C=o Bonded Directly To The Six-membered Hetero Ring Patents (Class 514/350)
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Patent number: 8067200Abstract: A single chain, polypeptide fusion protein, comprising: a non-cytotoxic protease, or a fragment thereof, which protease or protease fragment is capable of cleaving a protein of the exocytic fusion apparatus of a nociceptive sensory afferent; a Targeting Moiety that is capable of binding to a Binding Site on the nociceptive sensory afferent, which Binding Site is capable of undergoing endocytosis to be incorporated into an endosome within the nociceptive sensory afferent; a protease cleavage site at which site the fusion protein is cleavable by a protease, wherein the protease cleavage site is located between the non-cytotoxic protease or fragment thereof and the Targeting Moiety; and a translocation domain that is capable of translocating the protease or protease fragment from within an endosome, across the endosomal membrane and into the cytosol of the nociceptive sensory afferent. Nucleic acid sequences encoding the polypeptide fusion proteins, methods of preparing same and uses thereof are also described.Type: GrantFiled: December 1, 2005Date of Patent: November 29, 2011Assignees: Syntaxin Ltd., Allergan Inc.Inventors: Keith Foster, John Chaddock, Philip Marks, Patrick Stancombe, Kei Roger Aoki, Joseph Francis, Lance Steward
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Publication number: 20110288076Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particularly, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicant: EXELIXIS, INC.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Publication number: 20110281837Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: ApplicationFiled: January 3, 2011Publication date: November 17, 2011Inventors: Alan J. Hutchinson, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 8049037Abstract: This invention provides compounds as shown below, in which either all of Z1-6 are carbon or one of Z1-6 is nitrogen and the rest are carbon, and in which other substituents are defined herein, which are sphingosine-1-phosphate antagonists.Type: GrantFiled: August 12, 2009Date of Patent: November 1, 2011Assignee: Allergan, Inc.Inventors: Phong X. Nguyen, Todd M. Heidelbaugh, Ken Chow
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Publication number: 20110263657Abstract: The present invention relates to pharmaceutical compositions for treating, preventing or managing heart failure and/or connected diseases therewith comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound.Type: ApplicationFiled: June 18, 2009Publication date: October 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Barbara Albrecht-Küpper, Stefan Schäfer, Elodie Kienlen
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Publication number: 20110263626Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: August 28, 2008Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
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Patent number: 8030517Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: December 3, 2009Date of Patent: October 4, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
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Publication number: 20110217348Abstract: A textile material for use in an aquatic environment treated with an antifouling agent, where the antifouling agent comprises a) one or more organic antifouling biocides; b) a polymeric binder, selected from the group consisting of (A) a polyethylenic binder with an average molecular mass Mn of 1500 to 20000 g/mol, obtainable from the following monomers (A1) from 60 to 95% by weight of ethylene, (A2) from 5 to 40% by weight of at least one unsaturated carboxylic acid, selected from in the group of (A2a) monoethylenically unsaturated C3-C10 monocarboxylic acids, and (A2b) monoethylenically unsaturated C4-C10 dicarboxylic acids, and (A3) optionally from 0 to 30% by weight of other ethylenically unsaturated monomers which are copolymerizable with (A1) and (A2), the amounts of monomers being based in each case on the total amount of all monomers employed; (B) a poly(meth)acrylic binder with an average molecular mass Mn of 40,000 to 250,000, obtained by radical emulsion polymerization of at least 50% by weight (baType: ApplicationFiled: October 27, 2009Publication date: September 8, 2011Applicant: BASF SEInventor: Ulrich Karl
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Patent number: 8013002Abstract: The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.Type: GrantFiled: March 16, 2011Date of Patent: September 6, 2011Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Patent number: 7999109Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: December 17, 2009Date of Patent: August 16, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
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Patent number: 7994142Abstract: The invention relates to agents that contain folic acid, vitamin B6 and vitamin B12, and to the use thereof in hyperhomocysteinemia for controlling homocysteine levels. The agents are mainly suitable for the preventive and acute treatment of vascular diseases, of pregnant women and neurodegenerative diseases and are particularly advantageous in cases where the homocysteine levels to be controlled are found in an individual suffering from renal failure or being treated with immune suppressors. The invention particularly relates to pharmaceutical agents and food supplements comprising a corresponding active ingredient combination and to agents in the form of commercial packages containing corresponding combination preparations or monopreparations for the combined use.Type: GrantFiled: January 11, 2006Date of Patent: August 9, 2011Assignee: Phrontier S.A.R.L.Inventor: Martin Goerne
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Publication number: 20110183980Abstract: In one aspect, the invention relates to O-benzyl nicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: September 21, 2010Publication date: July 28, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Shaun Stauffer, Richard Williams, Gregor MacDonald, Ya Zhou, José Manuel Bartolomé-Nebreda
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Publication number: 20110184029Abstract: The present invention relates to 2-pyridone derivatives of Formula I or IV as herein described, compositions containing such compounds, synthetic processes for making such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 13, 2009Publication date: July 28, 2011Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Choung U. Kim, Michael L. Mitchell, Jong Chan Son
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Publication number: 20110178137Abstract: The present invention relates to pharmaceutical compositions and combinations for treating, preventing or managing heart failure and/or connected diseases therewith comprising 4{4-[3-(4-chloro-3-trifluoromethylphenyl)-ureido]-3-fluorophenoxy}-pyridine-2-carboxylic acid methylamide optionally combined with at least one additional therapeutic agent.Type: ApplicationFiled: June 16, 2009Publication date: July 21, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Barbara Albrecht-Küpper, Stefan Schäfer, Elodie Kienlen
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Publication number: 20110178089Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventors: Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ulmer
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Publication number: 20110178120Abstract: The present invention relates to pyridoxine (vitamin B6) derived compounds of formula (I), pharmaceutically acceptable salts, or solvates thereof, wherein R1, R2, R4, A, L B1 and B2 are as defined in the specification, and pharmaceutical compositions comprising the compounds. Compounds of formula (I) inhibit Human Immunodeficiency Virus (HIV)-integrase enzyme and are useful for preventing and treating HIV infection and AIDS.Type: ApplicationFiled: June 4, 2009Publication date: July 21, 2011Applicant: AMBRILIA BIOPHARMA, INC.Inventors: Brent Stranix, Francis Beaulieu, Jean-Emmanuel Bouchard, Guy Milot, Wang Zhigang, Réjean Ruel
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Publication number: 20110178138Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.Type: ApplicationFiled: July 28, 2008Publication date: July 21, 2011Applicant: The Regents of the University of CaliforniaInventors: Ohyun Kwon, Fuyuhiko Tamanoi, Hanna Fiji, Masaru Watanabe
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Publication number: 20110172234Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.Type: ApplicationFiled: March 28, 2011Publication date: July 14, 2011Applicants: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, UNIVERSITY OF MARYLAND, BALTIMORE A CONSTITUENT INSTITUTION OF THE UNIVERSITYInventors: Rakesh Srivastava, Sharmila Shankar, Alexander D. MacKerell, JR.
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Publication number: 20110160207Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: March 2, 2011Publication date: June 30, 2011Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
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Publication number: 20110158942Abstract: The present invention relates to pharmaceutical compositions for treating virus infections and/or diseases caused by virus infections comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound.Type: ApplicationFiled: March 9, 2011Publication date: June 30, 2011Inventors: Olaf WEBER, Bernd Riedl
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Publication number: 20110142923Abstract: The present invention relates to ophthalmic pharmaceutical compositions comprising Sorafenib, its derivatives or active metabolites, for the treatment and prevention of ocular neoangiogenic pathologies.Type: ApplicationFiled: August 6, 2009Publication date: June 16, 2011Inventors: Maria Grazia Mazzone, Vincenzo Papa, Francesco Giuliano, Manuela Marrano
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Publication number: 20110144164Abstract: The present invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.Type: ApplicationFiled: December 14, 2010Publication date: June 16, 2011Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Søren Møller Nielsen, Karsten Juhl, Lars Kyhn Rasmussen
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Publication number: 20110117073Abstract: The invention relates to protein conjugates that contain a protein kinase containg a cysteine residue in the ATP binding site and an inhibitor that is covalently and irreversibly bonded to said cysteine residue, such that the activity of the protein kinase is irreversibly inhibited. The invention also relates to compounds that irreversibly inhibit protein kinases.Type: ApplicationFiled: September 15, 2010Publication date: May 19, 2011Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Russell Colyn Petter, Deqiang Niu, Lixin Qiao, Arthur Kluge, Roy Lobb, Shomir Ghosh, Zhendong Zhu
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Publication number: 20110110886Abstract: Autotaxin (ATX) is a prometastatic enzyme initially isolated from the conditioned media of human melanoma cells that stimulates a myriad of biological activities including angiogenesis and the promotion of cell growth, survival, and differentiation through the production of lysophosphatidic acid (LPA). ATX increases the aggressiveness and invasiveness of transformed cells, and ATX levels directly correlate with tumor stage and grade in several human malignancies. To study the role of ATX in the pathogenesis of malignant melanoma, we developed antibodies and small molecule inhibitors against recombinant human protein. Immunohistochemistry of paraffin embedded human tissue demonstrates that ATX levels are markedly increased in human primary and metastatic melanoma relative to benign nevi. Chemical screens identified several small molecule inhibitors with binding constants ranging from nanomolar to low micromolar.Type: ApplicationFiled: June 15, 2009Publication date: May 12, 2011Inventor: Demetrios Braddock
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Publication number: 20110112153Abstract: Compounds of the formula (I) are disclosed and are suitable for the treatment of seborrheic dermatitis.Type: ApplicationFiled: January 31, 2011Publication date: May 12, 2011Inventors: Manfred Bohn, Karl Theodor Kraemer, Astrid Markus
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Publication number: 20110112114Abstract: The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds, and the compositions and methods that utilize them, can be used, either alone or in combination to inhibit viruses, particularly HCV virus.Type: ApplicationFiled: June 9, 2010Publication date: May 12, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Roger D. Tung, Govinda Rao Bhisetti, Luc J. Farmer
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Publication number: 20110110891Abstract: The present disclosure provides methods of treating a hepatitis C virus infection. The methods generally involve administering to an individual in need thereof an effective amount of an active agent that inhibits a RAS-RAF-MEK-ERK signal transduction pathway.Type: ApplicationFiled: May 11, 2009Publication date: May 12, 2011Inventors: Melanie Ott, Eva Herker
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Publication number: 20110104158Abstract: This invention relates to novel, substituted aralkyl heterocyclic compounds according to formula I, their derivatives, pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering aromatase inhibitors. Formula (I), or a pharmaceutically acceptable salt thereof, wherein: each R1 is independently selected from CH3, CH2D, CHD2 or CD3; each R2 is independently selected from CH3, CH2D, CHD2 or CD3; each Y is independently selected from H or D; and when each R variable is CH3, at least one Y is D.Type: ApplicationFiled: April 15, 2009Publication date: May 5, 2011Inventor: Scott L. Harbeson
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Publication number: 20110104307Abstract: To provide a fungicidal composition having stable and high fungicidal effects against cultivated crops infected with plant diseases resulting from plant diseases. A fungicidal composition containing, as active ingredients, (a) a benzoylpyridine derivative represented by the formula (I) or its salt: wherein when A is —N?, B is —CX4?; when A is —CH?, B is —N?; each of X1 and X2 which are independent of each other, is a halogen atom, an alkoxy group, a hydroxyl group, an alkyl group, a CF3 group or an alkylthio group; X3 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; X4 is a hydrogen atom, a halogen atom, an alkoxy group, an alkyl group, a CF3 group or an alkylthio group; R1 is an alkyl group; R2? is an alkoxy group; p is 0, 1 or 2; and each of R2? and R2?? is an alkoxy group, and (b) at least one additional fungicide.Type: ApplicationFiled: June 30, 2009Publication date: May 5, 2011Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Munekazu Ogawa, Akihiro Nishimura
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Publication number: 20110097321Abstract: The invention relates to agents which possess anti-angiogenic activity and are accordingly useful in methods of treatment of disease states associated with angiogenesis in the animal or human body. More specifically the invention concerns a combination of an antagonist of the biological activity of Angiopoietin-2 and an antagonist of the biological activity of VEGF-A, and/or KDR, and/or Flt1, and uses of such antagonists.Type: ApplicationFiled: September 24, 2010Publication date: April 28, 2011Applicant: ASTRAZENECA ABInventors: David Charles BLAKEY, Jeffrey Lester BROWN, Stephen Charles EMERY
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Publication number: 20110098324Abstract: The invention described herein relates to certain pyrimidinedione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: June 23, 2009Publication date: April 28, 2011Inventors: James A. Brackley, III, Antony Nicholas Shaw, Rosanna Tedesco, Yonghui Wang, Kenneth J. Wiggall, Hongyi Yu
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Patent number: 7923460Abstract: The BRAF gene has been found to be activated by mutation in human cancers, predominantly in malignant melanoma. We tested 476 primary tumors, including 214 lung, 126 head and neck, 54 thyroid, 27 bladder, 38 cervical, and 17 prostate cancers, for the BRAF T1796A mutation by polymerase chain reaction (PCR)-restriction enzyme analysis of BRAF exon 15. In 24 (69%) of the 35 papillary thyroid carcinomas examined, we found a missense thymine (T)?adenine (A) transversion at nucleotide 1796 in the BRAF gene (T1796A). The T1796A mutation was detected in four lung cancers and in six head and neck cancers but not in bladder, cervical, or prostate cancers. Our data suggested that activating BGRAF mutations may be an important even in the development of papillary thyroid cancer. Moreover, BRAF mutation reliably predicts a poor prognosis for papillary thyroid carcinomas.Type: GrantFiled: May 21, 2008Date of Patent: April 12, 2011Assignee: The Johns Hopkins UniversityInventors: David Sidransky, Yoram Cohen, Mingzhao Xing
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Patent number: 7910610Abstract: The present invention relates to methods involving avoiding adverse drug interactions with fluvoxamine and pirfenidone or other moderate to strong inhibitors of CYP enzymes.Type: GrantFiled: October 8, 2010Date of Patent: March 22, 2011Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Publication number: 20110065759Abstract: The present invention relates to a compound of formula I, in all its isomeric forms and pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 3, 2010Publication date: March 17, 2011Inventors: Stephan Roever, Matthew Wright
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Patent number: 7902372Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.Type: GrantFiled: April 2, 2008Date of Patent: March 8, 2011Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
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Publication number: 20110053938Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.Type: ApplicationFiled: September 2, 2010Publication date: March 3, 2011Applicant: CANTHERA THERAPEUTICS, INC.Inventors: Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam Lee
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Publication number: 20110039851Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.Type: ApplicationFiled: October 14, 2008Publication date: February 17, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
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Publication number: 20110034463Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.Type: ApplicationFiled: April 1, 2009Publication date: February 10, 2011Inventors: Jon Goguen, Ning Pan, Kyungae Lee
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Publication number: 20110021523Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: October 1, 2010Publication date: January 27, 2011Applicant: CHEMOCENTRYX, INC.Inventors: Solomon Ugashe, Zheng Wei, J.J. Wright, Andrew Pennell
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Publication number: 20110008461Abstract: A PEPCK inhibitor can include identifying a molecule that has a size capable of fitting into and interacting with the PEPCK binding site and at least one of the following: (a) a first terminal substituent having co-planar atoms acting as metal ligands to the active site metal ion PEPCK; (b) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent includes a neutral carbon center or include an oxygen, sulfur, selenium, or other atom with similar physiochemical properties; (c) at least one of an atom or substituent at positions 2 or 3 from the first terminal substituent is devoid of an electropositive atom or substituents; or (d) a second terminal substituent opposite of the first terminal substituent, said second terminal substituent having an atom that is a hydrogen boding acceptor and/or is negatively charged.Type: ApplicationFiled: July 12, 2010Publication date: January 13, 2011Inventors: Gerald Carlson, Todd Holyoak, Sarah Sullivan, Rose Mary Stiffin
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Publication number: 20100331374Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: August 20, 2010Publication date: December 30, 2010Inventors: Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer, Richard Masaru Kawamoto
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Publication number: 20100311689Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-1 or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-1 in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-1 and another therapeutic agent.Type: ApplicationFiled: October 31, 2008Publication date: December 9, 2010Applicant: ZIOPHARM Oncology, IncInventors: Barbara P. Wallner, Philip B. Komarnitsky
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Publication number: 20100298138Abstract: The present invention relates to the use of aminoazoline and urea derivatives for com-bating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds and to specific azoline and urea derivatives.Type: ApplicationFiled: May 23, 2008Publication date: November 25, 2010Applicant: BASF SEInventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
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Publication number: 20100298221Abstract: The present invention relates to novel 2-phenoxy-6-phenyl- and 2-phenoxy-6-pyridylnicotinic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prophylaxis of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis and heart failure.Type: ApplicationFiled: August 30, 2007Publication date: November 25, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Heinrich Meier, Peter kolkhof, Axel Kretschmer, Arounarith Tuch, Lars Barfacker, Yolanda Cancho Grande
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Patent number: 7838541Abstract: This invention relates to methods of using aryl ureas to treat diseases mediated by the VEGF induced signal transduction pathway characterized by abnormal angiogenesis or hyperpermeability processes.Type: GrantFiled: February 11, 2003Date of Patent: November 23, 2010Assignee: Bayer Healthcare, LLCInventors: Jacques Dumas, William J. Scott, James Elting, Holia Hatoum-Makdad
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Patent number: 7838526Abstract: Essential tremor can effectively be treated with high doses of Riboflavin (vitamin B2), either on its own or coupled with one or more other B vitamins and/or coenzyme Q10 (CoQ10). The treatment constitutes a significant improvement over prior treatment methods in that it not only alleviates essential tremor, but results in better performance of the affected body portion and may delay the progression of the disease. The preferred addition of other B vitamins and/or CoQ10 also provides balance to the nutrient energy requirements of a patient's body.Type: GrantFiled: July 20, 2006Date of Patent: November 23, 2010Inventor: Esther Baldinger
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Publication number: 20100285006Abstract: The present invention relates to novel thiazole-substituted indolin-2-ones as inhibitors of CSCPK and related kinases; to methods of inhibiting cancer stem cells by using a kinase inhibitor; to pharmaceutical compositions containing such compounds; and to methods of using such compounds in the treatment of a protein kinase related disorder in a mammal; and to processes of making such compounds and intermediates thereof.Type: ApplicationFiled: September 5, 2008Publication date: November 11, 2010Inventors: Chiang Jia LI, Ji-Feng Liu, Youzhi Li, Wei Li, Harry Rogoff
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Publication number: 20100286146Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: April 27, 2010Publication date: November 11, 2010Applicant: Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger
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Publication number: 20100285012Abstract: The subject application provides small compounds that are able to suppress autophagy in various cells. These compounds are useful in augmenting the existing treatments of various cancers and microbial/parasitic infections. Thus, the subject application also provides methods of treating various types of cancers and microbial/parasitic infections. Also provided by the subject application are methods of suppressing the expansion of autophagosomes within cells or individuals and inhibiting the lipidation of autophagy-related protein 8 (Atg8).Type: ApplicationFiled: January 5, 2009Publication date: November 11, 2010Applicant: University of FLorida Research Foundation Inc.Inventors: William A. Dunn, JR., Debra E. Akin, Ann Progulske-Fox, David A. Ostrov