Patents Issued in August 21, 2008
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Publication number: 20080200486Abstract: The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound, and b) an mTOR kinase inhibitor and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: July 19, 2006Publication date: August 21, 2008Inventors: Heidi Lane, Paul W. Manley
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Publication number: 20080200487Abstract: Salts of 4-methyl-N-[3-(4-methyl-imidazol-1-yl)-5-trifluoromethyl-phenyl]-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-benzamide are prepared by various processes.Type: ApplicationFiled: July 18, 2006Publication date: August 21, 2008Inventors: Paul W. Manley, Wen-Chung Shieh, Paul Allen Sutton, Piotr H. Karpinski, Raeann Wu, Stephanie Monnier, Jorg Brozio
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Publication number: 20080200488Abstract: The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound; and b) an HSP90 inhibitor, and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: August 10, 2006Publication date: August 21, 2008Inventors: Paul W. Manley, Kapil N. Bhalla
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Publication number: 20080200489Abstract: The invention provides a pharmaceutical combination comprising: a) a pyrimidylaminobenzamide compound; and b) an HDAC inhibitor compound, and a method for treating or preventing a proliferative disease using such a combination.Type: ApplicationFiled: August 10, 2006Publication date: August 21, 2008Inventors: Peter Wisdom Atadja, Kapil N. Bhalla, Paul W. Manley
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Publication number: 20080200490Abstract: This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 and R4 independently represents hydrogen or the like; R5 represents aryl or the like; —X—Y— represents —CH2O— or the like; and n represents 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.Type: ApplicationFiled: June 9, 2006Publication date: August 21, 2008Inventors: Yoshinobu Hashizume, Masako Hirota, Sachiko Mihara, Hiroshi Nakamura, Hiroki Koike, Yukari Matsumoto
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Publication number: 20080200491Abstract: The present invention relates to certain 1,2-dihydro-spiro[3H-indole-3,4?-piperidine]compounds of Formula (Ia): and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein G, R1, R2, R3, R4, R5, and Ar are as disclosed herein (“Compound(s) of the Invention”), which are useful, for example, as cardio-protective and/or neuro-protective agents. The invention also provides pharmaceutical compositions comprising a Compound of the Invention and methods for treating, preventing and/or managing a vascular, cardiovascular or neurological disease or disorder, comprising administering to a patient in need thereof a Compound of the Invention.Type: ApplicationFiled: June 21, 2006Publication date: August 21, 2008Inventors: Thuy-Anh Tran, Sangdon Han, P. Douglas Boatman
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Publication number: 20080200492Abstract: The present invention is directed to methods for the treatment of alcohol abuse, addiction and/or dependency, alone and in combination with one or more anti-addiction agents.Type: ApplicationFiled: November 15, 2007Publication date: August 21, 2008Inventor: Anil H. VAIDYA
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Publication number: 20080200493Abstract: It is possible to effectively treat moderate to severe visceral pain by administering analgesic medications comprising the opioid oxycodone or pharmaceutically acceptable salts thereof. Visceral pain and especially acute (i.e. non-chronic) visceral pain can be effectively treated by administering oxycodone at a dosage which is lower than the corresponding dosage of other opioids like morphine.Type: ApplicationFiled: January 17, 2006Publication date: August 21, 2008Applicant: EURO-CELTIQUE S.A.Inventors: Asbjorn Mohr Drewes, Lars Arendt Nielsen
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Publication number: 20080200494Abstract: The invention provides imidazopyridine derivatives represented by the general formula [I] [in which R1 and R2 may be the same or different and stand for C1-6 alkyl or the like, R3 and R4 stand for hydrogen atom, methyl group or the like, W stands for mono- or bi-cyclic 3- to 8-membered aromatic or aliphatic heterocycle or the like, and Ar stands for optionally substituted aromatic heterocycle or the like]. These compounds act as melanin-concentrating hormone receptor antagonist and are useful as medicines for central nervous system disorders, cardiovascular system disorders and metabolic disorders.Type: ApplicationFiled: August 13, 2004Publication date: August 21, 2008Inventors: Hiroyuki Kishino, Minoru Moriya, Toshihiro Sakamoto, Hidekazu Takahashi, Shunji Sakuraba, Takao Suzuki, Akio Kanatani
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Publication number: 20080200495Abstract: Pyrrolopyridine compounds corresponding to formula (I): as defined in the claims, pharmaceutically acceptable salts thereof, the process for preparing such compounds, pharmaceutical compositions containing such compounds, and their use as pharmacologically active substances, especially in the treatment of hypertriglyceridemia, hyperlipidemia, hypercholesterolemia, diabetes, endothelial dysfunction, cardiovascular diseases, inflammatory diseases and neurodegenerative diseases.Type: ApplicationFiled: February 29, 2008Publication date: August 21, 2008Applicant: LABORATOIRES FOURNIER S.A.Inventors: Benaissa Boubia, Martine Barth, Jean Binet, Pierre Dodey, Christiane Legendre, Olivia Poupardin-Olivier
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Publication number: 20080200496Abstract: The present invention discloses and claims compounds of formula (I) wherein M is N, and K and L are each C with the remaining substituents further defined herein. These compounds are effective as inhibitors of human casein kinase I?, and as such are useful in the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.Type: ApplicationFiled: April 21, 2008Publication date: August 21, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: William A. METZ, Frank HALLEY, Gilles DUTRUC-ROSSET, Yong Mi CHOI-SLEDESKI, Gregory Bernard POLI, David Marc FINK, Gilles DOERFLINGER, Bao-Guo HUANG, Ann Marie GELORMINI, Juan Antonio GAMBOA, Andrew GIOVANNI, Joachim E. ROEHR, Joseph T. TSAY, Fernando CAMACHO, William Joseph HURST, Stephen Wayne HARNISH, Yulin CHIANG
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Publication number: 20080200497Abstract: The compounds of formula I wherein R1, R2, R3, R4 and R5 are defined herein, are useful as inhibitors of the hepatitis C virus NS3 protease The invention further relates to azalactone compounds of the formula (II) which can be reacted with an amide anion to produce the HCV NS3 protease inhibitors of formula (I)Type: ApplicationFiled: July 17, 2006Publication date: August 21, 2008Inventors: Murray D. Bailey, Pasquale Forgione, Montse Llinas-Brunet, Marc-Andre Poupart
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Publication number: 20080200498Abstract: The invention relates to the use of a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof for the manufacture of a medicament for the for the treatment of sexual desire disorders.Type: ApplicationFiled: July 6, 2006Publication date: August 21, 2008Inventors: Angelo Ceci, Klaus Mendla
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Publication number: 20080200499Abstract: The present invention relates to the use of selective insecticidal and/or acaricidal compositions, characterized in that they comprise an effective amount of an active compound combination comprising (a) at least one substituted cyclic dicarbonyl compound of the formula (I) in which W, X, Y and Z are as defined in the description and CDC is one of the dicarbonyl radicals mentioned in the description, and (b) at least one crop plant compatibility-improving compound from the group of compounds given in the description. for controlling insects and/or arachnids, and also to a method for controlling insects and/or arachnids using the compositions.Type: ApplicationFiled: July 18, 2005Publication date: August 21, 2008Inventors: Reiner Fischer, Udo Reckmann, Chris Rosinger, Erich Sanwald, Christian Arnold
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Publication number: 20080200500Abstract: Compounds of Formula I wherein R1, A, R2, n, R3, m, R5 and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: May 30, 2006Publication date: August 21, 2008Applicant: AstraZeneca ABInventors: Thomas R. Simpson, James Kang, S. Jeffrey Albert, Cristobal Alhambra, M. Gerard Koether, M. James Woods, Yan Li
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Publication number: 20080200501Abstract: The present invention relates to novel cannabinoid receptor modulators, in particular cannabinoid 1 (CB1) or cannabinoid 2 (CB2) receptor modulators, and uses thereof for treating diseases, conditions and/or disorders modulated by a cannabinoid receptor (such as pain, neurodegenative disorders, eating disorders, weight loss or control, and obesity).Type: ApplicationFiled: November 2, 2007Publication date: August 21, 2008Applicant: Glenmark Pharmaceuticals S.A.Inventors: Meyyappan Muthuppalaniappan, Kumar Sukeerthi, Gopalan Balasubramanian, Srinivas Gullapalli, Neelima Khairatkar Joshi, Shridhar Narayanan, Pallavi V. Kamik
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Publication number: 20080200502Abstract: This invention relates to methods for lowering lipid levels in mammals using compounds that inhibit advanced glycation endproducts (AGEs), LR-9, LR-74 and LR-90. These compounds, which inhibit non-enzymatic protein glycation, also inhibit the formation of advanced lipoxidation endproducts (ALES) on target proteins by trapping intermediates in glycoxidation and lopoxidation and inhibiting oxidation reactions important in the formation of AGEs and ALEs.Type: ApplicationFiled: November 30, 2007Publication date: August 21, 2008Applicant: City of HopeInventors: Samuel RAHBAR, James L. FIGAROLA
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Publication number: 20080200503Abstract: Inhibitors of HCV of formula (I). and the N-oxides, salts, and stereoisomers thereof, wherein the dashed line represents an optional double bond between atoms C7 and C8; R1 is hydrogen or C1-6alkyl; R2 is hydrogen or C1-6alkyl; and n is 3, 4, 5, or 6; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I) are provided. Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.Type: ApplicationFiled: July 27, 2006Publication date: August 21, 2008Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Mats Stefan Lindstrom, Pia Cecilia Kahnberg, Dmitry Antonov, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist
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Publication number: 20080200504Abstract: Compounds of Formula (I) wherein R1, A, R2, R3, R4, R5,n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.Type: ApplicationFiled: August 9, 2006Publication date: August 21, 2008Applicant: AstraZeneca ABInventors: Jeffrey S. Albert, Cristobal Alhambra, James Kang, Gerard M. Koether, Thomas R. Simpson, James Woods, Yan Li
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Publication number: 20080200505Abstract: 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) or H1 mediated disease state.Type: ApplicationFiled: May 24, 2006Publication date: August 21, 2008Applicant: ASTRAZENECA ABInventors: Matthew Perry, Brian Springthorpe
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Publication number: 20080200506Abstract: The present invention discloses an oral preparation of dyclonine hydrochloride for the endoscope examination in upper gastrointestinal tract, which has the effects of anaesthetization and lubrication, and especially an oral preparation comprising dyclonine hydrochloride that has the advantages of avoiding the foam in the body cavity, preventing vomit, and offering a clear view. The preparation of the present invention comprises, as main ingredients, 0.2%-3% weight percent of dyclonine hydrochloride, 1%-12% weight percent of polyvinyl alcohol, 1%-10% volume percent of glycerin, 1%-10% volume percent of a defoaming agent, and a balance of a pharmaceutically acceptable adjuvant. The viscosity of the preparation is in a range of 30 to 300 mpa·s and the pH value is in a range of 2.0 to 8.0.Type: ApplicationFiled: January 13, 2004Publication date: August 21, 2008Inventors: Tianjiang Sun, Xiaohong Gu, Hongguo Lu, Min Chen
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Publication number: 20080200507Abstract: The present invention relates to the mesylate salt of 1-(4-(2-piperidinylethoxy)phenoxy)-2-(3-hydroxyphenyl)-6-hydroxynaphthalene.Type: ApplicationFiled: July 27, 2006Publication date: August 21, 2008Inventor: Jeanette Tower Dunlap
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Publication number: 20080200508Abstract: Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep.Type: ApplicationFiled: December 20, 2005Publication date: August 21, 2008Applicant: COLLEGIUM PHARMACEUTICAL, INC.Inventors: Roman V. Rariy, Michael Heffernan
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Publication number: 20080200509Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, 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; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: October 19, 2007Publication date: August 21, 2008Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Theresa Rachel Early, Adrian Liam Gill, Gary Trewartha, Alison Jo-Anne Woolford, Andrew James Woodhead, Paul Graham Wyatt
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Publication number: 20080200510Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, comprising of a DPP IV inhibitor or a pharmaceutically acceptable salt thereof and comprising at least one CB1 antagonist, or a pharmaceutically acceptable salt thereof. The present invention furthermore relates to the use of such a combination for the prevention of, delay of progression of, treatment of diseases and disorders that may be inhibited by DPP IV inhibition, appetency disorders or substance abuse disorders.Type: ApplicationFiled: July 11, 2006Publication date: August 21, 2008Inventor: Smiljana Milosavljevic-Ristic
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Publication number: 20080200511Abstract: The present invention relates to novel compounds of Formula (I) wherein ‘X’ represents an amino acid group, ‘n’ is an integer between 1 and 4, ‘R1’ represents benzyl, t-butyl or 9-fluorenylmethyl and ‘R2’ represents a tetramethylmercaptoimidazole derivative or —S+R3R4, wherein R3 and R4 each independently represent lower alkyl, or a pharmaceutically and/or veterinarily acceptable derivative thereof. The present invention further relates to pharmaceutical formulations of said compound and the use thereof in the preparation of a medicament for inhibiting diseases in which transglutaminase has been implicated. Advantageously, the medicament is for treating fibrosis, scarring and/or cancer. Additionally, the invention relates to a method of inhibiting autoimmune diseases such as coeliac disease, neurodegeneration and chronic inflammatory diseases (e.g. of the joints including rheumatoid arthritis and osteoarthritis in a subject).Type: ApplicationFiled: June 16, 2004Publication date: August 21, 2008Applicant: ASTON UNIVERSITYInventors: Martin Griffin, Ian George Coutts, Robert Edward Saint
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Publication number: 20080200512Abstract: The invention provides a compound of formula: and methods for making and using the same, where R1 and R2 are independently hydrogen, C1-6 alkyl or C1-6 haloalkyl; R3 is hydrogen, halogen, C1-6 alkyl or C1-6 alkoxy; R4 is hydrogen or halogen; and R5 is a mono- or di-amino acid moiety, a succinic acid moiety, a urea moiety, or a derivative thereof. The invention also provides pharmaceutical compositions comprising a compound of formula I, and methods for making and using the same.Type: ApplicationFiled: February 14, 2008Publication date: August 21, 2008Inventors: Jeffrey Mark Blaney, Normand Hebert, Stephanie Ann Hopkins, Elizabeth A. Jefferson, Masaki Tomimoto
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Publication number: 20080200513Abstract: The present invention relates to pyridinone derivatives of formula (I): wherein Z represents C2-6 alkynyl, aryl or heteroaryl, any of which groups may be optionally substituted, and R1 represents hydrogen, C1-6 alkyl, C3-7 heterocycloalkyl(C1-6)alkyl, di(C1-6)alkylamino(C1-6)alkyl, C2-6 alkylcarbonyloxy(C1-6)alkyl or C3-7 cycloalkoxycarbonyloxy(C1-6)alkyl, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C virus infections.Type: ApplicationFiled: June 1, 2004Publication date: August 21, 2008Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P ANGELETTI SPAInventors: Stafania Colarusso, Frank Narjes
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Publication number: 20080200514Abstract: The invention relates to new indications for direct thrombin inhibitors such as dabigatran etexilate in the CNS and other fields.Type: ApplicationFiled: July 17, 2007Publication date: August 21, 2008Applicant: Boehringer Ingelheim International GmbHInventors: Andreas Clemens, Paul A. Reilly
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Publication number: 20080200515Abstract: The invention relates to solid state forms of enantiopure ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfnyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a solid form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders such as those discussed above.Type: ApplicationFiled: December 28, 2007Publication date: August 21, 2008Applicant: TAP PHARMACEUTICAL PRODUCTS INC.Inventors: John M. BRACKETT, David T. JONAITIS, Wei LAI, Jih Hua LIU, Stephan D. PARENT
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Publication number: 20080200516Abstract: The invention relates to crystalline forms of racemic ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising a crystalline Form of ilaprazole according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.Type: ApplicationFiled: December 28, 2007Publication date: August 21, 2008Applicant: TAP PHARMACEUTICAL PRODUCTS INC.Inventors: John M. BRACKETT, David T. JONAITIS, Wei LAI, Jih Hua LIU, Stephan D. PARENT, Jinyu SHEN
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Publication number: 20080200517Abstract: The invention relates to crystalline forms of various solvates of ilaprazole, 2[[(4-methoxy-3-methyl-2-pyridinyl)-methyl]sulfinyl]-5-(1H-pyrrol-1-yl) 1H-Benzimidazole. The invention also relates to a pharmaceutical composition for inhibiting gastric acid secretion comprising crystalline ilaprazole hydrate according to the invention in an amount effective to inhibit gastric acid secretion and a pharmaceutically acceptable carrier. The invention also provides methods of treatment for various acid-related gastrointestinal (GI) disorders.Type: ApplicationFiled: December 28, 2007Publication date: August 21, 2008Applicant: TAP PHARMACEUTICAL PRODUCTS INC.Inventors: John M. BRACKETT, David T. JONAITIS, Wei LAI, Jih Hua LIU, Stephan D. PARENT
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Publication number: 20080200518Abstract: Certain novel phenyl substituted cyclic urea derivatives have unexpected insecticidal activity. These compounds are represented by formula I: where A, B a, D, b, E, G, c, d, J, X and R through R10, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: May 18, 2005Publication date: August 21, 2008Applicant: Bayer CropScience AGInventors: Edward J. Barron, Larry Y. Zhang, John W. Lyga, Matthew P. Whiteside
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Publication number: 20080200519Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.Type: ApplicationFiled: February 15, 2008Publication date: August 21, 2008Inventors: Markus BERGER, Hartmut Rehwinkel, Heike Schacke, Ekkehard May, Werner Skuballa, Hermann Kunzer
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Publication number: 20080200520Abstract: Iron modulator compounds of formula (I) are provided for treating amyloidoses wherein R1 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl, R2 is selected from H, C1-6 alkyl, C1-6 alkenyl, C1-6 hydroxyalkyl, C1-6 hydroxyalkenyl and C6-10 aralykyl in which the aryl group of the aralkyl group is optionally substituted by hydroxy, halo or C1-4 alkyl R3 is selected from H, C1-6 alkyl, C1-6 alkenyl and C1-12 acyl; R4 is selected from H and C1-3 alkyl R5, R6 and R7 are independently selected from H, C1-6 alkyl, C3-7 aryl, and C1-10 aralkyl; the alkyl, aryl and aralkyl groups being optionally substituted by one or more halo, hydroxy and nitro groups or R5 and R7 together with the nitrogen atom to which they are bonded form a heterocyclic ring optionally substituted by one or more hydroxyl groups or a pharmaceutically acceptable tautomer, ester or addition salt thereof.Type: ApplicationFiled: March 31, 2006Publication date: August 21, 2008Inventors: Robert Charles Hider, Alessandra Gaeta, Zu Dong Liu
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Publication number: 20080200521Abstract: Novel hydroxamic acid containing amino acid derivatives are provided that are useful for treatment of inflammation, inflammatory and immunological diseases; lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyceride levels; and for treatment or prophylaxis of metabolic disorders.Type: ApplicationFiled: January 3, 2008Publication date: August 21, 2008Inventors: Partha Neogi, Debendranath Dey, Abjiheet Nag, Sujata Neogi, Bishwajit Nag
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Publication number: 20080200522Abstract: The present invention provides a composition for controlling a house insect pest, such as termites, ants or cockroaches, which comprises, as active ingredients, at least two compounds selected from the group consisting of (a) a certain pyridine compound, (b) a benzoylurea compound, (c) a pyrethroid compound and (d) a certain hydrazone compound; and a composition for controlling a house insect pest, which comprises, as an active ingredient, a certain hydrazone compound.Type: ApplicationFiled: April 18, 2008Publication date: August 21, 2008Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Masayuki Morita, Osamu Imai
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Publication number: 20080200523Abstract: The present invention provides derivatives of squaric acid, in particular derivatives of 3,4-diamino-cyclobut-3-ene-1,2-dione and tautomers and isomers thereof, as a single stereoisomer or a mixture of stereoisomers, or as a pharmaceutically acceptable salt thereof. These compounds show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: February 21, 2007Publication date: August 21, 2008Inventors: Krishna K. Murthi, Roland Kostler, Chase Smith, Tilman Brandstetter, Arthur F. Kluge
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Publication number: 20080200524Abstract: Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: November 1, 2007Publication date: August 21, 2008Inventors: Michael G. Kelly, Satyanarayana Janagani, Guoxian Wu, John Kincaid
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Publication number: 20080200525Abstract: Compounds of formula wherein A0, A1 and A2 are each independently of the others a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge which is unsubstituted or substituted by from one to six identical or different substituents selected from halogen and C3-C8cycloalkyl; Y is, for example, O, S, SO or SO2; M is O or NOR6, X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylcarbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C2-C6alkynyl; Q is, for example, O, S, SO or SO2; W is, for example, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; D is CH or N; R4 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R5 is, for example, C1-C12alkyl, C3-C8cycloalkyl or —N(R7)2; R7 is H, C1-C6alkyl, C1-C3haloalkyl, C1-C6alkylcarbonyl, C1-C3haloalkylcarbonyl, C1-C6alkoxycarbonyl, C3-C8cycloalkyl, C3-C8 cycloalkylType: ApplicationFiled: April 7, 2008Publication date: August 21, 2008Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Werner Zambach, Roger Graham Hall, Peter Renold, Stephan Trah
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Publication number: 20080200526Abstract: Disclosed herein is a composition for the treatment and prevention of allergic inflammatory diseases comprising N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, 4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine or pharmaceutically acceptable salts. The composition exhibits excellent medicinal effects on allergic inflammatory diseases, with a great reduction in typical chronic inflammation symptoms, such as an increase of eosinophil level in bronchoalveolar lavage fluid, total leukocyte level and eosinophil level in blood, the hypertrophy or hyperplasia of bronchial epithelium due to an increase in the number of mucus cells, a reduction in alveolar surface area resulting from the hyptertrophy of alveolar walls, and the infiltration of inflammatory cells.Type: ApplicationFiled: July 5, 2005Publication date: August 21, 2008Inventors: Jin Soo Lee, Sae Kwang Ku, Sang Ho Lee, Jei Man Ryu
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Publication number: 20080200527Abstract: Compounds of formula (I), are cannabinoid CB1 receptors, useful, inter alia in the treatment of obesity: wherein A1 is hydrogen, —COOH, or tetrazolyl, and A2 is hydrogen, —COOH, tetrazolyl, —CN, —CF3, —COR6, —SO2R6, —OR7, —NR7R8, —NHCOR6, and —NR7SO2R8 provided that one of A1 and A2 is either —COOH or tetrazolyl; p is 0 or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5; q is 0 or 1; R1 is a bond, or —(CH2)aB1(CH2)b— wherein a and b are independently 0, 1, 2 or 3 provided that a+b is not greater than 4, and B1 is —CO—, —O—, —S—, —SO—, —SO2—, —CH2—, —CHOH— or —NR7—; R2 is a bond, —CH2)aB1(CH2)b— or —[(CH2)aB1(CH2)b]n-A4-[(CH2)cB2(CH2)d]m— wherein a, b, and B1 are as defined for R1; B2 is as defined for B1, c and d are independently 0, 1, 2 or 3; with the proviso that a+b+c+d is not greater than 6, n and m are independently 0 or 1 and A4 is a monocarbocyclic or monoheterocyclic ring, having 3 to 8 ring atoms, optionally substituted with one or more of —F, —Cl, —Br,Type: ApplicationFiled: June 14, 2006Publication date: August 21, 2008Applicant: Carex SAInventors: Remi Alain Amengual, Claire Nadelene Marsol, Eric Liu Mayeux, Michael laurence Sierra, Patrick Herve Wagner
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Publication number: 20080200528Abstract: Compounds of formula (I) wherein X is chloro or bromo; Y is chloro or trifluoromethyl; and A and B are hydrogen or methyl with the proviso that one of A or B must be methyl; or the enantiomers or sats thereof, use of compounds of formula I for combating insects or acarids and for treating, controlling, preventing or protecting animals against infestation or infection by parasites, and compositions comprising compounds of formula I.Type: ApplicationFiled: May 30, 2006Publication date: August 21, 2008Applicant: BASF AktiengesellschaftInventors: Christopher Koradin, Wolfgang Von Deyn, Michael Rack, Thomas Zierke, David G. Kuhn, Deborah L. Culbertson, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi
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Publication number: 20080200529Abstract: This invention relates to novel 2-amino benzimidazole derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: January 10, 2006Publication date: August 21, 2008Applicant: NEURO SEARCH A/SInventors: Ulrik Svane Sorensen, Lene Teuber, Dan Peters, Dorte Strobaek, Tina Holm Johansen, Karin Sandager Nielsen, Palle Christophersen
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Publication number: 20080200530Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of progressive multifocal leukoencephalopathy.Type: ApplicationFiled: January 17, 2006Publication date: August 21, 2008Inventors: David J. Unett, Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter I. Dosa
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Publication number: 20080200531Abstract: The invention provides new methods for inhibiting the CDKI pathway and specifically inhibiting tumor cell growth. The invention further provides new and specific inhibitors of tumor cell growth, as well as means for discovery of additional such inhibitors. The present inventors have surprisingly discovered that Cyclin-Dependent Kinase 3 (CDK3) is specifically required for tumor cell growth, in contrast to other members of the CDK family.Type: ApplicationFiled: May 15, 2007Publication date: August 21, 2008Inventors: Bey-Dih Chang, Igor B. Roninson, Donald Porter
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Publication number: 20080200532Abstract: Provided are polymorphic forms of fluvastatin sodium and processes for their preparation.Type: ApplicationFiled: April 23, 2008Publication date: August 21, 2008Inventors: Revital Lifshitz-Liron, Tamas Koltai, Judith Aronhime, Nurit Perlman
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Publication number: 20080200533Abstract: The administration of pharmaceuticals of drugs which are having less solubility, lower bioavailability, lower bioabsorbability, less rate of absorption has become a big challenge in day to day life. Therefore an attempt has been made to prepare a complex modified form of the said pharmaceutical or drug such that the modified complex drugs or pharmaceuticals exhibits the enhanced properties of solubility, bioavailability, bioabsorbability and rate of absorption despite the increased complexity of the molecule. Surprisingly such modification was found to enhance retentivity of the active drug ingredient in the blood. Higher amounts of the active drug ingredient has shown lower toxicity.Type: ApplicationFiled: June 29, 2006Publication date: August 21, 2008Inventor: Ramu Krishnan
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Publication number: 20080200534Abstract: Composition (A) containing, for 100% of its mass: from 10 mass % to 90 mass % of N-lauroyl proline (I) and from 10 mass % to 90 mass % of an ester (II) of anhydrohexitol and of a saturated or unsaturated, linear or branched aliphatic carboxylic acid containing from 12 to 20 carbon atoms optionally substituted with one or more hydroxyl groups, or of a mixture of esters (II); use thereof for preparing a medicament with lipolytic activity, intended to induce slimming of the human or animal body and/or the reduction of cellulite or of the orange-feel appearance; cosmetic formulation or therapeutic composition containing same; process for the preparation thereof and process for the solubilization of N-lauroyl proline (I) in a liquid medium.Type: ApplicationFiled: October 17, 2006Publication date: August 21, 2008Applicant: Societe D'Exploitation De Produits pour les Industries Chimiques (Seppic)Inventors: Alicia Roso, Christine Garcia
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Publication number: 20080200535Abstract: There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.Type: ApplicationFiled: August 24, 2007Publication date: August 21, 2008Applicant: Asahi Kasei Pharma CorporationInventors: Yutaka Ohmori, Masakazu Komatsu