Indenyl Or Hydrindenyl Patents (Class 562/428)
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Publication number: 20150148347Abstract: A compound of formula I, wherein the groups R1, R2, R3, X, m, and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.Type: ApplicationFiled: November 25, 2014Publication date: May 28, 2015Inventors: Iain LINGARD, Dieter HAMPRECHT
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Patent number: 8871971Abstract: The invention provides compositions comprising sulindac, R-epimer sulindac, S-epimer sulindac, derivatives, metabolites, and structural analogs thereof which protect normal cells against damage caused by solar rays, oxidative damage, environmental factors, diseases and organisms.Type: GrantFiled: July 16, 2013Date of Patent: October 28, 2014Assignee: CHS Pharma, Inc.Inventors: Herbert Weissbach, Nathan Brot
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20140309264Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 25, 2014Publication date: October 16, 2014Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK -
ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130225605Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 22, 2013Publication date: August 29, 2013Applicant: SANOFIInventor: SANOFI -
Patent number: 8487128Abstract: The invention provides compositions comprising sulindac, R-epimer sulindac, S-epimer sulindac, derivatives, metabolites, and structural analogs thereof which protect normal cells against damage caused by solar rays, oxidative damage, environmental factors, diseases and organisms.Type: GrantFiled: May 5, 2008Date of Patent: July 16, 2013Assignee: CHS Pharma, Inc.Inventors: Herbert Weissbach, Nathan Brot
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Publication number: 20100292157Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.Type: ApplicationFiled: November 22, 2007Publication date: November 18, 2010Inventor: Antonio Cruz
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Publication number: 20090326258Abstract: The present invention relates to novel processes for the preparation of substituted tetralin and substituted indane derivatives. The present invention is further directed to novel processes for the preparation of intermediates in the preparation of the substituted tetralin and substituted indane derivatives.Type: ApplicationFiled: July 13, 2009Publication date: December 31, 2009Inventors: Fan Zhan-Plasket, Hua Zhong, Frank Villani
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Patent number: 7576238Abstract: The present invention relates to novel processes for the preparation of substituted tetralin and substituted indane derivatives. The present invention is further directed to novel processes for the preparation of intermediates in the preparation of the substituted tetralin and substituted indane derivatives.Type: GrantFiled: December 18, 2007Date of Patent: August 18, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Fan Zhang-Plasket, Hua Zhong, Frank Villani
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Publication number: 20090163547Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: ApplicationFiled: November 7, 2006Publication date: June 25, 2009Inventors: Maria De Las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria De Les Neus Mesquida-Estevez, Sara Lopez-Perez
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Patent number: 7351857Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.Type: GrantFiled: June 3, 2005Date of Patent: April 1, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Xiaoli Chen, Keith T. Demarest, Jung Lee, Jay M. Matthews, Philip Rybczynski
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Patent number: 6921774Abstract: The invention provides novel compounds of the formula I below: wherein the meaning of each substituent is defined in the application. The compounds are useful as inhibitors of the glycine transporter and useful in the treatment of diseases responsive to the inhibition of the glycine transporter. The invention provides a pharmaceutical composition comprising a compound of Formula I as defined above and the use of compounds as above for the manufacture of medicaments for treatment of diseases responsive to ligands of the glycine transporter.Type: GrantFiled: January 17, 2003Date of Patent: July 26, 2005Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Paul Garrick Smith, Christian Krog-Jensen, Klaus Peter Bøgesø
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Publication number: 20040167211Abstract: The invention features tetralin and indane compounds, compositions containing them, and methods of using them as PPAR alpha modulators to treat or inhibit the progression of, for example, diabetes.Type: ApplicationFiled: October 17, 2003Publication date: August 26, 2004Inventors: Xiiaoli Chen, Keith T. Demarest, Jung Lee, Jay M. Matthews, Philip Rybczynski
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Publication number: 20040068016Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.Type: ApplicationFiled: September 22, 2003Publication date: April 8, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Publication number: 20030225158Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.Type: ApplicationFiled: January 22, 2003Publication date: December 4, 2003Inventors: Bruce J. Auerbach, Larry D. Bratton, Gary F. Filzen, Andrew G. Geyer, Bharat K. Trivedi, Paul C. Unangst
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Patent number: 6576664Abstract: This invention relates to molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.Type: GrantFiled: August 14, 1998Date of Patent: June 10, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Wenqing Yao, Carl P. Decicco
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Patent number: 6479646Abstract: A metallocene compound having an indenyl ligand substituted by a heteroaromatic group, which is useful as an olefin polymerization catalyst. The metallocene compound has the following structure wherein M is a transition metal atom; each Ra is a monocyclic or polycyclic heteroaromatic group; each R1 is halogen, a hydrocarbon group of 1-20 carbons, a halogenated hydrocarbon group of 1-20 carbons, etc., or adjacent R1's may be joined together to form a ring of 6-8 carbons; p and q are each 1-7; n and l are each 0 or 1-6; and each X is halogen, a hydrocarbon group of 1-20 carbons, a halogenated hydrocarbon group of 1-20 carbons, etc.Type: GrantFiled: October 12, 2000Date of Patent: November 12, 2002Assignees: Chisso Corporation, Chisso Petrochemical CorporationInventors: Masato Nakano, Tsutomu Ushioda, Seiki Mitani, Hiroshi Yamazaki
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Patent number: 6472430Abstract: Antiatherosclerotic compounds are provided which have the following structure: wherein R is lower alkyl; R1 is hydroxy, amino, or lower alkoxy, R2 and R3 are each independently hydrogen, alkyl or aryl; Ar is phenyl, indanyl, benzhydryl, or phenyl substituted with one or more member selected from the group consisting of halogen, lower alkyl, perfluoroalkyl, lower alkoxy, perfluoroalkylalkoxy, dialkylamino, and aryloxy; or pharmaceutically acceptable salts thereof.Type: GrantFiled: September 28, 2001Date of Patent: October 29, 2002Inventors: Hassan M. Elokdah, Theodore S. Sulkowski
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Patent number: 6355836Abstract: An isomerization process of trans-5-fluoro-2-methyl-1-[p-(methylthio)benzyliden]inden-3-acetic acid for the treatment of sodium salt in methanol and in the presence of a base at 70±2° C. is described.Type: GrantFiled: October 3, 2000Date of Patent: March 12, 2002Assignee: Zambon Group S.p.A.Inventors: Giuseppe Barreca, Vincenzo Cannata
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Patent number: 6344585Abstract: A tetrahydrofluorene, which is represented by the following formula (I) wherein R1 to R6 each independently represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R1 and R2 are combined together to represent ═O, ═N or ═S, R7 and R8 each independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, a hydroxyl group or a carboxyl group, is subjected to a hydrogen transfer reaction in the presence of a hydrogen acceptor and a catalyst, whereby a fluorene and a hydride of the hydrogen acceptor are formed at the same time.Type: GrantFiled: January 25, 2001Date of Patent: February 5, 2002Assignee: Adchemco CorporationInventor: Hiroaki Mori
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Patent number: 6214876Abstract: Indene-1-acetamide compounds of the general formula (I) below; inhibit sPLA2 mediated release of fatty acids and are useful for treatment of conditions such as septic shock.Type: GrantFiled: July 21, 1994Date of Patent: April 10, 2001Assignees: Eli Lilly and Company, Shionogi & Company, Ltd.Inventors: Robert D. Dillard, Sanji Hagishita, Mitsuaki Ohtani
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Patent number: 6172259Abstract: The invention relates to a continuous process for the preparation of enantiomerically pure biarylketocarboxylic acids, S-phenylethylamine being employed as an auxiliary base in the resolution. Biarylketocarboxylic acids, in particular substituted biaryl-4-ketocarboxylic acids, are inhibitors of enzymes of the matrix metalloproteinases class. By inhibition of the abovementioned enzymes, it is possible, for example, to control osteoarthritis, rheumatoid arthritis and metastases.Type: GrantFiled: September 20, 1999Date of Patent: January 9, 2001Assignee: Bayer AktiengesellschaftInventor: Michael Preiss
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Patent number: 6172109Abstract: 13-thia prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic, pharmaceutical compositions comprising said prostaglandins.Type: GrantFiled: June 3, 1998Date of Patent: January 9, 2001Assignee: Alcon Laboratories, Inc.Inventors: Paul W. Zinke, Mark R. Hellberg
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Patent number: 6156750Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic 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 and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 13, 1999Date of Patent: December 5, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6063807Abstract: Cyclo-oxygenase inhibitor and amidine derivative salts, preparation methods therefor, pharmaceutical compositions containing said salts and the use thereof particularly as NO synthase and cyclo-oxygenase inhibitors, are disclosed.Type: GrantFiled: January 6, 1998Date of Patent: May 16, 2000Assignee: Societe de Conseils de Recherches d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Etienne Chabrier de Lassauniere, Colette Broquet
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Patent number: 6020379Abstract: In position 7 substituted indenyl-3-acetic acid derivatives and pharmaceutically acceptable salts and amides thereof have anti-neoplastic activity.Type: GrantFiled: February 19, 1999Date of Patent: February 1, 2000Assignee: Cell Pathways, Inc.Inventor: Gerhard Sperl
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Patent number: 5908851Abstract: Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.Type: GrantFiled: October 7, 1997Date of Patent: June 1, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Andrew Miller, Zoe Marie Spavold, Mark Whittaker
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Patent number: 5869740Abstract: Compounds of the formula: ##STR1## wherein R is CH.sub.2 X or CHX.sub.2 and X is chloro or bromo and R.sup.1 is chloro, bromo or nitro which are useful as intermediates for preparing herbicidal 2-(2'-substituted)-4'-(alkylsulfonyl)benzoyl-1,3-cyclohexanedione compounds.Type: GrantFiled: March 20, 1997Date of Patent: February 9, 1999Assignee: Zeneca LimitedInventors: Richard D. Gless, Jr., Nancy Kerlinger
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Patent number: 5837807Abstract: This invention is directed to tetrahydronaphthalene compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, bromine, cyano, formyl, hydroxy, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, aryloxy, lower aralkoxy or aryl; R.sup.2 is an amino acid residue or a chain of 2 to 20 amino acid residues wherein reactive moieties in the side chains of the amino acid residue(s) is/are protected or unprotected, and wherein the amino group of the N-terminal amino acid is a free or protected amino group; A.sup.1, A.sup.2, A.sup.3 and A.sup.4 each are .alpha.-amino acid residues wherein A.sup.1 and A.sup.2 are in the L configuration and A.sup.3 and A.sup.4 are in the D configuration when the .alpha.-C atom of said .alpha.-amino acid residue is asymmetric; X is oxygen or sulphur; Y is a residue of the formula ##STR2## n is 0 or 1; R.sup.3 is hydrogen or lower alkyl; R.sup.Type: GrantFiled: February 27, 1996Date of Patent: November 17, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Christine Abrecht, Alfred Grieder, Klaus Muller, Daniel Obrecht
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Patent number: 5750558Abstract: Described herein are compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein L is selected from the group consisting of ##STR2## R.sup.2 is selected from (a) ##STR3## R.sup.3 is selected from optionally substituted phenyl, and optionally substituted pyridyl; Y is selected from halogen, alkyl, haloalkyl, alkoxy, pyridylmethoxy, thiazolylmethoxy, benzothiazolylmethoxy, quinolylmethoxy, and optionally substituted quinolylmethoxy; W is selected from hydrogen, alkyl, hydroxyalkyl, and hydroxy; A is absent or is selected from optionally substituted alkylene optionally substituted cycloalkylene, optionally substituted cycloalkylene wherein one or two of the carbon atoms is replaced with one or two heteroatoms independently selected from O, S, and N, and ##STR4## and X is absent or is alkylene; Z is selected from (a) hydrogen, (b) COM wherein M is selected from (b-1) a pharmaceutically acceptable metabolically cleavable group, (b-2)--OR.sup.10,(b-3)--O(CH.sub.2).sub.w --CH(OR.sup.Type: GrantFiled: June 6, 1996Date of Patent: May 12, 1998Assignee: Abbott LaboratoriesInventors: Clint D. W. Brooks, Teodozyj Kolasa, Wendy Lee, Andrew O. Stewart
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5712377Abstract: What are described are new glucosides and their sugar-free decomposition products, as well as synthetically produced derivatives, which can be used as active components of pharmaceutical compositions. The novel glucosides have been isolated from aqueous extracts of vegetable pollen. These novel glucosides, sugar-free decomposition products and their derivatives have the effectiveness to modulate the immune system of warm blooded animals and they can be used as active components in pharmaceutical compositions for the treatment of tumors and virus-related diseases.Type: GrantFiled: June 28, 1996Date of Patent: January 27, 1998Assignee: Cerbios-Pharma SAInventors: Jean-Claude Jaton, Fabrizio Marazza, Ari Lewenstein, Francis M. Sirotnak, Bernhard Jaun
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Patent number: 5578629Abstract: The present invention comprises peptidomimetic compounds which comprise a suitably substituted aminoalkylbenzamide moiety. The instant compounds inhibit the farnesyl protein transferase enzyme and the farnesylation of certain proteins. Furthermore, the instant farnesyl protein transferase inhibitors differ from those previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: March 29, 1995Date of Patent: November 26, 1996Assignee: Merck & Co., Inc.Inventors: Terrence M. Ciccarone, Theresa M. Williams, Suzanne C. MacTough
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Patent number: 5470832Abstract: The compounds disclosed am analogs of the CAAX motif of proteins that can be modified by geranylgeranylation in vivo that selectively inhibit the geranylgeranylation of several proteins. The relatively poor activity of the compounds against the farnesyl protein transferase, which modifies several proteins important in cellular replication, allows the use of the compounds of the instant invention to treat diseases which which am regulated by the function of a geranylgeranylated protein, such as certain cancers and inflammatory diseases. Further contained in this invention are chemotherapeutic compositions containing these geranylgeranyl protein transfcrase type I inhibitors and methods for their production.Type: GrantFiled: January 31, 1994Date of Patent: November 28, 1995Assignee: Merck & Co., Inc.Inventors: Jackson B. Gibbs, Samuel L. Graham
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Patent number: 5459134Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein R.sup.4 represents:(i) when B represents a closed ring, a group of the general formula: ##STR2## wherein U represents an oxygen atom or a sulfur atom; or (ii) when B represents a divalent group, a group of the general formula: ##STR3## wherein R.sup.5, R.sup.6, R.sup.7, R.sup.8, n, m, p and q are as defined in the specification, and exclusing certain compounds as defined in the specification, depending on whether A represents a single bond or a group. The compounds are useful for the prevention and/or treatment of diseases induced by leukotrienes, 5.alpha.-reductase, phospholipase and aldose reductase in mammals, especially human beings.Type: GrantFiled: October 21, 1994Date of Patent: October 17, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tsumoru Miyamoto, Yoshinobu Arai
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Patent number: 5446058Abstract: A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein A represents a single bond or a group as defined in the specification;B represents(i) a substituted or unsubstituted carbocyclic ring of 4 to 8 members being unreplaced or optionally having one, two or three carbon atom(s) replaced by oxygen, nitrogen and/or sulfur atom(s); or(ii) a divalent group of formula: ##STR2## T represents oxygen or sulfur; R.sup.1 represents a group of general formula: ##STR3## or (iv) a straight or branched alkyl, alkenyl or alkynyl group of from 1 to 20 carbon atom(s);R.sup.2 represents hydrogen or a straight or branched alkyl group of from 1 to 6 carbon atom(s);R.sup.' represents hydrogen, a halogen atom, a hydroxy group, a nitro group or a group --COOR.sup.7 ;R.sup.Type: GrantFiled: November 29, 1991Date of Patent: August 29, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Masaaki Toda, Tumoru Miyamoto, Yoshinobu Arai
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Patent number: 5409956Abstract: The present invention relates to indan derivatives represented by the formula (1) or pharmaceutically acceptable salts thereof: ##STR1## [wherein R.sup.1 represents C1 to C12 alkyl, benzyl, styryl, naphthyl, optionally substituted phenyl or optionally substituted thienyl; R.sup.2 represents carboxyl, C1 to C4 alkoxycarbonyl, ##STR2## Y represents --(CH.sub.2).sub.p -- (wherein p represents an integer of 0 to 5), --CO--(CH.sub.2).sub.q .about., --CH(OH)--(CH.sub.2).sub.q .about., (wherein q represents an integer of 1 to 4, and the symbol .about. represents a linkage to R.sup.2), oxymethylene or ethylene; and n represents an integer of 1 to 4]. The compounds according to the present invention potently antagonize the action of thromboxane A.sub.2, and therefore useful for the treatment and prevention of diseases caused by thromboxane A.sub.2 such as angiosis, vasospasm, asthma and the like.Type: GrantFiled: August 30, 1993Date of Patent: April 25, 1995Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Kiyoshi Yoshida, Yoshiaki Yamaji, Tadashi Kurimoto, Ryuichi Sato, Motoki Torizuka
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Patent number: 5399748Abstract: Arylsulfonamide derivatives of .alpha.-amino dicarboxylic acids such as aspartic acid and glutamic acid posses anti-cholecystokinin activity. They are useful in the treatment of cholecystokinin-related disorders such as anorexia nervosa, pancreatic inflammation, biliary tract disease, Zollinger-Ellison syndrome and various psychiatric disorders, as well as in the potentiation of opiate analgesia, and in the treatment of certain cancers.Type: GrantFiled: January 12, 1993Date of Patent: March 21, 1995Assignee: James Black Foundation LimitedInventors: Howard B. Broughton, Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley
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Patent number: 5385917Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.Type: GrantFiled: July 16, 1993Date of Patent: January 31, 1995Assignee: Mitsubishi Kasei CorporationInventors: Hiroaki Ueno, Masahiko Morioka, Fumiko Hatanaka
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Patent number: 5281626Abstract: A novel benzenesulfonamide derivative represented by the formula: ##STR1## has an inhibitory activity against phospholipase A.sub.2, so that it is effective in the treatment of diseases for which such an activity is efficacious.Type: GrantFiled: September 26, 1991Date of Patent: January 25, 1994Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Takashi Hasegawa, Tadanobu Takamura, Kenichi Nomoto, Yoshiharu Daiku, Toshihiko Naito, Sachiyuki Hamano
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Patent number: 5252601Abstract: The present invention relates to novel 2-mercaptomethylene-tetrahydronaphthalene derivatives which are useful as enkephalinase inhibitors.Type: GrantFiled: April 3, 1992Date of Patent: October 12, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Douglas W. Beight
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5081282Abstract: Bicyclo prostaglandin analogues have been prepared.Type: GrantFiled: January 13, 1988Date of Patent: January 14, 1992Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 5030653Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: October 23, 1990Date of Patent: July 9, 1991Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5030652Abstract: Indan derivatives of the formula: ##STR1## wherein R.sup.1 is substituted or unsubstituted phenyl, naphthyl or sulfur-containing heterocyclic group, and R.sup.2 is hydroxy-methyl or a group of the formula: ##STR2## wherein R.sup.3 is hydrogen atom or lower alkyl and R.sup.4 is cycloalkyl, lower alkoxycarbonyl-phenyl, carboxy-phenyl, nitrogen-containing heterocyclic group, lower alkyl, or lower alkyl having a substituent selected from lower alkoxycarbonyl, carboxy, lower alkoxycarbonyl-phenyl, carboxy-phenyl, lower alkoxycarbonyl-cycloalkyl and carboxy-cycloalkyl, or a pharmaceutically acceptable salt thereof, which are useful as a platelet aggregation-inhibiting agent and as an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis or embolism, coronary and cerebral vascular smooth muscle vellication, asthma, and the like, processes for the preparation thereof, and pharmaceutical composition containing said compound as an active ingredient.Type: GrantFiled: November 15, 1988Date of Patent: July 9, 1991Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Harumichi Kohno, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 4983628Abstract: Compounds having the formula: ##STR1## are antagonists of leukotrienes of C.sub.4, D.sub.4 and E.sub.4, the slow reaction substance of anaphylaxis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: January 3, 1989Date of Patent: January 8, 1991Assignee: Merck Frosst Canada, Inc.Inventors: Richard Frenette, Joshua Rokach, Masatoshi Kakushima, Robert N. Young
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Patent number: 4980372Abstract: A benzoylaminophenoxybutanoic acid derivative of general formula: ##STR1## [wherein R.sup.1 represents hydrogen atom or alkyl group of from 1 to 4 carbon atoms(s),A represents oxygen atom, sulfur atom or sulfinyl (SO) group, two R.sup.1 s represents methyl groups or chlorine atoms at the same time or cyclopentane, cyclohexane or benzene ring together with the carbon atoms of benzene ring each attaching,R.sup.2 represents a group of general formula: ##STR2## {wherein B represents oxygen atom, sulfur atom or a group of general formula:NR.sup.11 (wherein R.sup.11 represents hydrogen atom or alkyl group of from 1 to 4 carbon atom(s)),R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 represent, independently, hydrogen atom, alkyl group of from 1 to 4 carbon atom(s) halogen atom, trifluoromethyl group or cyclobutylmethyl group,m represents 0 or 1,n represents an integer of from 1 to 5, andR.sup.9 and R.sup.Type: GrantFiled: May 6, 1988Date of Patent: December 25, 1990Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Nakai, Hiroshi Terashima, Yoshinobu Arai
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Patent number: 4975460Abstract: Novel indanoxyacetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group, a substituted or unsubstituted phenyl group, naphtyl group or a sulfur-containing heterocyclic group, R.sup.2 is hydroxy group or a protected hydroxy group, p is an integer of 2 or 3, and q is an integer of 0 or 1, and a salt thereof are disclosed.Said derivative (I) and a salt thereof are useful as a platelet aggregation-inhibiting agent and an agent for the treatment, amelioration and/or prophylaxis of a variety of thrombosis, embolism, coronary and cerebral vascular smooth muscl vellication, asthma, and the like.Type: GrantFiled: February 17, 1989Date of Patent: December 4, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Harumichi Kohno, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 4963587Abstract: There are disclosed are glycine derivative of the formula: ##STR1## (wherein R.sup.1 represents a substituted or unsubstituted phenyl group, R.sup.2 represents a carboxyl group which may be protected, Q represents a lower alkylene group and m represents 0 or 1) or a pharmacologically acceptable salt thereof and a process for preparing the same.Type: GrantFiled: December 5, 1989Date of Patent: October 16, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Takeo Iwakuma, Yasuo Sekine, Yasuhiko Sasaki, Katsuo Ikezawa, Akio Odawara
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Patent number: 4929754Abstract: The invention relates to new benzenesulphonamidoindanyl compounds useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.Type: GrantFiled: February 1, 1989Date of Patent: May 29, 1990Assignee: Dr. Karl Thomae GmbHInventors: Josef Nickl, Armin Heckel, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4868210Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.Type: GrantFiled: March 30, 1988Date of Patent: September 19, 1989Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi