Novel dipeptide compounds and their use as medicines

Details Novel dipeptide compounds and their use as medicines Novel dipeptide compounds and their use as medicines

C - Chemistry, Metallurgy

07

K

C07K 5/023 (2006.01) A61K 31/426 (2006.01) A61P 31/18 (2006.01) C07D 207/14 (2006.01) C07D 207/16 (2006.01) C07D 277/04 (2006.01) C07D 277/06 (2006.01)

Patent

CA 2362849

A novel dipeptide compound which inhibits the enzymatic activity of an HIV protease and is represented by formula (I); and an anti-AIDS agent containing the dipeptide compound as the active ingredient. [In the formula, R?1~, R?2~, and R?3~ each represents C~1-4? alkyl, alkoxy, hydrogen, etc. (provided that not all of R?1~, R?2~, and R?3~ are hydrogen) and R?2~ and R?3~ may be bonded to each other to form a ring; R?4~ represents C~1-4? alkyl or hydrogen; X represents methylene or sulfur; Y represents, e.g., a five- or six-membered monocycle or aryloxyalkyl having up to 12 carbon atoms (provided that the aromatic ring may have been substituted by alkyl, etc.); and Z represents a C~1-6? aliphatic hydrocarbon or an aromatic hydrocarbon having up to 12 carbon atoms (provided that this aromatic ring may have been substituted by alkyl, etc. or at least one carbon atom of the aromatic hydrocarbon may have been replaced with a heteroatom).]

Cette invention, qui a trait à un nouveau composé dipeptidique inhibant l'activité enzymatique d'une VIH protéase et correspondant à la formule (I), concerne également un agent anti-SIDA contenant ce composé dipeptidique comme ingrédient actif. Dans cette formule, R<1>, R<2> et R<3> représentent, chacun, un alkyle porteur de 1 à 4 atomes de carbone, un alcoxy, un hydrogène, etc. (à condition que R<1>, R<2> et R<3> ne représentent pas tous un hydrogène), R<4> représente un alkyle porteur de 1 à 4 atomes de carbone ou un hydrogène, X représente un méthylène ou un soufre, Y représente, par exemple, un élément monocyclique à cinq ou six chaînons ou un arylalcoxyalkyle possédant jusqu'à 12 atomes de carbone (à condition que le noyau aromatique puisse avoir été substitué par un alkyle, etc.), Z représente un hydrocarbure aliphatique pourvu de 1 à 6 atomes de carbone ou un hydrocarbure aromatique possédant jusqu'à 12 atomes de carbone (à condition que ce noyau aromatique puisse avoir été substitué par un alkyle, etc. ou qu'au moins un atome de carbone de l'hydrocarbure aromatique puisse avoir été remplacé par un hétéroatome).

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