Abstract: Compounds of formulas (1) and (2): ##STR1## in which: X and Y are independently hydrogen, hydroxy, lower alkyl, lower alkoxy or halo, or X and Y taken together is methylenendioxy 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 .alpha..sub.2 -blockers, especially as antidepressants.

Abstract: A medicament for curing arteriosclerosis which comprises pyrimido [2,1-b] benzothiazole derivative.

Abstract: The invention relates to a novel 3-acylaminobenzisothiazole-S,S-dioxide of formula I ##STR1## to the preparation thereof, to insecticidal compositions containing said compound and to the use thereof for controlling insects, in particular plant-destructive sucking insects.

Abstract: Benzimidazolo-quinazolines of the general formula ##STR1## in which Y denotes a radical of the formula ##STR2## Y.sub.1 denotes hydrogen or alkyl, X and X.sub.1, independently of one another, denote hydrogen, alkyl, cycloalkyl, aryl or aralkyl, orX and X.sub.1, together with the nitrogen atom connecting them, denote a 5- or 6-membered ring,X.sub.2 denotes hydrogen, halogen, alkyl, alkoxy or alkoxycarbonyl,X.sub.3 denotes hydrogen, alkyl or aryl,X.sub.4 denotes hydrogen, cyano, halogen, alkyl or alkoxy,Z denotes hydrogen, alkyl, cycloalkyl or aralkyl,D denotes an optionally hydrogenated 5- or 6-membered ring, andm and n, independently of one another, denote 0 or 1,in which a double bond is in the positions labelled with 1 and 2 when m=0 and a single bond is in these positions when m=1, andin which the rings A, B and D are the radicals X, X.sub.1, X.sub.2, X.sub.3, X.sub.

Abstract: Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.

Abstract: A compound represented by the following formula ##STR1## wherein A represents a hydrogen atom or a lower alkanoyl group, Z represents an oxygen atom or the group ##STR2## in which R represents a hydrogen atom or a lower alkyl group, and X represents a halogen atom, the compound being useful for controlling androgen-dependent diseases, particularly for preventing prostatic hypertrophy.

Abstract: An organic carbonate such as dimethyl carbonate is prepared by reacting an alcohol such as methanol and carbon monoxide in the presence of a catalyst system containing Cu(OMe)Cl as catalyst and boron trifluoride, calcium chloride, benzyltriethylammonium chloride, etc. as promoters.

Abstract: Novel compounds of the general formula I ##STR1## where X and Y independently of one another are each carboxyl, a carboxylic ester group, cyano or an unsubstituted or substituted carbamyl or carboxylic hydrazide group and X and Y together form a radical of the formula ##STR2## where R.sup.1 is hydrogen or a radical of a primary amine and R.sup.2 and R.sup.3 are each hydrogen or unsubstituted or substituted alkyl, cycloalkyl or aryl, are very useful as diazo components.

Abstract: A series of novel heterocyclic-substituted 1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one compounds have been prepared, including their pharmaceutically acceptable salts, wherein the heterocyclic ring moiety is an optionally substituted 5- or 6-membered aromatic heterocyclic group attached to the 6-, 7-, 8- or 9-positions of the aforesaid tetrahydroquinaxolinone ring. These particular compounds are useful in therapy as highly potent inotropic and therefore, are of value in the treatment of various cardiac conditions. Preferred member compounds include 7-(2,4-dimethylimidaxol-1-yl)-9-methyl-1,2,4,5,-tetrahydroimidazo (2,1-b)quinazolin-2-(1H)-one, 3,9-dimethyl-7-(2,4-dimethylimidazol-1-yl) -1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-one and 9-methyl-7 -(1,2,4-triazol-4-yl)-1,2,3,5-tetrahydroimidazo(2,1-b)quinazolin-2-(1H)-on e, respectively. Methods for preparing these compounds from known starting materials are provided.

Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl or a mono- or bicyclic aryl or heteroaryl radical, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino, X represents--CH.sub.2 CR.sup.3 R.sup.4 CH.sub.2 --or --(CH.sub.2).sub.4 --where R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl or R.sup.3 and R.sup.4 together with the carbon atom to which they are attached represent a 5, 6 or 7 membered carbocyclic ring and R.sup.5 represents acyl and R.sup.6 represents hydrogen or R.sup.5 and R.sup.6 each independently represent hydrogen or lower alkyl, are useful as hypoglycaemics.

Abstract: Alkaloid dimers are formed by coupling vindoline and catharanthine in the presence of ferric ion. The predominant products are 3',4'-anhydrovinblastine and vinblastine when reaction conditions are selected appropriately.

Abstract: Fluorinated derivatives 3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoro-17-methylmorphinan ("fluorooxymorphone"; FOXY, compound 10) and 17-cyclopropylmethyl-3,14-dihydroxy-4,5.alpha.-epoxy-6.beta.-fluoromorphin an (CYCLOFOXY, compound 18) are prepared based upon the structures of the potent opioid agonist oxymorphone 4 and the antagonist naltrexone 11, respectively. Fluorine was introduced in the final stages of synthesis by a facile nucleophilic displacement with fluoride ion of the 6.alpha.-triflate functions in 8 and 16. The synthetic procedures were suitable for the production of the corresponding positron emitting .sup.18 F-labeled analogs .sup.18 F-FOXY and .sup.18 F-CYCLOFOXY, which are useful for in vivo studies of the opioid receptor system using positron emission transaxial tomography. In addition, the tritiation of FOXY (10) to high specific activity is noted.

Abstract: The invention provides a process for the preparation of pyrimidine, 2-methyl- and/or 2-ethylpyrimidine, characterized in that for pyrimidine a nitrogen reactant, chosen from the reaction product of formamide with 1,3-diaminopropane in the liquid phase, 1-amino-3-formamidopropane, 1,4,5,6-tetrahydropyrimidine and/or 1,3-diformamidopropane, that for 2-methylpyrimidine 1-amino-3-acetamidopropane, 2-methyl-1,4,5,6-tetrahydropyrimidine and/or 1,3-diacetamidopropane, and that for 2-ethylpyrimidine 1-amino-3-propionamidopropane, 2-ethyl-1,4,5,6-tetrahydropyrimidine and/or 1,3-dipropionamidopropane is/are contacted with a palladium-containing catalyst, this being effected in the gas phase at a temperature between 200.degree. and 550.degree. C. and in the presence of a carbon monoxide-hydrogen reactant, and that pyrimidine, 2-methyl-and/or 2-ethyl-pyrimidine is recovered from the reaction mixture obtained.

Abstract: The present invention relates to new derivatives selected from the group comprising:(i) the 5-phenylhydropyrimidines of the formula: ##STR1## in which: X.sub.1 and X.sub.2, which are identical or different, each represent H, F, Cl, Br or CF.sub.3, andA represents a polyhydropyrimidinyl group of the structure: ##STR2## in which: Y represents H or OH,R.sub.a represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.2 -C.sub.5 alkanoyl group, it being possible for R.sub.a to represent the hydrogen atom when at least one of the groups X.sub.1, X.sub.2 and Y is different from H,R.sub.b represents a C.sub.1 -C.sub.3 alkyl group, andR.sub.c.sup.1 and R.sub.c.sup.2, which are identical or different, each represent the hydrogen atom or a C.sub.1 -C.sub.3 alkyl group; and(ii) their addition salts.The said derivatives are useful as pharmaceuticals.

Abstract: Isotellurazolo[1,5-a]tellurazoles are disclosed. These heterocycles can be prepared by reacting a diarylformamidine with an aromatic tellurazolium salt which is substituted at its 2 ring position with a methine group precursor. The product heterocycles are useful directly for their blue light absorption and in forming stable heterocyclic nuclei containing compounds, such as a photographic addenda.

Abstract: In the preparation of a (thiono)phosphoric ester of the formula ##STR1## in which X represents oxygen or sulphur,R and R.sup.1 are identical or different and represent alkyl, andR.sup.2 represents optionally substituted aryl or represents optionally substituted hetaryl having at least one nitrogen atom,wherein a hydroxyl derivative of the formulaR.sup.2 --OHor an ammonium, alkali metal or alkaline earth metal salt thereof is reacted with a (thiono)phosphoric halide of the formula ##STR2## in which Hal represents halogen,the improvement which comprises effecting the reaction in the presence of a bicyclic organic amine as catalyst. Advantageously the reaction is effected in a diluent in the presence of potassium carbonate as an acid acceptor at 20.degree. to 100.degree. C., and 0.8 to 1.5 mols of the halide and 0.005 to 0.5 mol of 1,4-diazabicayclo-(2,2,2)-octane are used as bicyclic organic amine per mol of the hydroxyl compound.

Abstract: Insecticidally and fungicidally active novel 6-oxo-pyrimidinyl (thiono)-phosphate of the formula ##STR1## in which X represents oxygen or sulphur,R represents alkyl,R.sup.1 represents fluoroalkyl,R.sup.2 represents hydrogen, optionally substitutedalkyl, or alkoxy, alkylthio, dialkylamino or aryl,R.sup.3 represents alky or aryl andR.sup.4 represents hydrogen, halogen or alkyl.

Abstract: New heterocyclic compounds having the general formula ##STR1## wherein X is ##STR2## or CO.sub.2 R' whereinR' is C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl, or C.sub.3-7 -cycloalkylmethyl,R.sup.6 and R.sup.7 independently are hydrogen, halogen, alkoxy, or trifluoromethyl, andR" is hydrogen, C.sub.1-6 -alkyl, or C.sub.3-7 -cycloalkyl.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.

Abstract: The present invention relates to a process for the preparation of bis-indolic compounds, and the bis-indolic compounds produced by the process.

Abstract: Pesticidally active novel phosphates of the formula ##STR1## in which R represents hydrogen, alkyl, cycloalkyl, alkoxy, alkylthio, alkylamino, dialkylamino or aryl,R.sup.1 represents alkyl,R.sup.2 represents fluoroalkyl andX represents oxygen or sulphur.The acid halides of the formula ##STR2## are also new.