Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Six-membered Hetero Ring Patents (Class 546/298)
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Patent number: 6015820Abstract: Compounds of formula (3) in which:R.sub.1 and R.sub.2 independently represent an atom of hydrogen, an aliphatic group or an alkyloxyalkyl group in which the alkyl chains are from C.sub.1 to C.sub.4 or together form an aromatic ring;R.sub.3 represents:an atom of hydrogen, oran NHR.sub.5 group in which R.sub.5 represents an atom of hydrogen or a COR.sub.6 group in which R.sub.6 is an aliphatic or aromatic group, oran NO.sub.2 group ora COOR.sub.7 group in which R.sub.7 is an aliphatic group,R.sub.4 represents a phenyl or heterocyclic group.These compounds can be used in the treatment of illnesses linked to the HIV virus.Type: GrantFiled: April 15, 1998Date of Patent: January 18, 2000Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Emile Bisagni, Valerie Dolle, Chi Hung Nguyen, Michel Legraverend, Anne-Marie Aubertin, Andre Kirn, Marie-Line Andreola, Laura Tarrago-Litvak, Michel Ventura
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Patent number: 6015905Abstract: A process for preparing 2-(6-substituted pyrid-2-yloxymethyl)phenyacetates especially useful as intermediates for producing agricultural fungicides. The invention provides a compound having the formula (I): wherein A and D are independently selected from the group comprising halo, hydroxy, halo(C.sub.1-4)alkyl, C.sub.1-4 alkoxy, thio(C.sub.1-4)alkoxy, halo(C.sub.1-4)alkoxy, phenyl, phenoxy, nitro, amino, aclyamino, cyano, carboxy, C.sub.1-4 alkoxycarbonyl and C.sub.1-4 alkylcarbonyloxy, or D is C.sub.1-4 alkyl, and m is 0 or an integer of from 1 to 3. The process comprises treating a compound of formula (II): ##STR1## wherein A, D and m are defined as above and M is a metal atom, with a compound of formula (III): ##STR2## wherein L is a leaving group.Type: GrantFiled: December 2, 1997Date of Patent: January 18, 2000Assignee: Zeneca LimitedInventors: David John Ritchie, Gordon Richard Munns, Julie Forrester, Michael Charles Henry Standen, Paul Anthony Worthington, Raymond Vincent Heavon Jones
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Patent number: 6015569Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: November 17, 1997Date of Patent: January 18, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6011063Abstract: Ortho-substituted benzoylguanidines of the formula I ##STR1## in which R(1) to R(5) have the meanings given in the claims, are suitable as antiarrhythmic pharmaceuticals having a cardioprotective component for infarct prophylaxis and for infarct treatment and also for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes in the formation of ischemically induced damage, in particular in the illicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: June 3, 1997Date of Patent: January 4, 2000Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5985815Abstract: New compounds useful as bleach activators as well as new percarboxylic acids, which may be formed as intermediates upon reaction of such activators with peroxygen bleach source in aqueous solution, include nitrogen-containing heterocyclic groups. Preferred activators are symmetrical derivatives of dibasic carboxylic acids, having N,N'diacyl N-heterocyclic groups usually lactams. They are produced by reaction of 2 moles of the lactam with one mole of dibasic acid chloride or anhydride.Type: GrantFiled: April 3, 1997Date of Patent: November 16, 1999Assignee: Warwick International Group LimitedInventors: John Townend, Jan Darrel Crowther
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Patent number: 5972977Abstract: Ophthalmic pharmaceutical compositions containing a pharmaceutically acceptable ophthalmic carrier and an inflammation-treating amount of a nitrone compound are disclosed. Also disclosed are methods for treating ocular inflammation conditions, such as uveitis, using pharmaceutical compositions.Type: GrantFiled: April 23, 1997Date of Patent: October 26, 1999Assignee: Centaur Pharmaceuticals, Inc.Inventors: Kenneth W. Narducy, Efraim Duzman, John Michael Carney, Allan Lee Wilcox
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Patent number: 5968875Abstract: The present invention provides novel 2-methoximino-2-(pyridinyloxymethyl)phenyl acetamide compounds with carboxylic acid substituents on the pyridine ring, their use as fungicidal compounds, and their use in fungicidal compositions comprising at least one of the 2-methoximino-2-(pyridinyloxymethyl)phenyl acetamide compounds as the active ingredient.Type: GrantFiled: January 29, 1998Date of Patent: October 19, 1999Assignee: Dow AgroSciences LLCInventors: Scott J. Bis, Emily J. Canada, David H. Cooper, Christopher S. Galka, Neil Kirby, David G. Ouimette, David E. Podhorez, Mary Pieczko, Rebecca Rezac, Brent J. Rieder, John K. Swayze, Vidyadhar B. Hegde, Gary L. Sampson
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Patent number: 5962687Abstract: The invention relates to a method for the production of magnesium pyridoxal-5'-phosphate glutamate, in which pyridoxine or an acid addition salt thereof is oxidised with manganese (IV) oxide to pyridoxal; pyridoxal is reacted with p-phenetidine under formation of the Schiff's base p-phenetidyl-pyridoxal; p-phenedityl-pyridoxal is selectively phosphorylated on the 5'-hydroxymethyl group under formation of p-phenetidyl-pyridoxal-5'-phosphate; p-phenetidyl-pyridoxal-5'-phosphate is hydrolysed under formation of an alkali metal salt of pyridoxal-5'-phosphate; the alkali metal ions are removed in order to obtain pyridoxal-5'-phosphate; pyridoxal-5'-phosphate is reacted with a reaction product of a magnesium alcoholate and L-glutarnic acid; and the formed magnesium pyridoxal-5'-phosphate glutamate is isolated. Furthermore, the invention relates to intermediate products obtained with this method.Type: GrantFiled: June 29, 1998Date of Patent: October 5, 1999Assignee: Steigerwald Arzneimittelwerk GmbHInventors: Panagiotis Maidonis, Werner Schneider
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Patent number: 5962481Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.Type: GrantFiled: October 6, 1997Date of Patent: October 5, 1999Assignee: American Cyanamid CompanyInventors: Jeremy Ian Levin, Frances Christy Nelson
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Patent number: 5958956Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl;R.sup.2 is C.sub.1-6 -alkyl or adamantyl;R.sup.3 is C.sub.1-6 -alkyl or hydroxy; orR.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --;R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy;R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl;R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl;Y is oxygen or sulphur; andn is 3, 4 or 5,and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.Type: GrantFiled: January 15, 1998Date of Patent: September 28, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5942623Abstract: The invention relates to a process for the preparation of 2-(pyrid-2-yloxymethyl)phenylacetates of formula (I) useful as intermediates for agricultural pesticides, which comprises reacting a 2-pyridine of formula (II), wherein L is a leaving group and A, D and m are as defined in the description with a compound MO--CH.sub.2 R where M is a metal atom and R is the residue of a metal salt of phenylacetic acid. It also includes the compounds MO--CH.sub.2 R, a process for their preparation and a "one-pot" process for the preparation of 2-(pyrid-2-yloxymethyl) phenylacetates from 3-isochromanone.Type: GrantFiled: February 19, 1998Date of Patent: August 24, 1999Assignee: ZENECA LimitedInventors: Alfred Glyn Williams, Gordon Richard Munns, Paul Anthony Worthington
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Patent number: 5922710Abstract: Iminooxybenzylcrotonate esters of the formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen,unsubst. or subst. alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy orin the case where n is 2, additionally an unsubst. or subst. bridge bonded to two adjacent ring atoms;R.sup.1 is C.sub.1 -C.sub.4 -alkyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 -alkyl;R.sup.3 is hydrogen, cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio or cycloalkyl;R.sup.4 is a 5 to 10-membered mono- or bicyclic, substituted heteroaromatic ring system,processes for their preparation and their use are described.Type: GrantFiled: May 22, 1997Date of Patent: July 13, 1999Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Wassilios Grammenos, Hubert Sauter, Franz Rohl, Eberhard Ammermann, Gisela Lorenz, Norbert Gotz
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5891737Abstract: Predetermined combinatorial libraries of non-peptide compounds are disclosed. Compounds useful for generating such libraries are also disclosed.Type: GrantFiled: June 7, 1995Date of Patent: April 6, 1999Assignee: ZymoGenetics, Inc.Inventors: Nand Baindur, Virender M. Labroo
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Patent number: 5891917Abstract: The present invention relates to molecules capable of modulating tyrosine signal transduction to prevent and treat cell proliferative disorders or cell differentiation disorders associated with particular tyrosine kinases by inhibiting one or more abnormal tyrosine kinase activities.Type: GrantFiled: October 24, 1997Date of Patent: April 6, 1999Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Asaad S. Nematalla, Gerald McMahon
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Patent number: 5863930Abstract: Trisubstituted biphenyls are prepared by reacting corresponding pyridones with biphenylmethyl halogen compounds. The trisubstituted biphenyls can be employed as active compounds in medicaments.Type: GrantFiled: December 18, 1995Date of Patent: January 26, 1999Assignee: Bayer AktiengesellschaftInventors: Jurgen Dressel, Peter Fey, Rudolf Hanko, Walter Hubsch, Thomas Kramer, Ulrich E. Muller, Matthias Muller-Gliemann, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch, Siegfried Zaiss
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Patent number: 5830890Abstract: Compounds, useful as plant fungicides, having the formula (I): ##STR1## or a stereoisomer thereof, wherein A is CH or N, B is OCH.sub.3 or NHCH.sub.3, X is CH.sub.2, CH.sub.2 O, O or S, Y is R.sup.1 --C.dbd.C--R.sup.2 or R.sup.1 --CH--CH--R.sup.2 wherein R.sup.1 and R.sup.2 are independently H, halo, hydroxy, alkyl, haloalkyl, alkoxy, haloalkoxy, cyano, nitro, amino, mono- or dialkylamino, alkanoylamino, carboxy, alkoxycarbonyl, aminocarbonyl, mono- or di-alkylaminocarbonyl, alkylcarbonyloxy, optionally substituted aryl, optionally substituted aralkyl or optionally substituted aryloxy or R.sup.1 and R.sup.2 join to form with the carbon atoms to which they are attached an optionally substituted benzene ring, and Z is CH.sub.2, CHCH.sub.3, C(CH.sub.3).sub.2 or C.dbd.O.Type: GrantFiled: September 30, 1996Date of Patent: November 3, 1998Assignee: Zeneca LimitedInventors: Ian Richard Matthews, Paul John deFraine, Patrick Jelf Crowley, John Williams
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Patent number: 5811459Abstract: The invention relates to compounds of the formula (I): ##STR1## wherein A, B and D are various ring systems such as phenyl, R.sup.1 includes carboxy, R.sup.3 is hydrogen or C.sub.1-4 alkyl and Z is a linking group such as --(CH(R.sup.5)).sub.m -- wherein m is 2, 3 or 4, and R.sub.5 includes hydrogen and methyl; and pharmaceutically acceptable salts and in vivo hydrolysable esters or amides thereof, processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of pain.Type: GrantFiled: June 4, 1996Date of Patent: September 22, 1998Assignee: Zeneca LimitedInventors: Gloria Ann Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5808080Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: May 2, 1997Date of Patent: September 15, 1998Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, David Andrew Neel, Mark Alan Winter
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Patent number: 5786515Abstract: A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.Type: GrantFiled: August 30, 1996Date of Patent: July 28, 1998Assignee: Merck & Co., Inc.Inventors: Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen
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Patent number: 5770613Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of pyridine aldehydes, thioaldehyde, acetals, or thioacetals. Such compounds are characterized by the following structure: ##STR1## X.sub.1 is selected from the group consisting of oxygen, sulfur, sulfone, sulfinyl, and --NR-- where R is hydrogen, alkyl, aryl, and aralkyl. R.sub.1 is --Y.sub.n R.sub.6, in which n is an integer between 0 and 10 and each Y.sub.n for n greater than 0 independently is methylene, methine, or quarternary carbon. R.sub.6, for any value of n (i.e.Type: GrantFiled: September 29, 1995Date of Patent: June 23, 1998Assignee: Geron CorporationInventors: Federico C. A. Gaeta, Elaine C. Stracker
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Patent number: 5760062Abstract: Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds that are derivatives of pyrido?b!thiophenes, pyrido?b!furans, pyridine ethers or pyridine thioethers. Such compounds are characterized by the following structure: ##STR1## X.sub.3 is oxygen or sulfur; and the double dashed lines between X.sub.4 and X.sub.5 indicate an optional double bond, which, when present, forms a fused, bicyclic pyrido?b!furan or pyrido?b!thiophene ring system, depending upon whether X.sub.3 is oxygen or sulfur, respectively. When the double bond is not present, the compound is a monocyclic pyridine ether or thioether, again depending upon whether X.sub.3 is oxygen or sulfur. X.sub.4 is --CH.sub.2 R.sub.21 or --CR.sub.21 --, where R.sub.Type: GrantFiled: April 18, 1995Date of Patent: June 2, 1998Assignee: Geron CorporationInventors: Federico C.A. Gaeta, Adam A. Galan, Michael R. Kozlowski, Karen R. Prowse, Elaine C. Stracker, Patricia A. Peterli-Roth
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Patent number: 5760236Abstract: Substituted pyridines of the general formula: ##STR1## wherein R.sup.1 is hydroxyl or chlorine, and a) X is hydrogen or chlorine, R.sup.2 and R.sup.3 together are .dbd.O, R.sup.4 is a group of the formula --OR.sup.5 and R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl, orb) X is hydrogen and R.sup.2, R.sup.3 and R.sup.4 together are .dbd.N--NH--, orc) X and R.sup.2 each is hydrogen and R.sup.3 and R.sup.4 together are --O--, ord) X and R.sup.2 each is hydrogen, R.sup.3 is hydroxyl and R.sup.4 is amino or hydroxyl.The compounds are obtained by subjecting nicotine to microbiological oxidation to give 5-succinoyl-2-pyridone, followed by chemical reactions. The compounds are suitable as intermediates for the preparation of pharmaceutically active compounds.Type: GrantFiled: November 21, 1995Date of Patent: June 2, 1998Assignee: Lonza, Ltd.Inventors: Andreas Kiener, Jean-Paul Roduit, Alain Wellig
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Patent number: 5726315Abstract: The compounds of the invention are tri-substituted pyridine intermediates, useful in the preparation of final products, wherein said final products are involved in the preparation of medicaments. Said medicaments are useful for the treatment of various diseases including psoriasis. A compound of the formula (II): ##STR1## wherein R.sup.1 is hydrogen, benzyl or a group of the formula (A): ##STR2## in which n is 1 to 20; and R.sup.5 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or trifluoromethyl; and R.sup.7 is a leaving group consisting of halogen, OTf or (Trifluorate, e.g. OSO.sub.2 CF.sub.3), OSO.sub.2 alkyl and OSO.sub.2 Ar wherein Ar represents optionally substituted aryl.Type: GrantFiled: May 23, 1996Date of Patent: March 10, 1998Assignee: SmithKline Beecham plcInventors: Peter William Sheldrake, Laurence Charles Powling, Peter William Bickle
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Patent number: 5726191Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl;R.sup.2 is C.sub.1-6 -alkyl or adamantyl;R.sup.3 is C.sub.1-6 -alkyl or hydroxy; orR.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --;R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy;R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl;R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl;Y is oxygen or sulphur; andn is 3, 4 or 5,and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.Type: GrantFiled: October 23, 1996Date of Patent: March 10, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr
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Patent number: 5723450Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H, halogen, an aliphatic radical or an aromatic radical, X is O, S or optionally substituted imino, Y is a bond or an optionally substituted bivalent hydrocarbon radical and Z is optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and their use as pesticides, in particular as insecticides, acaricides and fungicides.Type: GrantFiled: September 12, 1994Date of Patent: March 3, 1998Assignee: Hoechst Schering AgrEvo GmbHInventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
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Patent number: 5712393Abstract: The present invention provides a compound of formula (1) ##STR1## in which: R.sub.4 represents a hydrogen atom, a halogen atom or a nitro group;R.sub.6 represents a hydrogen atom or a straight or branched (C.sub.1 -C.sub.6) alkyl group;R.sub.7 represents a chlorine atom or a hydroxyl group; andZ represents: a phenyl group optionally substituted with one or more halogen atoms, straight or branched (C.sub.1 -C.sub.4)alkyl groups, straight or branched (C.sub.1 -C.sub.4)alkoxy groups, or trifluoromethyl, formyl, --CH.sub.2 OR, --CH.sub.2 OCOR, --CH.sub.2 CONRR', --CH.sub.2 ONCOR, --COOR, nitro, --NHR, --NRR' or --NHCOR groups, wherein R and R' are each, independently, a hydrogen atom or a (C.sub.1 -C.sub.7) alkyl group; a heterocyclic group optionally substituted as defined above for phenyl; or a cyclo(C.sub.5 -C.sub.8)alkyl group; additionally, when R.sub.Type: GrantFiled: November 24, 1995Date of Patent: January 27, 1998Assignee: SynthelaboInventors: Jean Michel Altenburger, Gilbert Lassalle
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Patent number: 5696138Abstract: A compound having the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinX, Z, Y, A, D, E, F, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12 have the meanings set forth in the specification, pharmaceutical compositions comprising the same, and a method of treating therewith.The compounds are useful as potassium channel openers.Type: GrantFiled: December 27, 1995Date of Patent: December 9, 1997Assignee: NeuroSearch A/SInventors: S.o slashed.ren-Peter Olesen, Peter Moldt, Ove Pedersen
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Patent number: 5688817Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: November 18, 1997Assignee: Centre Int'l. De Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5681960Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: metal ion-ligand coordination complexes ("MLC"), novel ligands, antibodies specific for MLC, immunoassays utilizing the foregoing, and methods for selecting said antibodies.Type: GrantFiled: May 5, 1995Date of Patent: October 28, 1997Assignee: Abbott LaboratoriesInventor: David K. Johnson
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Patent number: 5670627Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: metal ion-ligand coordination complexes ("MLC"), novel ligands, antibodies specific for MLC, immunoassays utilizing the foregoing, and methods for selecting said antibodies.Type: GrantFiled: May 5, 1995Date of Patent: September 23, 1997Assignee: Abbott LaboratoriesInventor: David K. Johnson
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Patent number: 5670645Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: metal ion-ligand coordination complexes ("MLC"), novel ligands, antibodies specific for MLC, immunoassays utiliizing the foregoing, and methods for selecting said antibodies.Type: GrantFiled: May 23, 1995Date of Patent: September 23, 1997Assignee: Abbott LaboratoriesInventor: David K. Johnson
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Patent number: 5668290Abstract: Novel cephem derivatives represented by the general formula ##STR1## in which the Acyl substituent is a group of the formula ##STR2## wherein Ar is a lipophilic optionally substituted phenyl, naphthyl or pyridyl group; R.sup.1 represents either the residue of a heterocyclic amino acid or a C.sub.2 -C.sub.10 alkyl group substituted by both a carboxyl group and a group of the formula --NR.sup.9 R.sup.10 or ##STR3## in which R.sup.9 and R.sup.10 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl, said C.sub.2 -C.sub.10 alkyl group being optionally interrupted by one or more nitrogen atoms or carbonyl groups, and R.sup.2 and R.sup.3 are each independently hydrogen, alkyl or aminoalkyl are gram-positive antibacterial agents, especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus (also referred to below as MRSA or methicillin-resistant S. aureus).Type: GrantFiled: August 23, 1996Date of Patent: September 16, 1997Assignee: Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Stanley V. D'Andrea, Shelley E. Hoeft, John D. Matiskella, Peter F. Misco, Jr., Bing Yu Luh, Dane M. Springer, Yasutsugu Ueda, John A. Wichtowski
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Patent number: 5668156Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.Type: GrantFiled: April 28, 1995Date of Patent: September 16, 1997Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, William Robert Pilgrim
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Patent number: 5658933Abstract: The invention relates to compounds of the formula I, ##STR1## to a process for their preparation and to their use as pharmaceuticals. The compounds are employed, in particular, as ester prodrugs of prolyl hydroxylase inhibitors for inhibiting collagen biosynthesis and as fibrosuppressive agents.Type: GrantFiled: October 31, 1994Date of Patent: August 19, 1997Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
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Patent number: 5650417Abstract: Substituted pyridines, their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## and to salts thereof in which 1, 2, 3 or 4 of the radicals R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are an aliphatic, alicyclic or araliphatic radical bonded by a --O--CH.sub.2 -- or --O--CO--, and the remaining ones of these radicals are H, halogen or an aliphatic or aromatic radical, X is O, S or optionally substituted imino, Y is a bond or a bivalent radical and Z is an aromatic radical or optionally substituted cycloalkyl or cycloalkenyl. The invention furthermore relates to processes for their preparation and to their use as pesticides, in particular as insecticides, acaricides and fungicides.Type: GrantFiled: September 12, 1994Date of Patent: July 22, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Dieter Bernd Reuschling, Adolf Heinz Linkies, Volkmar Wehner, Rainer Preuss, Wolfgang Schaper, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
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Patent number: 5646285Abstract: The present invention relates to an orthogonally-protected compound of the formula: ##STR1## wherein PG.sub.1 is a first protecting group that is unreactive to a chemistry used at another position within the compound, and that is capable of selective removal without affecting PG.sub.2 or linkage to a solid support; PG.sub.2 is a second protecting group that is unreactive to a chemistry used at another position within the compound, and that is capable of selective removal without affecting PG.sub.1 or linkage to a solid support; Y is CH.sub.2 COOH, CH.sub.2 SO.sub.2 OH, CH.sub.2 PO.sub.2 ROH, CH.sub.2 Ph--COOH, CH.sub.2 Ph--SO.sub.2 OH, or CH.sub.2 Ph--PO.sub.2 ROH; R is H or a substituted or unsubstituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; and n is 1 or 2. PG.sub.1 is preferably a carbamate group, a trityl group, or a trifluoroacetyl group; and PG.sub.2 is preferably an ester.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: ZymoGenetics, Inc.Inventors: Nand Baindur, Virender M. Labroo
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Patent number: 5643914Abstract: This invention relates to a compound of formula 1 ##STR1## or an N-oxide, or a pharmaceutically acceptable salt, where A is CH.sub.2 and Z is S(O).sub.q where q is 0, 1 or 2, CH.sub.2, CHOH, CO, NR.sub.x, or O, orA is C.dbd.O and Z is NR.sub.x ;m is 0-5;R.sub.x is hydrogen or lower alkyl;R is C.sub.1 to C.sub.20 -aliphatic, unsubstituted or substituted five-membered heteroaryl-C.sub.1 to C.sub.10 -aliphatic-O--, unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic where substituted p from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo, or R is C.sub.1 to C.sub.20 -aliphatic-O--, or R is unsubstituted or substituted phenyl-C.sub.1 to C.sub.10 -aliphatic-O-- where substituted phenyl has one or more radicals selected from the group consisting of lower alkoxy, lower alkyl, trihalomethyl, and halo;R.sub.1 is R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)R.sub.4, --(C.sub.1 to C.sub.5 aliphatic)CHO, --(C.sub.1 to C.sub.5 aliphatic)CH.sub.2 OR.sub.5;R.sub.2 and R.sub.Type: GrantFiled: December 19, 1994Date of Patent: July 1, 1997Assignee: SmithKline Beecham CorporationInventor: Robert A. Daines
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Patent number: 5631172Abstract: The present invention relates to the field of immunoassays for metal ions. The invention presents: metal ion-ligand coordination complexes ("MLC"), novel ligands, antibodies specific for MLC, immunoassays utilizing the foregoing, and methods for selecting said antibodies.Type: GrantFiled: May 5, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventor: David K. Johnson
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Patent number: 5625069Abstract: A process of preparing 2-cyano-3,5-dimethyl-4-methoxypyridine. The process includes the steps of: acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-carboxamido-3,5-dimethyl-4(1H)-pyridone; methylating 2-carboxamido-3,5-dimethyl-4(1H)-pyridone to obtain 2-carboxamido-3,5-dimethyl-4-methoxypyridine; and dehydrating said 2-carboxamido-3,5-dimethyl-4-methoxypyridone to obtain 2-cyano-3,5-dimethyl-4-methoxypyridine.Type: GrantFiled: July 22, 1996Date of Patent: April 29, 1997Assignee: Development Center for BiotechnologyInventors: Shan-Yen Chou, Tsai-Mien Huang, Shyh-Fong Chen, Hao Ku
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Patent number: 5620995Abstract: The invention relates to compounds of the formula I, to a process for their preparation and to their use as pharmaceuticals. ##STR1## In particular, the compounds are used as inhibitors of prolyl-4-hydroxylase and as inhibitors of collagen biosynthesis, as pharmaceuticals against fibrotic diseases of the liver, the lung and the skin.Type: GrantFiled: December 28, 1994Date of Patent: April 15, 1997Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
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Patent number: 5616713Abstract: A process of preparing 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine including the steps of acylating 2-methyl-1-penten-1-alkoxy-3-one to obtain 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone; ammonolyzing 2-alkoxycarbonyl-3,5-dimethyl-4-pyrone to obtain 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone; halogenating 2-alkoxycarbonyl-3,5-dimethyl-4(1H)-pyridone to obtain 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine; methoxylating 2-alkoxycarbonyl-4-halo-3,5-dimethylpyridine to obtain 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine; and reducing 2-methoxycarbonyl-3,5-dimethyl-4-methoxypyridine to obtain 2-hydroxymethyl-3,5-dimethyl-4-methoxypyridine.Type: GrantFiled: July 22, 1996Date of Patent: April 1, 1997Assignee: Development Center for BiotechnologyInventors: Shan-Yen Chou, Tsai-Mien Huang, Shyh-Fong Chen, Hao Ku
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Patent number: 5608062Abstract: A process is described for preparing trifluoromethyl ketones of the formula I ##STR1## where R has the given meanings, wherein an alcohol of the formula II ##STR2## is reacted with a compound of the formula IVYO.sub.n H (IV)where n has the given meaning.Type: GrantFiled: September 21, 1994Date of Patent: March 4, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Uwe D oller, Bernd Scharbert, Laurent Weisse
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Patent number: 5596006Abstract: Antihypertensive and antiatherosclerotic trisubstituted biphenyls of the formula ##STR1## in which R.sub.1 represents a carboxyl radical or represents a C.sub.1 -C.sub.8 -alkoxycarbonyl radical,R.sub.2 represents straight-chain or branched C.sub.1 -C.sub.8 -alkyl,R.sub.3 represents halogen, hydroxyl, cyano, C.sub.1 -C.sub.6 -alkoxy, straight-chain or branched C.sub.1 -C.sub.8 -alkyl, trifluoromethyl, trifluoromethoxy, carboxamido, carboxyl, C.sub.1 -C.sub.8 -alkoxycarbonyl or nitroandR.sub.4 represents a carboxyl radical or represents tetrazolyl,and salts thereof.Type: GrantFiled: January 3, 1995Date of Patent: January 21, 1997Assignee: Bayer AktiengesellschaftInventors: J urgen Dressel, Peter Fey, Rudolf Hanko, Walter Hubsch, Thomas Kramer, Ulrich E. M uller, Matthias M uller-Gliemann, Martin Beuck, Stanislav Kazda, Stefan Wohlfeil, Andreas Knorr, Johannes-Peter Stasch, Siegfried Zaiss
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Patent number: 5584888Abstract: Bleaching compositions, laundry and automatic dishwashing detergent compositions comprising particular neutral or anionically charged substituted bleach activators are provided. More specifically, the invention relates to compositions which provide enhanced cleaning/bleaching benefits through the selection of perhydrolysis-selective bleach activators having specific leaving groups with a conjugate acid pK.sub.a above 13 and with specific ratios of the rate of perhydrolysis to the rate of hydrolysis and the rate of perhydrolysis to the rate of diacylperoxide production. Included are preferred activator compounds and methods for washing fabrics, hard surfaces, and tableware using the activators.Type: GrantFiled: August 31, 1994Date of Patent: December 17, 1996Inventors: Gregory S. Miracle, Alan D. Willey, Kevin L. Kott, Michael E. Burns
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Patent number: 5578136Abstract: Automatic dishwashing detergent compositions, comprising particular quaternary-substituted bleach activators, are provided. More specifically, the invention relates to granular automatic dishwashing detergents which provide enhanced cleaning/bleaching benefits through the selection of quaternary-substituted bleach activators having specific features, such as caprolactam or valerolactam leaving groups and/or the ability to form particular cationic aliphatic peracid structures in solution. Preferred automatic dishwashing compositions comprise amylase enzymes. Included are preferred activator compounds and methods for washing tableware in domestic automatic dishwashing appliances using the activators.Type: GrantFiled: August 31, 1994Date of Patent: November 26, 1996Assignee: The Procter & Gamble CompanyInventors: Lucille F. Taylor, Mark R. Sivik, Alan D. Willey, James C. T. Burckett-St. Laurent, Frederick A. Hartman
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Patent number: 5574164Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: April 21, 1995Date of Patent: November 12, 1996Assignee: Hoescht Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5565413Abstract: Herbicidal compounds have the formula ##STR1## in which: R.sub.1 is hydrogen, halogen; 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 haloalkoxy; C.sub.2 -C.sub.8 alkoxyalkyl; nitro; cyano; thiocyano; or R.sub.7 S(O).sub.m - where m is 0, 1 or 2 and R.sub.7 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl;R.sub.2 and R.sub.3 are independently hydrogen; halogen; C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 alkoxy; C.sub.1 -C.sub.4 haloalkyl; C.sub.1 -C.sub.4 haloalkoxy; C.sub.2 -C.sub.8 alkoxyalkyl; nitro; R.sub.8 S(O).sub.2 O- or R.sub.8 S(O).sub.n - where n is 0, 1 or 2 and R.sub.8 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 cyanoalkyl, phenyl or benzyl; NR.sub.9 R.sub.10 where R.sub.9 and R.sub.10 are independently hydrogen or C.sub.1 -C.sub.4 alkyl; R.sub.11 CO- where R.sub.11 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, SO.sub.2 NR.sub.12 R.sub.13 where R.sub.12 and R.sub.13 are independently hydrogen, C.sub.1 -C.sub.Type: GrantFiled: December 6, 1994Date of Patent: October 15, 1996Assignee: Zeneca LimitedInventor: David B. Kanne
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Patent number: 5552418Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification,and a medicinal product containing said compound for treating a disorder of the melatoninergic system.Type: GrantFiled: May 23, 1995Date of Patent: September 3, 1996Assignee: Adir et CompagnieInventors: Patrick Depreux, Hamid Ait Mansour, Daniel Lesieur, Fran.cedilla.ois Lefoulon, Pierre Renard, G erard Adam, Philippe Delagrange
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Patent number: 5543515Abstract: A process for preparing tertiary amine oxides with a low nitrosamine content by reacting a tertiary amine with an aqueous solution of hydrogen peroxide, which comprises using as starting material tertiary amines whose total content of primary and secondary amines is not more than 0.05% by weight.Type: GrantFiled: August 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Ulrich Koehler, Hardo Siegel, Guenther Seybold