Plural Ring Oxygens In The Tricyclo Ring System Patents (Class 549/387)
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Publication number: 20100137583Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: ApplicationFiled: September 8, 2008Publication date: June 3, 2010Inventors: Robert Edward Babine, Shu-Hui Chen, Jason Eric Lamar, Nancy June Snyder, Xicheng Sun, Mark Joseph Tebbe, Frantz Victor, Q. May Wang, Yvonne Yee Mai Yip, Ivan Collado, Cristina Garcia-Paredes, Raymond Samuel Parker, III, Ling Jin, Deqi Guo, John Irvin Glass
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Patent number: 7678929Abstract: Disclosed are furochroman compounds of formula I liquid-crystal media which contains the compounds of formula I, and the use of the media in electro-optical displays, in particular in VAN LCDs.Type: GrantFiled: December 3, 2007Date of Patent: March 16, 2010Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer, Georg Bernatz
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Patent number: 7642362Abstract: Compounds represented by the general formula (1) wherein R1 and R3 are each independently hydrogen or a carboxyl group and R2 and R4 are each independently hydrogen or a hydroxyl group, or pharmaceutically acceptable salts thereof, which exhibit semaphorin-inhibitory activity and are useful as preventives or remedies for neuropathic and neurodegenerative diseases are provided.Type: GrantFiled: January 22, 2003Date of Patent: January 5, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Kazuo Kumagai, Nobuo Hosotani
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Publication number: 20090312317Abstract: Coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a method for treating cancer with coumarin compounds.Type: ApplicationFiled: June 10, 2009Publication date: December 17, 2009Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Jang-Yang Chang, Ching-Chuan Kuo, Yu-Sheng Chao
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Publication number: 20090298931Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: October 4, 2007Publication date: December 3, 2009Applicant: BIONOMICS LIMITEDInventors: Bernard Luke Flynn, Jonathan B. Baell, Andrew J. Harvey, Jason Hugh Chaplin, Dharam Paul, Jorgen Alvar Mould
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Publication number: 20090170927Abstract: The present invention relates to compounds of formula I, which are functionalized phenolic compounds, and polymers formed from the same. Ar—[O—(X)p—R?]q??I Polymers formed from the functionalized phenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.Type: ApplicationFiled: October 16, 2006Publication date: July 2, 2009Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20090111836Abstract: The present invention relates to compounds, compositions for use in reversing multidrug resistance in cancer cells, process for the preparation thereof and their uses in treating cancers. More particularly, the present invention relates to 3?,4?-aromatic acyloxy substituted 7,8-pyranocoumarins compounds for use in reversing P-glycoprotein overexpression mediated multidrug resistance in cancer cells, pyranocoumarins containing compositions, process for the preparation thereof and their uses in treating cancers.Type: ApplicationFiled: October 31, 2007Publication date: April 30, 2009Inventors: Wangfun Fong, Xiaoling Shen, Guangying Chen, Guoyuan Zhu, Chikeung Wan, Kaiwing Tse
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Publication number: 20090093069Abstract: Diacetonefructose derivatives have substituents at the hydroxyl-position. Diacetonefructose derivatives may include immunogenic moieties to prepare anti-diacetonefructose derivative antibodies, or antigenic moieties for immunodiagnostic assays. Also, the diacetonefructose derivatives can include signal generating moieties for detecting the presence or amount of the diacetonefructose derivative in a sample. Additionally, the diacetonefructose derivatives can be used in immunodiagnostic assays to compete with topiramate for binding with anti-diacetonefructose derivative antibodies. Also, methods, compositions and kits are disclosed directed at diacetonefructose derivatives, immunogens, signal generating moieties and immunoassays for topiramate.Type: ApplicationFiled: June 7, 2008Publication date: April 9, 2009Applicant: ARK Diagnostics, Inc.Inventors: Johnny Valdez, Byung Sook Moon, Jacqueline Nguyen, Alejandro Orozco
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Publication number: 20090076128Abstract: The present application describes deuterium-enriched topiramate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 11, 2008Publication date: March 19, 2009Applicant: Protia LLCInventor: Anthony W. Czarnik
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Patent number: 7495111Abstract: 3-Amino chroman and 2-amino tetralin derivatives and compositions containing such compounds are disclosed. Such compounds are useful for modulating activity of a 5-HT1A receptor (agonizing or antagonizing) in a patient. These compounds are further useful for inhibiting binding to a serotonin receptor. Methods of using the 3-amino chroman and 2-amino tetralin compounds and compositions containing such compounds in the treatment of serotonin disorders, such as depression and anxiety, are also disclosed.Type: GrantFiled: June 15, 2006Date of Patent: February 24, 2009Assignee: WyethInventors: P. Sivaramakrishnan Ramamoorthy, Zhongqi Shen, Boyd L. Harrison
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Publication number: 20090043100Abstract: [Problems] To provide an efficient process for producing an optically active chromene oxide compound which is an important intermediate for a benzopyran compound effective in the treatment of arrhythmia. [Means For Solving Problems] The process for producing an optically active chromene oxide compound comprises using an optically active titanium complex represented by, e.g., the formula (1) or (2) as a catalyst to asymmetrically oxidize an optically active chromene compound with high enantioselectivity in high chemical yield.Type: ApplicationFiled: March 9, 2007Publication date: February 12, 2009Applicant: NISSAN CHEMICAL INDUSTRIES, LTDInventors: Shoichi Kondo, Kowichiro Saruhashi, Hisayuki Watanabe, Tsutomu Katsuki
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Publication number: 20080312312Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia.Type: ApplicationFiled: August 1, 2008Publication date: December 18, 2008Inventors: Gregory Lee Durst, Bryan Hurst Norman, Lance Allen Pfeifer, Timothy Ivo Richardson
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Publication number: 20080287527Abstract: The present invention discloses hydroxy-morusin, a method of extracting hydroxy-morusin, as well as various uses in manufacturing antibacterial medicaments or oral care products or for other antibacterial uses.Type: ApplicationFiled: May 16, 2008Publication date: November 20, 2008Applicant: HAWLEY & HAZEL (BVI) COMPANY LIMITEDInventor: Yao Shi
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Patent number: 7414126Abstract: The present invention relates to a process for the preparation of topiramate, intermediates in this process and a process for the preparation of these intermediates.Type: GrantFiled: April 29, 2005Date of Patent: August 19, 2008Assignees: Helm AG, CF Pharma Gyogyszergyarto Kft.Inventors: Geza Arvai, Sandor Garaczi, Attila Gergely Mate, Ferenc Lukacs, Zsolt Viski, Geza Schneider
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Publication number: 20080188549Abstract: The present invention has its object to provide a specific compound derived from a naturally occurring substance, and a composition for the prevention and/or treatment of metabolic syndrome and insulin resistance syndrome which comprises that as an active ingredient, easily and efficiently. The present invention relates to a composition for the prevention and/or treatment of metabolic syndrome and a composition for the prevention and/or treatment of insulin resistance syndrome, each of which comprises, as an active ingredient, at least one compound selected from among the compound represented by the formula (1), compounds represented by the formula (4) and compounds represented by the formula (5), or a salt or ester thereof.Type: ApplicationFiled: February 8, 2006Publication date: August 7, 2008Applicant: Kaneka CorporationInventors: Hozumi Tanaka, Shinichi Yokota, Misuzu Tsukagawa, Tatsumasa Mae, Minpei Kuroda, Yoshihiro Mimaki
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Publication number: 20080177095Abstract: Disclosed are furochroman compounds of formula I liquid-crystal media which contains the compounds of formula I, and the use of the media in electro-optical displays, in particular in VAN LCDs.Type: ApplicationFiled: December 3, 2007Publication date: July 24, 2008Inventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer, Georg Bernatz
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Publication number: 20080153872Abstract: Certain bis-(coumarin) compounds as well as the products of their intramolecular cyclization including pharmaceutically acceptable salts, hydrates, solvates, clathrates, prodrugs, tautomers and stereoisomers thereof are disclosed. Certain processes and intermediates for the preparation of certain bis-(coumarin) compounds, as well as for the use of these compounds as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diseases and conditions in mammals, especially humans are also disclosed.Type: ApplicationFiled: January 13, 2006Publication date: June 26, 2008Inventors: Mladen Mercep, Ivica Malnar, Boska Hrvacic, Stribor Markovic, Anita Filipovic Sucic, Berislav Bosnjak, Andreja Cempuh Klonkay, Renata Rupcic, Antun Hutinec, Ivaylo Jivkov Elenkov, Milan Mesic
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Patent number: 7385067Abstract: The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.Type: GrantFiled: June 2, 2006Date of Patent: June 10, 2008Assignee: Merck Patent GmbHInventors: Peer Kirsch, Andreas Taugerbeck, Alexander Hahn
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Publication number: 20080132566Abstract: A metabolic syndrome relieving agent that is free from a problem of side effects and can be taken for a long term is provided. Bergamottin is used as an agent for relieving a metabolic syndrome. Since bergamottin has functions of activating PPAR? and PPAR?, promoting the secretion of adiponectin in adipocytes and inhibiting the generation of VLDLs in hepatic cells, it is possible to prevent or treat diseases such as insulin resistance, hyperinsulinism, type 2 diabetes, obesity, visceral fat obesity, hypertension, hyperlipemia, arteriosclerosis and the like and thus prevent or treat the metabolic syndrome. Also, as understood from the fact that citrus fruits such as a grapefruit or the like containing bergamottin have been eaten for many years, they have no problems in terms of safety and have a low calorie content, and therefore, they can be taken for a long term.Type: ApplicationFiled: January 20, 2006Publication date: June 5, 2008Applicant: ARKRAY, Inc.Inventors: Takao Sasaki, Masamichi Yano
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Patent number: 7196209Abstract: The present invention is directed to a continuous process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein R1, R3, R4, R5, R6 and X are as herein defined. The present invention is further directed to a continuous process for the preparation of Topiramate.Type: GrantFiled: October 23, 2003Date of Patent: March 27, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Thomas W. Adkins, Charles F. Cicco, Penina Feibush, Donald A. Koch, Cynthia Maryanoff, Walter E. Stalzer
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Patent number: 7157589Abstract: The present invention is directed to a one-step process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein X, R1, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: March 1, 2004Date of Patent: January 2, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Joachim Ernst Berkner, Scott Duncan, John Mills
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Patent number: 7144885Abstract: This invention relates to a novel fused tricyclic heterocycle of the formula (Ia, Ib) and its use for the treatment of hyper-proliferative disordersType: GrantFiled: February 21, 2003Date of Patent: December 5, 2006Assignee: Bayer Pharmaceuticals CorporationInventors: Chengzhi Zhang, Michael Burke, Zhi Chen, Jacques Dumas, Dongping Fan, Benjamin D. Jones, Gaetan Ladouceur, Wendy Lee, Barton Phillips, Scott M. Wilhelm, Qian Zhao
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Publication number: 20040249167Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor &bgr; agonists. Such agonists are useful for the treating Estrogen Receptor &bgr; mediated diseases such as prostate cancer.Type: ApplicationFiled: April 20, 2004Publication date: December 9, 2004Inventors: Jeffrey Alan Dodge, Venkatesh Krishnan, Charles Willis Lugar, Blake Lee Neubauer, Bryan Hurst Norman, Lance Allen Pfeifer, Timothy Ivo Richardson
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Publication number: 20040176440Abstract: Novel compounds of the formula I 1Type: ApplicationFiled: December 2, 2003Publication date: September 9, 2004Inventors: Teresa Mujica-Fernaud, Herwig Buchholz, Christophe Carola, Wilfried Rautenberg, Christian Sirrenberg
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Patent number: 6774142Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-dioxyflavinoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavinoids may be avoided by administering such compounds by parenteral routes (e.g., sublingual, buccal, intranasal, injection, etc.).Type: GrantFiled: September 6, 2002Date of Patent: August 10, 2004Inventors: Thomas P. Lahey, Vithal J. Rajadhyasksha
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Patent number: 6737439Abstract: A composition and method of cancer treatment is disclosed. The composition and method utilized the extract of B. papyrifera, or compounds included therein having aromatase inhibition properties, as active cancer chemopreventative and treating agents in mammals, including humans.Type: GrantFiled: July 25, 2002Date of Patent: May 18, 2004Assignee: The Board of Trustees of the University of IllinoisInventors: Alan Douglas Kinghorn, John M. Pezzuto, Dongho Lee, Krishna P. L. Bhat
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Publication number: 20040039202Abstract: The present invention concerns compounds of formula (V) and (VI), a method for producing them and colorants containing compounds of formula (V) and/or (VI).Type: ApplicationFiled: March 28, 2003Publication date: February 26, 2004Inventors: Guido Sauter, Hans-Juergen Braun, Raymond Brouillard, Andre Fougerousse, Christine Roehri-Stoeckel, Emmanuel Gonzalez
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Patent number: 6696578Abstract: A novel cartilage-specific compound and methods of diagnosis in medical and veterinary contexts using the compound. Screening methods for therapeutic substances and methods of treatment are also provided.Type: GrantFiled: September 28, 2001Date of Patent: February 24, 2004Assignee: Mount Sinai HospitalInventors: Harpal Kaur Gahunia, Kenneth Pritzker, Reinhold Vieth
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Patent number: 6602903Abstract: The invention relates to compounds of formula (I): and medicinal products containing the same are useful in treating or in preventing melatoninergic disorders.Type: GrantFiled: August 28, 2001Date of Patent: August 5, 2003Assignee: Les Laboratories ServierInventors: Gérald Guillaumet, Marie-Claude Viaud, Ahmed Mamai, Isabelle Charton, Pierre Renard, Caroline Bennejean, Béatrice Guardiola, Philippe Daubos
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Patent number: 6465625Abstract: Highly specific biocatalytic reactions have been used to create a population of taxol derivatives.Type: GrantFiled: June 19, 2000Date of Patent: October 15, 2002Assignee: Albany Molecular Research, Inc.Inventors: Jonathan S. Dordick, Douglas S. Clark, Peter C. Michels, Yuri L. Khmelnitsky
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Publication number: 20020086333Abstract: A novel cartilage-specific compound and methods of diagnosis in medical and veterinary contexts using the compound. Screening methods for therapeutic substances and methods of treatment are also provided.Type: ApplicationFiled: September 28, 2001Publication date: July 4, 2002Inventors: Harpal Kaur Gahunia, Kenneth Pritzker, Reinhold Vieth
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Patent number: 6399653Abstract: The invention relates to compounds of the formula I in which the radicals R1, R2, R3 and A have the meaning mentioned in the description. The invention further relates to a process for the preparation of the compounds of the formula I by means of solid-phase synthesis, and use thereof as pharmaceuticals.Type: GrantFiled: June 30, 2000Date of Patent: June 4, 2002Assignee: Hoechst AktiengesellschaftInventor: Stephan Henke
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Patent number: 6384045Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: June 24, 1999Date of Patent: May 7, 2002Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 6365610Abstract: The invention provides a urokinase production inhibitor or angiogenesis inhibitor comprising as an active component an ozonide derivative represented by the formula (1), and method of prevention or therapy using the inhibitor wherein A is an oxygen atom or N—R (wherein R is phenyl or phenyl having as a substituent lower alkyl having 1 to 6 carbon atoms, lower alkoxyl having 1 to 6 carbon atoms or a halogen atom); B is an oxo group or —R4; and (1) when A is an oxygen atom, R1 is a hydrogen atom, etc., R2 is phenyl, etc., R3 is a hydrogen atom, etc., B is an oxo group or —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.; (2) when A is N—R, R1 is a hydrogen atom, etc., R2 is a hydrogen atom, etc., R3 is a hydrogen atom, etc., B is —R4, R4 is a hydrogen atom, etc., R5 is a hydrogen atom, etc.Type: GrantFiled: March 28, 2000Date of Patent: April 2, 2002Assignee: Taiho Pharmaceutical Company Ltd.Inventors: Takuma Sasaki, Masatomo Nojima
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Publication number: 20020013480Abstract: The present invention relates to methods for preparing 2,2-dimethyl-5-acyloxy-10-propyl-2H,8H-benzo[ 1,2-b:3,4-b ′]dipyran-8-one (5) and 2,2-dimethyl-5-hydroxy- 10-propyl-2H,8H-benzo[1,2-b:3,4-b ′]dipyran-8-one (6) and their use as intermediates for the synthesis of antiviral calanolide compounds. For example, Fries rearrangement on compound 5 or Friedel-Crafts reaction on 6, yields intermediate 2,2-dimethyl-5-hydroxy-6-propionyl-10-propyl-2H,8H-benzo[1,2-b:3,4-b′]dipyran-8-one (4), which, in turn, can be converted to (+)-calanolide A and (−)-calanolide B. The coupling of compound 6 with the appropriate chiral molecule under Mitsunobu or nucleophilic displacement leads to the asymmetric synthesis of antiviral calanolide compounds.Type: ApplicationFiled: July 31, 2001Publication date: January 31, 2002Applicant: Sarawak Medichem Pharmaceuticals, Inc.Inventors: Ze-Qi Xu, Hongwei Yuan, Jennifer Crabb, Raghu Samy, Ailing Li, Hua Cao
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Patent number: 6300339Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, T, X, Y, Z, R5, R6, R7, R8, Ar, k, m, n and p are as defined in the specification. These compounds are useful in treating or preventing conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: October 9, 2001Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6262083Abstract: The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not induce any side effects.Type: GrantFiled: May 5, 2000Date of Patent: July 17, 2001Assignee: Choongwae Pharma CorporationInventors: Sung-Hwan Moon, Hea-Jin Choi, Su-Jin Lee, Jea-Uk Chung, Jong-Ryul Ha, Kyoung-June Lee, Se-Woong Oh, Kwang-Won Jeong
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Patent number: 6255324Abstract: 5′-substituted, 4′,5′-dihydropsoralen compounds (5) bearing tertiary amines (and salts thereof), quaternary ammonium moieties or organomercurial moieties are described. Also described are 2-substituted mercurimethyl-2-3-dihydro-benzofurans of forumla (7): Also reported are versatile direct syntheses through a hitherto unknown compounds such as 3-R-4,8-dimethyl-4′,5′-dihydro-5′-bromomethylpsoralen or a 3-R-4,8-dimethyl-4′, 5′-dihydro-5′-iodomethylpsoralen to prepare a structurally diverse array of partially reduced psoralens and benzofurans. The presence of a permanent ammonium charge in these psoralens precludes membrane passage and the mono-unsaturation precludes the cross-linking of nuclear DNA, thereby minimizing the mutagenic/carcinogenic side effects long associated with psoralen-derived therapies.Type: GrantFiled: November 25, 1998Date of Patent: July 3, 2001Inventors: Ned D. Heindel, Jeffrey D. Laskin, Diane E. Heck, Robert D. Rapp, Marilyn S. Whittemore, Thomas E. McNeel, Ivan Jabin
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Patent number: 6225478Abstract: Novel iridoid derivatives represented by general formula (I): and a vascularization inhibitor having for its active ingredient said derivative are disclosed. This vascularization inhibitor has remarkable vascularization inhibitory effects unaccompanied by serious adverse side effects, which is useful for the treatment and prevention of various diseases accompanied by abnormal acceleration of vascularization.Type: GrantFiled: September 13, 1999Date of Patent: May 1, 2001Assignee: Tsumura & Co.Inventors: Hideaki Morishige, Yukiko Kurita, Yousuke Yamazaki, Chiaki Sakakibara, Masaharu Kigawa
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Patent number: 6136961Abstract: Highly specific biocatalytic reactions have been used to create a population of derivatives from a single starting compound. Examples demonstrate synthesis of derivatives of taxol, taxol-2'-adipate, taxol-2'-vinyl adipate, 2,3-(methylenedioxy) benzaldehyde, (.+-.)-(2-endo, 3-exo)-bicyclo (2.2.2)octo-5-ene-2,3-dimethanol, adenosine and erythromycin.Type: GrantFiled: June 29, 1998Date of Patent: October 24, 2000Assignee: EnzyMed, Inc.Inventors: Jonathan S. Dordick, Douglas S. Clark, Peter C. Michels, Yuri L. Khmelnitsky
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Patent number: 6071946Abstract: A compound selected from those of formula (I): ##STR1## in which A, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the Specification, and pharmaceutical compositions containing the same, which are useful for treating a mammal afflicted with a disorder of the melatoninergic system.Type: GrantFiled: September 1, 1999Date of Patent: June 6, 2000Assignee: Adir et CompagnieInventors: Daniel Lesieur, Patrick Depreux, Veronique Leclerc, Hamid Ait Mansour, Philippe Delagrange, Pierre Renard
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Patent number: 6034120Abstract: The present invention provides an antifeedant and a contact insecticide using the components contained in Cyperaceae species. In particular, the present invention provides an insect antifeedant and a contact insecticide comprising as an active ingredient at least one compound selected from the group consisting of scabequinone, remirol, cyperaquinone and the derivatives thereof.Type: GrantFiled: February 24, 1998Date of Patent: March 7, 2000Assignee: Morita Kaguku Kogyo Co., Ltd.Inventors: Koichiro Komai, Masanori Morimoto, Toyoshige Morita
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Patent number: 6034256Abstract: A class of benzopyran, derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I' ##STR1## wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.Type: GrantFiled: April 17, 1998Date of Patent: March 7, 2000Assignee: G.D. Searle & Co.Inventors: Jeffery S Carter, Mark G Obukowicz, Balekudru Devadas, John J Talley, David L Brown, Matthew J Graneto, Stephen R Bertenshaw, Donald J Rogier, Jr., Srinivasan R Nagarajan, Cathleen E Hanau, Susan J Hartmann, Cindy L Ludwig, Suzanne Metz
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Patent number: 6034239Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.Type: GrantFiled: March 6, 1997Date of Patent: March 7, 2000Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Osamu Uchikawa, Kohji Fukatsu, Masaomi Miyamoto
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Patent number: 6022888Abstract: Novel iridoid derivatives represented by general formula (I): and a vascularization inhibitor having for its active ingredient said derivative are disclosed. This vascularization inhibitor has remarkable vascularization inhibitory effects unaccompanied by serious adverse side effects, which is useful for the treatment and prevention of various diseases accompanied by abnormal acceleration of vascularization.Type: GrantFiled: September 8, 1998Date of Patent: February 8, 2000Assignee: Tsumura & Co.Inventors: Hideaki Morishige, Yukiko Kurita, Yousuke Yamazaki, Chiaki Sakakibara, Masaharu Kigawa
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Patent number: 5998461Abstract: This invention relates to benzofuran/pyran derivatives of a new tricyclic amide compound, their composition and method of use for treating disorders of the melatoninergic system.Type: GrantFiled: July 28, 1998Date of Patent: December 7, 1999Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Patrick Depreux, Ve'ronique Leclerc, Hamid Ait Mansour, Philippe Delagrange, Pierre Renard
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Patent number: 5986114Abstract: The invention relates to benzopyranol derivatives which are intermediates in a process for stereoselectively forming N-substituted dihydro-2,3 benzodiazopines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.Type: GrantFiled: March 2, 1999Date of Patent: November 16, 1999Assignee: Eli Lilly and CompanyInventors: Benjamin A. Anderson, Marvin M. Hansen
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Patent number: 5958970Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxyprone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.Type: GrantFiled: July 29, 1997Date of Patent: September 28, 1999Assignee: Kansas State University Research FoundationInventors: Duy H. Hua, Jean-Pierre Perchellet
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Patent number: 5856529Abstract: Novel derivatives of benzofuran and dihydrobenzofuran are provided which are useful as melatonergic agents.Type: GrantFiled: December 9, 1997Date of Patent: January 5, 1999Assignee: Bristol-Myers Squibb CompanyInventors: John D. Catt, Graham Johnson, Daniel J. Keavy, Ronald J. Mattson, Michael F. Parker, Katherine S. Takaki, Joseph P. Yevich
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Patent number: 5773609Abstract: A broad class of photosensitive compounds having enhanced in vivo target tissue selectivity and versatility in photodynamic therapy. Many furocoumarin compounds, such as psoralens, exhibit cytostatic activity when photoactivated but exhibit little in vivo specificity for selectively accumulating in any particular target tissue such as atheromatous plaques. Reactive Oxygen Producing Photosensitizers ("ROPPs") are photoactivatable compounds having an affinity for hyperproliferating cells (such as atheromatous plaque cells), which when photoactivated, produce cytotoxic reaction products. The photoactivity of a ROPP, such as a porphyrin, may be reduced by metalating the porphyrin while the selective affinity of the metalized ROPP for hyperproliferating tissue remains substantially unchanged.Type: GrantFiled: February 14, 1997Date of Patent: June 30, 1998Assignee: PDT Pharmaceuticals, Inc.Inventors: Byron Robinson, Alan R. Morgan, Hugh L. Narciso, Jr.