Quinuclidine compound and medicament comprising the compound...

Details Quinuclidine compound and medicament comprising the compound... Quinuclidine compound and medicament comprising the compound...

C - Chemistry, Metallurgy

07

D

C07D 453/02 (2006.01) A61K 31/439 (2006.01) A61K 31/444 (2006.01) A61K 31/4545 (2006.01) A61K 31/506 (2006.01) A61P 3/06 (2006.01) A61P 9/10 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2385995

The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. (see formula I) In which R1 represents (1) hydrogen atom or (2) hydroxyl group; HAr represents an aromatic heterocycle which may be substituted with 1 to 3 groups; Ar represents an optionally substituted aromatic ring; W represents a chain represented by (1) -CH2-CH2-- which may be substituted, (2) -CH=CH- which may be substituted, (3) -C.ident.C-, (4) -NH-CO-, (5) -CO-NH-, (6) -NH-CH2-, (7) -CH2-- NH-, (8) -CH2-CO-, (9) -CO-CH2-, (10) -NH-S(O)1-, (11) -S(O)1-NH-, (12) -CH2-S(O)1- or (13) -S (O)1-CH2- (1 denotes 0, 1 or 2); and X represents a chain represented by (1) a single bond, (2) an optionally substituted C1-6 alkylene chain, (3) an optionally substituted C2-6 alkenylene chain, (4) an optionally substituted C2-6 alkynylene chain, (5) a formula -Q- (wherein Q represents oxygen atom, sulfur atom, CO or N(R2) (wherein R2 represents a C1-6 alkyl group or a C1-6 alkoxy group)), (6) -NH-CO-, (7) -CO-NH-, (8) -NH-CH2-, (9) -CH2-NH-, (10) -CH2-CO-, (11) -CO-CH2-, (12) -NH-S(O)m-, (13) -S(O)m-NH-, (14) -CH2-S(O)m-, (15) -- S(O)m-CH2- (wherein m denotes 0, 1 or 2) or (16) -(CH2)n-O-- (wherein n denotes an integer from 1 to 6). 377

L'invention concerne des composés de la formule générale (I), des sels et/ou hydrates desdits composés, qui sont d'excellents inhibiteurs de la squalène synthase. Dans ladite formule, R<1> est hydrogène ou hydroxyle; HAr est un hétérocycle aromatique éventuellement substitué; Ar est un noyau aromatique éventuellement substitué; W est 1) un groupe -CH2=CH2- pouvant être substitué; 2) un groupe -CH=CH- pouvant être substitué; 3) -CC-; 4) -NH-CO- ou similaire; et X est une liaison simple, alkylène C1-6 éventuellement substitué; 5) -Q- [Q est oxygène, soufre, CO ou N(R<2>) (R<2> étant alkyle C1-6 ou alcoxy C1-6)]; 6) -NH-CO- ou similaire.

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