KR910002796A - Piperidine derivatives, preparation method thereof, and pharmaceutical composition comprising the same - Google Patents

Abstract

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Description

Piperidine derivatives, preparation method thereof, and pharmaceutical composition comprising the same

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Claims (15)

Pharmacologically acceptable salts of the piperidine derivative represented by the following general formula (I) and the compound of formula (I). Wherein R represents a hydrogen atom or a lower alkyl group, X represents -CH = CH-, -CH ₂ CH _2- , or -CH ₂ O-; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an -AOB group, wherein A and B are the same or different and each independently be optionally substituted with a lower alkyl group The alkylene group which may have 1-3 carbon atoms is also shown. 4- (5H-dibenzo [a, d] cyclohepten-5-ylidene) -1-piperidinepropionic acid and its pharmacologically acceptable salts. 2- [4- (5H-dibenzo [a, d] cyclohepten-5-ylidene) piperidino] ethoxyacetic acid and its pharmacologically acceptable salts. 4- (10,11-Dihydro-5H-dibenzo [a, d] cyclohepten-5-ylidene) -1-piperidine propionic acid and pharmacologically acceptable salts thereof. 4- (Dibenz [b, e] oxepin-11 (6H) -ylidene) -piperidine acetic acid and its pharmacologically acceptable salts. 2- (4- (dibenz [b, e] oxepin-11 (6H) -ylidene) piperidino] ethoxyacetic acid and its pharmacologically acceptable salts. In the method for preparing a pharmacologically acceptable salt of the piperidine derivative represented by the following general formula (I) and the compound of formula (I), (Wherein R represents hydrogen or lower alkyl group, X represents -CH = CH-, -CH ₂ CH _2- , or -CH ₂ O-; Y is 1 to 5 which may be optionally substituted with lower alkyl group) Represents an alkylene group having 3 carbon atoms or Y represents an -AOB group, wherein A and B each represent an alkylene group having 1 to 3 carbon atoms which may be the same or different and may be optionally substituted independently with a lower alkyl group. . General formula (Ⅱ) Wherein the piperidine derivative represented by X is as described above as ZY-COOR (IIIa) or CH ₂ = CHCOOR (IIIb), where R is as defined above and Z represents a halogen atom A process comprising the step of reacting with a compound represented, followed by hydrolysis in a solvent using an acid or a base if necessary. The method of claim 7, wherein the step of reacting is carried out in the presence of a solvent. 8. A process according to claim 7, wherein said step of reacting is carried out in the absence of a solvent. 8. The method of claim 7, wherein said step of reacting is carried out in the presence of a base as a dehydrohalogenating agent. 8. The method of claim 7, wherein said reacting is carried out in the absence of a base as a dehydrohalogenating agent. An antihistamine and an antiallergic agent comprising a piperidine derivative represented by the following general formula (I) and an effective pharmacologically acceptable salt amount of the compound of formula (I). R represents a hydrogen atom or a lower alkyl group, X represents -CH = CH-, -CH ₂ CH _2- , or -CH ₂ O-; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with lower alkyl, or Y represents an -AOB group, wherein A and B are the same or different and each independently be optionally substituted with a lower alkyl group The alkylene group which may have 1-3 carbon atoms is also shown. A pharmaceutical composition for the treatment of allergic diseases, comprising a piperidine derivative represented by the following general formula (I) and an effective pharmacologically acceptable salt amount of the compound of formula (I). R represents a hydrogen atom or a lower alkyl group, X represents -CH = CH-, -CH ₂ CH _2- , or -CH ₂ O-; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an -AOB group, where A and B are the same or different and each independently be optionally substituted with a lower alkyl group The alkylene group which may have 1-3 carbon atoms is also shown. (a) an antihistamine and an antiallergic agent comprising a piperidine derivative represented by the following general formula (I), (b) a pharmacologically acceptable salt of the compound of formula (I), (c) a compound of formula (I) Or (d) administering to a mammal an effective amount of a substance selected from the group consisting essentially of a pharmaceutical composition comprising the compound of formula (I). R represents a hydrogen atom or a lower alkyl group, X represents -CH = CH-, -CH ₂ CH _2- , or -CH ₂ O-; Y represents an alkylene group having 1 to 5 carbon atoms which may be optionally substituted with a lower alkyl group, or Y represents an -AOB group, wherein A and B are the same or different and each independently be optionally substituted with a lower alkyl group The alkylene group which may have 1-3 carbon atoms is also shown. The method of claim 14, wherein said administering step is performed on a human. ※ Note: The disclosure is based on the initial application.