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公开(公告)号:US08133907B2
公开(公告)日:2012-03-13
申请号:US11996126
申请日:2006-07-14
申请人: Larry Chris Blaszczak , Brian Michael Mathes , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
发明人: Larry Chris Blaszczak , Brian Michael Mathes , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
IPC分类号: A61K31/4425 , A61K31/44 , C07D213/56 , C07D401/06
CPC分类号: C07D213/82 , C07D213/38
摘要: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中A为(1); X选自CH,CF和N; R5选自H,C1-C6烷基,C1-C6氟烷基和-OR12; R 9选自H -NR 13 C(O)R 14和-C(O)NR 10 R 11; R12选自H,C1-C6烷基和C3-C6环烷基,用作DPP-IV酶的抑制剂,用于治疗或预防包括II型糖尿病的病症。
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公开(公告)号:US20080214616A1
公开(公告)日:2008-09-04
申请号:US11996126
申请日:2006-07-14
申请人: Larry Chris Blaszczak , Brian Michael Mathes , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
发明人: Larry Chris Blaszczak , Brian Michael Mathes , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
IPC分类号: A61K31/44 , C07D213/46 , A61K31/444 , A61P3/00
CPC分类号: C07D213/82 , C07D213/38
摘要: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C1-C6 fluoroalkyl, and —OR12; R9 is selected from H —NR13C(O)R14 and —C(O)NR10R11; R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中A为(1); X选自CH,CF和N; R 5选自H,C 1 -C 6氟代烷基和-OR 12; R 9选自H -NR 13 C(O)R 14和-C(O)NR 10 R 11; R 12选自H,C 1 -C 6烷基和C 3 -C 6环烷基,用于 作为DPP-IV酶的抑制剂,用于治疗或预防包括II型糖尿病的病症。
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3.
公开(公告)号:US20080221217A1
公开(公告)日:2008-09-11
申请号:US11996123
申请日:2006-07-14
申请人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
发明人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
IPC分类号: A61K31/166 , C07C233/65 , A61K31/155 , A61P3/00
CPC分类号: C07C237/44 , C07C237/30
摘要: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR11, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中A是(xx); X选自CH,CF和N,R 5选自H,C 1 -C 6烷基,C 1 -C 6 > - >烷基,-OR 12,R 9选自H和-C(O)NR 1 OR 11,R 12选自H,C 1 -C 6 - 烷基和C 3 -C 6环烷基,用作DPP-IV酶的抑制剂,用于治疗或预防包括II型糖尿病的病症。
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4.
公开(公告)号:US08076514B2
公开(公告)日:2011-12-13
申请号:US11996123
申请日:2006-07-14
申请人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
发明人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Brian Morgan Watson , Michael Robert Wiley
IPC分类号: C07C233/65 , A61K31/165
CPC分类号: C07C237/44 , C07C237/30
摘要: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR1 1, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中A是(xx); X选自CH,CF和N,R 5选自H,C 1 -C 6烷基,C 1 -C 6氟烷基和-OR 12,R 9选自H和-C(O)NR 1 OR 11,R 12选自H, C1-C6烷基和C3-C6环烷基,用作DPP-IV酶的抑制剂,用于治疗或预防包括II型糖尿病的病症。
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公开(公告)号:US08106090B2
公开(公告)日:2012-01-31
申请号:US11996128
申请日:2006-07-14
申请人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Michael Robert Wiley
发明人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Michael Robert Wiley
IPC分类号: C07D207/04 , A61K31/40
CPC分类号: C07C311/05 , C07C215/28 , C07C233/36 , C07C233/78 , C07D207/06 , C07D207/08 , C07D207/16 , C07D209/44 , C07D211/26 , C07D217/04 , C07D231/12 , C07D233/54 , C07D235/06 , C07D249/04 , C07D249/18 , C07D295/13 , C07D487/04
摘要: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中A为(II); X选自CH,CF和N,R8选自H,C1-C6烷基,芳基,杂芳基,C1-C6烷基芳基,C1-C6烷基杂芳基,C2-C6烷基-O-C1-C6烷基,C1-C6 卤代烷基,羟基C 2 -C 6烷基,-C(O)R 9和-SO 2 R 9,或R 7和R 8结合形成(III),(IV); W选自CR1O和CR15,R1O选自H,卤素,-C(O)NR13R14,C1-C6烷基,芳基,杂芳基,C1-C6烷基芳基,C1-C6烷基杂芳基,C1-C6烷基-O-C1 -C 1-6烷基和羟基C 1 -C 6烷基; Het是任选被1-3个选自甲氧基,Cl,F,CH 3,CF 3,芳基,杂芳基,C 1 -C 4烷基芳基或C 1 -C 4烷基杂芳基的取代基取代的N-连接的5元杂芳基环,用作 DPP-IV酶在治疗或预防包括II型糖尿病的病症中。
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公开(公告)号:US20080207735A1
公开(公告)日:2008-08-28
申请号:US11996128
申请日:2006-07-14
申请人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Michael Robert Wiley
发明人: Larry Chris Blaszczak , Shon Roland Pulley , Michael Alan Robertson , Scott Martin Sheehan , Qing Shi , Michael Robert Wiley
IPC分类号: A61K31/40 , C07C215/28 , A61K31/138 , A61P3/10 , A61P3/04 , C07D207/09
CPC分类号: C07C311/05 , C07C215/28 , C07C233/36 , C07C233/78 , C07D207/06 , C07D207/08 , C07D207/16 , C07D209/44 , C07D211/26 , C07D217/04 , C07D231/12 , C07D233/54 , C07D235/06 , C07D249/04 , C07D249/18 , C07D295/13 , C07D487/04
摘要: The present invention is directed to compounds of formula (I): or a pharmaceutically acceptable salt thereof; wherein A is (II); X is selected from CH, CF and N, R8 is selected from H, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C2-C6 alkyl-O—C1-C6 alkyl, C1-C6 haloalkyl, hydroxy C2-C6 alkyl, —C(O)R9 and —SO2R9, or R7 and R8 combine to form (III), (IV); W is selected from CR1O and CR15, R1O is selected from H, halo, —C(O)NR13R14, C1-C6 alkyl, aryl, heteroaryl, C1-C6 alkylaryl, C1-C6 alkylheteroaryl, C1-C6 alkyl-O—C1-C6 alkyl and hydroxy C1-C6 alkyl; Het is a N-linked 5-membered heteroaryl ring optionally substituted with 1-3 substituents selected from methoxy, Cl, F, CH3, CF3, aryl, heteroaryl, C1-C4 alkylaryl or C1-C4 alkylheteroaryl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
摘要翻译: 本发明涉及式(I)化合物或其药学上可接受的盐; 其中A为(II); X选自CH,CF和N,R 8选自H,C 1 -C 6烷基,芳基,杂芳基,C 1〜 C 6烷基芳基,C 1 -C 6烷基杂芳基,C 2 -C 6烷基芳基,C 1 -C 6烷基芳基,C 1 -C 6烷基芳基, 烷基-C 1 -C 6烷基,C 1 -C 6卤代烷基,羟基C
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