The Additional Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 514/337)
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Publication number: 20090221564Abstract: Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R1, R2, R3, R4, Y, m, n and q are as identified herein. R1 is in particular amidino. The invention further provides particular benzothiophene compounds. Compounds of the invention may be useful as inhibitors of Factor IXa and in the therapy of cardiovascular conditions and diseases, e.g. thrombosis.Type: ApplicationFiled: February 20, 2007Publication date: September 3, 2009Applicant: TRIGEN LIMITEDInventors: Shouming Wang, Toby Jonathan Blench, Frederic Marlin, Richard Beck, Roger Peter Dickinson
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Publication number: 20090214675Abstract: The present application relates to novel 4-chromenonyl-1,4-dihydropyridinecarbonitriles, processes for their preparation, pharmaceutical compositions containing them, and their use for the treatment and/or prophylaxis of diseases, especially cardiovascular disorders.Type: ApplicationFiled: July 14, 2006Publication date: August 27, 2009Applicant: Bayer HealthCare AGInventors: Alexander Kuhl, Peter Kolkhof, Heike Heckroth, Karl-Heinz Schlemmer, Ingo Flamme, Santiago Figueroa Perez, Heike Gielen-Haertwig, Rolf Grosser, Jens-Kerim Ergüden, Dieter Lang
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Publication number: 20090208449Abstract: Compounds having the formula I wherein R1, R2, R3, R4, R5 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: February 12, 2009Publication date: August 20, 2009Inventors: Sharada Shenvi Labadie, Clara Jeou Jen Lin, Francisco Xavier Talamas, Robert James Weikert
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Publication number: 20090209511Abstract: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N? or —CH?; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.Type: ApplicationFiled: March 24, 2009Publication date: August 20, 2009Inventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Yasunori Tsuboi, Takashi Mitsui, Jun Murakami
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Publication number: 20090202525Abstract: The present invention relates to compounds of Formula (1), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating glucokinase mediated disorders. More particularly, the compounds of the present invention are glucokinase modulators useful for treating disorders including, but not limited to, type II diabetes.Type: ApplicationFiled: April 15, 2009Publication date: August 13, 2009Inventors: Haiyan Bian, Joseph Dudash, Mona Patel, Philip Rybczynski, Yongzheng Zhang, Mary Pat Beavers, Maud Urbanski, Min (Amy) Xiang, Roxanne Zeck
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Publication number: 20090192179Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: February 26, 2009Publication date: July 30, 2009Inventors: Bing Wang, Jian Chen
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Publication number: 20090182011Abstract: Chimeric nitrate esters and their use in the treatment of depression are disclosed. The chimeric nitrate esters also are useful in the treatment of depression and comorbidity associated with aging.Type: ApplicationFiled: January 15, 2009Publication date: July 16, 2009Applicant: UNIVERSITY OF ILLINOIS CHICAGOInventor: Gregory R.J. Thatcher
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Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides
Publication number: 20090181968Abstract: The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical compositions including the compounds are prepared or thereof: wherein, A1, A2, R1, R2, R3, R4, and R5 and n are as defined in the specification. The compounds of formula (I) are useful in therapy.Type: ApplicationFiled: November 22, 2006Publication date: July 16, 2009Applicant: ASTRAZENECA ABInventors: Kosrat Amin, Johan Broddefalk, Yantao Chen, Karolina Nilsson, Claire Milburn, Helene Desfosses, Ziping Liu, Maxime Tremblay, Christopher Walpole, Zhong-yong Wei, Hua Yang -
Publication number: 20090170903Abstract: The invention provides inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are new ester derivatives, methods of preparing such compounds, compositions containing them, and therapeutic uses thereof.Type: ApplicationFiled: December 15, 2008Publication date: July 2, 2009Applicant: Chiesi Farmaceutici S.p.A.Inventors: Elisabetta ARMANI, Gabriele AMARI, Gino VILLETTI
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Publication number: 20090163550Abstract: Biocompatible intraocular implants include a retinoid component and a biodegradable polymer that is effective to facilitate release of the retinoid component into an eye for an extended period of time. The therapeutic agents of the implants may be associated with a biodegradable polymer matrix, such as a matrix that is substantially free of a polyvinyl alcohol. The implants may be placed in an eye to treat or reduce the occurrence of one or more ocular conditions, such as retinal damage, including glaucoma and proliferative vitreoretinopathy.Type: ApplicationFiled: February 18, 2009Publication date: June 25, 2009Applicant: ALLERGAN, INC.Inventors: Patrick M. HUGHES, Orest Olejnik, Glenn Tony Huang, Joan-En Chang-Lin, Thierry Nivaggioli, JaneGuo Shiah, Michele Boix, Christian Sarrazin
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Publication number: 20090149493Abstract: The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R1, R2, A and Z have defined meanings.Type: ApplicationFiled: March 19, 2007Publication date: June 11, 2009Inventors: Jean Fernand Armand Lacrampe, Christophe Meyer, Bruno Schoentjes, Delphine Yvonne Raymonde Lardeau, Alain Philippe Poncelet, Luc Van Hijfte
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Publication number: 20090149417Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.Type: ApplicationFiled: October 17, 2008Publication date: June 11, 2009Inventors: Valeria Ossovskaya, Barry M. Sherman
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Publication number: 20090143408Abstract: Methods of inhibiting cytochrome P450 2D6 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450 2D6. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 2D6 enzymes.Type: ApplicationFiled: November 26, 2008Publication date: June 4, 2009Applicant: Sequoia Pharmaceuticals, Inc.Inventors: Michael EISSENSTAT, Dehui Duan, Ji-Hye Kang
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Publication number: 20090143439Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.Type: ApplicationFiled: November 24, 2008Publication date: June 4, 2009Inventors: Wolfgang Haap, Paul Hebeisen, Eric A. Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
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Publication number: 20090136496Abstract: Provided herein are methods for identifying a subject afflicted with chronic lymphocytic leukemia who is responsive to treatment with a chemotherapeutic agent by detecting the presence or absence of at least one APOE4 allele in the subject, the presence of an APOE4 allele identifying the subject as responsive to the treatment. Also provided are methods of treating a subject afflicted with chronic lymphocytic leukemia, including administering an estrogenic agent, an androgen withdrawal agent, an apoE4 peptide or mimetic thereof, and/or a chemotherapeutic agent in an amount effective to treat said chronic lymphocytic leukemia. Methods of determining a prognosis for a patient diagnosed with chronic lymphocytic leukemia are also provided. In addition, methods for stratifying a subject into a subgroup of a clinical trial and methods for identifying a patient in a clinical trial of a treatment for chronic lymphocytic leukemia are herein provided.Type: ApplicationFiled: November 5, 2008Publication date: May 28, 2009Applicant: Duke UniversityInventors: J. Brice Weinberg, Warren J. Strittmatter
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Publication number: 20090131468Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.Type: ApplicationFiled: November 14, 2008Publication date: May 21, 2009Applicant: AstraZeneca ABInventors: Johan Bylund, Marie E. Ek, Annika Kers, Gunnar Nordvall, Liselotte Ohberg, Jenny Viklund, Stefan Von Berg, Jorg Holenz, Katja Narhi, Daniel Sohn, Martin H. Johansson
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Publication number: 20090124629Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; each R2 is independently hydrogen, fluorine or C1-4alkyl; n is 2, 3, 4, or 5; R3 is C1-4alkyl; R4 is hydrogen, or a C1-4alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5;or R4 is a —SR6 group; R5 is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido- 2-isothiType: ApplicationFiled: April 12, 2006Publication date: May 14, 2009Inventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Michel, Luca Tarsi, Silvia Terreni
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Publication number: 20090124613Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: ApplicationFiled: November 7, 2008Publication date: May 14, 2009Inventors: Joanne J. Bronson, Andrew P. Degnan, William D. Schmitz
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Patent number: 7531695Abstract: The present invention is directed to compounds having the structure (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.Type: GrantFiled: June 3, 2004Date of Patent: May 12, 2009Assignee: Auspex Pharmaceutical, IncInventors: Borcherng Hong, Sepehr Sarshar, Bruno Tse
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Patent number: 7531537Abstract: The present invention provides a benzofuran derivative of the formula [1]: wherein x is a group of the formula: —N? or —CH?; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R1 is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R3 is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.Type: GrantFiled: March 27, 2003Date of Patent: May 12, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Takayuki Kawaguchi, Hidenori Akatsuka, Toru Iijima, Yasunori Tsuboi, Takashi Mitsui, Jun Murakami
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Patent number: 7524862Abstract: Alkyne compounds of formula I wherein A, B, W, X, Y, Z, R1, and R2 have the meanings given herein, which have MCH-receptor antagonistic activity and are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.Type: GrantFiled: April 13, 2005Date of Patent: April 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Dirk Stenkamp, Stephan Georg Mueller, Philipp Lustenberger, Thorsten Lehmann-Lintz, Gerald Juergen Roth, Klaus Rudolf, Marcus Schindler, Leo Thomas, Ralf Lotz
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Patent number: 7524864Abstract: The invention relates to novel antihistamines and methods of modulating sleep by administering a doxepin analog or a pharmaceutically effective salt thereof.Type: GrantFiled: April 25, 2005Date of Patent: April 28, 2009Assignee: Hypnion, Inc.Inventors: Dale M. Edgar, David G. Hangauer, James F. White
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Patent number: 7524870Abstract: The present invention relates to compounds of formula (I) wherein Ar, Ar2, R2, R3, R4, m, p and s are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases that are associated with the activation of the glycogen synthase enzyme, such as diabetes.Type: GrantFiled: November 21, 2005Date of Patent: April 28, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Paul Gillespie, Robert Alan Goodnow, Jr., Jefferson Wright Tilley
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Patent number: 7524869Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: October 1, 2003Date of Patent: April 28, 2009Assignee: Florida State University Research Foundation, Inc.Inventor: Robert A. Holton
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Publication number: 20090093479Abstract: The present invention is in the area of novel compounds and salts thereof, their syntheses, and their use as anti-cancer agents. The compounds include compounds of Formula I: and solvates, hydrates and pharmaceutically-acceptable salts thereof, wherein A1 is N or CR1; A3 is N or CR3; A5 is N or CR5; R1, R3-R6 and L are defined in the specification; n is 0 or 1; and X is an optionally-substituted aryl group having 6-10 carbons in the ring portion, an optionally-substituted 6-membered heteroaryl group having 1-3 nitrogen atoms in the ring portion, an optionally-substituted 5-membered heteroaryl group having 0-4 nitrogen atoms in the ring portion and optionally having 1 sulfur atom or 1 oxygen atom in the ring portion, or an optionally-substituted heteroaryl group in which a 6-membered ring is fused either to a 5-membered ring or to a 6-membered ring, wherein in each case 1, 2, 3 or 4 ring atoms are heteroatoms independently selected from nitrogen, oxygen and sulfur.Type: ApplicationFiled: December 17, 2008Publication date: April 9, 2009Applicant: LOCUS PHARMACEUTICALS, INC.Inventors: Martha KELLY, Younghee LEE, Bin LIU, Ted FUJIMOTO, Joel FREUNDLICH, Bruce D. DORSEY, Gary A. FLYNN, Arifa HUSAIN
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Publication number: 20090093485Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).Type: ApplicationFiled: October 26, 2005Publication date: April 9, 2009Applicant: ASTRAZENECA ABInventors: Hakan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepisto
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Publication number: 20090082308Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide 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: April 14, 2006Publication date: March 26, 2009Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Patent number: 7507761Abstract: The invention relates to novel benzopyran derivatives of formula I, to their method of production, to composition comprising the derivatives and use thereof.Type: GrantFiled: January 21, 2005Date of Patent: March 24, 2009Assignees: Universite de Liege, Universite Libre de BruxellesInventors: Sophie Sebille, Bernard Pirotte, Stéphane Boverie, Pascal De Tullio, Philippe Lebrun, Marie-Hélène Antoine
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Publication number: 20090076088Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.Type: ApplicationFiled: October 30, 2008Publication date: March 19, 2009Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
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Patent number: 7504409Abstract: The claimed invention relates to methods of modulating mucin synthesis and the therapeutic application of compounds in controlling mucin over-production associated with diseases such as chronic obstructive pulmonary diseases (COPD) including asthma and chronic bronchitis, inflammatory lung diseases, cystic fibrosis and acute or chronic respiratory infectious diseases.Type: GrantFiled: May 5, 2004Date of Patent: March 17, 2009Assignee: Genaera CorporationInventors: Yuhong Zhou, Roy C. Levitt, Nicholas C. Nicolaides, Steve Jones, Mike McLane
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Publication number: 20090069383Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.Type: ApplicationFiled: October 30, 2008Publication date: March 12, 2009Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
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Patent number: 7501443Abstract: This invention generally relates to the derivatives of 3.6-disubstituted azabicyclo [3.1.0] hexanes of the following formula [IA]. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the :h1ethods for treating the diseases mediated through muscarinic receptors.Type: GrantFiled: December 23, 2002Date of Patent: March 10, 2009Assignee: Ranbaxy Laboratories LimitedInventors: Anita Mehta, Sanjay Kumar Srivastava, Jang Bahadur Gupta
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Publication number: 20090062348Abstract: The present invention provides an antifungal agent that has superior antifungal action and is also superior in terms of physical properties, safety and metabolic stability. The present invention discloses a compound represented by the formula (I): (wherein X represents an oxygen atom, a sulfur atom or —NH—, R1 represents a hydrogen atom, a halogen atom, a cyano group, an amino group or a substituent, and R2 and R3 independently represent a hydrogen atom, a halogen atom, a hydroxyl group or a substituent, except for a case in which R2 and R3 are both hydrogen atoms), and an antifungal agent containing the above compound.Type: ApplicationFiled: March 29, 2006Publication date: March 5, 2009Inventors: Kazutaka Nakamoto, Satoshi Inoue, Keigo Tanaka, Toru Haneda
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Publication number: 20090062239Abstract: Disclosed herein are methods of preventing, inhibiting, or ameliorating complications associated with cardiopulmonary bypass surgery by the use of a thrombin receptor antagonist compound. Among the thrombin receptor antagonist compounds useful in these methods are those of Formulas I and II, described herein.Type: ApplicationFiled: October 30, 2008Publication date: March 5, 2009Inventors: Enrico P. Veltri, John T. Strony, Gail Berman
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Patent number: 7498349Abstract: Aromatic compounds exemplified by exhibit antimicrobial activity.Type: GrantFiled: August 1, 2003Date of Patent: March 3, 2009Assignee: Genesoft Pharmaceuticals, Inc.Inventors: Roland W. Burli, Eldon E. Baird, Jacob A. Kaizerman, Dustin L. McMinn
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Publication number: 20090042907Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: ApplicationFiled: June 20, 2008Publication date: February 12, 2009Applicants: Cephalon, Inc., Cephalon FranceInventors: Edward R. Bacon, Sankar Chatterjee, Mohamed Iqbal, Brigitte Lesur, Philippe Louvet
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Patent number: 7488742Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.Type: GrantFiled: September 25, 2003Date of Patent: February 10, 2009Assignee: Schering CorporationInventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
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Publication number: 20090036492Abstract: The present invention relates to a novel cercosporamide derivative, a pharmacologically acceptable salt thereof or an ester thereof which has an excellent hypoglycemic effect and is useful as a therapeutic and/or prophylactic agent for diabetes.Type: ApplicationFiled: August 8, 2006Publication date: February 5, 2009Inventors: Akihiro Furukawa, Jun Ohsumi, Tsuyoshi Arita, Takehiro Fukuzaki, Kazushi Araki, Makoto Mori, Takayuki Momose, Takeshi Honda, Masanori Kuroha, Ryo Okuyama, Susumu Satoh
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Publication number: 20090030038Abstract: The present invention relates to new compounds of formula I. (I) wherein R1 to R12, X, Q and n are as defined as in formula I, or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.Type: ApplicationFiled: May 22, 2006Publication date: January 29, 2009Applicant: ASTRAZENECA ABInventors: Chester Chu, Andrew Lister, Gunnar Nordvall, Carl Petersson, Didier Rotticci, Daniel Sohn, Stefan Von Berg
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Publication number: 20090023783Abstract: The invention relates to novel benzofuran derivatives, processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disordersType: ApplicationFiled: August 29, 2008Publication date: January 22, 2009Inventors: Chengzhi Zhang, Jacques Dumas, Gaetan H. Ladouceur, Qian Zhao, Martin Hentemann, Sharad K. Verma, Qingming Zhu, Rico C. Lavoie, Jianmei Fan, Barton Phillips
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Publication number: 20090012075Abstract: The present invention relates to a novel class of fluorinated arylamide derivatives. The instant compounds can be used to treat cancer. The fluorinated arylamide derivatives 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: January 8, 2007Publication date: January 8, 2009Inventors: Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Patent number: 7473701Abstract: Substituted indazoles, compositions containing them, method of production and use. The present invention relates in particular to novel specific substituted indazoles exhibiting kinase-inhibiting activity, having therapeutic activity, in particular in oncology.Type: GrantFiled: October 13, 2004Date of Patent: January 6, 2009Assignee: Aventis Pharma S.A.Inventors: Dominique Damour, Jean-Christophe Carry, Patrick Nemecek, Corinne Terrier, Frederico Nardi, Bruno Filoche-Romme, Marie-Pierre Cherrier, Daniel Bezard
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Publication number: 20090005421Abstract: The invention relates to novel pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents.Type: ApplicationFiled: January 23, 2007Publication date: January 1, 2009Applicant: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
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Publication number: 20080319021Abstract: The present invention relates to selective inhibitors of phosphoinositide (PI) 3-kinase ?, use of the selective inhibitors in anti-thrombotic therapy, and a method for screening compounds useful for the new anti-thrombotic therapy by detecting selective inhibitory activity of PI 3-kinase ? of the compound. The invention also relates to novel compounds that are inhibitors of PI 3-kinase.Type: ApplicationFiled: December 27, 2007Publication date: December 25, 2008Inventors: Shaun P. Jackson, Alan D. Robertson, Vijaya Kenche, Philip Thompson, Hishani Prabaharan, Karen Anderson, Belinda Abbott, Isaac Goncalves, Warwick Nesbitt, Simone Shoenwaelder, Dilek Saylik
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Publication number: 20080293680Abstract: The invention relates to a compound of the formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are defined as in the specification and claims and to its use for treating or preventing Alzheimer's disease and other similar diseases.Type: ApplicationFiled: August 1, 2006Publication date: November 27, 2008Inventors: Stefan Peters, Christian Eickmeier, Klaus Fuchs, Werner Stransky, Cornelia Dorner-Ciossek, Marcus Kostka, Sandra Handschuh, Herbert Nar, Klaus Bornemann, Klaus Klinder, Margit Bauer
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Publication number: 20080286204Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: May 9, 2008Publication date: November 20, 2008Inventors: Sara S. Hadida-Ruah, Mark Miller, Brian Bear, Jinglan Zhou, Jason McCartney, Peter Grootenhuis
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Publication number: 20080280875Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: May 9, 2007Publication date: November 13, 2008Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukul, Ru Zhou
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Patent number: 7449459Abstract: The invention relates to compounds of general formula I as well as the production and use thereof as a medication.Type: GrantFiled: March 23, 2007Date of Patent: November 11, 2008Assignee: Bayer Schering Pharma AGInventors: Bernd Buchmann, Dirk Kosemund, Bernd Menzenbach, Martin Fritsch
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Publication number: 20080275048Abstract: Compounds of formula (I) Z-Ar1—Ar2 ??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: ApplicationFiled: June 3, 2008Publication date: November 6, 2008Applicant: ABBOTT LABORATORIESInventors: Jennifer M. Frost, Jianguo Ji, Tao Li, Diana L. Nersesian, Karin R. Tietje
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Patent number: 7442712Abstract: A compound represented by the structural formula and pharmaceutically acceptable salts and solvents thereof is disclosed, wherein: the single-dashed line between the ring carbons to which R10 and R34 are attached represents either a single bond or a double bond; the double-dashed line between X and the carbon to which Y is attached represents either a single bond or an absent bond; X is —O— or —NR6— when the double-dashed line represents a single bond; X is H, —OH or —NHR20 when the double-dashed line represents an absent bond; and other parameters are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing said compounds and their uses as thrombin receptor antagonists and binders to cannabinoid receptors.Type: GrantFiled: May 25, 2005Date of Patent: October 28, 2008Assignee: Schering CorporationInventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia, Martin C. Clasby, William J. Greenlee, Yuguang Wang, Enrico P. Veltri, Wenxue Wu, Michael P. Graziano, Teddy Kosoglou, Madhu Chintala