Title:
新規アセトアミド誘導体およびプロテアーゼ阻害
Document Type and Number:
Japanese Patent JP4199309
Kind Code:
B2
Abstract:
The present invention relates to novel acetamide derivatives having a substituted heterocyclic group and consecutive dicarbonyl structures, for example 1-pyrimidinylacetamide compounds, 1-pyrazinylacetamide compounds, 1-triazinylacetamide compounds etc., and these compounds have inhibitory activity on chymotrypsin type proteases and are useful as inhibitors for said enzymes, particularly as chymase inhibitors. The novel acetamide derivatives of the present invention are shown in formula (I) below: wherein R<0> is substituted or unsubstituted phenyl; R<1> is aryl, heteroaryl or aliphatic lower alkyl which may be substituted or unsubstituted; R<2> is substituted or unsustituted alkyl, arylalkyl, or heteroarylalkyl; R<3> is hydrogen; acyl group; sulfonyl group; isocyanate group; thiourea; or hydrogen, a lower alkyl or a substituted lower alkyl; aryl (1-7C) alkyl, heteroaryl (1-7C) alkyl, aryl and heteroaryl; X and Y independently represent a nitrogen atom or a carbon atom; and Z is a polymethylene group wherein a hydrogen atom in the polymethylene may be replaced.
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Inventors:
Ryoichi Suzuki
Koichi Ishida
Koichi Ishida
Application Number:
JP51248798A
Publication Date:
December 17, 2008
Filing Date:
September 05, 1997
Export Citation:
Assignee:
NIPPON KAYAKU KABUSHIKI KAISHA
International Classes:
C07D213/64; C07D239/42; A61K31/495; A61K31/497; A61K31/505; A61K31/513; A61K31/53; A61K31/535; A61K31/5377; A61P9/00; A61P11/06; A61P29/00; A61P37/06; A61P43/00; C07D239/46; C07D241/20; C07D253/06; C07D401/12; C07D401/14; C07D405/12; C07D417/06; C07D417/12; A61K31/44
Domestic Patent References:
| JP8143517A | ||||
| JP5239059A | ||||
| JP5213873A | ||||
| JP2134398A | ||||
| JP8506569A |
Foreign References:
| WO1994000420A1 | ||||
| EP0454302A1 |
Other References:
YUAN W ET AL, DEVELOPMENT OF SELECTIVE TIGHT-BINDING INHIBITORS OF LEUKOTRIENE A4HYDROLASE, JOURNAL OF MEDICINAL CHEMISTRY, 1993年, vol. 36, no. 2, pages 211-220
PEET N P ET AL, SYNTHESIS OF PEPTIDYL FLUOROMETHYL KETONES AND PEPTIDYL ALPHA-KETO ESTERS AS INHIBITORS OF PORCINE PANCREATIC ELASTASE, HUMAN NEUTROPHIL ELASTASE, AND RAT AND HUMAN NEUTROPHIL CATHEPSIN G, JOURNAL OF MEDICINAL CHEMISTRY, 1990年, vol. 33, no. 1, pages 394-407
PEGORIER L. ET AL, STEREOCONTROLLED SYNTHESIS OF SYN AND ANTI N-PROTECTED 3-AMINO-2-HYDROXY ALKANOIC ESTERS FROM AMINOALKYL EPOXIDES, SYNLETT, 1996年, vol. 6, pages 585-586
CHUNG Y.J. ET AL, SYNTHESIS AND INHIBITORY ACTIVITIES OF HIV-1 PROTEASE INHIBITORS CONTAINING 2-ISOXAZOLINE DERIVATIVES, KOREAN JOURNAL OF MEDICINAL CHEMISTRY, 1995年, vol. 5, no. 2, pages 141-161
HERRANDEZ R. ET AL, Ketomethylenebestatin: Synthesis and aminopeptidase inhibition, ARCHIV DER PHARMAZIE, 1993年, vol. 326, no. 7, pages 395-398
PEET N P ET AL, SYNTHESIS OF PEPTIDYL FLUOROMETHYL KETONES AND PEPTIDYL ALPHA-KETO ESTERS AS INHIBITORS OF PORCINE PANCREATIC ELASTASE, HUMAN NEUTROPHIL ELASTASE, AND RAT AND HUMAN NEUTROPHIL CATHEPSIN G, JOURNAL OF MEDICINAL CHEMISTRY, 1990年, vol. 33, no. 1, pages 394-407
PEGORIER L. ET AL, STEREOCONTROLLED SYNTHESIS OF SYN AND ANTI N-PROTECTED 3-AMINO-2-HYDROXY ALKANOIC ESTERS FROM AMINOALKYL EPOXIDES, SYNLETT, 1996年, vol. 6, pages 585-586
CHUNG Y.J. ET AL, SYNTHESIS AND INHIBITORY ACTIVITIES OF HIV-1 PROTEASE INHIBITORS CONTAINING 2-ISOXAZOLINE DERIVATIVES, KOREAN JOURNAL OF MEDICINAL CHEMISTRY, 1995年, vol. 5, no. 2, pages 141-161
HERRANDEZ R. ET AL, Ketomethylenebestatin: Synthesis and aminopeptidase inhibition, ARCHIV DER PHARMAZIE, 1993年, vol. 326, no. 7, pages 395-398
Attorney, Agent or Firm:
Norio Saeki