The -c(=x)- Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/170)
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Patent number: 4861887Abstract: A method for the preparation of o-carboxyl imidazolinone compounds including oxidizing the appropriate 2-{[(1-carbamoyl-1,2-dimethylpropyl)amino]methyl}-benzoic acid intermediate with a brominating agent. Compounds useful as intermediates in the oxidation method and methods for preparing them are disclosed.Type: GrantFiled: January 27, 1988Date of Patent: August 29, 1989Assignee: American Cyanamid CompanyInventor: Robert F. Doehner, Jr.
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Patent number: 4853392Abstract: Compounds of the formula ##STR1## where R.sup.1 is lower alkyl, R.sup.2 is chlorophenyl, Y is alkylene, X is heterocyclic and Z is a fused ring are useful as antiinflammatory and antiallergy agents.Type: GrantFiled: July 11, 1988Date of Patent: August 1, 1989Assignee: Pfizer Inc.Inventors: Kelvin Cooper, Peter E. Cross, Michael J. Fray, Kenneth Richardson
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Patent number: 4851409Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes and inhibitors of their biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.Type: GrantFiled: February 5, 1987Date of Patent: July 25, 1989Assignee: Merck Frosst Canada Inc.Inventors: Robert N. Young, Robert Zamboni, Serge Leger
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Patent number: 4847405Abstract: The present invention relates to novel methods for the preparation of anilinofumarate [quinoline- 2,3-dicarboxylic acid], a useful intermediate in the preparation of 2-(2-imidazolin-2-yl)-quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: March 19, 1987Date of Patent: July 11, 1989Assignee: American Cyanamid CompanyInventor: Donald R. Maulding
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Patent number: 4845226Abstract: A process for the preparation of 8-bromomethyl-3-methylquinoline compounds of the formula I ##STR1## where one of both substituents X are chlorine and, where relevant, the other substituent X is hydrogen, by bromination of the corresponding 8-methylquinoline compound in the presence of a 2-phase mixture of a solvent stable to bromination and of, preferably, buffered water.Type: GrantFiled: January 21, 1988Date of Patent: July 4, 1989Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Rolf-Dieter Kohler, Jacques Dupuis
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Patent number: 4843162Abstract: There are provided novel alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid; novel dialkyl 3-(substituted)phenylamino-2-ene-dioates, useful as intermediates for the preparation of highly effective 2-(2-imidazolin-2-yl)quinoline herbicidal agents and methods for the preparation thereof.Type: GrantFiled: February 21, 1987Date of Patent: June 27, 1989Assignee: American Cyanamid CompanyInventor: Robert F. Doehner, Jr.
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Patent number: 4839366Abstract: The compound of formula (I): ##STR1## N-cyclohexyl-N"-4-(2-methylthioquinolyl)-N'-2-thiazolyl-guanidine and pharmaceutically acceptable salts thereof is a valuable antiinflammatory, analgesic and antipyretic agent.The compound of the invention may be formulated with conventional pharmaceutically acceptable carriers or diluents to provide a pharmaceutical composition.Type: GrantFiled: February 23, 1988Date of Patent: June 13, 1989Assignee: Chiesi Farmaceutici S.p.A.Inventor: Giuseppe Quadro
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Patent number: 4826531Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur; A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 or --S(O).sub.n R.sup.3 groups; any two of the groups A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.Type: GrantFiled: April 17, 1987Date of Patent: May 2, 1989Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul DeFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
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Patent number: 4826986Abstract: 7- or 8-Substituted, partially hydrogenated pyrazolo[3,4-g]quinoline, thiazolo[4,5-g]quinoline, oxazolo[4,5-g]quinoline, and pyrrolo[3,4-g]quinoline derivatives, and 8- or 9-substituted, partially hydrogenated pyrido[2,3-g]quinazoline derivatives are D-2 dopamine agonists. 6-Oxo-1-substituted-octahydroquinolines and 6-oxo-1-substituted-decahydroquinolines which are additionally substituted in the 3- or 4-position are intermediates useful in preparation of the dopamine agonists. Acetals of 4,6-dioxo-1-substituted-decahydroquinoline 3-carboxylic acid esters enable synthesis of the foregoing compounds.Type: GrantFiled: June 16, 1986Date of Patent: May 2, 1989Assignee: Eli Lilly and CompanyInventors: Diane L. Huser, John M. Schaus
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Patent number: 4826987Abstract: The present invention relates to compounds of formula I ##STR1## in which formula I X stands for O, S, ##STR2## R.sub.1 and R.sub.2 which can be the same or different stand for hydrogen, straight or branched, saturated or unsaturated, unsubstituted or substituted C.sub.1 -C.sub.8 -alkyl, or for ar-C.sub.1 -C.sub.4 -alkyl, aryl and ar being unsubstituted or substituted phenyl; R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are the same or different and stand for hydrogen, halogen, pseudo halogen, cyano, nitro, amino, carboxy, hydroxy, alkyl, alkoxy; or R.sub.5 and R.sub.6 form an aromatic ring which is fused to the pyridyl ring, and which aromatic ring may substituted; provided that R.sub.1 and R.sub.2 cannot be hydrogen at the same time, and provided that when R.sub.5 and R.sub.6 both are chlorine and R.sub.1 is hydrogen, then R.sub.2 cannot be n-propyl; and salts and bioreversible derivatives thereof.Type: GrantFiled: February 28, 1986Date of Patent: May 2, 1989Assignee: Leo Pharmaceutical Products Ltd.Inventors: Ole Bent Iv rmose Nielsen, Ian Ahnfelt-Ronne
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Patent number: 4824850Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D--DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.Type: GrantFiled: October 29, 1984Date of Patent: April 25, 1989Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4814486Abstract: The present invention relates to an improved method for the preparation of anilinofumarates useful as intermediates in the preparation of 2-(2-imidazolin-2-yl) quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: October 1, 1987Date of Patent: March 21, 1989Assignee: American Cyanamid CompanyInventors: Donald R. Maulding, Albert A. Cevasco
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Patent number: 4808212Abstract: Oxime esters of substituted quinoline-8-carboxylic acids of the formula ##STR1## where X is hydrogen, C.sub.1 -C.sub.4 -alkyl or halogen, Z is hydrogen or methyl, R.sup.1 is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxymethyl, C.sub.1 -C.sub.4 -alkoxyethyl, C.sub.1 -C.sub.4 -alkylthiomethyl, C.sub.1 -C.sub.4 -alkylthioethyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, C.sub.3 -C.sub.6 -alkenyl or C.sub.5 -C.sub.8 -cycloalkyl, each of which is unsubstituted or bears up to 3 methyl substituents, hydrogen, cyano, acetyl, benzoyl, unsubstituted benzyl or phenyl, or benzyl or phenyl bearing up to 3 substitutents selected from the group consisting of halogen, cyano, trifluoromethyl, C.sub.1 -C.sub.4 -haloalkyloxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkyl, hydroxy, dimethylamino or acetamino, R.sup.2 is hydrogen if R.sup.1 is not hydrogen, R.sup.2 further denotes C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxymethyl, chloromethyl, azolylmethyl, 1,1-dimethoxymethyl, cyano, C.sub.Type: GrantFiled: December 22, 1986Date of Patent: February 28, 1989Assignee: BASF AktiengesellschaftInventors: Peter Plath, Karl Eicken, Bernd Zeeh, Ulrich Eichenauer, Helmut Hagen, Rolf-Dieter Kohler, Norbert Meyer, Bruno Wuerzer
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Patent number: 4806540Abstract: Novel microbicidally active 1-heteroaryl-4-arylpyrazole derivatives of the formulae (I) and/or (1A) ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents halogen, hydroxyl, optionally substituted alkyl, optionally substituted alkoxy, a radical --S(O).sub.p -alkyl which is optionally substituted in the alkyl part, nitro or optionally substituted amino, or represents a fused-on carbocyclic or heterocyclic radicalp represents the integer 0, 1 or 2,n represents an integer from 0 to 5,X represents .dbd.CH--, or represents a nitrogen atom,Y represents CO or SO.sub.2 andR.sup.2 represents hydrogen, in each case optionaly substituted alkyl, cycloalkyl or aryl or a heterocyclic radical, or represents OR.sup.3, or also represents SR.sup.3, if Y is CO,whereinR.sup.3 represents optionally substituted alkyl or aryl, orR.sup.2 represents a radical ##STR2## wherein R.sup.Type: GrantFiled: September 23, 1987Date of Patent: February 21, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Gerd Hanssler, Hans-Georg Schmitt, Wilfried Paulus
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Patent number: 4804404Abstract: Fluoroalkyl-substituted quinoline derivatives of the formula ##STR1## where R.sup.1 is chlorine, fluorine, hydroxyl, O.sup..crclbar. Met.sup..sym., C.sub.1 -C.sub.4 -alkoxy or a radical of the formula ##STR2## R.sup.2 and R.sup.3 independently of one another are each hydrogen, C.sub.1 -C.sub.3 -alkyl or C.sub.1 -C.sub.3 -fluoroalkyl, R.sup.4 is fluorine, chlorine or bromine, with the proviso that one or both of the radicals R.sup.2 and R.sup.3 are C.sub.1 -C.sub.3 -fluoroalkyl, herbicides containing these compounds as active ingredients, and their use for controlling unwanted plant growth.Type: GrantFiled: June 15, 1987Date of Patent: February 14, 1989Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Ulrich Eichenauer, Rolf-Dieter Kohler, Peter Plath, Thomas Liese-Sauer, Karl Eicken, Bruno Wuerzer, Norbert Meyer
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Patent number: 4788188Abstract: The present invention relates to new quinolylglycinamide derivatives corresponding to the following general formula: ##STR1## The invention also relates to a process for preparing these compounds and their therapeutic application as a psychotropic agent.Type: GrantFiled: May 6, 1986Date of Patent: November 29, 1988Assignee: Sanofi (S.A.)Inventors: Jean-Claude Vernieres, Etienne Mendes, Michel Morre, Peter Keane, Jacques Simiand
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Patent number: 4783535Abstract: 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. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.Type: GrantFiled: March 18, 1986Date of Patent: November 8, 1988Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Albert D. Cale, Jr.
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Patent number: 4772311Abstract: The invention relates to novel difluoromethoxy-, trifluoromethoxy-, 1,1,2,2-tetrafluoroethoxy-, alkenyloxy- and alkynyloxypyridine and quinoline compounds and a method for controlling undesirable plant species therewith.Type: GrantFiled: January 21, 1987Date of Patent: September 20, 1988Assignee: American Cyanamid Co.Inventor: Marinus Los
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Patent number: 4771059Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## X.sup.-, wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.Type: GrantFiled: August 29, 1985Date of Patent: September 13, 1988Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4769375Abstract: Circulation-active dihydropyridines of the formula ##STR1## in which R.sup.1 is optionally substituted aryl or heterocyclic,R.sup.2 is H, NO.sub.2, CN, C.sub.1 -C.sub.8 -alkylsulphonyl, aryl or carboalkoxy,R.sup.3 is alkyl or aryl,R.sup.4 is H or alkyl,X is C.dbd.O or a direct bond, andn is a number from 1 to 20,or physiologically acceptable salts thereof. A synthesis using morpholines or thiomorpholines is also disclosed.Type: GrantFiled: July 25, 1986Date of Patent: September 6, 1988Assignee: Bayer AktiengesellschaftInventors: Horst Meyer, Gerhard Franckowiak, Gunther Thomas, Matthias Schramm, Michael Kayser, Martin Bechem, Rainer Gross
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Patent number: 4766218Abstract: The present invention relates to novel methods for the preparation of quinoline-2,3-dicarboxylic acid, useful for the preparation of the highly effective 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: August 29, 1986Date of Patent: August 23, 1988Assignee: American Cyanamid CompanyInventor: Donald R. Maulding
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Patent number: 4757146Abstract: The present invention relates to novel methods for the preparation of quinoline-2,3-dicarboxylic acid, useful for the preparation of the highly effective 2-(2-imidazolin-2-yl)quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: August 29, 1986Date of Patent: July 12, 1988Assignee: American Cyanamid CompanyInventor: Donald R. Maulding
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Patent number: 4757071Abstract: 2,6-Dimethyl-4-(2- or 3-substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid diesters, having vasodilating and blood pressure lowering effects, in the ester moiety at the 3-position of which a heterocyclic group is linked to an alkylene group through an ester bond (carbonyloxy group). The diesters are used for treatment of cardiac diseases, cerebrovascular diseases and hypertension.Type: GrantFiled: December 9, 1985Date of Patent: July 12, 1988Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Hiroyasu Koyama, Yoshikuni Suzuki, Koichiro Hagihara
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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: 4720494Abstract: This invention relates to novel chemical compounds, methods and compositions for inhibiting the production of human perspiration, especially axillary perspiration. More particularly, the practice of the invention comprises the topical application to the axiallary area or other perspiration-producing portion of the body of an anticholinergic eucatropine ester having reduced mydriatic activity and distributed in a suitable dermatologically acceptable carrier.Type: GrantFiled: November 5, 1984Date of Patent: January 19, 1988Assignee: The Gillette CompanyInventors: Carl Felger, Edith Shulman
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Patent number: 4715889Abstract: Quinoline derivatives of the formula ##STR1## where X, n, R.sup.1, R.sup.2 and Y have the meanings given in the description, are used for controlling undesirable plant growth.Type: GrantFiled: September 7, 1983Date of Patent: December 29, 1987Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Rolf-Dieter Kohler, Jurgen Markert, Bruno Wuerzer
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Patent number: 4709036Abstract: The present invention provides a process for the preparation of herbicidal 2-(4,4-disubstituted-5-oxo-2-imidazolin-2-yl) benzoic, nicotinic and quinoline-3-carboxylic acids, esters and salts.Type: GrantFiled: June 13, 1985Date of Patent: November 24, 1987Assignee: American Cyanamid CompanyInventors: Marinus Los, Don W. Long, Gregory P. Withers
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Patent number: 4680299Abstract: Phenylquinolinecarboxylic acids and derivatives thereof, such as 2-(2'-fluoro-1,1'-biphenyl-4-yl)-6-fluoro-3-methyl-4-quinolinecarboxylic acid, or a sodium or potassium salt thereof, are useful as tumor inhibiting agents.Type: GrantFiled: April 26, 1985Date of Patent: July 14, 1987Assignee: E.I. Du Pont de Nemours and CompanyInventor: David P. Hesson
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Patent number: 4677210Abstract: Z is a chemical bond or an alkylene chain containing up to 5 carbons in the principal chain and up to a total of 7 carbons;X is O or S;R and R.sub.1 are independently hydrogen, hydroxy, lower alkoxy, lower alkanoyloxy, halo, cyano, carboloweralkoxy, carboxyloweralkyl, aryloxy or benzyloxy;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen, lower alkyl, lower aralkyl, lower alkenyl, lower alkynyl, aryl or carboxyloweralkyl;and pharmaceutically acceptable salts thereof have pharmaceutical activity, particularly as lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties.Type: GrantFiled: June 19, 1985Date of Patent: June 30, 1987Assignee: Rorer Pharmaceutical CorporationInventor: Fu-chih Huang
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Patent number: 4675432Abstract: The present invention relates to methods for the preparation of anilinofumarate, a useful intermediate in the preparation of quinoline-2,3-dicarboxylic acid and in the preparation of 2-(2-imidazolin-z-yl) quinoline-3-carboxylic acid herbicidal agents.Type: GrantFiled: August 29, 1986Date of Patent: June 23, 1987Assignee: American Cyanamid CompanyInventor: Donald R. Maulding
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Patent number: 4667040Abstract: This invention relates to a novel process for producing a 2-(2-aminothiazol-4-yl)glyoxylic acid derivative or a salt thereof which are useful in producing a cephalosporin antibiotic, and to intermediates for said derivative and salt and a process for producing the intermediates.Type: GrantFiled: July 9, 1985Date of Patent: May 19, 1987Assignee: Toyama Chemical Co., Ltd.Inventors: Hiroshi Sadaki, Hiroyuki Imaizumi, Kenji Takeda, Takihiro Inaba, Ryuko Takeno, Seishi Morita, Tetsuya Kajita, Isamu Saikawa
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Patent number: 4656283Abstract: There are provided novel alkyl esters of substituted 2-methyl-3-quinolinecarboxylic acid and quinoline-2,3-dicarboxylic acid; novel dialkyl 3-(substituted)phenylaminobut-2-ene-dioates, useful as intermediates for the preparation of highly effective 2-(2-imidazolin-2-yl)quinoline herbicidal agents and methods for the preparation thereof.Type: GrantFiled: February 4, 1985Date of Patent: April 7, 1987Assignee: American Cyanamid CompanyInventor: Robert F. Doehner, Jr.
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Patent number: 4638068Abstract: There are provided novel 2-(2-imidazolin-2-yl)pyridine and quinoline compounds, a process and intermediate compounds for the preparation thereof, and a method for controlling a wide variety of annual and perennial plant species therewith.Type: GrantFiled: May 25, 1982Date of Patent: January 20, 1987Assignee: American Cyanamid CompanyInventor: Marinus Los
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Patent number: 4608079Abstract: This invention relates to novel imidazolidinone and imidazolidinethione compounds, a process and intermediates for the preparation of said compounds and a method for controlling undesirable plant species therewith.Type: GrantFiled: June 4, 1984Date of Patent: August 26, 1986Assignee: American Cyanamid CompanyInventor: Marinus Los
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Patent number: 4585868Abstract: The compounds 5-carboxyl-6-fluoroquinaldine, 6-fluoro-5-methylquinaldine, 6-fluoro-5-methyl-1,2,3,4-tetrahydroquinaldine, 1,2-dihydro-6-fluoro-5-hydroxymethylquinaldine and diethyl 2-[N-(6-fluoro-5-methyl-1,2,3,4-tetrahydroquinaldinyl)]methylenemalonate are disclosed as useful intermediates for preparing the antimicrobial agent 6,7-dihydro-5,8-dimethyl-9-fluoro-1-oxo-1H,5H-benzol[ij]quinolizine- 2-carboxylic acid.Type: GrantFiled: June 25, 1984Date of Patent: April 29, 1986Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
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Patent number: 4576949Abstract: The present invention also provides novel compositions of matter. In particular, the present invention provides novel 3-substituted compounds of formula I which are from among the selected 5,6,7,8-tetrahydroquinolines and 5,6-dihydropyrindines having use as inhibitors of the synthesis of leukotrienes and as inhibitors of the action of lipoxygenase in mammalian metabolism.Type: GrantFiled: May 7, 1984Date of Patent: March 18, 1986Assignee: The Upjohn CompanyInventor: Herman W. Smith
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Patent number: 4529721Abstract: A compound of the formula: ##STR1## wherein u represents hydrogen, carboxamido, N-hydroxycarboxamido, carboxy, azido, an aryl, an acylamino, a protected carboxy or an N-alkoxycarboxamido, or, together with v, can represent --S-- or --CH.sub.2 S--; v represents hydrogen, halogen, cyano or an alkylthio, or, together with u, can represent --S-- or --CH.sub.2 S--, or, together with w, can represent --(CH.sub.2).sub.3 CO--; w represents hydrogen, carboamoyl, cyano, carboxy, an N-alkylcarbamoyl, an alkyl, an aryl, a protected carboxy or a heterocycle, or, together with v, can represents --(CH.sub.2).sub.Type: GrantFiled: September 21, 1983Date of Patent: July 16, 1985Assignee: Shionogi & Co., Ltd.Inventors: Wataru Nagata, Mitsuru Yoshioka, Yasuhiro Nishitani, Tsutomu Aoki, Toshiro Konoike, Tadatoshi Kubota
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Patent number: 4501919Abstract: Serine derivatives are synthesized by the condensation of an alkali metal salt of a glycine derivative and a carbonyl compound in the presence of a phase transfer catalyst.Type: GrantFiled: May 22, 1980Date of Patent: February 26, 1985Assignee: Gruppo Lepetit S.p.A.Inventors: Melvin V. Koch, Ambrogio Magni
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Patent number: 4499079Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.Type: GrantFiled: November 18, 1982Date of Patent: February 12, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Harold N. Weller, III
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Patent number: 4497651Abstract: Dichloroquinoline derivatives of the formula ##STR1## are prepared as described, and are used as herbicides.Type: GrantFiled: February 17, 1982Date of Patent: February 5, 1985Assignee: BASF AktiengesellschaftInventors: Helmut Hagen, Juergen Markert, Bruno Wuerzer
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Patent number: 4472405Abstract: The compound 6,7-dihydro-5,8-dimethyl-9-fluoro-1-oxo-1H,5H-benzo[ij]quinolizine-2-carbo xylic acid is disclosed as a potent antimicrobial agent with a broad spectrum of activity. Esters, acyl chlorides, alkylaminoalkyl ester salts and pharmaceutically acceptable carboxylate salts of the acid are also disclosed. Methods of using these compounds, pharmaceutical compositions comprising these compounds and synthetic intermediates for preparing these compounds are described.Type: GrantFiled: November 12, 1982Date of Patent: September 18, 1984Assignee: Riker Laboratories, Inc.Inventor: Richard M. Stern
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Patent number: 4460594Abstract: Compounds of the formula (I), and pharmaceutically acceptable salts thereof: ##STR1## wherein: R.sub.1 is hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group:R.sub.2 is hydrogen, C.sub.1-4 alkyl, hydroxy, C.sub.1-4 alkoxy or an in-vivo hydrolysable acyloxy group;R.sub.4 is benzofuryl, benzothienyl, indolyl, quinolyl, isoquinolyl,2,3-dihydrobenzofuryl, 2,3-dihydrobenzylthienyl or 2,3-dihydroindolyl optionally substituted by one or two substituents selected from C.sub.1-4 alkoxy, hydroxy or acyloxy, trifluoromethyl, halogen or nitro; andA is a bond or C.sub.1-6 alkylene,a process for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: September 15, 1982Date of Patent: July 17, 1984Assignee: Beecham Group p.l.c.Inventor: Roger E. Markwell
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Patent number: 4459408Abstract: The invention is related to a novel process for the prepartion of 2-(5-isopropyl-5-methyl-4-oxo-2-imidazolin-2-yl)-3-quinolinecarboxylic acid, a useful and valuable herbicide.Type: GrantFiled: May 25, 1982Date of Patent: July 10, 1984Assignee: American Cyanamid CompanyInventors: Donald R. Maulding, Robert F. Doehner, Jr.
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Patent number: 4459409Abstract: There is provided a novel process for the preparation of a substituted or unsubstituted 2,3-quinolinedicarboxylic acid, utilizing as the starting material, 2-methyl-3-quinolinecarboxylic acid or 3-methyl-2-quinolinecarboxylic acid or the alkyl ester of either of the above compounds.Type: GrantFiled: May 25, 1982Date of Patent: July 10, 1984Assignee: American Cyanamid CompanyInventor: David W. Ladner
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Patent number: 4426387Abstract: The invention concerns compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O,S,--CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or defined substituents and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.8 when adjacent, together with the carbon atoms to which they are attached also represent a fused five or six membered carbocyclic or heterocyclic ring optionally carrying one or more defined substituents; R is an optionally substituted aryl or heteroaryl radical or a cycloalkyl radical containing 5 to 7 carbon atoms; R.sup.1, R.sup.2, R.sup.3 and R.sup.9 are each hydrogen or a lower alkyl group; n is 0 or 1; X is .dbd.O, .dbd.S or .dbd.NH; Y is --O-- or a direct bond and Z is --CO-- or --CH.sub.Type: GrantFiled: April 7, 1982Date of Patent: January 17, 1984Assignee: John Wyeth & Brother Ltd.Inventors: John L. Archibald, Terrence J. Ward
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Patent number: 4416817Abstract: Novel 3-methoxy-2-oxoazetidine derivatives, which are shown by the following formula ##STR1## wherein R.sub.1 is amino, acylated amino or protected amino, are of value as intermediates for the synthesis of useful compounds represented by the formula ##STR2## wherein R.sub.1 has the same meaning as defined above, as drugs in the treatment of bacterial infections.Type: GrantFiled: November 18, 1981Date of Patent: November 22, 1983Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Michihiko Ochiai
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Patent number: 4395566Abstract: An improved process for exterifying carboxyaromatics is disclosed wherein an anhydride of a carboxyaromatic, such as pyromellitic dianhydride, is reacted with a fluorinated alcohol and an epoxide to give a mixed ester capable of imparting oil and/or water repellency to textiles. The improvement comprises utilizing the epoxide as the reaction medium to reduce reaction times and waste water treatment requirements.Type: GrantFiled: March 8, 1982Date of Patent: July 26, 1983Assignee: American Hoechst CorporationInventors: James H. Covill, Michael G. Kelly, Thomas F. Leahy
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Patent number: 4350704Abstract: Substituted acyl derivatives of octahydro-1H-indole-2-carboxylic acid and the pharmaceutically acceptable salts thereof are produced by acylating a suitably substituted octahydro-1H-indole with a suitably activated substituted carboxylic acid and when desired hydrolyzing the resulting product. The compounds of the invention, their salts and pharmaceutical compositions thereof are useful as antihypertensive agents.Type: GrantFiled: February 17, 1981Date of Patent: September 21, 1982Assignee: Warner-Lambert CompanyInventors: Milton L. Hoefle, George Bobowski
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Patent number: 4328168Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of a cyclic polyether compound and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.Type: GrantFiled: October 27, 1980Date of Patent: May 4, 1982Assignee: Emery Industries, Inc.Inventor: Richard G. Fayter, Jr.
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Patent number: 4328169Abstract: This invention provides a convenient and commercially adaptable process for the preparation of vinylcyclopropane derivatives in high yield. For the process an alkylating agent and activated methylene compound are reacted in the presence of an alkylene oxide derivative and alkali metal compound. Water can also be present and/or the reaction may be carried out in an inert organic diluent.Type: GrantFiled: October 27, 1980Date of Patent: May 4, 1982Assignee: Emery Industries, Inc.Inventor: Allen L. Hall