摘要:
The invention relates to new substituted o-phenylenediamine derivatives of the general formula ##STR1## in which R represents optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkinyl,X represents O, S, SO or SO.sub.2 andR.sup.1 and R.sup.2 are different from one another and individually represent ##STR2## in which R.sup.3 and R.sup.4 are identical or different and represent alkyl andR.sup.5 represents hydrogen, optionally substituted alkyl or optionally substituted alkoxy, and salts thereof.Also included in the invention are (1) methods for preparing the above-described compounds, (2) compositions containing the above-described compounds and (3) methods for the treatment of helminthiasis.
摘要:
Novel substituted benzenesulphonic acid esters, particularly useful as anthelmintics are provided. The novel compounds are those of the general formula ##STR1## in which R represents hydrogen, optionally substituted alkyl, cyano, alkoxy, halogen, trifluoromethyl, amino, acylamino or nitro,X represents SO.sub.3 andR.sup.1 and R.sup.2 are different from one another and individually represent one of the radicals ##STR2## wherein Y represents S andR.sub.3 represents hydrogen, optionally substituted alkyl or alkoxy,and salts thereof. Also included in the invention are methods for preparing the novel compounds, compositions containing them and methods for the use of the compounds and compositions.
摘要:
New 4-acylaminophenylacetamidines of the formula: ##STR1## in which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
摘要:
New 4-acylaminophenylacetamidines of the formula: ##SPC1##In which R is a straight or branched chain alkoxyalkyl having 3 to 8 carbon atoms or straight or branched chain alkenyloxyalkyl having 3 to 8 carbon atoms wherein the alkoxy moiety or alkenyloxy moiety may substituted by alkoxy or phenyl, and including the non-toxic pharmacologically acceptable salts thereof. The products have utility as parasiticides.The products are obtained by either of two methods: (1) via the reaction of an N'-(4-aminophenyl)-N,N-dimethylacetamidine with an acylating agent or (2) via the reaction of a 4-acylaminoaniline with an N,N-dimethylacetamide or N,N-dimethylthioacetamide.
摘要:
Anti-bacterially active penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom or optionally substituted alkoxy group,R.sub.3 denotes a hydrogen atom, COR.sub.4, SO.sub.2 -alkyl, SO.sub.2 -aryl or an optionally substituted alkyl group, but R.sub.2 and R.sub.3 do not simultaneously denote hydrogen atoms, andR.sub.4 denotes a hydrogen atom or any of many possible organic radicals.The compounds are also inhibitors of .beta.-lactamases so they can be used in conjunction with .beta.-lactamase-susceptible antibiotics. They are useful in fighting bacterial infection, in promoting animal growth and in preserving various materials.
摘要:
A new class of N'-(aminoacylaminophenyl) acetamidines: ##STR1## in which R.sup.1 and R.sup.2 are the same or different and represent hydrogen, alkyl, aryl or the substituted derivatives thereof or, together with the nitrogen atom to which they are attached, an heterocyclic ring; and R.sup.3 is hydrogen, alkyl, aryl, aralkyl, or a heterocyclic moiety including the substituted derivatives thereof. The products have utility as anthelmintics.The products are obtained by treating a suitable amino-acid or a carbonyl-activated amino-acid, with the appropriate N'-(4-aminophenyl)-N,N-dimethylacetamidine. In addition, the products are obtained by treating a suitable N'-(haloacylaminophenylacetamidine with an appropriate amine.
摘要:
The present invention refers to novel anellated 4H-1,4-benzothiazines, several processes for the synthesis thereof, their use as pharmaceutical agents, in particular their use as lipoxygenase-inhibiting agents, pharmaceutical compositions containing the novel benzothiazines and a process for their manufacture.
摘要:
Compounds of the formula ##STR1## in which R.sup.1 is an optionally substituted aryl or heteroaryl radical,R.sup.2 is an alkyl or alkenyl radical which is optionally substituted by alkoxy or cycloalkyl, or an optionally substituted aryl or heteroaryl radical, and X is an optionally aklyl-substituted methylene radical or a direct bond, but if X is a direct bond R.sup.2 is not aryl,or physiologically acceptable acid addition salts thereof, exhibit activity on the circulation system particularly as hypotensive agents.
摘要:
Trisubstituted cyanoguanidines of the formula ##STR1## in which R.sup.1 represents an optionally substituted phenyl or phenylalkyl radical, an alkyl radical with more than 1 carbon atom, a substituted alkyl radical, an alkenyl or alkinyl radical or an optionally substituted cycloalkyl radical,R.sup.2 represents an optionally substituted alkyl radical or an alkenyl or alkinyl radical andR.sup.3 represents an optionally substituted alkyl radical, an alkenyl or alkinyl radical, an optionally substituted cycloalkyl radical or an optionally substituted phenyl or phenylalkyl radical, orR.sup.2 and R.sup.3, together with the nitrogen atom to which they are bonded, represent an optionally substituted heterocyclic radical, which optionally contains an oxygen atom as a further hetero-atom,or a physiologically acceptable acid addition salt thereof, which possess fungicidal properties. Processes for their preparation are also taught.
摘要:
New penicillin 1,1-dioxides of the formula ##STR1## or a salt thereof, in which R.sub.1 denotes a hydrogen atom or an ester-forming radical,R.sub.2 denotes a hydrogen atom,R.sub.3 denotes a hydrogen atom,R.sub.4 denotes a hydrogen atom, an optionally substituted naphthyl radical or a radical of the general formula ##STR2## and the remaining variables can be various organic radicals.