The Bicyclo Ring System Consists Of The Hetero Ring And A Six-membered Carbocyclic Ring Patents (Class 549/398)
  • Patent number: 6759401
    Abstract: The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ri
    Type: Grant
    Filed: October 11, 2002
    Date of Patent: July 6, 2004
    Assignee: Biovitrum AB
    Inventors: Björn Nilsson, Jan Tejbrant, Benjamin Pelcman, Erik Ringberg, Markus Thor, Jonas Nilsson, Mattias Jönsson
  • Publication number: 20040106595
    Abstract: 2H-1-Benzopyran derivatives, processes for their preparation and use thereof for the preparation of pharmaceutical compositions for the prevention and treatment of postmenopausal pathologies.
    Type: Application
    Filed: December 22, 2003
    Publication date: June 3, 2004
    Inventors: Maurizio Delcanale, Gabriele Amari, Elisabetta Armani, Maurizio Civelli, Elisabetta Galbiati
  • Patent number: 6727239
    Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
    Type: Grant
    Filed: April 2, 2003
    Date of Patent: April 27, 2004
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jerry Harnett, Dominique Pons, Gérard Ulibarri, Dennis Bigg
  • Publication number: 20040072828
    Abstract: This invention relates to novel 2,6-substituted chroman derivatives which are useful in the treatment of beta-3 adrenoreceptor-mediated conditions.
    Type: Application
    Filed: September 17, 2003
    Publication date: April 15, 2004
    Applicant: Bayer Pharmaceuticals Corporation
    Inventors: Stephen J. O'Connor, Gaetan H. Ladouceur, William H. Bullock, Ann-Marie Campbell, Miao Dai, Robert Dally, Jacques Dumas, Holia N. Hatoum-Mokdad, Uday Khire, Wendy Lee, Qingjie Liu, Derek B. Lowe, Steven R. Magnuson, Ning Qi, Tatiana E. Shelekhin, Quanrong Shen, Roger A. Smith, Ming Wang
  • Patent number: 6716998
    Abstract: This invention provides a process for the stereospecific preparation of 2-yl-chroman and -chromene derivatives of the formula: These compounds are useful for the preparation of optically active 2-aminomethyl- and 2-azaheterocyclylmethyl-chromans.
    Type: Grant
    Filed: October 4, 2002
    Date of Patent: April 6, 2004
    Assignee: Wyeth
    Inventor: Jonathan L. Gross
  • Patent number: 6706724
    Abstract: The invention describes novel substituted aryl 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, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl
    Type: Grant
    Filed: December 21, 2001
    Date of Patent: March 16, 2004
    Assignee: NitroMed, Inc.
    Inventors: Subhash P. Khanapure, David S. Garvey, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Ricky D. Gaston
  • Patent number: 6706757
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Grant
    Filed: October 2, 2002
    Date of Patent: March 16, 2004
    Assignee: Wyeth
    Inventors: Lynne Padilla Greenblatt, Michael Gerard Kelly
  • Patent number: 6703416
    Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar; R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S; R4 is aryl radical; R5 is H, halogen, C1-C20 alkyl or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r′)(r″) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r′ and r″ are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of
    Type: Grant
    Filed: October 31, 2001
    Date of Patent: March 9, 2004
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Simon Trouille
  • Publication number: 20040039202
    Abstract: 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: Application
    Filed: March 28, 2003
    Publication date: February 26, 2004
    Inventors: Guido Sauter, Hans-Juergen Braun, Raymond Brouillard, Andre Fougerousse, Christine Roehri-Stoeckel, Emmanuel Gonzalez
  • Publication number: 20040034239
    Abstract: Novel benzopyran-based inhibitors of NADH:ubiquinone oxidoreductase are designed, synthesized, and shown to have anti-cancer activity.
    Type: Application
    Filed: July 23, 2003
    Publication date: February 19, 2004
    Inventors: Kyriacos C Nicolaou, Jeffrey Pfefferkorn, Guo-Qiang Cao, Anthony Roecker
  • Publication number: 20040014805
    Abstract: A fruit polyphenol obtained by subjecting a crab apple fruit to pressing and/or extraction. The fruit polyphenol is rich in such components as condensed tannins (procyanidins), chlorogenic acid, and epicatechin. The fruit polyphenol can be produced economically and efficiently.
    Type: Application
    Filed: March 11, 2003
    Publication date: January 22, 2004
    Inventor: Toshihiko Shoji
  • Patent number: 6680390
    Abstract: The invention relates to the use of compounds of the formula I in which X is the divalent radical of oxygen, a carbonyl radical, optionally aliphatically substituted imino or the radical ═CR9R10, Y is a carbonyl group or the radical ═CR9R10, R1 and R2 are identical or different electron-withdrawing radicals, chosen from the group consisting of cyano, alkyl- or arylcarbonyl, alkyloxy- or aryloxycarbonyl, optionally substituted aminocarbonyl, alkyl- or arylsulfinyl, alkyl- or arylsulfonyl and optionally substituted aminosulfonyl, R3 is a hydrogen atom, a cyano, hydroxyl, carboxyl or aminocarbonyl group or a C5-C20-aryl radical or C1-C20-alkylradical optionally bonded via an oxygen bridge, an aminocarbonyl bridge or oxycarbonyl bridge, R4 is a hydrogen atom, a hydroxyl group, an amino group, or a C5-C20-aryl radical or C1-C20-alkyl radical optionally bonded via an oxygen bridge, and R5 to R10 independently of one another are hydrogen or C1-C20-alkyl radicals and where in additio
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: January 20, 2004
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Prechtl, Thorsten Habeck, Horst Westenfelder, Thomas Wilnsch
  • Patent number: 6664411
    Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereosomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.
    Type: Grant
    Filed: March 27, 2001
    Date of Patent: December 16, 2003
    Assignees: Dr. Reddy's Laboratories Limited, Reddy-Cheminor Inc.
    Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli
  • Patent number: 6660871
    Abstract: Substituted 4H-chromene derivatives are a new class of compounds that bind to Bcl-2 protein and induce apoptosis in tumor cells. The present invention is directed to an efficient synthetic method for the preparation of these compounds from salicylaldehyde derivatives and alkyl cyanoacetates under solid phase.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: December 9, 2003
    Assignee: Thomas Jefferson Unversity
    Inventor: Ziwei Huang
  • Publication number: 20030225158
    Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing disipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of supressing appetite and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.
    Type: Application
    Filed: January 22, 2003
    Publication date: December 4, 2003
    Inventors: Bruce J. Auerbach, Larry D. Bratton, Gary F. Filzen, Andrew G. Geyer, Bharat K. Trivedi, Paul C. Unangst
  • Patent number: 6630461
    Abstract: A method for treating neurodegenerative diseases in a warm-blooded animal comprising administering to a warm-blooded animal in need thereof an amount of a compound of the formula wherein A selected from the group consisting of hydrogen and wherein the substituents are defined as set forth in the specification.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: October 7, 2003
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Publication number: 20030166932
    Abstract: Compounds of the formula 1
    Type: Application
    Filed: January 4, 2002
    Publication date: September 4, 2003
    Inventors: Richard L. Beard, Thong Vu, Diana F. Colon, Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Publication number: 20030162054
    Abstract: The present invention discloses a red organic EL device containing compound which allows EL emission to be shifted to the red spectral region, and a higher purity in color for red EL devices is obtained. The, synthesis of the compound is easy and the product yield is improved compared to the prior art. Moreover, the red organic EL devices fabricated conform with existing NTSC standards.
    Type: Application
    Filed: March 24, 2003
    Publication date: August 28, 2003
    Applicant: Industrial Technology Research Institute
    Inventors: Liang-Jyi Chen, Wen-Kou Weng, Chun-Neng Ku, Po-Yen Lu
  • Publication number: 20030153599
    Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.
    Type: Application
    Filed: October 3, 2002
    Publication date: August 14, 2003
    Applicant: Wyeth
    Inventors: Michael Gerard Kelly, Lynne Padilla Greenblatt, Gan Zhang, Yvette L. Palmer, Steven Edward Lenicek
  • Patent number: 6599903
    Abstract: Intermediate compounds having the formula wherein the substituents are defined as set forth in the disclosure.
    Type: Grant
    Filed: September 4, 2001
    Date of Patent: July 29, 2003
    Assignee: Societe de Conseils de Recherches d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Publication number: 20030134148
    Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1
    Type: Application
    Filed: November 8, 2002
    Publication date: July 17, 2003
    Applicant: FUJI PHOTO FILM CO., LTD.
    Inventors: Hisashi Okada, Terukazu Yanagi
  • Publication number: 20030130342
    Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
    Type: Application
    Filed: September 9, 2002
    Publication date: July 10, 2003
    Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Michael Paal, Gerd Ruhter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
  • Publication number: 20030105342
    Abstract: A process for the stereoselective synthesis of 2-hydroxymethyl-chromans of formula (II) is provided 1
    Type: Application
    Filed: October 4, 2002
    Publication date: June 5, 2003
    Applicant: Wyeth
    Inventors: Jonathan L. Gross, Gary P. Stack
  • Publication number: 20030100774
    Abstract: This invention provides a process for the stereospecific preparation of 2-yl-chroman and -chromene derivatives of the formula: 1
    Type: Application
    Filed: October 4, 2002
    Publication date: May 29, 2003
    Applicant: Wyeth
    Inventor: Jonathan L. Gross
  • Patent number: 6566397
    Abstract: A method of and compositions for suppressing the growth of tumor cells in a patient are disclosed. In one embodiment, the method comprises treating the patient with an effective amount of an isoprenoid ether-linked compound, wherein the isoprenoid ether-linked compound comprises a first acyclic isoprenoid molecule linked via an ether linkage to a second molecule, wherein the second molecule can suppress tumor formation.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: May 20, 2003
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Charles E. Elson, Manfred Jung, Huanbiao Mo
  • Publication number: 20030092695
    Abstract: The present invention relates to metal salts of 3-methyl-chromane or thiochromane derivatives, stereoisomers or hydrates thereof, and an anti-estrogenic pharmaceutical composition which comprises the above compound as an active component and exhibits a highly improved solubility.
    Type: Application
    Filed: June 13, 2002
    Publication date: May 15, 2003
    Inventors: Jaechon Jo, SungDae Park, HyunSuk Lim, SungOh Ahn, Kazumi Morikawa, Yoshitake Kanbe, Masahiro Nishimoto, MyungHwa Kim
  • Publication number: 20030087897
    Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.
    Type: Application
    Filed: May 10, 2002
    Publication date: May 8, 2003
    Inventors: Takashi Tsukamoto, Pavel Majer, Bunda Hin, Weizheng Xu, Qun Liu, Doris Stoermer
  • Publication number: 20030073839
    Abstract: This invention related to novel sulfonamide substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.
    Type: Application
    Filed: March 7, 2000
    Publication date: April 17, 2003
    Inventors: Gaetan H. Ladouceur, Richard D. Connell, Jeremy Baryza, Anne-Marie Campbell, Timothy G. Lease, James H. Cook
  • Publication number: 20030069303
    Abstract: The invention provides chroman compounds having Formula (1), wherein R1 is (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl, and independently R1 has a cis-orientation in relation to the exocyclic phenyl group at the 2-position of the skeleton; R4 is Hal, CF3, OH or (1C-2C)alkyloxy; R2, R3, and R5 are independently H, Hal, CF3, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl and prodrugs thereof for the manufacture of a medicine for estrogen-receptor related treatments.
    Type: Application
    Filed: August 30, 2002
    Publication date: April 10, 2003
    Inventors: Gerrit Herman Veeneman, Neeltje Miranda Teerhuis
  • Publication number: 20020164498
    Abstract: The present invention discloses a novel compound useful as the material for a red organic EL device. The novel compound is produced by connecting a benzene ring at the positions 2 and 3 of withdrawing group 2,5-dimethyl-4-(2,2-dicyano)pyrane, and connecting a conjugated donating group at position 5. Using this compound, the EL emission is shifted to the red spectral region, and a higher purity in color for red EL elements is obtained. The synthesis of the compound is easy and the product yield is improved compared to the prior art. Moreover, the red organic EL devices fabricated using the compound have properties that conform with existing NTSC standards.
    Type: Application
    Filed: March 19, 2001
    Publication date: November 7, 2002
    Inventors: Liang-Jyi Chen, Wen-Kuo Weng, Chun-Neng Ku, Po-Yen Lu
  • Publication number: 20020156054
    Abstract: Aryl-substituted and aryl and (3-oxo-1-propenly)-substituted benzopyran, benzothiopyran, 1,2-dihydroquinoline, and 5,6-dihydronaphthalene derivatives have retinoid negative hormone and/or antagonist-like biological activities. The invented RAR antagonists can be administered to mammals, including humans, for the purpose of preventing or diminishing action of RAR agonists on the bound receptor sites. Specifically, the RAR agonists are administered or coadministered with retinoid drugs to prevent or ameliorate toxicity or side effects caused by retinoids or vitamin A or vitamin A precursors. The retinoid negative hormones can be used to potentiate the activities of other retinoids and nuclear receptor agonists. For example, the retinoid negative hormone called AGN 193109 effectively increased the effectiveness of other retinoids and steroid hormones in in vitro transactivation assays. Additionally, transactivation assays can be used to identify compounds having negative hormone activity.
    Type: Application
    Filed: March 28, 2001
    Publication date: October 24, 2002
    Inventors: Elliott S. Klein, Alan T. Johnson, Andrew M. Standeven, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Sunil Nagpal, Vidyasagar Vuligonda, Min Teng, Roshantha A. Chandraratna
  • Publication number: 20020146588
    Abstract: The present invention discloses a novel compound useful as the material for a red organic EL device. The novel compound is produced by connecting a benzene ring at the positions 2 and 3 of withdrawing group 2, 5-dimethyl-4-(2,2-dicyano)pyrane, and connecting a conjugated donating group at position 5. Using this compound, the EL emission is shifted to the red spectral region, and a higher purity in color for red EL elements is obtained. The synthesis of the compound is easy and the product yield is improved compared to the prior art. Moreover, the red organic EL devices fabricated using the compound have properties that conform with existing NTSC standards.
    Type: Application
    Filed: May 16, 2001
    Publication date: October 10, 2002
    Inventors: Liang-Jyi Chen, Wen-Kuo Weng, Chun-Neng Ku, Po-Yen Lu
  • Patent number: 6455578
    Abstract: The present invention is directed to aromatic derivatives of formula (I), wherein: R1 is (a), wherein R3 and R4 are selected from between H and OH, provided that R3 and R4 are not simultaneously H, and R2 is H; or R1 and R2 taken together, are (b), wherein R5 is selected from between CH3 and (CH2)5OH, to the iron complexes thereof, and to their use for the preparation of pharmaceutical compositions for the normalization of iron level.
    Type: Grant
    Filed: April 30, 2001
    Date of Patent: September 24, 2002
    Assignee: Laboratoire Medidom S.A.
    Inventor: Guido Di Napoli
  • Patent number: 6448269
    Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
    Type: Grant
    Filed: June 18, 2001
    Date of Patent: September 10, 2002
    Assignee: Eli Lilly and Company
    Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Jr., Michael Paal, Gerd Rühter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
  • Patent number: 6420334
    Abstract: 2-Alkoxydecahydro-2,3a,4,4,7-pentamethyl-3,7a-methano-7aH-indeno[5,6-b]furans are valuable novel woody fragrances for the preparation of perfume oils.
    Type: Grant
    Filed: June 30, 2000
    Date of Patent: July 16, 2002
    Assignee: Haarmann & Reimer GmbH
    Inventors: Horst Surburg, Peter Wörner
  • Publication number: 20020077333
    Abstract: Substituted isoquinolines, isochromanones and isothiochromanones that inhibit the pro-inflammatory cytokines tumor necrosis factor-alpha (TNF-alpha) and/or interleukin-6 (IL-6) and/or the enzyme cyclooxygenase-2 (COX-2) and/or interleukin-10 (IL-10). Compositions containing such compounds and methods of using such compounds for treatment and/or prevention of inflammation, inflammatory diseases, immunologic diseases and other diseases mediated by TNF-alpha, IL-6, COX-2 and/or IL-10 are also disclosed.
    Type: Application
    Filed: October 10, 2001
    Publication date: June 20, 2002
    Inventors: Debendranath Dey, Partha Neogi, Ananda Sen, Somesh D. Sharma, Bishwajit Nag
  • Publication number: 20020068739
    Abstract: The present invention relates to the compounds of formula (I) in which X, R1, R2 and R3 are as defined in claim 1. These compounds are cholesteryl acyl transferase (ACAT) inhibitors.
    Type: Application
    Filed: November 1, 2001
    Publication date: June 6, 2002
    Applicant: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Diedier Festal, Jean Yves Nioche, Guy Augert, Jacques Deserprit
  • Patent number: 6399653
    Abstract: 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: Grant
    Filed: June 30, 2000
    Date of Patent: June 4, 2002
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Stephan Henke
  • Publication number: 20020035276
    Abstract: A method for producing a chroman-carboxylic acid is provided, which method includes reacting a dialkylphenol compound, a formaldehyde and an alcohol in the presence of a secondary amine and an acid to give an alkoxymethylated phenol compound (Step 1); reacting the obtained alkoxymethylated phenol compound with an ester having a carbon-carbon double bond at a temperature of not less than 100° C. to give a dialkylchroman carboxylic acid ester (Step 2); hydrolyzing the obtained dialkylchroman carboxylic acid ester to give a dialkylchroman-carboxylic acid (Step 3); and reacting the obtained dialkylchroman-carboxylic acid with an aromatic hydrocarbon in the presence of a Lewis acid (Step 4).
    Type: Application
    Filed: August 28, 2001
    Publication date: March 21, 2002
    Applicant: KURARAY CO., LTD.
    Inventors: Tatsuhiko Hayashibara, Junko Sato, Masahiro Torihara
  • Patent number: 6353014
    Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:
    Type: Grant
    Filed: June 2, 1999
    Date of Patent: March 5, 2002
    Assignee: Alcon Laboratories, Inc.
    Inventors: Verney L. Sallee, Mark R. Hellberg, Peter G. Klimko
  • Patent number: 6344558
    Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: April 20, 2001
    Date of Patent: February 5, 2002
    Assignee: Gruenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Patent number: 6340700
    Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.
    Type: Grant
    Filed: September 22, 1999
    Date of Patent: January 22, 2002
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet
  • Patent number: 6335445
    Abstract: A compound selected from the group consisting of a compound of the formula wherein A is selected from the group consisting of and the other substituents are defined in the specification having an inhibitory activity of NO-synthase enzymes producing nitrogen mono-oxide and/or an activity which traps the reactive oxygen species.
    Type: Grant
    Filed: December 7, 1999
    Date of Patent: January 1, 2002
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Etienne Chabrier de Lassauniere, Serge Auvin, Dennis Bigg, Michel Auguet, Jeremiah Harnett
  • Patent number: 6313162
    Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: November 6, 2001
    Assignee: Centre International de Recherche Dermatologiques Galderma (C.I.R.D.) Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 6288230
    Abstract: Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: n is an integer; R1 represents an organic or inorganic group; R2 represents halogen or C1-C6 alkyl; RN is an alkylene carrying a substituted piperazine, piperidine, or tetrahydropyridine; and R4 is hydrogen or C1-C6 alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
    Type: Grant
    Filed: September 29, 1999
    Date of Patent: September 11, 2001
    Assignee: Neurogen Corporation
    Inventors: Xi Chen, Xiao-shu He
  • Patent number: 6248737
    Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 19, 2001
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Patent number: 6239171
    Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiathermogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: May 29, 2001
    Assignee: Lipogenics, Inc.
    Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
  • Patent number: 6225480
    Abstract: The present invention relates to a linker shown by the following formula (I): X—SO2—R1—(A)m—R2  (I) wherein R1 is a group of the formula (A): [wherein R3, R4 and R5 are the same or different hydrogen, etc], etc, R2 is a group which can form a chemical bond to a resin which may be protected by a conventional protective group, A is lower alkylene, etc, X is a leaving group, and m is an integer of 0 or 1, with proviso that A is (C2-C6)alkylene, and m is an integer of 1, when R1 is a group of the formula (A).
    Type: Grant
    Filed: June 30, 1999
    Date of Patent: May 1, 2001
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Akito Tanaka, Hideo Tsutsumi
  • Patent number: 6204290
    Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: March 20, 2001
    Assignee: Lipogenics, Inc.
    Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
  • Patent number: 6201131
    Abstract: The present invention provides a safer and more efficient process for producing [2-(arylsulfonyl)ethenyl]benzene derivatives of the formula (3): wherein R1, R2, R3 and R4 are the same or different and each independently represent a hydrogen, fluorine, or chlorine atom, a lower alkyl group, or the like, and two adjacent R3 and R4 may bond each other at their terminals to form a ring, which the process is characterized in that a 2-(arylsulfonyl)ethanol of formula (1): wherein R1 and R2 are as defined above, and an acid anhydride are reacted in the presence of a base, and the reaction liquid obtained is supplied to a reaction with an aromatic halide of formula (2): wherein X represents a chlorine, bromine, or iodine atom, and R3 and R4 are the same as defined above, in the presence of a palladium catalyst and a base.
    Type: Grant
    Filed: March 22, 2000
    Date of Patent: March 13, 2001
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Jyunzou Otera, Akihiro Orita, Akio Kurihara