摘要:
The use of substituted 3,4-dihydro-2H-benzopyrans as remedies for obstructive functional disorders of the lungs and/or disorders of the efferent urinary passagesThe use of 3,4-dihydro-2H-benzo[b]pyrans of the formula I ##STR1## in which R.sup.1 represents H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5, where R.sup.4 and R.sup.5 are identical or different and represent H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkyl-carbonyl,R.sup.2 and R.sup.3 are identical or different and represent alkyl having 1-4 carbon atoms,Ar represents an aromatic or heteroaromatic system which is unsubstituted or substituted by 1 to 3 identical or different radicals (C.sub.1 -C.sub.2)-alkyl, (C.sub.1 -C.sub.2)-alkoxy, halogen, trifluoromethyl, CN, NO.sub.2, CO--(C.sub.1 -C.sub.2)-alkyl or SO.sub.m --(C.sub.1 -C.sub.2)-alkyl with m=1 or 2,n represents 1 or 2,X represents a chain (CH.sub.2).sub.r which can be interrupted by a heteroatom O, S or NR.sup.6, where R.sup.6 denotes H or (C.sub.1 -C.sub.4)-alkyl, and r represents the numbers 2, 3, 4 or 5,for the preparation of a remedy for obstructive functional disorders of the lungs and/or disorders of the efferent urinary passages, is described.
摘要:
3,4-Dihydro-2H-benzo[b]pyrans of the formula I ##STR1## are described, in which R.sup.1 is H, OH, (C.sub.1 -C.sub.2)-alkoxy, (C.sub.1 -C.sub.2)-alkyl or NR.sup.4 R.sup.5,R.sup.4 and R.sup.5 being identical or different and representing H, (C.sub.1 -C.sub.2)-alkyl or (C.sub.1 -C.sub.3)-alkylcarbonyl,R.sup.2 and R.sup.3 are identical or different and are alkyl having 1-4 carbon atoms,Ar is an aromatic or heteroaromatic system which is unsubstituted or substituted,n is 1 or 2 andX is a (CH.sub.2).sub.r chain which can be interrupted by a heteroatom O, S or NR.sup.6, R.sup.6 being H or (C.sub.1 -C.sub.4)-alkyl andr being one of the numbers 2, 3, 4 or 5.Processes for the preparation of these compounds, their use and pharmaceutical products based on these compounds are also described.
摘要:
Compounds I ##STR1## where R.sup.1 is H, alkyl, alkoxy, CO alkyl, COOH, carboxyalkyl, CONR.sub.2, CN, NO.sub.2, alkylsulfi(o)nyl, arylsulfi(i)-nyl; R.sup.2 is H, OH, alkoxy, alkyl or alkylcarbonyl, R.sup.3 /R.sup.4 are alkyl, m is zero or one and X is --CR.sup.6 .dbd.CR.sup.7 -(--CR.sup.8 .dbd.CR.sup.9) (R.sup.6 R.sup.9 are H or alkyl), where n is zero or 1, are described. They are active antihypertensives and spasmolytics for the bladder, intestine, gall bladder, uterus, trachea and ureter.
摘要:
2,3,4,5-Tetrahydro-1-benzoxepins of the formula I ##STR1## with R.sup.1 equaling, inter alia, H, alkyl, alkoxy, Hal, alkylsulfonyl, arylsulfonyl, R.sup.2 equaling H, alkyl, alkoxy, OH, R.sup.3 to R.sup.6 H or alkyl and X equaling ##STR2## have excellent efficacy as antihypertensives, as coronary therapeutics, as agents for the treatment of cardiac insufficiency, of disturbances of cerebral and peripheral blood flow or of disturbances of intestinal motility, premature labor, obstructions of the airways or of the urinary tract or of the biliary tract or as spasmolytics.
摘要:
Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylakyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 -C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(5) are together an alkylene chain,and where n is equal to zero, 1 or 2 and their pharmaceutically tolerable salts are outstanding antiarrhythmics.
摘要:
Benzo[b]pyran derivatives of the formula I ##STR1## with E--D equal to CH--CHOH or C.dbd.CH;X equal to oxygen or sulfur;Y equal to oxygen, sulfur, SO, SO.sub.2 or NR.sup.9 ;R.sup.1 equal to CN, NO.sub.2, Hal, alkoxycarbonyl, SO.sub.1-2 -alkyl or SO.sub.1-2 -aryl;R.sup.2 equal to H, OH, alkoxy, alkyl, Hal, NR.sup.10 R.sup.11 ;R.sup.3 /R.sup.4 equal to alkyl;R.sup.5 /R.sup.6 equal to alkyl, (CH.sub.2).sub.1-6 COO-alkyl, (CH.sub.2).sub.1-6 CONR.sup.10 R.sup.11, (CH.sub.2).sub.0-6 COOH, (CH.sub.2).sub.1-6 CO-alkyl, CO.sub.2 -alkyl, alkylmercaptoalkyl, alkylsulfi(i)(o)nyl, hydroxyalkyl, mercaptoalkyl, aminoalkyl, N-(di)-alkylaminoalkyl or (CH.sub.2).sub.f Ar with f equal to zero-3;R.sup.7 /R.sup.8 equal to hydrogen, alkyl or phenyl, and m equal to zero-2are outstanding antihypertensives and spasmolytics. Preparation processes and use are described.
摘要:
Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O).sub.n -- or R(7)R(8)N--O.sub.2 S--and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br, I, alkyl, alkoxy or phenoxy, R(6)--S(O).sub.n or R(7)R(8)N--and R(6) is equal to alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl,R(7) and R(8) are equal to alkyl or phenylalkyl or phenyl,and in which R(7) and R(8) may also together be a C.sub.4 --C.sub.7 chain, and in which R(7) and R(8), together with the nitrogen atom to which they are bonded, may be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where R(3), R(4) and R(5) are equal to hydrogen or alkyl, or R(3) and R(4) are together an alkylene chain or R(4) and R(4) are together an alkylene chain,and where n is equal to zero, 1 or 2and their pharmaceutically tolerable salts are outstanding antiarrhythmics.
摘要:
The present invention relates to use of an inhibitor of the renin-angiotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).
摘要:
Peptides of the formula IA-B-C-E-F-K-P-G-M-F'-I (I),wherein the terms A, B, C, E, F, K, P, G, M, F', and I are defined in the specification, have bradykinin antagonist action. Their therapeutic utility includes all pathological states which are mediated, caused or supported by bradykinin and bradykinin-related peptides.
摘要:
Peptides of the formula IZ-P-A-B-C-E-F-K-(D)Q-G-M-F'-I (I)and the physiologically tolerated salts thereof, are described.They have an excellent bradykinin-antagonistic action.They are obtained by reacting reacting a fragment with a C-terminal free carboxyl group or its activated derivative with a corresponding fragment with an N-terminal free amino group or assembling the peptide stepwise, where appropriate eliminating in the compound obtained in this way one or more protective groups introduced temporarily to protect other functionalities, and where appropriate converting the compounds of the formula I obtained in this way into the physiologically tolerated salt thereof.