Abstract:
The present invention relates to the use of pteridine derivatives of general formula (I) in which X is O or NH and R may, for instance, be hydrogen, phenyl or the radical R -CH2 and R is e.g. hydrogen, (C1-C4)-alkyl mercapto, the radical -NR R or the radical -OR , and in which R , R , R , R , R , R , R , R and R have the meanings given in claim 1, which are carbon monoxide-synthase inhibitors, for the treatment of diseases caused by a raised carbon monoxide level.
Abstract:
PROBLEM TO BE SOLVED: To obtain the subject composition capable of enhancing effects of either one of an angiotensin converting enzyme inhibitor and a calcium antagonist with each other and administration of the both is reduced without manifesting adverse effects, by making the composition include both the substances. SOLUTION: This pharmaceutical composition comprises (A) an angiotensin converting enzyme inhibitor or its physiologically permissible salt, ramipril 2-[N-(1,S-ethoxycarbonyl-3-phenylpropyl-S-alanyl]-(1S,3S,5S)-2- azabicyclo-[3.3.0]octane-3-carbonic acid} represented formula I and (B) a calcium antagonist or its physiologically permissible salt felodipine [4-(2,3- dichlorophenyl)-2,6-dimethyl-3-methoxycarbonyl-5-ethoxycarbonyl-1,4- dihydropyridine] represented by formula II at a ratio of e.g. 1-5 pts.wt. ingredient A to 15-1 pts.wt. ingredient B.
Abstract:
Disclosed are cis, exo- and trans-compounds of the formula I (see formula I) in which n denotes 0, 1 or 2, R1 denotes hydrogen, (C1-C6)- alkyl which can optionally be substituted by amino, (C1-C4)- acyl- or bezoylamino, (C2-C6)-alkenyl, (C5-C9)-cycloalkyl, (C5-C9)-cycloalkenyl, (C5-C7)-cycloalkyl-(C1-C4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C1-C2)-alkyl, (C1-C2)-alkoxy or halogen, aryl-(C1-C4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R2 denotes hydrogen, (C1-C6)-alkyl, (C2-C6)alkenyl or aryl-(C1-C4)- alkyl Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C1-C6)-alkyl, (C2-C6)-alkenyl, (C5-C9)-cycloalkyl or aryl which can be mono-, di- or tri- substituted by (C1-C4)-alkyl, (C1-C4)-alkoxy, hydroxyl, halogen, nitro, amino, (C1-C4)- alkylamino, di-(C1-C4-alkylamino or methylenedioxy, or indol-3-yl, or physiologically acceptable salts thereof, a process ofr the preparation thereof, agents containing them, their use as a medicine and intermediates for the prepara- tion thereof.
Abstract:
Compounds having a coginition adjuvant action, agents containing them and the use thereof in the treatment and prophylaxis of cognitive dysfunctions The invention relates to new compounds 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.
Abstract:
The use of angiotensin-converting-enzyme (ACE) inhibitors of formula (I) or their salts in the prodn. of medicaments for treatment of cardiac insufficiency in mammals is claimed. n = 1 or 2; R = H, ORa, SRa or an opt. substd. 1-8C aliphatic, 3-9C alicyclic, 6-12C aromatic, 7-14C araliphatic or 7-14C alicyclic-aliphatic gp.; Ra = an opt. substd. 1-4C aliphatic, 6-12C aromatic or 5- to 12-membered heteroaromatic gp.; R1 = H, an opt. substd. 1-6C aliphatic, 3-9C alicyclic, 4-13C alicyclicaliphatic, 6-12C aromatic, 7-16C araliphatic or 5- to 12-membered heteroaromatic gp., or the opt. protected side chain of a natural alpha-amino acid; R2 and R3 = H or opt. substd. 1-6C aliphatic, 3-9C alicyclic, 6-12C aromatic or 7-16C araliphatic gps.; R4+R5 completes a 5-15C mono-, bi- or tricyclic heterocyclic ring system. (I) are described in DE 3211397, DE3227055 and EP 46953, 79022, 84164, 89637 and 90362.
Abstract:
1. Claims for the Contracting states ; BE, CH, DE, FR, GB, IT, Li, Lu, NL, SE A compound of the formula I see diagramm : EP0084164,P21,F7 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts. 1. Claims for the Contracting state : Austria A process for the preparation of the compounds of the formula I see diagramm : EP0084164,P24,F4 in which the hydrogen atoms on the bridgehead C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2, R1 denotes methyl, R2 denotes hydrogen, (C1 -C4 )-alkyl or benzyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen and X denotes phenyl, and its physiologically acceptable salts, which a) comprises reacting a compound of the formula II see diagramm : EP0084164,P24,F6 wherein R1 , R2 , X, Y and Z have the meanings as in formula I, with a compound of the formula III see diagramm : EP0084164,P25,F1 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n denotes 0, 1 or 2 and W denotes a radical which can be cleaved off by hydrogenolysis or by acid, and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or b) for the preparation of compounds of the formula I, in which Y and Z together denote oxygen, comprises b1 ) reacting a compound of the formula IV see diagramm : EP0084164,P25,F3 in which the H atoms on the C atoms 3a and (6+n)a have the trans configuration relative to one another and wherein n and R1 have the meanings as in formula I and W has the meaning as in formula III, with a compound of the formula V, R2 O2 C-CH = CH-CO-X wherein R2 and X have the meanings as in formula I, and subsequently splitting off the radical W and, if appropriate, also the radical R2 to form the free carboxyl groups, or, b2 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the general formula VI, wherein R2 has the meaning as in formula I, and with a compound of the general formula VII OHC-CO2 R2 X-CO-CH3 wherein X has the meaning as in formula I, subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl group, or c) for the preparation of compounds of the formula I, in which Y and Z each denote hydrogen, comprises c1 ) reacting a compound of the formula IV mentioned under b1 ) with a compound of the formula VIII see diagramm : EP0084164,P25,F2 wherein R2 and X have the meanings as in formula I, reducing the Schiff's bases obtained and subsequently splitting off the radical W and, if appropriate, the radical R2 to form the free carboxyl groups, or c2 ) catalytically reducing a compound of the formula I in which Y and Z together denote oxygen, with hydrogen, or d) for the preparation of compounds of the formula I, in which Y denotes hydroxyl and Z denotes hydrogen, comprises reducing a compound of the formula I, in which Y and Z together denote oxygen, catalytically with hydrogen or with a reducing agent, such as sodium borohydride, and, if appropriate, converting the compounds obtained according to (a)-(d) into their physiologically acceptable salts.