Abstract: This invention relates to a method of treating basal cell carcinoma with purified human recombinant DNA interferon alpha-2, preferably purified human recombinant DNA interferon alpha-2b by administering intralesionally (by injection) to a patient in need of such treatment, a sufficient amount of the purified human recombinant DNA alpha interferon, preferably recombinant DNA interferon alpha-2b, to be effective as an antitumor agent.

Abstract: A series of novel N-alkyl-N-(alkanesulphonamidoheterocyclicmethyl)-4-alkanesulphonamidophene tyl mines have been prepared, including their pharmaceutically acceptable salts and various key novel intermediates therefor. The heterocyclic moiety present in these compounds is a benzo-fused heterocyclic group derived from either benzofuran, benzothiophene, benzoxazole or quinoline, and it is attached to the adjacent methyl group of the molecule by means of the available ring carbon atom which is situated alpha to the hetero atom. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrhythmias. Preferred member compounds include N-methyl-N-(5-methanesulphonamidobenzofur-2-ylmethyl)-4-methanesulphonamid op henethylamine and N-methyl-N-(6-methanesulphonamidoquinol-2-ylmethyl)-4-methanesulphonamidop hen thylamine. Methods for preparing all these compounds from known starting materials are provided.

Abstract: A 6-tertiary amino-2-(Z.dbd.CH--)benzofuran dye is disclosed, where Z represents the atoms providing an electron withdrawing group and a conjugated methine linkage completing a resonant dye chromophore including the 6-tertiary amino group as an electron donor and the electron withdrawing group as an electron acceptor. The dyes are formed by condensing a 6-tertiary amino-2-formylbenzofuran with an electron withdrawing dye nucleus precursor containing an active methyl or methylene site. The dyes exhibit bathochromically shifted absorption peaks.

Abstract: A 6-tertiary amino-2-(Z.dbd.CH--)benzofuran dye is disclosed, where Z represents the atoms providing an electron withdrawing group and a conjugated methine linkage completing a resonant dye chromophore including the 6-tertiary amino group as an electron donor and the electron withdrawing group as an electron acceptor. The dyes are formed by condensing a 6-tertiary amino-2-formylbenzofuran with an electron withdrawing dye nucleus precursor containing an active methyl or methylene site. The dyes exhibit bathochromically shifted absorption peaks.

Abstract: The present invention relates to 3-aminomethyl derivatives of indane, dihydrobenzofurane, dihydrobenzothiophene, and indoline, acid addition salts thereof, isomers thereof, methods of preparation, pharmaceutical compositions and method of treating CNS-disorders such as schizophrenia, Parkinson's disease, depression, anxiety, migraine and senile dementia, or in the cure of cardiovascular diseases, by administering such a derivative.

Abstract: (1H-azol-1-ylmethyl)substituted benzotriazole derivatives, compositions containing the same, and methods of treating estrogen dependent disorders.

Abstract: Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.

Abstract: A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizi ne-2,4'-imidazolidin]-3'-yl)ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2 -yl)amino]ethyl]methanesulfonamide is described.

Abstract: The invention relates to 1,8-dihydroxy-3-methylbenz[b]phenanthridine-7,12-dione and its derivatives of formula I ##STR1## wherein R.sup.1 is hydrogen or the radical of formula II ##STR2## and salts of the compound, wherein R.sup.1 is the radical of formula II. These compounds can be obtained by means of a novel microbiological process and used for the therapeutic treatment of tumors.

Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formula: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound through Friedlaender reaction. It has an excellent antitumor activity and a high degree of safety, and can be applied as an antitumor medicine for curing tumors of various kinds.

Abstract: A process is provided for preparing 2,2'-methylene-bis-(4-hydrocarbyl-6-benzotriazolyl-phenols) having formula III: ##STR1## wherein: R is selected from the group consisting of alkyl having from one to about twelve carbon atoms; arylalkyl having from seven to about fourteen carbon atoms and cycloalkyl having from three to about twelve carbon atoms;X is selected from the group consisting of hydrogen, halogen, alkyl having from one to about twelve carbon atoms, aryl having from six to ten carbon atoms, arylalkyl having from seven to about sixteen carbon atoms, alkoxy having from one to about twelve carbon atoms, aryloxy having from six to ten carbon atoms; and arylalkoxy having from seven to about sixteen carbon atoms;R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen; alkyl having from one to about six carbon atoms, and R.sub.1 and R.sub.2 taken together to form a four to six member heterocyclic ring including a nitrogen atom; provided, that at least one of R.sub.1 and R.sub.

Abstract: A process is described for the preparation of compounds of formula (1) ##STR1## [where OR is hydroxyl, protected hydroxyl or OP(O)(OCH.sub.2 Ph)(OR.sup.1) (where Ph is phenyl and OR.sup.1 is hydroxyl or protected hydroxyl)] and salts thereof, which comprises reacting a compound of formula (2) ##STR2## with a compound of formula (3) ##STR3## (where OR is as defined above and one of X.sup.1 and X.sup.2 is a leaving group and the other is a hydrogen atom) or a salt thereof, followed, if desired, by removal of the hydroxyl protecting group when present and/or by salt formation.The compounds of formula (1) are either anticancer agents or intermediates useful in the synthesis of anticancer agents.

Abstract: Novel 2,6-methanopyrrolo-3-benzazocines, intermediates, processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.

Abstract: A vat dye based on monobromofluoranthene is prepared by a process in which monobromofluoranthene which contains no more than 7% of dibromofluoranthene is reacted with 1-amino-4-benzoylaminoanthraquinone, the reaction product is condensed at from 50.degree. to 70.degree. C. in 83-88% strength sulfuric acid to give the carbazole compound, and the latter is then further brominated to a bromine content of from 20 to 23% by weight.The dyes obtained by the novel process are very useful for dyeing cotton.

Abstract: The invention is novel 2-carbamoylnicotinic and 3-quinolinecarboxylic acids and esters which are intermediate compounds for the preparation of 2-(2-imidazolin-2-yl)pyridine and quinoline herbicides.

Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.

Abstract: There is provided novel (2-imidazolin-2-yl)thieno and furo compounds, and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.

Abstract: Dihydrobenz[c]acridine carboxylic acid derivatives are provided which are useful in treating tumors in mammals. These dihydrobenz[c]acridine carboxylic acid derivatives have the formula: ##STR1## or a pharmaceutically acceptable salt thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are as defined in the specification. Also provided are pharmaceutical compositions of said compounds. In addition, processes for the preparation of these compounds are disclosed.

Abstract: New camptothecin derivatives, useful as antitumor agents or intermediates therefor, of the general formula (I) ##STR1## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C.sub.1 -C.sub.18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C.sub.3 -C.sub.19 alkenyl, C.sub.3 -C.sub.19 alkynyl or C.sub.3 -C.sub.8 cycloalkyl group; a C.sub.3 -C.sub.

Abstract: Muteins of biologically active proteins such as IFN-.beta. and IL-2 in which cysteine residues that are not essential to biological activity have been deleted or replaced with other amino acids to eliminate sites for intermolecular crosslinking or incorrect intramolecular disulfide bridge formation. These muteins are made via bacterial expression of mutant genes that encode the muteins that have been synthesized from the genes for the parent proteins by oligonucleotide-directed mutagenesis.