Abstract: The invention relates to polychromophoric dibenzoxazole compounds which have been found to be effective ultraviolet stabilizers. The invention also relates to ultraviolet degradable organic compositions containing a stabilizing amount of the polychromophoric dibenzoxazole composition to prevent such degradation. These stabilizers are effective in the presence of other additives commonly employed in polymeric compositions including, for example, pigments, colorants, fillers, reinforcing agents and the like. These ultraviolet stabilizers may also be incorporated into the organic compositions in the polymer melt or dissolved in the polymer dope, coated on the exterior of the molded article, film or extruded fiber.
Abstract: Disclosed is 6-(1'-Hydroxyethyl)-2-aminoethylthiooxapen-2-em-3-carboxylic acid: ##STR1## Such compound and its pharmaceutically acceptable salt and ester derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds pharmaceutical compositions comprising such compounds and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
Type:
Grant
Filed:
December 28, 1977
Date of Patent:
October 30, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, Frank P. DiNinno
Abstract: Methane-sulfonamide derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen or a halogen atom, R.sub.2 and R.sub.3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atom, provided that the group: --CH.sub.2 SO.sub.2 NR.sub.2 R.sub.3 is bonded to the carbon atom of either of X and Y,and an alkali metal salt thereof, and a process for the preparation of said methane-sulfonamide derivatives. Said compounds have an excellent anticonvulsant activity and are useful as anticonvulsants for controlling convulsions and seizures in patients with epilepsy.
Abstract: Quinazoline-2(1H)-ones are prepared by dehydrogenating a 5,6,7,8-tetrahydro-2(1H)-quinazolinone with sulfur in the presence of a metal oxide, hydroxide or halide.
Abstract: 5,5'-DIMETHYL-DI-(1,3-OXAZOLIDIN-3-YL) METHANE, A PROCESS FOR ITS PREPARATION OF REACTING A SOURCE OF FORMALDEHYDE WITH ISOPROPANOLAMINE AT ELEVATED TEMPERATURE FOLLOWED BY WATER REMOVAL, AN ANTI-MICROBIAL COMPOSITION COMPRISING SAID 5,5'-DIMETHYL-DI-(1,3-OXAZOLIDIN-3-YL) METHANE AND A DILUENT AND A PROCESS FOR COMBATTING MICRO-ORGANISMS BY APPLYING 5,5'-DIMETHYL-DI-(1,3-OXAZOLIDIN-3-YL) METHANE TO A MICRO-ORGANISM CONTAINING SAMPLE.
Abstract: 2,2-Dimethyl-3-vinyl-cyclopropanecarboxylic acid esters of the formula ##STR1## wherein R.sub.1 represents fluorine, chlorine or bromine, processes for their production and their use in pest control.
Type:
Grant
Filed:
November 9, 1977
Date of Patent:
August 7, 1979
Assignee:
Ciba-Geigy Corporation
Inventors:
Willy Meyer, Jozef Drabek, Laurenz Gsell, Friedrich Karrer
Abstract: Compounds of the formula ##STR1## where R.sub.1 is hydrogen or lower alkyl, andR.sub.2 is hydrogen or straight chain lower alkyl, andR.sub.3 is hydrogen, fluoro, chloro, lower alkoxy, lower alkyl or trifluoromethyl, andN is 1, 2, 3, and 4,Which are useful as minor tranquilizers, sleep inducers and muscle relaxants.
Abstract: The invention concerns a levulinic acid addition salt of the antihypertensive agent 4-amino-6,7-dimethoxy-2-[4-(5-methylthio-1,3,4-oxadiazole-2-carbonyl]piper azin-1-yl)quinazoline in which the base to acid mole ratio is 1 to from 1.25-1.35. The salt is characterized in having improved water solubility and stability compared to the levulinate salt having a 1:1 ratio of base to acid.
Abstract: 1-Methyl-6-substituted-4-phenyl-quinazolin-2-one-3-oxides and their use as intermediates in the preparation of 3-fluorobenzodiazepines which are useful as tranquilizers, muscle relaxants and sedatives.
Abstract: This invention relates to an improved process for the preparation of 1,3-dihydro-2H-1,4-benzodiazepin-2-ones and 2,3-dihydro-1H-1,4-benzodiazepines by the condensation of a 2-(2-haloacylamido)-benzophenone or a 2-(2-haloethylamino)-benzophenone, respectively, in the presence of hexamethylenetetramine, a water miscible alcohol containing 5 to 50 volume percent water, and an ammonium salt.
Abstract: Substituted 1,2-benzisoxazoles of the formula ##STR1## where: R.sup.1 and R.sup.3 =H or lower alkoxy;R.sup.2 =halo or .alpha.-branched lower alkyl;R.sup.4 =halo, halo lower alkyl, or lower alkylthio; provided, where R.sup.1 and R.sup.3 =H,R.sup.2 and R.sup.4 are other than simultaneously Cl or Br, which are active as antiinflammatory, antipyretic and analgesic agents, are derived from cyclodehydrating the corresponding salicylaldoximes with an isocyanate under extremely mild conditions.
Type:
Grant
Filed:
June 21, 1978
Date of Patent:
May 22, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Gerald E. Stokker, Edward J. Cragoe, Jr.
Abstract: The invention pertains to certain oxadiazolinones of the formula: ##STR1## in which R represents an alkyl radical containing 1 to 4 carbon atoms and R.sub.1 represents an alkyl radical containing 2 to 4 carbon atoms, an alkoxy radical of which the alkyl part contains 1 to 4 carbon atoms, an alkylthio radical of which the alkyl part contains 1 to 4 carbon atoms, or trifluoromethyl, and to their preparation and the compositions in which they are present, which compounds and compositions have utility as nematocides, acaricides and insecticides.
Abstract: 3-Phenyl-oxazolidine-2,4-dione derivatives can be halogenated directly, without splitting of the heterocyclic ring. The products thus obtained have a fungicidal action which is substantially wider than that of compounds hitherto known.
Abstract: Oxazoles which are substituted in the 2,4 or 5-position with an N-substituted-acylamino group have anti-allergic activity. Methods of making such compounds, pharmaceutical compositions containing the active compounds of the invention and methods of treating asthma utilizing such compounds are provided.
Abstract: Compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or CONHR.sub.7 and R.sub.7 is methyl or isopropyl,And whereinWhen R.sub.1 is hydrogen: R is p-nitro, p-cyano; p-aldehydo; p-acetyl; m-ethyl; m-nitro; m-bromo; 3,4-dimethyl; m-NH.sub.2 ; p-methylamino; p-dimethylamino; p-diethylamino; p-methylbenzylamino; p-pyrrolidino; p-piperidino; SR.sub.4 in para position in which R.sub.4 is alkyl having 1 to 4 carbon atoms or cyclohexyl; OR.sub.5 is para position in which R.sub.5 is alkyl having 2 to 7 carbon atoms, cyclohexyl, cyclohexylmethyl, acetylmethyl; cyanomethyl, alkene-2 yl having 3 to 5 carbon atoms, butene-3 yl, cyclohexene-1 methyl, propargyl, butyne-2 yl, ##STR2## in which n is one or 2 and when n is one, R.sub.6 is hydrogen, o-fluoro, o-methyl, m-chloro, m-fluoro, m-methyl, m-trifluoromethyl, p-chloro, p-bromo-, p-fluoro, p-cyano, p-nitro or p-dimethylamino and when n is 2, R.sub.6 is hydrogen; and 3-methyl-4-benzyloxy:When R.sub.1 is CONHR.sub.7 and R.sub.
Type:
Grant
Filed:
February 23, 1977
Date of Patent:
April 17, 1979
Assignee:
Delalande S.A.
Inventors:
Philippe L. Dostert, Colette A. Douzon, Guy R. Bourgery, Claude J. Gouret, Gisele C. Mocquet, Jean A. Coston
Abstract: Compounds of the formula ##STR1## wherein X and Y are the same or different and are hydrogen, fluoro, chloro, bromo, alkyl of one to six carbon atoms, inclusive, alkoxy of one to six carbon atoms, inclusive, nitro, cyano, amino, trifluoromethyl, ##STR2## wherein R.sub.1 is alkyl of one to six carbon atoms, inclusive, ##STR3## wherein R.sub.2 and R.sub.3 are the same or different and are hydrogen or alkyl of one to three carbon atoms inclusive, or CO.sub.2 Q where Q is alkyl of one to six carbon atoms, inclusive, hydrogen or a physiologically acceptable metal or amine cation; andR is hydrogen, alkyl of one to eight carbon atoms, inclusive, --CH.sub.2).sub.m phenyl wherein m is 0, 1 or 2 or (CH.sub.2).sub.n NR.sub.4 R.sub.5 wherein n is 1 or 2, and R.sub.4 and R.sub.
Abstract: This invention relates to the preparation of optically active d-2-aminobutanol by catalytic asymmetric reduction of appropriate dehydro precursors to produce selectively the desired isomer. The same substrates can also be used to prepare the dl-mixture using optically inactive catalysts. The novel substituted-4-ethyl-4-oxazolin-2-one and substituted-4-ethyl-2-oxazolidinone compounds of this invention are useful as intermediates in the production of the antituberculosis drug ethambutol (Myambutol.RTM.).