Abstract: Certain open chain purine nucleoside phosphonate derivatives have antiviral activity against the Herpes group of viruses, and also show effective antiviral activity against retroviruses, including human immunodeficiency virus (HIV). These compounds have the formula ##STR1## wherein B represents a substituted or unsubstituted purine base, especially adenine or guanine and their halogenated derivatives. R1 is selected from H, methyl, hydroxymethyl, halomethyl, azidomethyl, and cyano; R2 is selected from H, methyl, hydroxymethyl, halomethyl, azidomethyl, cyano, and OH; also when R2 is OH the carbon to which it is attached may be oxidized so that the H there shown and R2 together may be =0; and n is an integer of 0-5. The compounds of the invention further include the pharmaceutically acceptable mono and dibasic salts and the mono- and diesters of the phosphonate moiety and the acid addition salts of the murine-substituted purines. In addition, when R1 or R2 is --CH.sub.

Abstract: The present invention relates to the synthesis of dimer alkaloid compounds, particularly those of the Catharantus (Vinca) family, from an indole unit, such as cantharanthine, and a dihydroindole unit, such as vindoline. A multi-step process is disclosed including the steps of (1) of 1,4-reduction of a first dimeric iminium intermediate to an enamine compound by reaction with a 1,4-dihydropyridine compound; (2) oxidative transformation of the resulting enamine to a second iminium intermediate under controlled aeration; (3) reduction of the second iminium intermediate to form the target dimer alkaloid compounds. The entire process can be conducted in a one-pot operation to obtain the target compounds without isolation of the intermediates.

Abstract: A novel compound represented by the formula (I) ##STR1## wherein R represents a lower alkyl group having 1 to 4 carbon atoms which has an intense microbicidal activity over a wide range of microorganisms and is applicable to a microbicide.

Abstract: Derivatives of 4-desacetyl VLB C-3 carboxhydrazide, active anti-tumor agents and useful as intermediates for active anti-tumor conjugates.

Abstract: Cyclic imide derivatives of 4-desacetyl VLB C-3 carboxydrazide, active anti-tumor agents.

Abstract: This invention relates to oxetanocin-related compounds represented by the following formula (I): ##STR1## [in formula (I), R.sub.1, Y and B have the following meanings: (a) R.sub.1 represents --CH.sub.2 OH or --CH.sub.2 OCO-(alkyl),(b) Y represents ##STR2## provided that R.sub.2 is --H, --OH or --CH.sub.2 OH and R.sub.3 is --H, --OH, halogen atom, --CH.sub.2 OH, lower alkyl group, --CH.sub.2 -N.sub.3, --CH.sub.2 -F, --N.sub.3, --COOH, --NH.sub.2, --CH.sub.2 OSO.sub.3 H or --CH.sub.2 OCO-(lower alkyl), and(c) B represents a residue of purine base,(d) provided that R.sub.1 and R.sub.3 cannot simultaneously represents --CH.sub.2 OH]and their salts which have activities such as an antiviral activity and the like and are expectedly useful as a pharmaceutical and the like.

Abstract: There are provided novel 2-substituted-4-substituted-1,3-dioxolanes which are particularly useful as antiviral agents.

Abstract: There are disclosed novel compounds having the formula, ##STR1## wherein, m is an integer of 0-3;n is an integer of 1-4;R.sub.1 is hydrogen, alkyl, cycloalkyl, arylloweralkyl, aryl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; each R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or alternatively R.sub.2 and R.sub.3 taken together form a methylene or ethylene bridge;X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy, nitro, trifluoromethyl, formyl, loweralkoxycarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.4 or --NR.sub.5 R.sub.6, R.sub.4 being hydrogen or loweralkyl, and R.sub.5 and R.sub.6 being independently hydrogen, loweralkyl or cycloalkyl;Y is CH.sub.2, CH.dbd.CH, O, S or NR.sub.7, R.sub.7 being hydrogen, loweralkyl or arylloweralkyl; with the proviso that the number of said methylene or ethylene bridge shall not exceed 1 and that when Y is CH.sub.2, one and only one combination of R.sub.2 and R.sub.

Abstract: This invention concerns a method for the production of dimeric alkaloids, characterized by reacting of catharanthine with vindoline in the presence of Fe.sup.3+ and (1) removing or inactivating the Fe.sup.3+ and allowing the reaction product to react with a reducing agent or (2) allowing presence of oxygen and a dicarboxylic acid or a derivative thereof in the reaction system and allowing the reaction product to react with a hydride source.In accordance with this invention, such dimeric alkaloid as vinblastine, leurosidin, and 3',4'-anhydrovinblastine which are useful as antineoplastic drugs can be produced in high yields.

Abstract: In a process for the production of a thiophosphoric acid ester of formula I ##STR1## wherein R.sub.1 is lower alkyl, lower alkenyl, lower alkoxy(lower)alkyl or lower alkylmercapto(lower)alkyl, R.sub.2 is hydrogen, lower alkyl or lower alkenyl and R.sub.3 and R.sub.4 are lower alkyl, which comprises reacting a dialkyl phosphoric acid halide of formula II ##STR2## wherein Hal is chlorine or bromine and R.sub.3 and R.sub.4 are as defined hereinabove, with a hydroxypyrimidine of formula III ##STR3## wherein R.sub.1 and R.sub.2 have the significance given to them above, at elevated temperatures and in the presence of an organic solvent and an acid-binding agent, the improvement which comprises adding the reactant of formula II to an essentially dry mixture of the hydroxypyrimidine of formula III and the acid-binding agent in the presence of a low molecular weight water-insoluble aliphatic or cycloaliphatic ketone as organic solvent after removing the water of reaction from said mixture.

Abstract: The disclosure is directed to a compound which is a reaction product of at least one phosphonic acid group of an alpha-aminomethylene phosphonic acid containing at least one group corresponding to the formula, ##STR1## with an epoxy group of a compound containing at least one epoxy group. The disclosure is also directed to waterborne coating compositions, organic solvent-borne coating compositions, and powder coating compositions containing the aforesaid reaction product.

Abstract: This invention concerns a new process for the catalytic carbonylation of certain aryl halides or aryl tosylates to amides by use of a complex of palladium and at least one ligand. More specifically, the invention concerns carbonylation of halogenoaromaticsulfonamides or tosylatoaromaticsulfonamides to saccharin, saccharin analogues or their salts.

Abstract: 1,3-Alkyl substituted-8-phenylxanthines in which the straight chain alkyl substituents are different and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds have 1-n-propyl-3-methyl and 1-methyl-3-n-propyl substituents. The compounds are potent bronchodilators.

Abstract: The invention relates to .DELTA..sup.4 -androstene derivatives with aromatase-inhibiting activity having the formula: ##STR1## wherein R.sub.1 =O, (.alpha.R.sub.5,.beta.H) or N--O--R.sub.6 ;R.sub.2 =H, (1-12C)hydrocarbon radical, --SH, --S--(1-12C)-hydrocarbon radical or (1-12C)acyl;R.sub.3 =O or (.alpha.R.sub.7,.beta.R.sub.8);R.sub.4 =H or (1-12C)hydrocarbon radical;R.sub.5 =OH, O--(1-12C)hydrocarbon radical or O--(1-12C)acyl;R.sub.6 =H or (1-12C)hydrocarbon radical;R.sub.7 =H or (1-12C)hydrocarbon radical; andR.sub.8 =OH, O--(1-12C)acyl or O--(1-12C)hydrocarbon radical with the proviso that R.sub.1 is not O if R.sub.4 is H.

Abstract: Pyrazolo[5,1-b]quinazolones are prepared by reacting isatoic anhydrides with pyrazolones at from 100.degree. to 180.degree. C. in an inert organic solvent with simultaneous azeotropic removal of the water formed in the course of the reaction.

Abstract: Compounds of the formula ##STR1## (wherein Ar, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and m have the meanings given in the description), their preparation and pharmaceutical compositions containing them.The compounds of formula I are active on the cardiovascular system as antivasospastics, antiangina pectoris agents, antihypertensives and vasodilators.

Abstract: 6-Substituted purinyl piperazine derivatives and a method of synthesis for the derivatives are described. The 6-substituted purinyl piperazine derivatives are useful as cardiotonic agents and antiarrhythmic agents.

Abstract: This invention relates to a N-heteroaryl-purin-6-amine of the formula ##STR1## where R.sub.1 is hydrogen, lower alkyl, and arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, lower alkyl or R.sub.2 and R.sub.3 taken together are aryl; R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, or R.sub.4 and R.sub.5 taken together are aryl; R.sub.6 is hydrogen, lower alkyl, aryl, arylloweralkyl, ##STR2## where R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined above, and the pharmaceutically acceptable acid addition salts thereof and where applicable the geometric and optical isomers and racemic mixtures thereof. The compounds of this invention display utility as analgesic and anticonvulsant agents.

Abstract: A process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## which process comprises reacting a compound of formula (II): ##STR2## wherein the amino group is optionally protected, Y is iodo, optionally substituted benzylthio or (phenacylmethyl)thio, with a compound of formula (III): ##STR3## wherein Q is a leaving group, R.sub.x and R.sub.y are protected hydroxymethyl or acyloxymethyl, or group(s) convertible to hydroxymethyl or acyloxymethyl; and R.sub.z is hydrogen or a group convertible thereto; and thereafter converting Y to X is hydroxy by means of hydrolysis, or to X is hydrogen by means of reduction; converting R.sub.x and R.sub.y when other than hydroxymethyl or acyloxymethyl, to hydroxymethyl or acyloxymethyl, optionally converting R.sub.x /R.sub.y hydroxymethyl to acyloxymethyl or vice versa, deprotecting the 2-amino group where necessary and converting R.sub.

Abstract: Cyclopentyl purine derivatives, novel intermediate thereof and processes for their preparation are disclosed.