摘要:
2-Alkylthio-1-aminoalkyl-2-pyrroline-3-carbonitriles and pharmaceutically acceptable acid addition salts, processes for their preparation and formulation into pharmaceutical compositions as well as their activity as thrombocyte aggregation-inhibitors are described. The compounds are thus useful for the prophylaxis and therapy of thrombotic states.
摘要:
New 1,6-naphthyridinone derivatives of the formula I ##STR1## are herein described wherein R.sup.1 represents an unsubstituted or substituted aromatic or heteroaromatic ring;R.sup.2 is hydrogen, a straight-chained or branched alkyl, alkoxyalkyl, or a substituted or unsubstituted aminoalkyl group with up to ten carbon atoms;R.sup.3 is hydrogen, a straight-chained or branched alkyl group, or an alkoxycarbonyl radical with up to four carbon atoms;R.sup.4 is hydrogen, or a morpholinoethyl group;R.sup.5 is a straight-chained or branched alkyl group with up to four carbon atoms, or an amino group; andR.sup.6 is a carboxyl group, or an alkyl- or alkyloxyalkyl carbonyl radical, containing up to 12 carbon atoms and optionally interrupted by an oxygen, sulphur, or nitrogen atom;as well as optionally the pharmacologically acceptable salts thereof; processes for the preparation of these derivatives and their use in the control of vascular diseases.
摘要:
The present invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are unsubstituted or substituted aromatic rings, Alk is a straight-chained or branched lower hydrocarbon chain and Z is a hydrogen atom, with the proviso that when Alk is a straight-chained hydrocarbon chain, Z can also be a lower alkylamino radical of the general formula II ##STR2## in which R.sup.3 and R.sup.4 are the same or different and are hydrogen atoms or straight-chained or branched lower alkyl radicals or R.sup.3 and R.sup.4, together with the nitrogen atom to which they are attached, can also form a ring optionally containing further hetero atoms; and the pharmacologically acceptable salts thereof.The present invention also provides an inventive process for preparing these compounds, as well as pharmaceutical compositions containing them. The compounds I may be used in the therapy of inflammations and they are free of gastrointestinal side effects.
摘要:
The present invention provides compounds of the general formula I ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are unsubstituted or substituted aromatic rings, Alk is a straight-chained or branched lower hydrocarbon chain and Z is a hydrogen atom, with the proviso that when Alk is a straight-chained hydrocarbon chain, Z can also be a lower alkylamino radical of the general formula II ##STR2## in which R.sup.3 and R.sup.4 are the same or different and are hydrogen atoms or straight-chained or branched lower alkyl radicals or R.sup.3 and R.sup.4, together with the nitrogen atom to which they are attached, can also form a ring optionally containing further hetero atoms; and the pharmacologically acceptable salts thereof.The present invention also provides an inventive process for preparing these compounds, as well as pharmaceutical compositions containing them. The compounds I may be used in the therapy of inflammations and they are free of gastrointestinal side effects.
摘要:
1,2,4-Benzothiadiazine oxide derivatives of the general Formula I ##STR1## in which R.sup.1 represents an unsubstituted or substituted aryl radical;R.sup.2 and R.sup.5, which may be the same or different, and represent hydrogen, halogen, or a nitro group, andR.sup.3 represents a hydrogen atom or a hydroxy radical, an alkyl, alkoxy alkyl or alkoxy carbonyl radical with up to four carbon atoms, unsubstituted or substituted by halogen, hydroxy, amino, alkyl amino or dialkyl amino radicals, or a phenyl radical, unsubstituted or substituted by halogen,are described as having anxiolytic effects on the central nervous system.
摘要翻译:其中R 1表示未取代或取代的芳基的通式I(I)的1,2,4-苯并噻二嗪氧化物衍生物; R 2和R 5可以相同或不同,表示氢,卤素或硝基,R 3表示氢原子或羟基,具有至多4个碳原子的烷基,烷氧基烷基或烷氧基羰基, 被卤素,羟基,氨基,烷基氨基或二烷基氨基取代或被未取代或被卤素取代的苯基被描述为对中枢神经系统具有抗焦虑作用。
摘要:
4-Thioxobenzopyrano[2,3-d]-pyrimidine derivatives of the general formulae Ia or Ib ##STR1## are described. Compounds Ia and Ib are tautomers and are valuable intermediates for the preparation of 5H-[1]-benzopyrano[2,3-d]pyrimidine derivatives having ulcer-protective action without inhibition of secretion.
摘要:
The invention relates to 5H-[1]benzopyrano-[2,3-d]pyrimidine derivatives of the general formula I ##STR1## which may be prepared by means of a new chemical process and have a protective effect similar to that of cimetidine, but do not exhibit the undesired side effects of antisecretory agents. The invention is based on a new mucoprotective mode of action which prevents lesions of the mucous membrane epithelium to arise.
摘要:
New aminosulfonic acids of the general formula I ##STR1## wherein n represents the figures 4, 5, or 6, prepared according to previously known processes and characterized by very good tolerance and valuable cardiovascular properties, serve for the therapy of dysrhythmia and are superior to procaine.
摘要:
The present invention provides 5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, are hydrogen or halogen atoms or lower alkyl or alkoxy radicals, R.sup.3 is a hydrogen atom or a lower alkyl radical, R.sup.4 is a hydrogen atom or a lower alkyl or alkanoyl radical and n is 1 or 2; and the pharmaceutically acceptable salts thereof formed with inorganic and organic acids; but excluding 6-benzyl-2,12-dimethoxy-1-hydroxy-7-methyl-5,6;8,9-tetrahydro-7H-dibenz(d,f)azonine in which case R.sup.1, R.sup.2 and R.sup.4 are hydrogen, n is 1 and R.sup.3 is methyl. The lower alkyl, alkanoyl and alkoxy radicals are straight chained or branched radicals containing 1 to 5 carbon atoms.The present invention also provides a process for the preparation of these compounds, as well as pharmaceutical compositions containing them.
摘要:
4-Oxo-pyrido[2,3-d]pyrimidine derivatives are herein described as well as processes for their preparation.These compounds possess valuable pharmacological properties. As calcium antagonists they exert vasospasmolytic, vasodilatory, and antihypertensive activities. Surprisingly some of the compounds also have the effect of increasing contractility. They are therefore particularly suited for the treatment of vascular diseases.