Abstract: Chromogenic azaphthalides of the formula ##STR1## wherein R.sub.1 and R.sub.2 independently of each other are hydrogen, C.sub.1 -C.sub.12 alkyl which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or are cycloalkyl, benzyl or phenyl, or benzyl or phenyl which are substituted by halogen, nitro, cyano, lower alkyl, lower alkoxy or lower alkoxycarbonyl; or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are a 5-membered or 6-membered heterocyclic radical and in particular pyrrolidinyl;X is hydrogen, halogen, lower alkyl, lower alkoxy, benzyl, phenyl, benzyloxy, phenoxy, or benzyl or benzyloxy which are substituted by halogen, nitro, lower alkyl or lower alkoxy;Y is hydrogen, unsubstituted or substituted alkyl or benzyl or acyl and in particular C.sub.6 -C.sub.
Abstract: 3-(aminoalkylaminocarbonylmethoxy)-5-phenylpyrazole compounds corresponding to the formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.5, R.sub.6, R.sub.7, and R.sub.8 and R.sub.9 may be hydrogen or lower alkyl groups, or R.sub.5 with R.sub.6 and/or R.sub.8 with R.sub.9 may also form specified cyclic groups, R.sub.3 and R.sub.4 may be hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl, nitro, hydroxy or alkylene dioxy, and Z represents an alkylene chain or the 2-hydroxypropylene chain. The compounds possess pharmacological, in particular antiarrhythmic, properties.
Abstract: Phenyl chlorothioformates are produced in high yields easily and safely by (1) allowing sulfur dioxide to react with a mixed solution consisting of perchloromethyl mercaptan, an organic solvent and water, (2) removing the aqueous layer from the reaction mixture and (3) adding to the organic layer a phenol compound and a dehydrohalogenating agent in that order.
Abstract: 7-Oxabicyclo(2.2.1)heptane-based N-hydroxy-N-alkyl (or aryl) ureas, carbamic acids and carbamothioic acids are disclosed having the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, alkenyl, aryl or aralkyl; R.sub.2 is hydrogen, lower alkyl, aralkyl, alkanoyl or aroyl; R.sub.3 is lower alkyl, alkenyl or alkynyl; A is --CH.sub.2 --CH.dbd.CH-- or a single bond; X is oxygen, sulfur or NH; n is an integer from 1 to 8; and all stereoisomers thereof.These new compounds have been found to simultaneously inhibit the enzymes arachidonic acid cyclooxygenase and arachidonic acid 5-lipoxygenase and are therefore useful as antiinflammatory, antiasthma and antipsoriatic agents.
Type:
Grant
Filed:
September 23, 1986
Date of Patent:
September 22, 1987
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Ravi K. Varma, Sam T. Chao, Eric M. Gordon
Abstract: Certain substituted-4-hydroxy-(or 4-acyloxy-)2H-1,2-benzothiazine 1,1-dioxides having at the 3-position a 2-substituted-1,3,4-oxadiazol-5-yl, a 2-substituted-tetrazol-5-yl or a 1-substituted-tetrazol-5-yl group useful as selective 5-lipoxygenase pathway inhibitors; and methods for their preparation.
Abstract: Insecticidal and acaricidal organic esters formed from pyrethroid carboxylic acids and phenoxypyridinyltrifluoroethanols, agricultural compositions containing said esters and their use against anthropod pests including soil-dwelling species; also, intermediates for these insecticides and acaricides and a process for the preparation of said intermediates.
Abstract: A phenol derivative represented by the formula ##STR1## wherein R.sup.1 is a secondary or tertiary hydrocarbon residue of having 3 to 8 carbon atoms, R.sup.2 is a hydrocarbon residue having 1 to 12 carbon atoms, X is ##STR2## wherein R.sup.3, R.sup.4 and R.sup.5 each is an alkylene group having 1 to 4 carbon atoms, Z is an n-valent group and n is an integer of 1 to 8.This compound is effective to prevent the oxidation of organic materials.
Type:
Grant
Filed:
May 23, 1986
Date of Patent:
September 15, 1987
Assignee:
Mitsubishi Yuka Fine Chemicals Co., Ltd.
Abstract: Compounds of formula I or II ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, alkyl, cyclohexyl, phenyl, benzyl or tolyl, or are a --CH.sub.2 --CHR.sup.3 --CH.sub.2 --S--CO--R.sup.4 radical, R.sup.3 is hydrogen or methyl, R.varies.is alkyl, cyclohexyl, phenyl, benzyl or tolyl, X is alkylene, --S--, --SO--, --SO.sub.2 -- or substituted alkylene, in which R.sup.5 and R.sup.6 are hydrogen or alkyl, and n is an integer from 1 to 10, can be used as latent hardeners for epoxy resins.The compositions containing epoxy resins and these hardeners are particularly suitable for use as single component adhesive formulations. The cured products have good hot water resistance.
Abstract: S-n-butyl-N,N-diisopropyl thiocarbamate which has the structural formula ##STR1## which is useful as a selective herbicide in sugarbeets, carrots and cabbage.
Abstract: Process for preparing analgesic and narcotic antagonistic isoquinolines comprising:(a) contacting and reacting a lithiated anisole or alkyl phenyl ether, optionally substituted at the 3-position to the lithium atom, with a 4-piperidone to yield a 4-aryl-4-piperidinol;(b) dehydrating the piperidinol to a 4-aryl-1,2,3,6-tetrahydropyridine;(c) metalating and acylating the 1,2,3,6-tetrahydropyridine to yield a 1-(4-aryl-1,2,3,4-tetrahydropyrid-4-yl)-4-hydroxy-1-butanone;(d) reducing the ketone moiety of the butanone to yield a 5-aryl-7-oxa-2-azabicyclo[3.2.1]-octane-6-propanol;(e) converting the alcohol moiety of the propanol to L to yield a 5-aryl-6-[3-(L)propyl]-7-oxa-2-azabicyclo[3.2.1]octane in which L is a leaving group selected from the group consisting of --Cl, --Br, --I, p-MeC.sub.6 H.sub.4 SO.sub.3 and MeSO.sub.3 --.
Abstract: Polycyclic salts of the formulaA.sup.- XN.sup.+ CH.sub.2 --(Y).sub.n --(CH.sub.2).sub.p --(Z).sub.q --L--(T).sub.r --M IwhereinA.sup.- is the anion of a strong organic or inorganic acid;XN.sup.+ is pyridinium, pyrimidinium, thiazolium or imidazolium substituted by R.sup.1, R.sup.2 and R.sup.3 ;n, q and r individually are the integer 1 or 0 and p is an integer from 1 to 15;Y is CH.sub.2, C(H,OH) or C(O);Z is O, S, CH.sub.2, C(O), NQ.sup.1, SO.sub.2, C(O)O, OC(O), C(O)N(Q.sup.1) or N(Q.sup.1)C(O);L is p-phenylene substituted by R.sup.4 ; andM is phenyl substituted by R.sup.5 and R.sup.6,T has one of the meanings given above, for Z or is C(CH.sub.3).sub.2, C.sub.2 H.sub.4, C(Q.sup.2).dbd.C(Q.sup.3), C.tbd.C, CH.sub.2 C(O), C(O)CH.sub.2, CH.sub.2 O or OCH.sub.2,R.sup.1 is a group Ar, Ar--C.sub.1-4 -alkyl, ArO or Arc(O),Ar is phenyl substituted by R.sup.7, R.sup.8 and R.sup.9 ;R.sup.2 and R.sup.3 individually are H, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy or C.sub.6 H.sub.
Type:
Grant
Filed:
January 10, 1986
Date of Patent:
September 8, 1987
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
Abstract: This invention provides a benzene-fused heterocyclic compound of the formula: ##STR1## wherein R.sup.1 is halogen, nitro, amino, hydroxy, lower alkyl, lower alkoxy or acylamino,X is --S--, ##STR2## n is an integer of 1 or 2 and A is a group of the formula: ##STR3## in which R.sup.2 is hydrogen, lower alkyl, lower alkynyl, carboxy(lower)alkyl or protected carboxy(lower)alkyl, or pharmaceutically acceptable salts thereof. This compound possesses diuretic, uricosuric, and vasodilative activities and therefore is useful as a diuretic agent, uricosuric agent and anti-hypertensive agent. This invention further provides processes for the preparation of this compound and pharmaceutical composition comprising compound of the above formula.
Abstract: New 3,4-diamino-1,2,5-thiadiazole oxide derivatives which are histamine H.sub.1 -antagonists. A specific compound of this invention is 3-[3-(N-propyl-N-2-pyridylamino)-propylamino]-4-(4-pyridylmethyl)amino-1,2 ,5-thiadiazole-1-oxide.
Type:
Grant
Filed:
March 12, 1986
Date of Patent:
September 8, 1987
Assignee:
Smith Kline & French Laboratories Limited
Abstract: There are disclosed novel 2,6-substituted-3,5-pyridinedicarboxylic acids, esters, salts, amides, halides, and cyano compounds useful as herbicides, and as intermediates which provide herbicides.
Abstract: A method for synthesizing a magenta coupler. The synthesis is carried out through (1) 3-pyrazoline-5-ones which are obtained by substituting a blocking group at the nitrogen atom in the second position thereof; or (2) pyrazoles which are obtained by substituting a blocking group at the hydroxyl group bonded in the fifth position thereof. The magenta coupler obtained has the formula ##STR1## wherein R.sub.1 is an aryl or heterocyclic group, R.sub.2 is an acylamide, anilino or ureido group, and R3 is an alkyl, aryl, or heterocyclic group.
Abstract: Substituted (4-hydroxyphenylthioalkyl) derivatives of the formula ##STR1## are prepared by the reaction of the appropriate ring and hydroxybenzene thiol compounds and are useful stabilizers of organic materials.
Type:
Grant
Filed:
November 23, 1984
Date of Patent:
September 8, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
John D. Spivack, Ramanathan Ravichandran, Stephen D. Pastor
Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl group which may be substituted with hydroxy, lower alkyl or di-lower alkylamino; R.sub.2 is a hydrogen atom, an amino group or a lower alkylamino group; and R.sub.3 is a lower alkyl group, and a non-toxic salt thereof, and a process for preparing the same are disclosed.The compound and the salts thereof exhibit anti-allergic effects by the two different mechanisms and are expected to be useful as drugs for treating allergic diseases such as asthma, pollen allergy, atopic dermatitis and the like.
Abstract: A compound of the formula: ##STR1## wherein X is halogen, lower alkoxy, lower alkylthio, nitro or methyl,Y is hydrogen or chloro,R is hydrogen, lower alkyl or allyl,Z is hydrogen, lower alkyl halogen, nitro, methoxy, methylthio, methylsulfonyl, --CF.sub.3, phenyl, phenoxy or lower alkoxycarbonyl andn is integer of 1-3, their use as fungicide or bactericides.
Abstract: Compounds formula (I): ##STR1## in which: R.sup.1 represents a hydrogen atom, an alkyl group, a substituted alkyl group, a C.sub.2 -C.sub.6 alkenyl group, an aryl group, a substituted aryl group or an alkoxycarbonyl group wherein the alkoxy part has from 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.3 or C.sub.4 alkenyl group; R.sup.3 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.4 represents a hydroxy group, a C.sub.1 -C.sub.21 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.5 represents a C.sub.1 -C.sub.12 alkyl group, a C.sub.1 -C.sub.6 alkoxy group, a hydroxy group, a C.sub.1 -C.sub.7 aliphatic acyloxy group or a carbocyclic aryl carboxylic acyloxy group; R.sup.6 represents a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a C.sub.1 -C.sub.6 alkoxy group; and n is 0, 1, or 2; and pharmaceutically acceptable salts thereof are valuable in the treatment of circulatory disorders and allergies.