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公开(公告)号:US20060217433A1
公开(公告)日:2006-09-28
申请号:US10542579
申请日:2004-02-10
申请人: Scott Conner , Lynn Gosset , Jonathan Green , Winton Jones , Nathan Mantlo , Donald Matthews , Daniel Mayhugh , Daryl Smith , Jennifer Vance , Xiaodong Wang , Alan Warshawsky , Leonard Winneroski , Yanping Xu , Guoxin Zhu
发明人: Scott Conner , Lynn Gosset , Jonathan Green , Winton Jones , Nathan Mantlo , Donald Matthews , Daniel Mayhugh , Daryl Smith , Jennifer Vance , Xiaodong Wang , Alan Warshawsky , Leonard Winneroski , Yanping Xu , Guoxin Zhu
IPC分类号: A61K31/404 , A61K31/381 , A61K31/343 , A61K31/195 , C07D333/64
CPC分类号: C07D207/08 , A61K31/00 , A61K45/06 , C07C311/13 , C07C311/17 , C07C311/19 , C07C311/29 , C07C317/14 , C07C323/49 , C07C323/52 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/08 , C07D209/48 , C07D213/64 , C07D213/71 , C07D213/74 , C07D215/36 , C07D231/12 , C07D231/18 , C07D263/32 , C07D271/12 , C07D277/36 , C07D307/79 , C07D307/82 , C07D319/18 , C07D333/34 , C07D333/62 , C07D409/04 , C07D409/12 , C07D413/04 , A61K2300/00
摘要: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
摘要翻译: 本发明涉及式(I)化合物及其药学上可接受的盐,溶剂合物,水合物或立体异构体,其可用于治疗或预防由过氧化物酶体增殖物激活受体(PPAR)介导的病症,例如综合征X型 II型糖尿病,高血糖症,高脂血症,肥胖症,凝血病,高血压,动脉硬化以及与X综合症和心血管疾病有关的其他疾病。
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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:US20060166983A1
公开(公告)日:2006-07-27
申请号:US10541555
申请日:2003-12-31
申请人: Scott Conner , James Knobelsdorf , Nathan Mantlo , Daniel Mayhugh , Xiaodong Wang , Guoxin Zhu , Jeffrey Schkeryantz , Pierre-Yves Michellys
发明人: Scott Conner , James Knobelsdorf , Nathan Mantlo , Daniel Mayhugh , Xiaodong Wang , Guoxin Zhu , Jeffrey Schkeryantz , Pierre-Yves Michellys
IPC分类号: A61K31/5377 , A61K31/454 , A61K31/4439 , A61K31/405 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号: C07D209/08 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要: The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in (I) are defined herein. Also included are compounds, methods of making compounds, and pharmaceutical compositions. The compounds of the present invention are believed to be effective in treating and preventing Syndrome X, Type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases.
摘要翻译: 本发明涉及一种通过使用结构式(I)的化合物调节过氧化物酶体增殖物激活受体的治疗方法。 (I)中的变量在本文中定义。 还包括化合物,制备化合物的方法和药物组合物。 据信本发明的化合物在治疗和预防X综合征,II型糖尿病,高血糖症,高脂血症,肥胖,凝血病,高血压,动脉粥样硬化以及与X综合征和心血管疾病相关的其它疾病方面是有效的。
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公开(公告)号:US20060217374A1
公开(公告)日:2006-09-28
申请号:US10541502
申请日:2003-12-31
申请人: Scott Conner , James Knobelsdorg , Nathan Mantlo , Daniel Mayhugh , Xiaodong Wang , Guoxin Zhu , Jeffrey Schkeryantz
发明人: Scott Conner , James Knobelsdorg , Nathan Mantlo , Daniel Mayhugh , Xiaodong Wang , Guoxin Zhu , Jeffrey Schkeryantz
IPC分类号: A61K31/5377 , A61K31/4245 , A61K31/4196 , A61K31/4178 , C07D403/02 , C07D409/02 , C07D413/02
CPC分类号: C07D263/57 , C07D209/10 , C07D235/18 , C07D277/60 , C07D277/66 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
摘要: The present invention is directed to a method of treatment by modulating a peroxisome proliferator activated receptor by employing a compound of Structural Formula (I). The variables in I are defined herein. Also included are compounds, methods of making compounds, and pharmaceutical compositions. The compounds of the present invention are believed to be effective in treating and preventing Syndrome X, Type H diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, atherosclerosis, and other disorders related to Syndrome X and cardiovascular diseases.
摘要翻译: 本发明涉及一种通过使用结构式(I)的化合物调节过氧化物酶体增殖物激活受体的治疗方法。 I中的变量在此定义。 还包括化合物,制备化合物的方法和药物组合物。 认为本发明的化合物可有效治疗和预防X综合征,H型糖尿病,高血糖症,高脂血症,肥胖症,凝血病,高血压,动脉粥样硬化以及与X综合征和心血管疾病相关的其他疾病。
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公开(公告)号:US20050020652A1
公开(公告)日:2005-01-27
申请号:US10496770
申请日:2002-11-26
申请人: Tracey Gibson , Richard Johnston , Nathan Mantlo , Richard Thompson , Leonard Winneroski , Yanping Xu , Xiaodong Wang
发明人: Tracey Gibson , Richard Johnston , Nathan Mantlo , Richard Thompson , Leonard Winneroski , Yanping Xu , Xiaodong Wang
IPC分类号: A61K31/4174 , A61K31/443 , A61K31/4709 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/12 , A61P43/00 , C07D233/32 , C07D233/66 , C07D233/70 , C07D233/76 , C07D233/78 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , A61K31/4178 , A61K31/4166
CPC分类号: C07D401/06 , C07D233/32 , C07D233/70 , C07D233/76 , C07D403/12 , C07D405/06 , C07D405/12
摘要: The present invention is directed to compounds represented by the following structural Formula (I), (a) R1 is selected from the group consisting of hydrogen, substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C6 cycloalkylaryl-C0-2-alkyl, and —CH2—C(O)—R17-R18, wherein R17 is O or NH and R18 is optionally substituted benzyl; (b) R2 is selected from the group consisting of C1-C6 alkyl, C1-C6 alkenyl, aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, C1-C4 alkyl sulfonamide, C1-C4 alkyl amide, OR10 and C3-C6 cycloalkyl; (c) W is O or S; (d) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may optionally be replaced with O, NH, S, and optionally two carbons together may form a double bond; (e) Y is selected from the group consisting of C, O, S, NH and a single bond; and (f) E is selected from the group consisting of C(R3) (R4)A, A, and a substituted or unsubstituted group selected from the group consisting of (CH2)n COOR19.
摘要翻译: 本发明涉及由以下结构式(I)表示的化合物,(a)R 1选自氢,取代或未取代的选自C 1 -C 8烷基,芳基-C 0-4 - 烷基,杂芳基 -C 0-4 - 烷基,C6环烷基芳基-C0-2 - 烷基和-CH2-C(O)-R17-R18,其中R17是O或NH,R18是任选取代的苄基; (b)R 2选自C 1 -C 6烷基,C 1 -C 6烯基,芳基-C 0-4 - 烷基,杂芳基-C 0-4 - 烷基,C 1 -C 4烷基磺酰胺,C 1 -C 4烷基酰胺,OR 10 和C 3 -C 6环烷基; (c)W为O或S; (d)X是任选取代的C1-C5亚烷基连接体,其中连接体的一个碳原子可以任选地被O,NH,S取代,并且任选地两个碳可以一起形成双键; (e)Y选自C,O,S,NH和单键; 和(f)E选自C(R 3)(R 4)A,A和选自(CH 2)n COOR 19的取代或未取代的基团。
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公开(公告)号:US20070043220A1
公开(公告)日:2007-02-22
申请号:US10537282
申请日:2003-12-31
申请人: Scott Conner , Nathan Mantlo , Daniel Mayhugh , Guoxin Zhu
发明人: Scott Conner , Nathan Mantlo , Daniel Mayhugh , Guoxin Zhu
IPC分类号: C07D231/12 , A61K31/4152
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 a compound, {2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazol-4-ylmethylsulfanyl]-phenoxy}-acetic acid and pharmaceutical uses thereof.
摘要翻译: 本发明涉及化合物{2-甲基-4- [3-甲基-1-(4-三氟甲基 - 苯基)-1H-吡唑-4-基甲基硫烷基] - 苯氧基} - 乙酸及其药物用途。
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公开(公告)号:US20050107449A1
公开(公告)日:2005-05-19
申请号:US10505089
申请日:2003-02-13
申请人: Scott Conner , James Knobelsdorf , Nathan Mantlo , Jeffrey Schkeryantz , Quanrong Shen , Alan Warshawsky , Guoxin Zhu
发明人: Scott Conner , James Knobelsdorf , Nathan Mantlo , Jeffrey Schkeryantz , Quanrong Shen , Alan Warshawsky , Guoxin Zhu
IPC分类号: A61K31/421 , A61K31/422 , A61K31/426 , A61K31/429 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P3/10 , A61P9/10 , A61P43/00 , C07D263/02 , C07D263/32 , C07D277/20 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/30 , C07D403/10 , C07D413/04 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/10 , C07D417/14 , C07D513/04
CPC分类号: C07D263/32 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/30 , C07D403/10 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10 , C07D417/14
摘要: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I. (Formula I); wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, aryl (C0-C4) alkyl, aryloxy (C0-C4) alkyl, arylthio (C0-C4) alkyl, and further wherein when R5 is alkyl, R5 can optionally combine with W to form a 6 membered cycloheteroalkyl ring that is fused with the oxazole or thiazole ring to which the R5 group is attached; (b) R9 is selected from the group consisting of C1-C5 alkyl, C1-C5 alkenyl, and arylC0-C3alkyl. (c) T1 is selected from the group consisting of C and N, (d) W is selected from the group consisting of CH2, C(O)N(R21), N(R21), N(R21)CH2, O, OCH2, S, and SO2; and (e) X is selected from the group consisting of C, CH2C, and CCH2
摘要翻译: 本发明涉及由以下结构式表示的化合物及其药学上可接受的盐,式I(式I); 其中:(a)R 5选自(C 1 -C 6 -C 6)烷基,(C 1 -C 6 - C 烷基,芳基(C 0 -C 4 -C 4)烷基,芳氧基(C 1 -C 4)烷基, 烷基,芳硫基(C 0 -C 4 -C 4)烷基,并且其中当R 5为烷基时,R 5可任意地与W结合形成6元 与R5基团连接的恶唑或噻唑环稠合的环杂烷基环; (b)R 9选自C 1 -C 5烷基,C 1 -C 5烷基,C 1 -C 5 - 烯基和芳基C 0 -C 3烷基。 (c)T 1选自C和N,(d)W选自CH 2,C(O)N( R 21),N(R 21),N(R 21)CH 2,O,OCH 2,S和SO 2; 和(e)X选自C,CH 2 C和CCH 2,
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公开(公告)号:US20060257987A1
公开(公告)日:2006-11-16
申请号:US10566291
申请日:2004-08-17
申请人: Isabel Cristina Gonzalez Valcarcel , Nathan Mantlo , Qing Shi , Minmin Wang , Leonard Winneroski , Yanping Xu , Jeremy York
发明人: Isabel Cristina Gonzalez Valcarcel , Nathan Mantlo , Qing Shi , Minmin Wang , Leonard Winneroski , Yanping Xu , Jeremy York
IPC分类号: C12N9/96
CPC分类号: C07D213/30 , A61K31/095 , A61K31/185 , A61K45/06 , C07B2200/07 , C07C59/68 , C07C59/72 , C07C59/86 , C07C59/88 , C07C59/90 , C07C61/39 , C07C62/34 , C07C251/48 , C07C317/22 , C07C323/20 , C07C323/52 , C07C323/62 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/69 , C07D239/26 , C07D261/20 , C07D263/32 , C07D277/24 , C07D307/79 , A61K2300/00
摘要: The present invention is directed to a compound of formula I, or a pharmaceutically acceptable salt, solvate, hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
摘要翻译: 本发明涉及式I化合物或其药学上可接受的盐,溶剂合物,水合物或立体异构体,其可用于治疗或预防由过氧化物酶体增殖物激活受体(PPAR)介导的病症,例如综合征X,II型 糖尿病,高血糖症,高脂血症,肥胖症,凝血病,高血压,动脉硬化以及与X综合症和心血管疾病相关的其它疾病。
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公开(公告)号:US20070082907A1
公开(公告)日:2007-04-12
申请号:US10579028
申请日:2004-11-16
申请人: Emily Canada , Lynn Gossett , Nathan Mantlo , Qing Shi , Minmin Wang , Alan Warshawsky , Yanping Xu
发明人: Emily Canada , Lynn Gossett , Nathan Mantlo , Qing Shi , Minmin Wang , Alan Warshawsky , Yanping Xu
IPC分类号: A61K31/4245 , A61K31/53 , A61K31/515 , A61K31/4709 , A61K31/427 , A61K31/4178 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号: C07D213/81 , C07C211/29 , C07C233/73 , C07C235/46 , C07C235/48 , C07C235/54 , C07C235/84 , C07C271/16 , C07C311/04 , C07C311/17 , C07C317/44 , C07C323/62 , C07D209/30 , C07D209/42 , C07D213/56 , C07D333/70
摘要: The present invention is directed to a compound of formula (I), or a pharmaceutically acceptable salt, solvate hydrate or stereoisomer thereof, which is useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐,溶剂合物水合物或立体异构体,其可用于治疗或预防由过氧化物酶体增殖物激活受体(PPAR)介导的病症,例如综合征X型 II型糖尿病,高血糖症,高脂血症,肥胖症,凝血病,高血压,动脉硬化以及与X综合症和心血管疾病有关的其他疾病。
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公开(公告)号:US20060205744A1
公开(公告)日:2006-09-14
申请号:US10539477
申请日:2003-12-31
申请人: Scott Conner , Nathan Mantlo , Guoxin Zhu
发明人: Scott Conner , Nathan Mantlo , Guoxin Zhu
IPC分类号: A61K31/519 , A61K31/4745 , A61K31/428 , A61K31/423 , C07D498/02 , C07D491/02
CPC分类号: C07D209/10 , C07D235/18 , C07D263/57 , C07D277/60 , C07D277/66 , C07D413/12 , C07D417/12 , C07D471/04 , C07D513/04
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 C, O, 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, carboxamidek, sulfonamide and acylsulfonamide; (e) B is selected from the group consisting of S, O, C, and N; (f) Z is selected from the group consisting of N and C; with the proviso that when B is C then Z is N.
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C,O,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,羧酰胺,磺酰胺和酰基磺酰胺; (e)B选自S,O,C和N; (f)Z选自N和C; 条件是当B为C时,则Z为N.
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