Abstract: The present invention provides pyrazolo[3,4-d]-pyrimidines of the general formula: ##STR1## wherein R.sub.1 is a C.sub.1 to C.sub.6 -alkyl radical, a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aryl radical, R.sub.2 is a C.sub.2 to C.sub.6 -alkenyl radical, a C.sub.3 to C.sub.7 -cycloalkyl radical or an aralkyl or hetaralkyl radical with 1 to 6 carbon atoms in the alkyl moiety and substituted, if desired, one or more times by halogen, C.sub.1 to C.sub.6 -alkyl, hydroxyl, C.sub.1 to C.sub.6 -alkoxy, C.sub.1 to C.sub.3 -haloalkyl, C.sub.3 to C.sub.7 -alkoxy carbonyl, aminocarbonyl, C.sub.2 to C.sub.7 -alkylaminocarbonyl, C.sub.3 to C.sub.13 -dialkylaminocarbonyl, cyano or C.sub.1 to C.sub.6 -alkylthio and R.sub.3 is a hydrogen atom or a C.sub.2 to C.sub.6 -alkyl radical substituted, if desired, one or more times by hydroxyl or is a tetrahydrofuranyl or tetrahydropyranyl radical, with the proviso that R.sub.2 cannot be an unsubstituted benzyl radical when R.sub.

Abstract: Novel compounds selected from the group consisting of all possible racemic or optically active forms of compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 5 carbon atoms, -OH, -CF.sub.3 and -NO.sub.2 and ##STR2## is selected from the group consisting of ##STR3## and their non-toxic, pharmaceutically acceptable acid addition salts having a very good analgesic activity as well as antidepressive, neuronal protective, anti-anoxic, anti-ischemic and no-otropic activities.

Abstract: N-(Substituted-phenyl)-5-fluoromethyl-1,2,4-triazolo[1,5-a]pyrimidine-2-sul fonamides are prepared from 2-benzylthio-5-fluoromethyl-1,2,4-traizolo[1,5-a]pyrimidines and found to to be herbicidal. The compounds, illustrated by 5-fluoromethyl-7-methoxy-(2,6-dichloro-3-methylphenyl)-1,2,4-triazolo[1,5- a]pyrimidine-2-sulfonamide, are degradable in the soil.

Abstract: Insecticidal 1,2,3,4-tetrahydro-5-nitropyrimidines of the formula ##STR1## in which R.sup.1 stands for hydrogen or for optionally substituted radicals from the group consisting of benzyl, picolyl (pyridylmethyl) and phenoxyalkyl,n stands for the number 0 or 1 andR.sup.2 stands for the --A--R.sup.3 group, in whichA stands for a direct bond or for the --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.x --Y--(CH.sub.2).sub.z -- groupings, wherem stands for the numbers 1 to 4,x and z stand for the numbers 0, 1 or 2, it being possible for x and z to be identical or different, andY stands for oxygen, sulphur or for the --NH-- or ##STR2## groupings, whereR.sup.4 stands for optionally alkoxycarbonyl-substituted C.sub.1 -C.sub.4 -alkyl, cyano, hydroxyl or for phenyl, andR.sup.3 stands for halogeno-C.sub.1 -C.sub.

Abstract: Insecticidal 1,2,3,4-tetrahydro-5-nitro-pyrimidine derivatives of the formula ##STR1## in which n is 0 or 1,A is a direct bond, --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.x --Y--(CH.sub.2).sub.z,m is a number from 1 to 4,x and z each independently is 0, 1 or 2,Y is oxygen, sulphur, --NH-- or ##STR2## R.sup.2 is optionally alkoxycarbonyl-substituted C.sub.1 -C.sub.4 -alkyl, or cyano, hydroxyl or phenyl, andR.sup.1 is halogeno-C.sub.1 -C.sub.4 -alkyl or an optionally substituted radical from the group consisting of phenyl, naphthyl, anthryl, phenanthryl, pyridyl, furyl, thienyl, piperidyl and 1,3-benzodioxolyl,and their acid addition salts.

Abstract: Novel aminopropanol derivatives of 1,4:3,6-dianhydro-hexitol nitrates of the general formula I ##STR1## in which X has the meaning given in the specification, processes for their preparation and their use in preventing and treating angina pectoris, systemic hypertension and pulmonary hypertension in mammals.

Abstract: Derivatives of N-[2-(5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-6-yl)-alkyl]benzoyl-L-glut amic acid are antineoplastic agents. A typical embodiment is N-(2-fluoro-4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido-[2,3-d]pyrimi din-6-yl)ethyl]benzoyl)-L-glutamic acid.

Abstract: Carboxamides represented by the formula (I): ##STR1## wherein Z represents the carbon atoms necessary to complete a 5- to 7-membered ring,R.sup.1, R.sup.2, and R.sup.3 may be the same or different and are selected from the group consisting of a hydrogen atom, a lower alkyl group, a cycloalkyl group, a halogen atom, an amino group, a lower alkylamino group, an alkoxy group, an acylamido group, a sulfonamido group, and a nitro group; andA represents an aminoalkyl moiety and acid addition salts thereof.

Abstract: This disclosure describes novel 4,8-disubstituted-1,2-dihydro- and -1,2,3,4-tetrahydro -imidazo-[1,5-a] pyrimidines useful as antihypertensive agents and/or as anxiolytic agents in mammals and as intermediates for the synthesis of biologically active compounds.

Abstract: A method of inhibiting the replication of tumor cells is disclosed wherein Novel bis (2,2-dimethyl-1-aziridinyl)phosphinic amide antineoplastic agents of the formula: ##STR1## wherein X is R and R' are each, independently, hydrogen, alkyl, substituted alkyl, phenyl and substituted phenyl, Y is alkyl or substituted alkyl of 1-10 carbon atoms and, Z is oxygen or sulfur is administered to tumor cells.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or phenyl unsubstituted or substituted by one or two halo moieties, R.sup.2 is hydrogen or alkyl, A CX wherein X is halo, B is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.

Abstract: N-(Thienylcarbonyl)glutamic acid and N-(furylcarbonyl)glutamic acid derivatives in which the thienyl or furyl group is substituted with the 2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-ylethyl or 2,4-diamino-5,6,7,8-tetrahydropyrido[2,3-d]-pyrimidin-6-ylethyl group are antineoplastic agents. Typical embodiments are N-[5-(2-{2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl}e thyl)thien-2-ylcarbonyl]-L-glutamic acid and N-[5-(2-{2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl}e thyl)fur-2-ylcarbony]-L-glutamic acid.

Abstract: A pharmaceutically efficacious pteridine compound of formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, trifluoromethyl, nitro, a --(A).sub.n --OR.sub.3 group, wherein R.sub.3 is hydrogen or a C.sub.1-6 alkyl group, a --(A).sub.n --NR.sub.4 R.sub.5 group, wherein R.sub.4 and R.sub.5 independently of each other are hydrogen or a C.sub.1-6 alkyl group or R.sub.4 and R.sub.5 together with the nitrogen atom form a 5- or 6-membered ring that is substituted with a C.sub.1-4 alkyl group and wherein A is a linking group having 1 to 6 linking carbon atoms, one of which can be replaced by oxygen and wherein n is zero or one, and wherein R.sub.2 is hydrogen or, independently of R.sub.1, has the same meaning as R.sub.1, with the proviso that R.sub.1 and R.sub.2 are not simultaneously hydrogen, and the physiologically acceptable acid addition salts thereof.

Abstract: Triazolopyrimidines of the formula I ##STR1## in which R.sup.1 denotes CN, alkylsulphonyl, arylsulphonyl or arylR.sup.2 denotes H, alkyl or alkythio,R.sup.3 denotes alkyl, aralkyl, substituted aralkyl, alkenyl or alkynyl,R.sup.4 denotes alkyl, aralkyl or aryl, andR.sup.5 denotes alkyl, aralkyl or aryl, orR.sup.4 and R.sup.5, together with the carbon atom, denote a carbocyclic 5-, 6- or 7-membered ring which may be substituted or bridged,in which R.sup.4 cannot be methyl or aryl when R.sup.1 represents CN, R.sup.2 represents H, R.sup.3 represents methyl and R.sup.5 represents methyl or aryl, and in which alkyl preferably has 1-9 C atoms and aryl preferably has 6-12 C atoms, and also a process for their preparation, and their use as initiators.

Abstract: A novel process is described for preparing azetidine and 2 or 3 methyl and ethyl azetidine free bases by reacting primary arylmethylamine having suitable bulk providing substituents attached to the methyl carbon and an appropriate propane derivative having leaving groups in the one and three position in hot organic solvent containing a non-nucleophilic base and an amount of water sufficient to promote azetidine ring formation to give N-protected-azetidines and deprotecting by hydrogenolysis under acidic conditions to give an acid salt of the azetidines and thereafter flashing off vaporized azetidine from a hot, agitated strong base solution or slurry and condensing to give the liquid azetidine free bases.

Abstract: Spiro(bis)indane bis-oxyphthalic acid bisimides are prepared by the reaction of a nitro- or halo-substituted phthalimide with a salt of a 6,6'-dihydroxy-3,3,3'3'-tetramethylspiro(bis)indane. The bisimides may be converted to the corresponding dianhydrides, which react with diamines to form polyetherimides, or to the free tetracarboxylic acids or their salts, esters or amides.

Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sub.1 is alkyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl;Y.sub.1 is cycloalkyl, aryl, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2)).sub.m --S--, ##STR4## amino or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.

Abstract: The invention relates to the new (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2, 3,4,6,7,12,12b.alpha.-octa-hydroindolo[2,3-a] quinolizine of the formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of the compound of formula (I) and acid addition salts thereof by resolution of the corresponding racemic compound and optionally by subsequent hydrolysis and/or salt formation.The compound of formula (I) shows a remarkable peripheral vasodilating and antihypoxial activity. Pharmaceutical compositions comprising it as active ingredient are also within the scope of the invention.