Five-membered Alicyclic Ring Patents (Class 514/684)
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Patent number: 9622497Abstract: A carotenoid oil suspension and preparation method thereof are provided. The method includes the following steps: a) mixing carotenoid with organic solvent, heating the mixture to dissolve the carotenoid sufficiently to obtain carotenoid solution; b) introducing the carotenoid solution obtained in step a) into a vegetable oil solution stirred in high speed by spraying, meanwhile recovering the organic solvent generated during spraying under vacuum condition, then, simultaneously completing recycling and spraying, thereafter, obtaining carotenoid oil suspension; wherein, the carotenoid oil suspension comprises a carotenoid crystal with an average particle size of less than 5 ?m. The method is applicable in industrial scale with continuous operation and increased efficiency without additional carotenoid crystal grinding processes, and decreases the degradation of carotenoid during the preparation process of carotenoid oil suspension.Type: GrantFiled: January 30, 2011Date of Patent: April 18, 2017Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical FactoryInventors: Xinde Xu, Bin Shao, Xuejun Lao
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Patent number: 8846747Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.Type: GrantFiled: November 17, 2010Date of Patent: September 30, 2014Assignees: University of Rochester, Southern Research InstituteInventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucille White, Krister Wennerberg
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Patent number: 8710272Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.Type: GrantFiled: June 18, 2012Date of Patent: April 29, 2014Assignee: Androscience CorporationInventors: Charles C. Y. Shih, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
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Publication number: 20130261121Abstract: The present invention includes compounds, pharmaceuticals and cosmetics having at least one (substituted phenyl)-propenal moiety. The compounds and compositions of the present invention are useful in the treatment or prevention of medical conditions including androgen associated conditions, androgen associated inflammation, a wound (the compounds assist with wound healing), acne, rheumatoid arthritis, psoriasis, rosacea, and alopecia; Kennedy's disease (spinal and bulbar muscular atrophy, or SBMA), polyglutamine-mediated motor neuron degeneration; cancers such as prostate cancer, bladder cancer, breast cancer, ovarian cancer, hepatocellular (liver) cancer, and pancreatic cancer; and other medical conditions described herein. Treatment of such medical conditions includes administering to an individual suffering from a medical condition describe herein, a therapeutically effective amount of any of the disclosed compounds, their derivatives, or pharmaceutical compositions thereof.Type: ApplicationFiled: June 18, 2012Publication date: October 3, 2013Inventors: Charles C.Y. SHIH, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
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Publication number: 20130096175Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.Type: ApplicationFiled: November 17, 2010Publication date: April 18, 2013Applicants: SOUTHERN RESEARCH INSTITUTE, UNIVERSITY OF ROCHESTERInventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucile White, Krister Wennerberg
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Patent number: 8415505Abstract: The invention relates to 2-methylene-5-substituted-methylenecyclopentanone derivatives of formula I, and the use thereof. The derivatives of formula I as active components are useful for preparing a medicine for the treatment and/or prevention of cancer diseases such as breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, uterus cancer, pancreatic cancer and ovary cancer. The active compounds of the invention may be used as an anticancer drug alone or used in combination with one or more other antitumor drugs. A combined therapy can be carried out by administrating each therapeutic component concurrently, subsequently or separately.Type: GrantFiled: February 10, 2009Date of Patent: April 9, 2013Assignee: Shenyang Pharmaceutical UniversityInventors: Linxiang Zhao, Jingli Wang, Zhenjun Bian, Rui Wang, Dan Liu, Yongkui Jing
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Publication number: 20120058172Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.Type: ApplicationFiled: November 11, 2011Publication date: March 8, 2012Applicant: Intermed Discovery GmbHInventors: Ernst Roemer, Torsten Grothe
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Publication number: 20120053208Abstract: Curcumin analogues and methods of making and using the same are disclosed.Type: ApplicationFiled: April 15, 2010Publication date: March 1, 2012Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Pui-Kai Li, Chenglong Li, Jiayuh Lin, James R. Fuchs
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Publication number: 20120040976Abstract: Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, ALS, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for evaluation in animal models of neurodegenerative diseases.Type: ApplicationFiled: December 11, 2009Publication date: February 16, 2012Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventors: John R. Cashman, Kenneth J. Abel
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Publication number: 20110294783Abstract: The present invention concerns boosting the activity of crop protection materials comprising inhibitors of fatty acid biosynthesis (for example phenyl-substituted cyclic ketoenols) through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: August 10, 2011Publication date: December 1, 2011Applicant: BAYER CROPSCIENCE AGInventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
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Patent number: 8030359Abstract: A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer, and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol.Type: GrantFiled: February 9, 2007Date of Patent: October 4, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Sarah Geers, Michael Lowinger, Craig A. McKelvey, Robert F. Meyer, Dina Zhang
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Publication number: 20110060054Abstract: The invention relates to 2-methylene-5-substituted-methylenecyclopentanone derivatives of formula I, and the use thereof. The derivatives of formula I as active components are useful for preparing a medicine for the treatment and/or prevention of cancer diseases such as breast cancer, lung cancer, colon cancer, rectal cancer, stomach cancer, prostate cancer, bladder cancer, uterus cancer, pancreatic cancer and ovary cancer. The active compounds of the invention may be used as an anticancer drug alone or used in combination with one or more other antitumor drugs. A combined therapy can be carried out by administrating each therapeutic component concurrently, subsequently or separately.Type: ApplicationFiled: February 10, 2009Publication date: March 10, 2011Applicant: SHENYANG PHARMACEUTICAL UNIVERSITYInventors: Linxiang Zhao, Jingli Wang, Zhenjun Bian, Rui Wang, Dan Liu, Yongkui Jing
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Publication number: 20110021613Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.Type: ApplicationFiled: December 11, 2007Publication date: January 27, 2011Applicant: INTERMED DISCOVERY GMBHInventors: Ernst Roemer, Torsten Grothe
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Patent number: 7855310Abstract: The invention relates to the field of aryl hydrocarbon receptor (Ah receptor; AhR) antagonists and their uses.Type: GrantFiled: April 30, 2007Date of Patent: December 21, 2010Assignee: SYMRISE GmbH & Co. KGInventors: Martina Herrmann, Oskar Koch, Gabriele Vielhaber, Jean Krutmann
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Publication number: 20090227563Abstract: The present invention concerns boosting the activity of crop protection materials comprising active ingredients from the class of the phenyl-substituted cyclic ketoenols through the addition of ammonium salts and/or phosphonium salts or through the addition of ammonium salts and/or phosphonium salts and penetrants, the corresponding materials, processes for preparing them, and their use in crop protection.Type: ApplicationFiled: December 11, 2006Publication date: September 10, 2009Applicant: Bayer CropScience AGInventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Udo Bickers, Hans Philipp Huff, Erwin Hacker, Rainer Süssmann
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Patent number: 7109380Abstract: Compounds and methods useful in the control, treatment, and prevention of fungal activity, of the following formula: where R1-3 are independently H, alkyl, methyl, acyl, halogen, phenyl, R4 is H, alkyl, methyl, acyl, alkoxy, halogen, phenyl provided that when R3 is methyl and R4 is H, R1 and R2 are not both H; and stereoisomers, analogs, and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 29, 2005Date of Patent: September 19, 2006Assignees: The University of Mississippi, The United States of America as represented by the Secretary of AgricultureInventors: Xing-Cong Li, Melissa R. Jacob, David Wedge
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Patent number: 7091241Abstract: A combination of Vitamin C and a quinone used as a supplemental treatment for a cancer patient. The combination may be administered before, during and after the patient undergoes a conventional cancer treatment protocol. The combination may be administered orally, intravenously, or intraperitoneally. Oral administration may be in the form of capsules containing a predetermined ratio of Vitamin C to Vitamin K3. The supplemental treatment is effective to inhibit metastases of cancer cells and inhibit tumor growth. The ratio of Vitamin C to Vitamin K3 is in the range of about 50 to 1 to about 250 to 1. A method for evaluating the effectiveness of the supplemental treatment includes monitoring the patient's serum DNase activity throughout the course of treatment.Type: GrantFiled: June 3, 2002Date of Patent: August 15, 2006Assignee: Summa Health SystemInventors: Jacques Gilloteaux, Henryk S. Taper, James M Jamison, Jack L. Summers
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Patent number: 7064148Abstract: Disclosed is a novel use of a prostaglandin compound as a chloride channel opener. According to the instant invention, chloride channels in a mammalian subject can be opened by a prostaglandin compound to facilitate chloride ion transportation.Type: GrantFiled: August 30, 2002Date of Patent: June 20, 2006Assignee: Sucampo AGInventors: Ryuji Ueno, John Cuppoletti
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Patent number: 6903238Abstract: This invention provides estrogen receptor modulators of formula I, having the structure R1, R2, and R3 are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 11, 2002Date of Patent: June 7, 2005Assignee: WyethInventors: Robert E. McDevitt, Folake O. Adebi, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
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Patent number: 6887904Abstract: Substituted arylcycloalkanes, compositions containing them and use thereof. The present invention relates especially to substituted arylcycloalkanes with therapeutic activity, which may be used such as in oncology.Type: GrantFiled: December 4, 2002Date of Patent: May 3, 2005Assignee: Aventis Pharma S. A.Inventors: Patrick Mailliet, Marc Capet, Gilles Tiraboschi, Thomas Caulfield
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Patent number: 6806264Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) in which X represents halogen, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro, cyano or in each case optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy or phenylalkylthio, Y represents in each case optionally substituted cycloalkyl, aryl or hetaryl, W and Y independently of one another each represent hydrogen, halogen, alkyl, alkoxy, alkenyloxy, halogenoalkyl, halogenoalkoxy, halogenoalkenyloxy, nitro or cyano, CKE represents one of the groups in which A, B, D, G and Q1 to Q6 are each as defined in the description, to a plurality of processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: December 8, 2003Date of Patent: October 19, 2004Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretshneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
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Patent number: 6777447Abstract: Benzylidene cyclohexanone, cyclopentanone and acteone derivatives and therapeutic methods of using same are disclosed. The compounds are non-toxic and exhibit potent anti-inflammatory, antibacterial and antioxidation activity. Also, certain compounds of the invention inhibit glutathione S-transferase (“GST”), but do not irritate the gastrointestinal tract. Pharmaceutical compositions containing the compounds of the invention and pharmaceutically acceptable carriers are also disclosed.Type: GrantFiled: February 27, 2002Date of Patent: August 17, 2004Inventors: Mochammad Samhoedi Reksohadiprodjo, Henk Timmerman, Sardjiman Dummy, Supardjan Amir Margono, Sudibyo Martono, Sugiyanto Dummy, Lukman Rahman Hakim, Nurlaila Dummy, Arief Rahman Hakim, Ika Puspitasari, Arief Nurrochmad, Purwantiningsih Dummy, Oetari Dummy, Tedjo Yuwono
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Publication number: 20030232892Abstract: Zeaxanthin (ZX) or other medically or commercially important carotenoids can be prepared in microcrystalline form, in an oily carrier liquid, to increase their bioavailability following oral ingestion. Initial processing is carried out to prepare a “rough” or “coarse-grained” carotenoid preparation containing relatively large particles of the ZX or other carotenoid, in a suitable form such as a lyophilized stable powder. The coarse-grain preparation is dissolved in a suitable solvent such as tetrahydrofuran, and mixed with a carrier liquid comprising a digestible oil (such as a vegetable oil) and an emulsifying agent. The resulting oil-and-solvent mixture is injected, along with inert gas such as nitrogen, into a vacuum chamber, where a suitable vacuum and temperature combination is used to remove the solvent in a rapid “flash” manner which does not give the carotenoid crystals time to grow larger through accretion or aggregation.Type: ApplicationFiled: June 18, 2002Publication date: December 18, 2003Inventors: Luis H. Guerra-Santos, Dale K. Greenbury
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Publication number: 20030161867Abstract: A dermally deliverable pharmaceutical composition comprises at least one selective cyclooxygenase-2 (COX-2) inhibitory drug or prodrug thereof solubilized in a pharmaceutically acceptable carrier that comprises a low molecular weight monohydric alcohol, and exhibits a skin permeation rate of the therapeutic agent at least equal to that exhibited by a reference solution of the therapeutic agent in 70% aqueous ethanol. A method of effecting targeted delivery of a selective COX-2 inhibitory drug to a site of pain and/or inflammation in a subject comprises topically administering such a composition to skin of the subject, preferably at a locus overlying or adjacent to the site of pain and/or inflammation. A method of effecting systemic treatment of a subject having a COX-2 mediated disorder comprises transdermally administering such a composition, preferably by contacting the composition with an area of skin of the subject not greater than about 400 cm2.Type: ApplicationFiled: May 30, 2002Publication date: August 28, 2003Inventors: Guang Wei Lu, Gary D. Ewing, Praveen Tyle, Brenda M. Stoller, Rajeev Gokhale, Ashwini Gadre
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Publication number: 20030130352Abstract: Disclosed is a novel use of a prostaglandin compound as a chloride channel opener. According to the instant invention, chloride channels in a mammalian subject can be opened by a prostaglandin compound to facilitate chloride ion transportation.Type: ApplicationFiled: August 30, 2002Publication date: July 10, 2003Applicant: SUCAMPO, A.G.Inventors: Ryuji Ueno, John Cuppoletti
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Publication number: 20030092772Abstract: Benzylidene cyclohexanone, cyclopentanone and acteone derivatives and therapeutic methods of using same are disclosed. The compounds are non-toxic and exhibit potent anti-inflammatory, antibacterial and antioxidation activity. Also, certain compounds of the invention inhibit glutathione S-transferase (“GST”), but do not irritate the gastrointestinal tract. Pharmaceutical compositions containing the compounds of the invention and pharmaceutically acceptable carriers are also disclosed.Type: ApplicationFiled: February 27, 2002Publication date: May 15, 2003Inventors: Mochammad Samhoedi Reksohadiprodjo, Henk Timmerman, Sardjiman, Supardjan Amir Margono, Sudibyo Martono, Sugiyanto, Lukman Hakim, Nurlaila, Arief Rahman Hakim, Ika Puspitasari, Arief Nurrochmad, Purwantiningsih, Oetari, Tedjo Yuwono
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Patent number: 6514934Abstract: The present invention is directed to nitrosated or nitrosylated &agr;-adrenergic receptor antagonists, compositions comprising &agr;-adrenergic receptor antagonists that are optionally substituted with at least one NO or NO2 moiety and compounds that donate, transfer or release nitric oxide or elevate levels of endogenous endothelium-derived relaxing factor, and methods for treating sexual dysfunctions in males and females.Type: GrantFiled: March 30, 1999Date of Patent: February 4, 2003Assignee: NitroMed, Inc.Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
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Publication number: 20020183366Abstract: This invention describes novel compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent. The invention also provides novel kits comprising at least one COX-2 selective inhibitor, and, optionally, at least one nitric oxide donor, and/or, optionally, at least one therapeutic agent. The novel cyclooxygenase 2 selective inhibitors of the invention can be optionally nitrosated and/or nitrosylated.Type: ApplicationFiled: March 22, 2002Publication date: December 5, 2002Inventors: David S. Garvey, Joseph D. Schroeder
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Publication number: 20020128267Abstract: The present invention provides methods for the treatment and prevention of ocular COX-2 mediated disorders using COX-2 inhibitors.Type: ApplicationFiled: May 4, 2001Publication date: September 12, 2002Inventors: Rebanta Bandyopadhyay, David Eveleth, Thomas Joseph Van Haarlem, Tugrul T. Kararli, Satish K. Singh
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Publication number: 20020016342Abstract: The present invention provides a method for the treatment or prophylaxis of COX-2-mediated conditions in patients who are at risk of developing thromboembolic events which comprises administering to said patient a therapeutically or prophylactically effective amount of a COX-2 selective inhibitor and a cardiovascular protective amount of a thromboxane inhibitor, as well as compositions therefor.Type: ApplicationFiled: May 14, 2001Publication date: February 7, 2002Inventors: Edward Scolnick, Kathleen Metters, Denis Riendeau, Mervyn Turner
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Publication number: 20010023258Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.Type: ApplicationFiled: February 6, 2001Publication date: September 20, 2001Inventors: Thomas R. Dean, Jesse A. May, Verney L. Sallee, Louis Desantis
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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: 6172118Abstract: This invention relates to ketones, alcohols and amines represented by the likes of of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylethynylcyclobutan-1-one. They are useful as PDE 4 antagonists.Type: GrantFiled: April 8, 1999Date of Patent: January 9, 2001Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6150374Abstract: The invention relates to novel substituted cycloalkenes of the formula (I), ##STR1## to a plurality of processes for their preparation, and to novel intermediates and a plurality of processes for their preparation.Type: GrantFiled: September 29, 1997Date of Patent: November 21, 2000Assignee: Bayer AktiengesellschaftInventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 6121330Abstract: The novel 5-hydroxy-alkyl-substituted phenyls are prepared by either reacting the corresponding benzaldehydes with the Grignard compounds and subsequently reducing the other functional groups or by reducing the corresponding benzoic esters by customary methods to give the corresponding hydroxyl compounds. The 5-hydroxy-alkyl-substituted phenyls are suitable for use as active compounds in medicaments, in particular for the treatment of dyslipidaemia.Type: GrantFiled: September 2, 1999Date of Patent: September 19, 2000Assignee: Bayer AktiengesellschaftInventors: Matthias Muller-Gliemann, Rolf Angerbauer, Arndt Brandes, Michael Logers, Carsten Schmeck, Gunter Schmidt, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt
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Patent number: 6118017Abstract: This invention relates to ketones, alcohols and amines and acids represented by the likes of 3-(3-cyclopentyloxy-4-methoxyphenyl)-3-phenylcyanoclobutan-1-one. They are useful as PDE 4 antngionists.Type: GrantFiled: April 8, 1999Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: Siegfried B. Christensen, IV, Cornelia J. Forster
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Patent number: 6107346Abstract: The present application relates to a series of compounds, and pharmaceutical formulations thereof, of the formula ##STR1## which provide a method of inhibiting hyperlipidemia, especially hypercholesterolemia, and the pathological sequelae thereof, in mammals, including humans.Type: GrantFiled: August 4, 1998Date of Patent: August 22, 2000Assignee: Eli Lilly and CompanyInventor: George Joseph Cullinan
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Patent number: 6075044Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: July 17, 1998Date of Patent: June 13, 2000Assignee: The Regents of the University of CaliforniaInventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
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Patent number: 6051588Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.Type: GrantFiled: April 19, 1995Date of Patent: April 18, 2000Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
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Patent number: 6048877Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.Type: GrantFiled: January 20, 1998Date of Patent: April 11, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
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Patent number: 5994294Abstract: Disclosed are nitrosated and nitrosylated .alpha.-adrenergic receptor antagonists, compositions of an .alpha.-adrenergic receptor antagonist (.alpha.-antagonist), which can optionally be substituted with at least one NO or NO.sub.2 moiety, and a compound that donates, transfers or releases nitric oxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.cndot.); and uses for each of them in treating human impotence or erectile dysfunction.Type: GrantFiled: September 18, 1996Date of Patent: November 30, 1999Assignee: NitroMed, Inc.Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
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Patent number: 5843869Abstract: There are described a method for enriching the anabolic p-hydroxyphenylpyruvate dioxygenases from plant tissues and a method by means of which the enzymatic activity of the enzyme can be measured in a simple manner without complete purification of the enzyme being necessary. The invention furthermore describes an assay system for identifying inhibitors of p-hydroxyphenylpyruvate dioxygenase from plants, in which an enriched HPPD from plants is incubated with a test substrate to be examined and the enzymatic activity of the enzyme is determined in comparison with the activity of the uninhibited enzyme. The invention furthermore describes the novel herbicidal active substances of the formula (I) ##STR1## which were found using the assay method according to the invention.Type: GrantFiled: January 6, 1995Date of Patent: December 1, 1998Assignee: Hoechst AktiengesellschaftInventor: Arno Schulz
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Patent number: 5840661Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.Type: GrantFiled: December 31, 1996Date of Patent: November 24, 1998Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
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Patent number: 5677336Abstract: Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.Type: GrantFiled: October 21, 1993Date of Patent: October 14, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lawrence G. Hamann, Luc Farmer, Michael G. Johnson, Mark E. Goldman
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Patent number: 5665773Abstract: Disclosed is the use of cloprostenol and fluprostenol analogues for the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic compositions comprising said compounds.Type: GrantFiled: December 18, 1996Date of Patent: September 9, 1997Assignee: Alcon Laboratories, Inc.Inventors: Peter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke
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Patent number: 5663180Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from alkyl, hydrido, hydroxyalkyl, halo, haloalkyl, alkoxycarbonyl and carboxyl; wherein R.sup.5 is selected from alkylsulfonyl, haloalkylsulfonyl and sulfamyl; and wherein B is phenyl or pyridyl, wherein B is optionally substituted at a substitutable position with alkyl, halo, alkylthio, cyano, haloalkyl, alkoxy, hydroxyalkyl and alkoxyalkyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 15, 1994Date of Patent: September 2, 1997Assignee: G.D. Searle & Co.Inventors: David B. Reitz, Jinglin Li
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Patent number: 5618547Abstract: A series of 1,3-propanediones having a perfluoroalkyl group or a perfluorocycloalkyl group on one carbonyl, and a 3,5-disubstituted phenyl group on the other, are useful when administered to animals for the control of ectoparasites.Type: GrantFiled: March 10, 1994Date of Patent: April 8, 1997Assignee: British Technology Group LimitedInventors: Rudolph J. Boisvenue, Gary D. Crouse
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Patent number: 5618837Abstract: Methods for inhibiting intimal hyperplasia in the vasculature of mammals, including primates, are disclosed. The methods comprise administering to the mammal an effective amount of Brefeldin A or a derivative of Brefeldin A. The methods are useful in reducing intimal hyperplasia due to, for example, vascular injuries resulting from angioplasty, endarterectomy, reduction atherectomy or anastomosis of a vascular graft. The non-peptide PDGF antagonists Brefeldin A and its derivatives may optionally be administered coordinately with heparin, whereby the coordinately administered of non-peptide PDGF antagonist and heparin are combinatorially effective in inhibiting intimal hyperplasia.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: ZymoGenetics, Inc.Inventors: Charles E. Hart, Oliver J. McConnell, Robert R. West, Theresa Martinez
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Patent number: 5455265Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.Type: GrantFiled: February 11, 1993Date of Patent: October 3, 1995Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5149711Abstract: A 2-cyclopentenone derivative represented by the following formula ##STR1## wherein R.sup.1 represents an alkyl group having 1 to 10 carbon atoms which may be substituted by a substituted or unsubstituted phenyl or phenoxy group, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and each represents a hydrogen atom or a lower alkanoyl group, and the wavy line shows that the bonded state of the double bond is E or Z.This compound is useful for treating, for instance, malignant tumors.Type: GrantFiled: March 7, 1989Date of Patent: September 22, 1992Assignee: Teijin LimitedInventors: Atsuo Hazato, Seizi Kurozumi