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: 5834485Abstract: The subject invention pertains to quinolinesulfonamides. The subject compounds can be used to treat disease states, such as those that are associated with proteins that mediate cellular activity, for example, by inhibiting phosphodiesterase IV (PDE IV) or tumor necrosis factor (TNF). The invention also pertains to methods of treating disease states, including those states capable of being modulated by inhibition of PDE IV or TNF.Type: GrantFiled: May 20, 1997Date of Patent: November 10, 1998Assignee: Chiroscience LimitedInventors: Hazel Joan Dyke, John Gary Montana
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Patent number: 5831094Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.Type: GrantFiled: February 20, 1996Date of Patent: November 3, 1998Assignee: Merrell Pharamceuticals Inc.Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
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Patent number: 5808067Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives which can be dehydrated to 2-aminobut-2-ene dioic acid derivatives, which can be subsequently converted to pyridine and quinoline derivatives.Type: GrantFiled: December 21, 1994Date of Patent: September 15, 1998Assignee: Hoechst Celanese CorporationInventors: John Saukaitis, Franklin B. Gupton
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Patent number: 5708174Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.Type: GrantFiled: April 11, 1995Date of Patent: January 13, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
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Patent number: 5707844Abstract: The present invention is directed to immunoassay reagents including specific antibodies to quinoline carboxylic acids, such as brequinar; novel quinoline carboxylic acid haptens useful as standards in immunoassays or for conjugating to large molecular weight carriers as immunogens or conjugating to detectable fluorescent moieties as tracer compounds. The present invention also relates to immunoassays for detecting quinoline carboxylic acids in clinical samples, and finally to kits containing said reagents.Type: GrantFiled: January 13, 1995Date of Patent: January 13, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Douglas Guy Batt, William Galbraith, Paul Moore Simon
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Patent number: 5665881Abstract: A quinoline compound represented by the formula (1) or a salt thereof: ##STR1## wherein the definition of each substituents are described in the specification, which have angiotensin II antagonism and hypotensive action and are useful as an agent for the prevention and treatment of cardiovascular system diseases such as hypertension, heart failure and the like.Type: GrantFiled: October 10, 1995Date of Patent: September 9, 1997Assignees: The Green Cross Corporation, Asahi Glass Co., Ltd.Inventors: Yoshihisa Inoue, Hajime Ebisu, Naomichi Ishida, Norifumi Nakamura, Jun Sasaki, Takashi Okazoe, Yoshitomi Morizawa, Arata Yasuda
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Patent number: 5650514Abstract: The present invention relates to 3-substituted quinoline-5-carboxylic acid derivatives and processes for their preparation.Type: GrantFiled: July 17, 1995Date of Patent: July 22, 1997Assignee: Bayer AktiengesellschaftInventors: Jurgen Stoltefuss, Michael Negele, Karl-Heinz Wahl, Jan-Bernd Lenfers, Samir Samaan
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Patent number: 5624933Abstract: Method of preparation of 6-fluoro-2-halogen quinoline of general formula (I) wherein R is a hydrogen atom or an alkyl radical and Hal and Hal' are identical or different halogen atoms. The invention is characterized in that a halogenating agent is made to act on hydroxy-1 quinoline of general formula (II) wherein Hal is defined as above and R.sub.1 is defined as R excepting a hydrogen atom, the acid function being optionally released if a 6-fluoro-2-halogen quinoline is to be obtained for which R is a hydrogen atom.Type: GrantFiled: June 7, 1995Date of Patent: April 29, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Herve Garcia, Roland Jacquot, Patrick Leon
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Patent number: 5614635Abstract: The present invention provides an improved method for the preparation of pyridine-2,3-dicarboxylic acids by the continuous oxidation of substituted quinolines.Type: GrantFiled: August 16, 1995Date of Patent: March 25, 1997Assignee: American Cyanamid CompanyInventor: Paul E. Miller
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Patent number: 5605896Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: August 31, 1994Date of Patent: February 25, 1997Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5604227Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: April 13, 1995Date of Patent: February 18, 1997Assignee: Imperial Chemical Industries PLCInventors: Thomas M. Bare, Richard B. Sparks
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Patent number: 5599814Abstract: The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.Type: GrantFiled: April 24, 1995Date of Patent: February 4, 1997Assignee: Imperial Chemical Industries, PLCInventors: Thomas M. Bare, Richard B. Sparks
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Patent number: 5597833Abstract: Substituted quinol-2-yl-methoxy-phenylacetic acid derivatives are prepared by reacting correspondingly substituted phenols with quinolylmethyl halides or by reacting unsubstituted phenols with quinolylmethyl halides and subsequent alkylation. The substituted quinol-2-yl-methoxy-phenylacetic acid derivatives may be employed as active substances in medicaments.Type: GrantFiled: August 4, 1993Date of Patent: January 28, 1997Assignee: Bayer AktiengesellschaftInventors: Michael Matzke, Klaus-Helmut Mohrs, Siegfried Raddatz, Romanis Fruchtmann, Reiner M uller-Peddinghaus, Armin Hatzelmann
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Patent number: 5578609Abstract: This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, and chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, in a mammal.Type: GrantFiled: August 3, 1995Date of Patent: November 26, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Douglas G. Batt, Joseph J. Petraitis, Susan R. Sherk
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Patent number: 5559140Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.Type: GrantFiled: June 30, 1993Date of Patent: September 24, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
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Patent number: 5541323Abstract: Anhydride compounds which contain at least one rodlike mesogenic moiety and at least two anhydride groups per molecule, wherein each of said aromatic anhydride groups is linked to the mesogen via an ester linkage are prepared. These anhydride compounds are useful in curing epoxy resins to provide the cured products with one or more improved properties.Type: GrantFiled: January 18, 1995Date of Patent: July 30, 1996Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5523312Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 4, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
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Patent number: 5523408Abstract: This invention relates to 2-carbocyclic and 2-heterocyclic quinoline-4-carbocyclic acid compounds, and salts thereof, to pharmaceutical compositions comprising such compounds, and to methods of using such compounds for the treatment and/or prevention of organ transplantation rejection, graft versus host disease, and chronic inflammatory diseases, including but not limited to psoriasis and rheumatoid arthritis, in a mammal.Type: GrantFiled: March 25, 1994Date of Patent: June 4, 1996Assignee: The Dupont Merck Pharmaceutical CompanyInventors: Douglas G. Batt, Joseph J. Petraitis, Susan R. Sherk
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Patent number: 5519022Abstract: The invention concerns .alpha.,.alpha.-dialkylbenzyl derivatives of the formula I ##STR1## wherein Ar.sup.1 is phenyl or naphthyl, or a 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;A.sup.1 is a direct link to X.sup.1 or is (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl or sulphonyl;the phenylene group may optionally bear one or two substituents R.sup.3 ;each of R.sup.1 and R.sup.2, which may be the same or different is (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, fluoro-(1-4C)alkyl, phenyl or phenyl-(1-4C)alkyl, provided that both of R.sup.1 and R.sup.2 are not methyl or fluoromethyl; andQ is cyano, amino, nitro, formyl, (1-4C)alkoxy, thiazolyl or (2-4C)alkanoyl;or a pharmaceutically-acceptable salt thereof;processes for their manufacture; pharmaceutical compositions containing them and their use as 5-lipoxygenase inhibitors.Type: GrantFiled: November 10, 1993Date of Patent: May 21, 1996Assignees: Imperial Chemical Industries Plc, ICI PharmaInventors: Philip N. Edwards, David Waterson
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Patent number: 5478845Abstract: Piperidine derivatives of formula ##STR1## wherein A is straight or branched alkyl, alkoxy-alkyl, or alkenyl; X is O or NH; Y is O, S, NH, NCN, or N-alkyl; R.sup.1 is 6-fluoro-1,2-benzisoxazol-3-yl, 6-fluoro-1H-indazol-3-yl, or 6-fluoro-1-methyl-1H-indazol-3-yl; R.sup.2 is alkyl or phenyl; and R.sup.3 is phenyl optionally substituted, or R.sup.3 is ##STR2## wherein Z represents a 5- or 6-membered heterocyclic ring; or R.sup.2 and R.sup.3 together with the nitrogen atom form a fused heterocyclic ring system; or pharmaceutically acceptable salts thereof are useful in the treatment of indications related to the CNS-system, cardiovascular system or to gastrointestinal disorders.Type: GrantFiled: May 23, 1994Date of Patent: December 26, 1995Assignee: Novo Nordisk A/SInventors: John B. Hansen, Frederik C. Gronvald, John P. Mogensen
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Patent number: 5476940Abstract: The present invention relates to novel 3-substituted quinoline-5-carboxylic acids, a process for their preparation and their use in the preparation of 4-quinolyl-dihydropyridines.Type: GrantFiled: September 29, 1993Date of Patent: December 19, 1995Assignee: Bayer AktiengesellschaftInventor: Jurgen Stoltefuss
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Patent number: 5474994Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.Type: GrantFiled: May 26, 1993Date of Patent: December 12, 1995Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5416117Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: February 28, 1994Date of Patent: May 16, 1995Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5409835Abstract: Fluorescent, calcium-binding probe compounds having visible-light excitation and emission wavelengths, and a method of usage for these probe compounds in making wavelength-ratiometric or intensity-ratiometric measurements of calcium ion concentration in samples. The probe compounds generally relate to a heterocyclic part as bonded to a Ca.sup.2+ binding unit, namely, BAPTA, via an ethylenically unsaturated group; preferred examples of the heterocyclic group include benzothiazole, naphthothiazole, thiaflavin, indolenine, chloroindolenine, methoxybenzothiazole, and methoxyindolenine.Type: GrantFiled: December 30, 1992Date of Patent: April 25, 1995Assignee: The University of Maryland at BaltimoreInventors: Joseph R. Lakowicz, Engin U. Akkaya
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Patent number: 5410062Abstract: There are provided crystalline substituted-2,3-dicarboxypyridinium nitrate salts, the preparation thereof and the use thereof in the isolation and purification of important substituted pyridinedicarboxylic acid herbicide intermediates.Type: GrantFiled: February 2, 1994Date of Patent: April 25, 1995Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5393891Abstract: The present invention is directed to immunoassay reagents including specific antibodies to quinoline carboxylic acids, such as brequinar; novel quinoline carboxylic acid haptens useful as standards in immunoassays or for conjugating to large molecular weight carriers as immunogens or conjugating to detectable fluorescent moieties as tracer compounds. The present invention also relates to immunoassays for detecting quinoline carboxylic acids in clinical samples, and finally to kits containing said reagents.Type: GrantFiled: June 8, 1993Date of Patent: February 28, 1995Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Douglas G. Batt, William Galbraith, Paul M. Simon
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Patent number: 5391747Abstract: A (quinolin-2-yl-methoxy) phenylacyl-sulphonamide or -cyanamide of the formula ##STR1## and physiologically acceptable salts thereof. The (quinolin-2-yl-methoxy)phenylacylsulphonamide or -cyanamide is useful as an active compound in medicaments, particularly as a lipoxygenase inhibitor.Type: GrantFiled: September 23, 1991Date of Patent: February 21, 1995Assignee: Bayer AktiengesellschaftInventors: Siegfried Raddatz, Klaus-Helmut Mohrs, Romanis Fruchtmann, Christian Kohlsdorfer, Pia Theisen-Popp, Reiner Muller-Peddinghaus
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Patent number: 5384322Abstract: The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the nitrogen and carbon atoms to which it is bound, a heterocycle,B represents, with the nitrogen atom to which it is bound, a heterocycle,R.sub.1 represents alkoxy, benzyloxy, phenoxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or substituted or unsubstituted cycloalkyl,their enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid, medicinal products containing the same.Type: GrantFiled: September 30, 1993Date of Patent: January 24, 1995Assignee: Adir et CompagnieInventors: Michel Vincent, Georges Remond, Bernard Portevin, Yolande Herve, Jean Lepagnol, Guillaume de Nanteuil
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Patent number: 5344935Abstract: There are provided alkyl esters of 5-heterocyclic-pyridine-2,3-dicarboxylic acids useful as intermediates for the preparation of highly effective 5-heterocyclic-2-(2-imidazolin-2-yl)pyridine herbicidal agents and methods for the preparation thereof.Type: GrantFiled: May 27, 1993Date of Patent: September 6, 1994Assignee: American Cyanamid CompanyInventor: John M. Finn
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Patent number: 5338847Abstract: Described are a class of chemiluminescent compound characterized by the presence an aryl ester, thioester or amide of a carboxylic acid substituted heterocyclic ring that is susceptible to chemical attack (such as by oxidic attack) to dissociate the heterocyclic ring to a transient compound. The heterocyclic ring is ring carbon-bonded to the carbonyl of the ester, thioester and amide moiety and possesses a heteroatom in an oxidation state that allows chemiluminescence by dissociating a compound ("intermediate") that decays to produce chemiluminescence, at the carbon bonded to the carbonyl. The aryl ring or ring system is ring carbon-bonded to the oxygen, sulfur or nitrogen of the ester, thioester or amide, as the case may be, and contains at least three substituents on a six-member ring. The substitution on the six-member ring comprises three or more groups acting in concert to sterically and electronically hinder hydrolysis of the ester, thioester or amide linkage.Type: GrantFiled: March 30, 1992Date of Patent: August 16, 1994Assignee: London Diagnostics, Inc.Inventor: Frank McCapra
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Patent number: 5334724Abstract: A process for the preparation of a substituted 2-chloropyridine derivatives of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or various other radicals, which comprises reacting a pyridine-1-oxide of the formula ##STR2## with an aromatic carbonyl chloride in the presence of an inert organic solvent and in the presence of an acid acceptor at a temperature between about -20.degree. C. and 200.degree. C.Type: GrantFiled: June 24, 1992Date of Patent: August 2, 1994Assignee: Bayer AktiengesellschaftInventors: Dieter Kaufmann, Klaus Jelich, Rudolf Braden, Winfried Rosen
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Patent number: 5328909Abstract: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.Type: GrantFiled: June 25, 1992Date of Patent: July 12, 1994Assignee: Mitsubishi Kasei CorporationInventors: Ryoichi Ando, Yasuhiro Morinaka, Chizuko Takahashi, Yoshikuni Tamao, Akihiro Tobe
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Patent number: 5326770Abstract: This invention relates to monoamine oxidase-B (MAO-B) inhibitory 5-substituted 2,4-thiazolidinediones, such as Formula I, to pharmaceutical compositions thereof, process of preparation, and methods of use in mammals to treat cognitive disorders, neurological dysfunction, and/or mood disturbances such as, but not limited to degenerative nervous system diseases.Type: GrantFiled: July 17, 1992Date of Patent: July 5, 1994Assignee: The Du Pont Merck Pharmaceutical CompanyInventor: Wendell W. Wilkerson
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Patent number: 5322948Abstract: The present invention pertains to a method of preparing substituted and unsubstituted N-hydroxy-2-aminobutane diacid derivatives. The invention also pertains to the use of N-hydroxy-2-aminoethane derivatives (including the N-hydroxy-2-aminobutane diacid derivatives) in the preparation of pyridine derivatives.Type: GrantFiled: January 2, 1992Date of Patent: June 21, 1994Assignee: Hoechst Celanese CorporationInventors: Varadaraj Elango, Donald R. Larkin, John R. Fritch, Michael P. Bodman, Werner H. Mueller, Bernard F. Gupton, John C. Saukaitis
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Patent number: 5321136Abstract: A chemiluminescent label compound and conjugate containing the same, in which the compound involves a fused ring system comprising a(i) hetercyclic ring as a fused member thereof in which the heterocyclic ring contains(a) one or more nitrogen heteroatoms in the ring;(b) at least one saturated or unsaturated ring in fused state with the heterocyclic ring;(c) an available carbon atom in the heterocyclic ring that is adjacent to a carbon forming a fused ring with the heterocyclic ring; and(d) at least one substituent that is peri relative said available carbon of the heterocyclic ring, which substituent serves to enhance the hydrolytic stability of the chemiluminescent label compound; and(ii) a leaving group coupled to the heterocyclic ring through a carbon adjacent to a fused ring carbon such that the leaving group and heterocyclic ring join to form a difunctional carboxy-containing linkage in which the carboxy carbon is directly bonded to the carbon of the heterocyclic ring adjacent to a fused ring carbon,(a)Type: GrantFiled: March 30, 1992Date of Patent: June 14, 1994Assignee: London Diagnostics, Inc.Inventor: Frank McCapra
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Patent number: 5310915Abstract: Purification of 7-chloroquinoline-8-carboxylic acids I ##STR1## (X=H, halogen, lower alkyl group) by recrystallization from lower alcohols which are miscible with water, by carrying the recrystallization in the presence of small amounts of a base.The quinolinecarboxylic acids I are valuable crop protection agents.Type: GrantFiled: August 3, 1992Date of Patent: May 10, 1994Assignee: BASF AktiengesellschaftInventors: Gernot Reissenweber, Knut Koob, Winfried Richarz
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Patent number: 5306820Abstract: (Quinolin-2-yl-methoxy)phenylacetic acids are known as inhibitors of enzymatic reactions in the context of arachidonic acid metabolism.Enantiomerically pure (quinolin-2-yl-methoxy)phenylacetic acids can be prepared in a simple manner and in high purity and yield by diastereoselective alkylation of corresponding (quinolin-2-yl-methoxy)phenylacetic acid menthyl esters and subsequent specific removal of the ester radical with acids.Type: GrantFiled: April 10, 1992Date of Patent: April 26, 1994Assignee: Bayer AktiengesellschaftInventors: Matthias Decker, Klaus-Helmut Mohrs, Siegfried Raddatz
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Patent number: 5296601Abstract: A process for producing a carboxylic acid ester, which comprises reacting an organic chloride having at least one chlorine atom on its ring of a substituted or unsubstituted, aromatic or heterocyclic hydrocarbon with carbon monoxide and an amine or an alcohol in the presence of a base by using as catalysts a palladium compound and a phosphine compound represented by the general formula (V):(R).sub.2 P--X--P(R).sub.2 (V)wherein R is an alkyl group or a substituted or unsubstituted phenyl group, and X is an alkylene group having 1 to 6 carbon atoms, ##STR1## or a binaphthyl group.Type: GrantFiled: May 27, 1992Date of Patent: March 22, 1994Assignee: Nihon Nohyaku Co., Ltd.Inventors: Keiji Suto, Masaaki Kudo, Moriharu Yamamoto
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Patent number: 5290936Abstract: A novel chemiluminescent labeling compositions comprising an ester, thiolester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinguished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with --NO.sub.2 meta or para substituents thereon.Type: GrantFiled: March 30, 1992Date of Patent: March 1, 1994Assignee: London Diagnostics, Inc.Inventors: Iraj Beheshti, Harlen Koelling
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Patent number: 5284951Abstract: A novel chemiluminescent labeling compositions comprising an ester, thioester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinguished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with meta and/or para substituents thereon that possess an electron withdrawing capacity characterized as a .sigma..sub.p value greater than 0 and less than 1.Type: GrantFiled: March 30, 1992Date of Patent: February 8, 1994Assignee: London Diagnostics, Inc.Inventors: Frank McCapra, Iraj Beheshti
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Patent number: 5284952Abstract: A chemiluminescent labeling composition comprising an ester, thioester or amide covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinquished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with meta and/or para --SO.sub.2 -- substituents thereon.Type: GrantFiled: March 30, 1992Date of Patent: February 8, 1994Assignee: London Diagnostics, Inc.Inventor: Kastooriranganathan Ramakrishnan
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Patent number: 5283334Abstract: A chemiluminescent compound possessing an aryl ester, thioester or amide of a carboxylic acid substituted heterocyclic ring or ring system that is susceptible to chemical attack to dissociate the heterocyclic ring to a transient compound. The heterocyclic ring is ring carbon-bonded to the carbonyl of the ester, thioester or amide moiety and possesses a heteroatom in an oxidation state that allows chemiluminescence by dissociating a compound at the carbon bonded to the carbonyl that decays to produce chemiluminescence. The heterocyclic ring or ring sustem contains bonded to it through an organic moiety, a functional group that is functionally reactive with an active hydrogen containing compound. The aryl ring is a ring or ring system that is ring carbon-bonded to the oxygen, sulfur or nitrogen of the ester, thioester or amide, as the case may be, and contains substituents on a six-member ring that act to sterically and electronically hinder hydrolysis of the ester, thioester or amide linkage.Type: GrantFiled: March 30, 1992Date of Patent: February 1, 1994Assignee: London Diagnostics, Inc.Inventor: Frank McCapra
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Patent number: 5281712Abstract: A novel chemiluminescent labeling compositions comprising an ester or thiolester covalently and jointly bonded to (1) a carbon of a heterocyclic ring or ring system that is susceptible to attack by peroxide or molecular oxygen and (2) an aryl ring or ring system wherein the heterocyclic ring or ring system is distinquished by a heteroatom thereof in an oxidation state which causes the attacked carbon atom to form an intermediate that decays and produces chemiluminescence; the aryl ring or ring system contains at least three substituents on a six-member aromatic hydrocarbon that together sterically and electronically hinder hydrolysis of the linkage, which substituents involve ortho substituent groups on the aryl in conjunction with quaternary ammonium meta or para substituents thereon.Type: GrantFiled: March 30, 1992Date of Patent: January 25, 1994Assignee: London Diagnostics, Inc.Inventors: Frank McCapra, Beheshti Iraj, Kastooriranganathan Ramakrishnan
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Patent number: 5270469Abstract: A process for preparing 3-phenyl-quinoline-5-carboxylic acid comprising reacting 4-amino-3-hydroxyphthalide with phenylacetaldehyde.Type: GrantFiled: November 3, 1992Date of Patent: December 14, 1993Assignee: Bayer AktiengesellschaftInventor: Jurgen Stoltefuss
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Patent number: 5221791Abstract: This invention relates to hydrolysis resistant, water-soluble ammonium salt solids which are biologically active and which are described by the formula ##STR1## wherein m has a value of from 1 to 3; n has a value of from 1 to 4 and is equal to the free valences in anion R; p has a value of from 1 to 3; R.sub.1, R.sub.2 and R.sub.3 are each independently selected from the group of hydrogen, and C.sub.1 to C.sub.2 alkyl; R.sub.5 and R.sub.6 are each independently selected from the group of hydrogen, hydroxyalkyl and alkoxyalkyl radicals having from 1 to 10 carbon atoms and R is the anion of a biologically active, water-insoluble anion having at least 1 deprotonized hydrogen and is derived from a biologically active, acidic, organic compound selected from the group of a carboxylic, thiocarbonic, sulfonic, sulfinic, thiosulfonic, thioacid, mono- and di- thiophosphate and phosphorous containing acid, having a pKa* value less than 5.Type: GrantFiled: May 24, 1991Date of Patent: June 22, 1993Assignee: ISP Investments Inc.Inventors: Kolazi S. Narayanan, Ratan K. Chaudhuri, Robert B. Login
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Patent number: 5221678Abstract: Compounds having the Formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.Type: GrantFiled: July 12, 1991Date of Patent: June 22, 1993Assignee: Merck Frosst Canada, Inc.Inventors: Joseph G. Atkinson, John W. Gillard, Erich L. Grimm
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Patent number: 5220027Abstract: This invention provides azamethine compounds represented by the formula (I): ##STR1## wherein X represents ##STR2## R.sub.1 to R.sub.4 represent independently a hydrogen atom, an alkyl group, an alkoxyl group, a halogen atom, a nitro group, a cyano group, a hydroxyl group, an amino group, ##STR3## R.sub.5 and R.sub.6 represent independently a hydrogen atom or an alkyl group which may be substituted by a hydroxyl group; R.sub.7 represents a hydrogen atom, an alkyl group, an alkyoxyl group, a hydroxyl group, a halogen atom, a nitro group, a cyano group, ##STR4## wherein -A represents ##STR5## and R and R' represent independently a hydrogen atom or an alkyl group; and R.sub.10 to R.sub.12 represent independently a hydrogen atom or an alkyl group, a process for producing such compounds, and a medium for recording optical information using these compounds.Type: GrantFiled: April 12, 1991Date of Patent: June 15, 1993Assignee: Sumitomo Chemical Company, LimitedInventors: Takeshi Hioki, Kiyoteru Kojima, Jun Tomioka
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Patent number: 5214146Abstract: Quinolinecarboxylic acid derivatives of the formula: ##STR1## where R.sup.1 and R.sup.2 are identical or different and each is independently of the other hydrogen or halogen,R.sup.3 is C.sub.1 -C.sub.13 -alkoxy, C.sub.1 -C.sub.8 -monoalkylamino or di(C.sub.1 -C.sub.8 alkyl)amino andR.sup.4 and R.sup.5 are identical or different and each is independently of the other hydrogen, C.sub.1 -C.sub.13 -alkyl or C.sub.1 -C.sub.13 -alkoxy,with the proviso that R.sup.3 is not methoxy or ethoxy when at the same time R.sup.1, R.sup.2, R.sup.4 and R.sup.5 are each hydrogen, are useful as color formers for preparing pressure-sensitive papers.Type: GrantFiled: October 15, 1991Date of Patent: May 25, 1993Assignee: BASF AktiengesellschaftInventors: Ulrike Schloesser, Gerhard Wagenblast
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Patent number: RE35177Abstract: A pyridine-compound is reacted with fluorine together with a .[.Bronsted.]. .Iadd.Bronsted .Iaddend.acid-compound or Lewis acid to form a N-fluoropyridinium salt which is very active to other compounds but is very selective for the preparation of a desired product and this product is very useful for a fluorine-introducing agent which makes it useful for the preparation of fluoro-compounds such as thyroid inhibitor.Type: GrantFiled: February 17, 1994Date of Patent: March 12, 1996Assignees: Sagami Chemical Research Center, Chichibu Onoda Cement CorporationInventors: Teruo Umemoto, Kyoichi Tomita, Kosuke Kawada, Ginjiro Tomizawa