Five-membered Alicyclic Ring Patents (Class 514/684)
  • Patent number: 9622497
    Abstract: 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: Grant
    Filed: January 30, 2011
    Date of Patent: April 18, 2017
    Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical Factory
    Inventors: Xinde Xu, Bin Shao, Xuejun Lao
  • Patent number: 8846747
    Abstract: 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: Grant
    Filed: November 17, 2010
    Date of Patent: September 30, 2014
    Assignees: University of Rochester, Southern Research Institute
    Inventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucille White, Krister Wennerberg
  • Patent number: 8710272
    Abstract: 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: Grant
    Filed: June 18, 2012
    Date of Patent: April 29, 2014
    Assignee: Androscience Corporation
    Inventors: Charles C. Y. Shih, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Publication number: 20130261121
    Abstract: 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: Application
    Filed: June 18, 2012
    Publication date: October 3, 2013
    Inventors: Charles C.Y. SHIH, Qian Shi, Hui-Kang Wang, Ching-Yuan Su
  • Publication number: 20130096175
    Abstract: 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: Application
    Filed: November 17, 2010
    Publication date: April 18, 2013
    Applicants: SOUTHERN RESEARCH INSTITUTE, UNIVERSITY OF ROCHESTER
    Inventors: David S. Goldfarb, Joseph A. Maddry, Lynn Rasmussen, Ellie Lucile White, Krister Wennerberg
  • Patent number: 8415505
    Abstract: 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: Grant
    Filed: February 10, 2009
    Date of Patent: April 9, 2013
    Assignee: Shenyang Pharmaceutical University
    Inventors: Linxiang Zhao, Jingli Wang, Zhenjun Bian, Rui Wang, Dan Liu, Yongkui Jing
  • Publication number: 20120058172
    Abstract: 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: Application
    Filed: November 11, 2011
    Publication date: March 8, 2012
    Applicant: Intermed Discovery GmbH
    Inventors: Ernst Roemer, Torsten Grothe
  • Publication number: 20120053208
    Abstract: Curcumin analogues and methods of making and using the same are disclosed.
    Type: Application
    Filed: April 15, 2010
    Publication date: March 1, 2012
    Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION
    Inventors: Pui-Kai Li, Chenglong Li, Jiayuh Lin, James R. Fuchs
  • Publication number: 20120040976
    Abstract: 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: Application
    Filed: December 11, 2009
    Publication date: February 16, 2012
    Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTE
    Inventors: John R. Cashman, Kenneth J. Abel
  • Publication number: 20110294783
    Abstract: 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: Application
    Filed: August 10, 2011
    Publication date: December 1, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Reiner FISCHER, Stefan LEHR, Peter MARCZOK, Udo Reckmann, Christian Arnold, Waltraud Hempel, Erich SANWALD, Rolf Pontzen
  • Patent number: 8030359
    Abstract: 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: Grant
    Filed: February 9, 2007
    Date of Patent: October 4, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sarah Geers, Michael Lowinger, Craig A. McKelvey, Robert F. Meyer, Dina Zhang
  • Publication number: 20110060054
    Abstract: 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: Application
    Filed: February 10, 2009
    Publication date: March 10, 2011
    Applicant: SHENYANG PHARMACEUTICAL UNIVERSITY
    Inventors: Linxiang Zhao, Jingli Wang, Zhenjun Bian, Rui Wang, Dan Liu, Yongkui Jing
  • Publication number: 20110021613
    Abstract: 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: Application
    Filed: December 11, 2007
    Publication date: January 27, 2011
    Applicant: INTERMED DISCOVERY GMBH
    Inventors: Ernst Roemer, Torsten Grothe
  • Patent number: 7855310
    Abstract: The invention relates to the field of aryl hydrocarbon receptor (Ah receptor; AhR) antagonists and their uses.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: December 21, 2010
    Assignee: SYMRISE GmbH & Co. KG
    Inventors: Martina Herrmann, Oskar Koch, Gabriele Vielhaber, Jean Krutmann
  • Publication number: 20090227563
    Abstract: 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: Application
    Filed: December 11, 2006
    Publication date: September 10, 2009
    Applicant: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Dieter Feucht, Udo Bickers, Hans Philipp Huff, Erwin Hacker, Rainer Süssmann
  • Patent number: 7109380
    Abstract: 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: Grant
    Filed: March 29, 2005
    Date of Patent: September 19, 2006
    Assignees: The University of Mississippi, The United States of America as represented by the Secretary of Agriculture
    Inventors: Xing-Cong Li, Melissa R. Jacob, David Wedge
  • Patent number: 7091241
    Abstract: 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: Grant
    Filed: June 3, 2002
    Date of Patent: August 15, 2006
    Assignee: Summa Health System
    Inventors: Jacques Gilloteaux, Henryk S. Taper, James M Jamison, Jack L. Summers
  • Patent number: 7064148
    Abstract: 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: Grant
    Filed: August 30, 2002
    Date of Patent: June 20, 2006
    Assignee: Sucampo AG
    Inventors: Ryuji Ueno, John Cuppoletti
  • Patent number: 6903238
    Abstract: 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: Grant
    Filed: December 11, 2002
    Date of Patent: June 7, 2005
    Assignee: Wyeth
    Inventors: Robert E. McDevitt, Folake O. Adebi, Heather A. Harris, James C. Keith, Jr., Leo M. Albert
  • Patent number: 6887904
    Abstract: 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: Grant
    Filed: December 4, 2002
    Date of Patent: May 3, 2005
    Assignee: Aventis Pharma S. A.
    Inventors: Patrick Mailliet, Marc Capet, Gilles Tiraboschi, Thomas Caulfield
  • Patent number: 6806264
    Abstract: 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: Grant
    Filed: December 8, 2003
    Date of Patent: October 19, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretshneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 6777447
    Abstract: 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: Grant
    Filed: February 27, 2002
    Date of Patent: August 17, 2004
    Inventors: 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
  • Publication number: 20030232892
    Abstract: 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: Application
    Filed: June 18, 2002
    Publication date: December 18, 2003
    Inventors: Luis H. Guerra-Santos, Dale K. Greenbury
  • Publication number: 20030161867
    Abstract: 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: Application
    Filed: May 30, 2002
    Publication date: August 28, 2003
    Inventors: Guang Wei Lu, Gary D. Ewing, Praveen Tyle, Brenda M. Stoller, Rajeev Gokhale, Ashwini Gadre
  • Publication number: 20030130352
    Abstract: 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: Application
    Filed: August 30, 2002
    Publication date: July 10, 2003
    Applicant: SUCAMPO, A.G.
    Inventors: Ryuji Ueno, John Cuppoletti
  • Publication number: 20030092772
    Abstract: 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: Application
    Filed: February 27, 2002
    Publication date: May 15, 2003
    Inventors: 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
  • Patent number: 6514934
    Abstract: 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: Grant
    Filed: March 30, 1999
    Date of Patent: February 4, 2003
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
  • Publication number: 20020183366
    Abstract: 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: Application
    Filed: March 22, 2002
    Publication date: December 5, 2002
    Inventors: David S. Garvey, Joseph D. Schroeder
  • Publication number: 20020128267
    Abstract: The present invention provides methods for the treatment and prevention of ocular COX-2 mediated disorders using COX-2 inhibitors.
    Type: Application
    Filed: May 4, 2001
    Publication date: September 12, 2002
    Inventors: Rebanta Bandyopadhyay, David Eveleth, Thomas Joseph Van Haarlem, Tugrul T. Kararli, Satish K. Singh
  • Publication number: 20020016342
    Abstract: 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: Application
    Filed: May 14, 2001
    Publication date: February 7, 2002
    Inventors: Edward Scolnick, Kathleen Metters, Denis Riendeau, Mervyn Turner
  • Publication number: 20010023258
    Abstract: 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: Application
    Filed: February 6, 2001
    Publication date: September 20, 2001
    Inventors: Thomas R. Dean, Jesse A. May, Verney L. Sallee, Louis Desantis
  • Patent number: 6251833
    Abstract: 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: Grant
    Filed: August 31, 1999
    Date of Patent: June 26, 2001
    Inventors: Christoph Erdelen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Norbert Mencke, Andreas Turberg
  • Patent number: 6172118
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: January 9, 2001
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6150374
    Abstract: 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: Grant
    Filed: September 29, 1997
    Date of Patent: November 21, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Herbert Gayer, Peter Gerdes, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
  • Patent number: 6121330
    Abstract: 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: Grant
    Filed: September 2, 1999
    Date of Patent: September 19, 2000
    Assignee: Bayer Aktiengesellschaft
    Inventors: Matthias Muller-Gliemann, Rolf Angerbauer, Arndt Brandes, Michael Logers, Carsten Schmeck, Gunter Schmidt, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt
  • Patent number: 6118017
    Abstract: 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: Grant
    Filed: April 8, 1999
    Date of Patent: September 12, 2000
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Cornelia J. Forster
  • Patent number: 6107346
    Abstract: 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: Grant
    Filed: August 4, 1998
    Date of Patent: August 22, 2000
    Assignee: Eli Lilly and Company
    Inventor: George Joseph Cullinan
  • Patent number: 6075044
    Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: June 13, 2000
    Assignee: The Regents of the University of California
    Inventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
  • Patent number: 6051588
    Abstract: 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: Grant
    Filed: April 19, 1995
    Date of Patent: April 18, 2000
    Inventors: David S. Garvey, L. Gordon Letts, H. Burt Renfroe, Sang William Tam
  • Patent number: 6048877
    Abstract: 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: Grant
    Filed: January 20, 1998
    Date of Patent: April 11, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Philip D. Stein, Francis N. Ferrara, Karnail S. Atwal
  • Patent number: 5994294
    Abstract: 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: Grant
    Filed: September 18, 1996
    Date of Patent: November 30, 1999
    Assignee: NitroMed, Inc.
    Inventors: David S. Garvey, Joseph D. Schroeder, Inigo Saenz de Tejada
  • Patent number: 5843869
    Abstract: 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: Grant
    Filed: January 6, 1995
    Date of Patent: December 1, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Arno Schulz
  • Patent number: 5840661
    Abstract: 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: Grant
    Filed: December 31, 1996
    Date of Patent: November 24, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reiner Fischer, Jacques Dumas, Thomas Bretschneider, Christoph Erdelen, Ulrike Wachendorff-Neumann, Hans-Joachim Santel, Markus Dollinger, Andreas Turberg, Norbert Mencke
  • Patent number: 5677336
    Abstract: 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: Grant
    Filed: October 21, 1993
    Date of Patent: October 14, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lawrence G. Hamann, Luc Farmer, Michael G. Johnson, Mark E. Goldman
  • Patent number: 5665773
    Abstract: 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: Grant
    Filed: December 18, 1996
    Date of Patent: September 9, 1997
    Assignee: Alcon Laboratories, Inc.
    Inventors: Peter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke
  • Patent number: 5663180
    Abstract: 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: Grant
    Filed: July 15, 1994
    Date of Patent: September 2, 1997
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li
  • Patent number: 5618837
    Abstract: 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: Grant
    Filed: June 7, 1995
    Date of Patent: April 8, 1997
    Assignee: ZymoGenetics, Inc.
    Inventors: Charles E. Hart, Oliver J. McConnell, Robert R. West, Theresa Martinez
  • Patent number: 5618547
    Abstract: 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: Grant
    Filed: March 10, 1994
    Date of Patent: April 8, 1997
    Assignee: British Technology Group Limited
    Inventors: Rudolph J. Boisvenue, Gary D. Crouse
  • Patent number: 5455265
    Abstract: 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: Grant
    Filed: February 11, 1993
    Date of Patent: October 3, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5149711
    Abstract: 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: Grant
    Filed: March 7, 1989
    Date of Patent: September 22, 1992
    Assignee: Teijin Limited
    Inventors: Atsuo Hazato, Seizi Kurozumi