-
公开(公告)号:US07153878B2
公开(公告)日:2006-12-26
申请号:US10505089
申请日:2003-02-13
申请人: Scott Eugene Conner , James Allen Knobelsdorf , Nathan Bryan Mantlo , Jeffrey Michael Schkeryantz , Quanrong Shen , Alan M Warshawsky , Guoxin Zhu
发明人: Scott Eugene Conner , James Allen Knobelsdorf , Nathan Bryan Mantlo , Jeffrey Michael Schkeryantz , Quanrong Shen , Alan M Warshawsky , Guoxin Zhu
IPC分类号: A61K31/426 , A61K31/429 , A61K31/421 , A61K31/5377 , A61K31/506 , A61K31/497 , A61K31/443 , A61K31/4439 , A61K31/4525
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–C5alkyl, C1–C5alkenyl, 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,
-
公开(公告)号:US20060094768A1
公开(公告)日:2006-05-04
申请号:US10540330
申请日:2003-12-31
申请人: Nathan Mantlo , Xiaodong Wang , Guoxin Zhu
发明人: Nathan Mantlo , Xiaodong Wang , Guoxin Zhu
IPC分类号: A61K31/381 , C07D333/22 , A61K31/41 , C07D409/02 , A01N43/06 , A01N43/64 , A61K31/38 , C07D257/00
CPC分类号: C07D333/18 , C07D333/16
摘要: The present invention is directed to compounds represented by the following structural formula, Formula I: and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) X is selected from the group consisting of O, S, S(O)2, N, and a bond; (b) U is an aliphatic linker wherein one carbon atom of the aliphatic linker may be replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with R30; (c) Y is selected from the group consisting of C, O, S, NH and a single bond; and (d) E is C(R3)(R4)A or A.
摘要翻译: 本发明涉及由以下结构式式I表示的化合物及其立体异构体,药学上可接受的盐,溶剂合物和水合物,其中:(a)X选自O,S,S(O) 2,N和键; (b)U是脂族连接体,其中脂族连接体的一个碳原子可被O,NH或S取代,并且其中这种脂族连接基任选被R 30取代; (c)Y选自C,O,S,NH和单键; 和(d)E是C(R3)(R4)A或A。
-
13.
公开(公告)号:US20070249688A1
公开(公告)日:2007-10-25
申请号:US11570449
申请日:2005-06-08
申请人: Scott Conner , Guoxin Zhu , Jianke Li
发明人: Scott Conner , Guoxin Zhu , Jianke Li
IPC分类号: A61K31/195 , A61K31/44 , A61K31/4412 , A61P3/08 , C07C59/64 , C07D213/24 , C07D213/63
CPC分类号: C07D213/89 , C07C235/42 , C07C251/48 , C07C255/54 , C07C323/60 , C07C323/62 , C07C323/65 , C07C2601/02 , C07C2601/14 , C07D213/30 , C07D213/64 , C07D213/65 , C07D295/096 , C07D319/06 , C07D319/20
摘要: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译: 本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的新颖的式I化合物或其药学上可接受的盐,以及制备这些化合物的方法。 在另一个实施方案中,本发明公开了包含式I化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。
-
公开(公告)号:US07396850B2
公开(公告)日:2008-07-08
申请号:US10537282
申请日:2003-12-31
IPC分类号: A61K31/415 , C07D231/10
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。
-
公开(公告)号:US07259175B2
公开(公告)日:2007-08-21
申请号:US10505103
申请日:2003-02-13
IPC分类号: A61K31/497 , A61K31/501 , A61K31/506 , A61K31/4439 , C07D417/10 , C07D413/10
CPC分类号: C07D413/04 , C07D263/32 , C07D277/24 , C07D277/26 , C07D413/10 , C07D417/04 , C07D417/10
摘要: The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)n COOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethyl
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:其中:(a)R 5选自(C 1 -C 3) (C 1 -C 6)烷基,(C 1 -C 6 -C 6)链烯基,取代的芳基(C 0 -C 6 - 取代的芳氧基(C 0 -C 4 -C 4烷基)烷基,取代的芳硫基(C 0 -C 4 - 烷基,未取代的芳基(C 0 -C 4 -C 4)烷基,未取代的芳氧基(C 0 -C 4 - 烷基和未取代的芳硫基(C 0 -C 4 -C 4)烷基; (b)T1为C或N; (c)Q选自O,单键,O(CH 2 CH 2)q C和C; (d)q为1或2; (e)W选自O,S,(CH 2)n N(R 20)(CH 2 CH 2) C(O)N(R 20)(CH 2)n),(CH
-
16.
公开(公告)号:US08691856B2
公开(公告)日:2014-04-08
申请号:US12093601
申请日:2006-11-16
IPC分类号: A01N43/64 , A61K31/41 , C07D257/04 , C07D257/10 , C07D403/00 , C07D487/00
CPC分类号: C07D257/06 , C07D257/04
摘要: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
摘要翻译: 本发明公开了具有胰高血糖素受体拮抗剂或反向激动剂活性的式(I)的新化合物或其药学上可接受的盐,以及制备这些化合物的方法。 在另一个实施方案中,本发明公开了包含式(I)化合物的药物组合物以及使用它们治疗糖尿病和其它与胰高血糖素相关的代谢紊乱等的方法。
-
公开(公告)号:US08076374B2
公开(公告)日:2011-12-13
申请号:US12093598
申请日:2006-11-10
申请人: Mark Donald Chappell , Scott Eugene Conner , Philip Arthur Hipskind , Jason Eric Lamar , Guoxin Zhu
发明人: Mark Donald Chappell , Scott Eugene Conner , Philip Arthur Hipskind , Jason Eric Lamar , Guoxin Zhu
IPC分类号: A61K31/195 , C07C229/22 , A61P3/10
CPC分类号: C07C235/42 , C07C2601/08 , C07C2601/10 , C07D213/65
摘要: The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
-
公开(公告)号:US07696248B2
公开(公告)日:2010-04-13
申请号:US12093054
申请日:2006-11-07
申请人: Jianke Li , Scott Eugene Conner , Guoxin Zhu
发明人: Jianke Li , Scott Eugene Conner , Guoxin Zhu
IPC分类号: A61K31/195 , C07C229/00
CPC分类号: C07C237/36 , C07C255/50
摘要: The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
-
公开(公告)号:US07655641B2
公开(公告)日:2010-02-02
申请号:US10542579
申请日:2004-02-10
申请人: Scott Eugene Conner , Lynn Stacy Gossett , Jonathan Edward Green , Winton Dennis Jones, Jr. , Nathan Bryan Mantlo , Donald Paul Matthews , Daniel Ray Mayhugh , Daryl Lynn Smith , Jennifer Ann Vance , Xiaodong Wang , Alan M Warshawsky , Leonard Larry Winneroski, Jr. , Yanping Xu , Guoxin Zhu
发明人: Scott Eugene Conner , Lynn Stacy Gossett , Jonathan Edward Green , Winton Dennis Jones, Jr. , Nathan Bryan Mantlo , Donald Paul Matthews , Daniel Ray Mayhugh , Daryl Lynn Smith , Jennifer Ann Vance , Xiaodong Wang , Alan M Warshawsky , Leonard Larry Winneroski, Jr. , Yanping Xu , Guoxin Zhu
IPC分类号: A61K31/66 , A61K31/38 , C07D409/12 , C07D209/04
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。
-
公开(公告)号:US07544707B2
公开(公告)日:2009-06-09
申请号:US10596322
申请日:2004-12-16
IPC分类号: A61K31/416 , C07D231/56
CPC分类号: C07D409/12 , C07D231/56
摘要: The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) R2 is selected from the group consisting of C0-C8 alkyl and C1-4-heteroalkyl; (b) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (c) U is an aliphatic linker wherein one carbon atom of the aliphatic linker is optionally replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with from one to four substituents each independently selected from R30; (d) Y is selected from the group consisting of C, O, S, NH and a single bond; and (e) E is C(R3)(R4)A or A.
摘要翻译: 本发明涉及由下列结构式(I)表示的化合物及其立体异构体,药学上可接受的盐,溶剂化物和水合物,其中:(a)R 2选自C 0 -C 8烷基和C 1 -C 8烷基 -4-杂烷基; (b)X选自单键O,S,S(O)2和N; (c)U是脂族连接体,其中脂族连接体的一个碳原子任选被O,NH或S取代,并且其中这种脂族连接体任选地被1至4个独立地选自R 30的取代基取代; (d)Y选自C,O,S,NH和单键; 和(e)E是C(R3)(R4)A或A。
-
-
-
-
-
-
-
-
-