Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 514/443)
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Publication number: 20100167927Abstract: The invention relates to substituted amino-thiourea compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the substituted amino-thiourea compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such compounds. The substituted amino-thiourea compounds are defined by the following formula (I): wherein A, B, R1, R2, R3, R4, R5.1, R5.2 and R6 are defined as in the description.Type: ApplicationFiled: May 13, 2008Publication date: July 1, 2010Applicant: BASF SEInventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
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Publication number: 20100166881Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
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Publication number: 20100168217Abstract: The invention relates to novel compound of the general formula (I), in which R has the meanings indicated in claim 1, to the preparation thereof and to the use thereof as medicaments. The compounds (I) are inhibitors of steroid sulfatase and are used for the treatment of cancer.Type: ApplicationFiled: November 13, 2007Publication date: July 1, 2010Applicant: MERCK PATENT GMBHInventors: Wolfgang Staehle, David Bruge, Gerald Scholz, Benoit Rondot, Jean Lafay
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Patent number: 7745445Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of the Peroxisome Proliferator-Activated Receptor (PPAR) families, particularly the activity of PPAR?.Type: GrantFiled: May 13, 2005Date of Patent: June 29, 2010Assignee: IRM LLCInventors: Robert Epple, Mihai Azimioara
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Publication number: 20100160327Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 21, 2006Publication date: June 24, 2010Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, JR., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
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Publication number: 20100160337Abstract: 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 Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Inventor: Jay M. Matthews
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Publication number: 20100160289Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.Type: ApplicationFiled: December 15, 2009Publication date: June 24, 2010Inventors: Mark J. Macielag, James J. McNally
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Patent number: 7741323Abstract: An indene derivative for selectively modulating the activities of peroxisome proliferator activated receptors (PPARs) having the following formula (I): wherein, R1 is C1-6 alkyl, C1-6 alkenyl, or C3-6 cycloalkyl, each of which is unsubstituted or substituted with one or more phenyl groups; R2 is H, CN, CO2Ra, CH2CO2Ra, CONRbRc, or phenyl; R3 is C1-6 alkyl, C3-6 cycloalkyl, naphthyl, phenyl, being each unsubstituted or substituted with one or more substituents selected from the group consisting of halogen, CN, NH2, NO2, ORa, phenyloxy, C1-6 alkyl, and C3-6 cycloalkyl; and R4, R5, R6, and R7 are each independently H, OH, OSO2CH3, O(CH2)mRe, CH2Rf, OCOCH2ORg, OCH2CH2ORg, OCH2CH?CHRg, or pyridine-2-yloxy, or R5 and R6 together form OCH2O.Type: GrantFiled: April 13, 2005Date of Patent: June 22, 2010Assignees: Korea Research Institute of Chemical Technology, Jeil Pharm. Co., Ltd., Korea Research Institute of Bioscience and Biotechnology, CJ Corp.Inventors: Hyae Gyeong Cheon, Sung-Eun Yoo, Sung Soo Kim, Sung-Don Yang, Kwang-Rok Kim, Sang Dal Rhee, Jin Hee Ahn, Seung Kyu Kang, Won Hoon Jung, Sung Dae Park, Nam Gee Kim, Jang Hyuk Lee, Sun Chul Huh, Jae Mok Lee, Seog Beom Song, Soon Ji Kwon, Jong Hoon Kim, Jeong-Hyung Lee, Seung Jun Kim
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Patent number: 7741362Abstract: The invention relates to (hetero)arylsulfonylamino based peptidomimetics of formula (I), wherein R1, R2, R3, A, B, D, Q, k and n are defined as disclosed, or a pharmaceutically acceptable salt or ester thereof. Compounds of formula (I) possess high affinity and selectivity for the somatostatin receptor subtypes SSTR1 and/or SSTR4 and can be used for the treatment or diagnosis of diseases or conditions wherein an interaction with SSTR1 and/or SSTR4 is indicated to be useful.Type: GrantFiled: October 5, 2004Date of Patent: June 22, 2010Assignee: Siegfried WursterInventors: Jussi Tomperi, Paivi Hautamaki, Harri Salo, Mia Engstrom, Andrei Tauber, Anna-Marja Hoffren, Siegfried Wurster
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Patent number: 7737176Abstract: The invention relates to compounds of the formula I: and to the pharmaceutically acceptable salts thereof, to processes for the preparation of them and to pharmaceutical compositions comprising them, which are useful especially for the treatment and prevention of dyslipidaemia, atherosclerosis and diabetes.Type: GrantFiled: August 11, 2003Date of Patent: June 15, 2010Assignee: Merck Patent GmbHInventors: Michel Brunet, Jean-Jacques Zeiller, Gérard Ferrand, Yves Bonhomme
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Patent number: 7732483Abstract: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 are independently selected from hydrogen, an optionally substituted C1-7 alkyl group, C3-20 heterocyclyl group, or C5-20 aryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is —NH—C(?O)— or —O—; Y is an optionally substituted C1-5 alkylene group; X is selected from SR3 or NR4R5, wherein, R3, or R4 and R5 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groups, or R4 and R5 may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is —O—, X is additionally selected from —C(?O)—NR6R7, wherein R6 and R7 are independently selected from hydrogen, optionally substituted C1-7 alkyl, C5-20 aryl, or C3-20 heterocyclyl groType: GrantFiled: June 5, 2008Date of Patent: June 8, 2010Assignees: Kudos Pharmaceuticals Limited, Cancer Research Technology LimitedInventors: Graeme Cameron Murray Smith, Niall Morrison Barr Martin, Keith Allan Menear, Marc Geoffrey Hummersone, Laurent Jean Martin Rigoreau, Roger John Griffin, Bernard Thomas Golding, David Richard Newell, Hilary Alan Calvert, Nicola Jane Curtin, Ian Robert Hardcastle, Kappusamy Saravanan
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Publication number: 20100137298Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: ApplicationFiled: June 13, 2008Publication date: June 3, 2010Applicant: WyethInventors: Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
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Publication number: 20100130570Abstract: The present invention relates N-5-membered, fused, heteroaryl-methylene-N-cycloalkyl-carboxamide derivatives, their thiocarboxamide or N-substituted carboximidamide analogues, all of formula (I) wherein A represents a carbo-linked 5-membered heterocyclyl group; T represents O, S, N—Rc, N—ORd, N—NRcRd or N—CN; Z1 to Z3; W1 to W5; Y1 to Y3 and p represent various substituents; their process of preparation; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 31, 2008Publication date: May 27, 2010Applicant: Bayer SASInventors: Philippe Desbordes, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Arounarith Tuch, Jean-Pierre Vors
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Patent number: 7723378Abstract: The invention relates to novel thiophene derivatives, their preparation and their use as pharmaceutically active compounds particularly as immunosuppressant agents.Type: GrantFiled: March 20, 2006Date of Patent: May 25, 2010Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Jörg Velker, Thomas Weller
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Publication number: 20100125090Abstract: The present invention provides compounds of Formula I useful as modulators of ABC transporter activity, or a pharmaceutically acceptable salt thereof, wherein RB, n, B, RC, RD, RE, A, and Z are described generally and in classes and subclasses below. The present invention also provides pharmaceutical compositions, methods and kits associated with Formula I, useful for as modulators, and for the treatments of disease and disease conditions associated with ABC transporter proteins.Type: ApplicationFiled: August 14, 2009Publication date: May 20, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Mark Miller, Ashvani Singh, Matthew Hamilton, Peter D.J. Grootenhuis
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Publication number: 20100113579Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.Type: ApplicationFiled: January 15, 2010Publication date: May 6, 2010Applicant: ELI LILLY AND COMPANYInventors: Eric David Moher, James Allen Monn, Concepcion Pedregal-Tercero, Jaime Gonzalo Blanco-Urgoiti, Ivan Collado Cano
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Publication number: 20100105725Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: October 26, 2007Publication date: April 29, 2010Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
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Patent number: 7705022Abstract: Novel indoleamine 2,3-dioxygenase (IDO) inhibitors, compositions comprising the same, and methods of use thereof are disclosed.Type: GrantFiled: October 27, 2006Date of Patent: April 27, 2010Assignee: Lankenau Institute for Medical ResearchInventors: George C. Prendergast, William P. Malachowski, Alexander J. Muller, James B. DuHadaway
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Patent number: 7705034Abstract: The invention is concerned with novel vinylogous acid derivatives of formula I: wherein A and R1 to R5 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are useful as chymase inhibitors.Type: GrantFiled: September 24, 2007Date of Patent: April 27, 2010Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Hans Hilpert, Bernd Kuhn, Harald Mauser
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Patent number: 7700620Abstract: The present invention provides novel C-linked cyclic compounds and analogues of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.Type: GrantFiled: June 26, 2006Date of Patent: April 20, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James C. Sutton, Jennifer X. Qiao, Carl Thibeault, Rejean Ruel
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Patent number: 7696244Abstract: The invention provides compositions, including pharmaceutical preparations, which comprise one or more substituted thiophene, benzofuran, pyrimidinetrione, dihydropyridine, tetrahydrocarbazol or anthraquinone compounds. The invention also features methods of use of such compositions in increasing activity of mutant-cystic fibrosis transmembrane conductance regulator protein in a cell, e.g. by increasing ion transport in a mutant-CFTR.Type: GrantFiled: May 14, 2004Date of Patent: April 13, 2010Assignee: The Regents of the University of CaliforniaInventors: Alan Verkman, Luis J. V. Galietta, R. Kiplin Guy
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Publication number: 20100081631Abstract: Methods are provided directed to administering a therapeutically effective amount of a prostaglandin EP4 agonist component to a mammal afflicted with or prone to affliction with a disease or condition selected from an esophageal ulcer, alcohol gastropathy, a duodenal ulcer, a gastric ulcer, non-steroidal anti-inflammatory drug-induced gastroenteropathy and intestinal ischemia. Such administration results in treating or preventing the disease or condition.Type: ApplicationFiled: December 11, 2007Publication date: April 1, 2010Inventors: Guang Liang Jiang, Wha Bin Im, Larry A. Wheeler
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Publication number: 20100076065Abstract: The present invention relates to novel, non-secosteroidal, phenyl-benzothiophene compounds with vitamin D receptor (VDR) modulating activity that are less hypercalcemic than 1?,25 dihydroxy vitamin D3. These compounds are useful for treating bone disease and psoriasis.Type: ApplicationFiled: July 6, 2009Publication date: March 25, 2010Inventors: Jianliang Lu, Tainwei Ma, Sunil Nagpal, Quanrong Shen, Alan M. Warshawsky, Ying Kwong Yee, Michael John Rupp
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Publication number: 20100062065Abstract: Provided is an oral pharmaceutical composition with improved bioavailability and pharmacokinetic properties of a drug, by increasing a bioabsorption rate and an in vivo retention time of an active ingredient via intestine-targeted formulation of a particular naphthoquinone-based compound, or a pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as an active ingredient.Type: ApplicationFiled: November 26, 2007Publication date: March 11, 2010Applicants: MAZENCE INC., KT & G CP., LTDInventors: In Geun Jo, Sang-Ku Yoo, Myung-gyu Park, Taehwan Kwak
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Patent number: 7674822Abstract: This invention relates to modulating (e.g., inhibiting) protein tyrosine phosphatase 1B (PTP1B).Type: GrantFiled: November 22, 2005Date of Patent: March 9, 2010Assignee: WyethInventors: Jinbo Lee, Michael J. Smith, Alessandro Fabio Moretto, Zhao-Kui Wan, Eva Deanna Binnun, Weixin Xu, Kenneth W. Foreman, Diane M. Joseph-McCarthy, David V. Erbe, Steve Y. Tam
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Patent number: 7674815Abstract: Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: January 29, 2007Date of Patent: March 9, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Christoph Faeh, Holger Kuehne, Thomas Luebbers, Patrizio Mattei, Cyrille Maugeais, Philippe Pflieger
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Patent number: 7671081Abstract: Compounds of formula (I): wherein the substituents are as defined herein.Type: GrantFiled: November 2, 2007Date of Patent: March 2, 2010Assignee: Sun Chemical CorporationInventors: Shaun Lawrence Herlihy, Brian Rowatt, Robert Stephen Davidson
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Patent number: 7671082Abstract: This invention relates to synthetic excitatory amino acid prodrugs and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.Type: GrantFiled: March 31, 2008Date of Patent: March 2, 2010Assignee: Eli Lilly and CompanyInventors: Eric David Moher, James Allen Monn
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Publication number: 20100048513Abstract: The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.Type: ApplicationFiled: August 20, 2008Publication date: February 25, 2010Inventors: Michael J. Hawkins, Michael N. Greco, Eugene Powell, Lawrence de Garavilla, Bruce E. Maryanoff
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Patent number: 7666866Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: November 15, 2005Date of Patent: February 23, 2010Assignee: Eli Lilly and CompanyInventors: Jeffry Bernard Franciskovich, David Kent Herron, Valentine Joseph Klimkowski, Angela Lynn Marquart, John Joseph Masters, David Mendel, Andrew Michael Ratz, Gerald Floyd Smith, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100035854Abstract: A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period time that is less than 60 minutes.Type: ApplicationFiled: August 6, 2009Publication date: February 11, 2010Inventors: Rudi Mueller-Walz, Roland Steiner
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Patent number: 7655641Abstract: The present invention is directed to a compound of Formula (I): and pharmaceutically acceptable salts, solvates, hydrates or stereoisomers thereof, which are useful in treating or preventing disorders mediated by a peroxisome proliferator activated receptor (PPAR) such as syndrome X, type II diabetes, hyperglycemia, hyperlipidemia, obesity, coagaulopathy, hypertension, arteriosclerosis, and other disorders related to syndrome X and cardiovascular diseases.Type: GrantFiled: February 10, 2004Date of Patent: February 2, 2010Assignee: Eli Lilly and CompanyInventors: Scott Eugene Conner, Lynn Stacy Gossett, Jonathan Edward Green, Winton Dennis Jones, Jr., Nathan Bryan Mantlo, Donald Paul Matthews, Daniel Ray Mayhugh, Daryl Lynn Smith, Jennifer Ann Vance, Xiaodong Wang, Alan M Warshawsky, Leonard Larry Winneroski, Jr., Yanping Xu, Guoxin Zhu
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Patent number: 7652063Abstract: A compound comprising or a pharmaceutically acceptable salt or a prodrug thereof, wherein the dashed line represents the presence or absence of a double bond; J is C?O or CHOH; A is —(CH2)6—, or cis —CH2CH?CH—(CH2)3—, wherein 1 or 2 carbons may be substituted with S or O; B is CO2H, or CO2R, CONR2, CONHCH2CH2OH, CON(CH2CH2OH)2, CH2OR, P(O)(OR)2, CONRSO2R, SONR2, or R is H, C1-6 alkyl; D is —(CH2)n—, —X(CH2)n, or —(CH2)nX—, wherein n is from 0 to 3 and X is S or O; and E is an aromatic or heteroaromatic moiety having from 0 to 4 substituents, said substituents each comprising from 1 to 6 non-hydrogen atoms is disclosed herein. Methods, compositions, and medicaments related thereto, as well as experimental results showing prostaglandin EP4 selective agonist activity for certain compounds disclosed herein, are also disclosed.Type: GrantFiled: September 15, 2006Date of Patent: January 26, 2010Assignee: Allergan, Inc.Inventor: Yariv Donde
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Publication number: 20100016310Abstract: Disclosed are methods of using soluble epoxide hydrolase (sEH) inhibitors for treating diseases related to cardiovascular disease.Type: ApplicationFiled: August 15, 2007Publication date: January 21, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Richard Harold Ingraham
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Patent number: 7645791Abstract: Novel salicylic anilides are chemical uncouplers useful e.g. for the treatment of obesity.Type: GrantFiled: June 27, 2008Date of Patent: January 12, 2010Assignee: High Point Pharmaceuticals, LLCInventors: Preben Houlberg Olesen, Thomas Kruse Hansen, Lise Brown Christiansen, Holger Claus Hansen
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Benzothiophene hydroxamic acid derivatives with carbamate, urea, amide and sulfonamide substitutions
Publication number: 20090318541Abstract: The present invention relates to a novel class of hydroxamic acid derivatives carbamate, urea, amide and sulfonamide substitutions. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention are also useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: December 24, 2009Inventors: Joey Methot, Thomas A. Miller, David J. Witter -
Publication number: 20090318542Abstract: The present invention relates generally to ophthamological drugs. More specifically, the invention relates to a method of modifying (derivatizing) ophthamological drugs so as to increase their penetration through the cornea. The invention also relates to drugs modified (derivatized) in accordance with the instant method and to the use of same in treating conditions associated with elevated intraocular pressure, particularly, glaucoma.Type: ApplicationFiled: July 29, 2009Publication date: December 24, 2009Inventors: Eric J. Toone, David L. Epstein, Pratap Challa, Phillip W. Snyder, Xin Chen, Mitchell A. deLong
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Patent number: 7632859Abstract: By using a composition comprising rotigotine and at least one chloride salt in a concentration of 1 to 140 mmol/l, the composition having a pH of 4 to 6.5 in a iontophoretic device for the treatment of Parkinson's disease, it became possible to obtain a rotigotine flux across the human stratum corneum which was higher than the one previously obtained with conventional passive diffusion systems.Type: GrantFiled: November 17, 2003Date of Patent: December 15, 2009Assignee: Schwarz Pharma AGInventors: Gai Ling Li, Johanna Aaltje Bouwstra, Hans-Michael Wolff, Akhmad Karis Nugroho
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Publication number: 20090306169Abstract: The present invention provides the use of fused pyrrole carboxylic acids of formula (I) for the manufacture of a medicament to inhibit D-amino acid oxidase, particularly for the treatment of neurodegenerative and psychiatric disorders or diseases; certain compounds of formula I being novel, pharmaceutical compositions containing them, their use in medicine and methods of treatment using them are also disclosed.Type: ApplicationFiled: October 5, 2006Publication date: December 10, 2009Inventors: Philip E. Brandish, Timothy Sparey, Alister Campbell, Andrew Pike, Nicholas Brandon, Wei Zheng
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Publication number: 20090298842Abstract: Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases.Type: ApplicationFiled: August 1, 2009Publication date: December 3, 2009Inventors: János Pató, György Kéri, László Örfi, Frigyes Wáczek, Zoltán Horváth, Péter Banhegyi, Istaván Szabadkai, Jenö Marosfalvi, Bálint Hegymegi-barakonyi, Zsolt Székélyhidi, Zoltán Greff, Axel Choidas, Gerald Bacher, Andrea Missio, Anil Koul
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Publication number: 20090298925Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof useful as Estrogen Receptor beta agonists for treating Estrogen Receptor beta mediated diseases such as benign prostatic hyperplasia.Type: ApplicationFiled: July 31, 2009Publication date: December 3, 2009Inventors: Gregory Lee Durst, Bryan Hurst Norman, Lance Allen Pfeifer, Timothy Ivo Richardson
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Publication number: 20090298924Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers: wherein Y1 is a bond, —(C?O)—, —S(O2)—, —C(?O)O—, —OC(?O)—, —(C?O)NR3—, —NR3(C?O)—, —S(O2)NR3—, —NR3S(O2)—, or —NR3(C?O)NR5—, wherein R3 and R5 are independently hydrogen or optionally substituted (C1-C6)alkyl, L1 is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n, p, Alk1, Alk2 and Q are as defined in the claims; z is 0 or 1; A represents an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; -[Linker]- represents a divalent linker radical; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C?O)R3, —(C?O)OR3, or —(C?O)NR3 wherein RType: ApplicationFiled: May 4, 2006Publication date: December 3, 2009Applicant: Chroma Therapeutics LtdInventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, David Festus Charles Moffat
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Patent number: 7625944Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.Type: GrantFiled: July 30, 2007Date of Patent: December 1, 2009Assignee: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Publication number: 20090291978Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, C(?O)—, —S(?O)2—, —C(—O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L is a divalent radical of formula -(Alk1)m(O)n(Alk2)p— wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or hetero-cyclic rType: ApplicationFiled: May 4, 2006Publication date: November 26, 2009Applicant: CHROMA THERAPEUTICS LTD.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Moffat, Kenneth William John Baker, Alistair David Graham Donald
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Publication number: 20090286863Abstract: The invention relates to novel compound of the general formula (I), in which R has the meanings indicated in Claim 1, to the preparation thereof and to the use thereof as medicaments. The compounds (I) are inhibitors of steroid sulfatase and are used for the treatment of cancer.Type: ApplicationFiled: June 5, 2007Publication date: November 19, 2009Inventors: David Bruge, Wolfgang Staehle, Gerald Scholz, Benoit Rondot, Jean Lafay
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Publication number: 20090286862Abstract: The present invention relates to a preventive and/or therapeutic agent for psychoneurotic diseases, comprising an EP3 antagonist represented by the general formula (I): (wherein the meanings of characters are defined in the description). This compound has an antagonistic potency against EP3 and exhibits efficacy through unusual action mechanism as a preventive and/or therapeutic agent for psychoneurotic disorder, psychosomatic disorder, anxiety disorder, depression and disorder caused by stress.Type: ApplicationFiled: August 5, 2005Publication date: November 19, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Masami Narita, Kazutoyo Sato
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Patent number: 7612107Abstract: The present invention contemplates methods of treating, reducing, inhibiting or preventing several diseases by the administration of flexible heteroarotinoids. Among the diseases or conditions which can benefit from treatment with flexible heteroarotinoids as described herein are, (1) cancers and other diseases that involve abnormal differentiation, (2) diabetes, (3) hemophilia, (4) liver disease, (5) diseases involving human aldehyde dehydrogenase 2, (6) polycystic kidney disease, (7) lysosomal storage diseases, (8) high cholesterol, (9) obesity, (10) high triglycerides, (11) glycoprotein metabolism diseases, and (12) diseases involving abnormal angiogenesis.Type: GrantFiled: April 14, 2006Date of Patent: November 3, 2009Assignee: The Board of Regents of the University of OklahomaInventors: Doris M. Benbrook, Martin Turman, Suresh Guruswamy
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Publication number: 20090264474Abstract: 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 A, B, G, Y, R1, R2, R3, and R4 are defined herein.Type: ApplicationFiled: July 18, 2008Publication date: October 22, 2009Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
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Publication number: 20090264470Abstract: The present invention relates to methods of treating obesity, anorexia nervosa, or bulimia nervosa comprising administering a compound of the invention. The present invention further relates to the treatment of metabolic syndrome comprising administering a compound of the invention.Type: ApplicationFiled: February 21, 2007Publication date: October 22, 2009Inventors: Teresa A. Bennett, James R. Hauske, Fu-Yue Zeng
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Publication number: 20090264411Abstract: A series of 4,5,6,7-tetrahydrothieno[2,3-c]azepin-8-one derivatives, and analogues thereof, which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: February 13, 2009Publication date: October 22, 2009Applicant: UCB Pharma S.A.Inventors: Victoria Elizabeth Laing, Daniel Christopher Brookings, Rachel Jane Carbery, Jose Miguel Gascon Simorte, Martin Clive Hutchings, Barry John Langham, Martin Alexander Lowe