Abstract: The present invention relates to new, pharmacologically valuable 2,4,5,6-tetrahydro-1H-pyrazino-[3,2,1-jk]-carbazoles substituted in the 8-position having the formula I ##STR1## wherein R stands for an alkyl or alkoxy group having 1 to 4 carbon atoms or a fluorine, chlorine or bromine atom comprising reacting a 6,9-disubstituted 1,2,3,4-tetrahydrocarbazol-1-one of the formula II ##STR2## and X denotes a bromine, chlorine or iodine atom or the radical of the formula defined --O--SO.sub.2 --R' and R' is an alkyl radical having 1 to 3 carbon atoms, phenyl or tolyl, with ammonia.
Abstract: 3-Amino-5-(t-butyl)isoxazole, in optimum yield, is prepared in a stepwise manner by reacting a lower alkyl pivalate and acetonitrile in the presence of a base to yield pivalyl acetonitrile, which in turn is allowed to react with hydroxylamine under controlled conditions of pH to yield the desired compound. The compound is a useful intermediate for the preparation of isoxazole derivatives having utility as herbicides.
Type:
Grant
Filed:
December 7, 1978
Date of Patent:
March 31, 1981
Assignee:
Eli Lilly and Company
Inventors:
Kenneth W. Burow, Jr., Richard F. Eizember
Abstract: N-acyl sydnonimines of the formula: ##STR1## wherein R is phenyl, .beta.-phenylethyl, dl-.alpha.-methyl-.beta.-phenylethyl or l-.alpha.-methyl-.beta.-phenylethyl; R' is hydrogen, phenyl; X is a lower alkyl, phenyl, ##STR2## wherein R" is hydrogen, a halogen, a lower fluorinated alkyl; R'" is hydrogen, a halogen, a lower alkyl; when R is dl-.alpha.-methyl-.beta.-phenylethyl, R' is H, R" is Cl, R'" is only Cl, while when R' is H, X is NHC.sub.6 H.sub.5 R is only l-.alpha.-methyl-.beta.-phenylethyl; when X is phenyl, R and R' are each phenyl only.The method for preparing sydnonimine N-acylderivatives comprises reacting N-nitrosoderivatives of N-substituted nitriles of .alpha.-aminoacids of the formula: ##STR3## wherein R is phenyl, .beta.-phenylethyl, di-.alpha.-methyl-.beta.-phenylethyl or l-.alpha.-methyl-.beta.
Type:
Grant
Filed:
November 28, 1977
Date of Patent:
January 13, 1981
Assignees:
Vsesojuzny nauchno-issledovatelsky khimikofarmatsevtichesky institut imeni S. Ordzhonikidze, Institut biofiziki
Inventors:
Leonid E. Kholodov, Vladimir G. Yashunsky, Roald A. Altshuler, Mikhail D. Mashkovsky, Valentina V. Ogorodnikova, Zoya A. Olovyanishnikova, Anna S. Vitvitskaya, Valery A. Parshin, Ekaterina A. Kelekhsaeva
Abstract: Herbicidal compounds having the formula: ##STR1## where R is alkyl having 1-6 carbon atoms, alkenyl having 2-6 carbon atoms, cycloalkyl having 4-6 carbon atoms, unsubstituted or substituted with alkyl of 1-4 carbon atoms, or alkyleneoxyalkyl of 2-8 carbon atoms,R' is hydrogen or alkyl of 1-3 carbon atoms, and,X is chloro or bromo.are provided herein.The compounds of the invention are effective herbicides, particularly against wild grasses.
Abstract: Substituted 7H-thiazolo- and 7H-thiadiazolo-pyrimidine-7-ones compounds and the drug composition containing same. The compounds are immunostimulants for mammals. A process of making these compounds and of using the drug composition.
Abstract: An imidazolidinedione compound of the formula: ##STR1## wherein X is a chlorine atom or a bromine atom, Y is an oxygen atom or a sulfur atom, and R.sub.1 and R.sub.2 are each a C.sub.1 -C.sub.4 alkyl group, a C.sub.1 -C.sub.4 alkoxy group, a C.sub.1 -C.sub.4 alkylthio group, an ar(C.sub.1 -C.sub.4)alkylthio group, a C.sub.1 -C.sub.4 alkoxy(C.sub.2 -C.sub.4)alkoxy group, a phenyl group, a phenoxy group, a C.sub.1 -C.sub.4 alkylthiophenoxy group, a C.sub.1 -C.sub.8 alkylamino group, a C.sub.2 -C.sub.8 alkenylamino group or a cyano(C.sub.1 -C.sub.4)alkylamino group, which is useful as an agricultural chemical such as insecticides, acaricides, nematocides and/or fungicides with high safety to mammalian animals and human beings.
Abstract: Novel 2-benzhydrylimino-1,3-diazacarbocyclic compounds of the formula ##STR1## wherein R' and R" independently are selected from the group consisting of hydrogen and methyl, X and Y independently are selected from the group consisting of hydrogen, lower alkoxy, lower alkyl and halo, and n is an integer of from 2 to 4, inclusive; and their acid addition salts are disclosed. Compounds have antisecretory properties. Certain of the compounds also have hypoglycemic properties.
Abstract: Intermediate-duration reversible neuromuscular blocking agents of the formula (I) ##STR1## where B and C are preferably para or may be meta and are each ##STR2## where W is CH.sub.2 or most preferably CH.dbd.CH R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are each hydrogen or lower alkoxy of 1 to 4 carbon atoms and preferably methoxy, Y is lower alkyl of 1 to 4 carbon atoms and preferably methyl, Z is hydrogen, lower alkyl of 1 to 4 carbon atoms, cyclopentyl, cyclohexyl, benzyl, or ##STR3## where ALKYL has 1 to 4 carbon atoms preferably where the O-ALKYL is at the 2, 3, 4 or 5 positions such as 4-methoxy benzyl and is most preferably 3,4-dimethoxy benzyl or 3, 4, 5-trimethoxybenzyl, n is 2, 3 or 4, most preferably 2 or 3 provided that at least one of R.sub.1 to R.sub.4 is lower alkoxy and most preferably where R.sub.1 and R.sub.4 is hydrogen and R.sub.2 and R.sub.3 are methoxy and X is a pharmaceutically acceptable anion.
Type:
Grant
Filed:
January 31, 1979
Date of Patent:
November 25, 1980
Assignee:
Massachusetts General Hospital
Inventors:
John J. Savarese, Richard J. Kitz, Sara Ginsburg
Abstract: Compounds of the formula: ##STR1## wherein R is alkyl, alkenyl or cycloalkyl optionally substituted with chlorine, cycloalkylalkyl and (CH.sub.2).sub.n R'whereinn is 1-3 andR' is phenyl optionally substituted with CH.sub.3, CH.sub.3 O, NO.sub.2 or 1-2 halogens are useful to control a broad range of fungus diseases and insect and larval pests.
Abstract: Improved processes for preparing 2'-alkoxy-2,5-di-substituted-9-oxo-6,7-benzomorphans from benz[e]indolines and synthesis of the benz[e]indoline intermediates are described. A representative example involves synthesis of 9b-allyl-8-methoxy-3-methyl-5,9b-dihydrobenz[e]indoline and bromination thereof to 9b-allyl-4-bromo-8-methoxy-2,4,5,9b-tetrahydro-1H-benz[e]indole methylbromide which is then hydrolyzed with a weak base such as ammonium bicarbonate to provide 5-allyl-2'-methoxy-2-methyl-9-oxo-6,7-benzomorphan.
Abstract: Compounds of the formula ##STR1## wherein X is oxygen or sulfur;R.sub.1 is hydrogen, methyl or ethyl; andR.sub.2 is methyl or ethyl;and non-toxic, physiologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as sweetening agents.
Type:
Grant
Filed:
October 20, 1978
Date of Patent:
November 11, 1980
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Gunter Trummlitz, Ernst Seeger, Wolfhard Engel
Abstract: Spiro amine derivatives having excellent antihypertensive activity and central nervous system depressant activity, and represented by the formula: ##STR1## and their preparation and use.
Abstract: Isoindolinone pigments of the formula ##STR1## wherein X.sub.1, X.sub.2, X.sub.3 and X.sub.4 represent hydrogen or halogen atoms, or one or two of X.sub.1 -X.sub.4 represent alkoxy groups of 1 to 4 carbon atoms or phenoxy groups and the others represent hydrogen or halogen atoms, R and R" represent hydrogen or halogen atoms or methyl or methoxy groups, R.sub.1, R.sub.2, R.sub.4 and R.sub.5 represent hydrogen, chlorine or bromine atoms or alkyl groups of 1 to 2 carbon atoms, R.sub.3 and R.sub.6 represent hydrogen or halogen atoms, alkyl or alkoxy groups of 1 to 2 carbon atoms or radicals of the formula ##STR2## Q represents a direct bond or a p-phenylene group, n is 1 or 2 and X represents a group of the formula ##STR3## wherein R.sub.7 and R.sub.8 represent hydrogen or chlorine atoms or methyl groups.
Abstract: N-(Heterocyclicaminocarbonyl)arylsulfonamides, such as N-[(4-methoxy-6-methylamino-1,3,5-triazin-2-yl) aminocarbonyl]benzenesulfonamide, are useful for the regulation of plant growth and as herbicides, particularly for controlling volunteer corn in soybeans.
Abstract: This invention relates to phenol sulfam(na)phthaleins possessing a 2-(2'-halomethylbenzoyl) group substituted on the N atom of the sulfam(na)phthalein ring, which compounds find utility as photographic optical filter agents and filter agent precursors.
Type:
Grant
Filed:
September 23, 1977
Date of Patent:
November 4, 1980
Assignee:
Polaroid Corporation
Inventors:
Stanley M. Bloom, Alan L. Borror, James W. Foley
Abstract: Isothiazolidin-3-ones of the formula ##STR1## wherein R.sup.1 is a hydrogen atom, or an alkyl, cycloalkyl, aryl, aralkyl, carbamoyl, or thiocarbamoyl group,R.sup.2 and R.sup.3 are halogen atoms or alkyl groups, andX is a halogen atom and compositions containing them are useful in controlling microorganisms, such as bacteria, fungi, algae, and the like.
Abstract: The disclosed compounds such as 3-[5-(1-(2-nitrophenoxy)ethyl)-1,3,4-thiadiazol-2-yl]-4-hydroxy-1-methyl-2 -imidazolidinone are useful for preemergence control of weeds such as jimsonweed.
Abstract: Oxo-pyrido[1,2-a]thienopyrimidine compounds, salts thereof, methods of production, intermediates in their production, pharmaceutical compositions containing said compounds and methods for treating allergies using said compositions are disclosed.
Type:
Grant
Filed:
August 27, 1979
Date of Patent:
October 28, 1980
Assignee:
Warner-Lambert Company
Inventors:
Francis J. Tinney, David T. Connor, Wiaczeslaw A. Cetenko, Joseph J. Kerbleski, Roderick J. Sorenson