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 anti-leukemic and anti-tumor activity.

Abstract: A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a longacting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R.sub.1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.

Abstract: Compounds of the formula (1): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy, andR is lower alkyl, optionally substituted phenyl, --(CH.sub.2).sub.m OR.sup.1 or --NR.sup.1 R.sup.2, wherein m is an integer of 1 to 6 and R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or --NR.sup.1 R.sup.2 taken together is a heterocycle of the formula: ##STR2## wherein A is --CH.sub.2 --, --NR.sup.1 -- or oxygen; or a pharmaceutically acceptable salt thereof, are useful as selective .alpha..sub.2 -blockers.

Abstract: This invention relates to purinone derivatives which have bronchodilator, vasodilator and anti-allergic activities. A compound of the invention is 2-(2-propoxyphenyl)-6-purinone.

Abstract: Oxime ethers of 2,6-dioxabicyclo[3.3.0]octanones of the formula I ##STR1## have pharmacological activity and are especially applicable as drugs for the prophylaxis and therapy of cardiac and circulatory diseases.

Abstract: Vincaminic acid derivatives represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or an alkoxyalkyl group having 2 to 6 carbon atoms, R.sup.2 is a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a halogenated alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, an alkoxycarbonylallyl group having 3 to 8 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, a phenyl group, a phenyl group substituted by alkoxy groups each having 1 or 2 carbon atoms or a thienyl group, A is a hydroxy group, B is a hydrogen atom, or A and B together form a valence bond, and the acid addition salts thereof are disclosed. These compound are useful as thereapeutic effect on cerebovascular injuries.

Abstract: Pesticidally active pyrimidinyl (thiono)(thio)-phosphates of the formula ##STR1## in which R.sup.1 stands for alkoxy,R.sup.2 stands for alkoxy or alkylthio andX stands for oxygen or sulphur,with the proviso that the two radicals R.sup.1 and R.sup.2 are identical when they stand for alkoxy.

Abstract: Arthropodicidally active O-(6-alkoxy-2-tert-butylpyrimidin-4-yl)-O-methyl-thionoethanephosphonic acid diesters of the formula ##STR1## in which R represents alkyl with 1 to 4 carbon atoms or cycloalkyl with 3 or 4 carbon atoms. The intermediate where R is replaced by H is also new.

Abstract: The invention relates to a process for preparing a 2-alkyl-1,4,5,6-tetrahydropyrimidine with the formula ##STR1## where R represents a straight or branched chain with 1-8 C-atoms or a phenyl group from 1,3-diaminopropane and an alkanecarboxylic acid, in which the alkyl group of such an acid is the same as the R group described above, wherein the starting materials are reacted in the gas phase in the presence of an oxide catalyst at a temperature of between 250.degree. and 450.degree. C. and from the reaction mixture thus obtained the 2-alkyl-1,4,5,6-tetrahydropyrimidine is recovered.

Abstract: Compounds are described of the formula ##STR1## where: R.sup.1 is --H or --CH.sub.3,n is 1, m is 2-4 and X is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;Y is a saturated heterocyclic amino group,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thineylalkyl or naphthylalkyl or (ii) cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formualted for use as antithrombotic or antiasthmatic agents.

Abstract: A process for recovering from caffeine-loaded activated carbon by treatment f the loaded carbon with an acid. According to the present invention, activated carbon is treated with a compound having the formula ##STR1## wherein R.sub.1 is methyl, H or Cl, and R.sub.2 is Cl, OH or phenyl.

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: Novel compositions are prepared by reacting hydrocarbyl substituted nitrogen-containing aromatic heterocyclic compounds such as 2,5-dimethylpyridine or 2,4,6-collidine, an aldehyde such as formaldehyde, or a ketone such as acetone, or mixtures thereof and an amine having a combined total of at least seven carbon, nitrogen, oxygen or sulfur atoms and at least one reactive amine hydrogen atom such as 1-dodecanamine in the presence of a suitable catalyst such as hydrogen chloride. These novel compositions, as well as their free amine forms are useful as oil and gas well corrosion inhibitors.

Abstract: Aromatically substituted azacycloalkylalkanediphosphonic acids of the formula ##STR1## in which R represents an aromatically substituted azacycloaliphatyl radical that is bonded to the group alk by way of a nitrogen atom and that optionally contains an additional nitrogen atom, and alk represents a divalent aliphatic radical, and their salts, can be used for the treatment of illnesses that can be attributed to calcium metabolism disorders. They are manufactured, for example, by reacting a compound of the formulaR--alk--X.sub.3 (IV)in which X.sub.3 represents carboxy, carbamoyl or cyano, with phosphorus acid and phosphorus trichloride and in an intermediate of the formula ##STR2## obtained by starting from compounds of the formula IV in which X.sub.3 represents cyano or carbamoyl and by working up by hydrolysis, or in a salt thereof, replacing the amino group by hydroxy by treatment with nitrous acid.

Abstract: Novel alkaloid compounds that are derivatives of methaniminoetheno[d,e]acridine are derived from marine sponges of the genus Dercitus. These compounds and pharmaceutical compositions containing therapeutic effective amounts thereof are useful as antitumor and immunomodulatory medications.

Abstract: New derivatives of theophylline are described, which have the general formula: ##STR1## in which R is selected from the group consisting of 2'-(1'-oxy-1', 3'-dithiolanyl), 2'-(1', 3'-dithiolanyl) and 2'-(1',3'-dithianyl), possibly substituted in position 4'. The derivatives have high antibronchospastic, antitussive and mucolytic activities.

Abstract: New heterocyclic compounds having the general formula ##STR1## wherein ##STR2## wherein R' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;R.sup.4 is C.sub.1-6 -alkyl;--S-- is ##STR3## and wherein R.sup.5 and R.sup.6 independently are hydrogen, C.sub.1-6 -alkyl, or aryl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and in improving the cognitive function of the brain of mammals.

Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.

Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a C.sub.8-13 fused heterotricyclic ring system containing at least two aromatic rings and no more than 3 heteroatoms (in separate rings), or a C.sub.10-17 fused heterotetracyclic ring system containing at least two aromatic rings and no more than 4 heteroatoms (in separate rings) or a C.sub.

Abstract: A series of novel alkanesulphonamidophenyl-N-alkyl-N-(heterocyclic-alkyl)alkylamine derivatives have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic moiety is a 5- or 6-membered nitrogen-containing heterocyclic group which is attached to the adjacent carbon atom by a carbon or nitrogen atom and optionally contains a further heteroatom selected from oxygen and nitrogen, said nitrogen-containing heterocyclic group being either (i) substituted by a phenyl or benzyl group or (ii) fused at two adjacent carbon atoms to a benzene ring, with the resulting heterocyclic ring moiety also being optionally substituted. These particular compounds are useful in therapy as highly effective anti-arrhythmic agents and therefore, are of value in the treatment of various cardiac arrythmias. The most preferred member compound of the series is 2-hydroxy-2-(4-methanesulphonamidophenyl)-N-methyl-N-[2-(6-chloro-2H-isoin dolin-1-on-2-yl)ethyl]ethylamine.