Bicyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/462)
  • Publication number: 20030139462
    Abstract: The present invention relates to compounds of Formula (I) 1
    Type: Application
    Filed: September 17, 2002
    Publication date: July 24, 2003
    Inventors: Soan Cheng, David Michael Goldstein, Teresa Alejandra Trejo Martin, Eric Brian Sjogren
  • Publication number: 20030118924
    Abstract: The present invention relates to a diarylethene derivative and a photochromic thin film using the same. More particularly, it relates to a diarylethene derivative and a photochromic thin film having excellent transparency prepared by depositing the same on the surface of a substrate, without crystallization or agglomeration to have effective photochromic property. This method also provides homogenous thin photochromic films with film thickness of a nano meter level and improved processability compared to conventional deposition processes thus, being suitable for coloring change with light repeatedly, optical information recording systems, and optical communication media.
    Type: Application
    Filed: July 29, 2002
    Publication date: June 26, 2003
    Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Eun Kyoung Kim, Hyowon Lee
  • Publication number: 20030105343
    Abstract: There is disclosed a method of preparing a branched benzofuran compound comprising a core moiety which contains at least one aromatic ring and which has at least three substituted or unsubstituted benzofuran groups covalently linked thereto.
    Type: Application
    Filed: September 25, 2002
    Publication date: June 5, 2003
    Inventors: Peter Neil Taylor, Sally Anderson, Christopher James Booth, Geraldine Laura Ballantyne Verschoor
  • Patent number: 6569894
    Abstract: Novel benzofuran and dihydrobenzofuran derivatives which have a binding affinity for the human melatonin receptor and, therefore, are useful as melatonergic agents.
    Type: Grant
    Filed: October 3, 2002
    Date of Patent: May 27, 2003
    Assignee: Bristol-Myers Squibb Company
    Inventors: Katherine S. Takaki, Li-Quang Sun, Graham Johnson, James R. Epperson, Stephen R. Bertenshaw
  • Patent number: 6562989
    Abstract: The present invention is directed to a transition metal catalyst, comprising a Group 8 metal and a ligand having the structure wherein R, R′ and R″ are organic groups having 1-15 carbon atoms, n=1-5, and m=0-4. The present invention is also directed to a method of forming a compound having an aromatic or vinylic carbon-oxygen, carbon-nitrogen, or carbon-carbon bond using the above catalyst. The catalyst and the method of using the catalyst are advantageous in preparation of compounds under mild conditions of approximately room temperature and pressure.
    Type: Grant
    Filed: August 3, 2001
    Date of Patent: May 13, 2003
    Assignee: Yale University
    Inventors: John F. Hartwig, Quinetta Shelby, Noriyasu Kataoka
  • Publication number: 20030060640
    Abstract: A method for the preparation of 5-cyano-1-(4-fluorophenyl)-1,3-dihydroisobenzo-furan comprising conversion of a 5-substituted 1-(4-fluorophenyl)-1,3-dihydro-isobenzofuran derivative.
    Type: Application
    Filed: August 30, 2002
    Publication date: March 27, 2003
    Applicant: H. Lundbeck A/S
    Inventor: Hans Petersen
  • Publication number: 20030055084
    Abstract: The present invention provides substituted benzofuran, indene, thianaphthene and oxidized thianaphthene compounds and methods of treatment and pharmaceutical compositions that comprise such compounds. Preferred compounds of the invention contain benzofuran, indene or thianaphthene group substituted with a tetrahydrofuran or other alicyclic group.
    Type: Application
    Filed: July 30, 2002
    Publication date: March 20, 2003
    Applicant: Millennium Pharmaceutical, Inc.
    Inventors: Gurmit Grewal, Ralph Scannell, Xiong Cai, Michelle Young, Aberra Fura
  • Publication number: 20030045571
    Abstract: The present invention is a novel intermediate, compound of the formula (VI) 1
    Type: Application
    Filed: June 25, 2002
    Publication date: March 6, 2003
    Inventor: Kevin E. Henegar
  • Patent number: 6518264
    Abstract: Disclosed are azetidine derivatives of formula: their optical isomers, their salts, their preparation and medicaments containing them.
    Type: Grant
    Filed: March 9, 2001
    Date of Patent: February 11, 2003
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Hervé Bouchard, Jean Bouquerel, Marc Capet, Serg Grisoni, Jean-Luc Malleron, Serge Mignani, Augustin Hittinger
  • Publication number: 20030027853
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; 1
    Type: Application
    Filed: June 14, 2001
    Publication date: February 6, 2003
    Applicant: Allergan Sales, Inc.
    Inventors: Robert M. Burk, Mark Holoboski, Mari F. Posner
  • Patent number: 6514996
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): wherein R1 and R2 independently represent hydrogen, lower alkyl, cyano, —(CH2)n—E1—CO—G1 (wherein E1 represents a bond, O, or NH; and G1 represents hydrogen, substituted or unsubstituted lower alkyl, OR6, or NR7R8; and n represents an integer of 0 to 4), or the like; R1 and R2 are combined to represent a saturated carbon ring together with a carbon atom adjacent thereto; or R2, and R11 or R13 described below are combined to form a single bond; R3 represents hydrogen, phenyl, or halogen; R4 represents hydroxy, lower alkoxy, or the like; A represents —C(R9)(R10)— or O; B represents O, NR11, —C(R12)(R13)—, or —C(R14)(R15)—C(R16)(R17)—; D represents (i) —C(R18)(R19)—X— (wherein X represents —C(R21)(R22)—, S, or NR23), (ii) —C(R19a)═Y— [Y represents —C(R24)—Z— (wherein Z represents C
    Type: Grant
    Filed: November 19, 1997
    Date of Patent: February 4, 2003
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Takashi Kawakita, Koji Yanagawa, Kyoichiro Iida, Rie Koike, Yoshisuke Nakasato, Tohru Matsuzaki, Kenji Ohmori, Soichiro Sato, Hidee Ishii, Haruhiko Manabe, Michio Ichimura, Fumio Suzuki
  • Publication number: 20030018067
    Abstract: This invention provides compounds which act as inhibitors of plasminogen activator inhibitor-1 (PAI-1) of the formula: 1
    Type: Application
    Filed: June 18, 2002
    Publication date: January 23, 2003
    Applicant: Wyeth
    Inventors: Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, Scott Christian Mayer, David LeRoy Crandall
  • Publication number: 20030018064
    Abstract: The present invention relates to novel substituted benzofurans and benzothiophenes compounds that are antagonists of alpha V (&agr;v) integrins, for example &agr;v&bgr;3 and &agr;v&bgr;5 integrins, their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds may be used in the treatment of pathological conditions mediated by &agr;v&bgr;3 and &agr;v&bgr;5 integrins, including such conditions as tumor growth, metastasis, restenosis, osteoporosis, inflammation, macular degeneration, diabetic retinopathy, and rheumatoid arthritis.
    Type: Application
    Filed: April 26, 2002
    Publication date: January 23, 2003
    Applicant: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Beth M. Anaclerio, Juan Jose Marugan Sanchez, Victor J. Marder, David C. U'Prichard
  • Publication number: 20030013887
    Abstract: This invention relates to a series of substituted aromatic ethers of the formula I 1
    Type: Application
    Filed: February 28, 2002
    Publication date: January 16, 2003
    Applicant: Pfizer Inc.
    Inventor: John A. Lowe
  • Publication number: 20030008862
    Abstract: Novel sulfatase inhibitor/estrogen receptor blocker compounds useful in the treatment of estrogen dependent illnesses are disclosed. The compounds generally comprise a sulfamate moiety and an aromatic, estrogen receptor blocker moiety. Methods for synthesizing these compounds and using them in the therapeutic and/or prophylactic treatment of an estrogen-dependent disease are also disclosed.
    Type: Application
    Filed: June 18, 2002
    Publication date: January 9, 2003
    Inventors: Pui-Kai Li, Kyle W. Selcer
  • Publication number: 20030008898
    Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: 1
    Type: Application
    Filed: May 3, 2002
    Publication date: January 9, 2003
    Inventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
  • Publication number: 20020198251
    Abstract: Substituted 2-dialkylaminoalkylbiphenyl derivatives, processes for their preparation, pharmaceutical compositions comprising these compounds and methods using these compounds for the preparation of medicaments and for the treatment of diseases.
    Type: Application
    Filed: February 11, 2002
    Publication date: December 26, 2002
    Inventors: Bernd Sundermann, Babette-Yvonne Koegel, Helmut Buschmann
  • Patent number: 6489365
    Abstract: Compounds of the formula which is explained more fully in the specification, may be prepared by conventional methods and used therapeutically in conventional galenic preparations.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: December 3, 2002
    Assignee: Boehringer Ingelheim KG
    Inventors: Ralf Anderskewitz, Kurt Schromm, Ernst-Otto Renth, Frank Himmelsbach, Franz Birke, Armin Fugner
  • Publication number: 20020173663
    Abstract: A class of aryloxyacetic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Application
    Filed: August 17, 2001
    Publication date: November 21, 2002
    Inventors: Kun Liu, Libo Xu, A. Brian Jones
  • Publication number: 20020169184
    Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.
    Type: Application
    Filed: February 23, 2001
    Publication date: November 14, 2002
    Applicant: American Home Products Corporation
    Inventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
  • Patent number: 6479604
    Abstract: A diarylethene compound of the following formula (1) wherein R1 is a hydrogen or a substituted or unsubstituted C1-22 alkyl group, a fluoro group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted phenylalkyl group, R2 is a C1-22 alkylene group which may be unsubstituted or substituted with fluorine, R3 is a chemical bond, O, S, NR1, N(R2R1), or a C1-3 alkylene group which may be unsubstituted or substituted with one or more oxygen atoms or fluorine atoms, X and Y independently of one another O, S, nitrogen, NR1, or N(R2R1), and Z is a carbonyl group or a methylene group which may be unsubstituted or substituted with fluorine.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: November 12, 2002
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Eun-Kyoung Kim, Yun-Ki Choi
  • Patent number: 6455710
    Abstract: The present invention relates to the process for the preparation and purification of citalopram (I) in which a compound of formula (II) wherein Z is iodo, bromo, chloro or CF3—(CF2)n—SO2—O—, n being 0, 1, 2, 3, 4, 5, 6, 7 or 8, is subjected to a cyanide exchange reaction with a cyanide source; the resultant crude citalopram product is optionally subjected to some initial purification and subsequently treated with an amide or an amide-like group forming agent; the reaction mixture is then subjected to an acid/base wash and/or crystallisation and recrystallisation of citalopram in order to remove the amides formed from the crude citalopram mixture; and the resulting citalopram product is optionally further purified, worked up and isolated as the base or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: September 24, 2002
    Assignee: H. Lundbeck A/S
    Inventors: Marco Villa, Federico Sbrogiò, Robert Dancer
  • Publication number: 20020128290
    Abstract: An oxygen-containing heterocyclic compound represented by following Formula (I): 1
    Type: Application
    Filed: November 19, 1997
    Publication date: September 12, 2002
    Inventors: ETSUO OHSHIMA, TAKASHI KAWAKITA, KOJI YANAGAWA, KYOICHIRO IIDA, RIE KOIKE, YOSHISUKE NAKASATO, TOHRU MATSUZAKI, KENJI OHMORI, SOICHIRO SATO, HIDEE ISHII, HARUHIKO MANABE, MICHIO ICHIMURA, FUMIO SUZUKI
  • Patent number: 6444709
    Abstract: The invention relates to novel heteroethynylenic compounds having 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: February 7, 2000
    Date of Patent: September 3, 2002
    Assignee: Galderma Research & Development S.N.C.
    Inventors: Philippe Diaz, Jean-Michel Bernardon
  • Patent number: 6441196
    Abstract: Novel processes and intermediates useful in the preparation of 11-oxa prostaglandin analogs are disclosed.
    Type: Grant
    Filed: May 18, 2001
    Date of Patent: August 27, 2002
    Assignee: Alcon, Inc.
    Inventors: Pete Delgado, Raymond E. Conrow, William D. Dean, Michael S. Gaines
  • Publication number: 20020099223
    Abstract: A process for the preparation heterocyclic indene analogs, especially with the preparation of 4-hydroxycarbazole or N-protected 4-hydroxycarbazole, involves cyclocarbonylation followed by saponification. This process avoids high temperatures and high catalyst loadings.
    Type: Application
    Filed: January 22, 2002
    Publication date: July 25, 2002
    Inventors: Michelangelo Scalone, Thomas Albert Zeibig
  • Patent number: 6407243
    Abstract: The present invention provides novel compound of the formula: wherein Ra is —OH or —O—(C1-C4 alkyl); R1a is —OH or —O—(C1-C4 alkyl); n is 2 or 3; R2 and R3 are each independently: —C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidinyl, 1-pyrrolidinyl substituted with one or two methyl groups, 4-morpholino or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 10, 1995
    Date of Patent: June 18, 2002
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, George J. Cullinan, Jeffrey A. Dodge, Kennan J. Fahey, Charles D. Jones
  • Patent number: 6403639
    Abstract: 2,3-Dihydrobenzofuran derivatives of general formula (1): wherein R1 represents a hydrogen atom or an acyl group; R2, R3 and R4 represent a hydrogen atom, a lower alkyl group or a lower alkenyl group; R5 and R6 represent a hydrogen atom or an optionally substituted alkyl group, or R5 and R6 combine to form a cycloalkyl group or a saturated heterocyclic group containing one or more oxygen atoms or alkyl-substituted nitrogen atoms, provided that R2 and R3 can not simultaneously represent a t-butyl group, or optically active isomers or pharmaceutically acceptable salts thereof are useful as therapeutic or prophylactic agents for various renal diseases and as organ preservatives.
    Type: Grant
    Filed: November 23, 1999
    Date of Patent: June 11, 2002
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Akira Ishikawa, Yoshiaki Kato, Kunio Tamura, Yoshiaki Takashima, Osamu Cynshi
  • Patent number: 6395738
    Abstract: The present invention relates to benzofuran derivatives represented by following general formula (I): wherein R1 represents lower alkyl, R2 represents hydrogen or substituted or unsubstituted lower alkyl, R3, R4, R5 and R6 independently represent hydrogen or lower alkyl, X represents CH2 or C═O, and Y represents CH2 or NH, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 29, 2000
    Date of Patent: May 28, 2002
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Ohshima, Tohru Matsuzaki, Haruhiko Manabe
  • Patent number: 6391916
    Abstract: Novel C3-substituted cyclodeca-1,5-diynes can be prepared through novel synthetic procedures using starting (E)-C3-substituted-4-(aryl- or heteroarylmethylidene)cyclodeca-1,5-diynes reagents. Both the C3-substituted cyclodeca-1,5-diyn-3-enes and the starting reagents have improved thermal stability compared to unsubstituted counterparts.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: May 21, 2002
    Assignee: The Hong Kong University of Science and Technology
    Inventors: Wei-Min Dai, Anxin Wu, Yuk Ha Lee, Wataru Hamaguchi, Sei-ichi Nishimoto, Ling Zhou, Atsushi Ishii
  • Patent number: 6391919
    Abstract: This invention relates generally to bis-amino acid sulfonamides containing substituted benzyl amines of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as HIV protease inhibitors, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.
    Type: Grant
    Filed: January 12, 2000
    Date of Patent: May 21, 2002
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Robert F. Kaltenbach, George L. Trainor
  • Patent number: 6384281
    Abstract: A pharmaceutical compound of formula (I) in which R1 and R2 are each hydrogen or C1-4 alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, or morpholino group, said group being optionally substituted with 1 to 3 C1-4alkyl substituents, R3 is a naphythyl, indolyl, benzothienyl, benzofuranyl, benzothiazolyl, quinolinyl or isoquinolinyl group, said group being optionally substituted, and n is 1 or 2; or a salt or ester thereof.
    Type: Grant
    Filed: October 3, 2001
    Date of Patent: May 7, 2002
    Assignee: Eli Lilly and Company
    Inventors: Martine Keenan, Sandra Ginette Milutinovic, David Edward Tupper
  • Publication number: 20020041976
    Abstract: Benzofuran, benzothiophene or indole oligomers, co-oligomers, polymers and copolymers, methods for their production, and their use in charge transport and light emission regions of electroluminescent devices are described.
    Type: Application
    Filed: March 26, 2001
    Publication date: April 11, 2002
    Inventors: Sally Anderson, Michael Stuart Weaver
  • Patent number: 6369225
    Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.
    Type: Grant
    Filed: August 29, 2000
    Date of Patent: April 9, 2002
    Assignee: Allergan Sales, Inc.
    Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
  • Publication number: 20020037918
    Abstract: The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.
    Type: Application
    Filed: July 19, 2001
    Publication date: March 28, 2002
    Inventors: Peter Wipf, Jonathan T. Reeves, Billy W. Day, Raghavan Balachandran
  • Patent number: 6358980
    Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
    Type: Grant
    Filed: January 27, 2000
    Date of Patent: March 19, 2002
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
  • Publication number: 20020026060
    Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.
    Type: Application
    Filed: April 23, 2001
    Publication date: February 28, 2002
    Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
  • Patent number: 6350909
    Abstract: The invention relates to new imides, to a plurality of processes for their preparation and to their use as fungicides.
    Type: Grant
    Filed: January 2, 2001
    Date of Patent: February 26, 2002
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Martin Vaupel, Astrid Mauler-Machnik, Gerd Hänssler, Klaus Stenzel, Martin Kugler, Thomas Jaetsch, Peter Wachtler
  • Publication number: 20020010178
    Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I 1
    Type: Application
    Filed: April 20, 2001
    Publication date: January 24, 2002
    Applicant: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Wolfgang Strassburger, Elmar Friderichs
  • Publication number: 20020004604
    Abstract: A method for the preparation of citalopram wherein the aldehyde of formula 1
    Type: Application
    Filed: February 26, 2001
    Publication date: January 10, 2002
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock
  • Publication number: 20010056194
    Abstract: The present invention provides a production method of a 5-phthalancarbonitrile compound, which comprises the use of a novel compound of the formula [I] 1
    Type: Application
    Filed: July 20, 2001
    Publication date: December 27, 2001
    Inventors: Tetsuya Ikemoto, Masami Igi
  • Publication number: 20010031784
    Abstract: The crystalline base of the compound citalopram, 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, having the formula 1
    Type: Application
    Filed: December 5, 2000
    Publication date: October 18, 2001
    Inventors: Hans Petersen, Klaus Peter Bogeso, Per Holm
  • Publication number: 20010031766
    Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed.
    Type: Application
    Filed: February 12, 2001
    Publication date: October 18, 2001
    Applicant: Merck Frosst Canada & Co.
    Inventors: Michel Belley, Nicholas Lachance, Marc Labelle, Michel Gallant, Nathalie Chauret, Laird A. Trimble
  • Publication number: 20010027256
    Abstract: The present invention relates to a method for the preparation of citalopram comprising reaction a compound of formula (I) 1
    Type: Application
    Filed: February 26, 2001
    Publication date: October 4, 2001
    Applicant: H. Lundbeck A/S
    Inventors: Hans Petersen, Michael Harold Rock, Haleh Ahmadian
  • Patent number: 6281240
    Abstract: This invention provides methods of treating secretory diarrhea or cystic fibrosis in a mammal which comprises administering to a mammal in need thereof an effective amount of diarylsulfonylurea. This invention also describes specific diarylsulfonylureas for use in treating secretory diarrhea or cystic fibrosis.
    Type: Grant
    Filed: January 31, 2000
    Date of Patent: August 28, 2001
    Assignee: Eli Lilly and Company
    Inventor: Bruce D Schultz
  • Patent number: 6265428
    Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (1): where X and Y are selected from groups that include O, S, and NH; and Ar1, Ar2 and Ar3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteroaryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.
    Type: Grant
    Filed: June 8, 1999
    Date of Patent: July 24, 2001
    Assignee: Texas Biotechnology Corporation
    Inventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
  • Patent number: 6258816
    Abstract: A novel composition of Nimesulide and salts thereof and Cetrizine possessing antileukotriene, antihistaminic, antiallergic and antiinflammatory action is disclosed. The composition is useful in the cure of allergic disorders such as rhinitis, bronchitis, asthama, urticaria and the like.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: July 10, 2001
    Assignee: Panacea Biotec Limited
    Inventors: Amarjit Singh, Rajesh Jain
  • Patent number: 6258851
    Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.
    Type: Grant
    Filed: October 8, 1999
    Date of Patent: July 10, 2001
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
  • Patent number: 6255277
    Abstract: A method for preventing adverse effects associated with the use of a medical device in a patient by introducing into the patient a device of which at least a portion includes a prophylactic or therapeutic amount of a nitric oxide adduct. The nitric oxide adduct can be present in a matrix coating on a surface of the medical device; can be coated per se on a surface of the medical device; can be directly or indirectly bound to reactive sites on a surface of the medical device; or at least a portion of the medical device can be formed of a material, such as a polymer, which includes the nitric oxide adduct. Also disclosed is a method for preventing adverse effects associated with the use of a medical device in a patient by introducing the device during a medical procedure and before or during said procedure locally administering a nitric oxide adduct to the site of contact of said device with any internal tissue.
    Type: Grant
    Filed: May 10, 1995
    Date of Patent: July 3, 2001
    Assignees: Brigham and Women's Hospital, NitroMed, Inc.
    Inventors: Jonathan Stamler, Joseph Loscalzo, John D. Folts
  • Patent number: 6251925
    Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,
    Type: Grant
    Filed: December 13, 2000
    Date of Patent: June 26, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: Kelly Horne Donaldson, Barry George Shearer, David Edward Uehling