Aldehyde Or Ketone Patents (Class 562/459)
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Patent number: 6759548Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: July 18, 2002Date of Patent: July 6, 2004Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 6706918Abstract: The present invention relates to 3-cyano-2,4,5-trifluorobenzoyl fluoride and to intermediates for its preparation and to the process for the preparation of 3-cyano-2,4,5-trifluoro-benzoyl fluoride, which starts from 5-fluoro-1,3-xylene (VIII); which is bichlorinated in the ring in the presence of a catalyst under ionic conditions to give 2,4-dichloro-5-fluoro-1,3-dimethylbenzene (VII). The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene (VI).Type: GrantFiled: October 22, 2002Date of Patent: March 16, 2004Assignee: Bayer AktiengesellschaftInventors: Albrecht Marhold, Peter Wolfrum
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Patent number: 6703421Abstract: A method for prevention or treating myocarditis, dilated cardiomyopathy and heart failure comprising administering to a patient in need of such treatment a NF-&kgr;B inhibitor in a therapeutically effective amount, wherein said NF-&kgr;B inhibitor is a benzoquinone derivative represented by the following formula (I): wherein R1, R2 and R3 are each independently a hydrogen atom, an alkyl group having 1 to 5 carbons or an alkoxy group having 1 to 5 carbons; R4 is a hydrogen atom, a hydroxymethyl group, an alkyl group, or a carboxyl group which is optionally esterified or amidated; Z is and n is an integer from 0 to 6, or its hydroquinone form, or a pharmaceutically acceptable salt thereof, is provided.Type: GrantFiled: May 17, 2001Date of Patent: March 9, 2004Assignee: Daiichi Suntory Pharma Co., Ltd.Inventors: Yoichi Nunokawa, Akira Matsumori
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Patent number: 6693199Abstract: A method of making HIV protease inhibitors of general formula (1): These HIV compounds inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and optically other antiviral agents as active ingredients, are suitable for treating patients or hosts infected with the HIV virus, which is known to cause AIDS.Type: GrantFiled: November 21, 2002Date of Patent: February 17, 2004Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Publication number: 20030232989Abstract: A new process for the preparation of specific aromatic aldehydes by ozonolysis of aromatic alkenes is provided. This new process can be advantageously integrated into a synthesis of specific chiral diols using aromatic aldehydes of this type.Type: ApplicationFiled: April 14, 2003Publication date: December 18, 2003Inventors: Stefan Antons, Joachim Rehse, Herbert Diehl, Christian Laue
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Publication number: 20030220517Abstract: A novel process affords &ohgr;-ketocarboxylic acid derivatives of the formula (I) 1Type: ApplicationFiled: March 14, 2003Publication date: November 27, 2003Inventor: Albrecht Marhold
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Patent number: 6649657Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: September 26, 2002Date of Patent: November 18, 2003Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6602907Abstract: Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (0F-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2).Type: GrantFiled: June 7, 2002Date of Patent: August 5, 2003Assignee: University of Central FloridaInventors: Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Pimenova Elena Valentinovna, Elena A. Goun
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Publication number: 20030144541Abstract: The invention concerns a method for preparing &agr;-halogenated ketones from secondary &agr;-halogenated alcohols. More particularly, the invention concerns the preparation of &agr;-trihalogenated ketones from secondary &agr;-trihalogenated alcohols. The method for preparing said &agr;-halogenated ketone is characterized in that it consists in oxidizing in liquid phase, a secondary &agr;-halogenated alcohol, using molecular oxygen or a gas containing same, in the presence of a catalyst based on a metal M1 selected among metals of group 1b and 8 of the periodic system of elements and optionally an activating element.Type: ApplicationFiled: November 4, 2002Publication date: July 31, 2003Inventor: Roland Jacquot
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Patent number: 6590119Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.Type: GrantFiled: November 7, 2001Date of Patent: July 8, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael P. Ferro, Kathleen A. McCoy
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Patent number: 6548546Abstract: The present invention relates to HIV integrase inhibitors of the formula wherein R1 and Z are as defined in the specification.Type: GrantFiled: February 28, 2002Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Timothy D. Johnson, Oak K. Kim, Yunhui Zhang
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Publication number: 20030045725Abstract: A method for the production of substituted aromatic aldehydes or ketones and optionally substituted heteroaromatic aldehydes or ketones of formula (I) by reacting a compound of formula (II) in a suitable solvent in the presence of a carbonyl compound of formula (III), optionally in the presence of oxygen at a normal pressure or high temperature and at temperatures of 5-200° C.Type: ApplicationFiled: September 20, 2002Publication date: March 6, 2003Inventors: Wolfram Hendel, Ferdinand Heu, Peter Poechlauer, Berthold Winkler
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Patent number: 6525215Abstract: Compounds useful as intermediates in the preparation of HIV protease inhibitors.Type: GrantFiled: June 21, 2001Date of Patent: February 25, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Bruce A. Dressman, James E. Fritz, Marlys Hammond, William J. Hornback, Stephen W. Kaldor, Vincent J. Kalish, John E. Munroe, Siegfried Heinz Reich, John H. Tatlock, Timothy A. Shepherd, Michael J. Rodriguez
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Publication number: 20020188121Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives.Type: ApplicationFiled: July 18, 2002Publication date: December 12, 2002Inventors: Andrew Michael Derrick, Nicholas Murray Thomson
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Patent number: 6469056Abstract: Pharmaceutically active compounds are prepared as described and used to produce pharmaceutical preparations for treating diseases.Type: GrantFiled: April 10, 2000Date of Patent: October 22, 2002Assignee: Abbott LaboratoriesInventors: Michael Puhl, Johann-Christian Zechel, Klaus Ditrich, Heinz Hillen, Tanja Kohl, Melanie Erhardt, Stefan Hergenröder, Claus Otto Markert
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Publication number: 20020123527Abstract: The present invention relates to the inhibition of HIV integrase, and to the treatment of AIDS or ARC by administering compounds of the following formula, or a tautomer of said compound, or a pharmaceutically acceptable salt, solvate or prodrug of said compound or of a tautomer thereof.Type: ApplicationFiled: February 28, 2002Publication date: September 5, 2002Inventors: Michael A. Walker, Timothy D. Johnson, Oak K. Kim, Yunhui Zhang
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Patent number: 6441218Abstract: Adipic acid diester is caused to react with alkoxide M(OR)n, wherein R is an alkyl group and M is an alkali metal or alkaline earth metal, the reaction product is successively subjected either to coupling with halomethylstyrene followed by carbonylation, or to coupling with 2-(halomethylphenyl)propionic acid or its ester followed by decarboxylation and hydrolysis. With this process, it is possible to produce more efficiently a specific 2-substituted propionic acid, loxoprofen.Type: GrantFiled: January 23, 2001Date of Patent: August 27, 2002Assignee: Nippon Petrochemicals Company, LimitedInventors: Saisuke Watanabe, Kazuharu Suyama
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Patent number: 6413936Abstract: The invention relates to novel mimetics of the tetrasaccharides sialyl-Lewis-X and sialyl-Lewis-A having an improved action as inhibitors of cell adhesion, to a process for the preparation of these compounds and to their use as pharmacological active compounds and diagnostic agents.Type: GrantFiled: October 30, 1996Date of Patent: July 2, 2002Assignee: Glycorex ABInventors: Wolfgang Schmidt, Ulrich Sprengard, Gerhard Kretzschmar, Robert Klein, Horst Kunz
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Patent number: 6380257Abstract: The present invention relates to new aromatic di-keto derivatives and to their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents. The derivatives are glucose-6-phosphate translocase inhibitors and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of the derivatives, to the use of the derivatives and their pharmaceutically acceptable salts, esters, ethers and other chemical equivalents as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising the derivatives, pharmaceutically acceptable salts, esters, ethers or other chemical equivalents thereof.Type: GrantFiled: October 24, 2000Date of Patent: April 30, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: László Vértesy, Michael Kurz, Erich Paulus
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Patent number: 6380249Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: June 1, 1999Date of Patent: April 30, 2002Assignees: Merck & Co., Inc., Tularik Inc.Inventors: Steven D. Young, Melissa Egbertson, Linda S. Payne, John S. Wai, Thorsten E. Fisher, James P. Guare, Jr., Mark W. Embrey, Lekhanh Tran, Linghang Zhuang, Joseph P. Vacca, H. Marie Langford, Jeffrey Melamed, Juan C. Jaen, David L. Clark, Julio C. Medina
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Publication number: 20020037923Abstract: The invention provides a resorcinol derivative and a method of using the resorcinol derivative to attenuate the growth of a neoplasm.Type: ApplicationFiled: August 13, 2001Publication date: March 28, 2002Inventor: Craig R. Travis
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Patent number: 6346546Abstract: Biaromatic compounds connected by a propynylene or ailenylene bond, corresponding to the formula (I).Type: GrantFiled: May 25, 2000Date of Patent: February 12, 2002Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Simon Trouille
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Patent number: 6329547Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.Type: GrantFiled: November 22, 2000Date of Patent: December 11, 2001Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Eiichi Shirasawa, Koji Konomi, Masaki Ichikawa, Hiroshi Suhara
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Publication number: 20010041742Abstract: Adipic acid diester is caused to react with alkoxide M(OR)n, wherein R is an alkyl group and M is an alkali metal or alkaline earth metal, the reaction product is successively subjected either to coupling with halomethylstyrene followed by carbonylation, or to coupling with 2-(halomethylphenyl)propionic acid or its ester followed by decarboxylation and hydrolysis. With this process, it is possible to produce more efficiently a specific 2-substituted propionic acid, loxoprofen.Type: ApplicationFiled: January 23, 2001Publication date: November 15, 2001Inventors: Saisuke Watanabe, Kazuharu Suyama
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Patent number: 6307089Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells.Type: GrantFiled: December 14, 2000Date of Patent: October 23, 2001Assignee: Warner-Lambert CompanyInventors: Claude Forsey Purchase, Jr., Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Publication number: 20010025084Abstract: A substrate for solid phase synthesis comprising a solid phase-linker combination of the formula I is disclosed. Also disclosed are processes for preparing the substrate and chemical intermediates useful therein. Among the novel intermediates are compounds of the formula II wherein R1 is —NO2 or —CHO; R2 is —OCH3, —CHO or —H; R3 is chosen from the group consisting of hydroxyl, the residue of a solid support having a plurality of amino groups, and the residue of an ester, and n=1 or 3-12.Type: ApplicationFiled: January 22, 2001Publication date: September 27, 2001Inventors: Vinh D. Tran, Vu Van Ma, Ruiyan Liu
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Patent number: 6265607Abstract: The invention relates to a process for the preparation of 4-(4′-chlorobiphenyl-4-yl)-4-keto-2-methylenebutyric acid of the formula (I) by Friedel-Crafts acylation of 4-chlorbiphenly with itaconic anhydride, which comprises carrying out the Friedel-Crafts acylation in aromatic solvents at a temperature from −20 to +80° C.Type: GrantFiled: August 3, 1999Date of Patent: July 24, 2001Assignee: Clariant GmbHInventors: Andreas Meudt, Wilfried Pressler, Antje Noerenberg, Steffen Haber, Michael Erbes, Robert Cosmo
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Patent number: 6251833Abstract: The present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.Type: GrantFiled: August 31, 1999Date of Patent: June 26, 2001Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
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Patent number: 6214877Abstract: This invention provides compounds of Formula I having the structure wherein: B, C, D, and R1 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: April 10, 2001Inventors: John A. Butera, Craig E. Caufield, Russell F. Graceffa, Alexander Greenfield, Eric G. Gundersen, Lisa Marie Havran, Alan H. Katz, Joseph R. Lennox, Scott C. Mayer, Robert E. McDevitt
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Patent number: 6180815Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: April 10, 2000Date of Patent: January 30, 2001Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6175034Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: April 10, 2000Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6166082Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula(T).sub.x A--B--D--E--Gwherein A and B are aryl or heteroaryl rings; each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR1## the group E represents a three carbon chain bearing one to three substituent groups which are independent or are involved in ring formation, possible structures being shown in the text and claims; and the group G represents --M, ##STR2## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; andR.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids, and include pharmaceutically acceptable salts thereof.Type: GrantFiled: April 9, 1998Date of Patent: December 26, 2000Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Heinz Herbert Benz, David Ross Brittelli, William Harrison Bullock, Kerry Jeanne Combs, Brian Richard Dixon, Stephan Schneider, Jill Elizabeth Wood, Michael Christopher VanZandt, Donald John Wolanin, Scott M. Wilhelm
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Patent number: 6143787Abstract: The present invention relates to a pharmaceutical composition comprising, as active principle, a compound of formula: ##STR1## in which the groups A and B are chosen, independently of each other, from: a mono-, bi- or tricyclic aryl group having from 6 to 14 carbon atoms;a heteroaromatic group chosen from pyridyl, pyrimidyl, pyrrolyl, furyl and thienyl groups;an alkyl group having from 1 to 14 carbon atoms;a cycloalkyl group having from 5 to 8 carbon atoms;a saturated heterocyclic group chosen from tetrahydrofuryl, tetrahydropyranyl, piperidyl and pyrrolidinyl groups;to its solvate or to a salt of this acid with a pharmaceutically acceptable base.Figures: none.Type: GrantFiled: February 2, 1999Date of Patent: November 7, 2000Assignee: Merck Patent Gesellschaft MitInventors: Gerard Moinet, Liliane Doare, Micheline Kergoat, Philippe Maizeray, Didier Mesangeau
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Patent number: 6096762Abstract: The present invention relates to the design, synthesis, and the peptidyl-prolyl isomerase (PPIase or rotamase) inhibitory activity of novel .alpha.,.alpha.-difluoroacetamido compounds that are neurotrophic agents (i.e. compounds capable of stimulating growth or proliferation of nervous tissue) and that bind to immunophilins such as FKBP12 and inhibit their rotamase activity. This invention also relates to pharmaceutical compositions comprising these compounds.Type: GrantFiled: May 21, 1999Date of Patent: August 1, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Gene M. Dubowchik, Bireshwar Dasgupta, Dolatrai M. Vyas
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Patent number: 6051584Abstract: Novel compounds of the general formula (I) which have hemoregulatory activities and can be used to stimulate haematopolesis and for the treatment of viral, fungal and bacterial infectious diseases ##STR1##Type: GrantFiled: November 23, 1998Date of Patent: April 18, 2000Assignees: SmithKline Beecham Corporation, Nycomed Austria GmbHInventors: Pradip Kumar Bhatnagar, Michael Hartmann, Johann Hiebl, Peter Kremminger, Franz Rovenszky
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Patent number: 6048896Abstract: 4-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: May 4, 1998Date of Patent: April 11, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Antonio Giordani, Paolo Pevarello, Carmela Speciale, Mario Varasi
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Patent number: 6046220Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: January 26, 1998Date of Patent: April 4, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6001877Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: May 20, 1998Date of Patent: December 14, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5973190Abstract: The present invention provides a process for the preparation of pesticidal fluoroolefin compounds having the structural formula I ##STR1## The present invention also provides intermediate compounds which are utilized in the process of this invention.Type: GrantFiled: June 18, 1998Date of Patent: October 26, 1999Assignee: American Cyanamid CompanyInventors: Brian Lee Buckwalter, Timothy Claude Barden
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Patent number: 5965741Abstract: The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.Type: GrantFiled: February 21, 1997Date of Patent: October 12, 1999Assignee: Zeneca LimitedInventors: Gloria Anne Breault, Howard Tucker, John Oldfield, Peter Warner
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Patent number: 5932577Abstract: The present invention provides pharmaceutical compositions and methods for treating certain conditions associated with matrix metalloproteases comprising administering an amount of a compound or composition of the invention which is effective to inhibit the activity of at least one matrix metalloprotease, resulting in achievement of the desired effect. The compounds of the present invention are either of the generalized formula: ##STR1## wherein y is 0, 2, or, 3, r is 0-6, Z is (CH.sub.2).sub.7 or (CH.sub.2).sub.e --C.sub.6 H.sub.4 --(CH.sub.2).sub.f, wherein e is 0-1 and f is 0-5, and R.sup.15 is --H, --Cl, --OMe or ##STR2## wherein n is 0-4, R.sup.17 is C.sub.2 H.sub.5, alkyl, benzyl, and R.sup.16 is ##STR3## wherein t is 0-2, x is 0-4, and R.sup.4 is one of the following: halide, alkyl of 1-6 carbons, OR, NR.sub.2, NO.sub.2 (R=H or alkyl of 1-6 carbons).Type: GrantFiled: May 15, 1997Date of Patent: August 3, 1999Assignee: Bayer CorporationInventors: Brian R. Dixon, Jinshan Chen, Michael C. VanZandt, David R. Brittelli
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Patent number: 5929117Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.Type: GrantFiled: August 11, 1997Date of Patent: July 27, 1999Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire
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Patent number: 5910596Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5- ?1-(C.sub.1-5 alkyl) -4-halo-5-(C.sub.1-3 haloalkyl) -1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyl-diketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.Type: GrantFiled: October 3, 1997Date of Patent: June 8, 1999Assignee: Monsanto CompanyInventor: Michael K. Mao
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Patent number: 5886043Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the group R6 represents variety of possible substituent groups on the carbon chain between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12, and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 30, 1997Date of Patent: March 23, 1999Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, William Harrison Bullock
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Patent number: 5883263Abstract: Processes for preparing substituted 3-aryl-5-haloalkyl-pyrazoles and, specifically, for preparing C.sub.1-5 alkyl esters of 5-?1-(C.sub.1-5 alkyl)-4-halo-5-(C.sub.1-3 haloalkyl)-1H-pyrazole-3-yl!-2,4-dihalo-benzoic acids such as isopropyl 5-?4-bromo-1-methyl-5-(trifluoromethyl)-1H-pyrazole-3-yl!-2-chloro-4-fluor obenzoate, are presented. The described processes include novel approaches for forming phenyldiketones, forming and alkylating pyrazoles, brominating heterocyclic compounds, oxidizing alkyl-substituted benzene compounds, and esterifying carboxylic acids. These processes may be combined to prepare 3-aryl-5-haloalkyl pyrazoles, or alternatively, used in subcombinations or individually to prepare intermediates or other useful compounds.Type: GrantFiled: October 3, 1997Date of Patent: March 16, 1999Assignee: Monsanto CompanyInventors: Bruce C. Hamper, Michael K. Mao, Wendell Gary Phillips
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Patent number: 5863915Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein R.sup.1 represents C.sub.6 -C.sub.12 alkyl; C.sub.5 -C.sub.12 alkoxy; C.sub.5 -C.sub.12 alkylthio; a polyether of formula R.sup.2 O(C.sub.2 H.sub.4 O).sub.a -- in which a is 1 or 2 and R.sup.2 is C.sub.1 -C.sub.5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R.sup.3 (CH.sub.2).sub.b --C.tbd.C--; in which b is 1-10 and R.sup.3 is H--, HO--, or R.sup.4 O-- in which R.sup.4 is C.sub.1 -C.sub.3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R.sup.1 may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R.sup.Type: GrantFiled: May 15, 1997Date of Patent: January 26, 1999Assignee: Bayer CorporationInventors: Harold C. E. Kluender, Brian R. Dixon, David R. Brittelli
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Patent number: 5859295Abstract: This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.Type: GrantFiled: June 18, 1996Date of Patent: January 12, 1999Assignee: University of Kentucky Research FoundationInventors: Peter A. Crooks, Gerald A. Rosenthal
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Patent number: 5856560Abstract: A process and intermediates for preparing .alpha.Type: GrantFiled: December 10, 1996Date of Patent: January 5, 1999Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Heinz Isak, Horst Wingert, Hubert Sauter, Michael Keil, Markus Nett, Remy Benoit, Ruth Muller
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Patent number: 5776977Abstract: Compounds of formula I, ##STR1## wherein the substituents R.sub.1 -R.sub.4 and a have the given meanings and show an activity against inflammatory conditions.Type: GrantFiled: August 5, 1996Date of Patent: July 7, 1998Assignee: Hoechst AktiengesellschaftInventors: Ramachandra Ganapati Naik, Vilas Narayan Mumbaikar, Rangarajan Vasumathy, Aftab Dawoodbhai Lakdawala, Mandakini Vithalrao Shirole, Bansi Lal, Jurgen Blumbach, Klaus Ulrich Weithmann, Robert Ryder Bartlett
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Patent number: 5739376Abstract: Fullerene derivatives, methods of preparing the same and methods of using the same, wherein the fullerene derivatives are of the formula I ##STR1##Type: GrantFiled: October 20, 1995Date of Patent: April 14, 1998Assignee: Hoechst AktiengesellschaftInventor: Carsten Bingel