Dibenzofurans (including Hydrogenated) Patents (Class 549/460)
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Publication number: 20090069408Abstract: 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: ApplicationFiled: March 7, 2008Publication date: March 12, 2009Applicant: 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
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Patent number: 7498356Abstract: 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: GrantFiled: November 18, 2005Date of Patent: March 3, 2009Assignee: The Institutes for Pharmaceutical Discovery LLCInventors: Darren Whitehouse, Shaojing Hu, Michael C. Van Zandt, Garrett Parker
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Publication number: 20090054376Abstract: 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: ApplicationFiled: May 31, 2006Publication date: February 26, 2009Inventors: Avihai Yacovan, Flavio Grynszpan, Alexander Aizikovich, Marcus Stephen Brody, Avi Bar-Joseph, Sigal Meilin
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Patent number: 7491245Abstract: 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: GrantFiled: December 19, 2007Date of Patent: February 17, 2009Assignee: The Procter & Gamble CompanyInventors: Robert Wayne Glenn, Jr., Anthony McMeekin, Mu'Ill Lim, John Michael Gardlik, Stevan David Jones, Bryan Patrick Murphy
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Publication number: 20090036501Abstract: 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: ApplicationFiled: November 30, 2005Publication date: February 5, 2009Applicant: AmorePacific CorporationInventors: 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
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Publication number: 20090033210Abstract: To provide a novel fluoranthene derivative and an organic light emitting device having the fluoranthene derivative.Type: ApplicationFiled: April 19, 2007Publication date: February 5, 2009Applicant: CANON KABUSHIKI KAISHAInventors: Akihito Saitoh, Keiji Okinaka, Satoshi Igawa, Jun Kamatani, Naoki Yamada, Masashi Hashimoto, Masanori Muratsubaki, Takao Takiguchi, Akihiro Senoo, Shinjiro Okada, Minako Nakasu
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Publication number: 20090030202Abstract: 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: ApplicationFiled: July 10, 2007Publication date: January 29, 2009Applicant: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro Iwakuma, Jun Endo, Masaki Numata, Kenichi Fukuoka
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Publication number: 20080315754Abstract: 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: ApplicationFiled: May 21, 2008Publication date: December 25, 2008Applicants: Idemitsu Kosan Co., Ltd., Sony CorporationInventors: Masahiro KAWAMURA, Takashi Obikawa, Shigeyuki Matsunami, Ichinori Takada, Yasunori Kijima
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Publication number: 20080220285Abstract: 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: ApplicationFiled: April 21, 2006Publication date: September 11, 2008Applicant: Merck Patent GmbHInventors: Horst Vestweber, Holger Heil, Philipp Stoessel, Arne Buesing, Amir Hossain Parham, Rocco Fortte
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Patent number: 7417157Abstract: 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: GrantFiled: April 24, 2007Date of Patent: August 26, 2008Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer
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Publication number: 20080188645Abstract: 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: ApplicationFiled: April 12, 2006Publication date: August 7, 2008Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventors: Graham Ellis-Davies, Atsuya Momotake
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Publication number: 20080152950Abstract: 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: ApplicationFiled: November 30, 2007Publication date: June 26, 2008Applicant: SFC CO., LTD.Inventors: Jong-Tae JE, Sug-Kwang Hwang, Sung-Hoon Kim, Seung-Hyuck Choi, Seon-Keun Yoo
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Publication number: 20080111478Abstract: 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: ApplicationFiled: August 3, 2007Publication date: May 15, 2008Applicant: 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
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Publication number: 20080100207Abstract: 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: ApplicationFiled: July 18, 2007Publication date: May 1, 2008Inventors: Sang-Hoon Park, Yu-Jin Kim, Jhun-Mo Son
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Patent number: 7358364Abstract: 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: GrantFiled: April 14, 2004Date of Patent: April 15, 2008Assignee: The Institute for Pharmaceutical Discovery LLCInventors: Michael C. Van Zandt, Darren Whitehouse, Kerry Combs, Shaojing Hu
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Patent number: 7288543Abstract: 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 disclosedType: GrantFiled: March 8, 2005Date of Patent: October 30, 2007Assignee: Eli Lilly and CompanyInventors: Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
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Publication number: 20070247585Abstract: 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: ApplicationFiled: April 24, 2007Publication date: October 25, 2007Inventors: Axel Jansen, Andreas Taugerbeck, Melanie Klasen-Memmer
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Publication number: 20070224446Abstract: 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: ApplicationFiled: March 30, 2006Publication date: September 27, 2007Applicant: Idemitsu Kosan Co., Ltd.Inventors: Yuki Nakano, Toshihiro Iwakuma, Masahide Matsuura, Hidetsugu Ikeda
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Patent number: 7244516Abstract: 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: GrantFiled: May 28, 2004Date of Patent: July 17, 2007Assignee: Sony CorporationInventors: Yukinari Sakamoto, Mari Ichimura, Mitsuhiro Kashiwabara, Shinichiro Tamura
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Patent number: 7196089Abstract: 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: GrantFiled: January 29, 2004Date of Patent: March 27, 2007Assignee: Asterand UK LimitedInventors: 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
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Patent number: 7186752Abstract: 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: GrantFiled: April 26, 2005Date of Patent: March 6, 2007Assignee: SCRASInventors: Dennis Bigg, Pierre-Etienne Chabrier de Lassauniere, Serge Auvin, Jeremiah Harnett, Gérard Ulibarri
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Patent number: 7119214Abstract: 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: GrantFiled: April 12, 2005Date of Patent: October 10, 2006Assignee: Cephalon FranceInventors: Brigitte Lesur, Christophe Yue, Sophie Chasset, Olivier Renault
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Patent number: 7026478Abstract: 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: GrantFiled: May 10, 2002Date of Patent: April 11, 2006Assignee: Studiengesellschaft Kohle mbHInventors: Alois Fürstner, Andreas Leitner, María Méndez
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Patent number: 6864254Abstract: 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: GrantFiled: November 1, 2000Date of Patent: March 8, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masakazu Sato, Noriyuki Miyata, Takaaki Ishii, Yuko Kobayashi, Hideaki Amada
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Patent number: 6800656Abstract: 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: GrantFiled: July 5, 2002Date of Patent: October 5, 2004Assignee: Warner Lambert CompanyInventors: Richard John Booth, Vara Prasad Venkata Nagendra Josyula, Annette Lynn Meyer, Bruce Allan Steinbaugh
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Patent number: 6720431Abstract: 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: GrantFiled: June 1, 2001Date of Patent: April 13, 2004Assignee: Xenobiotic Detection Systems International, Inc.Inventors: Michael D. Chu, George C. Clark
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Patent number: 6710089Abstract: 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: GrantFiled: May 23, 2002Date of Patent: March 23, 2004Assignee: Pharmacia CorporationInventors: 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
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Patent number: 6696573Abstract: 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: GrantFiled: March 4, 2002Date of Patent: February 24, 2004Assignee: Asahi Kasei Kabushiki KaishaInventors: Koki Matsubara, Naoyuki Ishii, Masami Ogawa
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Publication number: 20040034052Abstract: 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: ApplicationFiled: August 28, 2003Publication date: February 19, 2004Inventors: Gisuseppe. Giannini, Mauro Marzi, Maria Ornella Tinti, Clauido Pisano
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Publication number: 20030229083Abstract: The present invention relates to novel antidiabetic, hypolipidemic, antiobesity and hypocholesterolemic compounds of formula (I), 1Type: ApplicationFiled: November 27, 2002Publication date: December 11, 2003Applicant: DR. REDDY'S LABORATORIES LIMITEDInventors: Bhuniya Debnath, Saibal Kumar Das, Gurram Ranga Madhavan, Javed Iqbal, Ranjan Chakrabarti, Reeba Kannimel Vikramadithyan
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Publication number: 20030229102Abstract: 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 1Type: ApplicationFiled: November 15, 2002Publication date: December 11, 2003Inventors: James Allen Knobelsdorf, Timothy Alan Shepherd, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20030225289Abstract: 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: ApplicationFiled: June 11, 2003Publication date: December 4, 2003Applicant: ASAHI KASEI KABUSHIKI KAISHAInventors: Koki Matsubara, Naoyuki Ishii, Masami Ogawa
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Publication number: 20030220340Abstract: 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: ApplicationFiled: May 15, 2003Publication date: November 27, 2003Inventors: Christoher Don Roberts, Jesse Daniel Keicher, Mikail Hakan Gazginci, Mark Douglas Velligan
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Patent number: 6653346Abstract: 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: GrantFiled: February 6, 2003Date of Patent: November 25, 2003Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Jian Chen
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Publication number: 20030144526Abstract: A novel calcium receptor active compound having the formula is provided:Type: ApplicationFiled: December 19, 2002Publication date: July 31, 2003Applicant: NPS Pharmaceuticals, Inc.Inventors: Teruyuki Sakai, Atsuya Takami, Rika Nagao
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Patent number: 6495701Abstract: 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: GrantFiled: September 26, 2001Date of Patent: December 17, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Koki Matsubara, Hitoshi Kida
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Patent number: 6448295Abstract: 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: GrantFiled: November 14, 2001Date of Patent: September 10, 2002Assignee: 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
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Publication number: 20020099223Abstract: 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: ApplicationFiled: January 22, 2002Publication date: July 25, 2002Inventors: Michelangelo Scalone, Thomas Albert Zeibig
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Publication number: 20020077347Abstract: Compounds of formula (I) 1Type: ApplicationFiled: August 23, 2001Publication date: June 20, 2002Inventors: Gang Liu, Zhonghua Pei
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Patent number: 6350885Abstract: 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: GrantFiled: February 20, 2001Date of Patent: February 26, 2002Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6294674Abstract: 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: GrantFiled: March 2, 1999Date of Patent: September 25, 2001Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6172104Abstract: 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: GrantFiled: June 24, 1999Date of Patent: January 9, 2001Assignee: The University of North Carolina at Chapel HillInventors: Richard R. Tidwell, James Edwin Hall
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Patent number: 6172099Abstract: 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: GrantFiled: March 27, 2000Date of Patent: January 9, 2001Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Shiro Miyoshi, Kohei Ogawa
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Patent number: 6037479Abstract: 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: GrantFiled: June 26, 1998Date of Patent: March 14, 2000Assignee: Hoffman-La Roche Inc.Inventors: Emil Albin Broger, Marco Cereghetti, Frank Kienzle
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Patent number: 6037361Abstract: 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: GrantFiled: March 9, 1998Date of Patent: March 14, 2000Assignee: Warner-Lambert CompanyInventors: Bruce David Roth, Patrick Michael O'Brien, Drago Robert Sliskovic
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Patent number: 6020366Abstract: 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: GrantFiled: October 27, 1998Date of Patent: February 1, 2000Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 5942532Abstract: 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: GrantFiled: September 5, 1997Date of Patent: August 24, 1999Assignee: Ortho Pharmaceutical CorporationInventors: Kwasi Adomako Ohemeng, Van Nhatton Nguyen
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Patent number: 5935992Abstract: 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: GrantFiled: June 3, 1998Date of Patent: August 10, 1999Assignee: Eli Lilly and CompanyInventors: Michael E. Flaugh, Anton D. Kiefer, Jr.
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Patent number: 5869662Abstract: 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: GrantFiled: July 17, 1997Date of Patent: February 9, 1999Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5858995Abstract: 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: GrantFiled: October 25, 1996Date of Patent: January 12, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Kawai, Hitoshi Yamazaki, Natsuko Kayakiri, Kousei Yoshihara, Takumi Yatabe, Teruo Oku