Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/241)
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Patent number: 7893275Abstract: The present application provides polycyclic ketone compounds that have a quarternary asymmetric carbon center and conform to Formula (I): Also provided is a stereoselective method for synthesizing the polycyclic ketone compounds.Type: GrantFiled: March 10, 2005Date of Patent: February 22, 2011Assignee: Japan Science and Technology AgencyInventor: Keisuke Suzuki
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Publication number: 20110039902Abstract: A process for preparing a crystalline form compound of 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one is described, comprising the step of reacting 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydroben-zo[d]isoxazol-4-one with oxalic acid in one or more solvents, wherein at least one solvent is a solvent having a carbon atom number of from 3 to 6, said solvent being non-halogenated and having a dielectric constant ? within the range from 4 to 25. The process of the invention enables a co-crystal comprising 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one and oxalic acid to be obtained.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Applicant: ABIOGEN PHARMA S.P.A.Inventors: Fabio Neggiani, Elio Napolitano, Simone Basagni, Barbara Politi
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Publication number: 20110039901Abstract: A process for preparing a crystalline form compound of 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one is described, comprising the step of reacting 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one and fumaric acid in one or more solvents, wherein at least one solvent is a solvent having a carbon atom number of from 3 to 6, said solvent being non-halogenated and having a dielectric constant ? in the range from 4 to 25. The process of the invention enables to obtain a co-crystal comprising 3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one and fumaric acid.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Inventors: Simone Basagni, Fabio Neggiani, Barbara Politi, Elio Napolitano
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Publication number: 20110009371Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.Type: ApplicationFiled: May 12, 2010Publication date: January 13, 2011Inventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel
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Publication number: 20100316607Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 15, 2010Publication date: December 16, 2010Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
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Publication number: 20100311778Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 16, 2008Publication date: December 9, 2010Inventors: V S Prasadarao Lingam, Abraham Thomas, Laxmikant Atmaram Gharat, Deepak Vitthal Ukirde, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Patent number: 7846925Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.Type: GrantFiled: July 10, 2003Date of Patent: December 7, 2010Assignee: Merck Serono SAInventors: Thomas Rueckle, Xuliang Jiang, Pascale Gaillard, Dennis Church, Tania Grippi Vallotton
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Publication number: 20100297250Abstract: 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate.Type: ApplicationFiled: November 21, 2008Publication date: November 25, 2010Applicant: University of Georgia Research Foundation, Inc.Inventors: Geert-Jan Boons, Jun Guo, Xinghai Ning, Margaretha Wolfert
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Patent number: 7820664Abstract: This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: January 18, 2008Date of Patent: October 26, 2010Assignee: Bayer Schering Pharma AGInventors: Jean-Michel Vernier, Andreas Maderna, Yung-hyo Koh, Zhi Hong
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Publication number: 20100267945Abstract: A compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, where R1 is optionally substituted lower alkyl, Y is —S(O)2—, R2 is hydrogen or optionally substituted lower alkyl, R7 is hydrogen or optionally substituted lower alkyl, X is a group of the formula: where R5 and R6 are each independently hydrogen, a group of the formula: is optionally substituted cycloalkylene, p is 0, and q is 1 or 2, Z is optionally substituted carbocyclyl or optionally substituted heterocyclyl, and provided that a compound wherein Z is fused heterocyclyl consisting of three rings or optionally substituted pyrimidinyl is excluded.Type: ApplicationFiled: June 25, 2010Publication date: October 21, 2010Applicant: Shionogi & Co., Ltd.Inventors: Takayuki Okuno, Naoki Kouyama, Masahiro Sakagami
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Publication number: 20100255005Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: May 28, 2008Publication date: October 7, 2010Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
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Patent number: 7807842Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.Type: GrantFiled: May 20, 2005Date of Patent: October 5, 2010Assignee: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel
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Publication number: 20100249179Abstract: The present invention provides novel isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.Type: ApplicationFiled: June 13, 2008Publication date: September 30, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: David Norman Deaton, Frank Navas, III, Paul Kenneth Spearing
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Publication number: 20100247534Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein.Type: ApplicationFiled: June 10, 2010Publication date: September 30, 2010Inventors: James A. Johnson, John Lloyd, Alexander Kover
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Publication number: 20100240891Abstract: Pharmaceutical agents characterized by containing benzophenone derivatives represented by the general formula: wherein the each substituent is as defined in the specification, or salts thereof have suppressive effect on RANKL production, suppressive effect on OPG reduction and inhibitory effects on differentiation/activation of osteoclasts, and are extremely useful for treating, for example therapy and/or prevention, of various diseases in which differentiation/activation of osteoclast are involved, such as osteoporosis.Type: ApplicationFiled: September 28, 2007Publication date: September 23, 2010Applicant: TOYAMA CHEMICAL CO., LTD.Inventors: Yukihiko Aikawa, Kimiko Morimoto, Mari Yamamoto, Shunichi Shiozawa
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Patent number: 7790722Abstract: The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain. Further, this invention relates to novel compounds for example, indoles, 1H-indazoles, 1,2-benzisoxazoles, and 1,2-benzisothiazoles, which act as ligands for the ?7 nAChR subtype, methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.Type: GrantFiled: May 29, 2008Date of Patent: September 7, 2010Assignee: Memory Pharmaceuticals CorporationInventors: Wenge Xie, Brian Herbert, Jianguo Ma, Truc Minh Nguyen, Richard Schumacher, Carla Maria Gauss, Ashok Tehim
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Patent number: 7772285Abstract: A benzophenone derivative represented by the following formula: wherein R1 represents, for example, an optionally substituted heterocyclic group, or a substituted phenyl group; Z represents, for example, an alkylene group; R2 represents, for example, a carboxyl group optionally protected with alkyl; R3 represents, for example, an optionally protected hydroxyl group; R4 represents, for example, an optionally substituted cycloalkyloxy group; and R5 represents, for example, a hydrogen atom, or a salt thereof has anti-arthritic activity, inhibits bone destruction caused by arthritis, and provides high safety and excellent pharmacokinetics and thus is useful as therapeutic agent for arthritis. These compounds have inhibitory effect on AP-1 activity and are useful as preventive or therapeutic agent for diseases in which excessive expression of AP-1 is involved.Type: GrantFiled: November 13, 2002Date of Patent: August 10, 2010Assignee: Toyama Chemical Co., Ltd.Inventors: Hisaaki Chaki, Hironori Kotsubo, Tadashi Tanaka, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Patent number: 7772232Abstract: A compound of formula I wherein m, n, A, B, D, E, G, H, Y, R1, R2, R3, R4, R5, and R8, are described herein. Said compounds being useful as inhibitors of potassium channel function and in the treatment of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.Type: GrantFiled: April 13, 2005Date of Patent: August 10, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, John Lloyd
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Publication number: 20100184992Abstract: C-nitroso compound capable of releasing neutral nitric oxide is made stable by forming a Diels Alder adduct thereof which is functionalized at the Diels-Alder double bond to impart the stability. Treatment of the stabilized adduct with agent that removes functionalization and regenerates Diels Alder double bond triggers delivery of neutral nitric oxide via retro Diels-Alder reaction and homolytic scission.Type: ApplicationFiled: April 16, 2008Publication date: July 22, 2010Applicant: Duke UniversityInventors: Eric J. Toone, Harinath Chakrapani
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Patent number: 7750026Abstract: Compounds of formula (I): are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38.Type: GrantFiled: January 27, 2005Date of Patent: July 6, 2010Assignee: GlaxoSmithKline LLCInventors: Vipulkumar Kantibhai Patel, Stephen Swanson
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Publication number: 20100168192Abstract: This invention relates to novel benzisoxazole derivatives that are found to be potent modulators of potassium channels and, as such, are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to the modulation of potassium channels e.g. a respiratory disease, epilepsy or convulsions. X represents a substituent selected from the group consisting of CO—NR?R?, CO—O—R?, CO—NH—S, CO—NH—SO2R??, CO—NH—C?N, SO2—NR?R?, 2,3-dihydro-1-H-tetrazol-5-yl and [1,2,4]oxadiazolidin-5-one; wherein R? and R?, independently of each other, represent hydrogen or alkyl or phenyl; and R?? represents alkyl, cycloalkyl, haloalkyl or phenyl, which phenyl may optionally be substituted one or more times with substituents selected from halo, trifluoromethyl, trifluoromethoxy, cyano and nitro.Type: ApplicationFiled: May 22, 2008Publication date: July 1, 2010Applicant: NeuroSearch A/SInventors: Antonio Nardi, Claus Mathiesen, Jeppe Kejser Christensen
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Patent number: 7745471Abstract: Derivatives of 1,2-benzisoxazole-3-methanesulfonic acid, which are non-hygroscopic and non-hydrated and their use as intermediates from the preparation of zonisamide are disclosed. Further disclosed are processes of preparing zonisamide from these 1,2-benzisoxazole-3-methanesulfonic acid derivatives, processes of preparing exemplary 1,2-benzisoxazole-3-methanesulfonic acid derivatives and crystalline forms of exemplary 2-benzisoxazole-3-methanesulfonic acid derivatives. A novel process of preparing zonisamide is also disclosed.Type: GrantFiled: June 16, 2005Date of Patent: June 29, 2010Assignee: Chemagis Ltd.Inventors: Vladimir Naddaka, Eyal Klopfer, Shady Saeed, Oded Arad, Joseph Kaspi
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Publication number: 20100152246Abstract: The present invention relates to 5-oxoisoxazole derivatives of the formula I, the pharmaceutically usable salts thereof and the use thereof as medicinal substances.Type: ApplicationFiled: October 5, 2009Publication date: June 17, 2010Applicant: SANOFI-AVENTISInventors: Stefan PETRY, Manfred SEIDEL, Gerhard ZOLLER, Gunter MÜLLER, Karl-Heinz BARINGHAUS, Hubert HEUER
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Publication number: 20100105671Abstract: The present invention is directed to a compound represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (A) are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula (A) and its therapeutic use.Type: ApplicationFiled: August 7, 2009Publication date: April 29, 2010Inventors: Jingye Zhou, Xiao-Yi Xiao, Louis Plamondon, Diana Katharine Hunt, Roger B. Clark, Robert B. Zahler
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Publication number: 20100099682Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.Type: ApplicationFiled: September 17, 2009Publication date: April 22, 2010Inventors: Ralf GLATTHAR, Thomas J. Troxler, Thomas Zoller, Joachim Nozulak
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100093788Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.Type: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Senath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Patent number: 7696238Abstract: Substituted benzo[d]isoxazol-3-yl amine compounds corresponding to formula I which exhibit an strong affinity to the KCNQ2/3 K+ channel, and which are suitable for treating or inhibiting pain and/or disorders or disease states that are at least partly mediated by the KCNQ2/3 K+ channel.Type: GrantFiled: November 16, 2007Date of Patent: April 13, 2010Assignee: Gruenenthal GmbHInventors: Beatrix Merla, Robert Frank, Gregor Bahrenberg, Wolfgang Schroeder, Saskia Zemolka
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Patent number: 7696230Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A-(B)b0-(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R-T1-, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from aminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: February 14, 2007Date of Patent: April 13, 2010Assignee: Nicox S.A.Inventors: Piero Del Soldato, Ennio Ongini
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Publication number: 20100069451Abstract: The present invention relates to oxalate salt of the compound of formula (I) in all its stereochemical configurations, a process for its preparation and its use in treating mood disorders, disorders of anxiety, depression and convulsive conditions, in the improvement of learning ability, in the reversal of amnesia, in resolving the abstinence syndrome from drugs and drugs of abuse. Preferably, the invention concerns oxalate salt of rel-(3R,3aS,7aS)-3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one.Type: ApplicationFiled: October 31, 2007Publication date: March 18, 2010Applicant: ABIOGEN PHARMA S.P.AInventors: Fabio Neggiani, Laura Dini
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Publication number: 20100069450Abstract: The present invention relates to fumarate salt of the compound of formula (I) in all its stereochemical configurations, a process for its preparation and its use in treating mood disorders, disorders of anxiety, depression and convulsive conditions, in the improvement of learning ability, in the reversal of amnesia, in resolving the abstinence syndrome from drugs and drugs of abuse. Preferably, the invention concerns fumarate salt of rel-(3R,3aS,7aS)-3-benzyl-2-methyl-2,3,3a,4,5,6,7,7a-octahydrobenzo[d]isoxazol-4-one.Type: ApplicationFiled: October 31, 2007Publication date: March 18, 2010Applicant: ABIOGEN PHARMA S.P.AInventors: Fabio Neggiani, Laura Dini
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Publication number: 20100029949Abstract: A compound having the following formula (II) or its salt is used as an activator for PPAR ?: [in which W3 is a nitrogen atom or CH; Z1 is an oxygen atom or a sulfur atom; each of R11 and R12 is a hydrogen atom, a halogen atom, a C1-C8 alkyl group, a C1-C8 alkoxy group, a C1-C8 alkyl group having a halogen substituent, or the like; each of R13 and R14 is a hydrogen atom or a C1-C8 alkyl group; A1 is pyrazole or thiophene which may have a substituent; and m is an integer of 2 to 4].Type: ApplicationFiled: July 4, 2006Publication date: February 4, 2010Inventors: Shogo Sakuma, Nobutaka Mochiduki, Rie Takahashi, Toshitake Hirai, Tomio Yamakawa, Seiichiro Masui
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Publication number: 20100022530Abstract: Compounds of the formula (I) in which A1, A2, R1, X1, X2, X3, Y, R2, Cy and n have meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 22, 2007Publication date: January 28, 2010Applicant: MERCK PATENT GMBHInventors: Kai Schiemann, Dirk Finsinger, Frank Zenke
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Patent number: 7645885Abstract: The invention provides non-steroidal ligands for the androgen receptor, methods for making non-steroidal ligands of the androgen receptor, compositions of non-steroidal ligands of the androgen receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the androgen receptor for treating or preventing diseases (e.g., prostate cancer) associated with androgen binding to the androgen receptor.Type: GrantFiled: August 28, 2006Date of Patent: January 12, 2010Assignee: The Regents of the University of CaliforniaInventors: Thomas S. Scanlan, Dmitry V. Kadnikov
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Patent number: 7642276Abstract: Compounds of formula (I): wherein A is a 5-membered heteroaryl ring are inhibitors of p38 kinase and are useful in the treatment of conditions or disease states mediated by p38 kinase activity or mediated by cytokines produced by the activity of p38, such as rheumatoid arthritis.Type: GrantFiled: July 30, 2003Date of Patent: January 5, 2010Assignee: SmithKline Beecham CorporationInventors: Richard Martyn Angell, Ian Robert Baldwin, Paul Bamborough, Nigel Marc Deboeck, Timothy Longstaff, Stephen Swanson
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Patent number: 7629372Abstract: A class of compounds having Formula I and pharmaceutically acceptable salts thereof are useful as therapeutic compounds, particularly in the treatment of hyperlipidemia, hypercholesterolemia, dyslipidemia, and other lipid disorders, and in delaying the onset of or reducing the risk of developing conditions and sequelae that are associated with these diseases, such as atherosclerosis.Type: GrantFiled: September 12, 2005Date of Patent: December 8, 2009Assignee: Merck & Co., Inc.Inventors: James F. Dropinski, Guo Q. Shi, Yong Zhang
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Patent number: 7629469Abstract: A new compound of formula (IV) R represents a protecting group which is removable by hydrogenation, and use thereof as an intermediate for preparing paliperidone.Type: GrantFiled: January 16, 2009Date of Patent: December 8, 2009Assignee: Scinopharm Taiwan, Ltd.Inventors: Tsung-Cheng Hu, Hsiao-ping Fang, Hong-Tsung Huang
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Publication number: 20090298854Abstract: This invention is directed to indole acetic acid derivatives and their use in pharmaceutical compositions for the treatment of diseases such as diabetes, obesity, hyperlipidemia, and atherosclerotic disease. The invention is also directed to intermediates useful in preparation of indole acetic derivatives and to methods of preparation.Type: ApplicationFiled: July 23, 2009Publication date: December 3, 2009Inventors: Xin Ma, Louis-David Cantin, Soongyu Choi, Roger Clark, Martin Hentemann, Joachim Rudolph, Rico Lavoie, Zhonghua Zhang
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Publication number: 20090275628Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: ApplicationFiled: May 17, 2006Publication date: November 5, 2009Applicant: Gruenenthal GmbHInventors: Robert Frank, Ruth Jostock, Melanie Reich, Gregor Bahrenberg, Hans Schick, Helmut Sonnenschein
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Publication number: 20090275757Abstract: The crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.0, 16.0, 23.3, 23.7 and 26.3° and the crystal of 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid having peaks at the position of 14.6, 23.1, 24.7, 25.6 and 26.0° on 2? of diffraction angle in a powder X-ray diffraction pattern have a small specific volume, are hard to be charged with electricity, are easily handled and are useful for an active pharmaceutical ingredient of excellent anti-rheumatic agents.Type: ApplicationFiled: May 25, 2007Publication date: November 5, 2009Applicant: Toyama chemical Co., LtdInventors: Kenji Yonezawa, Hironori Kotsubo, Yasutaka Baba, Yukie Tada
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Patent number: 7598283Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: GrantFiled: October 5, 2007Date of Patent: October 6, 2009Assignee: Abbott Laboratories, Inc.Inventors: Yujia Dai, Steven K. Davidsen, Anna M. Ericsson, Kresna Hartandi, Zhiqin Ji, Michael R. Michaelides
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Publication number: 20090197884Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: ApplicationFiled: October 26, 2006Publication date: August 6, 2009Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20090143422Abstract: This invention relates to inhibitors of p38 and methods of utilizing the inhibitors and pharmaceutical compositions thereof in the treatment and prevention of various disorders mediated by p38.Type: ApplicationFiled: February 2, 2009Publication date: June 4, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Mark Munson, David A. Mareska, Youngboo Kim, Robert D. Groneberg, James Rizzi, Martha Rodriguez, Ganghyeok Kim, Guy Vigers, Chang Rao, Devan Balachari, Darren Harvey
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Publication number: 20090099369Abstract: A preparation method using as an intermediate 6-(halomethyl)-1,2-benzisoxazol-3(2H)-one derivative represented by general formula wherein R5 is a methyl group that is substituted with one or more optionally substituted phenyl groups, or an optionally substituted oxygen-containing heterocyclic group; X represents a halogen atom, can be used as a method for safely and easily preparing 3-{5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl}propionic acid, which is useful as an antirheumatic agent, with a high yield.Type: ApplicationFiled: February 19, 2007Publication date: April 16, 2009Applicant: TOYAMA CHEMICAL CO., LTD.Inventors: Kenji Yonezawa, Tamotsu Takamatsu, Naokatu Aoki, Tomohiro Hashimoto, Masahiro Takebayashi, Yoshiaki Suzuki, Yuji Oonishi
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Patent number: 7511046Abstract: The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: July 21, 2006Date of Patent: March 31, 2009Assignee: Aventis Hoklings Inc.Inventors: David M Fink, Brian S Freed, Nicholas J Hrib, Raymond W Kosley, George E Lee, Gregory H Merriman, Barbara S Rauckman
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Publication number: 20090061141Abstract: [Problems] To provide a monomethine dye compound that enables formation of a thin film with high refractive index and excellent optical properties through formation of a homogeneous thin film of dye molecule J-association complex by easy means (spin coating technique) and that has high sensitivity and excels in short mark recording capability so as to be suitable for high speed recording and high density recording, and further to provide an optical information recording medium utilizing the monomethine dye compound and a process for producing the same.Type: ApplicationFiled: March 30, 2005Publication date: March 5, 2009Inventors: Daisuke Morishita, Mamoru Uchida, Takuo Kodaira, Isao Okitsu, Hiroshi Hiratsuka, Hiroaki Horiuchi, Maiko Fukita
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Publication number: 20090054430Abstract: Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.Type: ApplicationFiled: July 16, 2008Publication date: February 26, 2009Applicant: Abbott LaboratoriesInventors: Yujia Dai, Ji Zhiqin, Michael R. Michaelides
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Patent number: 7495020Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.Type: GrantFiled: January 18, 2006Date of Patent: February 24, 2009Assignee: Merck & Co., Inc.Inventors: Alan D. Adams, A. Brian Jones, Joel P. Berger, James F. Dropinski, Alexander Elbrecht, Kun Liu, Karen Lamb MacNaul, Guo-Qiang Shi, Derek J. Von Langen, Gaochao Zhou
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Publication number: 20090042945Abstract: The present invention relates to substituted benzo[d]isoxazol-3-yl-amine compounds, methods for their production, medicaments containing these compounds and the use of these compounds to produce medicaments.Type: ApplicationFiled: May 18, 2006Publication date: February 12, 2009Applicant: Gruenenthal GmbHInventors: Robert Frank, Beatrix Merla, Melanie Reich, Ruth Jostock
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Publication number: 20090023779Abstract: The present invention relates to compounds of formula (I): in which R1, R2, R3, X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.Type: ApplicationFiled: October 14, 2005Publication date: January 22, 2009Applicant: Laboratoire TheramexInventors: Benoit Rondot, Jean Lafay, Paule Bonnet, Thierry Clerc, Igor Duc, Eric Duranti, Francois Puccio, Jacqueline Shields, Christian Blot, Philippe Maillos