Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen or lower alkyl, R.sub.3 represents lower alkyl and A is a monovalent group of formula: ##STR2## wherein Y is hydrogen or the acyl radical of a hydrocarbon carboxylic acid having from 2 to 18 carbon atoms, inclusive, are employed as anticonvulsants in treating mammals, including humans.Novel compounds within the scope of the above formula are also disclosed, wherein R.sub.1 is specifically lower alkyl and provided that R.sub.1 is located in a position ortho or meta to the substituent group A when R.sub.2 is hydrogen. Disclosed also are novel intermediate compounds for preparing the above-described novel compounds of the invention, which correspond thereto but wherein the group A is replaced by a nitro-group.
Type:
Grant
Filed:
September 8, 1975
Date of Patent:
January 18, 1977
Assignee:
The Upjohn Company
Inventors:
Robert James Collins, Charles E. Coverdale
Abstract: A process for the prevention or treatment of osteoporosis induced as a side effect of the administration of glucocorticoid steroids by the administration of a compound of the formula: ##STR1## WHEREIN R.sub.1 and R.sub. 2 are the same or different radicals selected from the group consisting of hydrogen, alkyl of less than 9 carbon atoms, and phenyl; R.sub.3 and R.sub. 5 are selected from the group consisting of hydrogen and lower acyl; n is an integer, selected from the group consisting of 2, 3, and 4; or a hydrate thereof in association with a pharmaceutical carrier to a human or animal being treated or having been treated with a gluco-corticoid hormone.
Abstract: An animal feed comprising a compound of the group consisting of 6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula: ##STR1## WHEREIN R is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, phenyl, benzyl and -COOR' in which R' is alkyl of 1 to 4 carbon atoms, inclusive; wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atom, inclusive and their pharmacologically acceptable acid addition salts in combination with a nutrient feed.
Abstract: A known compound, 2-ethyl-4-methyl diester of 3,5-dimethyl-2,4-pyrroledicarboxylic acid, has been found to be an excellent herbicide. A new method of controlling weeds and growth of plants with the compound is described along with herbicidal compositions.
Abstract: Preparation of C. malvarum spores, spore concentrates and agricultural formulations for use as a mycoherbicide by application onto undesired vegetation; e.g., teaweed or to the situs of the undesirable vegetation, controlling the undesired vegetation in cropland and other locales where the presence of the vegetation is undesired.
Type:
Grant
Filed:
June 19, 1975
Date of Patent:
December 28, 1976
Assignee:
The Board of Trustees of the University of Arkansas
Abstract: Novel pesticidal compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl of from 1 to 4 carbon atoms; R.sub.2 is hydrogen, halogen or lower alkyl of from 1 to 4 carbon atoms; R.sub.3 and R.sub.4 are the same or different and are hydrogen, alkyl of 1 to 8 carbon atoms, inclusive; haloalkyl, arylalkyl and ##STR2## WHEREIN ALKYL IS FROM 1 TO 4 CARBON ATOMS, CYCLOALKYL OF FROM 3 TO 6 CARBON ATOMS, ARYL AND R.sub.3 and R.sub.4 taken together are a member selected from the group piperidine, morpholine, pyrazole, tribromopyrazole, N-methylpiperazine, pyrrole, pyrrolidine, pyrrolidone.The compounds are combined with carriers to prepare compositions and are useful in controlling insect pests either as an insecticide or behavioral modifier and are particularly effective as miticides.
Abstract: A process for inhibiting platelet aggregation by the addition of a member selected from the group consisting of a compound of the formula: ##SPC1##Wherein is cyclohexane or phenyl; Y is hydrogen, halogen, --CF.sub.3, --OH, lower alkyl of 1 to 8 carbon atoms, lower alkoxy of 1 to 8 carbon atoms, --CN, --NH.sub.2, --SH, or --S-lower alkyl of 1 to 8 carbon atoms; and R is hydrogen, lower alkyl of 1 to 8 carbon atoms, inclusive, or a pharmacologically acceptable cation, to in vivo and in vitro platelet systems. In vitro systems include whole blood as kept in blood banks, whole blood as used in heart-lung machines, and platelet-rich concentrates. In vivo systems include human or animal bodies. The process provides a means for treating hemorrhage due to thrombocytopenia which in turn is caused by irradiation, cancer chemotherapy, or immunosuppressants as well as hemophilia due to congenital defects.
Abstract: Certain new 6-amino-2-lower-alkyl-4-nitropyridine N-oxides, particularly 6-amino-4-nitro-2-picoline N-oxide, have been found to be effective coccidiostats. The amino group can be varied and acid addition and quaternary ammonium salts are included.
Abstract: An improvement in the method of treating paralysis agitans by administration of 3,4-dihydroxy-phenyl-1-alanine, its hydrates and salts thereof is disclosed, which comprises administering it concurrently with a benzodiazepine compound having sedative-hypnotic and anxiolytic activity. Disclosed also are therapeutic compositions which comprise mixtures of 3,4-dihydroxyphenyl-1-alanine with benzodiazepines. The therapeutic compositions are useful in the treatment of humans afflicted with paralysis agitans.
Abstract: Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-chloro-1-methyl-6-(o-chlorophenyl)-4H-s-triazolo[4,3-a][1,4]benzodiazepi ne compound of the formula ##SPC1##Including the N-oxides and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier. The compositions are useful as soporifics and provide a process for inducing sleep.
Abstract: Therapeutic compositions for treating humans and animals comprising, in dosage unit form, a 8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepine compound of the formula ##SPC1##Including the N-oxides and pharmacologically acceptable acid addition salts thereof in combination with a pharmaceutical carrier. The compositions are useful as soporifics and provide a process for inducing sleep.
Abstract: Certain new 1-(3',5'-O-Variable-.beta.-D-arabinofuranosyl)-N.sup.4 -.alpha.-aminoacylcytosines, for example, 1-(5'-O-palmitoyl-.beta.-D-arabinofuranosyl)-N.sup.4 -[N.sup..alpha.-[N-(tert-butoxycarbonyl)glycyl]-L-arginyl]cytosine hydrochloride, have been found active against neoplastic cells, viruses, and as immunosuppressants. The 3'-O-, or 5'-O-, variability includes the hydrogen atom and acyl groups. The N.sup.4 -.alpha.-aminoacyl group comprises .alpha.-amino acids, N-protected .alpha.-amino acids, and similar peptidyl sequences of .alpha.-amino acids. Acid addition salts are an embodiment of the invention.
Type:
Grant
Filed:
August 30, 1974
Date of Patent:
August 17, 1976
Assignee:
The Upjohn Company
Inventors:
Duane T. Gish, Gary D. Gray, William J. Wechter
Abstract: Some new 1-(2- or 3-deoxy-.beta.-D-pentofuranosyl)-2-thiouracils and 1-.beta.-D-pentofuranosyl-2-thio-6-azauracils have been prepared. Further, it has been found that the known nucleoside compound, 1-.beta.-D-ribofuranosyl-2-thiouracil is active against Herpes virus and against L-1210 leukemia in mice. An improved method of preparing corresponding 2-0-methyluracil and 2-0-methyl-6-azauracil intermediates is described. The method preserves the .beta.-configuration of the starting nucleoside.
Abstract: A process for the therapeutic treatment of allergy by the systemic administration of a compound of the formula: ##SPC1##Wherein ##SPC2##Is cyclohexane or ##SPC3##And X and Y can be the same or different and are hydrogen, fluoro, chloro, bromo, alkyl of from 1 to 8 carbon atoms, inclusive, or alkoxy of from 1 to 8 carbon atoms, inclusive, and the pharmacologically acceptable salts thereof in association with a pharmaceutical carrier.
Abstract: Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula: ##SPC1##Wherein R, R.sub.1, R.sub.2 and R.sub.3 are hydrogen, methyl or ethyl, and R.sub.4 is hydrogen, fluorine, chlorine, bromine, --NO.sub.2, --CF.sub.3, or methylthio, inclusive; including the pharmacologically acceptable acid addition salts thereof, in association with a pharmaceutical carrier. The process is the administration of the above compositions to humans at a dose of from about 0.1 mg./kg./day to about 10 mg./kg./day for anti-depressant therapy with minimum sedative side-effects.
Abstract: Pharmaceutical compositions comprising, in unit dosage form, from about 0.5 mg. to about 100 mg. of a compound of the formula: ##SPC1##Where R, R.sub. 1, R.sub.2 and R.sub.3 is hydrogen, methyl or ethyl, and R.sub.4 is hydrogen, fluorine, chlorine, bromine, --NO.sub.2, --CF.sub.3, or methylthio, inclusive; including the pharmacologically acceptable acid addition salts thereof, in association with a pharmaceutical carrier. The process is the administration of the above compositions to humans at a dose of from about 0.1 mg./kg./day to about 10 mg./kg./day for antidepressant therapy with minimal sedative side effects.
Abstract: Compounds of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are the same or different and are hydrogen, alkyl of from 1 to 6 carbon atoms, inclusive, or phenyl; R.sub.3 is hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, phenyl, or benzyl; R.sub.4 is hydrogen or alkyl of from 1 to 6 carbon atoms, inclusive, and R.sub.3 and R.sub.4 can be joined together to form a heterocyclic ring selected from the group consisting of morpholine, pyrrolidine or piperidine; X is oxygen or sulfur; A and B are the same or different, and are hydrogen, alkyl of from 1 to 6 carbon atoms inclusive, cycloalkyl of from 3 to 7 carbon atoms, inclusive, haloalkyl, and halogen; Z is an alkyl group of from 1 to 6 carbon atoms, inclusive, or a cycloalkyl group of from 3 to 7 carbon atoms provided that when A and B are halogen, Z is located at the 4 or 5 positions.
Abstract: Novel pesticidal N-hydrocarbylsulfenyl derivatives of N-alkyl-N'-aryl formamidines are disclosed with novel compositions thereof and methods of their use in controlling invertebrate pests, particularly insects and acarina. Certain of the novel compounds are particularly effective miticides.
Abstract: Novel pesticidal compounds of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are the same or different and are selected from the group consisting of lower alkyl of from 1 to 4 carbon atoms; R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, halogen, and lower alkyl of from 1 to 4 carbon atoms, n = 1 or 2 provided that when n is 2 then R.sub.1 and R.sub.2 are the same as R.sub.3 and R.sub.4 are the same.The compounds are combined with carriers to prepare compositions and are useful in controlling insect pests either as an insecticide or behavioral modifier and are particularly effective as miticides.
Abstract: Compounds of the formula: ##SPC1##Wherein R is hydrogen prepared in unit dosage form with appropriate pharmaceutical carrier for oral and parenteral administration and process of producing regression in subjects with advanced or disseminated mammary cancer in woman.