Dibenzofurans (including Hydrogenated) Patents (Class 549/460)
  • Publication number: 20090069408
    Abstract: This invention is directed to, for example, compounds of formula (I): wherein n, m, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.
    Type: Application
    Filed: March 7, 2008
    Publication date: March 12, 2009
    Applicant: XENON PHARMACEUTICALS INC.
    Inventors: Mikhail Chafeev, Nagasree Chakka, Jean-Jacques Cadieux, Jianmin Fu, Rajender Kamboj, Vishnumurthy Kodumuru, Jonathan Langille, Shifeng Liu, Jianyu Sun, Serguei Sviridov, Zaihui Zhang
  • Patent number: 7498356
    Abstract: Disclosed are compound and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or hyperglycemia. Compound of the invention include inhibitors of protein tyrosine phosphatase, in particular protein tyrosine phosphatase-1B (PTP-1B), that are useful in the treatment of diabetes and other PTP mediated diseases, such as cancer, neurodegenerative diseases and the like. Also disclosed are pharmaceutical compositions comprising aforementioned conditions using such compounds.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: March 3, 2009
    Assignee: The Institutes for Pharmaceutical Discovery LLC
    Inventors: Darren Whitehouse, Shaojing Hu, Michael C. Van Zandt, Garrett Parker
  • Publication number: 20090054376
    Abstract: The present invention relates to novel benzofuran compounds, to pharmaceutical compositions that include such compounds, and to methods of use thereof. Certain compounds of the invention share some pharmacological properties with cannabinoids and have a common wide range of beneficial therapeutic indications. In particular, compounds of the invention are useful as analgesic, neuroprotective, immunomodulatory and anti-inflammatory agents.
    Type: Application
    Filed: May 31, 2006
    Publication date: February 26, 2009
    Inventors: Avihai Yacovan, Flavio Grynszpan, Alexander Aizikovich, Marcus Stephen Brody, Avi Bar-Joseph, Sigal Meilin
  • Patent number: 7491245
    Abstract: Compositions for the oxidative dyeing of keratin fibers, comprising a medium suitable for dyeing and one or more tricyclic fused 6-5-6 heteroaromatic keratin dyeing compounds having one heteroatom. A method for oxidative dyeing of keratin fibers, comprising applying such compositions in the presence of an oxidizing agent, for a period sufficient to develop the desired coloration.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: February 17, 2009
    Assignee: The Procter & Gamble Company
    Inventors: Robert Wayne Glenn, Jr., Anthony McMeekin, Mu'Ill Lim, John Michael Gardlik, Stevan David Jones, Bryan Patrick Murphy
  • Publication number: 20090036501
    Abstract: 2-cyclopenten-1-one oxime derivatives represented by Formula (I), or pharmaceutically acceptable salts thereof inhibit the production of TNF-? or PDE4, and therefore show therapeutic effect in inflammatory or immunological disorders mediated through TNF-? or PDE4.
    Type: Application
    Filed: November 30, 2005
    Publication date: February 5, 2009
    Applicant: AmorePacific Corporation
    Inventors: Yeonjoon Kim, Sun-Young Kim, Jung Sun Hwang, Kyoung Min Lim, Miyoung Park, Hyun Ju Koh, Sa-yong Hong, Song Seok Shin, Jin Kyu Choi, Joo Hyun Moh, Chin Chung, Byoung Young Woo, Sung II Kim
  • Publication number: 20090033210
    Abstract: To provide a novel fluoranthene derivative and an organic light emitting device having the fluoranthene derivative.
    Type: Application
    Filed: April 19, 2007
    Publication date: February 5, 2009
    Applicant: CANON KABUSHIKI KAISHA
    Inventors: Akihito Saitoh, Keiji Okinaka, Satoshi Igawa, Jun Kamatani, Naoki Yamada, Masashi Hashimoto, Masanori Muratsubaki, Takao Takiguchi, Akihiro Senoo, Shinjiro Okada, Minako Nakasu
  • Publication number: 20090030202
    Abstract: A material for organic electroluminescence devices for use as a host material in combination with at least one phosphorescent metal complex, which comprises a compound having a specific heterocyclic structure, is described. Also described is an organic electroluminescence device having an anode, a cathode and an organic thin film layer having one or more layers. The organic thin film layer is interposed between the anode and cathode and has a light emitting layer containing a host material in combination with at least one phosphorescent metal complex. At least one layer of the organic thin film layer contains the material for organic electroluminescence devices. The material for organic electroluminescence devices provides an organic electroluminescence device which has a high emitting efficiency, causes little pixel defects, is excellent in heat resistance, and show a long lifetime.
    Type: Application
    Filed: July 10, 2007
    Publication date: January 29, 2009
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
  • Publication number: 20080315754
    Abstract: Provided are a novel anthracene derivative of a specific structure in which benzofuran or benzothiophene is bonded to anthracene through an arylene group, a material for an organic electroluminescence device and a light emitting material for an organic electroluminescence device each containing the anthracene derivative, and an organic electroluminescence device including an organic thin film layer formed of one or plural layers including at least a light emitting layer, the organic thin film layer being interposed between a cathode and an anode, in which at least one layer of the organic thin film layer contains the anthracene derivative alone or as a component of a mixture. The organic electroluminescence device has high luminous efficiency and is capable of emitting light with a long lifetime, and the device can be realized by the anthracene derivative.
    Type: Application
    Filed: May 21, 2008
    Publication date: December 25, 2008
    Applicants: Idemitsu Kosan Co., Ltd., Sony Corporation
    Inventors: Masahiro KAWAMURA, Takashi Obikawa, Shigeyuki Matsunami, Ichinori Takada, Yasunori Kijima
  • Publication number: 20080220285
    Abstract: The present invention relates to the improvement of organic electroluminescent devices, in particular blue-emitting devices, by using compounds of the formula (1) as dopants in the emitting layer.
    Type: Application
    Filed: April 21, 2006
    Publication date: September 11, 2008
    Applicant: Merck Patent GmbH
    Inventors: Horst Vestweber, Holger Heil, Philipp Stoessel, Arne Buesing, Amir Hossain Parham, Rocco Fortte
  • Patent number: 7417157
    Abstract: Disclosed are hexahydrodibenzofuran compounds of formula I, the preparation thereof, the use thereof as components in liquid-crystalline media, and to electro-optical display elements which contain the liquid-crystalline media according to the invention.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: August 26, 2008
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer
  • Publication number: 20080188645
    Abstract: Inventors have developed a chromophore (nitrodibenzylfuranyl, or NBDF) for ultra efficient uncaging of a caged substrate (e.g., an organic molecule such as, for example, an amino acid, a biological molecules, such as, for example, second messengers inside cells). Photolysis of a NBDF derivative of EGTA (i.e. caged calcium) is about 50 times more efficient than others calcium cages (the quantum yield of photolysis is 0.6 and the extinction coefficient is 18,400. NDBF-EGTA has a 2-photon cross section of about 0.3-0.6 GM).
    Type: Application
    Filed: April 12, 2006
    Publication date: August 7, 2008
    Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of Medicine
    Inventors: Graham Ellis-Davies, Atsuya Momotake
  • Publication number: 20080152950
    Abstract: An anthracene derivative and an organic electroluminescent device using the same are provided. More specifically, provided are an anthracene derivative represented by Formula 1: wherein each R1 is aryl; and each R2 is independently C6-C20 aryl or C3-C19 heteroaryl, which are unsubstituted or substituted with one or more substituents selected from the group consisting of C1-C10 alkyl, C1-C10 alkoxy, cyano, C1-C10 alkylamino, C1-C10 alkylsilyl, halogen, C6-C10 aryl, C6-C10 aryloxy, C6-C10 arylamino, C6-C10 arylsilyl, C3-C19 heteroaryl and hydrogen; and an organic electroluminescent device using the same. The present invention can provide an organic electroluminescent device having excellent power and luminance efficiencies in conjunction with a long service life.
    Type: Application
    Filed: November 30, 2007
    Publication date: June 26, 2008
    Applicant: SFC CO., LTD.
    Inventors: Jong-Tae JE, Sug-Kwang Hwang, Sung-Hoon Kim, Seung-Hyuck Choi, Seon-Keun Yoo
  • Publication number: 20080111478
    Abstract: Provided are an anthracene derivative compound represented by Formula 1 below and an organic light-emitting device using the same: wherein Ar1 and Ar2 are each independently aromatic groups, R1 and R2 are each independently substituent groups, and X is a heteroatom or substituted heteroatom. The use of the anthracene derivative compound enables to produce an organic light-emitting device with better driving voltage, brightness, efficiency, and color purity.
    Type: Application
    Filed: August 3, 2007
    Publication date: May 15, 2008
    Applicant: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Yi-yeol LYU, Eun-sil HAN, Young-hun BYUN, Myeong-suk KIM, Dong-woo SHIN, Byoung-ki CHOI, O-hyun KWON, Woon-jung PAEK
  • Publication number: 20080100207
    Abstract: Provided are a cyclopentaphenanthrene-based compound and an organoelectroluminescent device employing the same. The cyclopentaphenanthrene-based compound is easy to prepare and excellent in solubility, color purity, color stability, and thermal stability. The cyclopentaphenanthrene-based compound is useful as a material for forming an organic layer, in particular, an emitting layer, in an organoelectroluminescent device, and as an organic dye or an electronic material such as a nonlinear optical material.
    Type: Application
    Filed: July 18, 2007
    Publication date: May 1, 2008
    Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son
  • Patent number: 7358364
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.
    Type: Grant
    Filed: April 14, 2004
    Date of Patent: April 15, 2008
    Assignee: The Institute for Pharmaceutical Discovery LLC
    Inventors: Michael C. Van Zandt, Darren Whitehouse, Kerry Combs, Shaojing Hu
  • Patent number: 7288543
    Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed
    Type: Grant
    Filed: March 8, 2005
    Date of Patent: October 30, 2007
    Assignee: Eli Lilly and Company
    Inventors: Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
  • Publication number: 20070247585
    Abstract: Disclosed are hexahydrodibenzofuran compounds of formula I, the preparation thereof, the use thereof as components in liquid-crystalline media, and to electro-optical display elements which contain the liquid-crystalline media according to the invention.
    Type: Application
    Filed: April 24, 2007
    Publication date: October 25, 2007
    Inventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer
  • Publication number: 20070224446
    Abstract: A material for organic electroluminescence device with specific structure. An an organic electroluminescence device comprising a cathode, an anode and an organic thin film layer which is sandwiched between the cathode and the anode and comprises at least one layer, wherein at least one layer in the organic thin film layer contains a material for the organic electroluminescence device described above. An organic electroluminescence device with excellent efficiency of light emission, without pixel defects, which is superior in heat resistance and prolonged lifetime is obtained.
    Type: Application
    Filed: March 30, 2006
    Publication date: September 27, 2007
    Applicant: Idemitsu Kosan Co., Ltd.
    Inventors: Yuki Nakano, Toshihiro Iwakuma, Masahide Matsuura, Hidetsugu Ikeda
  • Patent number: 7244516
    Abstract: An organic electroluminescence device including an organic layer having a light emission region and being disposed between an anode and a cathode is provided. The organic layer contains, as an organic light-emitting material, a compound represented by the following formula (1): wherein each of R1 to R26 represents a substituents, such as a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, a nitro group, an amino group, a cyano group, an alkyl group, an alkenyl group, a cycloalkyl group, an alkoxy group, an alkylthio group, a silyl group, an alkylsilyl group, a siloxanyl group, an aralkyl group, an aromatic hydrocarbon group, an aromatic heterocyclic group, an ester group, an aryloxy group, a formyl group, an alkoxycarbonyl group, and a carboxyl group, and n1 is a numeric value from 1 to 3.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: July 17, 2007
    Assignee: Sony Corporation
    Inventors: Yukinari Sakamoto, Mari Ichimura, Mitsuhiro Kashiwabara, Shinichiro Tamura
  • Patent number: 7196089
    Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): ?wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.
    Type: Grant
    Filed: January 29, 2004
    Date of Patent: March 27, 2007
    Assignee: Asterand UK Limited
    Inventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
  • Patent number: 7186752
    Abstract: N-(imino)amines and their preparation and their use as NO synthase inhibitors and selective or non-selective traps for a reactive oxygen species.
    Type: Grant
    Filed: April 26, 2005
    Date of Patent: March 6, 2007
    Assignee: SCRAS
    Inventors: Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
  • Patent number: 7119214
    Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, Y, R1 and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.
    Type: Grant
    Filed: April 12, 2005
    Date of Patent: October 10, 2006
    Assignee: Cephalon France
    Inventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
  • Patent number: 7026478
    Abstract: A process for the production of compounds Ar—R1 by means of a cross-coupling reaction of an organometallic reagent R1-M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or several iron salts or iron complexes as catalysts or pre-catalysts, present homogeneously or heterogeneously in the reaction mixture. This new invention exhibits substantial advantages over established cross coupling methodology using palladium- or nickel complexes as the catalysts. Most notable aspects are the fact that (i) expensive and/or toxic nobel metal catalysts are replaced by cheap, stable, commercially available and toxicologically benign iron salts or iron complexes as the catalysts or pre-catalysts, (ii) commercially attractive aryl chlorides as well as various aryl sulfonates can be used as starting materials, (iii) the reaction can be performed under “ligand-free” conditons, and (iv) the reaction times are usually very short.
    Type: Grant
    Filed: May 10, 2002
    Date of Patent: April 11, 2006
    Assignee: Studiengesellschaft Kohle mbH
    Inventors: Alois Fürstner, Andreas Leitner, María Méndez
  • Patent number: 6864254
    Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: March 8, 2005
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
  • Patent number: 6800656
    Abstract: The present invention provides a compound of the formula and pharmaceutically acceptable salts having useful antiviral activity against viruses of the herpes family. Wherein: X=O, (CH2)m, S, SO, SO2, NH, NR8; Y=O, (CH2)m, S, SO, SO2, NH, NR8 or a chemical bond; Z=NH, O, NR8, S, SO, SO2; The remaining substituents are described in the specification.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: October 5, 2004
    Assignee: Warner Lambert Company
    Inventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
  • Patent number: 6720431
    Abstract: Sample processing methods that utilize a graphitised carbon matrix are useful for determining the relative amounts polyhalogenated biphenyls (PHBs), polyhalogenated dibenzofurans (PHDFs), and polyhalogenated dibenzo-p-dioxins (PHDDs) in a mixture of polyhalogenated diaromatic hydrocarbons (PHDHs). The methods are particularly useful when used in conjunction with cell-based assays for determining the toxicity of PHDH compounds.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: April 13, 2004
    Assignee: Xenobiotic Detection Systems International, Inc.
    Inventors: Michael D. Chu, George C. Clark
  • Patent number: 6710089
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: March 23, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6696573
    Abstract: A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.
    Type: Grant
    Filed: March 4, 2002
    Date of Patent: February 24, 2004
    Assignee: Asahi Kasei Kabushiki Kaisha
    Inventors: Koki Matsubara, Naoyuki Ishii, Masami Ogawa
  • Publication number: 20040034052
    Abstract: Compounds of formula (I), in which the groups are as definite in the description, useful as medicaments endowed with cytotoxic and antiangiogenic activity, are described.
    Type: Application
    Filed: August 28, 2003
    Publication date: February 19, 2004
    Inventors: Gisuseppe. Giannini, Mauro Marzi, Maria Ornella Tinti, Clauido Pisano
  • Publication number: 20030229083
    Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1
    Type: Application
    Filed: November 27, 2002
    Publication date: December 11, 2003
    Applicant: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Bhuniya Debnath, Saibal Kumar Das, Gurram Ranga Madhavan, Javed Iqbal, Ranjan Chakrabarti, Reeba Kannimel Vikramadithyan
  • Publication number: 20030229102
    Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof which is useful for the treatment of conditions associated with glutamate hypofunction, such as psychiatric and neurological disorders 1
    Type: Application
    Filed: November 15, 2002
    Publication date: December 11, 2003
    Inventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Publication number: 20030225289
    Abstract: A process for the preparation of tricyclic amino alcohol derivatives including 2-[N-[2-(9H-carbazol-2-yloxy)ethyl]]amino-1-[(3-methylsulfonylamino)phenyl]ethanol useful in the treatment of diabetes, obesity, hyperlipidemia and so on; and intermediates as represented by formula (5) or (6) or the like useful in the preparation, wherein R11 is hydrogen or the like; and *1 represents an asymmetric carbon atom. 2-Halo-1-(3-nitrophenyl)ethanone derivatives and 1-(3-nitrophenyl)oxirane derivatives, which are intermediates for the preparation of tricyclic amino alcohol derivatives, are easy of purification, and particularly optically active 1-(3-nitrophenyl)oxirane derivatives are effective in enhancing the optical purities of the final products.
    Type: Application
    Filed: June 11, 2003
    Publication date: December 4, 2003
    Applicant: ASAHI KASEI KABUSHIKI KAISHA
    Inventors: Koki Matsubara, Naoyuki Ishii, Masami Ogawa
  • Publication number: 20030220340
    Abstract: This invention provides novel compounds possessing antibacterial and/or antifungal and/or antitumor activity. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.
    Type: Application
    Filed: May 15, 2003
    Publication date: November 27, 2003
    Inventors: Christoher Don Roberts, Jesse Daniel Keicher, Mikail Hakan Gazginci, Mark Douglas Velligan
  • Patent number: 6653346
    Abstract: Cytoprotective compounds, many of which are benzofuran derivatives are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: November 25, 2003
    Assignee: Galileo Pharmaceuticals, Inc.
    Inventors: Bing Wang, Jian Chen
  • Publication number: 20030144526
    Abstract: A novel calcium receptor active compound having the formula is provided:
    Type: Application
    Filed: December 19, 2002
    Publication date: July 31, 2003
    Applicant: NPS Pharmaceuticals, Inc.
    Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
  • Patent number: 6495701
    Abstract: The present invention is directed to processes for the preparation of a compound useful for treating diabetes, obesity, hyperlipidemia and the like, which compound is represented by the formula (1): wherein R1 represents a lower alkyl group or a benzyl group; *1 represents an asymmetric carbon atom; R2 hydrogen atom, a halogen atom or a hydroxyl group; and A represents one of the following groups: wherein X represents NH, O or S; R6 represents a hydrogen atom, a hydroxyl group, an amino group or an acetylamino group; and *2 represents an asymmetric carbon atom when R6 is not a hydrogen atom, and to intermediates useful for the said processes. The processes of the present invention are convenient, practical preparing processes with low cost which comprise a small number of steps with good industrial work efficiency.
    Type: Grant
    Filed: September 26, 2001
    Date of Patent: December 17, 2002
    Assignee: Asahi Kasei Kabushiki Kaisha
    Inventors: Koki Matsubara, Hitoshi Kida
  • Patent number: 6448295
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 10, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • 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
  • Publication number: 20020077347
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: August 23, 2001
    Publication date: June 20, 2002
    Inventors: Gang Liu, Zhonghua Pei
  • Patent number: 6350885
    Abstract: Tricyclic heteroaromatic compounds and derivatives are described as well as methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A, collagenase-3, and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurysm, heart failure, left ventricular dilation, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, osteoporosis, renal disease, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Grant
    Filed: February 20, 2001
    Date of Patent: February 26, 2002
    Assignee: Warner-Lambert Company
    Inventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
  • Patent number: 6294674
    Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds. wherein Q is an un-natural amino acid. More particurlarly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthiritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.
    Type: Grant
    Filed: March 2, 1999
    Date of Patent: September 25, 2001
    Assignee: Warner-Lambert Company
    Inventors: Joseph Armand Picard, Drago Robert Sliskovic
  • Patent number: 6172104
    Abstract: Methods of treating Pneumocystis carinii pneumonia comprise administering a therapeutically effective amount of a dicationic dibenzofuran compound described by Formula (I). Methods of treating Pneumocystis carinii pneumonia also comprise administering a therapeutically effective amount of a dicationic dibenzothiophene compound described by Formula (II). Novel compounds are also disclosed, and are represented by the Formulae (I) and (II).
    Type: Grant
    Filed: June 24, 1999
    Date of Patent: January 9, 2001
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Richard R. Tidwell, James Edwin Hall
  • Patent number: 6172099
    Abstract: Compounds represented by general formula (I) or their salts, having &bgr;3-adrenoceptor agonism and being efficacious when employed in drugs for treating and preventing diabetes, obesity, hyperlipemia, etc. wherein R represents hydrogen or methyl; R1 represents hydrogen, halogeno, hydroxy, benzyloxy, amino or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4 ′ or nitro (wherein R3 represents hydrogen, methyl, SO2R5, formyl or CONHR6′; R5 represents lower alkyl, benzyl or NR4R4′; R4 and R4′ may be the same or different and each represents hydrogen, lower alkyl or benzyl; and R6′ represents hydrogen or lower alkyl); R6 represents hydrogen or lower alkyl; n is 1 or 2; X represents secondary nitrogen, oxygen or sulfur; and when n is 1, then one of R7 and R8 represents hydrogen while another represents hydrogen, amino, acetylamino or hydroxy, or when n is 2, then R8 represents hydrogen while R7 represents hydrogen, amino, acetylamino or hydroxy.
    Type: Grant
    Filed: March 27, 2000
    Date of Patent: January 9, 2001
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Shiro Miyoshi, Kohei Ogawa
  • Patent number: 6037479
    Abstract: Novel, chiral diarsine compounds, which are present in the (R)- or (S)- or (rac)-form, of the formula ##STR1## wherein R signifies an optionally substituted aryl from the group of phenyI, naphthyl, furyl and thienyl; C.sub.3-8 -cycloalkyl or C.sub.1-8 -alkyl;R.sup.1, R.sup.2, R.sup.3 each independently signify C.sub.1-8 -alkyl, C.sub.1-8 -alkoxy, aryloxy, F or Cl,R.sup.2 and R.sup.3 each independently also signify hydrogen orR.sup.1 and R.sup.2 together signify tetramethylene or a benzo or benzofuro system or dioxymethylene on the respective benzene ring; orR.sup.2 and R.sup.3 together signify dioxymethylene,and the manufacture of the diarsine compounds of formula I, as well as complexes of the compounds of formula I with Group VIII metal and their use for enantioselective reactions.
    Type: Grant
    Filed: June 26, 1998
    Date of Patent: March 14, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Emil Albin Broger, Marco Cereghetti, Frank Kienzle
  • Patent number: 6037361
    Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.
    Type: Grant
    Filed: March 9, 1998
    Date of Patent: March 14, 2000
    Assignee: Warner-Lambert Company
    Inventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
  • Patent number: 6020366
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2 include hydrogen, alkyl, substituted alkyl, halo, and arylalkyl; R.sub.3 is hydroxy, alkoxy, or hydroxyamino; X is O, S, or NOH; and R.sub.4 and R.sub.5 include hydrogen, alkyl, and aryl are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: February 1, 2000
    Assignee: Warner-Lambert Company
    Inventors: Joseph Armand Picard, Drago Robert Sliskovic
  • Patent number: 5942532
    Abstract: The invention relates to benzimidazole antibacterial compounds of the Formula I: ##STR1## as described herein, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: August 24, 1999
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
  • Patent number: 5935992
    Abstract: The invention provides substituted-2-amino-1,2,3,4-tetrahydrodibenzofurans and 2-aminocyclohepta?b!benzo-furans useful as 5-HT.sub.1F agonists.
    Type: Grant
    Filed: June 3, 1998
    Date of Patent: August 10, 1999
    Assignee: Eli Lilly and Company
    Inventors: Michael E. Flaugh, Anton D. Kiefer, Jr.
  • Patent number: 5869662
    Abstract: Benzopyran compounds represented by the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.
    Type: Grant
    Filed: July 17, 1997
    Date of Patent: February 9, 1999
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 5858995
    Abstract: This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.
    Type: Grant
    Filed: October 25, 1996
    Date of Patent: January 12, 1999
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshio Kawai, Hitoshi Yamazaki, Natsuko Kayakiri, Kousei Yoshihara, Takumi Yatabe, Teruo Oku