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Title:
CYCLOPROPYLGLYCINE COMPOUND FOR TREATING DISEASES OF CENTRAL NERVE SYSTEM
Document Type and Number:
Japanese Patent JPH10287633
Kind Code:
A
Abstract:

To obtain a new cyclopropylglylcine compound useful as an antipsychotic medicine, an anticonvulsant, an analogesic and an antiemetic.

This compound is shown by formula I (R1 is a 1-10C alkyl, a 2-10C alkenyl, etc.; R2 is H or one of R1) such as (1SR,2SR,3SR) 3-methyl-α- methyl-2-carboxycyclopropylglycine. The compound is obtained by hydrolyzing a compound of formula II (R10 and R11 are each H, a 1-4C alkyl, etc.) in the presence of an acid (e.g. hydrochloric acid) in water 100-250°C or deprotecting (an alkylcarboxyl group is removed in the presence of a base, etc., by heating at 100-300°C and an aralkylcarboxyl group is eliminated by adding hydrogen) a compound of formula III (one or both R12 and R13 are each a carboxyl- protecting group and the other is H; R14 is H or an amine-protecting group) by a conventional method. A typical dose of the medicine of the compound of formula I is about 0.05-about 50 mg/kg daily.


Inventors:
PEDREGAL TERCERO CONCEPCION
COLLADO CANO IVAN
MAZON RUIZ ANGEL
Application Number:
JP9442398A
Publication Date:
October 27, 1998
Filing Date:
April 07, 1998
Export Citation:
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Assignee:
LILLY SA
International Classes:
A61K31/195; A61K31/215; A61K31/35; A61K31/352; A61P25/00; A61P25/26; C07C227/22; C07C227/26; C07D311/82; C07C229/28; C07C229/46; C07D233/78; C07D241/08; (IPC1-7): C07C229/46; A61K31/195; A61K31/215; A61K31/35; C07C227/22; C07C227/26; C07D311/82
Attorney, Agent or Firm:
Minoru Nakamura (7 outside)