Polycyclo Ring System Which Includes Ring Chalcogen Patents (Class 548/525)
Plural ring chalcogens in the polycyclo ring sytem (e.g., methylenedioxyphenyl containing, etc.) (Class 548/526)
  • Compounds, compositions and methods
    Publication number: 20040082638
    Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.
    Type: Application
    Filed: April 11, 2003
    Publication date: April 29, 2004
    Applicant: Cytokinetics, Inc.
    Inventors: Andrew McDonald, Gustave Bergnes, Bainian Feng, David J. Morgans, Steven David Knight, Kenneth A. Newlander, Dashyant Dhanak, Christopher A. Brook
  • Anti-inflammatory compounds
    Publication number: 20040082601
    Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure: 1
    Type: Application
    Filed: October 21, 2003
    Publication date: April 29, 2004
    Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, Richard Cordova, Kevin Pan, Joseph Meschino
  • 2,6-Substituted chroman derivatives useful as beta-3 adrenoreceptor agonists
    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
  • Derivatives of benzofuran or benzodioxazole compounds
    Patent number: 6716987
    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
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: April 6, 2004
    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
  • Benzothiophene derivatives and herbicidal compositions containing the same
    Publication number: 20040058957
    Abstract: The benzothiophene derivative of the present invention is represented by the general formula (I): 1
    Type: Application
    Filed: June 20, 2003
    Publication date: March 25, 2004
    Inventors: Seiji Tomita, Masatoshi Saitou, Hiroki Sekiguchi, Shin-ichiro Ogawa
  • Radicicol derivatives
    Publication number: 20040053990
    Abstract: Radicicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: 1
    Type: Application
    Filed: July 30, 2003
    Publication date: March 18, 2004
    Applicant: KYOWA HAKKO KOGYO CO., LTD
    Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu
  • Process for preparing amine-substituted benzofurans
    Publication number: 20040054185
    Abstract: The present invention relates to processes for preparing amine substituted benzofurans, and more particularly 4-(2-{2-[(2R)-2-methyl-1-pyrrolidinyl]ethyl}-1-benzofuran-5-yl)benzonitrile, and salts thereof. Compounds prepared by the processes of the invention have demonstrated activity as histamine-3 receptor ligands.
    Type: Application
    Filed: July 2, 2003
    Publication date: March 18, 2004
    Inventors: Marlon D. Cowart, Yu-Ming Pu, Yi-Yin Ku, Timothy A. Grieme, Ashok K. Gupta, Daniel J. Plata, Ramin Faghih, Gregory A. Gfesser
  • Pyrrolecarboxamides and pyrrolethioamides as fungicides
    Publication number: 20040049035
    Abstract: Novel pyrrole derivatives of formula (I) wherein X is oxygen or sulfur; R1 is C1-C4alkyl unsubstituted or substituted, with the exception of CF3; C3-C6cycloalkyl unsubstituted or substituted; or halogen; R2 is hydrogen, C1-C4alkyl unsubstituted or substituted, C1-C4alkoxy unsubstituted or substituted, cyano or halogen; R3 is C1-C4alkyl unsubstituted or substituted; and A is orthosubstituted aryl; orthosubstituted heteroaryl; bicycloaryl unsubstituted or substituted; or bicycloheteroaryl unsubstituted or substituted. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms.
    Type: Application
    Filed: October 8, 2002
    Publication date: March 11, 2004
    Inventors: Harald Walter, Hermann Schneider
  • Substituted biaryl amides as C5a receptor modulators
    Publication number: 20040048913
    Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: March 27, 2003
    Publication date: March 11, 2004
    Inventors: Yang Gao, Alan J. Hutchison, John M. Peterson, Wallace C. Pringle, Andrew Thurkauf, Taeyoung Yoon, He Zhao
  • Benzofuran compounds, compositions, and methods
    Patent number: 6703407
    Abstract: The present invention provides novel, reduced benzothiophenes of formula I wherein R is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl) chloro or bromo; n is 2 or 3; and R2 and R3 each are independently C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidino, dimethyl-1-pyrrolidino, 4-morpholino or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Further provided are methods for alleviating the symptoms of post-menopausal syndrome, and inhibiting endometriosis, uterine fibrosis, and aortal smooth muscle cell proliferation.
    Type: Grant
    Filed: September 20, 1994
    Date of Patent: March 9, 2004
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, George J. Cullinan, Jeffrey A. Dodge, Kennan J. Fahey, Charles D. Jones
  • Aminoalkylpyrrolidine serotonin receptor ligands and compositions, their pharmaceutical uses, and methods for their synthesis
    Publication number: 20040039044
    Abstract: Novel aminoalkylpyrrolidine 5-HT7 receptor ligands, methods of preparing such ligands, intermediate compounds useful in the preparation of the receptor ligands, pharmaceutical compositions comprising the receptor ligands, and methods of treating sleep disorders, pain, depression, and schizophrenia employing the receptor ligands are disclosed. The receptor ligands have formula (1): wherein the formula variables are as defined herein, and pharmaceutically acceptable salts, solvates, active metabolites, or prodrugs thereof.
    Type: Application
    Filed: April 29, 2003
    Publication date: February 26, 2004
    Inventors: Yuanjin Rui, Atsuo Kuki, Yufeng Hong, Zhengwei Peng, David Robert Luthin
  • 5-Nitrobenzofurans
    Publication number: 20040034220
    Abstract: The present invention relates to 5-nitrobenzofurans, to a process for preparing 5-nitrobenzofurans, and to 5-nitro-2,3-dihydrobenzofuran-3-ols, to a process for the preparation thereof and to intermediates.
    Type: Application
    Filed: August 18, 2003
    Publication date: February 19, 2004
    Inventor: Wolfgang Magerlein
  • 3,4-Di-substituted maleimide compounds as CXC chemokine receptor antagonists
    Publication number: 20040034229
    Abstract: Disclosed are compounds of the formula (I) 1
    Type: Application
    Filed: October 11, 2002
    Publication date: February 19, 2004
    Applicant: Schering Corporation
    Inventors: Arthur G. Taveras, Michael Dwyer, Johan A. Ferreira, Viyyoor M. Girijavallabhan, Jianping Chao, John J. Baldwin, J. Robert Merritt, Ge Li
  • Frangible compounds for pathogen inactivation
    Publication number: 20040029897
    Abstract: Compounds and methods for inactivating pathogens in materials are described, including compositions and methods for inactivating pathogens in biological materials such as red blood cell preparations and plasma. The compounds and methods may be used to treat materials intended for in vitro or in vivo use, such as clinical testing or transfusion. The compounds are designed to specifically bind to and react with nucleic acid, and then to degrade to form breakdown products. The degradation reaction is preferably slower than the reaction with nucleic acid.
    Type: Application
    Filed: January 13, 2003
    Publication date: February 12, 2004
    Applicant: Cerus Corporation
    Inventors: David Cook, John E. Merritt, Aileen Nerio, Henry Rapoport, Adonis Stassinopoulos, Susan Wollowitz
  • Novel coumarin derivatives and the salts thereof, a process for the preparation thereof and their use in the pharmaceutical field
    Publication number: 20040023893
    Abstract: The present invention relates to novel coumarin derivatives of formula (I) wherein: X═O or S; n=zero, 1, 2, 3 or 4; R5 and R6, which can be the same or different, are optionally unsaturated C1-C4 alkyl groups, or together with the nitrogen atom they form a residue of cyclic amines optionally containing other heteroatoms; R1═CH3 or phenyl; R2 and R4, which can be the same or different, are H, OH, allyl, halogen or methyl.
    Type: Application
    Filed: May 30, 2003
    Publication date: February 5, 2004
    Inventors: Marco Prosdocimi, Giampaolo Menon, Giovanni Monastra, Enrico Galbiati, Mario Finesso
  • N-substituted benzothiophenesulfonamide derivatives
    Publication number: 20030229126
    Abstract: The present invention relates to an N-substituted benzothiophenesulfonamide derivative or a pharmaceutically acceptable salt thereof and applications thereof. Furthermore, it provides an agent for preventing or treating cardiac or circulatory disease and so on caused by abnormal increase of production of angiotensin II or endothelin I based on chymase activity, or by activation of mast cell, and an agent for preventing adhesion after surgery, wherein the agent has a selective inhibitory action on chymase.
    Type: Application
    Filed: March 13, 2003
    Publication date: December 11, 2003
    Applicant: TOA EIYO Ltd.
    Inventors: Shoji Satoh, Akira Tatsui, Takeshi Hasegawa, Hideki Yamada, Shin-Ichi Kazayama, Takahiro Morita, Hidekazu Masaki, Atsuo Takahashi, Fumiya Yoneyama, Tetsuo Kuze, Yusuke Mizuno, Mizuo Miyazaki, Shinji Takai
  • Glucagon antagonists/inverse agonists
    Publication number: 20030220350
    Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any glucagon-mediated conditions and diseases such as hyperglycemia, Type 1 diabetes, Type 2 diabetes and obesity.
    Type: Application
    Filed: August 30, 2002
    Publication date: November 27, 2003
    Inventors: Jesper Lau, Peter Madsen, Christian Sams, Carsten Behrens, Josef Vagner, Inge Thoger Christensen, Behrend Frederik Lundt, Ulla Grove Sidelmann, Henning Thogersen, Anthony L. Ling, Michael Bruno Plewe, Larry Kenneth Truesdale, Anker Steen Jogensen, Janos Tibor Kodra, Shenghua Shi
  • Crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b] thiophene hydrochloride
    Patent number: 6653479
    Abstract: The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, including inhibition of disease states associated with estrogen deprivation including cardiovascular disease, hyperlipidemia, and osteoporosis; and inhibition of other pathological conditions such as endometriosis, uterine fibrosis, estrogen-dependent cancer (including breast and uterine cancer), prostate cancer, benign prostatic hyperplasia, CNS disorders including Alzheimer's disease, prevention of breast cancer, and up-regulating ChAT.
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: November 25, 2003
    Assignee: Eli Lilly and Company
    Inventors: Julie Kay Bush, Preston Charles Conrad, Merlyn Gerard Flom, Wayne Douglas Luke
  • 3-benzyl-benzothiophenes
    Patent number: 6653328
    Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: November 25, 2003
    Assignee: Eli Lilly and Company
    Inventor: Brian S. Muehl
  • Condensed heterocylic compounds and herbicides containing them as active ingredients
    Publication number: 20030216258
    Abstract: Condensed heterocyclic compounds of the general formula: 1
    Type: Application
    Filed: April 25, 2003
    Publication date: November 20, 2003
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Minoru Takano, Shinichi Kawamura, Takashi Komori
  • Antipicornaviral compounds and compositions, their pharmaceutical uses, and materials for their synthesis
    Patent number: 6632825
    Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
    Type: Grant
    Filed: June 13, 2001
    Date of Patent: October 14, 2003
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Theodore O. Johnson, Jr., Shao Song Chu, Brian Walter Eastman, Ye Hua, Hiep The Luu, Siegfried Heinz Reich, Donald James Skalitzky, Yi Yang, Thomas F. Hendrickson, Fora P. Chan
  • 2-(2-methylphenyl)-3,4-dihydro-2H-pyrrole derivatives
    Patent number: 6632833
    Abstract: The invention relates to novel 2-(2-methylphenyl)-3,4-dihydro-2H-pyrrole derivatives of the formula (I) in which Ar represents substituted phenyl, to a plurality of processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: October 14, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Andrew Plant, Dirk Backhaus, Christoph Erdelen, Andreas Turberg, Norbert Mencke
  • Stable hydrate of a muscarinic receptor antagonist
    Publication number: 20030191176
    Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.
    Type: Application
    Filed: March 25, 2003
    Publication date: October 9, 2003
    Applicant: Pfizer Inc.
    Inventors: Peter James Dunn, John George Matthews, Trevor Jack Newbury, Garry O'Connor
  • Benzofurylpyrone derivatives
    Publication number: 20030186976
    Abstract: There is provided benzofuryl-&agr;-pyrone derivative represented by the following structural formula (I): 1
    Type: Application
    Filed: May 12, 2003
    Publication date: October 2, 2003
    Applicant: TEIJIN LIMITED, MICROBIAL CHEMISTRY RESEARCH FOUNDATION
    Inventors: Yoshimitsu Naniwa, Hiroshi Imai, Tomohide Ida, Emiko Muratani, Kazuo Kitai, Yoshinori Sugimoto, Tomomi Kosugi, Akiko Takeuchi, Kunihito Watanabe, Takami Tomiyama, Tomio Takeuchi, Masa Hamada
  • Antithrombotic agents
    Patent number: 6620837
    Abstract: This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of defined compounds of formula (I) as thrombin inhibitors.
    Type: Grant
    Filed: April 23, 2002
    Date of Patent: September 16, 2003
    Assignee: Eli Lilly and Company
    Inventors: Daniel Jon Sall, John Eldon Toth, Kumiko Takeuchi, Todd Johnathan Kohn, Jolie Anne Bastian
  • Benzopyrazone compounds, compositions thereof, and methods of treatment therewith
    Patent number: 6620838
    Abstract: Benzopyranone compounds having the following structure: wherein R1, X, Y and n are as defined here, are disclosed. The compounds of formula (I), wherein R1 is H, can be prepared by demethylation of the corresponding phenolic methyl ether. The compounds are useful for treating a bone-resorbing disease, cancer, arthritis or an estrogen-related condition such as breast cancer, osteoporosis and endometriosis.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: September 16, 2003
    Assignee: Signal Pharmaceuticals, Inc.
    Inventors: Jeffrey A. McKie, Shripad S. Bhagwat, Johanne Renaud, Martin Missbach
  • Method for preparing sulfone or sulfoxide compound
    Publication number: 20030171589
    Abstract: There is provided a method for preparing a sulfone or sulfoxide compound, characterized in that a sulfide compound is allowed to react with hydrogen peroxide in the presence of a metal oxide catalyst formed by the reaction of hydrogen peroxide with at least one metal or metal compound selected from tungsten metal; molybdenum metal; a tungsten compound comprising tungsten and a Group IIIb, IVb, Vb, or VIb element exclusive of oxygen; and a molybdenum compound comprising molybdenum and a Group IIIb, IVb, Vb, or VIb element exclusive of oxygen.
    Type: Application
    Filed: January 23, 2003
    Publication date: September 11, 2003
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Jun Oguma, Koji Hagiya, Takashi Miyawaki
  • 1,4-Disubstituted benzo-fused urea compounds
    Publication number: 20030162968
    Abstract: Disclosed are compounds of the formulas (I) & (II) shown below which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds.
    Type: Application
    Filed: October 11, 2002
    Publication date: August 28, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John R. Regan
  • Non-psychotropic cannabinoids
    Patent number: 6610737
    Abstract: Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) enantiomer, having (3S,4S) configuration of &Dgr;6 tetrahydrocannabinol type compounds. The compositions are particularly effective in alleviating and even preventing neurotoxicity due to acute injuries to the central nervous system, including mechanical trauma, compromised or reduced blood supply as may occur in cardiac arrest or stroke, or poisonings. They are also effective in the treatment of certain inflammatory disorders and chronic degenerative diseases characterized by neuronal loss and chronic pain including neuropathic pain.
    Type: Grant
    Filed: November 26, 2002
    Date of Patent: August 26, 2003
    Assignee: Pharmos Corporation
    Inventors: Aaron Garzon, George Fink
  • Combination product of a 1,4-benzothiepine 1,1-dioxide compound with at least on
    Publication number: 20030158119
    Abstract: The present invention is directed to a 1,4-benzothiepine 1,1-dioxide compound of formula I 1
    Type: Application
    Filed: August 22, 2002
    Publication date: August 21, 2003
    Inventors: Heiner Glombik, Wendelin Frick, Hans-Ludwig Schafer, Werner Kramer
  • Derivatives of flavones, xanthones and coumarins
    Patent number: 6608089
    Abstract: Compounds having the formula (I) Z—OCH2—C≡CCH2—NRR1  (I) or a pharmaceutically acceptable salt or solvate thereof wherein Z can represent the formula (1A) or (1B). The compounds possess antiproliferative activity and are useful as modulators of multiple drug resistance in cancer chemotherapy. The compounds may also be useful for the manufacture of a medicament for the treatment or prevention of neoplasms, menopausal disorders and osteoporosis.
    Type: Grant
    Filed: February 15, 2002
    Date of Patent: August 19, 2003
    Assignee: Indena S.p.A.
    Inventors: Ezio Bombardelli, Piero Valenti
  • Alpha-hydroxy-gamma-[[(carbocyclic-or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives and uses thereof
    Patent number: 6589962
    Abstract: Certain &agr;-hydroxy-&ggr;-[[(carbocyclic- or heterocyclic-substituted)amino]carbonyl]alkanamide derivatives are described as inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.
    Type: Grant
    Filed: April 16, 2002
    Date of Patent: July 8, 2003
    Assignee: Merck & Co., Inc.
    Inventors: James R Tata, Zhijian Lu, Subharekha Raghavan, Tracy T. Huening, Thomas A. Rano, Mark G. Charest
  • Flavone derivatives, preparation method and use as medicines
    Publication number: 20030119816
    Abstract: The invention concerns novel products of formula (I) wherein: R1 represents a carbocyclic or heterocyclic radical optionally substituted; R2 and R3 are such that one represents hydrogen and the other represents piperidinyl optionally substituted; R4 represents hydrogen, alkyl or phenyl optionally substituted, said products being in all isomeric and salt forms and used as medicines.
    Type: Application
    Filed: September 4, 2002
    Publication date: June 26, 2003
    Inventors: Jean-Luc Haesslein, Dominique Lefrancois, Eric Uridat, Jidong Zhang
  • Transition-metal-catalyzed process for the preparation of sterically hindered N-substituted aryloxyamines
    Patent number: 6579328
    Abstract: Sterically hindered N-substituted aryloxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: June 17, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Stephen D. Pastor, Sai Ping Shum
  • Taxoids, their preparation and pharmaceutical compositions containing them
    Publication number: 20030083497
    Abstract: New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them.
    Type: Application
    Filed: March 13, 2002
    Publication date: May 1, 2003
    Applicant: Aventis Pharma, S.A.
    Inventors: Herve Bouchard, Jean-Dominique Bourzat, Alain Commercon
  • Photochromic bis-naphthopyran compounds and methods for their manufacture
    Publication number: 20030078441
    Abstract: The invention provides photochromic bis-naphthopyran compounds as well as methods for their manufacture and their use. The bis-naphthopyran compounds of the invention exhibit a wide range of color, i.e., from pink to purple to blue gray, upon activation by a source of UV light. Additionally, the bis-naphthopyran compounds of the present invention exhibit broad coloration ability, fast response as to both color change on activation and return to original color, and good fatigue-resistance.
    Type: Application
    Filed: September 4, 2001
    Publication date: April 24, 2003
    Inventors: Weili Zhao, Erick M. Carreira
  • Process for the preparation of chiral glucocorticoid receptor agents
    Publication number: 20030073844
    Abstract: The present invention relates to the preparation of chiral glucocorticoid receptor agents via biaryl atropisomers.
    Type: Application
    Filed: June 28, 2002
    Publication date: April 17, 2003
    Inventors: Yi-Yin Ku, Tim Grieme, Howard E. Morton, Steven A. King
  • Transition-metal-catalyzed process for the preparation of sterically hindered N-substituted alkoxy amines
    Patent number: 6547841
    Abstract: Sterically hindered N-substituted alkoxyamines are prepared by the transition-metal-catalyzed decomposition of diazonium salts in the presence of a sterically hindered nitroxyl radical. These compounds are useful as thermal and light stabilizers for a variety of organic substrates.
    Type: Grant
    Filed: April 2, 2001
    Date of Patent: April 15, 2003
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Stephen D. Pastor, Sai Ping Shum
  • Inhibition by 3-deoxyflavonoids of T-lymphocyte activation and therapies related thereto
    Publication number: 20030069192
    Abstract: 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: Application
    Filed: September 6, 2002
    Publication date: April 10, 2003
    Applicant: SynorX, Inc.
    Inventors: Thomas P. Lahey, V.J. Rajadhyaksha
  • 2,3-Olefinic epothilone derivatives
    Publication number: 20030060623
    Abstract: The present invention relates to 2,3-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.
    Type: Application
    Filed: September 13, 2002
    Publication date: March 27, 2003
    Applicant: Bristol-Myers Squibb Co.
    Inventors: Gregory D. Vite, Robert M. Borzilleri, Gerhard Hofle, Thomas Leibold
  • Pharmaceutical compounds and methods of use thereof
    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
  • Novel chalcones
    Publication number: 20030055056
    Abstract: The present invention discloses new and useful compounds including methyl p-hydroxyphenyllactate, its analogues, chemical derivatives and chemically related compounds and their use as antitumor and immune suppressive agents, as inhibitors of proliferative cell growth and as prophylactic agents to inhibit and prevent cancer and non-malignant cell growth.
    Type: Application
    Filed: February 15, 2002
    Publication date: March 20, 2003
    Inventors: Ezio Bombardelli, Piero Valenti
  • Preparation and use of ortho-sulfonamido bicyclic heteroaryl hydroxamic acids as matrix metalloproteinase and tace inhibitors
    Patent number: 6534491
    Abstract: This invention provides, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stroinelysins and collagenases) and TNF-&agr; converting enzyme (TACE, tumor necrosis factor-&agr;converting enzyme) which are useful for the treatment of diseases in which these enzymes are implicated.
    Type: Grant
    Filed: December 11, 2000
    Date of Patent: March 18, 2003
    Assignee: American Cyanamid Company
    Inventors: Jeremy I. Levin, Arie Zask, Yansong Gu, Jay D. Albright, Xuemei Du
  • Inhibitors of caspases
    Patent number: 6531474
    Abstract: The present invention relates to novel classes of compounds which are caspase inhibitors, in particular interleukin-1&bgr; converting enzyme (“ICE”) inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting caspase activity and consequently, may be advantageously used as agents against interleukin-1-(“IL-1”), apoptosis-, interferon-&ggr; inducing factor-(IGIF), or interferon-&ggr;-(“IFN-&ggr;”) mediated diseases, including inflammatory diseases, autoimmune diseases, destructive bone disorders, proliferative disorders, infectious diseases, and degenerative diseases.
    Type: Grant
    Filed: September 19, 2000
    Date of Patent: March 11, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Marion W. Wannamaker, Guy W. Bemis, Paul S. Charifson, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, Keith P. Wilson, James W. Janetka, Robert J. Davies, Anne-Laure Grillot, Zhan Shi, Cornelia J. Forster
  • Benzofurane derivatives
    Patent number: 6531503
    Abstract: Benzofurane derivatives of formula (I), wherein R and R′ have the meanings given in claim no. (1), and salts thereof are suitable for use as intermediate products in the synthesis of medicaments.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: March 11, 2003
    Assignee: Merck Patent GmbH
    Inventors: Andreas Bathe, Bernd Helfert, Henning Böttcher
  • Nicotine receptor ligands
    Publication number: 20030027810
    Abstract: The invention provides nicotine receptor agonists of formula I: 1
    Type: Application
    Filed: November 30, 2001
    Publication date: February 6, 2003
    Applicant: Regents of the University of Minnesota
    Inventor: S. Mbua Ngale Efange
  • Urotensin-II receptor antagonists
    Patent number: 6514970
    Abstract: The present invention relates to pyrrolidiones, pharmaceutical compostions containing them and their use as antagonist of urotensin II.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: February 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Steven David Knight, Gregory Lee Warren, Jian Jin, Katherine L. Widdowson, Richard McCulloch Keenan
  • Derivatives of benzofuran or benzodioxole
    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
  • Halogen substituted tetracyclic tetrahydrofuran derivatives
    Patent number: 6511976
    Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: January 28, 2003
    Assignee: Jannsen Pharmaceutica, N.V.
    Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui, Adolfo Díaz-Martinez
  • Glucose and lipid lowering compounds
    Patent number: 6509480
    Abstract: Provided are, among other things, lipid-lowering or glucose-lowering methods and compounds, particularly lipid-lowering or glucose-lowering compounds, with an A-B ring structure as follows: wherein the dotted line between carbons 5 and 6, the dotted line between carbon 4 and R2, and the dotted line between carbon 11 and R3 each independently represent an optional double bond from the respective numbered carbon to a linked carbon, and wherein X is hydroxy or, together with Y is oxy linking carbon 8 and carbon 12.
    Type: Grant
    Filed: October 23, 2001
    Date of Patent: January 21, 2003
    Assignee: Alteon, Inc.
    Inventors: Dilip R. Wagle, Sheng Ding Fang, Ihor Terleckyj, John Resek, John J. Egan