Chalcogen Bonded Directly To Ring Carbon Of The Oxazole Ring Patents (Class 548/225)
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Patent number: 5063208Abstract: A renin inhibiting compound having an aminodiol functional group is useful for treating hypertension, congestive heart failure and glaucoma and inhibits retroviral protease.Type: GrantFiled: June 29, 1990Date of Patent: November 5, 1991Assignee: Abbott LaboratoriesInventors: Saul H. Rosenberg, Kenneth P. Spina, Steven R. Crowley
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Patent number: 5043454Abstract: 1-Aryl- and 1-hetarylimidazolecarboxylic esters of the general formulae Ia and Ib ##STR1## where R.sup.1 is halogen or substituted or unsubstituted C.sub.1 -C.sub.4 -alkyl;R.sup.2 is substituted or unsubstituted C.sub.1 -C.sub.6 -alkyl; C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl or C.sub.3 -C.sub.6 -cycloalkyl;R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.4 is substituted or unsubstituted phenyl or 5- or 6-membered heteroaromatic,processes for their manufacture, and agents containing them.Type: GrantFiled: January 9, 1990Date of Patent: August 27, 1991Assignee: BASF AktiengesellschaftInventors: Ulrich Wriede, Gerhard Hamprecht, Hermann Koehler, Bruno Wuerzer
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 5032590Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical,are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: March 8, 1990Date of Patent: July 16, 1991Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 5032168Abstract: Disclosed herein are derivatives of 4-((aryloxy)phenoxy)fluoroalkanoic acid and their use as active herbicides for the pre- and postemergent control of grassy weeds, especially in the presence of broadleaf crops.Type: GrantFiled: July 10, 1989Date of Patent: July 16, 1991Assignee: DowElancoInventor: James A. Turner
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Patent number: 5032577Abstract: A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is C.dbd.O or CHOH; U is CH.sub.2 or NR.sub.2, provided that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, (alpha,alpha)-dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R.sub.2 is hydrogen or loweralkyl; R.sub.3 is loweralkenyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R.sub.4 is loweralkyl, cycloalkylmethyl or benzyl; R.sub.5 is vinyl, formyl, hydroxymethyl or hydrogen; R.sub.7 is hydrogen or loweralkyl; R.sub.8 and R.sub.9 are independently selected from OH and NH.sub.2 ; and R.sub.6 is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R.sub.5 and R.sub.7 are both hydrogen and R.sub.8 and R.sub.9 are OH, the carbon bearing R.sub.5 is of the "R" configuration and the carbon bearing R.sub.Type: GrantFiled: December 18, 1987Date of Patent: July 16, 1991Assignee: Abbott LaboratoriesInventors: Anthony K. L. Fung, Dale J. Kempf, Jay R. Luly, Saul H. Rosenberg, Jacob J. Plattner
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 4999351Abstract: Novel forskolin derivatives, intermediates and processes for the preparation thereof, and methods for treating cardiac failure and memory deficit utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: January 11, 1989Date of Patent: March 12, 1991Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Gerard O'Malley, Bettina Spahl
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Patent number: 4992457Abstract: Compounds useful as cholinergic drugs are disclosed which have the formula A--B and pharmaceutically acceptable salts thereof having the formula [(A--B)Q]+.sub.q M.sup.-q wherein M is a pharmaceutically acceptable anion, Q is a proton or lower alkylating group, q is an integer from 1 to 3, A is a saturated or unsaturated five- or six-membered heterocyclic moiety having the formula: ##STR1## and B is a saturated or unsaturated five-membered heterocyclic moiety having the formula: ##STR2## wherein R.sup.1 and R.sup.2 are each independently hydrogen, halo branched or straight-chain C.sub.1 -C.sub.6 alkyl, branched or straight-chain C.sub.1 -C.sub.6 haloalkyl, branched or straight-chain C.sub.1 -C.sub.6 alkoxy, hydroxyl, keto or aryl; Y is --N.dbd. or ##STR3## Z is --N.dbd., ##STR4## --O--, --S--, ##STR5## and R.sup.3, R.sup.4 and R.sup.5 are each independently H, lower alkyl or aryl; W is --O--, --N.dbd.Type: GrantFiled: September 15, 1989Date of Patent: February 12, 1991Inventors: Jerome M. Schulman, Raj K. Goyal
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Patent number: 4987146Abstract: N-hetaryl imidazole derivatives of general Formula I ##STR1##are disclosed in whichHet represents an optionally substituted monocyclic or bicyclic heteroaromate,R.sup.3 represents hydrogen, a straight or branched C.sub.1-6 -alkyl group, or a C.sub.1-6 -alkoxy-alkyl group, andR.sup.4 represents --COOR.sup.5 --CONR.sup.6 R.sup.7 --CN, ##STR2##with R.sup.5 meaning hydrogen, a straight or branched C.sub.1-6 -alkyl group, R.sup.6 and R.sup.7 are the same of different and represent hydrogen or a straight, branched, or cyclic alkyl group with up to 7 carbon atoms or, together with the nitrogen atom, form a saturated five or six ring optionally containing another heteroatom and R.sup.8 means hydrogen or a straight, branched or cyclic alkyl group with up to 7 carbon atoms.Type: GrantFiled: July 14, 1989Date of Patent: January 22, 1991Assignee: Schering AktiengesellschaftInventors: Ralph Rohde, Helmut Biere, Ralph Schmiechen, John S. Andrews, David N. Stephens
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Patent number: 4977286Abstract: Novel, optically active azido alcohols are synthesized from N-haloacetyl oxazolidinone and are coupled with protected, activated carbohydrate residues in stereoselective glycosidic fashion to provide glycolipids in substantially pure stereochemical form. In accordance with certain preferred embodiments, the glycosphingolipids globotriaosylceramide, lactosyl ceramide, and galactosyl ceramide are synthesized in substantially pure stereochemical form from alkenyl, C-18 azido alcohols and protected fluoroglycosides and are employed as antigens in the production of antibodies useful, for example, in the treatment of disease.Type: GrantFiled: September 9, 1988Date of Patent: December 11, 1990Assignee: Trustees of the University of PennsylvaniaInventors: Kyriacos C. Nicolaou, Thomas J. Caulfield
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Patent number: 4968681Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.Type: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4950678Abstract: Novel substituted N-(heterocyclic-substituted phenyl)-N'-benzoyl-ureas, processed for producing these compounds, intermediates therefor, compositions thereof and the use of the compounds for the control of pests.Type: GrantFiled: July 27, 1989Date of Patent: August 21, 1990Assignee: Sandoz Ltd.Inventors: Robert L. Carney, John M. Gruber, Alfred S. T. Lui
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Patent number: 4943584Abstract: Novel (p-phenoxyphenoxy)-methyl-five-membered heeroaromatic radicals of the formula ##STR1## where the substituents have the following meanings: R.sup.1, R.sup.2, R.sup.3 hydrogen, halogen, C.sub.1 -C.sub.8 -alkyl, C.sub.1 -C.sub.8 -alkoxy, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, C.sub.3 -C.sub.10 -cycloalkyl, nitro or cyano,R.sup.4 hydrogen or C.sub.1 -C.sub.4 -alkyl, and a five-membered heteroaromatic ring, and their use for combating pests.Type: GrantFiled: April 20, 1988Date of Patent: July 24, 1990Assignee: BASF AktiengesellschaftInventors: Hans Theobald, Christoph Kuenast, Peter Hofmeister, Hans-Juergen Neubauer, Thomas Kuekenhoehner, Wolfgang Krieg, Joachim Leyendecker, Uwe Kardorff
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Patent number: 4939172Abstract: Novel cyclopropane carboxylic acid esters of all possible stereoisomeric forms and mixtures thereof of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, fluorine, chlorine and bromine, R is selected from the group consisting of optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, optionally unsaturated cycloalkyl of 3 to 8 carbon atoms optionally substituted, optionally substituted aryl of 6 to 14 carbon atoms and optionally substituted heterocycle, Z is selected from the group consisting of hydrogen, --CH.sub.3, --CN and --C.tbd.CH and Y is selected from the group consisting of hydrogen, --OH, optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, --CN, --(CH.sub.2).sub.m --OAlk, --(CH.sub.2).sub.m --S--Alk, ##STR2## m is 0,1,2,3 or 4, Alk is alkyl of 1 to 12 carbon atoms, --Si(Alk').sub.3, Alk' is optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted, --O--Ar and --(CH.sub.2).sub.Type: GrantFiled: February 8, 1988Date of Patent: July 3, 1990Assignee: Roussel UclafInventors: Joseph Cadiergue, Jacques Demassey, Jean-Pierre Demoute, Jean Tessier
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Patent number: 4937255Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.Type: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4935423Abstract: A substituted, 1,2,4-triazinedione of the formula ##STR1## in which R.sup.1 stands for an unsubstituted or substituted heteroaromatic radicals bonded via carbon,X stands for one or more, identical or different radicals selected from the group consisting of hydrogen, halogen, nitro, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy and halogenoalkylthio.R.sup.3 stands for hydrogen, unsubstituted or substituted alkyl, alkenyl, alkinyl or aralkyl. The substituted 1,2,4-triazinedione is useful to combat parasitic protozoa in warmblooded animals.Type: GrantFiled: February 14, 1989Date of Patent: June 19, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Lindner, Axel Haberkorn
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Patent number: 4914206Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.Type: GrantFiled: December 15, 1988Date of Patent: April 3, 1990Assignee: Takeda Chemical Industries, LTD.Inventors: Isao Minamida, Naoto Hashimoto
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Patent number: 4906750Abstract: A merocyanine dye having the formula: ##STR1## wherein: R.sub.1 and R.sub.2 independently are H, alkyl, alkoxy or aryl; R.sub.7 and R.sub.8 are H orany of R.sub.1 and R.sub.2, R.sub.1 and R.sub.7, and R.sub.2 and R.sub.8 can together comprise the atoms necessary to form a fused aromatic ring on the benzene radical to which they are attached and with the stipulation that only one of R.sub.1 and R.sub.2 can be H;R.sub.5 and R.sub.6 comprise alkyl of from 1-18 carbon atoms, provided that the sum of the carbon atoms in R.sub.5 and R.sub.6 together is at least 8;R.sub.9 is an alkylene group of 2-9 nuclear carbon and hetero atoms; andZ.sup.+ is a cation.This dye is useful in a method for inactivating viruses comprising contacting the viruses with the compound and exposing the resulting mixture to visible light to excite and inactivate the viruses. The compounds are also useful in the irradiation-induced inactivation of leukemia cells.Type: GrantFiled: June 8, 1988Date of Patent: March 6, 1990Assignee: Eastman Kodak CompanyInventors: Wolfgang H. H. Gunther, Frederick J. Sauter
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4877883Abstract: The synthesis of quaternary five membered N-n-alkyl-heterocycles, especially of 4-hydroxy-N(1)-n-alkyl-imidazolium, 2,5-substituted N(3)-n-alkyl-thiazolium and substituted N(2) pyrazolium salts are described. The N-surfactants obtained have a very small critical micelle concentration (CMC) of 10.sup.-5 -10.sup.-7 Mol/Liter, and are capable of forming micelles of different sizes and forms depending on the nature of the anions. The N-detergents can be used as pharmaceuticals.Type: GrantFiled: August 6, 1987Date of Patent: October 31, 1989Assignee: Medice chem.-pharm. Fabrik Putter GmbH & Co. KGInventor: Henrich H. Paradies
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Patent number: 4863947Abstract: This invention relates to novel N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: August 11, 1986Date of Patent: September 5, 1989Assignee: Rohm and HaasInventor: Richard M. Jacobson
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Patent number: 4855441Abstract: 5-pyrazolone compounds which are substituted with a thioether group in the 4-position may be prepared by the reaction of a 5-pyrazolone compound which is unsubstituted in the 4-position with a sulphenic acid amide. The resulting 5-pyrazolone compounds substituted in the 4-position are suitable for use as 2-equivalent magenta couplers in color photographic recording materials.Type: GrantFiled: December 14, 1987Date of Patent: August 8, 1989Assignee: Agfa-Gevaert AktiengesellschaftInventors: Gunter Renner, Erich Illner
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Patent number: 4854961Abstract: The invention relates to a herbicidally and/or algicidally active compound of the general formula ##STR1## wherein R.sub.1 is a substituted or non-substituted alkyl group having 1-6 carbon atoms, or an alkenyl or alkynyl group having 2-6 carbon atoms;R.sub.2 is a halogen atom; a nitro group; a cyano group; a substituted or non-substituted benzyl, phenyl, phenoxy, phenylthio, phenylsulphinyl, phenylsulphonyl or phenylsulphonyloxy group; or a halogenated or non-halogenated alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkylsulphonyloxy group having 1-4 carbon atoms;R.sub.3 is a hydrogen atom, a halogen atom, or an alkyl group having 1-4 carbon atoms; andX is O or S;or a salt of this compound with an organic or inorganic acid.Type: GrantFiled: October 30, 1987Date of Patent: August 8, 1989Assignee: Duphar International Research B.V.Inventors: Kobus Wellinga, Jacobus H. H. Eussen
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Patent number: 4851406Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.Type: GrantFiled: September 4, 1986Date of Patent: July 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
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Patent number: 4846875Abstract: A herbicidal compound which is a Q-substituted 1-aryl-4,5-dihydro-1,2,4-triazol-5(1H)-one in which the Q-substituent is on the ring-carbon atom at the 5-position of the aryl group and in which: Q is(a) --CH(R.sup.1)ZR in which Z is O or S(O).sub.n and n is zero, one or two; or(b) --CH(R.sup.1)N(R.sup.4)(R.sup.5); or(c) --C(R.sup.9).dbd.NR.sup.Type: GrantFiled: July 21, 1987Date of Patent: July 11, 1989Assignee: FMC CorporationInventor: Jun H. Chang
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Patent number: 4835280Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.Type: GrantFiled: July 14, 1987Date of Patent: May 30, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
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Patent number: 4833252Abstract: Substituted N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N'-triazinylureas of the general formula ##STR1## and the salts thereof with amines, alkali metal bases or alkaline earth metal bases, or with quaternary ammonium bases, have good pre- and postemergence selective herbicidal and growth regulating properties.In the above formula the symbols have the following meanings:R.sup.1 is hydrogen, halogen, nitro, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkylsulfinyl, --CO--R.sup.8, --NR.sup.9 R.sup.10, --CO--NR.sup.11 R.sup.12 or --SO.sub.2 --NR.sup.13 R.sup.14,R.sup.2 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl or C.sub.1 -C.sub.4 alkylsulfonyl,R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or cyano,R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.5 is hydrogen, C.sub.Type: GrantFiled: September 28, 1988Date of Patent: May 23, 1989Assignee: Ciba-Geigy CorporationInventors: Werner Topfl, Georg Pissiotas
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Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4826990Abstract: There are disclosed compounds of the formula ##STR1## wherein X is ##STR2## Y is ##STR3## Z is ##STR4## R.sup.1 is ##STR5## n is 0-5; R.sup.2 is hydrogen, loweralkyl, loweralkoxy, lower alkoxycarbonyl, trifluoromethyl, nitro, cyano or halo;R.sup.3 is ##STR6## W represents a bond or ##STR7## m is 1-15; R.sup.4 is hydrogen or loweralkyl;R.sup.5 is lower alkyl, monofluoroloweralkyl, difluoroloweralkyl, polyfluoroloweralkyl, perfluoroloweralkyl or ##STR8## R.sup.6 is hydrogen, lower alkyl, ##STR9## and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like, and as antiinflammatory agents.Type: GrantFiled: September 30, 1987Date of Patent: May 2, 1989Assignee: American Home Products CorporationInventors: John H. Musser, Reinhold H. W. Bender, Anthony F. Kreft, III
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Patent number: 4808588Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.Type: GrantFiled: July 30, 1987Date of Patent: February 28, 1989Assignee: Beecham Group, p.l.c.Inventor: Francis D. King
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Patent number: 4798893Abstract: A method for the synthesis of the 2-propanone (I) is described starting from alkoxide (II) through the lactone (IV). ##STR1## Excellent control of the location of the substitution on the phenyl ring is achieved and the reaction proceeds in high yield.Type: GrantFiled: September 21, 1987Date of Patent: January 17, 1989Assignee: McNeilab, Inc.Inventors: David A. Cherry, Cynthia A. Maryanoff, John E. Mills, Roy A. Olofson, James D. Rodgers
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Patent number: 4798892Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: April 14, 1986Date of Patent: January 17, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
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Patent number: 4795755Abstract: This invention relates to heterocyclic derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen-substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W- in which W is 2-6 alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O,S,SO,SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.Type: GrantFiled: March 1, 1982Date of Patent: January 3, 1989Assignee: Imperial Chemical Industries PLCInventors: Derrick F. Jones, Keith Oldham
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Patent number: 4786646Abstract: The invention relates to compounds of the formula ##STR1## Y is O or S, *A is paraphenylene or *--(CH.sub.2).sub.n --(X).sub.m --(CH.sub.2).sub.r --, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, s is an integer from 0 to 1, m is an integer from 0 to 1, provided that when m is 1, n+s must be at least 2, R.sub.1 and R.sub.2, independently, are hydrogen, lower alkyl, cycloalkyl, lower alkenyl, Het or aryl, *E is ##STR2## or --(CH.sub.2).sub.k -- wherein k is an integer from 0 to 4, R.sub.3, R.sub.4 and R.sub.8 are independently hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently are hydrogen or lower alkyl, R.sub.Type: GrantFiled: July 10, 1987Date of Patent: November 22, 1988Assignee: Hoffmann-La Roche Inc.Inventors: Robert W. Guthrie, Richard W. Kierstead, Jefferson W. Tilley
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Patent number: 4772694Abstract: 2,5-Disubstituted oxazolidin-4-one-3-ylacetyl chlorides and 1,2,5-substituted imidazolidin-4-one-3-yl-acetyl chlorides function as chiral auxiliary moieties in the asymmetric cycloaddition with aldimines to provide cis-azetidinones. The azetidinones are useful intermediates in the preparation of antibiotics.Type: GrantFiled: July 24, 1986Date of Patent: September 20, 1988Assignee: Eli Lilly and CompanyInventor: Robin D. G. Cooper
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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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Substituted pyrazolin-5-ones, composition containing them, and method of combating fungi or bacteria
Patent number: 4767775Abstract: Microbicidal substituted pyrazolin-5-ones of the formula ##STR1## in which R.sup.1 and R.sup.2 independently of one another each represent hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonyl, hydroxycarbonylalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonylalkyl or dialkylaminocarbonylalkyl, or represent in each case optionally substituted oxiranylalkyl, aralkyl, heterocyclyl or aryl andHet represents an optionally substituted heterocyclic radical.Intermediates therefor of the formula ##STR2## in which R is alkyl, are also disclosed.Type: GrantFiled: July 24, 1986Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Klaus Jelich, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke -
Patent number: 4762848Abstract: Heterocyclic sulfides of the general formula heterocycle-S-R, a process for their preparation and, in particular, their use for immunostimulation, immunorestoration and cytostatic treatment, and pharmaceutical agents, which contain a sulfide of this type, for these indications.Type: GrantFiled: March 10, 1986Date of Patent: August 9, 1988Assignee: Hoechst AktiengesellschaftInventors: Karl-Heinz Scheunemann, Walter Durckheimer, Jurgen Blumbach, Michael Limbert, Hans-Ulrich Schorlemmer, Gerhard Dickneite, Hans-Harald Sedlacek
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Patent number: 4760067Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: March 9, 1987Date of Patent: July 26, 1988Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4742073Abstract: Compounds are disclosed of the general formula I ##STR1## wherein R.sub.1 is a group of the formula IIR.sub.3 --X-- IIwherein R.sub.3 is alkyl; phenyl; phenyl substituted with halogen, lower alkyl, hydroxy, lower alkoxy, or phenoxy; phenyl-lower alkyl in which the phenyl group may be substituted with halogen, lower alkyl, hydroxy, lower alkoxy, or phenoxy; phenyl-lower alkenyl in which the phenyl group may be substituted with halogen, lower alkyl, hydroxy, lower alkoxy or phenoxy; and X is oxygen or sulfur; or R.sub.1 is a group of the formula III ##STR2## wherein R.sub.4 has the same meaning as R.sub.3 as defined above; or R.sub.4 is a group of the formula IV ##STR3## wherein R.sub.7 has the same meaning as R.sub.3 as defined above; or R.sub.7 is an aromatic 5- or 6-membered heterocyclic ring containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur; and wherein R.sub.5 and R.sub.6 are the same or different and each represent hydrogen or have the same meaning as R.Type: GrantFiled: September 16, 1983Date of Patent: May 3, 1988Inventors: Hans Bundgaard, Erik Falch, Claus S. Larsen, Thomas J. Mikkelson
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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: 4725682Abstract: Sulfur-containing bis-amino carbamate compounds exhibit outstanding acaricidal, nematocidal and insecticidal activity.Type: GrantFiled: December 2, 1986Date of Patent: February 16, 1988Assignee: Rhone-Poulenc Nederland, B.V.Inventor: Themistocles D. J. D'Silva
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Patent number: 4670470Abstract: Organic sulfoxides having a latent allyl group bound to the sulfur are enzyme inhibitors of the suicide or K.sub.cat type.Type: GrantFiled: August 29, 1985Date of Patent: June 2, 1987Assignee: Merck & Co., Inc.Inventor: Raymond A. Firestone
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Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
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Patent number: 4650512Abstract: A substituted oxazolidone compound having the formula ##STR1## wherein Ar.sup.1 and Ar.sup.2 are the same or different and are aromatic or a substituted aromatic group wherein the substituent is selected from chlorine, bromine, chloride or trifluoromethyl, and R is lower alkyl having from 1 to 6 carbon atoms.Type: GrantFiled: September 27, 1984Date of Patent: March 17, 1987Assignee: Stauffer Chemical CompanyInventors: Raymond A. Felix, Eugene G. Teach
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Patent number: 4634783Abstract: 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.Type: GrantFiled: January 23, 1984Date of Patent: January 6, 1987Assignee: Torii & Co. Ltd.Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Ryoji Matsui, Shin-ichi Watanabe, Kimio Sudo, Toshiyuki Okutome, Masateru Kurumi, Yojiro Sakurai, Takuo Aoyama
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Patent number: 4629794Abstract: A series of novel antibacterially active derivatives of indolmycin as well as some prodrug forms of indolmycin is disclosed. A novel process for the production of these compounds is also disclosed.Type: GrantFiled: January 23, 1986Date of Patent: December 16, 1986Assignee: Pfizer Inc.Inventor: John P. Dirlam
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas