Title:
キサンチン誘導体、それらの調製及び医薬組成物としてのそれらの使用
Document Type and Number:
Japanese Patent JP4395304
Kind Code:
B2
Abstract:
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.
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Inventors:
Himmelsbach Frank
Marc michael
Eckhart Matthias
Langkov Elke
Meier Lorant
Lots Ralph
Marc michael
Eckhart Matthias
Langkov Elke
Meier Lorant
Lots Ralph
Application Number:
JP2002567932A
Publication Date:
January 06, 2010
Filing Date:
February 21, 2002
Export Citation:
Assignee:
Boehringer Ingelheim Pharma Gesellshaft Mitt Beschlenktel Haftung Und Company Comandito Gesellshaft
International Classes:
C07D473/04; A61K31/522; A61K31/55; A61K31/551; A61P3/04; A61P3/10; A61P5/00; A61P19/02; A61P19/10; A61P37/02; C07D473/06; C07D473/08; C07D473/10; C07D473/12
Domestic Patent References:
| JP37004895B1 | ||||
| JP2004502690A | ||||
| JP7509456A | ||||
| JP2273676A | ||||
| JP5504129A | ||||
| JP6501251A | ||||
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| JP2003501356A |
Foreign References:
| WO2002024698A1 | ||||
| WO2000073307A1 | ||||
| DE2205815A |
Other References:
Cygankiewicz, A. et al,"Piperazine derivatives of dimethylxanthines. V. Preparation and properties of 8-piperazino- and 1-β-hydroxypropyl-8-piperazinotheobromines",Chem. Abstr., 抄録番号第89:109376,Romuald Acta Poloniae Pharmaceutica,1978年,Vol.34, No.6, 1977, ,pp.607-612
European Journal of Organic Chemistry ,1999年,(9),2419-2428
Photochemistry and Photobiology,1974年,19(1),21-7
Khimiko-Farmatsevticheskii Zhurnal,1984年,18(12),1456-61
European Journal of Organic Chemistry ,1999年,(9),2419-2428
Photochemistry and Photobiology,1974年,19(1),21-7
Khimiko-Farmatsevticheskii Zhurnal,1984年,18(12),1456-61
Attorney, Agent or Firm:
Minoru Nakamura
Fumiaki Otsuka
Sadao Kumakura
Shishido Kaichi
Toshio Imajo
Nobuo Ogawa
Village shrine Atsuo
Takaki Nishijima
Atsushi Hakoda
Fumiaki Otsuka
Sadao Kumakura
Shishido Kaichi
Toshio Imajo
Nobuo Ogawa
Village shrine Atsuo
Takaki Nishijima
Atsushi Hakoda