Substituent Q Is Monocyclic Patents (Class 564/182)
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Patent number: 6420605Abstract: The invention relates to benzamidoxim derivatives of formula (I) wherein the substituents have the following meanings: R1 represents difluoromethyl or trifluoromethyl, R2 represents hydrogen or fluorine, R3 represents C1-C4 alkyl optionally substituted with cyano, C1-C4 halogenalkyl, C1-C4 alkoxy-C1-C4 alkyl, C3-C6 alkenyl, C3-C6 halogenalkenyl, C3-C6 alkinyl, C3-C8 cycloalkyl-C1-C4 alkyl, R4 represents phenyl-C1-C6 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the phenyl ring, or thienyl-C1-C4 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 halogenalkoxy on the thienyl ring, or pyrazol-C1-C4 alkyl, which can carry one or more substituents selected from the group composed of halogen, C1-C4 alkyl, C1-C4 halogenalkyl, C1-C4 alkoxy or C1-C4 halogenalkoxy on the pyrazol ring.Type: GrantFiled: March 14, 2000Date of Patent: July 16, 2002Assignee: BASF AktiengesellschaftInventors: Karl Eicken, Joachim Rheinheimer, Frank Wetterich, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6420428Abstract: The present invention provides new methods for the treatment of viral hepatitis C involving the administration of vitamin E and other compounds with antioxidant properties. Treatment with high doses of vitamin E is effective in treating chronic hepatitis C in patients refractory to interferon. In addition, new methods are described for the treatment of hepatic fibrosis and hepatic conditions manifesting hepatic fibrosis involving the administration of butylated hydroxytoluene and a metabolite of pentoxifylline, 1-[3-carboxypropyl]-3,7-dimethylxanthine. Furthermore, new methods are described for the treatment and prevention of hepatic disorders involving the use of 2,6-di-tert-butylphenol derivatives.Type: GrantFiled: November 28, 2000Date of Patent: July 16, 2002Assignee: The Regents of the University of CaliforniaInventors: Mario Chojkier, Martina Buck
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Patent number: 6417398Abstract: The invention concerns benzamidoxim derivatives of formula (I) in which the substituents have the following meanings: R1 represents hydrogen or fluorine; R2 represents C1-C6 phenyl-alkyl, bearing on the cyclic phenyl compound one or several substituents selected in the group comprising halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy halide, or C1-C4 thienyl-alkyl, optionally bearing one or several substituents selected in the group comprising halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy or C1-C4 alkoxy halide, or C1-C4 pyrazol-alkyl, optionally bearing one or several substituents selected in the group comprising halogen, C1-C4 alkyl, C1-C4 alkyl halide, C1-C4 alkoxy or C1-C4 alkoxy halide.Type: GrantFiled: March 14, 2000Date of Patent: July 9, 2002Assignee: BASF AktiengesellschaftInventors: Karl Eicken, Joachim Rheinheimer, Frank Wetterich, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6407120Abstract: The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.Type: GrantFiled: January 28, 2000Date of Patent: June 18, 2002Assignee: Pfizer Inc.Inventors: Philip A. Carpino, Marlys Hammond, Richard F. Hank
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Patent number: 6372779Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: December 28, 1998Date of Patent: April 16, 2002Assignee: Ortho Pharmaceutical CorporationInventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6369111Abstract: The invention relates to novel substituted oximes, to a process for their preparation and to their use as fungicides.Type: GrantFiled: May 30, 2001Date of Patent: April 9, 2002Assignee: Bayer AktiengesellschaftInventors: Dirk Backhaus, Herbert Gayer, Stefan Hillebrand, Peter Gerdes, Martin Vaupel, Astrid Mauler-Machnik
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Patent number: 6339157Abstract: Aldehydes are catalytically combined with amines to form carboxamides in one step using an oxidant and a metal-ligand complex or metal/ligand composition.Type: GrantFiled: July 28, 2000Date of Patent: January 15, 2002Assignee: Symyx Technologies, Inc.Inventors: Xiaohong Bei, Anil Guram
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Patent number: 6316669Abstract: Bis-amido polybiguanides and their use as antimicrobial agents in pharmaceutical compositions are disclosed. A method of synthesis of bis-amido polybiguanides is also disclosed. The bis-amido polybiguanides are useful in the preservation of pharmaceutical compositions, particularly ophthalmic and otic pharmaceutical compositions and compositions for treating contact lenses. The compounds are especially useful for disinfecting/cleaning contact lenses.Type: GrantFiled: September 19, 2000Date of Patent: November 13, 2001Assignee: Alcon Manufacturing, Ltd.Inventors: Joonsup Park, Nathaniel D. McQueen
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Patent number: 6310246Abstract: Herbicidal fluorovinyloxyacetamide compounds of formula (I) are useful for protecting crops from weeds: wherein: R1 is a phenyl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy and halogen; R2 is a C1-6 alkyl; or R1 and R2 together with the nitrogen atom to which they are bound form a 5-, 6- or 7-membered nitrogen heterocycle optionally having one or more ring oxygen atoms, double bonds and C1-6 alkyl substituents; R3 is a phenyl or thiophen-2-yl group optionally having one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, methylenedioxy and halogen; and R4is a perfluoro C1-6 alkyl group.Type: GrantFiled: August 14, 2000Date of Patent: October 30, 2001Assignee: Korea Research Institute of Chemical TechnologyInventors: Bum-Tae Kim, No-Kyun Park, Kyung-Sik Hong, Jae-Eup Park, Yong-Woong Kwon
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Patent number: 6291491Abstract: Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: October 12, 2000Date of Patent: September 18, 2001Assignee: Merck & Co., Inc.Inventors: Ann E. Weber, Emma R. Parmee, Robert Mathvink, Wallace T. Ashton, Elizabeth M. Naylor
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Patent number: 6288122Abstract: Novel inhibitors of potassium flux are disclosed. The inhibitors show surprising resistance to degradation in biological media and enhanced in vivo half-lives relative to non-fluorine substituted homologues. Methods for the use of these compounds include treating sickle cell disease, preventing erythrocyte dehydration and inhibiting potassium flux.Type: GrantFiled: August 31, 1999Date of Patent: September 11, 2001Assignee: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, Gregory Cooksey Rigdon, Jonathan Walter Stocker
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Patent number: 6255326Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: January 27, 1999Date of Patent: July 3, 2001Assignee: Aventis Pharma LimitedInventors: Michael John Ashton, David Charles Cook, Garry Fenton, Susan Jacqueline Hills, Ian Michael McFarlane, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Nigel Vicker
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Patent number: 6242609Abstract: A method for manufacturing a color coupler used in a silver halide photographic light-sensitive material using an ammonium trihalide. Said method for manufacturing the color coupler comprising the following step: a step for halogenating a coupling position of a four equivalent coupler using a halogenating agent, wherein said halogenating agent is said ammonium trihalide.Type: GrantFiled: April 7, 1999Date of Patent: June 5, 2001Assignee: Konica CorporationInventor: Fumio Ishii
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Patent number: 6211244Abstract: The present invention features compounds able to modulate one or more activities of an inorganic ion receptor and methods for treating diseases or disorders by modulating inorganic ion receptor activity. Preferably, the compound can mimic or block the effect of extracellular Ca2+ on a calcium receptor.Type: GrantFiled: October 23, 1995Date of Patent: April 3, 2001Assignee: NPS Pharmaceuticals, Inc.Inventors: Bradford C. Van Wagenen, Scott T. Moe, Manuel F. Balandrin, Eric G. DelMar, Edward F. Nemeth
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Patent number: 6172060Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO•) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: February 10, 1999Date of Patent: January 9, 2001Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
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Patent number: 6172262Abstract: Disclosed are amphiphilic compounds comprising Formula I: wherein R1, R2, and R3 are C2-C12 straight or branched alkyl; unsubstituted phenyl, biphenyl, C3-C8 cycloalkyl, or C3-C8 cycloalkenyl; or phenyl, biphenyl, C3-C8 cycloalkyl, or C3-C8 cycloalkenyl substituted with one, two, or three C1-C6 straight or branched alkyl groups; or R1 and R2 combined are C3-C8 cycloalkyl, C3-C8 cycloalkenyl; or C3-C8 cycloalkyl or C3-C8 cycloalkenyl substituted with one, two, or three C1-C6 straight or branched alkyl groups; one of R4 or R5 is selected from the group consisting of C2-C6-straight or branched alkyl-(dimethyl-N-oxide), alkyl-(dimethylamine), alkyl-(trimethylammonium), alkyl-glucosyl, alkyl-maltosyl, glucosyl, maltosyl, and polyethylene(glycosyl); the other of R4 or R5 is selected from the group consisting of H, C2-C6 straight or branched alkyl or alkenyl, C2-C6-straight or branched alkyl-(dimethyl-N-oxide); alkyl-(dimethylamine), alkyl-(trimethylammonium), alkyl-glucosyl, alkyl-maltosyl, glucosType: GrantFiled: January 27, 1999Date of Patent: January 9, 2001Assignee: Wisconsin Alumni Research FoundationInventors: D. Tyler McQuade, Samuel H. Gellman
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Patent number: 6150413Abstract: Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: May 26, 1998Date of Patent: November 21, 2000Assignee: Centre International de Recherches DermatologiquesInventors: Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 6114381Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a .beta.-phenyl-.alpha.-aminopropionic acid N phenyl amide compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.5 is independently selected from hydrido, fluoro, chloro, bromo, methyl and ethyl; wherein R.sup.3 is selected from hydroxy, methoxy, ethoxy, methoxycarbonyloxy, ethoxycarbonyloxy, (2-methylpropoxy)carbonyloxy and (2-propenyloxy) carbonyloxy; wherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrido; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, methyl and ethyl; wherein R.sup.Type: GrantFiled: October 13, 1998Date of Patent: September 5, 2000Assignee: G. D. Searle & Co.Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Michael Clare
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Patent number: 6083987Abstract: A phenylenediamine derivative or a salt thereof in accordance with the present invention is expressed by the following formula 1: ##STR1## wherein A represents a group expressed by --CO--, --CH.sub.2 CO--, --CS--, or --SO.sub.2 --; Y represents a carbon atom or nitrogen atom; R.sub.1 represents a lower alkyl group; R.sub.2 represents a hydrogen, lower alkyl, alkenyl, benzyl, or benzoyl group; and each of R.sub.3 and R.sub.4 represents an alkyl group having 1-10 carbon atoms. The phenylenediamine derivative above mentioned, as a radical scavenger, has antioxidant effect and lipid peroxidation inhibitory activity so as to be available for inhibiting brain infarction or brain edema.Type: GrantFiled: June 2, 1998Date of Patent: July 4, 2000Assignee: Shiseido Co., Ltd.Inventors: Chikao Nishino, Kazuyuki Miyazawa, Hideo Kanno
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Patent number: 6075055Abstract: A phenylalkane amide compound having the formula (1): ##STR1## wherein R.sup.1 -R.sup.4, X, n, Y, Z and Q are as defined herein. The compound is useful as an agricultural or horticultural fungicide.Type: GrantFiled: December 1, 1997Date of Patent: June 13, 2000Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Katsumi Masuda, Ikumi Urushibata, Tsuyoshi Asahara, Katsumi Furuse, Yoshiyuki Kojima, Hiroshi Abe
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Patent number: 6069247Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: October 5, 1998Date of Patent: May 30, 2000Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
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Patent number: 6028131Abstract: The invention relates to compounds of the formula I ##STR1## in which R is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl, --CH.sub.2 --A--R.sub.2 or a group of the formula II, ##STR2## R.sub.1 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl or a group of the formula (II),R.sub.2 is C.sub.4 -C.sub.18 alkyl, --(CH.sub.2).sub.m --COOR.sub.5 or a group of the formula III, ##STR3## R.sub.3 is hydrogen, C.sub.5 -C.sub.8 cycloalkyl or C.sub.1 -C.sub.12 alkyl,R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl or a group of the formula II or IV, ##STR4## A is S or SO, E is a direct bond, --CH.sub.2 --, --CH.sub.2 --O-- or --CH.sub.2 --NH--,G is --O-- or --NR.sub.3 --,Y is C.sub.1 -C.sub.18 alkyl, cyclohexyl, phenyl or alpha- or beta-naphthyl,R.sub.5 is C.sub.1 -C.sub.18 alkyl, andm is 1 or 2,with the provisos thateither at least one of the radicals R and R.sub.Type: GrantFiled: April 27, 1998Date of Patent: February 22, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Hans-Rudolf Meier, Gerrit Knobloch
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Patent number: 6025349Abstract: Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, a process for their preparation, their use as a medicament or diagnostic agent, and also a medicament containing them.Phenyl-substituted alkenylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## in which the substituents have the meanings stated in the description, and their pharmaceutically suitable salts, are described. They are obtained by reacting a compound II ##STR2## with guanidine, in which R(1) to R(5) and R(A), R(B), R(C) and R(D) have the stated meaning, and L is a leaving group which easily undergoes nucleophilic substitution. Compounds I are excellent cardiovascular therapeutic agents.Type: GrantFiled: July 20, 1998Date of Patent: February 15, 2000Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5998481Abstract: There are described benzoylguanidines of the formula I ##STR1## having the definitions of R(1) to R(4) indicated in the text, and their pharmaceutically tolerable salts. They are obtained by reaction of a compound II ##STR2## with guanidine. They are outstanding agents for the treatment of disorders of the cardiovascular system.Type: GrantFiled: February 24, 1998Date of Patent: December 7, 1999Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5998653Abstract: Compounds of the formula ##STR1## are useful as intermediates to new herbicidal 4-benzoylisoxazoles.Type: GrantFiled: May 19, 1997Date of Patent: December 7, 1999Assignee: Rhone Poulenc Agriculture LimitedInventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
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Patent number: 5985881Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: August 2, 1997Date of Patent: November 16, 1999Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schnorrenberg, Hans Briem, Birgit Jung, Georg Speck
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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: 5917038Abstract: The present invention relates to a process for preparing acrylamides; wherein, a propiolamide is reacted with an activated aromatic ring to yield a wide variety of acrylamides.Type: GrantFiled: April 11, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Lynne Ann Hay, David Mitchell
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Patent number: 5872296Abstract: A process for preparing enantiomerically pure cis-1-amino-2-hydroxyindane, which comprisesa) converting racemic trans-1-aminoindan-2-ol with acids or acid derivatives of the general formula RCOX by conventional methods into amides of type A ##STR1## b) adding seed crystals of one enantiomer to a super-saturated solution or melt of the racemic amide A,c) isolating the crystals which have separated out, and again supersaturating the remaining mother liquor or melt after dissolving racemic amide A, and adding seed crystals of the other enantiomer, leading to selective crystallization of the latter,d) converting the resulting enantiomerically pure trans amide by conventional methods into the enantiomerically pure cis-1-amino-2-hydroxyindane.Type: GrantFiled: October 28, 1997Date of Patent: February 16, 1999Assignee: BASF AktiengesellschaftInventors: Christoph Nubling, Wolfgang Ladner
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Patent number: 5837720Abstract: A compound of formula (I): ##STR1## and its pharmaceutically acceptable salt, wherein R is hydrogen or hydroxy; Ar is unsubstituted or substituted phenyl; X is unsubstituted or substituted phenyl or heterocyclic, mono-, di- or trihalomethyl, cyano, or the like; and X.sup.2 is phenyl, naphthyl, furyl, thienyl, pyridyl, thiazolyl, benzofuryl or benzothienyl, each of which may either be unsubstituted or substituted. These compounds have agonist activity toward opioid kappa receptors and are thus useful as analgesic, anti-inflammatory, diuretic and neuroprotective agents.Type: GrantFiled: April 17, 1997Date of Patent: November 17, 1998Assignee: Pfizer Inc.Inventor: Fumitaka Ito
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5824817Abstract: The invention relates to the use of the known compound 2,6-dichloro-3-fluoro-benzonitrile as active compound in selectively-herbicidal compositions, and to new preparation processes and new intermediates for the preparation of this compound.Type: GrantFiled: July 28, 1997Date of Patent: October 20, 1998Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Werner Bussmann, Josef Kasbauer, Markus Dollinger, Hans-Joachim Santel
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Patent number: 5804595Abstract: The invention provides certain amino acid conjugates of substituted 2-phenyl-N-?1-(phenyl)-2-(1-heterocycloalkyl- or heterocycloaryl-)ethyl!acetamides useful for selectively agonizing kappa opioid receptors in mammalian tissue.Type: GrantFiled: December 5, 1995Date of Patent: September 8, 1998Assignee: Regents of the University of MinnesotaInventors: Philip S. Portoghese, An-Chih Chang
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Patent number: 5801195Abstract: Novel aryl amides are inhibitors of tumor necrosis factor .alpha. and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is N-benzoyl-3-amino-3-(3',4'-dimethoxyphenyl)propanamide.Type: GrantFiled: December 30, 1994Date of Patent: September 1, 1998Assignee: Celgene CorporationInventors: George W. Muller, Mary Shire, David I. Stirling
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Patent number: 5792776Abstract: Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.Type: GrantFiled: June 27, 1994Date of Patent: August 11, 1998Assignee: Cytomed, Inc.,Inventors: Tesfaye Biftu, Ralph Scannell, Xiong Cai, Sajjat Hussoin
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Patent number: 5779941Abstract: Novel compounds, 1,2-N-acyl-N-methylene-ethylenediamines of formula (I) are useful as dispersants, rust inhibitors, curing promoters for epoxy resins, electroconductivity-imparting agents, mold lubricants, etc. ##STR1## where R is a hydrogen atom or a hydrocarbon group. An electroconductive paste with excellent electroconductivity and much improved long-term stability is obtained by mixing 100 parts by weight of a thermosetting resin with from 250 to 900 parts by weight of a metal filler and from 1 to 50 parts by weight of the 1,2-N-acyl-N-methylene-ethylenediamine; or by adding from 250 to 900 parts by weight of a metal filler coated with the 1,2-N-acyl-N-methylene-ethylenediamine to 100 parts by weight of a thermosetting resin.Type: GrantFiled: April 22, 1997Date of Patent: July 14, 1998Assignee: Tatsuta Electric Wire and Cable Co., Ltd.Inventors: Hiroaki Umeda, Tsunehiko Terada, Hisatoshi Murakami
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Patent number: 5750575Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: June 7, 1995Date of Patent: May 12, 1998Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
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Patent number: 5750574Abstract: A compound of the general formula (I) ##STR1## wherein R.sub.1 is straight chain alkyl, branched chain alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl or polyfluoroalkyl; R.sub.2 and R.sub.3 are, independently, hydrogen or an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.4 is F, perfluoroalkyl group of 1 to 10 carbon atoms or perfluoroalkoxy of 1 to 10 carbon atoms; or a pharmaceutically acceptable salt thereof relax smooth muscles.Type: GrantFiled: July 7, 1997Date of Patent: May 12, 1998Assignee: American Home Products CorporationInventor: Adam M. Gilbert
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Patent number: 5723444Abstract: The invention concerns the compounds of the formulas: ##STR1## and protected forms and salts thereof which serve as starting materials in an improved method of synthesizing thrombin and kininogenase inhibitors. The invention further concerns an improved method for synthesizing the inhibitors which utilizes the compounds.Type: GrantFiled: June 6, 1995Date of Patent: March 3, 1998Assignee: Astra ABInventors: Karl Thomas Antonsson, Ruth Elvy Bylund, Nils David Gustafsson, Nils Olov Ingemar Nilsson
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Patent number: 5712312Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.Type: GrantFiled: April 12, 1996Date of Patent: January 27, 1998Assignee: Adir et CompagnieInventors: Michel Langlois, Monique Mathe-Allainmat, Philippe Delagrange, Pierre Renard, Beatrice Guardiola
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Patent number: 5710331Abstract: Preparation of N-alkenyl carboxamides of the general formula I ##STR1## in which the radicals R.sup.1 to R.sup.4 independently stand for hydrogen or for aliphatic, cycloaliphatic, or aromatic radicals, which optionally carry inert substituents, wherein an amide of the general formula II ##STR2## in which the radical R.sup.1 has the above meaning, and a carbonyl compound of the general formula III ##STR3## in which the radicals R.sup.2 to R.sup.4 have the above meanings, are caused to react in the presence of a base, said reaction being eithera) carried out in the presence of a carboxylic acid derivative of the general formula IV ##STR4## in which the radical R.sup.5 stands for hydrogen or an alkyl or aryl group and X is a halogen, alkoxy, or carboxylalkyl radical, orb) continued in the presence of a carboxylic acid derivative of the formula IV, and the amide of the formula I is isolated.Type: GrantFiled: October 26, 1995Date of Patent: January 20, 1998Assignee: BASF AktiengesellschaftInventors: Marc Heider, Thomas Ruhl, Jochem Henkelmann
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Patent number: 5705167Abstract: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 26, 1995Date of Patent: January 6, 1998Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Philippe Nedoncelle
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Patent number: 5698735Abstract: Description here is a novel process for preparing phenyl acetic acid derivatives of the formula (I)Ar--CH.sub.2 --R.sup.1 (I)in which Ar and R.sup.1 are as defined in the description by reaction of sulfonyloxy-activated hydroxyacetic acid derivatives of the formula (II)R.sup.3 --SO.sub.2 --O--CH.sub.r --R.sup.1 (II)in which R.sup.3 is as defined in the description. with aromatics of the formula (III)Ar--H (III)has been found. The intermediates of the formula (II), some of which are novel, are obtained from hydroxyacetic acid derivatives by reaction with sulfonyl halides or sulfonic anhydrides. The phenylacetic acid derivatives are important starting materials for preparing pesticides.Type: GrantFiled: January 20, 1995Date of Patent: December 16, 1997Assignee: Bayer AktiengesellschaftInventor: Uwe Stelzer
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Patent number: 5696123Abstract: The invention relates to new compounds of general formula I ##STR1## and the pharmaceutically acceptable salts thereof, wherein A, B, Z, R.sup.1, R.sup.2, R.sup.3 and m are defined as in the specification, processes for preparing them and pharmaceutical compositions containing these compounds. The compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: Boehringer Ingelheim KGInventors: Horst Dollinger, Gerd Schorrenberg, Hans Briem, Birgit Jung, Georg Speck
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Patent number: 5693846Abstract: A process for preparation of 4-mercapto-1-naphthol compounds which comprises the steps of:(i) obtaining a 4-heterocyclylthio-1-naphthol compound by reacting a 1-naphthol compound with a heterocyclylsulfur chloride or by reacting a 4-iodo-1-naphthol compound with an alkali metal or ammonium salt of a mercaptoheterocyclic compound,(ii) hydrolyzing the resulting 4-heterocyclylthio-1-naphthol compound in the presence of a base to form a reaction product, and(iii) acidifying said reaction product.The resulting compounds are useful as intermediates in the synthesis of bleach accelerator releasing couplers for use in silver halide color photographic materials.Type: GrantFiled: August 1, 1996Date of Patent: December 2, 1997Assignee: Imation Corp.Inventors: Ivano Delprato, Massimo Bertoldi
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Patent number: 5688955Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided.The compounds of formulae I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ;R.sub.1, R.sub.2, R.sub.3, R.sub.4 ; andY, Z and n are as described in the specification.Type: GrantFiled: February 5, 1997Date of Patent: November 18, 1997Assignee: Adolor CorporationInventors: Lawrence I. Kruse, An-Chih Chang, Diane L. DeHaven-Hudkins, John J. Farrar, Forrest Gaul, Virendra Kumar, Michael Anthony Marella, Alan L. Maycock, Wei Yuan Zhang
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Patent number: 5675034Abstract: Process for preparing 3-(p-fluorophenyl)-2-methylpropionic acid and derivatives thereof of the formula (I), ##STR1## in which R is a hydroxy group, a linear or branched (C.sub.1 -C.sub.8)-alkoxy group, an aryloxygroup, an amino group or a (C.sub.1 -C.sub.8)-alkylamino group or a (C.sub.1 -C.sub.8)-dialkylamino group, bya) converting p-fluoroaniline into the p-fluorophenyldiazonium salt of the formula (II) ##STR2## in which X is the equivalent of an anion of an organic or inorganic acid having a pKa value of less than 7,b) reacting the diazonium salt of the formula (II) with a methacrylic acid derivative of the formula (III) ##STR3## in which R is as defined above in the presence of a palladium catalyst, if desired in the presence of a base and/or a solvent, to give the compounds of the formulae (IV) and (V) in which R is as defined above, ##STR4## and c) hydrogenating the resulting compounds of the formulae (IV) and (V) in the presence of a palladium catalyst with hydrogen.Type: GrantFiled: January 2, 1996Date of Patent: October 7, 1997Assignee: Hoechst AktiengesellschaftInventors: Matthias Beller, Hartmut Fischer, Heinz Strutz
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Patent number: 5633403Abstract: Substantive UV-absorbing cinnamido amine cationic quaternary salts are disclosed. Detergent and household cleaning product compositions and hair and skin personal care product compositions, as well as sunscreen and tanning lotion compositions, containing the compounds of the present invention are also described.Type: GrantFiled: June 6, 1995Date of Patent: May 27, 1997Assignee: Croda, Inc.Inventors: Kevin F. Gallagher, Abel G. Pereira
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Patent number: 5633404Abstract: A method of making ( R)- N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of ( R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.Type: GrantFiled: April 19, 1996Date of Patent: May 27, 1997Assignee: NPS Pharmaceuticals, Inc.Inventors: Bradford C. VanWagenen, Steven R. Duff, William A. Nelson
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Patent number: 5621133Abstract: Novel compounds having the formula ##STR1## and the pharmaceutically acceptable salts, esters and amides thereof, whereinA is --O--, --S-- or --CR.sup.2 R.sup.8 --;R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, X and Y are specifically defined; andup to one combination of (a) R.sup.2 and R.sup.5, (b) R.sup.5 and R.sup.6, (c) R.sup.5 and R.sup.7, (d) R.sup.6 and R.sup.7, and (e) R.sup.7 and Y, taken together with the atoms to which they are attached, may form a ring, the compounds being useful for treating dopamine-related neurological, psychological and cardiovascular disorders as well as in the treatment of cognitive impairment, attention deficit disorder, and substance abuse and other addictive behavior disorders.Also disclosed are intermediates and processes useful in the preparation of the above compounds.Type: GrantFiled: June 5, 1995Date of Patent: April 15, 1997Inventors: Michael P. DeNinno, Richard J. Perner