Glycine derivatives

C - Chemistry – Metallurgy – 07 – K

Patent

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530/5.04, 530/7.

C07K 7/06 (2006.01) A61K 38/04 (2006.01) C07K 5/02 (2006.01) C07K 5/04 (2006.01) C07K 5/09 (2006.01) C07K 5/10 (2006.01) C07K 5/11 (2006.01) C07K 14/47 (2006.01) C07K 14/75 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2008116

The glycine derivatives of the formula R-CONH-CH2-CONH-CH(R')-CH2COOH I wherein R is a group of the formula -CH(NH-R a)-(CH2)1-6-NH-R b ~~(R-1) -(T)1 or O-C6H4-CH2NH-R c ~~(R-2) -(T)1 or O-C6H4-(NH)n-C(NH)-L ~~(R-3) or -(T)1 or (see formula I) ~~~(R-4) and R a is hydrogen, -COO-C1-4-alkyl, Z, -COC6H5, -COC6H4N3, -SO2C6H5, -SO2-naphthyl or -COCH2N(Y)-CH2CH2NH-Y, Y is hydrogen, Boc or Z, R b is a group of the formula -C(NH)(CH2)O-3-CH3 or (see formula II) or, where R a is a group of the formula -COC6H4N3, -SO2C6H5, SO2-naphthyl or -COCH2N(Y)-CH2CH2NH-Y, R b is also amidino, R c is hydrogen or amidino, n is the number 1 or 0, L is amino or, where n is the number 1, L is also -(CH2)O-3-CH3, T is a group of the formula -CH2-(O)1 or O-, -CH=CH-, -CH(R d)-CH2- or -CH2CO-, whereby a carbonyl group present in the group T can also be present as a ketal, R d is hydrogen or -NH-R a, R' is hydrogen or -CO-R o, R o is amino, -NH-C1-4-alkyl, -NH(CH2)1-4-C6H5, -NH(CH2)1-4-C6H4-Hal, -NH-C6H4-COON, -NH-C6H4-COO-C1-4-alkyl or an .alpha.-amino- carboxylic acid attached via the amino group, as well as hydrates or solvates and physiologically usable salts thereof inhibit the binding of adhesive proteins to blood platelets as well as blood platelet aggregation and cell-cell adhesion. They are manufactured starting from corresponding compounds which contain one or more ester groups or amino, amidino or guanidino protecting groups.

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