摘要:
There are described (+)-6-chloro-5,10-dihydro-5-[(1-methyl-4-piperidinyl)-acetyl]-11H-dibenzo [b,e][1,4]diazepin-11-one, the isolation thereof from a mixture of enantiomers and its use as a pharmaceutical material.The compound is characterized by a powerful activity against ulcers of the gastro-intestinal tract.
摘要:
Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.
摘要:
Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.4 alkyl; and Z is a single bond, oxygen, methylene or 1,2-ethylene; and NR.sub.1 R.sub.2 --N oxides and nontoxic, pharmaceutically acceptable addition salts thereof. Also disclosed are pyrrolobenzodiazepinone intermediates, pharmaceutical compositions containing the condensed diazepinones and methods of using them to treat cardiovascular disorders, particularly bradycardia and bradyarrhythmia.
摘要:
Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.
摘要:
New substituted pyrido[2,3-b][1,4]benzodiazepin-6-ones suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human and veterinary medicine are described.
摘要:
(.+-.)-1-[4-[Ethyl[2-(4-methoxyphenyl)-1-methylethyl]-amino]-1-oxobutyl]-N,N-dimethyl-4-piperidine carboxamide and (+)-1-[4-[ethyl[2-(4-methoxyphenyl)-1-methylethyl]-amino]-1-oxobutyl]N,N-dimethyl-4-piperidinecarboxamide, as well as the physiologically acceptable acid addition salts of these compounds are suitable for the treatment of bradycardia and bradyarrhythmia.
摘要:
New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
摘要:
New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
摘要:
Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-�(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.
摘要:
New diazepinones of formula I ##STR1## wherein the substituents are defined herein, which compounds exhibit favorable effects on heart rate and in view of the absence of inhibitory effects on gastric acid secretion and salivation and the absence of mydriatic effects, are suitable as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia in human and veterinary medicine.