Abstract: Preparation of 3-isothiazolones by a single-kettle synthesis from a 3,3'-dithiodipropionic acid, a 3-thiopropionic acid, or their related acid halide by reacting sequentially with a thionyl halide (if the (di)acid halide has not previously been formed), followed by reaction with a halogenating agent, then a primary amine and base, and then with a halogenating agent.

Abstract: A novel crystalline L-carnosine zinc complex is produced by reacting L-carnosine, a zinc salt and an alkali metal compound in an anhydrous or hydrous polar organic solvent.The crystalline L-carnosine zinc complex substantially corresponds to the formula C.sub.9 H.sub.12 N.sub.4 O.sub.3 Zn and has physical properties clearly different from the known amorphous L-carnosine zinc complex.As compared with the amorphous complex, the crystalline complex is very low in impurity, stable to heat and moisture, and easy to filtrate, and has higher anti-ulcer activity.

Abstract: The new compound 3-deazaneplanocin A has been discovered to have potent anti-viral, anti-tumor activity and differentiating activity. A simple method for preparing 3-deazaneplanocin A has been developed involving nucleophilic substitution, which method can also be used to prepare a great variety of carbocyclic nucleosides.

Abstract: A compound of the formula: ##STR1## wherein R is a hydroxyl group which may be protected and Y is a purine base which may be protected, and the saltts thereof, which are useful as an antiviral agent.

Abstract: Dioxazocine derivatives, their preparation and composition containing them, said derivatives being represented by the formula I ##STR1## wherein R.sub.1 represents hydrogen or alkyl having from 1 to 4 carbon atoms,R.sub.2 represents alkyl having from 1 to 4 carbon atoms, andn is equal to 0 or 1,and pharmaceutically acceptable acid addition salts thereof formed with an inorganic or organic acid.Two different reactions are described for making these compounds. They can be formulated into pharmaceutical compositions in the usual manner and exhibit central nervous system affecting activities.

Abstract: The present invention relates to certain amino acid exters of the purine nucleoside acyclovir, pharmaceutically acceptable salts thereof and their use in the treatment of herpes virus infections. The invention also includes pharmaceutical formulations and processes for the preparation of such compounds.

Abstract: Dihydroquinacridones, quinacridones and quinacridonequinones are prepared by cyclizing 2,5-dianilino-3,6-dihydroterephthalic acid derivatives or 2,5-dianilinoterephthalic acid derivatives in the liquid or solid state or in solution, in each case in finely divided form, or in the gas phase, in the presence or absence of an oxidizing agent.

Abstract: The present invention provides tricyclic benzimidazoles of the formula: ##STR1## wherein R.sub.1 is a phenyl radical of the general formula: ##STR2## wherein R.sub.2, R.sub.3 and R.sub.4 can be the same or diferent as in claim 1. For A, B, C and D are understood those compounds where one or two of A, B, C or D are nitrogen. These compounds are useful to inhibit the aggregation of thrombocytes and erythrocytes, lower blood pressure and can increase the power of the heart.

Abstract: The compound of the formula I ##STR1## wherein R, R.sub.3 and R.sub.5 independently represent hydrogen or hydroxy provided that at least one of R, R.sub.3 and R.sub.5 represents hydroxy; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -alkenyl, hydroxy-lower alkyl, optionally substituted cycloalkyl or optionally substituted cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, adamantyl, tetrahydropyranyl, tetrahydrothiopyranyl, tetrahydropyranyl-lower alkyl, tetrahydrothiopyranyl-lower alkyl, adamantyl-lower alkyl, aryl-hydroxy-lower alkyl, aryl, aryl-lower alkyl, aryl-C.sub.3 -C.sub.6 -cycloalkyl, 9-fluorenyl, 9-fluorenyl-lower alkyl or cycloalkenyl-lower alkyl; or R.sub.

Abstract: Antiviral and antitumor compounds are disclosed of general formula: ##STR1## wherein Z is H, OR' or NH.sub.2, wherein R' is H, (C.sub.1 -C.sub.4)-alkyl, aryl, CHO, (C.sub.1 -C.sub.16)alkanoyl or O.dbd.P(OH).sub.2, Y is CH or N, and X is selected from the group consisting of H, N(R.sub.2), SR, OR' or halogen, wherein R is H, lower-(C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically-acceptable salts thereof.

Abstract: A compound for use as a chemiluminescent label in immunoassay comprises an aryl acridinium ester linked to an N-succinimidyl moiety. The compound is conveniently linked to a monoclonal antibody or other protein and is used in a two-site immunoassay for the quantitation of an antigen of interest, by initiation of the luminescent reaction and subsequent measurement of the photonic emission of the immune complex formed during the immunological reaction.

Abstract: The invention relates to N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkylene radical containing from 1 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and capable of bearing a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidzolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each denote a linear or branched alkyl radical containing from 1 to 4 carbon atoms,in the form of a mixture of diastereoisomers or of pure isomers, their N.sup.b' -oxides and their addition salts with a pharmaceutically acceptable inoranic or organic acid.These compounds are antitumor agents.

Abstract: Water-soluble derivatives of camptothecin have the formulae: ##STR1## wherein R' is selected from the group consisting of R=CO CH.sub.2 NH.sub.2.HClR=CO CH.sub.2 NHCH.sub.3.HClR=CO CH.sub.2 NHC.sub.2 H.sub.5.HClR=CO CH.sub.2 N(C.sub.2 H.sub.5).sub.2.HClR=CO CH(NH.sub.2) CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2.2HClR=CO CH(NH.sub.2) CH.sub.2 CH.sub.2 COOH. HClR=CO CH.sub.2 CH.sub.2.COO.sup.- Na.sup.+R=HPO.sub.3.sup.- Na.sup.

Abstract: Insecticidal O-(6-methyl-2-alkyl-pyrimidin-4-yl) O-alkyl thionoalkanephosphonates of the formula ##STR1## in which R stands for methyl or ethyl,R.sup.1 stands for methyl or ethyl andR.sup.2 stands for isopropyl or tert-butyl.

Abstract: As new compounds are now provided 7,7,8,8,-tetramethyl-cis-diaza-bicyclo{4.2.0}octane-3,5,-dione derivatives which have an activity to induce the differentiation of tumor cells and are useful as antitumor agent, and which also have an antiviral activity against various viruses and are useful as antiviral agent. These new derivatives may be produced by a photo-addition reaction of a uracil compound with 2,3-dimethyl-2-butene.

Abstract: A process for the preparation of 2-(arylamino)-3-carboxy-9(10H)-acridones of the formula A ##STR1## in which R and R' represent hydrogen, fluorine, chlorine or bromine atoms, alkyl(C.sub.1 -C.sub.4)-, oxalkyl(C.sub.1 -C.sub.4)- or carbonamide groups and x and y denote integers from 1 to 4, by cyclizing 2,5-diarylaminoterephthalic acids of the formula D ##STR2## in which R, R', x and y have the meanings mentioned previously, in a 5- to 15-fold amount by weight of polyphosphoric acid (P.sub.4 O.sub.10 content 80 to about 85%) or of an acidic polyphosphate (P.sub.4 O.sub.10 contents 75 to about 85%) as a water-abstracting agent at about 60.degree. C. to about 100.degree. C.

Abstract: Compounds which are active against retroviruses have the following formulaHOH.sub.2 C--CH.dbd.C.dbd.CH--Bwherein B is a purine or pyrimidine heterocyclic ring which is preferably selected from the group consisting of cytosine, 5-halo substituted cytosine, 5-alkyl substituted cytosine, 6-aminopurine, 2,6-diaminopurine, 6-hydroxypurine, 2-amino-6-hydroxypurine, 3-deazapurines, 7-deazapurines, 8-azapurines, and 6-azapyrimidines.

Abstract: Antiviral and antitumor compounds are disclosed of general formula: ##STR1## wherein Z is H, OR' or NH.sub.2, wherein R' is H, (C.sub.1 -C.sub.4)alkyl, aryl, CHO, (C.sub.1 -C.sub.16)alkanoyl or O.dbd.P(OH).sub.2, Y is CH or N, and X is selected from the group consisting of H, N(R.sub.2), SR, OR' or halogen, wherein R is H, lower(C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically-acceptable salts thereof.

Abstract: A compound of the formula: ##STR1## A process for its preparation and pharmaceutical compositions comprising the compound or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable diluent or carrier. The compound exhibits analgesic activity.

Abstract: A method for stabilizing compositions containing one or more 3-isothiazolinones, which method includes adding to the 3-isothiazolinone composition an amount effective to stabilize the composition of one or more stabilizing compounds having the formula:[R.sub.x A-C.sub.6 H.sub.2 R.sup.1 R.sup.2 ].sub.y -Zwherein Z is selected from AR.sub.x, R.sup.1, R.sup.2, alkoxymethylene, methylene and alkylidene; R, R.sup.1 and R.sup.2 are independently selected from hydrogen, straight-chained, branched and cyclic alkyl, aryl and arylalkyl; A is oxygen or nitrogen, provided that when A is oxygen, x is 0 or 1, when A is nitrogen, x is 1 or 2; and y is 1 or 2.