C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/96 (2006.01) A61K 31/445 (2006.01) C07D 211/22 (2006.01) C07D 211/40 (2006.01) C07D 211/42 (2006.01) C07D 211/46 (2006.01) C07D 295/185 (2006.01) C07D 295/26 (2006.01) C07D 405/02 (2006.01)
Patent
CA 2136841
The present invention relates to certain novel piperidyl amides, sulfonamides and sulfoxamides of formula (I) and (II) which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof, wherein A is a C2-C14 alkylene; Y is a methylene, oxygen, sulfur, sulfinyl or sulfonyl; B is a C2-C14 alkylene, (a) or (b); m is an integer 0 or l; v is an integer 0, 1 or 2; and R is -(CH2)mOH, with the proviso that when m is 0, R cannot be in the 2-position of the piperidine ring or a radical of formula (c), wherein n is an integer 0, 1, 2, or 3; and Rl is hydrogen, phenyl, vinyl or a C1-C4 alkyl; provided that when R is a radical of formula (c), Y is not methylene.
La présente invention porte sur certains nouveaux sulfonamides, sulfoxamides et amides pipéridyliques de formules (I) et (II) - qui sont utiles comme inhibiteurs de la biosynthèse du cholestérol, et comme agents abaissant le cholestérol sérique total chez des patients traités à cette fin -, où A est un alkylène C2-C14; Y est un méthylène, de l'oxygène, du soufre, un sulfinyle ou un sulfonyle; B est un alkylène C2-C14, (a) ou (b); m est l'entier 0 ou l; v est l'entier 0, 1 ou 2; R est -(CH2)mOH, à la condition que si m est égal à 0, R ne peut être en position 2 du noyau de la pipéridine ou un radical de formule (c), où n est l'entier 0, 1, 2 ou 3; enfin, Rl est un hydrogène, un phényle, un vinyle ou un alkyle C1-C4; à la condition que si R est un radical de formule (c), Y n'est pas le méthylène.
Moore William R.
Vansickle William A.
Wannamaker Marion W.
Merrell Pharmaceuticals Inc.
Osler Hoskin & Harcourt Llp
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