Nitrogen Attached Indirectly To The Morpholine Ring By Acyclic Nonionic Bonding Patents (Class 514/237.8)
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Patent number: 7632836Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.Type: GrantFiled: November 28, 2007Date of Patent: December 15, 2009Assignee: CeNeRx Biopharma, Inc.Inventor: Michael Rafferty
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Patent number: 7632835Abstract: The present invention relates to morpholine and thiomorpholine derivatives or the general formula I or pharmaceutically acceptable salts thereof and their use.Type: GrantFiled: January 28, 2009Date of Patent: December 15, 2009Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornoe, Mario Rottlander, Nikolay Khanzhin, Andreas Ritzen, William Patrick Watson
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Publication number: 20090306078Abstract: Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.Type: ApplicationFiled: July 3, 2007Publication date: December 10, 2009Applicant: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGYInventors: Jung Joon Lee, Jeong-Hyung Lee, Kyeong Lee, Young-Soo Hong, B.K. Shanthaveerappa, Yinlan Jin, Jin Hwan Kim, Xuejun Jin
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Publication number: 20090306077Abstract: The present invention relates to a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork cells and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pressure. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group, or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group, or the like; l and m represent 0, 1, 2, or the like.Type: ApplicationFiled: December 26, 2007Publication date: December 10, 2009Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Publication number: 20090306079Abstract: There are disclosed compounds of the formula or a pharmaceutically acceptable salt or solvate thereof which are useful for the treatment of chemokine-mediated diseases such as acute and chronic inflammatory disorders and cancer.Type: ApplicationFiled: January 13, 2009Publication date: December 10, 2009Inventors: Arthur G. Taveras, Cynthia J. Aki, Richard W. Bond, Jianping Chao, Michael Dwyer, Johan A. Ferreira, Jianhua Chao, Younong Yu, John J. Baldwin, Bernd Kaiser, Ge Li, J. Robert Merritt, Purakkattle J. Biju, Kingsley H. Nelson, JR., Laura L. Rokosz, Gaifa Lai, James P. Jakway, Minglang Wu, Evan A. Hecker, Daniel Lundell, Jay S. Fine
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Patent number: 7619115Abstract: Novel ortho-substituted N?-benzylidene-(3-hydroxyphenyl)acetohydrazides of the formula (I), in which R1-R9 have the meanings indicated in claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.Type: GrantFiled: June 6, 2005Date of Patent: November 17, 2009Assignee: Merck Patent GmbHInventors: Rolf Gericke, Dieter Dorsch, Werner Mederski, Norbert Beier, Florian Lang
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Publication number: 20090275583Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection.Type: ApplicationFiled: April 13, 2009Publication date: November 5, 2009Applicant: Myriad Genetics, IncorporatedInventors: Kraig Yager, In Chul Kim, Michael Saunders, David Gerrish, Dange Vijay Kumar, Mark B. Anderson
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Publication number: 20090253701Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: ApplicationFiled: June 12, 2009Publication date: October 8, 2009Inventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, holger Sellner
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Publication number: 20090247522Abstract: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.Type: ApplicationFiled: April 22, 2009Publication date: October 1, 2009Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Shinji Nara, Hiroshi Nakagawa, Yutaka Kanda, Takayuki Nakashima, Shiro Soga, Jiro Kajita, Jun-ichi Saito, Yukimasa Shiotsu, Shiro Akinaga
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Publication number: 20090233909Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: ApplicationFiled: December 1, 2005Publication date: September 17, 2009Applicant: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Publication number: 20090209474Abstract: The present invention relates to novel therapeutic uses of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof. Furthermore, the present invention relates to the use of tianeptine, salts, isomers, pro-drugs, metabolites and structural analogs thereof, in obtaining methods of screening and of developing drugs. Finally, the present invention relates to the novel therapeutic use of other glutamine synthetase (GS) ligands and to the use of these ligands in obtaining methods for screening and developing drugs.Type: ApplicationFiled: August 8, 2006Publication date: August 20, 2009Applicant: NEWTHERAInventors: Jean-Christophe Roegel, Pierre Eftekhari
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Publication number: 20090203681Abstract: The present invention provides novel compounds of the general formula (I) and pharmaceutically acceptable salts thereof, processes for the manufacture of these novel compounds and medicaments containing such compounds. The compounds of the present invention show anti-proliferative and differentiation-inducing activity, which results in inhibition of tumor cell proliferation, induction of apoptosis and inhibition of invasion. The invention also covers the use of such compounds for the treatment of diseases such as cancer and for the manufacture of corresponding medicaments.Type: ApplicationFiled: January 23, 2009Publication date: August 13, 2009Inventors: Li Chen, Yun He, Jason Christopher Wong
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Patent number: 7572790Abstract: Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.Type: GrantFiled: April 7, 2004Date of Patent: August 11, 2009Assignee: SmithKline Beecham CorporationInventors: Nicola Mary Aston, Paul Bamborough, Katherine Louise Jones, Vipulkumar Kantibhai Patel, Stephen Swanson, Ann Louise Walker
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Patent number: 7566789Abstract: Novel compounds of the formula I in which D, X, X?, W, Y, T and R1 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.Type: GrantFiled: July 4, 2003Date of Patent: July 28, 2009Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Wrner Mederski, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20090176786Abstract: The present invention relates to a benzoylurea compound represented by formula (I): wherein, X and Y represent a fluorine atom or a chlorine atom, R1 represents a lower alkyl group or the like, R2 represents a lower alkyl group, R3 represents a halogen atom or the like, R4 represents an alkylthio group optionally substituted with one or more of halogen atoms, or a salt thereof, and use thereof for controlling pests and the like.Type: ApplicationFiled: October 16, 2006Publication date: July 9, 2009Inventors: Masato Konobe, Shigeyuki Itoh, Norihisa Sakamoto, Araki Tomohiro, Yoshitomo Tohyama
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Publication number: 20090176773Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.Type: ApplicationFiled: May 18, 2006Publication date: July 9, 2009Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer
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Publication number: 20090163496Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: October 30, 2007Publication date: June 25, 2009Applicant: UNIVERSITY OF WASHINGTONInventors: Niels H. ANDERSEN, Jason BOWMAN
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Patent number: 7544716Abstract: This invention relates to tetrahydro-naphthalene derivatives of formula (I) in which the variable groups are as defined in the specification and claims, and tautomeric and stereoisomeric forms and salts thereof which are useful as active ingredients of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonists and are useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, urge urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD. The compounds, pharmaceutical compositions containing them, and methods of treatment using them are disclosed and claimed.Type: GrantFiled: November 28, 2003Date of Patent: June 9, 2009Assignee: Xention LimitedInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Patent number: 7544676Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.Type: GrantFiled: November 9, 2006Date of Patent: June 9, 2009Assignee: Adolor CorporationInventors: Roland E. Dolle, Karin Worm
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Publication number: 20090131441Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: January 24, 2006Publication date: May 21, 2009Applicant: DOMPE phar.r.ma S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
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Patent number: 7531651Abstract: Compounds of formula (I): wherein A? represents the benzenesulphonate (besylate) anion;. R represents H or C1-6 alkyl; and n is a number from 0.8 to 2.2 are CCR3 antagonists and are therefore indicated to be useful in therapy are described.Type: GrantFiled: March 27, 2003Date of Patent: May 12, 2009Assignee: Glaxo Group LimitedInventors: John Spencer Cook, Robert Philip Landon, Andrew John Walker, Mark Wilkinson
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Patent number: 7531538Abstract: ?- and ?-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 15, 2006Date of Patent: May 12, 2009Assignee: G.D. Searle LLCInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Publication number: 20090118288Abstract: The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) mediated disease state.Type: ApplicationFiled: July 19, 2006Publication date: May 7, 2009Applicant: ASTRAZENECA ABInventors: Christopher Luckhurst, Brian Springthorpe
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Publication number: 20090118268Abstract: This invention relates to the use of a group of aryl ureas in treating p38 mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: October 10, 2008Publication date: May 7, 2009Inventors: Bernd Riedl, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, Mary-Katherine Monahan, Reina Natero, Joel Renick, Robert N. Sibley
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Patent number: 7528131Abstract: This disclosure relates to novel substituted morpholinyl compounds and their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a 5HT4 serotonin receptor agonist.Type: GrantFiled: April 18, 2008Date of Patent: May 5, 2009Assignee: Concert Pharmaceuticals Inc.Inventors: Rose A. Persichetti, Scott L. Harbeson
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Publication number: 20090111813Abstract: The present embodiments are related to the compound of Formula 1 or Formula 2 below and pharmaceutical formulations thereof as well as treatments for a wide variety of Central Nervous System disorders with the pharmaceutical formulations. Some embodiments include the use of a variety of the instant compounds which surprisingly and advantageously exhibit improved pharmacokinetic and therapeutic profiles in comparison to pivagabine.Type: ApplicationFiled: November 28, 2007Publication date: April 30, 2009Applicant: CeNeRx Biopharma, Inc.Inventor: Michael Rafferty
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Publication number: 20090111812Abstract: The present invention relates generally to the fields of molecular biology. More particularly, it concerns materials and methods for the treatment of nitric oxide and cytokind mediated disorders. In a preferred embodiment, PDMP may be used to inhibit the expression of iNOS and pro-inflammatory cytokines such as TNF? and IL1?.Type: ApplicationFiled: June 13, 2005Publication date: April 30, 2009Applicant: MUSC Foundation for Research DevelopmentInventors: Inderjit Singh, Avtar Singh
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Publication number: 20090105258Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salt thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, and heart disease.Type: ApplicationFiled: March 15, 2006Publication date: April 23, 2009Applicant: AMOREPACIFIC CORPORATIONInventors: Hee-Doo Kim, Young-Ger Suh, Hyeung-Geun Park, Uh Taek Oh, Seol Rin Park, Joo Hyun Kim, Mi Jung Jang, Young-Ho Park, Song Seok Shin, Sun-Young Kim, Jin Kwan Kim, Yeon Su Jeong, Ki-Wha Lee, Jin Kyu Choi, Kyung Min Lim, Hyun Ju Koh, Joo Hyun Moh, Sung-II Kim, Byoung Young Woo
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Publication number: 20090105257Abstract: The present invention relates generally to novel therapeutic compounds and more particularly to novel compounds, their use as GPR40 agonists, processes for their manufacture, and intermediates useful in their preparation.Type: ApplicationFiled: November 15, 2004Publication date: April 23, 2009Inventors: David Francis Corbett, Kate Anna Dwornik, Dulce Maria Garrido, Stephen Carl McKeown, Wendy Yoon Mills, Andrew James Peat, Terrence Lee Smalley, JR.
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Patent number: 7517880Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: GrantFiled: February 1, 2002Date of Patent: April 14, 2009Assignee: Bayer Pharmaceuticals CorporationInventors: Scott Miller, Martin Osterhout, Jacques Dumas, Uday Khire, Timothy B. Lowinger, William J. Scott, Roger A. Smith, Jill E. Wood, David E. Gunn, Holia Hatoum-Mokdad, Marell Rodriguez, Robert Sibley, Ming Wang, Tiffany Turner, Catherine Brennan
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Publication number: 20090093483Abstract: Compounds of Formula I and Formula II are useful as inhibitors of HIF prolyl hydroxylases. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: ApplicationFiled: December 17, 2007Publication date: April 9, 2009Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Marian C. Bryan, Roland Burli, Guo-Qiang Cao, Michael J. Frohn, Jennifer E. Golden, Stephanie Mercede, Susana Neira, Tanya Peterkin, Alexander J. Pickrell, Anthony Reed, Christopher M. Tegley, Xiang Wang
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Publication number: 20090088433Abstract: The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment.Type: ApplicationFiled: January 25, 2006Publication date: April 2, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello, Fabien (Jacques) Schweighoffer
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Patent number: 7501414Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: GrantFiled: December 21, 2005Date of Patent: March 10, 2009Assignee: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzèn, William Patrick Watson
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Publication number: 20090062286Abstract: The invention relates to SMYD3 methyltransferase (SMYD3), SMYD3 binding pockets or SMYD3-like binding pockets. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to SMYD3 methyltransferase protein, complexes of SMYD3 methyltransferase protein, homologues thereof, or SMYD3-like protein or protein complexes.Type: ApplicationFiled: May 5, 2008Publication date: March 5, 2009Inventors: Kenneth William Foreman, Frances E. Park, Lee Arnold
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Publication number: 20090062287Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, and ring B are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: November 7, 2008Publication date: March 5, 2009Inventors: James R. Corte, Mimi L. Quan, Joanne M. Smallheer, Donald J. Pinto
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Publication number: 20090048233Abstract: Provided are combinations of pharmaceutical agents capable of eliciting a therapeutic effect. A first therapeutic agent in the combination has 5HT2/5HT3 antagonist and alpha-2 antagonist activity. A second therapeutic agent possesses both serotonin reuptake inhibitory activity and norepinephrine reuptake inhibitory activity or is a reversible inhibitor of monoamine oxidase A (RIMA). In some embodiments, a combination of a first therapeutic agent and a second therapeutic agent results in reduction in one or deleterious side effects associated with the first therapeutic agent, the second therapeutic agent or both. Also provided are methods of treatment employing a first therapeutic agent and a second therapeutic agent. Also provided are kits containing a first therapeutic agent, a second therapeutic agent and instructions for administering the first therapeutic agent and the second therapeutic agent.Type: ApplicationFiled: August 15, 2008Publication date: February 19, 2009Applicant: CYPRESS BIOSCIENCES, INC.Inventors: Srinivas RAO, Jay Kranzler, Jeffery J. Anderson
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Publication number: 20090042855Abstract: In one aspect, the invention relates to compounds, including phenylethynylbenzamide derivatives, cycloalkylethynylbenzamide derivatives, styrylbenzamide derivatives, 4-(3-phenyl-1,2,4-oxadiazol-5-yl)benzamide derivatives, 4-(pyridinylethynyl)benzamide derivatives, and N1-phenylterephthalamide derivatives, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: June 3, 2008Publication date: February 12, 2009Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20090042883Abstract: The present invention provides a therapeutic agent for a tumor selected from a hematopoietic tumor and a solid tumor which comprises, as an active ingredient, a benzoyl compound represented by General Formula (I): (wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; R3 and R5 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl or the like; R4 represents a hydrogen atom, hydroxy or halogen; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl or the like), a prodrug thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: February 21, 2006Publication date: February 12, 2009Applicant: KYOWA HAKKOKOGYO CO.Inventors: Yutaka Kanda, Shiro Soga, Takayuki Nakashima, Shinji Nara, Hiroshi Nakagawa, Yukimasa Shiotsu
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Publication number: 20090036420Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Publication number: 20090029999Abstract: This invention provides compounds having the structural formula: wherein: R1 is an acyl or sulfonyl group, R2 is an acyl group selected from the group consisting of acyl groups derived from cycloaliphatic, aromatic or heterocyclic monocarboxylic acids, imidazolylcarbonyl and triazolylcarbonyl, and R3 is hydrogen or an amino-protecting group, a stereoisomer thereof, a solvate thereof, or a salt thereof, being useful as anti-inflammatory agents and anti-cancer agents.Type: ApplicationFiled: June 23, 2008Publication date: January 29, 2009Applicant: UNIVERSITEIT GENTInventors: Wim VANDEN BERGHE, Karolien DE Bosscher, Serge Van Calenbergh, Guy Haegeman, Carl Jeffrey Lacey, Valerie Gossye, Ruben Hoya Arias, Sarah Gerlo
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Publication number: 20090023730Abstract: The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: February 25, 2008Publication date: January 22, 2009Applicant: ACHILLION PHARMACEUTICALSInventors: Avinash Phadke, Dawei Chen, Milind Deshpande, Andrew Thurkauf, Xiangzhu Wang, Yiping Shen, Cuixian Liu, Jesse Quinn, Junko Ohkanda, Shouming Li
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Publication number: 20090023731Abstract: Disclosed are urea and thiourea compounds and compositions that inhibit soluble epoxide hydrolase (sEH), methods for preparing the compounds and compositions, and methods for treating patients with such compounds and compositions. The compounds, compositions, and methods are useful for treating a variety of sEH mediated diseases, including hypertensive, cardiovascular, inflammatory, and diabetic-related diseases.Type: ApplicationFiled: March 21, 2008Publication date: January 22, 2009Inventors: Richard D. Gless, JR., Sampath Kumar Anandan
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Publication number: 20090023734Abstract: The invention provides compounds and methods for treating cell proliferative diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.Type: ApplicationFiled: January 8, 2007Publication date: January 22, 2009Applicant: METHYLGENE INC.Inventors: Stephane Raeppel, Frederic Gaudette, Isabelle Paquin, Arkadii Vaisburg, Daniel Delorme
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Patent number: 7476672Abstract: This invention is directed to acetylenic compounds as inhibitors of a nicotinamide adenine dinucleotide oxidase hydride donor useful in treating or ameliorating a reactive oxygen species mediated inflammatory disorder.Type: GrantFiled: January 10, 2006Date of Patent: January 13, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: Scott Beers, Elizabeth A. Malloy, Michael P. Wachter
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Publication number: 20090012090Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: ApplicationFiled: September 10, 2008Publication date: January 8, 2009Inventors: Matthias Friebe, Peter Muschick, Andreas Huth
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Publication number: 20080317883Abstract: The present invention is a method for the treatment of depression comprising administering to a subject in need thereof a therapeutically effective amount of one or more carbamate compounds of Formula 1 and/or Formula 2 as herein defined and shown below for the treatment of depression. The present invention is directed to a method for the treatment of depression, which includes mono-therapy and alternatively, co-therapy with at least one additional antidepressant.Type: ApplicationFiled: October 22, 2007Publication date: December 25, 2008Inventors: Yong Moon Choi, Robert Gordon, Magali Haas, Ewa Malatynska
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Publication number: 20080318957Abstract: Disclosed are compounds having polybasic functionalities. The compounds inhibit bacterial efflux pump inhibitors and are used in combination with an anti-bacterial agent to treat or prevent bacterial infections. These combinations can be effective against bacterial infections that have developed resistance to anti-bacterial agents through an efflux pump mechanism.Type: ApplicationFiled: May 6, 2008Publication date: December 25, 2008Applicant: Mpex Pharmaceuticals, Inc.Inventors: TOMASZ GLINKA, Olga Lomovskaya, Keith Bostian, David M. Wallace
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Publication number: 20080311074Abstract: A method of inhibiting NF-?B activation in a mammal including a human, which comprises the step of administering an effective dose of a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof:Type: ApplicationFiled: April 11, 2008Publication date: December 18, 2008Applicant: INSTITUTE OF MEDICAL MOLECULAR DESIGN INC.Inventors: Susumu MUTO, Akiko ITAI
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Publication number: 20080312236Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and or immunostimulant effect in mammals.Type: ApplicationFiled: January 25, 2006Publication date: December 18, 2008Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Publication number: 20080306054Abstract: The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; C1-5 hydrocarbyl and C1-5 hydrocarbyloxy; wherein the C1-5 hydrocarbyl and C1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C1-2 alkoxy, amino, mono- and di-C1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C1-5 hydrocarbyl-amino, wherein the acyclic C1-5 hydrocarbyl group and the mono and di-C1-5 hydrocarbylamino moieties in each instance are optionally substitType: ApplicationFiled: April 13, 2006Publication date: December 11, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead