Abstract: 2-Aryl-4,6-dihalopyrimidines of the formula I ##STR1## wherein Hal is halogen,E is unsubstituted or substituted phenyl, thienyl or furyl, andY is a group bound by way of nitrogen, oxygen or sulfur,are able as antidote or `safener` to protect cultivated plants against the phytotoxic action of herbicides. Cultivated plants concerned are particularly sorghum, cereals, maize, rice and soya bean, and herbicides concerned are chloroacetanilides or other herbicidally effective substances.
Abstract: Novel pigmentary forms of isoindoline pigments which contain(a) a pigmentary form of the compound of the formula (I) ##STR1## and (b) from 2 to 50% by weight, based on (I), of one or more isoindoline pigments of the formula (II) ##STR2## where R is --CN, --CONH.sub.2, N--C.sub.1 -C.sub.4 -alkylcarbamyl, N-phenylcarbamyl, 2-quinazolonyl, 2-quinoxazolonyl and 2-benzimidazolyl, and the phenyl radical in the phenylcarbamyl and/or the heterocyclic radicals stated for R are unsubstituted or substituted, are obtained by heating a mixture of the finely divided pigments (I) and (II) in an aqueous medium.Advantageously, the mixture is prepared directly by synthesizing (I) in the presence of finely divided (II) in water.The novel pigmentary forms are transparent pigments which have high color strength, and whose transparency and color strength are substantially superior to those of very similar pigments.
Abstract: Novel imidazo[1,2-c]pyrimidines of the formula ##STR1## wherein R is an aryl of 6 to 12 carbon atoms, R.sub.1 is selected from the group consisting of hydrogen and alkyl, alkoxy and alkylthio of 1 to 5 carbon atoms when R.sub.2 and R.sub.3 together form a carbon-nitrogen bond or R.sub.1 and R.sub.2 together are .dbd.0 when R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms and alkenyl of 2 to 5 carbon atoms, R.sub.4 is selected from the group consisting of alkoxy and alkylthio of 1 to 5 carbon atoms, R.sub.5 is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anxiolytic properties.
Abstract: Novel quinazoline and cinnoline derivatives having the formula ##STR1## (wherein one of A and B is CH and the other one of A and B is N; X.sub.1 is halogen or CF.sub.3 and X.sub.3 is one of the groups II, III, IV or V ##STR2## where Q is lower alkylene; R.sub.1 is hydrogen or lower alkyl; R.sub.2 and R.sub.3 are independently lower alkyl or R.sub.2 and R.sub.3 are a divalent radical such that HNR.sub.2 R.sub.3 is a secondary cyclic amine with 5 to 7 ring atoms; R.sub.4 is lower alkyl; n is 0 or 1; the rings shown in formulae III and IV are piperidine or pyrrolidine optionally substituted by lower alkyl; and the ring shown in formula V is piperazine optionally substituted by lower alkyl) and their pharmaceutically acceptable salts are useful as pharmaceuticals particularly as anti-hypertensives. Novel intermediates are also described including the corresponding sulphonic acids of formula I (where A, B and X.sub.1 are defined above and X.sub.3 is OH).
Abstract: Novel 5-pyrimidinecarboxamides useful for regressing or inhibiting the growth of leukemia and tumors. The compounds have the formula: ##STR1## wherein R.sub.1 is hydrogen or an alkoxy group having from one to four carbon atoms;R.sub.2 is hydrogen; alkyl, aryl, aralkyl, allyl, aralkenyl or aralkynyl, the alkyl, alkenyl or alkynyl moieties of which have from one to six carbon atoms, or a carbohydrate residue;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or aryl;R.sub.
Type:
Grant
Filed:
April 22, 1985
Date of Patent:
January 13, 1987
Assignees:
Uniroyal Chemical Company, Inc., Uniroyal Ltd.
Abstract: This invention provides for certain phenyl-substituted imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents and vasodilators.
Abstract: Griseolic acid derivatives of formula (I): ##STR1## wherein A represents: ##STR2## have enzyme-inhibitory activity, especially against cAMP PDE and cGMP PDE. When formulated as compositions with appropriate carriers or diluents, they may be used for the treatment of a variety of organic disorders and show toxicities less than griseolic acid itself.
Abstract: Novel 5-pyrimidinecarboxamides useful for regressing or inhibiting the growth of leukemia and tumors in mammals. The compounds have the formula: ##STR1## wherein: R is hydrogen, 2- or 3-halo, 4-fluoro, 2-methyl, 2- or 4-alkoxy, or 2- or 4-trifluoromethyl, and R.sub.1 is hydrogen; orR is 2-fluoro and R.sub.1 is 4-fluoro; orR is 2-methoxy and R.sub.1 is 5-methyl; andR.sub.2 and R.sub.3 are hydrogen atoms or carbohydrate residues; and,with the exception of the compound wherein R is 4-methoxy and R.sub.1 is hydrogen, the pharmacologically acceptable acid-addition salts thereof.
Type:
Grant
Filed:
February 8, 1985
Date of Patent:
January 6, 1987
Assignees:
Uniroyal Chemical Company, Uniroyal Ltd.
Abstract: Preparation of ethyl {6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl}hydrazino carboxylate is disclosed, from 3-chloro-6-hydrazinopyridazine in protected form, which is oxidized to yield the corresponding azo derivative, which is treated with ethyl-(2-hydroxypropyl)amine in the presence of strong bases, the corresponding amino derivative being subjected to reduction and deprotection, and finally acylated to yield ethyl{6-[ethyl-(2-hydroxypropyl)amino]-3-pyridazinyl}hydrazinocarboxylate.
Type:
Grant
Filed:
February 20, 1986
Date of Patent:
December 30, 1986
Assignee:
I.S.F. S.p.A.
Inventors:
Carlo Farina, Giorgio Pifferi, Mario Pinza
Abstract: 2-Guanidino-4-(2-methyl-4-imidazolyl)thiazole dihydrobromide and a one-pot, high yield process for its preparation from 2-methyl-4(or 5)-acetylimidazole.
Abstract: A process for producing 5-fluorouracil using an aqueous phosphoric acid solution as a solvent which is a good solvent for an intermediate resulting from the reaction between uracil and elemental fluorine, and permits the reaction to proceed smoothly, but which can precipitate the final product, 5-fluorouracil, after cooling the heat-treated reaction solution to room temperature, with no need to evaporate the solvent.The process comprises reacting uracil in an aqueous phosphoric acid solution with elemental fluorine and heating the resultant reaction solution to form 5-fluorouracil.
Type:
Grant
Filed:
March 7, 1985
Date of Patent:
December 23, 1986
Assignees:
Onoda Cement Company, Ltd., Sagami Chemical Research Center
Abstract: There are disclosed novel intermediates useful in the preparation of pyrido[2,3-d]pyrimidines having the following structures: ##STR1## wherein R is CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CH.sub.2 CH.sub.2, CH.sub.2 .dbd.CHCH.sub.2 or CH.tbd.CCH.sub.2 ; and ##STR2## wherein R is CH.sub.3, CH.sub.3 CH.sub.2, CH.sub.3 CH.sub.2 CH.sub.2, CH.sub.2 .dbd.CHCH.sub.2 or CH.tbd.CCH.sub.2. These intermediates have the formulas: ##STR3## wherein Y is CHO, CH.sub.2 OH or CH.sub.2 Br; and Z is CH.sub.2 OH or CH.sub.2 Br.
Type:
Grant
Filed:
March 15, 1985
Date of Patent:
December 9, 1986
Assignee:
Southern Research Institute
Inventors:
Carroll G. Temple, John A. Montgomery, Robert D. Elliott
Abstract: There are disclosed novel oxopyrimidine derivatives of the general formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and are each hydrogen or lower alkyl optionally substituted by lower alkoxy, and R.sub.3 and R.sub.4 may be the same or different and are each phenyl optionally substituted by lower alkyl or halogen, provided that when R.sub.1 and R.sub.2 are both hydrogen, R.sub.3 and R.sub.4 are each substituted phenyl. Pharmaceutical compositions containing these compounds and their use as anticonvulsant, antianxiety and muscle relaxant agents are described.
Abstract: A novel process is described for preparing substituted pyridazines, where a less substituted pyridazine is reacted with a carboxylic acid in the presence of a silver ion as catalyst, using peroxydisulfate ion. The reaction is run at a temperature from about 40.degree. to 80.degree. C. in an aqueous solvent system and mineral acid. The substituted pyridazines are useful as intermediates to herbicidal and fungicidal compounds.
Abstract: Novel [7-(3-disubstituted amino)phenyl]pyrazolo[1,5-a]pyrimidines useful as anxiolytic, antiepileptic and sedative-hypnotic agents as well as skeletal muscle relaxants, methods of using these compounds, compositions of matter containing them and processes for their production.
Type:
Grant
Filed:
May 13, 1985
Date of Patent:
December 2, 1986
Assignee:
American Cyanamid Company
Inventors:
John P. Dusza, Andrew S. Tomcufcik, Jay D. Albright
Abstract: The invention is a composition which comprises a nitrogen-containing coordination compound copper hydrocarbyloxy halide complex supported on activated carbon. This composition is useful as a catalyst for the preparation of dihydrocarbyl carbonates from alcohols, carbon monoxide and oxygen.
Abstract: Pyrazolo[3,4,5-kl]acridines are described as antibacterial agents and antitumor agents as well as pharmaceutical compositions and methods for their preparation.