摘要:
This invention is directed to novel benzoxazin-2-ones of the formula ##STR1## wherein A is a sulfur atom or an SO, SO.sub.2, R--N.dbd.S, or R--N.dbd.SO.sub.2 group where R is a hydrogen atom or an acyl group;D is an alkylene group;R.sub.1 is an alkyl, phenylalkyl, cycloalkyl, or phenyl group;R.sub.4 is a hydrogen atom or an alkyl group;R.sub.5 is a hydrogen or halogen atom or a nitro or alkyl group; andR.sub.6 is a hydrogen or halogen atom or an alkyl group,having valuable pharmacological properties, particularly an antithrombotic activity. The compounds of Formula I may be prepared by the methods used for analogous compounds.
摘要:
Compounds of the formula ##STR1## wherein W is vinylene, methyl-vinylene, methylene or ethylene;m is 0, 1 or 2;D is straight or branched alkylene of 2 to 6 carbon atoms, straight or branched hydroxy-alkylene of 3 to 6 carbon atoms, or xylylene;R.sub.1 is hydrogen or alkyl of 1 to 3 carbon atoms;R.sub.2 is cycloalkyl of 3 to 6 carbon atoms, aryl of 6 to 10 carbon atoms, aralkyl of 7 to 11 carbon atoms, heteroaryl, heteroarlkyl, 1,2,4-triazolyl, triphenylmethyl, 4,5-bis-(p-chlorophenyl)-oxazol-2-yl, N-methyl-cyclohexylamino-carbonylmethyl,-amino-iminomethyl or, when m is 1 or D is hydroxyalkylene or xylylene, also alkyl of 1 to 6 carbon atoms; andR.sub.3 and R.sub.4 are each hydrogen, halogen, alkyl of 1 to 4 carbon atoms, amino, acetylamino or nitro.The compounds of the invention are useful as cardiotonics and as antithrombotics.
摘要:
Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or halogen,R.sub.2 is hydroxyl, alkoxy of 1 to 6 carbon atoms, aralkoxy of 7 to 10 carbon atoms, amino, (alkyl of 1 to 3 carbon atoms)-amino, piperidino or morpholino, andn is 0, 1 or 2,Diastereoisomers thereof and, when R.sub.2 is hydroxyl, non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base; the compounds, their diastereoisomers and the salts are useful as antithrombotics, anti-hypercholesteremics and anti-hyperglyceridemics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is mono- or di-substituted amino, where the substituents are selected from the group consisting of alkyl of 1 to 6 carbon atoms, cyclohexyl, allyl and benzyl; unsubstituted, mono-substituted or di-substituted pyrrolidino, piperidino, hexamethyleneimino, morpholino, piperazino, thiomorpholino, 1-oxido-thiomorpholino or 1,1-dioxido-thiomorpholino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl; 1,2,5,6-tetrahydropyridino; 1,2,3,4-tetrahydroisoquinolino; indolino; or 3,6-ethylene-hexamethyleneimino;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is phenylalkylamino, alkylamino, dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino;R.sub.2 is dialkylamino, piperidino, morpholino, thiomorpholino or 1-oxido-thiomorpholino; andR.sub.3 is halogen, alkoxy, alkylthio, phenylalkoxy or phenylalkylthio;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics and antimetastatics.
摘要:
Compounds of the formula ##STR1## wherein n is 0 or 1;A is methylene, vinylene or ethylene optionally substituted by lower alkyl;B is alkylene;R.sub.1 is an optionally substituted alkyl, phenyl or naphthyl group, or a cycloalkyl or pyridyl group; andR.sub.2 is hydrogen or acyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antithrombotics.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is unsubstituted, mono-substituted or di-substituted piperidino, where the substituents are selected from the group consisting of methyl, hydroxymethyl, hydroxyl, phenyl and benzyl;R.sub.2 is hydrogen, methyl or benzyl; andR.sub.3 is hydrogen, halogen, alkyl of 1 to 3 carbon atoms or alkoxy of 1 to 3 carbon atoms;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiphlogistics and antithrombotics.