Abstract: A method for synthesizing camptothecin and camptothecin analogs using a novel hydroxyl-containing tricyclic intermediate and the camptothecin analogs produced by the process. The camptothecin analogs are effective inhibitors of topoisomerase I and show antileukemic and anti-tumor activity.

Abstract: This invention pertains to novel methods of synthesizing fludarabine, fludarabine phosphate and related nucleoside pharmacologic agents utilizing 6-azido-2-fluoropurine as a novel intermediate.In particular this invention pertains to a synthesis of fludarabine where the relatively low yield fluorination step is done before the costly coupling step.

Abstract: A process for the N-arylation of isatins with organo bismuth reagents is disclosed.

Abstract: This invention relates to new nucleotide analogues and solves the technical problem of their use as biologically active compounds. The subject of this invention are N-(2-phosphonylmethoxyethyl) and N-(3-hydroxy-2-phosphonylmethoxypropyl) derivatives of pyrimidine and purine bases, easily accessible from heterocyclic bases andd their N-(2-hydroxyethyl) or N-(2,3-dihydroxypropyl) derivatives. Some of the compounds, according to this invention, exhibit a marked antiviral activity or can be converted into such active compounds by chemical transformations.

Abstract: 17.beta.-Acyl-4-aza-5.alpha.-androst-1-in-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl R.sup.2 is methoxy, a monovalent radical selected from straight and branched chain alkyl of from 1-12 carbons, or monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents, aralkyl selected from benzyl and phenethyl and heterocyclic selected from 2- or 4-pyridyl, 2-pyrrolyl, 2-furyl or thiophenyl; and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulations of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, and benign prostatic hypertrophy.

Abstract: Isomeric derivatives of 2',3'-dideoxyadenosine and 2',3'-dideoxyguanosine wherein the adenine or guanine base is attached to the 1' position of the iso-dideoxysugar residue by the 9-N position, the novel intermediates used in the synthesis of these compounds, and a method for treating a subject infected with a retrovirus by administering the compounds of the invention.

Abstract: 17.beta.-Acyl-4-aza-5.alpha.-Androst-1-end-3-ones of the formula: ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.3 is cycloalkyl of from 4-8 carbons;and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, androgenic alopecia, prostatic carcinoma and benign prostatic hypertrophy.

Abstract: Square-planar four-coordinate complexes of cis-platinum (II) with neutral bidentate aminoalkyl-substituted cycloalkylamine ligands and bromo-, chloro-, iodo-, nitrato-, oxalato-, or malanato-ligands possess antimicrobial activity as well as activity against transplanted L1210 and P388 murine leukemia cell lines.

Abstract: 3,17-(diethoxycarbonyl)normorphine, which may be prepared by reaction of morphine with ethyl chloroformate, is converted to 3,17-(diethoxycarbonyl)normorphinone, a novel compound, by oxidation. The novel normorphinone derivative is converted to 3,17-(diethoxycarbonyl)normorphinone enol acetate, a second novel compound, by esterification with acetic anhydride or acetyl halide.A 14-hydroxy group is introduced into the novel dienol ester by oxidation with peracid. The resultant 14-hydroxy-3,17-(diethoxycarbonyl)normorphinone, a third novel compound, may be catalytically hydrogenated to produce 3,17-(diethoxycarbonyl)noroxymorphone. The latter intermediate may be converted to noroxymorphone by hydrolysis.

Abstract: Water-soluble triphendioxazine compounds of the formula (1) with quaternary ammonium groups ##STR1## in which the substituents are defined in claim 1. The compounds (1) have fiber-reactive dyestuff properties and dye, for example, cellulose fiber materials, wool and synthetic polyamide in deep, fast shades.

Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or a methyl group, each of R.sup.2 and R.sup.3 which may be the same or different, is a hydrogen atom or a lower alkyl group, or R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a heterocyclic group selected from the group consisting of an aziridinyl group, an azetidinyl group, a pyrrolidinyl group, a piperidino group, a piperazinyl group and a morpholino group, A is a carbonyl group or a single bond, and n is an integer of from 0 to 3; or a pharmaceutically acceptable salt or ester thereof.

Abstract: A process is described for the preparation of carbocyclic guanosine from aristeromycin in a multi-step procedure, the final step of which is the hydrolysis of a compound of the formula ##STR1## wherein R.sup.1 represents a C.sub.1-6 alkyl group or an arylC.sub.1-4 alkyl group and R.sup.2, R.sup.3 and R.sup.4 each independently represent a hydrogen atom or a hydroxyl protecting group.Carbocyclic guanosine is an intermediate in the synthesis of carbocyclic analogues of nucleosides having use in therapy, particularly as antiviral agents.

Abstract: This invention relates to N-heteroalkyl-substituted 1-aryloxy-2-propanolamine and proplyamine derivatives possessing anti-arrhythmic activity, to pharmaceutical compositions and to method for production thereof.

Abstract: This invention relates to phenylpurinone derivatives which have bronchodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxy-5-chlorophenyl)purin-6-one.

Abstract: A process for the preparation of a compound of formula (I): ##STR1## which process comprises the reduction of a compound of formula (II): ##STR2## by catalytic hydrogenation using palladium on charcoal as catalyst.

Abstract: There are disclosed certain 6-piperazinopurines and heteroaromatic derivatives thereof which have oral hypoglycemic acitivity and with such ability to lower blood sugar are useful in the treatment of type II diabetes and/or obesity with associated insulin resistance. Processes for the preparation of such compounds and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 whereinR.sub.7 is C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-2 alkyl either of which phenyl moieties may be substituted by one or two substituents selected from halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sub.2 amino or, when R.sub.1 is hydroxy or amino, R.sub.2 may also be hydrogen;X is --CH.sub.2 CH.sub.2 -- or a moiety of structure (a), (b) or (c): ##STR2## wherein n is 1 or 2;m is 0, 1 or 2; andR.sub.3 is hydrogen or acyl;R.sub.4 is a group of formula: ##STR3## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; having antiviral activity, processes for their preparation and their use as pharmaceuticals.

Abstract: The invention relates to a method of producing 20(S)-comptothecin, 20(R)-camptothecin and analogs thereof. The method involves the resolution of an mixture of enantiomers of an intermediate lactone.

Abstract: 17.beta.-Acyl-4-aza-5.alpha.-androst-1-ene-3-ones of the formula ##STR1## wherein R is selected from hydrogen, methyl and ethyl andR.sup.2 is monocyclic aryl optionally containing 1 or more lower alkyl substituents of from 1-2 carbon atoms and/or 1 or more halo (Cl or Br) substituents;and R', R" and R'" are each selected from hydrogen and methyl and pharmaceutical formulation of the above compounds are active as testosterone 5.alpha.-reductase inhibitors and thus are useful for treatment of acne, seborrhea, female hirsutism, androgenic alopecia, prostatic carcinoma and benign prostatic hypertrophy.

Abstract: The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmaceutical formulations and processes for the preparation of compounds according to the invention.