HIMMELSBACH FRANK DR.,MARK MICHAEL DR.,LOTZ RALF R.H. DR.,MAIER ROLAND DR.,LANGKOPF ELKE DR.,ECKHARDT MATTHIAS DR.
申请号：
SI200230996
公开号：
SI1953162T1
申请日:
2002.02.21
申请国别(地区):
SI
年份:
2012
代理人:
摘要：
8-substituted-xanthine derivatives (I), their tautomers, enantiomers, diastereomers or mixtures, and salts. 8-substituted xanthine derivatives of formula (I), their tautomers, enantiomers, diastereomers or mixtures, and salts, are new: [Image] R 1>hydrogen 1-8C alkyl 3-8C alkenyl or alkynyl 3-4C alkenyl substituted by 1-2C alkoxycarbonyl, aminocarbonyl (optionally substituted by 1 or 2 1-3C alkyl) or het-CO 1-6C alkyl substituted by Ra phenyl(1-6C)alkyl, optionally ring-substituted by R 1> 0>-R 1> 4> phenyl(1-4C)alkyl, optionally substituted in alkyl by Rz and in the ring by R 1> 0>-R 1> 4> R 1> 0>-R 1> 4>-substituted phenyl phenyl(2-3C) alkenyl, phenyl (or naphthyl)-(CH 2) m-(A or B)-(CH 2) n, naphthyl(1-3C)alkyl or phenylcarbonylmethyl (all optionally ring-substituted by R 1> 0>-R 1> 4>) [1,4-napththoquinon-2-yl chromen-4-on-3-yl 1-oxo- or 1,3-dioxo-indan-2-yl 2,3-dihydro-3-oxo-benzofuran-2-yl heteroaryl-(CH 2) m-(A or B)-(CH 2) n 1-6C alkyl-A-(CH 2) n 3-7C cycloalkyl-(CH 2) m-A or B)-(CH 2) n R 2> 1>-A-(CH 2) n phenyl- or naphthyl-(CH 2) m-D-(1-3C)alkyl Rb-substituted 2-6C alkyl, or 3-6C cycloalkyl amino, or arylcarbonylamino het : pyrrolidin-1-yl, piperidin-1-yl or morpholin-4-yl R 1> 0>-R 1> 4>, Rb and Rz : various substituents m : 0-2 n : 1-3 A, B and D : various linking groups R 2>hydrogen or a wide range of substituents R 3>various substituents R 4>a wide range of substituents. The full definitions are given in the DEFINITIONS (Full Definitions) Field. ACTIVITY : Antidiabetic antiarthritic antiinflammatory immunosuppressive osteopathic antilipemic antiarteriosclerosis anabolic cardiant nephrotropic antinfertility. MECHANISM OF ACTION : Inhibition of dipeptidylpeptidase-IV (DPPIV). The compound (R)-1,3-dimethyl-7-(3-methyl-2-buten-1-yl)-8-(3-aminopiperidin-1- yl)xanthine had IC50 against DDPIV expressed in Caco-2 cells of 22 nM.
