The Five-membered Nitrogen Hetero Ring Has Chalcogen As A Ring Member Patents (Class 514/253.1)
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Publication number: 20100022543Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: July 28, 2009Publication date: January 28, 2010Inventors: Lawrence S. Melvin, JR., Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20100022544Abstract: The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: ApplicationFiled: November 17, 2007Publication date: January 28, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Jörg Keldenich, Joachim Telser
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Publication number: 20100010007Abstract: Compounds of formula (I): compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).Type: ApplicationFiled: September 18, 2009Publication date: January 14, 2010Applicant: AstraZeneca ABInventors: Alan Faull, Howard Tucker
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Publication number: 20100004258Abstract: The present invention relates to compounds of the general formula (III): or pharmaceutically acceptable salts thereof with an acid or a base, or pharmaceutically acceptable prodrugs or a stereoisomer thereof.Type: ApplicationFiled: September 9, 2009Publication date: January 7, 2010Applicant: 4SC AGInventors: Johann LEBAN, Harald SCHMITT, Kristina WOLF, Stefano PEGORARO, Andreas WUZIK
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Publication number: 20090325924Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 29, 2006Publication date: December 31, 2009Inventors: Stuart Edward, Graham John Dawson, Matthew Colin Thor Fyfe Oxford, Lisa Sarah Bertram, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Neela Sumit Mistry, Martin James Procter, Chrystelle Marie Rasamison, Philip John Rushworth, Colin Peter Sambrook-Smith, David French Stonehouse
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Publication number: 20090318464Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.Type: ApplicationFiled: July 2, 2007Publication date: December 24, 2009Applicant: ASTRAZENECA ABInventors: Kay Brickmann, Fabrizio Giordanetto, Johan Johansson, Fredrik Zetterberg
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Patent number: 7625889Abstract: The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, R1 and R2 are as defined herein. The compounds of this invention are selective 5HT2A antagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.Type: GrantFiled: July 25, 2007Date of Patent: December 1, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: Paul Robert Eastwood, Hazel Hunt, David Mark Fink, Helen Katherine Smith, Richard Simon Todd
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Patent number: 7615550Abstract: The present invention relates to novel piperazine and azepine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurodegenerative disorders including Alzheimer's disease.Type: GrantFiled: October 14, 2003Date of Patent: November 10, 2009Assignee: Glaxo Group LimitedInventors: Thomas Daniel Heightman, Simon Teanby Hodgson, Matthew J Lindon, David Matthew Wilson
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Publication number: 20090275594Abstract: The present invention is directed to novel 3-hydrazone piperazinyl rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes.Type: ApplicationFiled: May 4, 2009Publication date: November 5, 2009Inventors: Mark J. MACIELAG, Manomi Tennakoon
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Publication number: 20090264405Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 30, 2006Publication date: October 22, 2009Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Patent number: 7601721Abstract: Disclosed are novel piperazine and piperazine derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, diabetes, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction.Type: GrantFiled: September 17, 2007Date of Patent: October 13, 2009Assignee: Gilead Palo Alto, Inc.Inventors: Jeff Zablocki, Dmitry Koltun
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Publication number: 20090247526Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: ApplicationFiled: January 24, 2007Publication date: October 1, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
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Patent number: 7592347Abstract: The present invention relates to novel piperidine carbonyl piperazine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders.Type: GrantFiled: April 21, 2004Date of Patent: September 22, 2009Assignee: Glaxo Group LimitedInventors: Gordon Bruton, Barry Sidney Orlek, Kishore Kalidas Rana
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Publication number: 20090215766Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: ApplicationFiled: August 6, 2008Publication date: August 27, 2009Inventors: James D. Rodgers, Darius J. Robinson, Argyrios G. Arvanitis, Thomas P. Maduskuie, JR., Stacey Shepard, Louis Storace, Haisheng Wang, Maria Rafalski, Ravi Kumar Jalluri, Andrew P. Combs, Matthew L. Crawley
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Publication number: 20090203676Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.Type: ApplicationFiled: June 30, 2006Publication date: August 13, 2009Inventors: Oscar Barba, Stuart Edward Bradley, Matthew Colin Thor Fyfe, Lisa Sarah Bertram, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Simon Andrew Swain
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Patent number: 7572786Abstract: This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.Type: GrantFiled: December 17, 2003Date of Patent: August 11, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Francois Maria Sommen, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20090176796Abstract: The invention relates to compounds of formula IA? and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: April 25, 2008Publication date: July 9, 2009Applicant: Purdue Pharma L. P.Inventor: Laykea Tafesse
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Publication number: 20090170868Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: April 25, 2008Publication date: July 2, 2009Applicant: Purdue Pharma L. P.Inventor: Laykea Tafesse
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Publication number: 20090170864Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.Type: ApplicationFiled: May 1, 2008Publication date: July 2, 2009Inventors: David Robert Bolin, Adrian Wai-Hing Cheung, Fariborz Firooznia, Matthew Michael Hamilton, Lee Apostle McDermott, Yimin Qian, Jenny Tan, Weiya Yun
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Publication number: 20090163508Abstract: An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.Type: ApplicationFiled: October 9, 2008Publication date: June 25, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masakuni KORI, Mitsunori Kouno
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Patent number: 7528134Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.Type: GrantFiled: May 23, 2003Date of Patent: May 5, 2009Assignee: Abbott Laboratories Inc.Inventors: Pramila A. Bhatia, Jerome F. Daanen, Ahmed A. Hakeem, Teodozyj Kolasa, Mark A. Matulenko, Kathleen H. Mortell, Meena V. Patel, Andrew O. Stewart, Xueqing Wang, Zhiren Xia, Henry Q. Zhang
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Publication number: 20090105271Abstract: The present invention relates to pyridyl sulfonamide derivatives useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: September 17, 2008Publication date: April 23, 2009Inventors: Esther Martinborough, Nicole Zimmermann, Timothy Neubert, Tara Hampton
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Publication number: 20090076009Abstract: The invention concerns thiazole derivatives of Formula I or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R1, R2 and R3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.Type: ApplicationFiled: May 2, 2007Publication date: March 19, 2009Inventors: Jean-Claude (Retired) Arnould, Kevin Michael Foote, Edward Jolyon Griffen
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Publication number: 20090062293Abstract: A compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1 represents a branched lower alkyl group having from 3 to 9 carbon atoms or the like; R2 represents a 6-membered heteroaryl group having 1 or 2 nitrogen atoms or the like; R3 represents a hydrogen atom, an alkanoylamino group or the like; R4 represents a hydrogen atom, a lower alkyl group or the like; X1 represents an oxygen atom or a sulfur atom; X2 represents an oxygen atom or a single bond; and m indicates an integer of from 0 to 4. This compound has a metabotropic glutamate receptor 1 inhibitory effect, and therefore is useful for the treatment of a brain disorder such as convulsion, acute pain, inflammatory pain, chronic pain, cerebral infraction or transient cerebral ischemic attack, a mental dysfunction such as schizophrenia, and a disease such as anxiety and drug addition.Type: ApplicationFiled: April 5, 2006Publication date: March 5, 2009Inventors: Hiroshi Kawamoto, Toshifumi Kimura, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
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Publication number: 20090048263Abstract: A compound represented by the formula (I) or a salt thereof; and an agent for protecting a brain/neuronal cell or a therapeutic agent for sleep disorder comprising the compound or salt: wherein Z represents an oxygen or sulfur; R1 represents an aryl or heterocyclic group which may be substituted, provided that R1 is not a 3-ethyl-6-methoxy-2-methyl-5-naphthalen-1-yl group; R1a represents a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxyl group or the like; R2 represents a piperidin-1,4-diyl or piperazin-1,4-diyl which may be substituted; R3 represents a bivalent group which is formed by removing two hydrogen atoms from a benzene ring or 6-membered aromatic heterocyclic ring which may have a substituent, provided that R3 is not a pyridazin-3,6-diyl; and R4 represents a group which is formed by removing one hydrogen atom from a benzene ring or 5- to 6-membered heterocyclic ring which may be substituted, provided that the substituent on the heterocyclic ring is not a phenylethyl group whicType: ApplicationFiled: August 11, 2006Publication date: February 19, 2009Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Takahiro Matsumoto, Masakuni Kori, Mitsunori Kouno
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Publication number: 20090028787Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.Type: ApplicationFiled: January 25, 2007Publication date: January 29, 2009Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
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Patent number: 7482346Abstract: The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.Type: GrantFiled: August 22, 2006Date of Patent: January 27, 2009Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Tak Adrien Li
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Patent number: 7482347Abstract: Compounds of formula I in free or salt form, wherein Ar, R1, R2, R3, X and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: August 9, 2005Date of Patent: January 27, 2009Inventor: Darren M Legrand
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Publication number: 20090018117Abstract: The disclosure relates to 2-carbamide-4-phenylthiazole derivatives having the following general formula (I): wherein R1, R2, R3, Y and p are as defined in the disclosure. The disclosure also relates to pharmaceutical compositions containing a compound of formula (I), to processes for preparing the compounds of formula (I), and to methods of using the compounds of formula (I).Type: ApplicationFiled: June 26, 2008Publication date: January 15, 2009Applicant: sanofi-aventisInventors: Pierre CASELLAS, Daniel FLOUTARD, Pierre FRAISSE, Stephane HOURCADE, Samir JEGHAM
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Publication number: 20080317671Abstract: Certain non-imidazole heterocyclic compounds are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: August 20, 2008Publication date: December 25, 2008Inventors: Nicholas I. Carruthers, Chandravadan R. Shah, Devin M. Swanson
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Publication number: 20080312246Abstract: The invention relates to compounds of formula I or pharmaceutically acceptable salts or solvates thereof: where Ar1, Ar2, Hy, L, R1, m and n are as defined in the description. The invention also includes pharmaceutical compositions and uses thereof, processes for making the compounds, as well as methods for the medical treatment of mGluR5-mediated disorders.Type: ApplicationFiled: August 4, 2006Publication date: December 18, 2008Applicant: AstraZeneca ABInventors: Louise Edwards, Abdelmalik Slassi, Methvin Isaac, Donald Mcleod, Tao Xin
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Publication number: 20080306083Abstract: The present invention relates to novel biaryl derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.Type: ApplicationFiled: December 1, 2006Publication date: December 11, 2008Inventors: Gregor James MacDonald, Darren Jason Mitchell, Mervyn Thompson, Susan Marie Westaway
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Publication number: 20080293733Abstract: Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.Type: ApplicationFiled: April 11, 2008Publication date: November 27, 2008Applicant: SUPERGEN, INC.Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu
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Publication number: 20080261971Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, (II) or (III) R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO2R6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl;Type: ApplicationFiled: July 29, 2005Publication date: October 23, 2008Inventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20080255141Abstract: Novel compounds selected from 2-(3-aminoaryl)amino-4-aryl-thiazoles of formula (I) that selectively modulate, regulate, and/or inhibit signal transductions mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferation metabolic, allergic and degenerative disorders. More particularly, these compounds are potent and selective c-kit inhibitors.Type: ApplicationFiled: July 18, 2007Publication date: October 16, 2008Inventors: Marco Ciufolini, Camille Wermuth, Bruno Gielthen, Alain Moussy
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Publication number: 20080221116Abstract: The present invention relates to isoxazolines useful as selective ?1a/?1d adrenoreceptor antagonists for the treatment of benign prostatic hypertrophy and/or lower urinary tract symptoms as well as to pharmaceutical compositions comprising said compounds, processes to prepare these compounds, and the use of these compounds as ?1a/?1d adrenoreceptor modulators in a method of treatment.Type: ApplicationFiled: September 14, 2007Publication date: September 11, 2008Inventors: Ellen W. Baxter, Samuel O. Nortey, Allen B. Reitz
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Patent number: 7419980Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.Type: GrantFiled: October 12, 2004Date of Patent: September 2, 2008Assignee: WyethInventors: Eugene John Trybulski, Paige Erin Mahaney, Lori Krim Gavrin, Joseph Peter Sabatucci, Gary Paul Stack
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Publication number: 20080207572Abstract: The present invention relates to a method for treating Multiple Myeloma (MM), FGFR3+ myeloma, especially relapsed or refractory multiple myeloma (4/14) expressing FGFR3, comprising administering a dual C-KIT/FGFR3 inhibitor, such as 2-aminoarylthiazoles and 2-aminoaryloxazoles.Type: ApplicationFiled: July 13, 2006Publication date: August 28, 2008Inventors: Alain Moussy, Jean-Pierre Kinet
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Publication number: 20080200405Abstract: The present invention is directed to compounds, compositions, and methods for halting or reversing the effects of chemoresistance in neoplastic diseases. In particular the use of hydroxylamines is described.Type: ApplicationFiled: February 15, 2008Publication date: August 21, 2008Inventors: Ghanshyam Patil, Shaker A. Mousa
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Publication number: 20080167309Abstract: The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): and salts, tautomers, N-oxides or solvates thereof, wherein A is a bond, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; Q is S or CR2; J is S or CH; provided that one of Q and J is S, and the other of Q and J is not S; when Q is S, there is a double bond between the ring carbon atoms “a” and “b” and a double bond between the ring nitrogen N and J; and when J is S, there is a double bond between Q and the ring carbon atom “a” and a double bond between the ring nitrogen N and the ring carbon atom “b”; and R1 to R4 are as defined in the claims.Type: ApplicationFiled: July 22, 2005Publication date: July 10, 2008Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio Berdini, Theresa Rachael Early, Michael Alistair O'Brien, Andrew James Woodhead, Paul Graham Wyatt
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Publication number: 20080167320Abstract: Compounds of the general formula (I) below: are provided along with a process for preparing them, and these compounds may be used as therapeutic agents, e.g., for prevention and/or treatment of a neuropsychiatric illness or any illness involving the dopamine D3 receptor.Type: ApplicationFiled: March 7, 2008Publication date: July 10, 2008Inventors: Marc Capet, Denis Danvy, Nicolas Levoin, Marcel Morvan, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jean-Charles Schwartz, Jeanne-Marie Lecomte
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Patent number: 7393845Abstract: A heteroaryl derivative having the formula (I).Type: GrantFiled: June 5, 2007Date of Patent: July 1, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen
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Publication number: 20080146585Abstract: The present invention relates to a method for treating inflammatory muscle disorders including myositis and muscular dystrophy comprising administering a compound capable of depleting mast cells or a compound inhibiting mast cell degranulation, to a human in need of such treatment. Such compounds can be chosen from c-kit inhibitors and more particularly non-toxic, selective and potent c-kit inhibitors. Preferably, said inhibitor is unable to promote death of IL-3 dependent cells cultured in presence of IL-3.Type: ApplicationFiled: April 19, 2005Publication date: June 19, 2008Inventors: Alain Moussy, Jean-Pierre Kinet
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Patent number: 7384944Abstract: The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v.Type: GrantFiled: September 23, 2003Date of Patent: June 10, 2008Assignee: Schering CorporationInventors: Bahige M. Baroudy, John W. Clader, Hubert B. Josien, Stuart W. McCombie, Brian A. McKittrick, Michael W. Miller, Bernard R. Neustadt, Anandan Palani, Elizabeth M. Smith, Ruo Steensma, Jayaram R. Tagat, Susan F. Vice, Mark A. Laughlin, Eric Gilbert, Marc A. Labroli
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Publication number: 20080108600Abstract: The present invention provides a genus of polycyclic pyridines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and diagnostic methods.Type: ApplicationFiled: April 13, 2005Publication date: May 8, 2008Applicants: Icagen, Inc., Astellas Parma Inc.Inventors: Xiaodong Wang, Kerry L. Spear, Alan B. Fulp, Darrick Seconi, Takeshi Suzuki, Takahiro Ishii, Ayako Moritomo, Hideki Kubota, Jun-ichi Kazami
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Patent number: 7361654Abstract: The present invention relates to new class of non-steroidal compounds which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory- and immune-associated diseases, and have the structure including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, wherein X is selected from N, O, and S; Y is N or CR6; Z is a ring; and where R, Ra, Rb, Rc, Rd, R1, R2, R3, R4, and R5 are as defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising such compounds.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Bristol-Myers Squibb Co.Inventors: James Sheppeck, T. G. Murali Dhar, Lidia Doweyko, John Gilmore, David Weinstein, Hai-Yun Xiao, Bingwei V. Yang, Arthur M. Doweyko
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Publication number: 20080064689Abstract: Compounds of the formula (I): or a pharmaceutically-acceptable salt or pro-drug thereof: wherein R1 is selected for example from hydrogen, halogen, optionally substituted methyl; R2 and R3 are independently selected from hydrogen, fluoro, chloro and trifluoromethyl; R4 and R5 are independently selected, for example, from hydrogen, methyl, optionally substituted (2-4C)alkyl, C(O)R6 or R4 and R5 together with the nitrogen to which they are attached form an optionally substituted 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring or an optionally substituted imidazole ring. Methods for making the compounds of formula (I), compositions containing them and their use as antibacterial agents are also described.Type: ApplicationFiled: May 24, 2004Publication date: March 13, 2008Applicant: AstraZeneca ABInventors: Daniel Robert Carcanague, Michael Barry Gravestock
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Patent number: 7300939Abstract: Substituted 1-propiolylpiperazine compounds corresponding to formula I in which X denotes N or C—R2, and n is an integer from 0 to 8, a method for producing such substituted 1-propiolylpiperazine compounds, pharmaceutical compositions containing such substituted 1-propiolylpiperazine compounds, and the use of such substituted 1-propiolylpiperazine compounds for modulating mGluR5 receptor activity or for treating or inhibiting pain and various other conditions, especially conditions at least partly mediated by the mGluR5 receptor.Type: GrantFiled: January 4, 2007Date of Patent: November 27, 2007Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Stefan Oberboersch, Michael Haurand, Ruth Jostock, Klaus Schiene
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Patent number: 7297693Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.Type: GrantFiled: September 5, 2002Date of Patent: November 20, 2007Assignee: SmithKline Beecham P.L.C.Inventors: Mark James Bamford, David Kenneth Dean, Antoinette Naylor, Andrew Kenneth Takle, David Matthew Wilson
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Publication number: 20070173501Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: January 23, 2007Publication date: July 26, 2007Applicant: ALLERGAN, INC.Inventors: Xialing Guo, Zhen Zhu, Thomas C. Malone