Amino acid derivatives
First Claim
1. A compound of the formula ##STR19## wherein L is a group of the formula ##STR20## or
R is amidino or guanidino, each of X and Y is CH,Ro is hydrogen or amidino,t is an integer between 2 and 6,R'"'"' and R" together with the N atom and C atom to which they are attached form an optionally substituted 4- to 6-membered ring;
R"'"'"' is hydrogen or optionally substituted lower alkyl;
Q is a group of the formula ##STR21##
space="preserve" listing-type="equation">--N(V'"'"')CH.sub.2 .sub.v --C(V",V'"'"'")CH.sub.2 OCH.sub.2 COO-T Q.sup.8or ##STR22## n is the number 0 or 1, v is an integer between 0 and 3,T and T'"'"' are hydrogen or a lower-alkyl or phenyl-lower-alkyl group which is cleavable under physiological conditions,V to V"'"'"' are hydrogen or lower-alkyl,U and U'"'"' are hydrogen, C1-6 alkanoyl or aroyl,Ar is aryl andR2 to R5 are hydrogen, lower-alkyl, lower-alkoxy, halogen or a group --OCH2 COO-T'"'"' orR2 and R3 together with the phenyl group to which they are attached form a 1-naphthyl group,as well as hydrates or solvates and physiologically usable salts thereof.
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Abstract
N-Acyl-α-aminocarboxylic acid derivatives of the formula ##STR1## wherein L, R'"'"' to R"'"'"' and Q have the significance given in the description, can be used for the treatment or prophylaxis of illnesses which are caused by the binding of adhesive proteins to blood platelets and by blood platelet aggregation and cell-cell adhesion. They are manufactured by cleaving off protecting groups in corresponding protected compounds or by converting the cyano group into the amidino group in corresponding nitriles.
9 Citations
9 Claims
- 1. A compound of the formula ##STR19## wherein L is a group of the formula ##STR20## or
- space="preserve" listing-type="equation">R.sup.o -NH(CH.sub.2).sub.t L.sup.2
R is amidino or guanidino, each of X and Y is CH, Ro is hydrogen or amidino, t is an integer between 2 and 6, R'"'"' and R" together with the N atom and C atom to which they are attached form an optionally substituted 4- to 6-membered ring; R"'"'"' is hydrogen or optionally substituted lower alkyl; Q is a group of the formula ##STR21##
space="preserve" listing-type="equation">--N(V'"'"')CH.sub.2 .sub.v --C(V",V'"'"'")CH.sub.2 OCH.sub.2 COO-T Q.sup.8or ##STR22## n is the number 0 or 1, v is an integer between 0 and 3, T and T'"'"' are hydrogen or a lower-alkyl or phenyl-lower-alkyl group which is cleavable under physiological conditions, V to V"'"'"' are hydrogen or lower-alkyl, U and U'"'"' are hydrogen, C1-6 alkanoyl or aroyl, Ar is aryl and R2 to R5 are hydrogen, lower-alkyl, lower-alkoxy, halogen or a group --OCH2 COO-T'"'"' or R2 and R3 together with the phenyl group to which they are attached form a 1-naphthyl group, as well as hydrates or solvates and physiologically usable salts thereof. - View Dependent Claims (2, 3, 9)
- 4. A method for the control or prevention of blood platelet thrombi, thrombosis, stroke, cardiac infarct, inflammation, or arteriosclerosis, comprising administering an effective amount of a compound of the formula ##STR23## wherein L is a group of the formula ##STR24## or
- space="preserve" listing-type="equation">R.sup.o --NH(CH.sub.2).sub.t L.sup.2
R is amidino or guanidino, each of X and Y is CH, Ro is hydrogen or amidino, t is an integer between 2 and 6, R'"'"' and R" together with the N atom and C atom to which they are attached form an optionally substituted 4- to 6-membered ring; R"'"'"' is hydrogen or optionally substituted lower alkyl; Q is a group of the formula ##STR25##
space="preserve" listing-type="equation">--N(V'"'"')(CH.sub.2).sub.v --C(V'"'"',V'"'"'")CH.sub.2 OCH.sub.2 COO-TQ.sup.8or, ##STR26## n is the number 0 or 1, v is an integer between 0 and 3, T and T'"'"' are hydrogen or a lower-alkyl or phenyl-lower-alkyl group which is cleavable under physiological conditions, V to V"'"'"' are hydrogen or lower-alkyl, U and U'"'"' are hydrogen, C1-6 -alkanoyl or aroyl, Ar is aryl and R2 to R5 are hydrogen, lower-alkyl, lower-alkoxy, halogen or a group --OCH2 COO-T'"'"' or R2 and R3 together with the phenyl group to which they are attached form a 1-naphthyl group, as well as hydrates or solvates and physiologically usable salts thereof. - View Dependent Claims (5, 6, 8)
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7. The compound, p 1-(p-amidinobenzoyl)-2-pyrrolidinyl!carbonyl!phenoxy!-acetic acid.
Specification