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公开(公告)号：EP1169312A2
公开(公告)日：2002-01-09
申请号：EP00918816.0
申请日：2000-03-20
发明人： BIZZARRO, Fred, Thomas , CORBETT, Wendy, Lea , FOCELLA, Antonino , GRIPPO, Joseph, Francis , HAYNES, Nancy-Ellen , HOLLAND, George, William , KESTER, Robert, Francis , MAHANEY, Paige, E. , SARABU, Ramakanth
IPC分类号： C07D277/46 , A61K31/426 , C07D277/56 , C07D213/75 , A61K31/42 , A61P3/10
CPC分类号： C07D213/75 , C07C275/50 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/80 , C07D213/82 , C07D233/88 , C07D237/22 , C07D239/42 , C07D253/07 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/56 , C07D277/58 , C07D285/135
摘要： The present invention relates to compounds of formula (I) wherein R?1, R2, R3 and R4¿ are as defined in claim 1 and pharmaceutically acceptable salts thereof. The compounds are glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
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2.发明公开
公开(公告)号：EP1282611A1
公开(公告)日：2003-02-12
申请号：EP01933901.9
申请日：2001-04-27
IPC分类号： C07D277/46 , C07D277/56 , C07D213/75 , C07D213/80 , C07D417/12 , C07D213/56 , C07D209/18 , C07D295/155 , C07C317/44 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/404 , A61K31/17 , A61P3/10
CPC分类号： C07D213/75 , C07C317/44 , C07C2601/08 , C07C2601/14 , C07D209/18 , C07D213/56 , C07D213/80 , C07D277/46 , C07D277/56 , C07D295/155 , C07D417/12
摘要： Compounds of formula (I) wherein X is oxygen or sulfonyl, R is a ring, R1 is cycloalkyl, y and z are 0 or 1, and R2 is -CO-NHR3 or a heteroaromatic ring having a ring nitrogen atom adjacent to the connecting ring carbon atom, are active as glucokinase activators to increase insulin secretion, which makes them useful for treating type II diabetes.
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公开(公告)号：EP1341774B1
公开(公告)日：2006-02-01
申请号：EP01999565.3
申请日：2001-11-28
发明人： CORBETT, Wendy, Lea , GRIMBSY, Joseph, Samuel , HAYNES, Nancy-Ellen , KESTER, Robert, Francis , MAHANEY, Paige, Erin , SARABU, Ramakanth
IPC分类号： C07D263/58 , C07D277/82 , C07D235/30 , C07D215/38 , A61K31/423 , A61K31/428 , A61K31/4184 , A61K31/47 , A61P3/10
CPC分类号： C07D215/38 , C07D235/30 , C07D263/58 , C07D277/82
摘要： Glucokinase activating compounds or pharmaceutically acceptable salts of Formula I-0: wherein M is Formula II or Formula III; Q is Formula IV or Formula V; R1 is an alkyl having from 1 to 3 carbon atoms; R2 is hydrogen, halo, nitro, cyano, or perfluoro-methyl; R3 is a cycloalkyl having from 4 to 7 carbon atoms or 2-propyl; R5 is halogen; R6 is halogen; W is O, S or NH; each Y is independently CH or N; Z is CH¿2?-CH2-CH2-CH2 or CH=CR?4¿-CH=CH-, wherein R4 is hydrogen, halo, or an alkyl sulfone having from 1 to 3 carbon atoms; and dotted lines collectively represent O or 2 additional double bonds in the heterocyclic ring structure. Compounds of Formula 1-0 may be present either as a racemate or in the isolated 'R' configuration at the asymmetric carbon shown.
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4.发明公开
公开(公告)号：EP1501815A1
公开(公告)日：2005-02-02
申请号：EP03749855.7
申请日：2003-04-14
发明人： CORBETT, Wendy, Lea , GRIMSBY, Joseph, Samuel , HAYNES, Nancy-Ellen , KESTER, Robert, Francis , MAHANEY, Paige, Erin , RACHA, Jagdish, Kumar , SARABU, Ramakanth , WANG, Ka
IPC分类号： C07D307/16 , C07D309/04 , C07D417/12 , C07D405/12 , C07D241/20 , C07D409/12 , C07D277/46 , C07D213/75 , C07C275/52 , A61K31/335 , A61K31/38 , A61K31/425 , A61K31/4965 , A61K31/44 , A61P3/10
CPC分类号： C07D213/75 , C07C275/50 , C07C2601/08 , C07D241/20 , C07D277/46 , C07D307/16 , C07D309/04 , C07D405/12 , C07D409/12 , C07D417/12
摘要： Compounds of the formula (I); wherein formula (II) represents a substituted group, an oxa-cycloalkyl group or a thia-cycloalkyl group, are glucokinase activators useful in the treatment of type II diabetes.
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公开(公告)号：EP1169312B1
公开(公告)日：2004-10-06
申请号：EP00918816.0
申请日：2000-03-20
发明人： BIZZARRO, Fred, Thomas , CORBETT, Wendy, Lea , FOCELLA, Antonino , GRIPPO, Joseph, Francis , HAYNES, Nancy-Ellen , HOLLAND, George, William , KESTER, Robert, Francis , MAHANEY, Paige, E. , SARABU, Ramakanth
IPC分类号： C07D277/46 , A61K31/426 , C07D277/56 , C07D213/75 , A61K31/42 , A61P3/10
CPC分类号： C07D213/75 , C07C275/50 , C07C317/44 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07D213/80 , C07D213/82 , C07D233/88 , C07D237/22 , C07D239/42 , C07D253/07 , C07D261/14 , C07D263/48 , C07D277/46 , C07D277/56 , C07D277/58 , C07D285/135
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公开(公告)号：EP1549638B1
公开(公告)日：2007-10-03
申请号：EP03750648.2
申请日：2003-09-26
发明人： CORBETT, Wendy, Lea
IPC分类号： C07D403/12 , C07D401/12 , C07D417/12 , A61K31/427 , A61P3/10
CPC分类号： C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention provides glucokinase activators of formula (I), wherein R1, R2 and R3 are defined in the specification. Glucokinase activators are useful for increasing insulin secretion in the treatment of type II diabetes.
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公开(公告)号：EP1572670B1
公开(公告)日：2007-08-22
申请号：EP03767788.7
申请日：2003-12-11
发明人： CHEN, Shaoqing , CORBETT, Wendy, Lea , GUERTIN, Kevin, Richard , HAYNES, Nancy-Ellen , KESTER, Robert, Francis , MENNONA, Francis, A. , MISCHKE, Steven, Gregory , QIAN, Yimin , SARABU, Ramakanth , SCOTT, Nathan, Robert , THAKKAR, Kshitij, Chhabilbhai
IPC分类号： C07D241/26 , A61P3/10 , A61K31/50 , C07D213/78 , C07D241/20 , C07D213/76 , C07D213/75 , C07D413/04 , C07D417/06 , C07D403/06 , C07D405/04 , C07D405/06 , C07D403/04 , C07D409/04 , A61K31/501 , A61K31/44 , A61K31/4436
CPC分类号： C07D213/75 , C07D213/76 , C07D213/78 , C07D241/20 , C07D241/26 , C07D403/06 , C07D405/04 , C07D405/06 , C07D409/04 , C07D413/04 , C07D417/06
摘要： The present invention provides a compound according to formula (I) where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula (I) are also provided, said compounds being glucokinase activators which are useful in the treatment of type II diabetes.
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公开(公告)号：EP1549638A1
公开(公告)日：2005-07-06
申请号：EP03750648.2
申请日：2003-09-26
发明人： CORBETT, Wendy, Lea
IPC分类号： C07D403/12 , C07D401/12 , C07D417/12 , A61K31/427 , A61P3/10
CPC分类号： C07D401/12 , C07D403/12 , C07D417/12
摘要： The present invention provides glucokinase activators of formula (I), wherein R1, R2 and R3 are defined in the specification. Glucokinase activators are useful for increasing insulin secretion in the treatment of type II diabetes.
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9.发明授权SUBSTITUTED PHENYLACETAMIDES AND THEIR USE AS GLUCOKINASE ACTIVATORS 有权SUBSTITUIERTE PHENYLACETAMIDE UND IHRE VERWENDUNG ALS GLUKOKINASE AKTIVATOREN
公开(公告)号：EP1282611B1
公开(公告)日：2004-10-20
申请号：EP01933901.9
申请日：2001-04-27
IPC分类号： C07D277/46 , C07D277/56 , C07D213/75 , C07D213/80 , C07D417/12 , C07D213/56 , C07D209/18 , C07D295/155 , C07C317/44 , A61K31/426 , A61K31/427 , A61K31/44 , A61K31/4427 , A61K31/404 , A61K31/17 , A61P3/10
CPC分类号： C07D213/75 , C07C317/44 , C07C2601/08 , C07C2601/14 , C07D209/18 , C07D213/56 , C07D213/80 , C07D277/46 , C07D277/56 , C07D295/155 , C07D417/12
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公开(公告)号：EP1242397A1
公开(公告)日：2002-09-25
申请号：EP00987392.8
申请日：2000-12-12
IPC分类号： C07D277/46 , A61K31/426 , C07D213/75 , C07D277/56 , C07C275/50 , A61K31/4402 , A61K31/44 , A61K31/17 , A61P3/10
CPC分类号： C07D213/75 , C07C275/50 , C07C317/44 , C07C2601/08 , C07C2601/14 , C07D277/46
摘要： 2,3-Di-substituted trans olefinic N-heteroaromatic or urido proprionamides of formula (I) with said substitution at the 2-position being a substituted phenyl group and at the 3-position being a cycloalkyl ring, said proprionamides being glucokinase activators which increase insulin secretion in the treatment of type II diabetes.
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