Tyrosin-derivate as alpha-v-integrin inhibitors

Details Tyrosin-derivate as alpha-v-integrin inhibitors Tyrosin-derivate as alpha-v-integrin inhibitors

C - Chemistry, Metallurgy

07

C

C07C 311/06 (2006.01) A61K 31/195 (2006.01) A61K 31/215 (2006.01) A61K 31/27 (2006.01) A61K 31/445 (2006.01) A61K 31/655 (2006.01) C07C 247/04 (2006.01) C07C 257/14 (2006.01) C07C 271/22 (2006.01) C07C 271/28 (2006.01) C07C 279/08 (2006.01) C07C 311/13 (2006.01) C07C 311/14 (2006.01) C07C 311/19 (2006.01) C07D 211/62 (2006.01)

Patent

CA 2241149

Disclosed are compounds of formula (I) in which X represents alkylene with 1-6 C atoms or 1,4-piperidyl; Y is absent or represents O, CONH or -CC-; R1 represents H, CN, N3, NH2, H2N-C(=NH) or H2N-(C=NH)-NH (the primary amino groups can also be provided with conventional amino protective groups); R2, R3 each independently of one another represent H, A, A-SO2-, Ar-SO2, campher-10- SO2-, COOA or a conventional amino protective group; A, R4 each independently of one another represent H or alkyl with 1-10 C atoms; and Ar represents phenyl or benzyl which is unsubstituted or single-substituted with CH3. Also disclosed are the physiologically tolerable salts of these compounds. The compounds and salts thereof can be used as .alpha.v-integrin inhibitors, in particular for treating tumours, osteoporoses, osteolytic disorders and for suppressing angiogenesis.

L'invention a pour objet des composés de formule (I), dans laquelle X est un alkylène de 1 à 6 C ou un 1,4-pipéridyle, Y ou bien fait défaut, ou bien désigne O, CONH ou -C?C-, R?1¿ désigne H, CN, N¿3?, NH¿2?, H¿2?N-C(=NH) ou H¿2?N-(C=NH)-NH, où les groupes amino primaires peuvent être également pourvus de groupes amino-protecteurs conventionnels, R?2¿, R?3¿ désignent chacun, indépendamment l'un de l'autre H, A, A-SO¿2?-, Ar-SO¿2?-, camphre- 10-SO¿2?-, COOA ou un groupe amino-protecteur conventionnel, A, R?4¿ désignent chacun, indépendamment l'un de l'autre, H ou un alkyle de 1 à 10 atomes C, et Ar désigne un phényle ou un benzyle non substitué ou substitué uniquement par CH¿3?, ainsi que les sels physiologiquement tolérables de ces composés. Lesdits composés et leurs sels peuvent être utilisés comme inhibiteurs d'.alpha.¿v?-intégrine, en particulier pour le traitement de pathologies tumorales, d'ostéoporoses, de pathologies ostéolytiques, ainsi que pour la suppression de l'angiogenèse.

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