Title:
2-アミノチアゾリン誘導体およびNO-合成酵素の阻害剤としてのその使用
Document Type and Number:
Japanese Patent JP4238026
Kind Code:
B2
Abstract:
The invention concerns 2-aminithiazoline derivatives of formula (I) wherein: either R1 is a hydrogen atom or an alkyl radical and R2 is an alkyl, -alk-NH2, -CH-R3, -CH2-S-R4 or phenyl radical substituted by a nitro or NH-C(=NH)CH3 radical; or R1 is an alkyl radical and R2 is a hydrogen atom; R3 is a cycloalkyl (3-6C), pyridyl, pyridyl N-oxide, thienyl, thiazolyl, imidazolyl, pyrazinyl, triazolyl, phenyl or phenyl radical substituted by a nitro, hydroxy or carboxy radical; R4 represents a pyridyl or pyridyl N-oxide radical; alk represents an alkylene radical or their pharmaceutically acceptable salts excluding some known compounds, and the use of said derivatives as inducible NO-synthase inhibitors.
Inventors:
Jean-Christoph Cali
Dominique damour
Claude Guillon
Serge Mignani
Antoni Bigo
Eric Burke
Michelle Tavar
Dominique damour
Claude Guillon
Serge Mignani
Antoni Bigo
Eric Burke
Michelle Tavar
Application Number:
JP2002501875A
Publication Date:
March 11, 2009
Filing Date:
June 07, 2001
Export Citation:
Assignee:
Aventis Pharma Societe Anonym
International Classes:
C07D277/18; A61K31/426; A61K31/427; A61K31/4439; A61K31/444; A61P1/04; A61P3/10; A61P9/10; A61P11/06; A61P19/02; A61P25/00; A61P35/00; C07C335/08; C07D277/28; C07D417/06; C07D417/12
Domestic Patent References:
| JP8503940A | ||||
| JP9504028A |
Foreign References:
| US5066662 | ||||
| WO1996014842A1 | ||||
| WO2001047931A1 |
Other References:
LEVY, O. E., et al.,Potent and Selective Thrombin Inhibitors Incorporating the Constrained Arginine Mimic L-3-Piperidyl(N-guanidino)alanine at P1,Journal of Medicinal Chemistry,1996年,39(23),p. 4527-4530
FRYDMAN, B., et al.,1,4-Diaminobutanes From Furans: A New Synthetic Approach to Substitued Putrescines,Tetrahedron Letters,1998年,39,p. 4765-4768
DEFAUW, J. M., et al.,Synthesis and Protein Kinase C Inhibitory Activities of Acyclic Balanol Analogs That Are Highly Selective for Protein Kinase C over Protein Kinase A,Journal of Medicinal Chemistry,1996年,39,p. 5215-5227
ENDO, Y., et al.,Synthesis, Conformation, and Biological Activity of Teleocidin Mimics, Benzolactams. A Clarification of the Conformational Flexibility Problem in Structure-Activity Studies of Teleocidins,Journal of American Chemical Society,1996年,118,p. 1841-1855
OCAIN, T. D., et al.,Synthesis of Sulfur-Containing Analogues of Bestain. Inhibition of Aminopeptidases by α-Thiolbestatin Analogues,Journal of Medicinal Chemistry,1988年,31,p. 2193-2199
FENG, X., et al.,Synthesis of (S,S)-Isodityrosinol in a Fully Differentiated Form via Diels-Alder Methodology,Journal of Organic Chemistry,1992年,57(22),p. 5811-5812
FRYDMAN, B., et al.,1,4-Diaminobutanes From Furans: A New Synthetic Approach to Substitued Putrescines,Tetrahedron Letters,1998年,39,p. 4765-4768
DEFAUW, J. M., et al.,Synthesis and Protein Kinase C Inhibitory Activities of Acyclic Balanol Analogs That Are Highly Selective for Protein Kinase C over Protein Kinase A,Journal of Medicinal Chemistry,1996年,39,p. 5215-5227
ENDO, Y., et al.,Synthesis, Conformation, and Biological Activity of Teleocidin Mimics, Benzolactams. A Clarification of the Conformational Flexibility Problem in Structure-Activity Studies of Teleocidins,Journal of American Chemical Society,1996年,118,p. 1841-1855
OCAIN, T. D., et al.,Synthesis of Sulfur-Containing Analogues of Bestain. Inhibition of Aminopeptidases by α-Thiolbestatin Analogues,Journal of Medicinal Chemistry,1988年,31,p. 2193-2199
FENG, X., et al.,Synthesis of (S,S)-Isodityrosinol in a Fully Differentiated Form via Diels-Alder Methodology,Journal of Organic Chemistry,1992年,57(22),p. 5811-5812
Attorney, Agent or Firm:
Chika Takagi
Kosuke Nishimura
Hiroshi Sugimoto
Kosuke Nishimura
Hiroshi Sugimoto