Chalcogen Or Nitrogen Bonded Directly At 1-, 2- Or 3-position Of The Diazole Ring By Nonionic Bonding Patents (Class 514/395)
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Publication number: 20100286220Abstract: Disclosed are methods and compositions relating to antagonists of HNF4?.Type: ApplicationFiled: April 30, 2010Publication date: November 11, 2010Applicants: Burnham Institute for Medical Research, Regents of the University of CaliforniaInventors: Fred Levine, Mark Mercola, Suzette Farber-Katz, Marcia I. Dawson, Pamela Itkin-Ansari
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Publication number: 20100273793Abstract: The disclosure relates to compounds of formula (I): wherein A, W, R, R5, and R6 are as defined in the disclosure, or a salt thereof, and to their use as drugs, in particular as c-Met inhibitors.Type: ApplicationFiled: April 16, 2010Publication date: October 28, 2010Applicant: SANOFI-AVENTISInventors: Conception Nemecek, Sylvie Wentzler
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Publication number: 20100256155Abstract: A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): wherein R1 is a substituent being one selected from a group consisting of i) a first substituent being one selected from a group consisting of a hydryl group, an amino group, a nitro group, a hydroxyl group and a cyan group, ii) a second substituent being one selected from a group consisting of (CH2)nX, a straight (CH2)n alkyl group, a (CH2)n alkoxyl group, a branched (CH2)n alkyl group, a C3˜C12 nephthenic group, and a C3˜C12 cyclic alkoxyl group, wherein 1?n?12, and X is a halogen, iii) a third substituent being one selected from a group consisting of a straight C1˜C8 alkyl group with a double-bond, a C1˜C8 alkoxyl group with a double-bond, a branched C1˜C8 alkyl group with a double-bond and a C3˜C8 nephthenic group with a double-bond, and iv) a fourth substituent of a C5˜C12 heterocyclic group.Type: ApplicationFiled: March 29, 2010Publication date: October 7, 2010Applicant: National Defense Medical CenterInventor: Hsu-Shan Huang
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Publication number: 20100256188Abstract: The present invention relates to compounds of general formula I in which A, L, M, Q2, Q3, Q4, R1, R5, Ra, Rb, Rc, W, X, Y, Z1, Z2, Z3 are defined in the description, the salts thereof, particularly the physiologically acceptable salts thereof. The compounds are of potential utility in the treatment and/or prevention of inflammatory diseases and associated conditions, in particular, in the treatment and/or prevention of pain. The invention also relates to the use of such compounds as medicaments, to pharmaceutical compositions containing them, and to their preparation.Type: ApplicationFiled: March 4, 2010Publication date: October 7, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Roland PFAU, Kirsten ARNDT, Henri DOODS, Klaus KLINDER, Raimund KUELZER, Dimitrijs LUBRIKS, Juergen MACK, Benjamin PELCMAN, Henning PRIEPKE, Robert ROENN, Dirk STENKAMP, Edgars SUNA
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Publication number: 20100249030Abstract: The present invention relates to a method of treating cancer by pretreatment with anti-mitotic agents followed by at least one aurora kinase inhibitor. Extensive illustrations are provided for the antimitotic agents and aurora kinase inhibitors that are useful in the inventive treatment.Type: ApplicationFiled: July 28, 2008Publication date: September 30, 2010Inventor: Andrea Dawn Basso-Porcaro
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Publication number: 20100240702Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.Type: ApplicationFiled: May 15, 2008Publication date: September 23, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Brian Nicholas Cook, Stephane De Lombaert, Michel Jose Emmanuel, Xin Guo, Ming-Hong Hao, Jin Mi Kim, Ho Yin Lo, Chuk Chui Man, Tina Marie Morwick, Peter Allen Nemoto, Kevin Chungeng Qian, Hidenori Takahashi, Steven John Taylor
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Publication number: 20100204252Abstract: The present invention relates to a method of treating hypertension in a subject or patient needing treatment thereof by administering to said subject or patient at least one angiotensin II receptor blocker in combination with chlorthalidone.Type: ApplicationFiled: December 22, 2009Publication date: August 12, 2010Applicant: TAKEDA PHARMACEUTICALS NORTH AMERICA, INC.Inventor: Stuart R. Kupfer
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Publication number: 20100196368Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: March 12, 2010Publication date: August 5, 2010Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.Inventors: Payman Amiri, Wendy Fantl, Teresa Hansen, Barry Haskell Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Leonard Sung
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Publication number: 20100190796Abstract: Provided herein are methods for identifying and characterizing agents that alter the volume of a cell. Methods are provided for rapid screening and identification of an agent that alters the capability of a small, neutrally charged solute transporter to transport the solute across a cell membrane. The methods described herein may be used to identify and characterize inhibitors of urea transporters, to identify and characterize inhibitors of aquaporins, and to identify and characterize inhibitors of other small, neutrally charged solutes such as glucose.Type: ApplicationFiled: November 16, 2007Publication date: July 29, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Alan S. Verkman, Marc Harris Levin
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Patent number: 7763643Abstract: The present invention comprises compounds and compositions comprising substituted thiophene derivatives with the following backbone structure: The compounds of this type are of useful in the treatment of various disorders, such as, respiratory disorders and snoring, acute and chronic disorders, disorders induced by ischemic and/or reperfusion events and by proliferative or fibrotic events, disorders of the central nervous system and lipid metabolism, diabetes, blood coagulation and infection by parasites.Type: GrantFiled: January 30, 2009Date of Patent: July 27, 2010Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hans-Jochen Lang, Uwe Heinelt, Armin Hofmeister, Klaus Wirth, Michael Gekle, Markus Bleich
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Publication number: 20100179147Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.Type: ApplicationFiled: December 10, 2009Publication date: July 15, 2010Inventors: Chih-Shiang Chang, Jih-Hwa Guh, Che-Ming Teng, Shiow-Lin Pan, Wei-Ling Chang, Ju-Fang Liu, Kai-Wei Chang, Sheng-Chu Kuo
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Publication number: 20100168203Abstract: The present invention relates to a method of preventing or treating a disease caused by bacterial infection by administering an effective amount of a modulator of bacterial adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of bacterial adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of bacterial adenylyl cyclase that do not substantially modulate adenylyl cyclase of the subject. The invention also provides methods for culturing bacterial pathogens and methods for inducing the pathogenic state in vitro.Type: ApplicationFiled: January 11, 2008Publication date: July 1, 2010Inventors: Lonny Levin, Jochen Buck, Leo Brizuela, Michael Pinnisi
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Publication number: 20100168196Abstract: This invention is directed to the compound of formula (I), compositions containing said compounds to inhibit the sodium-proton exchanger of subtype 3 (NHE3) which are useful in the prevention or treatment of various disorders in a patient suffering from a disease state, such as, renal disorders including acute or chronic renal failure, disorders of biliary function and for respiratory disorders such as snoring or sleep apnea or for stroke.Type: ApplicationFiled: March 12, 2010Publication date: July 1, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Uwe HEINELT, Hans-Jochen LANG, Armin HOFMEISTER, Klaus WIRTH, Martin HUG
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Publication number: 20100158996Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.Type: ApplicationFiled: February 12, 2010Publication date: June 24, 2010Inventors: Atsushi Hagiwara, Yasuhiro Ohe, Naoya Odani, Shizue Watanabe, Taku Ikenogami, Takashi Kawai, Kenya Madono, Toshio Taniguchi
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Publication number: 20100152170Abstract: The present invention relates to compounds and methods from the treatment of cancer. The invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising compounds that inhibit Aurora kinase, and methods for the treatment of cancer using the compounds of the presentation invention or pharmaceutical compositions comprising compounds of the present invention.Type: ApplicationFiled: February 10, 2010Publication date: June 17, 2010Applicant: TransTech Pharma, Inc.Inventors: Adnan M.M. Mjalli, Brian S. Grella, Govindan Subramanian, Murty N. Arimilli, Ramesh Gopalaswamy, Robert C. Andrews, Stephen Davis, Xiaochuan Guo, Jeff Zhu
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Publication number: 20100151035Abstract: The present invention relates to a stable pharmaceutical composition of a poorly water-soluble drug with a view to increasing its solubility and bioavailability. The present invention relates to a solid dispersion of a poorly water-soluble drug.Type: ApplicationFiled: March 10, 2008Publication date: June 17, 2010Applicant: Sandoz AGInventors: Bharatrajan Ramaswami, Manisha Rajesh Patil, Aditi Das
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Patent number: 7737167Abstract: 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: GrantFiled: August 3, 2005Date of Patent: June 15, 2010Assignee: Neurosearch A/SInventors: Ulrik Svane Sørensen, Lene Teuber, Dan Peters, Dorte Strøbæk, Tina Holm Johansen, Karin Sandager Nielsen, Palle Christophersen
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Publication number: 20100137384Abstract: The invention relates to a novel formulation having the advantage of including triclabendazole in solution. In addition a further anthelmintic may be included. The formulation is made by mixing the abamectin and benzyl alcohol and mixing this with triclabendazole and butyl dioxitol. The mix is then heated to dissolve the active, and allowed to cool at which stage the solution is diluted to volume with PEG 4000. The present invention overcomes the solubility difficulties of triclabendazole and presents the triclabendazole in a solution.Type: ApplicationFiled: December 7, 2009Publication date: June 3, 2010Inventor: Colin Mason Harvey
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Publication number: 20100130513Abstract: Provided are compounds of the formula: wherein RN1 is a substituent of formula G1-NX1X2, wherein G1 is an optionally further substituted alkylene, which optionally forms, together with RN2, a cyclic group, and each of X1 and X2 is independently H or an N-substituent, or X1 and X2 together form a heterocyclic ring, or X1 together with G1 forms a cyclic group and X2 is H or an N-substituent; and each of Z1, Z2, Z3 and Z4 is H or a substituent, or two of Z1, Z2, Z3 and Z4 together form an optionally substituted ring, and further wherein at least one of Z1, Z2, Z3 and Z4 is other than H, and salts thereof, pharmaceutical compositions and methods of using the compounds. The compounds have antiviral activity.Type: ApplicationFiled: November 17, 2009Publication date: May 27, 2010Applicant: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Elizabeth Anne Jefferson, Richard H. Griffey, Eric E. Swayze
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Publication number: 20100113548Abstract: The present invention relates to antagonists of the human bitter-taste receptors hTAS2R38. The invention also relates to methods for identifying further molecules that suppress hTAS2R38 mediated bitter taste transduction or bitter taste response and uses thereof.Type: ApplicationFiled: April 18, 2008Publication date: May 6, 2010Applicant: DEUTSCHES INSTITUT FUR ERNAHRUNGSFORSCHUNG POTSDAM-REHBRUCKEInventors: Bernd Bufe, Christina Kuhn, Wolfgang Meyerhof
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Publication number: 20100105749Abstract: The present invention provides compounds of the formulae (I) and (II), and derivatives thereof, for the treatment of cardiovascular conditionsType: ApplicationFiled: January 30, 2008Publication date: April 29, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jon Loren Collins, Jodi Maglich Goodwin, Millard Hurst Lambert, III
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Publication number: 20100099643Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: December 22, 2009Publication date: April 22, 2010Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20100093613Abstract: Agents that stabilize and/or prevent fibrosis are identified by assaying test agents in a battery of assays to measure the effect of the test agent on matrix deposition and remodeling, epithelial health, and inflammation. Treatment for fibrosis is provided using compositions of the invention.Type: ApplicationFiled: March 10, 2008Publication date: April 15, 2010Inventors: Eric J. Kunkel, Elen S. Rosler, Sylvie Private, Jennifer E. Melrose
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Publication number: 20100087427Abstract: Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.Type: ApplicationFiled: December 21, 2005Publication date: April 8, 2010Inventors: Werner Breitenstein, Sylvain Cottens, Claus Ehrhardt, Edgar Jacoby, Edwige L. Lorthiolis, Juergen K. Maibaum, Nils Ostermann, Holger Sellner, Oliver Simic
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Publication number: 20100081643Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.Type: ApplicationFiled: September 21, 2009Publication date: April 1, 2010Inventors: BRETT C. BOOKSER, Qun Dang, Tony S. Gibson, Hongjian Jiang, De Michael Chung, Jianming Bao, Jinlong Jiang, Andy Kassick, Ahmet Kekec, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, David Wilson, Dariusz Wodka
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Patent number: 7687529Abstract: The present invention is directed to substituted propylamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, 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: September 27, 2006Date of Patent: March 30, 2010Assignee: Wyeth LLCInventors: Casey Cameron McComas, Puwen Zhang, Eugene Anthony Terefenko, An Thien Vu, Stephen Todd Cohn
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Patent number: 7687471Abstract: The present invention provides a stable veterinary oral composition which comprises one or more surfactants, a water-miscible solvent, optionally an oil and an effective amount of each of a benzimidazole antihelmintic compound, such as triclabendazole and a macrocyclic lactone, such as moxidectin. Said composition is useful for treating and controlling endo- and ectoparasitic infection and infestation in a homeothermic animal.Type: GrantFiled: December 5, 2006Date of Patent: March 30, 2010Assignee: Wyeth LLCInventors: Jon C. Hayes, Debora L. Guido, Jacob A. Zupan
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Publication number: 20100063099Abstract: The present invention relates to a method of preventing or treating a disease caused by infection by a eukaryotic pathogen, wherein the method comprises administering an effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides pharmaceutical compositions useful for preventing or treating a disease, with the compositions containing a therapeutically effective amount of a modulator of a eukaryotic pathogen's adenylyl cyclase. The invention also provides screening methods for identifying selective modulators of a eukaryotic pathogen's adenylyl cyclase that do not substantially modulate an adenylyl cyclase of the subject. The invention also provides methods for culturing eukaryotic pathogens and methods for inducing the pathogenic state in vitro.Type: ApplicationFiled: January 11, 2008Publication date: March 11, 2010Inventors: Lonny Levin, Jochen Buck, Leo Brizuela, Michael Pinnisi, Leo Brizuela, Michael Pinnisi
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Publication number: 20100056515Abstract: There is provided a compound of the formula (I): wherein R1 is an optionally substituted C1-10 alkyl; R2 is H, or a C1-6 alkyl which may be substituted with 1 to 3 substituents; R3 is a 5- or 6-membered aromatic group which may be substituted with 1 to 5 substituents, wherein the 5- or 6-membered aromatic group may be fused with a 5- or 6-membered ring which may be substituted with 1 to 3 C1-6 alkyls; R4 is a hydrogen, a halogen, a hydroxy, a cyano, a C1-6 alkyl or a C1-6 alkoxy; Z is —O—, —S—, —SO—, —SO2—, or —NR5— wherein R5 is a hydrogen or a C1-6 alkyl; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.Type: ApplicationFiled: October 24, 2007Publication date: March 4, 2010Inventors: Kazuyoshi Aso, Michiyo Mochizuki, Takuto Kojima, Katsumi Kobayashi, Scott Alan Pratt, Albert Charles Gyorkos, Christopher Peter Corrette, Suk Young Cho
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Publication number: 20100048658Abstract: There is provided a compound of the formula: wherein R1 is an optionally substituted hydrocarbyl, a substituted amino, etc.; R2 is an aromatic group substituted with one or two substituents at the positions adjacent to the position bonded to Z, and said aromatic group may have additional substituent(s); X is —NR3— wherein R3 is a hydrogen, an optionally substituted hydrocarbyl or an acyl, or sulfur; Y1, Y2 and Y3 are an optionally substituted methine or a nitrogen, etc.; and Z is an optionally substituted methylene, provided that carbonyl is excluded; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.Type: ApplicationFiled: December 28, 2007Publication date: February 25, 2010Inventors: Kazuyoshi Aso, Michiyo Mochizuki, Katsumi Kobayashi
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Publication number: 20100048565Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immune-related conditions or disorders. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, immune response regulation and cell proliferation. The subject compounds are 2-amino-imidazole derivatives.Type: ApplicationFiled: October 28, 2009Publication date: February 25, 2010Inventors: Alexander David Frenkel, Sarah Elizabeth Lively, Jay P. Powers, Andrew Smith, Daqing Sun, Craig Tomooka, Zhulun Wang
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Publication number: 20100035951Abstract: This invention relates to 2-amino benzimidazole derivatives of Formula 1a or 1b: which are 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: July 5, 2007Publication date: February 11, 2010Applicant: NEUROSEARCH A/SInventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strøbaek, Tina Holm Johansen, Palle Christophersen
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Publication number: 20100029736Abstract: The present invention is directed to 2-substituted proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: July 13, 2007Publication date: February 4, 2010Applicant: MERCK & CO., INC.Inventors: Christopher D. Cox, David B. Whitman, Michael J. Breslin
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Patent number: 7649008Abstract: Various crystal forms of 4-(1-((4-methylbenzothiophen-3-yl)methyl)benzimidazol-2-ylthio)butanoic acid from a solvent, and a process for production thereof are provided.Type: GrantFiled: May 14, 2004Date of Patent: January 19, 2010Assignee: Teijin Pharma LimitedInventors: Mitsuru Teramoto, Naoki Tsuchiya, Hiroshi Saitoh
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Patent number: 7642275Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with histone deacetylases (HDACs) that comprise a compound of the formulae: wherein the variables are as defined herein.Type: GrantFiled: December 16, 2005Date of Patent: January 5, 2010Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Jason W. Brown, Robert J. Skene, Jeffrey A. Stafford, Phong H. Vu, Anthony R. Gangloff, Andrew J. Jennings, Stephen W. Kaldor
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Publication number: 20090325955Abstract: The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or pharmaceutically salts thereof. The present invention also relates to methods of using compounds of formula I or formula VII in combination with one or more additional antibacterial agents and/or one or more additional therapeutic agents that increase the susceptibility of bacterial organisms to antibiotics.Type: ApplicationFiled: June 12, 2009Publication date: December 31, 2009Inventors: PAUL Charifson, David Deininger, Anne-Laure Grillot, Yusheng Liao, Steven Ronkin, Dean Stamos, Emanuele Perola, Tiansheng Wang, Arnaud Le Tiran, Joseph Drumm
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Publication number: 20090325944Abstract: The invention relates to methods and products for modulating glycosylation of proteins. The invention is useful for treating glycosylation-associated disorders such as neurodegeneration, diabetes, including complications of diabetes such as insulin resistance, nephropathy, microvascular damage, and endothelial dysfunction. The invention also relates in part to assays that are useful for identifying and testing candidate compounds for modulating glycosylation of proteins.Type: ApplicationFiled: April 11, 2007Publication date: December 31, 2009Inventors: Suzanne Walker Kahne, Benjamin Gross
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Patent number: 7638545Abstract: A formulation having triclabendazole in solution. In addition a further anthelmintic may be included. The formulation is made by mixing the abamectin and benzyl alcohol and mixing this with triclabendazole and butyl dioxitol. The mix is then heated to dissolve the active, and allowed to cool at which stage the solution is diluted to volume with PEG 4000.Type: GrantFiled: April 14, 2000Date of Patent: December 29, 2009Assignee: Merial LimitedInventor: Colin Manson Harvey
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Publication number: 20090298824Abstract: Compounds of formula I in free or salt form, where Y, R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the CXCR2 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: January 20, 2005Publication date: December 3, 2009Inventors: Neil J. Press, David Porter, Catherine Leblanc, Clive McCarthy, Nicolas Soldermann, Lyndon N. Brown
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Publication number: 20090298811Abstract: This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein.Type: ApplicationFiled: September 3, 2007Publication date: December 3, 2009Inventors: Kazuo Ando, Ingrid Price Buchler, Shridhar Gajanan Hedge, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Patent number: 7625876Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: GrantFiled: August 20, 2007Date of Patent: December 1, 2009Assignee: Hopital-Sainte-JustineInventors: Ernest G. Seidman, Yves Theoret
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Publication number: 20090286838Abstract: The present invention provides methods for the treatment of tumors, comprising administration of an effective amount of at least one taxoid and an effective amount of at least one benzimidazol carbamate compound of formula (I). The invention also provides a method for the treatment of tumors insensitive to one or more anti-mitotic drugs, the method comprising administering an effective amount of at least one benzimidazole carbamate compound of formula (I). Also provide are compositions for carrying out methods of the invention.Type: ApplicationFiled: December 6, 2005Publication date: November 19, 2009Applicant: NewSouth Innovations Pty LimitedInventors: David L. Morris, Mohammad Hossein Pourgholami
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Publication number: 20090270468Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: September 5, 2008Publication date: October 29, 2009Inventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Minghao Zhang, Lei Zhu
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Publication number: 20090270372Abstract: A subject of the present Application is novel derivatives of benzimidazole and imidazopyridine which have a good affinity for certain sub-types of melanocortin receptors, in particular the MC4 receptors. They are particularly useful for treating pathological conditions and diseases in which one or more melanocortin receptors are involved. The invention also relates to pharmaceutical compositions containing said products.Type: ApplicationFiled: January 21, 2009Publication date: October 29, 2009Applicant: Societe de Conseils de Recherches etInventors: Lydie POITOUT, Valerie Brault, Carole Sackur, Roubert Pierre, Pascale Plas
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Publication number: 20090258868Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 10, 2008Publication date: October 15, 2009Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
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Publication number: 20090258869Abstract: The present disclosure provides methods of treating or preventing a substance-related disorder using Hsp90 inhibitors, Hsp90 modulators, tyrosine hydroxylase modulators, and modulators that reduce the interaction between Hsp90 and tyrosine hydroxylase.Type: ApplicationFiled: February 6, 2009Publication date: October 15, 2009Inventors: Dorit RON, Dao-Yao He
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Patent number: 7601745Abstract: 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, wherein R3 is H, —C(O)NRaRb, halogen, alkyl, haloalkyl, aryl, heteroaryl, OH, SH, NR4?OR5?, NH2, amine, alkylamine, alkoxy, cycloalkyl, heterocycloalkyl, hydroxyalkyl, or haloalkyloxy; R4 is H, halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hyodroxyalkylamino, alkylamino, heteroaryl, or aryl; R5 is halogen, alkyl, —C(NR7)NR7R8, —(CH2)paryl, —(CH2)pNR7R8, —C(O)NR7R8, —N?CR7R8, —NR7C(O)R8, cycloalkyl, heterocycloalkyl, haloalkyl, hydroxyalkyl, hydroxyalkylamino, alkylamino, heteroaryl, or aryl.Type: GrantFiled: March 15, 2006Date of Patent: October 13, 2009Assignee: 4SC AGInventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
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Publication number: 20090253762Abstract: This invention relates to certain aryl alkyl acid compounds, compositions, and methods for treating or preventing obesity and related diseases.Type: ApplicationFiled: September 8, 2008Publication date: October 8, 2009Inventors: Roger Smith, Ann-Marie Campbell, Philip Coish, Miao Dai, Susan Jenkins, Derek Lowe, Stephen O'Connor, Ning Su, Gan Wang, Mingbao Zhang, Lei Zhu
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Publication number: 20090239921Abstract: A pharmaceutical composition exhibiting an anti-neoplastic activity, comprising: a pharmaceutically-effective amount of a compound of Formula 1 and at least one inert, pharmaceutically acceptable carrier or diluent; wherein R1 is a hydrogen or an aliphatic group; and R2 is an aliphatic group, optionally substituted with a substituent selected from a hydroxyl and a substituted amino group; and methods of treating human neoplasms and for inhibiting caseine kinase 2 activity with said pharmaceutical composition.Type: ApplicationFiled: April 24, 2009Publication date: September 24, 2009Applicant: Selvita Sp. z.o.o.Inventor: Zygmunt KAZIMIERCZUK
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Publication number: 20090233949Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: ApplicationFiled: March 9, 2009Publication date: September 17, 2009Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Markus FOLLMANN, Jochen GOERLITZER, Herman SCHREUDER