New inhibitors of platelet aggregation

Details New inhibitors of platelet aggregation New inhibitors of platelet aggregation

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/505 (2006.01) A61K 31/70 (2006.01) C07H 19/06 (2006.01) C07H 19/23 (2006.01)

Patent

CA 2226758

Compounds of formula (I), wherein B is O or CH2; X is selected from NR1R2, SR1, and C1-C7 alkyl; Y is selected from SR1NR1R2, and C1-C7 alkyl; R1 and R2 are each and independently selected from H, or C1-C7 alkyl optionally substituted upon or within the alkyl chain by one or more of O, S, N or halogen; R3 and R4 are both H, <u>or</u> R3 and R4 together form a bond; A is COOH, C(O)NH(CH2)pCOOH, C(O)N[(CH2)qCOOH]2; C(O)NHCH(COOH)(CH2)rCOOH, <u>or</u> 5-tetrazolyl, wherein p, q and r are each and independently 1, 2, or 3; as well as pharmaceutically acceptable salts and prodrugs thereof, pharmaceutical compositions comprising the novel compounds and use of the compounds in therapy. Also within the scope of the invention are novel intermediates to the novel compounds. The novel compounds are in particular useful in the prevention of platelet aggregation.

L'invention porte sur des composés de formule (I) dans laquelle: B est O ou CH¿2?; X est choisi parmi NR?1¿R?2¿, SR?1¿, et alkyle C¿1?-C¿7?; Y est choisi parmi SR?1¿,NR?1¿R?2¿, et alkyle C¿1?-C¿7?; R?1¿ et R?2¿ sont chacun sélectionnés indépendamment parmi H, alkyle C¿1?-C¿7? facultativement substitué sur ou dans la chaîne alkyle par un ou plusieurs des éléments O, S, N ou halogène, R?3¿ et R?4¿ sont tous deux H, ou forment ensemble une liaison; A est COOH, C(O)NH(CH¿2?)¿p?COOH, C(O)N[(CH¿2?)¿q?COOH]¿2?; C(O)NHCH(COOH)(CH¿2?)¿r?COOH, ou 5-tétrazolyle et où p, q et r sont chacun 1, 2, ou 3. L'invention porte également sur leurs sels pharmacocompatibles et leurs précurseurs, des préparations pharmaceutiques les contenant, et leur utilisation à des fins thérapeutiques, ainsi que sur de nouveaux intermédiaires de ces composés. Ces nouveaux composés peuvent notamment servir pour prévenir l'agrégation plaquettaire.

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