摘要:
Compounds I ##STR1## in which R(1) and R(4) equal H, alkyl, alkoxy, Hal, CF.sub.3, NO.sub.2, OH, acetamido or amino;R(2) equals H, alk(en)yl or phenylalkyl (optionally substituted);R(3) equals H, (cyclo)alk(en)yl-(alkyl), phenyl or phenylalkyl (optionally substituted);A equal CHOH, CO, CH.dbd.CH, C.tbd.C, CH.sub.2, O or S;m equals 1 or 2;n equals 1 to 3;p equals 0 to 4;R(5) equals some amino groups, and their salts, exhibit excellent calcium-antagonistic activity.Processes for their preparation are described.
摘要:
The invention relates to compounds of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.4 represent optionally substituted aliphatic, alicyclic, alicyclic-aliphatic, aromatic, araliphatic, heteroaromatic or heteroaromatic-aliphatic radicals, with R.sup.2, if not already covered by the above-mentioned definitions, denoting the side-chain, which is protected if necessary, of a naturally occurring .alpha.-amino acid, R.sup.4 can additionally represent ##STR2## R.sup.3 denotes an optionally substituted aliphatic, alicyclic, aromatic or araliphatic radical, or R.sup.3 and R.sup.4 form, together with the atoms carrying them, a mono-, bi- or tricyclic heterocyclic ring system,agents containing these, and the use thereof as pharmaceuticals having a psychotropic action for the prophylaxis of disorders of the central nervous system, especially having a nootropic action for the treatment of cognitive dysfunctions.
摘要:
The invention relates to amino acid esters of the formula I ##STR1## in which n is 2 and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning indicated in the description, to a process and intermediates for the preparation thereof, to agents containing them, and the use thereof.
摘要:
The invention relates to new comoounds having a cognition adjuvant action, to the use of ACE inhibitors as medicaments having a cognition adjuvant action, to agents containing them, and to the use thereof for the treatment and prophylaxis of cognitive dysfunctions.
摘要:
Compounds of the formula I ##STR1## where R(1), R(2), R(3), R(4) and R(5) are, inter alia, hydrogen and alkyl, m is 1-4, n is 0 or 1, p is 0-4 and R(6) is identical or different dialkylamine derivatives, and salts thereof, have a calcium-antagonistic action. They are obtained by reacting corresponding amines with a compound II which carries, on the side chain, a leaving group which can be displaced nucleophilically, or from a hydroxyphenyl-dihydroquinolin-2-one compound by reaction with a corresponding side chain compound which has a leaving group which can be displaced nucleophilically.
摘要:
Calcium antagonists of the formula ##STR1## with R(1), R(2), R(3) and R(4) being, inter alia, H, alkyl, alkoxy, halogen, in some cases phenyl; m being 1-4; n being 0-3; X being CH.sub.2, O, S, CO, CHOH or CR.sub.2, and R(5) being various groups containing nitrogen atoms, are described.They are obtained by reaction of compounds II which are likewise new and which contain in place of R(5) a leaving group Y (Cl, Br, I) with the appropriate (cyclic) amino compound.Another synthesis comprises reaction of the appropriate indolinone derivative IV which has a non-etherified hydroxyl group with a side chain which contains a terminal leaving group Z (Cl, Br, I) in the presence of a base.Furthermore, indolinone derivatives VI with an ether side chain with a terminal epoxide group can be reacted with (cyclic) amines to give compounds I.
摘要:
Benzothiazine derivatives of the formula I ##STR1## with (R(1), R(1)', R(1)", R(4) and R(4)' equal to hydrogen, alkyl, alkoxy, halogen, nitro, hydroxyl, acetamido or amino; R(2) equal to hydrogen, alkyl, alkenyl, phenyl; R(3) equal to hydrogen, alkyl, alkenyl, phenyl; R(5) equal to hydrogen or (C.sub.1 -C.sub.3)-alkyl; R(6) equal to one of the following groups, ##STR2## with R(7) and R(8) equal to hydrogen, alkyl, cycloalkyl, phenyl; R(9) equal to hydrogen, alkyl, phenyl, pyridyl, pyrimidinyl or benzoyl; R(10) equal to hydrogen, alkyl, phenyl; R(11) equal to hydrogen, hydroxyl, alkoxy or, together with R(12), a bond; and R(12) equal to hydrogen or, together with R(11), a bond; m equal to 1, 2, 3 or 4; n equal to 0 or 1; p equal to 0, 1, 2, 3 or 4, and X equal to oxygen or two hydrogen atoms, and salts of the compounds of the formula I with physiologically tolerated acids and a process for the preparation of compounds I, likewise a method of treatment of disturbances of the calcium balance of a human body are described.
摘要:
The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 and R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
摘要:
The invention relates to a method of treating cardiac insufficiency by using compounds of the formula I ##STR1## in which n is 1 or 2, R, R.sup.1, R.sup.2 and R.sup.3 are identical or different and each denote hydrogen or an organic radical and R.sup.4 R.sup.5, together with the atoms carrying them, form a mono-, bi- or tri-cyclic heterocyclic ring system. The invention furthermore relates to compounds of the formula I and agents containing these for use in the treatment of the abovementioned disease.
摘要:
What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.