Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.
Abstract: A derivative of 3,5,3'-triiodothyronine having the following general formula: ##STR1## in which m is an integer from 2 to 4, n is an integer from 1 to 4, and R is a monovalent, unsubstituted, fully unsaturated five- or six-membered monocyclic heterocyclic group containing either one or two nitrogen atoms as the only hetero atoms.
Abstract: Shown is the process which comprises heating 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid to produce a mixture of 4-(2-fluorophenyl)-2,6-dimethylpyridine and 2,4-dimethyl-5H-[1]benzopyrano[3,4-c]pyridin-5-one, separating the components of said mixture and nitrating 4-(2-fluorophenyl)-2,6-dimethylpyridine to produce 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Also shown are the 3-step synthesis of 4-(2-fluorophenyl)-2,6-dimethyl-3,5-pyridinedicarboxylic acid from 2-fluorobenzaldehyde and the five step synthesis of 1-ethyl-6-fluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-oxo-3-quinolin ecarboxylic acid, a highly potent antibacterial agent, starting with 4-(2-fluoro-5-nitrophenyl)-2,6-dimethylpyridine. Other intermediates shown in said five step synthesis include 3-(2,6-dimethyl-4-pyridinyl)-4-fluorobenzeneamine and diethyl 4-fluoro-3-(2,6-dimethyl-4-pyridinyl)anilinomethylenemalonate.
Abstract: Alpha-L-Aspartyl-D-heteroaromatic-substituted glycine esters and amides are disclosed to be useful as high intensity sweeteners. These compounds can be used to sweeten a variety of foods, beverages and other oral products.
Type:
Grant
Filed:
December 20, 1985
Date of Patent:
September 8, 1987
Assignee:
The Procter & Gamble Company
Inventors:
Robert B. Blum, John M. Gardlik, John M. Janusz, George P. Rizzi
Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.
Type:
Grant
Filed:
February 15, 1985
Date of Patent:
August 11, 1987
Assignee:
Rhone-Poulenc Sante
Inventors:
Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
Abstract: The invention relates to pyrrolinones of formula (1) ##STR1## wherein R.sub.1 is an alkyl group containing at least 2 carbon atoms, an aralkyl group, an isocyclic or heterocyclic aromatic radical and R is an alkyl or aryl group.The invention also relates to aminodicarboxylates of formula (2) ##STR2## wherein R.sub.1 is as defined in claim 1 and R and R' are the same or different and are alkyl or aryl.The aminodicarboxylates of formula (2) are prepared by condensing a disuccinate of the formulaR'OOCCH.sub.2 CH.sub.2 COORwith a nitrile of the formula R.sub.1 CN, in the presence of a strong base and zinc chloride.The pyrrolinones of formula (1) are obtained by reacting the aminodicarboxylates of formula (2) in the presence of a strong base in an organic solvent.The compounds of formulae (1) and (2) are valuable intermediates for pigments.
Type:
Grant
Filed:
November 1, 1985
Date of Patent:
July 21, 1987
Assignee:
Ciba-Geigy Corporation
Inventors:
Johannes Pfenninger, Abul Iqbal, Alain C. Rochat
Abstract: There is described a photographic system wherein development of an exposed photosensitive element with an aqueous alkaline photographic developing composition is effected in the presence of a compound which releases a quaternary in alkaline environment. Photographic products and processes utilizing such compounds are also disclosed.
Abstract: (Arylthio)pyridylalkanol derivatives of the formula: ##STR1## in which: Ar denotes an optionally substituted aryl radical,R denotes a hydrogen atom or an optionally substituted alkyl radical, an optionally substituted aryl radical or an optionally substituted aralkyl radical,R.sub.1 denotes an alkyl radical, and n equals 0, 1, 2, 3 or 4.
Type:
Grant
Filed:
February 26, 1985
Date of Patent:
June 30, 1987
Assignee:
Rhone-Poulenc Agrochimie
Inventors:
Pierre Place, Claude Anding, Jean-Claude Debourge
Abstract: Polycyclic salts of the formulaA-XN+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 15, 1986
Date of Patent:
June 23, 1987
Assignee:
Hoffmann-LaRoche Inc.
Inventors:
Jean-Marie Cassal, Albrecht Edenhofer, Henri Ramuz
Abstract: A 4-cyclohexenylpyridine is brominatively aromatized to the corresponding 4-phenylpyridine by brominating the cyclohexenylpyridine, such as a 4-(halocyclohexenyl)pyridine, especially a 4-(4-halocyclohex-3-enyl)pyridine hydrochloride, and heating the brominated product in the presence or absence of any added base or hydrogen acceptor to form, e.g., a 4-(halophenyl)pyridine. The invention is of particular utility in the manufacture of intermediates of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-(4-pyridyl)-3-quinolinecarboxylic acids.
Type:
Grant
Filed:
March 22, 1985
Date of Patent:
March 10, 1987
Assignee:
Ethyl Corporation
Inventors:
Paul F. Ranken, Venkataraman Ramachandran
Abstract: The disclosure concerns novel 1-benzyl-1,2,3,6-tetrahydropyridine derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or a (1-4C)-alkyl radical, and benzene ring A bears one or two substituents selected from combinations of halogeno, (1-4C)-alkyl, (1-4C)-alkoxy, hydroxy, nitro, cyano, carboxamido, carboxyl, [(1-4C)-alkoxy]carbonyl, hydroxymethylene, amino, (1-4C)-alkanoylamino, (1-4C)-alkylsulphonamido, [(1-4C)-alkoxy]carbonyloxy, (1-4C)-alkanoyloxy and optionally substituted benzoyloxy radicals, and their pharmaceutically acceptable salts; pharmaceutical compositions thereof; analogy processes for their manufacture; and methods of medical treatment employing such derivatives.The compounds of formula I are inhibitors of the aggregation of blood platelets and are of application in the treatment or prophylaxis of thrombosis or occlusive vascular disease.
Abstract: A base precursor represented by the following general formula (A) or (B): ##STR1## wherein A.sub.1, A.sub.2, A.sub.5, A.sub.6, A.sub.7, and A.sub.8 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, an alkenyl group, an aralkyl group, an aryl group, a substituted aryl group, an acyl group, or a heterocyclic group, and A.sub.1 and A.sub.2 can combine to form a ring and two of A.sub.5, A.sub.6, A.sub.7, and A.sub.8 can combine to form a ring, A.sub.3 and A.sub.4 each represents a hydrogen atom, an alkyl group, a substituted alkyl group, a cycloalkyl group, or an aralkyl group, and A.sub.3 and A.sub.4 can combine to form a ring or A.sub.3 and A.sub.4 can be a double bond forming an imino group from ##STR2## and X represents a nucleophilic group.
Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.
Abstract: Compounds of formula I ##STR1## in which n=0 or 1; in which, when n=0, R.sub.1 is H, an alkyl, a cycloalkyl, a cycloalkylmethyl, an alkenyl or, an alkynyl group a heterocyclic ring or an optionally substituted phenyl ring or when n=1, R.sub.1 is H or an alkyl group;in which R.sub.2 and R.sub.3 are H or an alkyl group;in which A is a group of formula III--(CH.sub.2).sub.x --W--(CH.sub.2).sub.y -- IIIin which W is an oxygen atom or a group of formula --S(O).sub.m --, a group of formula --CR.sub.12 R.sub.13 --, a cycloalkylidene group or a cycloalkylene group; x is 0 or an integer from 1 to 5; y is 0 or an integer from 1 to 5.in which R.sub.4 is a carbocyclic ring, a heterocyclic ring, a cyano group, a carbamoyl group, an alkoxycarbonyl group, an amido group, an acyloxy group, a hydroxy group, a thiol group, or a group of formula --OR.sub.20, --SR.sub.20, --SOR.sub.20 or SO.sub.2 R.sub.20.in which R.sub.5, R.sub.6 and R.sub.
Abstract: A process for preparing 1H-pyrrolo-[3,2-c]-pyridine or 5-aza-indole in high yield, comprising condensing 3-methyl-4-nitropyridine-1-oxide with a compound having a formula ##STR1## wherein R represents a di-loweralkylamino, morpholino, piperidino or pyrrolidino group and R.sub.1 and R.sub.2, which are the same or different, each represent a loweralkoxy group or a group R as defined; to form an enamine having a formula: ##STR2## wherein R is as define and subjecting the enamine IV to reduction cyclization; the enamines IV are new compounds.
Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed.
Abstract: Compounds containing a cation of formula Ia ##STR1## and a pharmaceutically acceptable anion are anti-fungal agents. In formula Ia and Ib R.sub.1 is alkyl of at least 3 carbon atoms or aralkyl; R.sub.2 and R.sub.5 are hydrogen, lower alkyl, lower alkoxy, halogen or nitro; R.sub.6 and R.sub.7, when separate, are lower alkyl or aryl(lower)alkyl or, when joined together, are --(CH.sub.2).sub.2 --A--(CH.sub.2).sub.2 -- (where A is --(CH.sub.2).sub.n --, O, S or NR.sub.8 where n is O, 1 or 2 and R.sub.8 is lower alkyl) or a mono- or di-(lower alkyl) substitution product thereof.
Abstract: A 4-cyclohexenylpyridine is brominatively aromatized to the corresponding 4-phenylpyridine by brominating the cyclohexenylpyridine, such as a 4-(halocyclohexenyl)pyridine, especially a 4-(4-halocyclohex-3-enyl)pyridine hydrohalide, and heating the brominated product in an inert solvent and in the presence of a base to form, e.g., a 4-(halophenyl)pyridine. The invention is of particular utility in the manufacture of intermediates of antibacterial 1-alkyl- 1,4-dihydro-4-oxo-7-(4-pyridyl)-3-quinolinecarboxylic acids.
Type:
Grant
Filed:
March 25, 1985
Date of Patent:
August 5, 1986
Assignee:
Ethyl Corporation
Inventors:
Venkataraman Ramachandran, Paul F. Ranken
Abstract: The distyrylbiphenyls of the formula ##STR1## in which X and X' independently of one another are a direct bond, oxygen, sulfur, --O--C.sub.1-3 -alkylene-CON(R.sub.4)--CON(R.sub.4)--, --O--C.sub.1-3 alkylene-COO--, OCO or --COO--, with the proviso that if n+n'=O, X and X' may not be --CON(R.sub.4)-- or O--C.sub.1-3 -alkylene-CON(R.sub.4)--, and if n+n'=2 and X and X' are --CON(R.sub.4)-- or --COO--, A.sup..crclbar. may not be a phosphite or phosphonate anion, and Y and Y' independently of one another are C.sub.1-20 -alkyene, R.sub.1 and R.sub.1 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, R.sub.1 together with R.sub.2, or R.sub.1 ' together with R.sub.2 ', is a heterocyclic ring, R.sub.2 and R.sub.2 ' independently of one another are unsubstituted or substituted C.sub.1-8 -alkyl or C.sub.3-4 -alkenyl, or R.sub.2 together with R.sub.1, or R.sub.2 ' together with R.sub.1 ', is a heterocyclic ring, or R.sub.1 and R.sub.2, or R.sub.1 ' and R.sub.
Type:
Grant
Filed:
May 18, 1984
Date of Patent:
July 22, 1986
Assignee:
Ciba-Geigy Corporation
Inventors:
Christian Luthi, Hans R. Meyer, Kurt Weber
Abstract: Compounds of the formula: ##STR1## where R.sup.1 is halogen or nitro; R.sup.2 is C.sub.1-4 alkyl; and R.sup.3 is a C.sub.1-3 alkylene group are intermediates to 2-(3,5-disubstituted pyridyl-alkyl amino)-5-pyridylmethyl-4-pyrimidone derivatives which are useful as histamine H.sub.1 -antagonists.
Type:
Grant
Filed:
September 17, 1984
Date of Patent:
April 22, 1986
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Hypoglycemic 5-chromanyl, 2,3-dihydro-5-benzo[b]-furanyl, 5-pyridyl, 5-quinolyl, 5-pyrrolyl, 5-indolyl, 5-thiazolyl, 5-oxazolyl, 5-isothiazolyl and 5-isoxazolyl oxazolidine-2,4-diones and the pharmaceutically-acceptable salts thereof; certain 3-acylated derivatives thereof; a method of treating hyperglycemic animals therewith; and intermediates useful in the preparation of said compounds.
Abstract: Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is H or ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of 3-hydroxyphenyl, 4-hydroxyphenyl, 3-pyridyl, 4-pyridyl, ##STR3## where X is S, O or NH; and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.
Abstract: Novel dyestuffs of the general formula ##STR1## wherein R designates a lower alkyl or alkenyl radical andR.sup.1 and R.sup.2 designate lower alkyl or alkenyl radicals which, together with the nitrogen atom to which they are bonded, can form a 5-membered or 6-membered heterocyclic ring,and whereinR, R.sup.1 and R.sup.2 can be substituted by non-ionic radicals, and at least one of the radicals R, R.sup.1 and R.sup.2 is substituted by an aryl radical, directly or via a bridge, orone of the radicals R.sup.1 or R.sup.2 represents an aryl radical, the ring a can be substituted by 1 or 2 methyl or ethyl radicals,the ring b can be substituted by 1 or 2 methyl, ethyl, methoxy or ethoxy radicals or by 1 halogen atom andAn.sup.- represents an anion,are particularly suitable for dyeing paper.
Abstract: New substituted 2,2-dimethyl-5-phenoxypentanoic acid benzamides which are useful as anti-arteriosclerotic agents are disclosed. These compounds elevate the high density lipoprotein fraction of cholesterol, and also lower the low density lipoprotein fraction of cholesterol.
Abstract: 4-(Bromophenyl)pyridines, useful in preparing bactericides, are prepared by reacting a 4-phenylpyridine with bromine in the presence of an excess of a Lewis acid catalyst, preferably aluminum chloride.
Abstract: A 4-(1-chlorovinyl)pyridine, preferably 4-(1-chlorovinyl)pyridine itself, is reacted with a butadiene, preferably chloroprene, to prepare a 4-(1-chlorocyclohex-3-enyl)pyridine. The preferred products are useful as intermediates in the preparation of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.
Abstract: The yield of Diels-Alder product obtained by reacting a haloprene with a 4-vinylpyridine is increased by conducting the reaction in the presence of a boron trifluoride catalyst, preferably a boron trifluoride etherate. The product obtained by the reaction, a mixture of 4-(chlorocyclohex-3-enyl)pyridines, is useful in the production of antibacterial 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids.
Abstract: Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.
Abstract: Diels-Alder products obtained by reacting a haloprene with a 4-vinylpyridine, i.e., mixtures of 4-(halocyclohex-3-enyl)pyridine isomers, are reacted with a relatively strong acid, i.e., an acid having a dissociation constant of at least 1.7.times.10.sup.-5 at 25.degree. C., to form salts which are readily separated and/or reduced.
Abstract: Disclosed are novel condensed diazepinones of formula I ##STR1## wherein B is a fused ring selected from ##STR2## X is --CH-- or, when B is ortho-phenylene, X can also be nitrogen; A.sub.1 is C.sub.1 -C.sub.2 alkylene; A.sub.2 is C.sub.1 -C.sub.2 when it is in the 2-position relative to the saturated heterocyclic ring nitrogen or a single bond or methylene when it is in the 3- or 4-position; R.sub.1 is C.sub.1 -C.sub.3 alkyl; R.sub.2 is C.sub.1 -C.sub.7 alkyl, optionally hydroxy-substituted on at least one of its second to seventh carbon, or C.sub.3 -C.sub.7 cycloalkyl, optionally hydroxy substituted, or C.sub.3 -C.sub.7 cycloalkylmethyl; or R.sub.1 and R.sub.2 can, together with the nitrogen therebetween, be a 4- to 7-membered saturated monocyclic, heterocyclic ring which can optionally include an oxygen or N--CH.sub.3 ; R.sub.3 is hydrogen, chlorine, or methyl; R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.5 is hydrogen, chlorine or C.sub.1 -C.sub.
Type:
Grant
Filed:
March 14, 1985
Date of Patent:
October 29, 1985
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfhard Engel, Gunter Trummlitz, Wolfgang Eberlein, Gerhard Mihm, Gunther Schmidt, Rudolf Hammer, Antonio Giachetti
Abstract: 4-(3-Aminophenyl)pyridines, useful in the preparation of 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids, are prepared by heating a 2-amino-4-(4-pyridinyl)benzoic acid at decarboxylation temperatures.
Abstract: The invention provides a process for preparing 2-pyridylalkylamines by reacting an alkali metal derivative of a 2-methylpyridine with a haloalkylamine. The compounds are useful as intermediates in the preparation of compounds having histamine H.sub.1 - and H.sub.2 -antagonist activity.
Type:
Grant
Filed:
March 22, 1983
Date of Patent:
July 2, 1985
Assignee:
Smith Kline & French Laboratories Limited
Inventors:
Brian M. Adger, Antonietta R. Mastrocola
Abstract: The invention provides a process for preparing 2-pyridylalkylamines, substituted in one of the 3- or 5-positions by bromo and in the other by C.sub.1-4 alkyl, by reacting an appropriate C.sub.1-4 alkyl substituted 2-pyridylalkylamine with an electrophilic brominating agent. Said 2-pyridylalkylamines are useful as intermediates in the synthesis of compounds useful as histamine H.sub.1 -antagonists.
Type:
Grant
Filed:
March 22, 1983
Date of Patent:
May 7, 1985
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Novel substituted phenylphosphinyloxy- and phenylphosphinylthio-iminocarboxylates, synthesis thereof, intermediates therefor, and the use of said novel compounds for the control of weeds.
Abstract: 3-Methyl-4-(4-pyridinyl)benzeneamines, useful as cardiotonic agents, are prepared by reaction of pyridine, benzoyl chloride and an appropriate 3-methyl-N,N-di-lower-alkylbenzeneamine in the presence of copper powder and decomposing the reaction mixture with alkali and, if desired, reacting a resulting 3-methyl-4-(4-pyridinyl)N,N-di-lower-alkylbenzeneamine with hydrogen bromide and pyridine to obtain 3-methyl-4-(4-pyridinyl)benzeneamine.
Abstract: The present invention provides a multistep process for the preparation of .beta.-cyclo-substituted ethylamines of the general formula:-Ar--CH.sub.2 --CH.sub.2 --NH.sub.2 (I)in which AR is a heterocyclic or non-heterocyclic aromatic radical, which is optionally mono- or poly- substituted, wherein said compounds represent a class of intermediates which can be converted to 4,5,6,7-tetrahydro[3,2-C] or [2,3-C]pyridines wherein the latter are useful for anti-inflammatory, vasodilator or blood platelet aggregation inhibition activities.
Abstract: The present invention provides novel 2-, 3-, or 4-pyridinylmethylamino arylic acids which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and 5-lipoxygenase inhibitors and as such represent useful pharmacological agents.
Abstract: 2-And/or 6-pyridylethylamino-substituted fluorans useful as color formers, particularly in pressure-sensitive carbonless duplicating systems and thermal-responsive marking systems are prepared by the interaction of (pyridylethylaminophenyl)carbonylbenzoic acids with 4-hydroxy- or alkoxyanilines or by the interaction of (disubstituted aminophenyl)carbonylbenzoic acids with N-pyridylethyl-4-hydroxy- or alkoxy acetanilides. The (pyridylethylaminophenyl)carbonylbenzoic acid intermediates required for the fluorans are prepared by interacting a N-pyridylethyl-3-hydroxyaniline with a substituted or unsubstituted phthalic anhydride. The N-pyridylethyl-4-hydroxy- or alkoxyanilines and the N-pyridylethyl-3-hydroxyanilines are prepared by interacting the respective aniline with a vinylpyridine.
Abstract: Novel 4-aryl-or heteroaryl-2,6-bis[(substituted-amino)phenyl]pyridines which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting a 2-, 3- or 4-R.sub.1 R.sub.2 N-acetophenone with an aryl or heteroaryl aldehyde in the present of ammonia or an ammonia-releasing agent.
Abstract: This invention relates to 4-substituted aminomethyl pyridines with a butanamine, oxypropioamine or thiomethylamine substituent at the 2 position. The compounds are reacted with pyridones to form compounds which have histamine H.sub.2 -antagonist activity.
Type:
Grant
Filed:
February 16, 1983
Date of Patent:
March 27, 1984
Assignee:
Smith Kline & French Laboratories Limited
Abstract: 3-Methyl-4-(4-pyridinyl)benzeneamines, useful as cardiotonic agents, are prepared by reaction of pyridine, benzoyl chloride and an appropriate 3-methyl-N,N-di-lower-alkylbenzeneamine in the presence of copper powder and decomposing the reaction mixture with alkali and, if desired, reacting a resulting 3-methyl-4-(4-pyridinyl)-N,N-di-lower-alkylbenzeneamine with hydrogen bromide and pyridine to obtain 3-methyl-4-(4-pyridinyl)benzeneamine.
Abstract: This invention relates to 2-amino-4-pyrimidone derivatives, in which the amino group is substituted by a methylthioethyl, butyl or oxypropyl group bearing a terminal 4-dialkylaminomethyl-2-pyridyl group. The compounds have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(4-dimethylaminomethyl-2-pyridylmethylthio)ethylamino]-5-(6-methyl-3- pyridylmethyl)-4-pyrimidone.
Type:
Grant
Filed:
September 16, 1981
Date of Patent:
May 24, 1983
Assignee:
Smith Kline & French Laboratories Limited
Abstract: Chiral Schiff bases according to the general formula: ##STR1## and transition metal complexes thereof, wherein C.sup.* is an asymmetric carbon atom, R.sup.1 and R.sup.2, which may be the same or different are alkyl, aralkyl, aryl or alkaryl, R.sup.3 is hydrogen, alkyl, aralkyl, aryl or alkaryl, R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or lower alkyl or, where n is 1, may with the cyclic ring to which CR.sup.4 R.sup.
Abstract: New derivatives of 1,2-ethylenediamine and salts thereof endowed with vascular antispasmodic and antiallergic activity; processes for preparing them, some new intermediates useful in their preparation and pharmaceutical compositions containing them.
Abstract: This invention relates to new decaprenylamines and the acid addition salts thereof, which are useful for controlling virus infection of vertebrate animals.
Abstract: Disclosed and claimed are a cardiac composition and a method for increasing cardiac contractility using an effective amount of a cardiotonic 4-[4-(or 3)-AcNH-phenyl]-2-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -pyridine (I) or pharmaceutically-acceptable salt thereof, where R.sub.2 is hydrogen, methyl, ethyl or hydroxyl, R.sub.6 is hydrogen, methyl or ethyl, R.sub.3 and R.sub.5 are each hydrogen or methyl, and Ac is hydrogen, hydroxyacetyl, acetoxyacetyl, .alpha.-hydroxypropionyl, .alpha.-acetoxypropionyl, methyoxyacetyl, 2-butenoyl or carbamyl or when NHAc is attached to the 4-position of the phenyl ring Ac also is formyl, n-propanoyl, 2,2-dimethyl-n-propanoyl or 3-carboxypropanoyl or when NHAc is attached to the 3-position of the phenyl ring Ac also is acetyl. Novel compounds shown and claimed are 4-[4-(or 3)-Ac'NH-phenyl]-2-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -pyridines (II) or pharmaceutically-acceptable acid-addition salts thereof, where R.sub.2, R.sub.3, R.sub.5 and R.sub.
Abstract: Novel 4-aryl-or heteroaryl-2,6-bis[(substituted-amino)phenyl]pyridines which are useful as color formers in pressure-sensitive carbonless duplicating systems and thermal marking systems are prepared by reacting a 2-, 3- or 4-R.sub.1 R.sub.2 N-acetophenone with an aryl or heteroaryl aldehyde in the present of ammonia or an ammonia-releasing agent.