Novel 1-[(heterocyclyl)alkyl]-4-diarylmethoxy piperidine derivatives are disclosed having the formula ##STR1## where n is 2-6, Ar.sup.1 and Ar.sup.2 are aryl and B is a substituted benzimidazolyl radical. These compounds are useful for their antianaphylactic and antihistaminic properties. Specific claimed compounds are 1-{3-[4-(diphenylmethoxy)-1-piperidinyl]-propyl}-1,3-dihydro-2H-benzimidaz ol-2-one, 1-{2-[4-(diphenylmethoxy)-1-piperidinyl]ethyl}1-, 3-dihydro-2H-benzimidazol-2-one, and 1-{4-[4-(diphenylmethoxy)-1-piperidinyl]butyl}-1,3-dihydro-2H-benzimidazol -2-one.
Intermediates useful for the preparation of antihistaminic piperidine derivatives
申请人:Merrell Pharmaceuticals Inc.
公开号:US06340761B1
公开(公告)日:2002-01-22
The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula
wherein
W represents —C(═O)— or —CH(OH)—;
R1 represents hydrogen or hydroxy;
R2 represents hydrogen;
R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2;
n is an integer of from 1 to 5;
m is an integer 0 or 1;
R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and
pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.
Process for the preparation of 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone and acid addition salts thereof
申请人:Arevipharma GmbH
公开号:EP2371817A1
公开(公告)日:2011-10-05
The present invention describes processes for the preparation of 1-[4-(1,1-dimethylethyl)phenyl]-4-[4-(diphenylmethoxy)-1-piperidinyl]-1-butanone and acid addition salts thereof.
Novel 1-substituted 4-(diarylmethyl)piperazine derivatives having antianaphylactic and antihistaminic properties, in which the 1-substituent is optionally substituted 2(3H) benzimidazol-2-one, 2(3H) benzothiazol-2-one, or 2(3H) benzoxazol-2-one.
N-alkyleneiminoalkyl-dicarboximides as antiallergics and antiasthmatics
申请人:Ciba-Geigy Corporation
公开号:US04261990A1
公开(公告)日:1981-04-14
N-(diphenylmethoxy-mono- or bicyclic-alkyleneiminoalkyl)-dicarboximides, e.g. those of the formula ##STR1## A=aliphatic or cycloaliphatic radical R,R'=H, alkyl, halogen or CF.sub.3 R"=H or both are ethylene q=2-4 and salts thereof are antiallergics and antiasthmatics.