Title:
AZABICYCLO DERIVATIVE
Document Type and Number:
Japanese Patent JP3251954
Kind Code:
B2
Abstract:
PURPOSE: To provide the new compound useful as a selective low antagonistic agent against 5HT in a 5-HT3 receptor and especially useful for the therapy of emesis and nausea induced by the therapy of cancers.
CONSTITUTION: The compound of the formula I [A is group of formula II, III or IV (R1 is H, 1-10C alkyl, arylalkyl, etc.; R3, R4, R5 are H, amino, halogen, etc.,); X is 0, NH; R is 1-4C alkyl; Y is NR, O, S], e.g. 1H-indole-3-carboxylic acid (endo-9-methyl-3-thia-9-azabicyclo[3,3.1]nona-7-yl) ester. The compound of formula I is obtained by reacting an aromatic carboxylic acid of formula: A-COOH with 3,9-diaza-3-oxa-9-aza- or 3-thia-9-aza-bicyclo[3,3,1]nonane derivative in the presence of a base (e.g. potassium carbonate) in an inert solvent (e.g. dimethylformamide) at -20°C to the boiling point of the solvent.
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Inventors:
Haruhiko Kikuchi
Hiroaki Sato
Nobuhiro Yawata
Koichiro Hagiwara
Toru Hayakawa
Setsuko Mino
Makoto Taniuchi
Hiroaki Sato
Nobuhiro Yawata
Koichiro Hagiwara
Toru Hayakawa
Setsuko Mino
Makoto Taniuchi
Application Number:
JP19139391A
Publication Date:
January 28, 2002
Filing Date:
July 31, 1991
Export Citation:
Assignee:
Nisshin Pharma Inc.
International Classes:
A61K31/495; A61K31/4995; A61K31/535; A61K31/54; A61P1/00; A61P1/04; A61P1/08; A61P1/12; A61P1/14; A61P25/04; A61P25/06; A61P25/18; A61P25/20; A61P25/22; A61P25/24; A61P25/26; A61P25/28; A61P25/30; A61P43/00; C07D471/08; C07D498/08; C07D513/08; (IPC1-7): C07D471/08; A61K31/4995; A61P1/00; A61P1/04; A61P1/08; A61P1/12; A61P1/14; A61P25/06; A61P25/18; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P43/00
Other References:
【文献】欧州特許出願公開377967(EP,A2)
Attorney, Agent or Firm:
Chika Takagi (2 outside)
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