公开(公告)号：US5914339A

公开(公告)日：1999-06-22

申请号：US854199

申请日：1997-05-09

申请人： Fuk-Wah Sum ,  Adam M. Gilbert ,  George T. Grosu ,  Michael S. Malamas ,  Aranapakam M. Venkatesan ,  Gerardo D. Francisco

发明人： Fuk-Wah Sum ,  Adam M. Gilbert ,  George T. Grosu ,  Michael S. Malamas ,  Aranapakam M. Venkatesan ,  Gerardo D. Francisco

IPC分类号： C07D317/68 ,  C07D413/06 ,  A61K31/42 ,  A61K31/36 ,  C07D263/06 ,  C07D317/58

CPC分类号： C07D413/06 ,  C07D317/68

摘要： The present invention provides new compounds having anti-diabetic and/or antihyperglycemia and/or anti-obesity activity, as well as pharmaceutical compositions and methods of treatment utilizing the compounds and processes for making the compounds, the compounds having the formula (II): ##STR1## wherein: R.sub.1 and R.sub.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sub.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl;R.sub.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sub.2 and R.sub.3 are joined to form a ring: ##STR2## wherein R' is hydrogen, C.sub.1 to C.sub.6 alkyl, or aryl; R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sub.7 and R.sub.8 are independently OR.sub.9 or NR.sub.10 R.sub.11 ;R.sub.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, aryl, arylalkyl, alkoxyalkyl, heteroaryl, --CHR.sub.12 COOR.sub.13, --CHR.sub.12 C(O)R.sub.13, --CHR.sub.12 CONR.sub.1 R.sub.11, --CHR.sub.12 OCOOR.sub.13, or --CHR.sub.12 OC(O)R.sub.13, with the provision that R.sub.9 is not hydrogen in both R.sub.7 and R.sub.8 ;R.sub.10 and R.sub.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aralkyl, aryl, furanylalkyl, or alkoxycarbonylalkyl;R.sub.12 and R.sub.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aryl, or aralkyl; and the pharmaceutically acceptable salts thereof, the enantiomers thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.

摘要翻译： 本发明提供具有抗糖尿病和/或抗高血糖和/或抗肥胖活性的新化合物，以及利用该化合物的药物组合物和治疗方法以及制备该化合物的方法，具有式（II）的化合物： 其中：R 1和R 6独立地为氢，C 1至C 6烷基，三氟甲基，氰基，C 1至C 6烷氧基或卤素; R2是氢或C1-C6三烷基甲硅烷基; R3是氢或C1-C6烷氧基羰基; 或R2和R3连接形成环：其中R'是氢，C1-C6烷基或芳基; R4和R5独立地是氢或C1-C6烷基; R7和R8独立地是OR9或NR10R11; R 9是氢，C 1至C 12烷基，C 1至C 12环烷基，C 1至C 12甲硅烷基烷基，芳基，芳基烷基，烷氧基烷基，杂芳基，-CHR 12 COOR 13，-CHR 12 C（O）R 13，-CHR 12 CONR1R 11，-CHR 12 COOOR 13或-CHR 12 OC（O）R 13 ，其中R7和R8中的R9不是氢; R 10和R 11独立地为氢，C 1至C 12烷基，芳烷基，芳基，呋喃基烷基或烷氧基羰基烷基; R 12和R 13独立地为氢，C 1至C 12烷基，芳基或芳烷基; 及其药学上可接受的盐，其对映异构体，其外消旋混合物及其非对映体混合物。

公开(公告)号：US06395726B1

公开(公告)日：2002-05-28

申请号：US09489623

申请日：2000-01-24

申请人： Yang-I. Lin ,  Panayota Bitha ,  Zhong Li ,  Gerardo D. Francisco

发明人： Yang-I. Lin ,  Panayota Bitha ,  Zhong Li ,  Gerardo D. Francisco

IPC分类号： A01N4300

CPC分类号： C07D499/00

摘要： Compounds are provided having the following formulae I and II: wherein n is 0 or 1 and when n=1, R is a 5 or 6 membered heterocyclic ring, hydroxy, halogen, oxo, carbamoyl, alkoxy, or disubstituted amino, when n=0, R is an ester, cyano or amide group; X is CH or NH; R3 is cyano, methoxy, or acetamido; R1 is hydrogen, alkyl, a negative charge, a cation selected from the group consisting of sodium, potassium and tetraalkylammonium and acyloxyalkyl, or alkoxycarbonyloxyalkyl; and R2 is hydrogen, acyl, trisubstituted silyl carbamoyl or an amino acid residue; or pharmaceutically acceptable salts thereof.

摘要翻译： 提供具有下列通式I和II的化合物：其中n为0或1，当n = 1时，当n = 0时，R为5或6元杂环，羟基，卤素，氧代，氨基甲酰基，烷氧基或二取代的氨基， R是酯，氰基或酰胺基; X是CH或NH; R3是氰基，甲氧基或乙酰氨基; R1是氢，烷基，负电荷，选自钠，钾和四烷基铵的阳离子和酰氧基烷基 ，或烷氧基羰氧基烷基; 和R2是氢，酰基，三取代甲硅烷基氨基甲酰基或氨基酸残基; 或其药学上可接受的盐。