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Title:
3-AMINO-3-ARYLPROPAN-1-OL DERIVATIVE, ITS PRODUCTION AND USE
Document Type and Number:
Japanese Patent JP2000327643
Kind Code:
A
Abstract:

To obtain a new compound effective for painkilling for the therapy of pain, and useful as a local anesthetic or for treatment and therapy of cardiovascular disease or the like.

This new compound is the one of formula I [R1 and R2 are each a 1-6C alkyl or form a (CH2)2-6 ring with each other; R3 is H or methyl; R4 and R5 are each a 1-6C alkyl, a 3-6C cycloalkyl or the like; A is an aryl residue; X is a benzyl of formula II (R12 to R14 are each H, F or the like)] in a base or a salt form with a physiologically compatible acid, e.g. dimethyl-{[2-(2-methylbenzyloxy)cyclohexyl]phenylmethyl}-amine. The compound of formula I is obtained by reacting a Mannich-base of formula IV with a nucleophilic reagent, e.g. an organometallic compound, preferably at (-70)-110°C.


Inventors:
SUNDERMANN BERND
HENNIES HAGEN-HEINRICH
KOEGEL BABETTE-YVONNE
BUSCHMANN HELMUT
Application Number:
JP2000105260A
Publication Date:
November 28, 2000
Filing Date:
April 06, 2000
Export Citation:
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Assignee:
GRUENENTHAL GMBH
International Classes:
A61K31/137; A61K31/138; A61K31/221; A61K31/235; A61K31/341; A61K31/381; A61P1/00; A61P1/08; A61P1/12; A61P9/00; A61P9/04; A61P9/06; A61P13/02; A61P17/00; A61P17/04; A61P21/00; A61P23/00; A61P23/02; A61P25/00; A61P25/04; A61P25/28; A61P25/30; A61P25/32; C07D333/58; A61P29/00; C07B61/00; C07C213/06; C07C217/52; C07C219/24; C07D307/52; (IPC1-7): C07C217/52; A61K31/138; A61K31/221; A61K31/341; A61K31/381; A61P1/08; A61P1/12; A61P9/04; A61P9/06; A61P13/02; A61P17/04; A61P23/02; A61P25/00; A61P25/04; A61P25/28; A61P25/30; A61P25/32; A61P29/00; C07C213/06; C07C219/24; C07D307/52; C07D333/58
Domestic Patent References:
JPS306474B1
Foreign References:
US3937818A1976-02-10
US4017637A1977-04-12
US4143158A1979-03-06
US3975436A1976-08-17
Attorney, Agent or Firm:
Mitsufumi Ezaki (3 others)