KR890013001A - Tetrazole Derivatives, Stimulating Amino Acid Receptor Antagonists - Google Patents

Abstract

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Description

Tetrazole Derivatives, Stimulating Amino Acid Receptor Antagonists

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Claims (10)

Compounds of formula (I) and pharmaceutically acceptable salts thereof. In the above formula, or R ² is hydrogen or C ₁ -C ₃ alkyl, n is 0, 1 or 3, m is 0 or 1, provided that m + n is 0, 1, 2 or 3, R ³ is hydrogen, C ₁ -C ₄ alkyl, phenyl or oral ester forming group, Y is —CH, and R ⁴ is each independently hydrogen, C ₁ -C ₄ alkyl or phenyl. The compound of claim 1, wherein R ¹ is Phosphorus compounds. The compound of claim 1 or 2, wherein R ² and R ³ are hydrogen. Cis- (±) -4-[(1 (2) H-tetrazol-5-yl) methyl] -2-piperidinecarboxylic acid and pharmaceutically acceptable salts thereof. Cis- (±) -4- [2- (1 (2) H-tetrazol-5-yl) ethyl] -2-piperidinecarboxylic acid and pharmaceutically acceptable salts thereof. Cis- (±) -4- [3- (1 (2) H-tetrazol-5-yl) propyl] -2-piperidinecarboxylic acid and pharmaceutically acceptable salts thereof. Z- (±) -4-[(1 (2) H-tetrazol-5-yl) methylidene] -2-piperidinecarboxylic acid and pharmaceutically acceptable salts thereof. A pharmaceutical formulation, characterized in that it contains a compound according to any one of claims 1 to 7 as an active ingredient in combination with one or more pharmaceutically acceptable carriers or diluents therefor. (A) esterifying a compound of formula (II ') with an alcohol of formula (Q), or (B) a compound of formula (II) is an amine of formula (P), (Y) or (Z) Or (C) alkylate the compound of formula (III) with a halide of formula (O), or (D) deblock the compound of formula (IV) by acid or base hydrolysis, or (E A process for preparing the compound of formula (I) according to any one of claims 1 to 7, characterized in that a salt of the compound of formula (I) is prepared with an acidic or basic salt-forming agent. Wherein R ¹ is R ² is C ₁ -C ₃ alkyl, R ³ is C ₁ -C ₄ alkyl, phenyl or oral ester forming group, R ⁴ is each independently C ₁ -C ₄ alkyl or phenyl, and R ⁵ is C ₁ -C ₄ alkyl, R ⁶ is a blocking group, preferably C ₁ -C ₆ alkoxycarbonyl, n is 0, 1, 2 or 3, m is 0 or 1, provided that m + n is 0, 1, 2 or 3, Y is -CH = and X is bromo, chloro or iodo. A compound of formula (I) prepared by the process according to claim 9. ※ Note: The disclosure is based on the initial application.