Ciba-geigy Corporation

Novartis Corporation

Tibur Schmidlin

Peter Buhlmayer

Franz Ostermayer

Paul Zbinden

Peter B Uhlmayer

Compounds of the formula ##STR1## and their salts, in which R.sub.1, is a C.sub.1 -C.sub.7 aliphatic hydrocarbon radical; X.sub.1 is --CO; X.sub.2 is a divalent aliphatic hydrocarbon radical which comprises an ethyl group and an alkylene of 2 to 6 carbon atoms; R.sub.2 is hydroxy, carboxy or alkoxycarbonyl in which alkoxy is from 1 to 7 carbon atoms; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl or 5-tetrazolyl; and the rings A and B independently of one another are otherwise unsubstituted; can be prepared in a known manner and may be used as active ingredients for medicaments.

Acyl compounds

The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## R.sub.1 is C.sub.1 -C.sub.7 alkyl that is unsubstituted or substituted by halogen or by hydroxy, or is C.sub.2 -C.sub.7 -alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.7 alkoxy or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.7 alkoxy;

N-acyl-N-heterocyclylalkyamino acids compositions and method of use

The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## wherein Y.sub.1 is O, S or N(R) and R is hydrogen or C.sub.1 -C.sub.7 alkyl; X.sub.1 is --CO-- or --S(O).sub.m -- and the index m is 0, 1 or 2; one of the variables X.sub.2 and X.sub.4 is C.sub.1 -C.sub.4 alkylene and the other of the variables X.sub.2 and X.sub.4 is a bond; or each of the variables X.sub.2 and X.sub.4 is a bond; X.sub.3 is C.sub.3 -C.sub.7 cycloalkylidene or the structural element --C(X.sub.a)(X.sub.b)-- and X.sub.a is hydrogen or C.sub.1 -C.sub.7 alkyl and X.sub.b is C.sub.1 -C.sub.7 alkyl; and the rings A, B and C, with the exception of the substituents indicated in the formula, and also aromatic substituents are, independently of one another, unsubstituted or mono- or poly-substituted by substituents selected from the group consisting of halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy, C.sub.2 -C.sub.7 alkenyloxy, phenoxy, benzyloxy, trifluoromethyl and S(O).sub.m --R, wherein m is 0, 1 or 2 and R is hydrogen or C.sub.1 -C.sub.7 alkyl; or a salt thereof.

N-acyl-N-heterocyclylalkylamino acid compounds and method of use thereof

The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## The compounds and their pharmaceutically acceptable salts can be used as antihypertensives, agents for the treatment of glaucoma, or for increasing the flow of the retinal ocular fluid.

N-acyl-n-quinolinyl or isoquinounyl alkylamino acids compositions and

Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.m --R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO.sub.n H.sub.2 where n is 2 or 3; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl, 5-tetrazolyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.

Biphenylyl compounds of formula ##STR1## wherein the variables R.sub.1, R.sub.2, R.sub.3, p, q and X and the rings A and B are as defined in claim 1, in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as active ingredients in medicaments.

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Basel, Switzerland

Tibur Schmidlin