Additional Hetero Ring Containing Patents (Class 544/96)
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Patent number: 4785016Abstract: Indole derivatives are disclosed of formula (I): ##STR1## wherein R.sub.1 represents H, alkyl or alkenyl;R.sub.2 represents H, alkyl, alkenyl, cycloalkyl or phenyl or phenyl alkyl the phenyl ring being optionally substituted by halogen, alkyl, alkoxy, hydroxyl or by a group --NR.sub.a R.sub.b, or --CONR.sub.a R.sub.b, wherein R.sub.a and R.sub.b are H, alkyl, alkenyl, or with the nitrogen atom form a saturated monocyclic ring;R.sub.3 and R.sub.4 are H, alkyl or propenyl or together form an aralkylidene group;Alk represents a Cf.sub.2-3 alkyl chain optionally substituted by one or two alkyl groups; andA.sup.1 represents a C.sub.2-5 alkenyl chain and salts and solvates thereof.The compounds have selective vasoconstrictor activity and are useful in treating and/or preventing pain resulting from dilatation of the cranial vasculature, particularly migraine. The compounds may be formulated in conventional manner with pharmaceutically acceptable carriers or excipients.Type: GrantFiled: December 3, 1985Date of Patent: November 15, 1988Assignee: Glaxo Group LimitedInventors: Brian Evans, Alexander W. Oxford, Darko Butain
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Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
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Patent number: 4772706Abstract: An improved process for the preparation of 7-substituted amino-1-alkyl- or cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1-cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxoquinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product.Type: GrantFiled: January 13, 1986Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventors: James N. Wemple, James R. Zeller, John M. Domagala
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4767443Abstract: There are described novel, microbicidally active 5-(arylmethylimino)-pyrimidines of the formula I ##STR1## wherein R.sub.n --A-- is an unsubstituted or substituted phenyl, naphthyl, biphenyl, phenoxyphenyl or phenylthiophenyl, and R.sub.1 is an ether, thioether or amino function, these substances being produced according to the invention by substitution of the halogen atom in the claimed intermediates of the formula II ##STR2## The use of these substances in plant protection, and also further important intermediates, are likewise described.Type: GrantFiled: September 13, 1985Date of Patent: August 30, 1988Assignee: Ciba-Geigy CorporationInventors: Helmut Zondler, Wolfgang Eckhardt, Robert Nyfeler
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Patent number: 4762550Abstract: This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.Type: GrantFiled: August 13, 1987Date of Patent: August 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Stephen L. Hartzell
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Patent number: 4759790Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.Type: GrantFiled: May 21, 1987Date of Patent: July 26, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joel R. Christensen
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Patent number: 4755599Abstract: 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 6 C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.Type: GrantFiled: February 3, 1987Date of Patent: July 5, 1988Assignee: Rhone-Poulenc SanteInventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
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Patent number: 4743294Abstract: A selective herbicide of the formula ##STR1## in which m is 0, 1 or 2,R.sup.5 is an organic radical,R.sup.3 is hydrogen or an organic radical,R.sup.9 is hydrogen or an optionally substituted alkyl radical,R.sup.10 is an organic radical or forms a ring with R.sup.9,R.sup.40 and R.sup.41 are alkyl or alkoxy, andM is hydrogen or a metal or ammonium radical, or an acid adduct thereof.Type: GrantFiled: April 22, 1987Date of Patent: May 10, 1988Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt, Koichi Moriya, Ludwig Eue, Klaus Lurssen
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Patent number: 4740231Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.Type: GrantFiled: May 22, 1986Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4737500Abstract: Thiazoles or pharmaceutically acceptable acid addition salts thereof are useful as anxiolytic, psychogeriatric, antidepressant and antischizophrenic agents.Type: GrantFiled: June 20, 1986Date of Patent: April 12, 1988Assignee: Sandoz Pharm. Corp.Inventor: Dieter Sorg
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Patent number: 4735942Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3 dioxolan-2-yl]methyl]-1H-imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.Type: GrantFiled: June 2, 1986Date of Patent: April 5, 1988Assignee: Janssen Pharmaceutica, N.V.Inventors: Jan Heeres, Raymond A. Stokbroekx, Leo J. J. Backx
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Patent number: 4732898Abstract: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.Type: GrantFiled: March 3, 1987Date of Patent: March 22, 1988Assignee: Warner-Lambert CompanyInventors: Edward W. Badger, Michael D. Taylor
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Patent number: 4725679Abstract: The novel 2-amino-alkenylsulfonylureas of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 denote hydrogen, alkyl, cycloalkyl or (substituted) phenyl, or R.sub.1 and R.sub.2, together with the common nitrogen atom, form a 5-membered to 7-membered (hetero)aliphatic ring, R.sub.3 denotes hydrogen, cycloalkyl, alkyl, alk(en)(yn)yloxy, alkylsulfen(in)(on)yl, --SO.sub.2 (N)(mono- or di-alkyl), (substituted) phenyl, benzyl, substituted hydroxycarbonyl or (substituted) aminocarbonyl, R.sub.4 has the meaning of R.sub.3 and additionally denote formyl, alkanoyl, (substituted) benzoyl, cycloalkylcarbonyl or C.sub.6 H.sub.5 --CH.sub.2 --O--CO--, or R.sub.3 and R.sub.4, together with the olefinic carbon atoms connecting them, form a 5-membered to 8-membered aliphatic ring system, R.sub.5 denotes H, alkyl, alkenyl, alkynyl, alkoxy or alkoxycarbonyl and R.sub.Type: GrantFiled: February 7, 1986Date of Patent: February 16, 1988Assignee: Hoechst AktiengesellschaftInventor: Lothar Willms
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Patent number: 4725305Abstract: Herbicidally active novel N,N'-bis-sulphonyl guanidines of the formula ##STR1## in which M is hydrogen, a metal or an ammonium radical, andR.sup.4, R.sup.5, R.sup.40 and R.sup.41 are various organic radicals.Type: GrantFiled: November 14, 1986Date of Patent: February 16, 1988Assignee: Bayer AktiengesellschaftInventors: Koichi Moriya, Theodor Pfister, Hans-Jochem Riebel, Ludwig Eue, Robert R. Schmidt, Klaus Lurssen, Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Uwe Priesnitz, Wolfgang Roy, Hans-Joachim Santel
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Patent number: 4723988Abstract: Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophen esulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: March 27, 1987Date of Patent: February 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Rafael Shapiro
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Patent number: 4715984Abstract: Dihydroazines of the formula IR.sub.1 --A.sup.1 --Z.sub.1 --A.sub.2 --R.sup.2 Iwherein R.sup.1, R.sup.2, A.sup.1, A.sup.2 and Z.sub.1 have the meanings specified herein may be used as components of liquid crystalline phases.Type: GrantFiled: January 22, 1986Date of Patent: December 29, 1987Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Joachim Krause, Wachtler, Bernhard Scheuble
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Patent number: 4713456Abstract: A process for the preparation of a 5-acylpyrimidine of the formula ##STR1## in which R is an organic radical comprising reacting a methyl ketone of the formulaR--CO--CH.sub.3in a first stage with a formylating reagent in the presence of a base to form an enolketone of the formulaR--CO--CH.dbd.CH--OR.sup.10in which R.sup.10 represents hydrogen or a base radical, thereafter reacting the enolketone in 2nd and 3rd stages with formamidine or a formamidine salt, and with an amino-formylating agent, and, in a 4th stage heating to cyclize the compound formed.The end products, some of which are new, are intermediates for making herbicides.Type: GrantFiled: August 26, 1985Date of Patent: December 15, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Graham Holmwood
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Patent number: 4710500Abstract: The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses and, at the same time, a low degree of undesired side effects.Moreover, the invention relates to methods for the preparation of said indole derivatives, pharmaceutical compositions containing same, and methods for the treatment of psychic disorders, especially psychoses, by administering a therapeutically active amount of one of said derivatives to a living animal body, including human beings.The novel indole derivatives of the present invention are represented by the following formula: ##STR1## wherein R is phenyl, optionally substituted with halogen, lower alkyl or trifluoromethyl, or a hetero aromatic group, such as 2-thienyl, 3-thienyl, 2-furoyl, 3-furoyl, 2-thiazol, 2-oxazol, 2-imidazole, 2-pyridyl, 3-pyridyl or 4-pyridyl; R.sup.Type: GrantFiled: April 1, 1986Date of Patent: December 1, 1987Assignee: H. Lundbeck A/SInventor: Jens K. Perregaard
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Patent number: 4707479Abstract: 1,4-Dihyropyridinecarboxamides of the formula ##STR1## and salts thereof, are effective for treating cardiac insufficiency, thromboses, thromboembolisms and ischaemias, for influencing the blood-sugar level and the circulation and as coronary therapeutic agents and anti-arrhythmic agents.Type: GrantFiled: December 5, 1985Date of Patent: November 17, 1987Assignee: Bayer AktiengesellschaftInventors: Horst Meyer, Gerhard Franckowiak, Ulrich Rosentreter, Rainer Gross, Gunter Thomas, Matthias Schramm, Michael Kayser, Friedel Seuter, Elisabeth Perzborn, Martin Bechem
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Patent number: 4699647Abstract: This invention relates to herbicidal benzene sulfonamides containing a five or six membered heterocyclic ring consisting of 2-3 heteroatoms and 1-2 carbonyl groups as a substituent on benzene.Type: GrantFiled: March 27, 1986Date of Patent: October 13, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4696927Abstract: This invention relates to 4-(2-pyrimidinyl)-1-piperazinyl heterocyclic carbonyl derivatives, to a process for their preparation, and to their use as anxiolytic agents.Type: GrantFiled: December 17, 1986Date of Patent: September 29, 1987Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Maurice W. Gittos, Marcel Hibert
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Patent number: 4689414Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.Type: GrantFiled: February 24, 1986Date of Patent: August 25, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4684650Abstract: The present invention relates to indane derivatives with the following formula: ##STR1## wherein R.sub.1 is H, Halogen, an alkyl group having from one to three carbon atoms inclusive, methoxy, a methylthio-group, or a trifluoromethyl group,n is 2-4X is O or S,Y is O, CH.sub.2 or N--R.sub.2, where R.sub.2 is hydrogen or an (1-6 C) alkyl, (2-6 C) alkenyl or cycloalkyl-methyl group having from three to six carbon atoms,Z is --(CH.sub.2).sub.n --, n is 2 or 3 or Z is 1,2-phenylene optionally substituted with halogen or trifluoromethyl or Z=1,2--C.sub.6 H.sub.4 CO-- (to form a quinazolidinone or -thione ring system). U=N or C.Each compound exists as geometric isomers and each of these as a pair of optical isomers; and the separation and isolation of these are also within the scope of the invention.Moreover, pharmaceutically acceptable acid addition salts of the compounds of Formula I are within the scope of the present invention.Type: GrantFiled: October 10, 1985Date of Patent: August 4, 1987Assignee: H. Lundbeck A/SInventor: Klaus P. Bogeso
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Patent number: 4684656Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.Type: GrantFiled: March 14, 1986Date of Patent: August 4, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4683228Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.Type: GrantFiled: January 22, 1985Date of Patent: July 28, 1987Assignees: ICI Americas Inc., Imperial Chemical Industries PLCInventors: Karin M. Kirkland, Derrick M. Mant
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Patent number: 4672062Abstract: 3-amino-2,3-dihydro-1-benzoxepine compounds corresponding to the general Formula I ##STR1## wherein R.sub.1 and R.sub.2 may each be hydrogen, halogen, lower alkyl or lower alkoxy, or if one of R.sub.1 and R.sub.2 is hydrogen, the other may also be nitro or trifluoromethyl, R.sub.3 represents hydrogen or a lower alkyl group which optionally may be substituted by hydroxy, lower alnoxy, an optionally substituted phenyl group or an optionally substituted amino group, and R.sub.4 represents hydrogen or lower alkyl, or R.sub.3 and R.sub.4 together with the nitrogen atom form a 5 or 6 member heterocycle. The compounds exhibit pharmacological, especially antidepressive, activity.Type: GrantFiled: November 4, 1985Date of Patent: June 9, 1987Assignee: Kali-Chemie Pharma GmbHInventors: Heinrich-Wilhelm Ohlendorf, Michael Ruhland, Klaus-Ullrich Wolf
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Patent number: 4668690Abstract: This invention relates to 1,2,3,4,4a,9b-hexahydro-4a-aminoalkyldibenzofurans of the formula ##STR1## where X is hydrogen, loweralkyl, F and Cl; R.sub.1 is hydrogen, loweralkyl, arylloweralkyl, loweralkenyl, loweralkoxyloweralkyl, aryloxyloweralkyl, cycloalkylloweralkyl and heteroarylloweralkyl: R.sub.2 is hydrogen, lower alkyl or R.sub.1 and R.sub.2 taken together with the N ring atom constitute a saturated or unsaturated heterocyclic ring having 5 or 6 members; R.sub.3 is hydrogen, lower alkyl; n is an interger of 1 to 3; and the pharmaceutically acceptable acid addition salts thereof and where applicable the stereo, optical and geometrical isomers of the foregoing.Type: GrantFiled: December 30, 1985Date of Patent: May 26, 1987Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventor: Gregory M. Shutske
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Patent number: 4668279Abstract: Novel pyridinesulfonamide compounds containing ortho-heterocyclic substituents such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-(1H-1,2,4-triazol-1-yl)-3 -pyridinesulfonamide display utility as herbicides and plant growth regulants.Type: GrantFiled: April 22, 1985Date of Patent: May 26, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4666902Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.Type: GrantFiled: June 8, 1984Date of Patent: May 19, 1987Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
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Patent number: 4665177Abstract: This invention relates to new tetrahydropyrimidines, to a process for their production and to their use as catalysts in the production of polyurethane plastics, including polyurethane foams.Type: GrantFiled: August 5, 1985Date of Patent: May 12, 1987Assignee: Bayer AktiengesellschaftInventors: Werner Rasshofer, Gerhard Grogler, Richard Kopp
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Patent number: 4652649Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.Type: GrantFiled: February 20, 1985Date of Patent: March 24, 1987Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4647557Abstract: This invention relates to novel heterocyclic derivatives bearing an amino group and to processes for making said compounds.More particularly this invention provides novel heterocyclic compounds the hetero ring of which has two hetero atoms, the same or different, substituted with a free or substituted amino group.These compounds are useful as active ingredients of drugs.Type: GrantFiled: December 23, 1983Date of Patent: March 3, 1987Inventors: Gerard Moinet, Michel Schaeffer, Pierre Bessin, Jacqueline Bonnet
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Patent number: 4640800Abstract: This invention provides a novel class of quinodimethane compounds which can exhibit nonlinear optical response.Type: GrantFiled: June 25, 1985Date of Patent: February 3, 1987Assignee: Celanese CorporationInventors: Eui W. Choe, Alan Buckley, Anthon F. Garito
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Patent number: 4639436Abstract: The invention includes certain 3,4,5-trihydroxypiperidine compounds, methods for their preparation, compositions containing said 3,4,5-trihydroxypiperidine compounds and methods for the use of said compounds and compositions.The subject matter of the invention is useful against diabetes, hyperlipaemia and adiposity as well as in animal nutrition.Type: GrantFiled: August 23, 1978Date of Patent: January 27, 1987Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Hans P. Krause, Lutz Muller, Walter Puls
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Patent number: 4638066Abstract: Compounds of formula (I), ##STR1## or an N-oxide or pharmaceutically acceptable salt thereof, wherein R.sub.1 is hydrogen, C.sub.1-7 alkyl, C.sub.3-7 cycloalkyl, C.sub.4-7 cycloalkenyl or C.sub.1-4 alkyl substituted by C.sub.2-7 alkenyl, C.sub.2-7 alkynyl, C.sub.3-7 cycloalkyl, hydroxy, thiol, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, carboxy, C.sub.1-4 alkoxycarbonyl, C.sub.1-4 alkanoyl, amino optionally substituted by one or two C.sub.1-4 alkyl or by C.sub.4-6 polymethylene optionally containing an oxygen or nitrogen atom, aminocarbonyl optionally N-substituted by one or two C.sub.1-4 alkyl, or benzoyl or phenyl either being optionally ring-substituted by C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or trifluoromethyl, R.sub.2 and R.sub.3 are the same or different and are hydrogen, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen or trifluoromethyl, m is 1 to 3 and n is 1 or 2, the hydrogen atom bonded to the C.sub.a carbon atom being trans to the hydrogen atom bonded to the C.sub.Type: GrantFiled: December 20, 1984Date of Patent: January 20, 1987Assignee: Beecham Group p.l.c.Inventors: Laramie M. Gaster, Barry S. Orlek
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Patent number: 4631276Abstract: Compounds of Formula I ##STR1## wherein R.sub.1 is a prostaglandin or prostacyclin residue;Y is oxygen, sulfur, imino, or N-(C.sub.1 -C.sub.4 -alkyl) imino;Q is (CR.sub.6 R.sub.7).sub.p wherein p is an integer of 0 to 3;R.sub.2 is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; C.sub.1 -C.sub.4 -alkoxycarbonyl; benzyloxycarbonyl; cyano; or di-C.sub.1 -C.sub.4 -alkylamino-carbonyl;R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 each independently is hydrogen; alkyl of 1-6 carbon atoms optionally substituted by hydroxy or amino; or aryl; andR.sub.3 and R.sub.4 together form a trimethylene, tetramethylene, or 1,3-butadienylene group when R.sub.2 and R.sub.5 together represent a direct bond;have valuable pharmacological properties, e.g., as blood-pressure-lowering or abortive agents.Type: GrantFiled: July 3, 1984Date of Patent: December 23, 1986Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Walter Elger, Michael-Harold Town, Ekkehard Schillinger
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Patent number: 4629495Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.Type: GrantFiled: July 13, 1983Date of Patent: December 16, 1986Assignee: May & Baker LimitedInventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts
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Patent number: 4616002Abstract: Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.Type: GrantFiled: January 6, 1986Date of Patent: October 7, 1986Assignee: Ciba-Geigy CorporationInventors: Bruno Kamber, Thomas Leutert, Hans Kuhnis, Kurt Eichenberger
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Patent number: 4607031Abstract: An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4.The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.Type: GrantFiled: May 22, 1985Date of Patent: August 19, 1986Assignee: Kanebo Ltd.Inventors: Koichiro Yoshino, Tominori Morita, Masaru Moriyama, Keizo Ito, Goro Tsukamoto
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Patent number: 4602940Abstract: This invention relates to ortho-heterocyclic benzene sulfonylureas which are useful as herbicides and growth regulants.Type: GrantFiled: May 20, 1985Date of Patent: July 29, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Anthony D. Wolf
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Patent number: 4595539Abstract: Certain 2-substituted-2-penem-3-carboxylic acid compounds and pharmaceutically-acceptable salts thereof can be prepared from the appropriate xanthate or trithiocarbonate by desulfurization and addition of an electrophilic sulfur compound followed by halogenation and ring closure. The corresponding desulfurized and halogenated olefinic intermediates are disclosed.Type: GrantFiled: June 10, 1983Date of Patent: June 17, 1986Assignee: Pfizer Inc.Inventor: Ernest S. Hamanaka
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Patent number: 4576749Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).Type: GrantFiled: April 13, 1984Date of Patent: March 18, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
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Patent number: 4567276Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.Type: GrantFiled: June 13, 1983Date of Patent: January 28, 1986Assignee: Merck & Co., Inc.Inventor: John J. Baldwin
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Patent number: 4556654Abstract: Substituted anthra[1,9-cd]pyrazol-6(2H-ones have antimicrobial activity. Methods for their preparation, use and pharmaceutical compositions are disclosed.Type: GrantFiled: June 28, 1983Date of Patent: December 3, 1985Assignee: Warner-Lambert CompanyInventors: Howard D. H. Showalter, Judith L. Johnson, Leslie M. Werbel, Edward F. Elslager
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Patent number: 4556658Abstract: The invention relates to 7-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-quinoline-3-carboxyli c acids, processes for their preparation and compositions containing them as antibacterial agents. Also included in the invention are methods for treating bacterial infection using the compounds and compositions of the invention.Type: GrantFiled: April 24, 1984Date of Patent: December 3, 1985Assignee: Bayer AktiengesellschaftInventors: Klaus Grohe, Uwe Petersen, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4555261Abstract: This invention relates to a novel class of sulfonamides and their use as herbicides and plant growth regulants.Type: GrantFiled: November 1, 1984Date of Patent: November 26, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Wallace C. Petersen
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Patent number: 4521597Abstract: A novel process for producing sulfonylureas of the formula I having a herbicidal action and an action regulating plant growth ##STR1## wherein A is an unsubstituted or substituted phenyl, naphthyl, furan, thiophene or pyridine group, E is a nitrogen atom or the methine group, R.sub.a is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -haloalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -haloalkoxy, C.sub.1 -C.sub.5 -alkylthio or C.sub.2 -C.sub.10 -alkoxyalkoxy, and R.sub.b is the same as R.sub.Type: GrantFiled: October 14, 1983Date of Patent: June 4, 1985Assignee: Ciba Geigy CorporationInventors: Haukur Kristinsson, Werner Topfl
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Patent number: 4521599Abstract: This invention relates to the use of 6-aryluracils as antiinflammatory and antiarthritic agents and also to both novel intermediates and novel processes for the preparation of selected 6-aryluracils.Type: GrantFiled: September 17, 1984Date of Patent: June 4, 1985Assignee: The Upjohn CompanyInventors: Harvey I. Skulnick, Herman W. Smith, Robert J. Smith, Wendell Wierenga
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Patent number: 4515946Abstract: This invention relates to 6,11-dihydro-11-oxo-dibenz[b,e]oxepin derivatives of the formula ##STR1## where Y is alkyl, alkoxy, halogen or trifluoromethyl, n is 0, 1, 2 or 3; R is ##STR2## where Hal is a halogen; ##STR3## where n is 0, 1, 2 or 3; p is 1 or 2; q is 0, 1, or 2; R.sup.1 to R.sup.7 are the same or different and are hydrogen and alkyl and R.sup.8 is hydrogen, alkyl and phenyl; and R.sup.9 is alkyl and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: December 23, 1981Date of Patent: May 7, 1985Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Lawrence L. Martin, Linda L. Setescak