , C07D249/08 , C07D271/107 , C07D285/12
摘要: The present invention is directed to compounds represented by the following structural formula, Formula (I): wherein: (a) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (b) U is an aliphatic linker; (c) Y is selected from the group consisting of O, C, S, NH and a single bond; (d) W is N, O or S; (e) E is C(R3)(R4)A or A and wherein; (f) A is selected from the group consisting of carboxyl, tetrazole, C1-C6 alkylnitrile, carboxamide, sulfonamide and acylsufonamide. The other substituents are defined in the claims; the compounds are modulators of peroxisome proleferator activated receptors (PPARs) and are useful for the treatment of diabetes and other metabolic disorders.
摘要翻译: 本发明涉及由下列结构式(I)表示的化合物:其中:(a)X选自单键,O,S,S(O)2, SUB>和N; (b)U是脂族连接体; (c)Y选自O,C,S,NH和单键; (d)W是N,O或S; (e)E是C(R3)(R4)A或A,其中; (f)A选自羧基,四唑,C 1 -C 6烷基腈,甲酰胺,磺酰胺和酰基磺酰胺。 其它取代基在权利要求书中定义; 该化合物是过氧化物酶体促进剂激活受体(PPAR)的调节剂,可用于治疗糖尿病和其他代谢紊乱。
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公开(公告)号:US20070106095A1
公开(公告)日:2007-05-10
申请号:US10579563
申请日:2004-11-16
申请人: Jianliang Lu , Tianwei Ma , Sunil Nagpal , Quanrong Shen , Alan Warshawsky , Jason Ochoada , Ying Yee
发明人: Jianliang Lu , Tianwei Ma , Sunil Nagpal , Quanrong Shen , Alan Warshawsky , Jason Ochoada , Ying Yee
IPC分类号: C07C303/00
CPC分类号: C07D405/12 , C07D307/80 , C07D407/12
摘要: The present invention relates to novel, non-secosteroidal, phenyl-benzofuran compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
摘要翻译: 本发明涉及具有维生素D受体(VDR)调节活性的新颖非壬基苯基 - 苯并呋喃化合物,其比1α,25二羟基维生素D3低高钙血症。 这些化合物可用于治疗骨病和牛皮癣。
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公开(公告)号:US20100099725A1
公开(公告)日:2010-04-22
申请号:US12522723
申请日:2008-02-12
申请人: Lance Allen Pfeifer , Tianwei Ma , Nathan Bryan Mantlo , Laura Frey Michael , Fese Mambo Mokube , Chahrzad Montrose-Rafizadeh
发明人: Lance Allen Pfeifer , Tianwei Ma , Nathan Bryan Mantlo , Laura Frey Michael , Fese Mambo Mokube , Chahrzad Montrose-Rafizadeh
IPC分类号: A61K31/4196 , C07D249/12 , A61P9/10
CPC分类号: C07D401/06 , C07D249/12
摘要: The present invention is directed to compounds of the structural Formula: wherein: R1 is H or —C1-C3 alkyl; R2 is selected from the group consisting of —H, —C1-C4 alkyl, —C1-C3 alkyl-CF3, phenyl, and pyridinyl; and R3 is selected from the group consisting of —H, —C1-C4 alkyl, —C1-C3 alkyl-O—CH3, —CH2-cyclopropyl, CH2—C═CH2, —CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; provided that when R1 and R2 are each H, then R3 is selected from the group consisting of —C1-C4 alkyl, —C1-C3 alkyl-O—CH3, —CH2-cyclopropyl, —CH2—C═CH2, —CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; or stereoisomers and pharmaceutically acceptable salts thereof.
摘要翻译: 本发明涉及结构式的化合物:其中:R 1是H或-C 1 -C 3烷基; R 2选自-H,-C 1 -C 4烷基,-C 1 -C 3烷基-CF 3,苯基和吡啶基; 并且R 3选自-H,-C 1 -C 4烷基,-C 1 -C 3烷基-O-CH 3,-CH 2 - 环丙基,CH 2-C≡CH2,-CH 2 CH 2 - (2-F-苯基), 和被1至2个氟取代的苯基; 条件是当R 1和R 2各自为H时,R 3选自-C 1 -C 4烷基,-C 1 -C 3烷基-O-CH 3,-CH 2 - 环丙基,-CH 2-C≡CH2,-CH 2 CH 2 - (2-F-苯基)和被1至2个氟取代的苯基; 或立体异构体及其药学上可接受的盐。
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公开(公告)号:US07601850B2
公开(公告)日:2009-10-13
申请号:US10515403
申请日:2003-05-22
申请人: Karl Robert Dahnke , Robert Peter Gajewski , Charles David Jones , Jared Harris Linebarger , Jianliang Lu , Tianwei Ma , Sunil Nagpal , Todd Parker Simard , Ying Kwong Yee , Emilio Enrique Bunel , Ryan Edward Stites
发明人: Karl Robert Dahnke , Robert Peter Gajewski , Charles David Jones , Jared Harris Linebarger , Jianliang Lu , Tianwei Ma , Sunil Nagpal , Todd Parker Simard , Ying Kwong Yee , Emilio Enrique Bunel , Ryan Edward Stites
IPC分类号: C07D333/06 , C07D333/26
CPC分类号: C07F9/655345 , C07D333/18 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/34 , C07D333/38 , C07D333/40 , C07D409/06 , C07D409/12 , C07D413/04
摘要: The present invention relates to novel, non-secosteroidal, phenyl-thiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
摘要翻译: 本发明涉及具有维生素D受体(VDR)调节活性的新型非甾体类苯基噻吩化合物,其比1α,25二羟基维生素D3低钙高。 这些化合物可用于治疗骨病和牛皮癣。
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公开(公告)号:US07468449B2
公开(公告)日:2008-12-23
申请号:US10578991
申请日:2004-11-16
申请人: Robert Peter Gajewski , Charles David Jones , Jianliang Lu , Tianwei Ma , Sunil Nagpal , Ying Kwong Yee
发明人: Robert Peter Gajewski , Charles David Jones , Jianliang Lu , Tianwei Ma , Sunil Nagpal , Ying Kwong Yee
IPC分类号: C07D307/02 , A61K31/34
CPC分类号: C07D307/68
摘要: The present invention relates to novel, non-secosteroidal, phenyl-furan compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
摘要翻译: 本发明涉及具有维生素D受体(VDR)调节活性的新型非甾体甾体苯基呋喃化合物,其比1α,25二羟基维生素D3低钙高。 这些化合物可用于治疗骨病和牛皮癣。
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公开(公告)号:US07772425B2
公开(公告)日:2010-08-10
申请号:US12470677
申请日:2009-05-22
申请人: Emilio Enrique Bunel , Robert Peter Gajewski , Charles David Jones , Jianliang Lu , Tianwei Ma , Sunil Nagpal , Ying Kwong Yee
发明人: Emilio Enrique Bunel , Robert Peter Gajewski , Charles David Jones , Jianliang Lu , Tianwei Ma , Sunil Nagpal , Ying Kwong Yee
IPC分类号: C07C229/00 , C07C233/64 , A61K31/59 , A61K31/195 , A61K31/166
CPC分类号: C07D207/27 , C07C59/48 , C07C59/64 , C07C59/66 , C07C59/90 , C07C65/24 , C07C65/34 , C07C65/40 , C07C69/732 , C07C69/734 , C07C69/738 , C07C69/76 , C07C69/94 , C07C235/34 , C07C235/42 , C07C311/51 , C07C317/28 , C07D207/26 , C07D233/78 , C07D257/04 , C07D257/06 , C07D261/12 , C07D271/113 , C07D277/34 , C07D295/185
摘要: The present invention relates to novel, non-secosteroidal, diaryl compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
摘要翻译: 本发明涉及具有维生素D受体(VDR)调节活性的新型非 - 非甾体二芳基化合物,其比1α,25二羟基维生素D3低钙血红素。 这些化合物可用于治疗骨病和牛皮癣。
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公开(公告)号:US07579488B2
公开(公告)日:2009-08-25
申请号:US10579563
申请日:2004-11-16
申请人: Jianliang Lu , Tianwei Ma , Sunil Nagpal , Quanrong Shen , Alan M. Warshawsky , Jason Matthew Ochoada , Ying Kwong Yee
发明人: Jianliang Lu , Tianwei Ma , Sunil Nagpal , Quanrong Shen , Alan M. Warshawsky , Jason Matthew Ochoada , Ying Kwong Yee
IPC分类号: C07D307/87 , C07D307/00
CPC分类号: C07D405/12 , C07D307/80 , C07D407/12
摘要: The present invention relates to novel, non-secosteroidal, phenyl-benzofuran compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1α,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.
摘要翻译: 本发明涉及具有维生素D受体(VDR)调节活性的新颖非壬基苯基 - 苯并呋喃化合物,其比1α,25二羟基维生素D3低高钙血症。 这些化合物可用于治疗骨病和牛皮癣。
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公开(公告)号:US08106077B2
公开(公告)日:2012-01-31
申请号:US12298769
申请日:2007-05-22
申请人: Michael Gregory Bell , Robert Anthony Doti , Matthew Scott Dowling , Michael James Genin , Peter Ambrose Lander , Tianwei Ma , Nathan Bryan Mantlo , Jason Matthew Ochoada , Lindsay Scott Stelzer , Ryan Edward Stites , Alan M Warshawsky
发明人: Michael Gregory Bell , Robert Anthony Doti , Matthew Scott Dowling , Michael James Genin , Peter Ambrose Lander , Tianwei Ma , Nathan Bryan Mantlo , Jason Matthew Ochoada , Lindsay Scott Stelzer , Ryan Edward Stites , Alan M Warshawsky
IPC分类号: A61K31/4192 , C07D249/06
CPC分类号: C07D249/06 , C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12
摘要: Compounds of formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
摘要翻译: 公开了其中变量如本文所定义的式(I)化合物及其药物组合物和使用方法用于治疗血脂异常和相关疾病。
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公开(公告)号:US07863302B2
公开(公告)日:2011-01-04
申请号:US12159224
申请日:2007-02-02
申请人: Michael Gregory Bell , Michael James Genin , Peter Ambrose Lander , Lindsay Scott Stelzer , Robert Anthony Doti , Francisco Javier Agejas-Chicharro , Ana Belen Bueno Melendo , Peter Rudolph Manninen , Jason Matthew Ochoada , Quanrong Shen , Alan M. Warshawsky , Tianwei Ma , Ryan Edward Stites
发明人: Michael Gregory Bell , Michael James Genin , Peter Ambrose Lander , Lindsay Scott Stelzer , Robert Anthony Doti , Francisco Javier Agejas-Chicharro , Ana Belen Bueno Melendo , Peter Rudolph Manninen , Jason Matthew Ochoada , Quanrong Shen , Alan M. Warshawsky , Tianwei Ma , Ryan Edward Stites
IPC分类号: A61K31/4245 , A61K31/422 , A61K31/428 , A61P3/10 , C07D261/06 , C07D275/04 , C07D277/20
CPC分类号: C07D413/12 , C07D413/14 , C07D417/12
摘要: Compounds of formula and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
摘要翻译: 公开的化合物及其药物组合物和使用方法可用于治疗血脂异常和相关疾病。
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