Abstract: Antihypertensively active thiourea derivatives of the formulas ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3 and X are as hereinafter described, as well as a method of using a compound of the formula ##STR2## wherein R.sub.1 ', R.sub.2 ', R.sub.3 and X are as previously described, or a compound of formula II as an anti-hypertensive agent, is described.
Type:
Grant
Filed:
October 25, 1977
Date of Patent:
September 12, 1978
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Michael Robert Cohen, Richard Wightman Kierstead, Jefferson Wright Tilley
Abstract: Benzoyl cyanide is made by reacting benzoyl chloride with an alkali cyanide in the presence of a carboxylic acid nitrile and a copper (I) salt at a temperature of about 50.degree. to 160.degree. C.
Type:
Grant
Filed:
June 20, 1977
Date of Patent:
September 12, 1978
Assignee:
Deutsche Gold- und Silber-Scheideanstalt Vormals Roessler
Inventors:
Herbert Klenk, Theodor Lussling, Alfred Maierhofer, Heribert Offermanns, Hans Wagner
Abstract: Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group have been prepared. These compounds are valuable antibacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.
Abstract: N-Substituted alkanesulfenyl-N-alkyl and N-substituted alkanethiosulfenyl-N-alkyl carbamoyl halide compounds are useful as intermediates in the preparation of pesticidal carbamate compounds.
Abstract: In the process for preparing an organic compound of the formulaA' -- Xin whichX is an amino group, a hydroxyl group or a carboxyl group, andA' is the remainder of the molecule, from an organic compound of the formulaA -- Xin whichA is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formulaA -- Z -- COORin whichZ is --NH--, --O-- or a direct C--C bond, andR is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CH.dbd.CH-- group or an arylene group,R.sup.1 to R.sup.4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, orR.sup.1 + r.sup.2 and R.sup.3 + R.sup.4 each independently completes a 5- or 6-membered carbocyclic ring, orR.sup.1 and R.sup.
Type:
Grant
Filed:
April 28, 1977
Date of Patent:
September 5, 1978
Assignee:
Bayer Aktiengesellschaft
Inventors:
Heiner Eckert, Ivar Ugi, Hans-Joachim Kabbe
Abstract: A process for the preparation of benzoyl halide and meta-halosulfonyl benzoyl halide comprises adding to oleum and reacting therewith a benzotrihalide compound characterized by the formula: ##STR1## wherein X is bromine or chlorine and Y is individually selected from the group consisting of fluorine, chlorine, bromine, iodine, alkyl, preferably of one to six carbon atoms, halosubstituted alkyl, preferably trichloromethyl or tribromomethyl, aryl, preferably phenyl, and hydrogen, with the proviso that at least one Y substituent at a meta position is hydrogen.
Abstract: There are prepared acyl cyanides of the formula ##STR1## where R is a straight or branched chain alkyl group having 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms, and which also can be substituted by one or more phenyl groups or halogen atoms, preferably chlorine, or R is preferably a cycloalkyl group having 3 to 8 carbon atoms, preferably cyclopropyl, which can have one or more 1 to 3 carbon atom alkyl or halogen, preferably chlorine, substituents wherein in all of the above set forth substitutions the halogen atoms and the phenyl groups are not on the carbon atom adjacent to the carbonyl group or R is a substituted phenyl group, a naphthyl group, a substituted naphthyl group or a five membered heterocyclic group, e.g., furyl, thienyl or alkyl substituted thienyl, wherein the substituents on the phenyl or naphthyl are halogen atoms, nitro groups or alkyl or alkoxy groups having 1 to 5 carbon atoms.
Type:
Grant
Filed:
June 2, 1977
Date of Patent:
August 22, 1978
Assignee:
Deutsche Gold- und Silber-Scheideanstalt Vormals Roessler
Inventors:
Herbert Klenk, Heribert Offermanns, Werner Schwarze
Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is aryl and both R.sub.2 groups are hydrogen or alkyl, have useful antiinflammatory activity.
Abstract: The disclosure relates to novel 15-(3-aryl- or 3-aralkyl-cyclobutyl, -cyclopentyl and -cyclohexyl)-.omega.-pentanor prostaglandin analogues, for example 9.alpha.,11.alpha.,15.alpha.-trihydroxy-15-(trans-3-phenylcyclobutyl)-16,1 7,18,19,20-pentanor-5-cis, 13-trans-prostadienoic acid, to pharmaceutical or veterinary compositions containing such a compound, and to a method of inducing luteolysis in animals by orally administering such a compound.
Abstract: There are prepared acyl cyanides of the formula ##STR1## where R is a straight or branched chain alkyl group having 1 to 18 carbon atoms, preferably 1 to 10 carbon atoms, and which also can be substituted by one or more phenyl groups or halogen atoms, preferably chlorine, or R is preferably a cycloalkyl group having 3 to 8 carbon atoms, preferably cyclopropyl, which can have one or more 1 to 3 carbon atom alkyl or halogen, preferably chlorine, substituents wherein in all of the above set forth substitutions the halogen atoms and the phenyl groups are not on the carbon atom adjacent to the carbonyl group or R is a substituted phenyl group, a naphthyl group, a substituted naphthyl group or a five membered heterocyclic group, e.g., furyl, thienyl or alkyl substituted thienyl, wherein the substituents on the phenyl or naphthyl are halogen atoms, nitro groups or alkyl or alkoxy groups having 1 to 5 carbon atoms.
Type:
Grant
Filed:
June 2, 1977
Date of Patent:
August 22, 1978
Assignee:
Deutsche Gold- und Silber-Scheideanstalt Vormals Roessler
Inventors:
Herbert Klenk, Heribert Offermanns, Werner Schwarze
Abstract: An improvement in the process for preparing benzenesulphonic acid chloride by reacting benzenesulphonic acid with thionyl chloride, the improvement residing in carrying out the process in the presence of a sulphonating agent.
Abstract: Production of methyldichlorophosphane. The compound is made by reacting methane and phosphorus trichloride in a reaction zone in which a temperature higher than 500.degree. C is maintained. More specifically, hot reaction gas coming from the reaction zone is mechanically freed from solid matter, and the reaction gas freed from solid matter is passed to a quenching zone in which it is quenched with liquefied reaction mixture having 0.3 to 5 weight % of an organic barium compound or a non-ionic surfactant dissolved therein.
Type:
Grant
Filed:
July 11, 1977
Date of Patent:
August 1, 1978
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Stefan Schafer, Klaus Gehrmann, Alexander Ohorodnik, Karl-Heinz Steil, Wernfried Riechmann, Friedhelm Bylsma
Abstract: In a process for preparing substituted or unsubstituted carboxylic acid chlorides of the benzene series by contacting the corresponding carboxylic acid ester with an aromatic compound containing at least one nuclearly bound trichlormethyl group in the presence of a molybdenum catalyst, the improvement which comprises introducing into the reaction mixture prior to distillation of the carboxylic acid chloride a complexing agent which complexes with the molybdenum catalyst.
Type:
Grant
Filed:
July 7, 1977
Date of Patent:
August 1, 1978
Assignee:
Dynamit Nobel Aktiengesellschaft
Inventors:
Gunter Zoche, Hermann Richtzenhain, Wilhelm Vogt
Abstract: Pure methyldichlorophosphane is recovered from a mixture containing phosphorus trichloride and methyldichlorophosphane as its principal constituents by distillation in two stages. Phosphorus trichloride and other low-boiling material are distilled off overhead in the first stage and methyldichlorophosphane is distilled off from high-boiling material in the second stage, the latter being fed with base product coming from the first stage. More specifically, there is dissolved in the said mixture, prior to admitting it to the first distillation stage, 0.01 to 1 weight % of an organic barium compound or 0.1 to 10 weight % of a non-ionic surfactant, and the base product coming from the first distillation stage is admixed, prior to admitting it to the second distillation stage, with 1 to 10 weight % of phosphorus oxychloride.
Type:
Grant
Filed:
July 22, 1977
Date of Patent:
August 1, 1978
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Alexander Ohorodnik, Klaus Gehrmann, Stefan Schafer, Albert Mainski
Abstract: A penicillin compound of the formula ##STR1## wherein R is a formyl or acetyl group, and a nontoxic pharmaceutically acceptable salt thereof. The penicillin compound is prepared by (A) reacting a compound of the formula ##STR2## or its salt or its reactive derivative at the carboxyl group, with 6-.alpha.-amino-p-hydroxybenzylpenicillin or its salt or its derivative, or reacting a compound of the formula ##STR3## or its salt or its reactive derivative at the carboxyl group, with 6-aminopenicillanic acid or its salt or its derivative, (B) optionally hydrolyzing or catalytically hydrogenolyzing the reaction product, and (C) optionally converting the reaction product to a nontoxic pharmaceutically acceptable salt. The penicillin compound has low toxicity and superior antibacterial activity especially against bacteria of the genus Pseudomonas and is suitable for parenteral administration, especially for an intramuscular, intravenous or subcutaneous injection.
Abstract: This invention comprises certain analogs PGE or 11-deoxy-PGE compounds in which the carbonyl at C-9 is replaced by methylene. Also provided in this invention, are novel chemical processes and novel chemical intermediates useful in the preparation of the above prostaglandin analogs. These prostaglandin analogs exhibit prostaglandin-like activity, and are accordingly useful for the same pharmacological purposes as the prostaglandins. Among these purposes are blood pressure lowering, labor induction at term, reproductive-cycle regulation, gastric antisecretory action, and the like.