Watersoluble azole antifungals

Details Watersoluble azole antifungals Watersoluble azole antifungals

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/675 (2006.01) C07D 521/00 (2006.01) C07F 9/6558 (2006.01)

Patent

CA 2179640

A compound of formula (I), an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form - N=CH-, -CH=N-, -CH2-CH2, CH=CH-, -C(=O)-CH2-, -CH2-C(=O); D is a radical of formula (D1), (D2), (D3); L is a radical of formula (L1), (L2); Alk is a C1- 4alkanediyl radical; R1 is halo; R2 is hydrogen or halo; R3 is hydrogen, C1- 6alkyl, phenyl or halophenyl; R4 is hydrogen, C1-6alkyl, phenyl or halophenyl; R5 is hydrogen or C1-6alkyl; R6 is hydrogen, C1-6alkyl, C1-6alkyloxycarbonyl, or R5 and R6 taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.

L'invention concerne un composé de la formule (I), un de ses sels d'addition d'acide ou de base ou une de ses formes stéréo-isomères. A et B forment conjointement -N=CH-, -CH=N-, -CH¿2?-CH¿2?, CH=CH-, -C(=O)-CH¿2?-, -CH¿2?-C(=O); D est un radical de la formule (D¿1?), (D¿2?), (D¿3?); L est un radical de la formule (L¿1?), (L¿2?); Alk désigne un radical alcanediyl C¿1-4?; R?1¿ désigne halo; R?2¿ désigne hydrogène ou halo; R?3¿ désigne hydrogène, alkényle C¿1-6?, phényle ou halophényle; R?4¿ désigne hydrogène, alkyle C¿1-6?, phényle ou halophényle; R?5¿ désigne hydrogène ou alkyle C¿1-6?; R?6¿ désigne hydrogène, alkyle C¿1-6?, alkyloxycarbonyle C¿1-6?, ou R?5¿ et R?6¿ forment conjointement avec l'atome d'azote auquel ils sont liés, un composé hétérocyclique. L'invention concerne en outre des intermédiaires actifs, des compositions et des procédés de préparation des composés et des compositions décrits.

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