Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Publication number: 20130324529Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: JANSSEN PHARMACEUTICA NVInventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
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Publication number: 20130324541Abstract: The present invention relates to an agent for potentiating an antitumor activity of a chemotherapeutic agent against a cancer containing cancer stem cells, which contains at least one kind of branched chain amino acid selected from isoleucine, leucine and valine, or a salt thereof. In addition, the present invention relates to an agent for treating a cancer containing cancer stem cells, which contains a combination of a chemotherapeutic agent and at least one kind of branched chain amino acid selected from isoleucine, leucine and valine, or a salt thereof. Furthermore, the present invention relates to an agent for preventing metastasis or recurrence of a cancer containing cancer stem cells, which contains a combination of a chemotherapeutic agent and at least one kind of branched chain amino acid selected from isoleucine, leucine and valine, or a salt thereof.Type: ApplicationFiled: August 13, 2013Publication date: December 5, 2013Applicant: Kurume UniversityInventors: Shinobu NISHITANI, Hirohisa Yano
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Patent number: 8598188Abstract: This invention relates to an antitumor agent comprising carboplatin and a combination drug of tegafur/gimeracil/oteracil potassium to be administered to a cancer patient selected according to an expression level of thymidylate synthase gene.Type: GrantFiled: March 8, 2010Date of Patent: December 3, 2013Assignees: Kinki University, Taiho Pharmaceutical Co., Ltd.Inventors: Kazuhiko Nakagawa, Isamu Okamoto
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Patent number: 8598175Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: December 3, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Nathalie Chereze, Thierry Gallet, Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Publication number: 20130317048Abstract: The invention relates to the combination of an endothelin receptor antagonist of formula (I) with paclitaxel, and in particular to this combination for therapeutic use, simultaneously, separately or over a period of time, in the treatment of ovarian cancer.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Martine Clozel, Urs Regenass
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Publication number: 20130315983Abstract: The invention provides compositions with low toxicity and high bioavailability for treating cancer or for inhibiting the development of cancerType: ApplicationFiled: May 24, 2013Publication date: November 28, 2013Applicant: The Research Foundation of the City University of New YorkInventors: Linda S. Einbond, Stephen Redenti
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Publication number: 20130317044Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: ApplicationFiled: November 27, 2012Publication date: November 28, 2013Applicant: Abbott Gmbh & Co. KGInventor: Abbott Gmbh & Co. KG
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Publication number: 20130317040Abstract: The present invention is directed to a method of treating systemic lupus erythematosus (SLE) in a subject comprising administering to the subject an amount of an HIV protease inhibitor effective to treat SLE. The present invention is also directed to a pharmaceutical product comprising an HIV protease inhibitor formulated in a pharmaceutically acceptable carrier, and a package insert providing instructions for the administration of the HIV protease inhibitor for the treatment of SLE. In addition, the present invention is directed to the use of an HIV protease inhibitor for the preparation of a medicament for the treatment of SLE.Type: ApplicationFiled: December 21, 2011Publication date: November 28, 2013Applicant: The Feinstein Institute of Medical ResearchInventors: Yousef Al-Abed, Betty A. Diamond
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Publication number: 20130317024Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: May 22, 2013Publication date: November 28, 2013Applicant: NOVARTIS AGInventors: Simona Cotesta, Pascal Furet, Vito Guagnano, Philipp Holzer, Joerg Kallen, Robert Mah, Keiichi Masuya, Achim Schlapbach, Stefan Stutz, Andrea Vaupel
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Patent number: 8592437Abstract: The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.Type: GrantFiled: October 27, 2009Date of Patent: November 26, 2013Assignees: Sanofi, Mitsubishi Tanabe Pharma CorporationInventors: Alistair Lochead, Mourad Saady, Corinne Veronique, Philippe Yaiche
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Publication number: 20130310403Abstract: The present invention relates to a fluoro-homoneplanocin A, its nucleoside derivative, and synthetic methods. The novel fluoro-homoneplanocin A and its nucleoside derivative in the present invention have an effect on cancer prevention or treatment, and therefore can be used as anticancer drugs.Type: ApplicationFiled: April 11, 2013Publication date: November 21, 2013Applicant: EWHA UNIVERSITY - INDUSTRY COLABORATION FOUNDATIONInventor: EWHA UNIVERSITY - INDUSTRY COLLABORATION FOUNDATION
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Publication number: 20130310347Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.Type: ApplicationFiled: May 21, 2013Publication date: November 21, 2013Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
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Publication number: 20130310358Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, and L, A, and Ra are defined herein.Type: ApplicationFiled: July 25, 2013Publication date: November 21, 2013Applicant: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Haiyan Bian, Peter J. Connolly, Giles Bignan, Chaozhong Cai, Scott L. Dax, Bart L. DeCorte, Shu-Chen Lin, Li Liu, Mark J. Macielag, Philip M. Pitis, Yue-Mei Zhang, Bin Zhu, Wei He
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Publication number: 20130310374Abstract: The present invention relates to substituted imidazo[4,5-c]quinoline derivatives of formula (I), wherein R1, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of the present invention and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammation and angiogenesis related disorders.Type: ApplicationFiled: December 5, 2011Publication date: November 21, 2013Applicant: PIRAMAL ENTERPRISES LIMITED`Inventors: Sanjay Kumar, Rajiv Sharma, Vijaykumar Bhagwan Deore, Nilambari Nilkanth Yewalkar, Veena R. Agarwal, Nilesh Dagia, Nishigandha Naik
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Publication number: 20130310379Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.Type: ApplicationFiled: November 21, 2011Publication date: November 21, 2013Applicant: CONSTELLATION PHARMACEUTICALSInventors: Brian K. Albrecht, James Edmund Audia, Alexandre Gagnon, Jean-Christophe Harmange, Christopher G. Naveschuk
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Publication number: 20130310406Abstract: The disclosure provides a correlation between the expression level of the miR-193a gene, which can be regulated by its methylation status, and both tumorigenesis of and the resistance of a cancer cell to a pyrimidine antimetabolite (5-FU) based chemotherapy. In addition to the methylation status and the expression of miR-193a, its downstream genes, such as E2F1, SRSF2, and apoptotic genes such as caspase 2, are also involved and can serve as useful markers for cancer therapy prognosis and for therapy selection.Type: ApplicationFiled: March 14, 2013Publication date: November 21, 2013Inventor: JINGDE ZHU
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Publication number: 20130310407Abstract: The invention relates to the use of macitentan in combination with a cytotoxic therapy agent (such as temozolomide or paclitaxel), with radiotherapy or with both a cytotoxic therapy agent and radiotherapy, in the treatment of malignant glioma, in particular glioblastoma multiforme.Type: ApplicationFiled: February 3, 2012Publication date: November 21, 2013Applicant: ACTELION PHARMACEUTICALS LTD.Inventor: Urs Regenass
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Patent number: 8586536Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.Type: GrantFiled: December 14, 2011Date of Patent: November 19, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Melissa Fleury, Adam D. Hughes
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Publication number: 20130302319Abstract: A composition comprising a pharmaceutically effective amount of zeaxanthin or its derivative for use in treating a malignant tumor and a method of using a pharmaceutically effective amount of zeaxanthin or its derivative either alone or together with one or more pharmaceutical agents for treating a malignant tumor. The tumor may be, but is not limited to breast cancer, cervix cancer, colon cancer, cutaneous melanoma, cutaneous squamous carcinoma, hepatocellular carcinoma, lung cancer, osteosarcoma, prostate cancer, and uveal melanoma. The pharmaceutically effective amount of zeaxanthin is generally above about 0.5 mg/kg/d to about 20 mg/kg/d.Type: ApplicationFiled: March 15, 2013Publication date: November 14, 2013Applicant: The New York Eye and Ear InfirmaryInventors: Richard B. Rosen, Dan-Ning Hu
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Publication number: 20130303492Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
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Patent number: 8580805Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: August 30, 2011Date of Patent: November 12, 2013Inventor: Hubert Maehr
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Publication number: 20130296352Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has applicability as a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.Type: ApplicationFiled: June 11, 2013Publication date: November 7, 2013Inventors: Yoshihiko Norimine, Kunitoshi Takeda, Koji Hagiwara, Yuichi Suzuki, Yuki Ishihara, Nobuaki Sato
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Publication number: 20130296351Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.Type: ApplicationFiled: May 2, 2013Publication date: November 7, 2013Inventor: Pfizer Inc.
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Patent number: 8575342Abstract: Compounds of formula (I), N-oxides, pharmaceutical acceptable salts, quaternary amines or stereoisomeric forms thereof, and their use as HIV replication inhibitors, In the formula, -a1=a2-a3=a4- and -b1=b2-b3=b4- may be —C?C—C?C—; X1 may be O, NR1, etc.; R1, R2, R2a, R3, R4 and R5 are assorted substituents as defined in the specification.Type: GrantFiled: September 29, 2005Date of Patent: November 5, 2013Assignee: Tibotech Pharmaceuticals Ltd.Inventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Patent number: 8574563Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 11, 2012Date of Patent: November 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20130289013Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.Type: ApplicationFiled: June 24, 2013Publication date: October 31, 2013Inventors: Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
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Publication number: 20130287688Abstract: Methods and compositions for improving the delivery and/or efficacy of a therapy (e.g., a cancer therapy) are disclosed. In one embodiment, methods and compositions for treating or preventing a cancer (e.g., a solid tumor such as a desmoplastic tumor) by administering to a subject an anti-hypertensive agent, as a single agent or in combination with a microenvironment modulator and/or a therapy, e.g., a cancer therapy (for example, a therapeutic agent or therapy, including immunotherapy (e.g., antibodies, vaccine, cell-based), nanotherapeutics, radiation therapy, photodynamic therapy, low molecular weight chemotherapeutics, molecularly targeted therapeutics and/or oxygen radical) are disclosed.Type: ApplicationFiled: March 15, 2013Publication date: October 31, 2013Applicants: XTUIT PHARMACEUTICALS, INC., THE GENERAL HOSPITAL CORPORATIONInventors: The General Hospital Corporation, Xtuit Pharmaceuticals, Inc.
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Patent number: 8569321Abstract: The disclosure describes methods of synthesis of phosphonate ester derivatives. Preferred methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of phosphonate ester derivatives without the use of chromatographic purification methods and in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of phosphonate ester derivatives.Type: GrantFiled: August 31, 2011Date of Patent: October 29, 2013Assignee: Chimerix, Inc.Inventors: Roy W. Ware, Merrick R. Almond, Bernhard M. Lampert
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Patent number: 8569302Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: GrantFiled: July 19, 2010Date of Patent: October 29, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
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Patent number: 8569320Abstract: The invention relates to a topical gel composition for use in the treatment of actinic keratosis comprising (a) an active agent for treatment of actinic keratosis, (b) a keratolytically active agent, (c) a gel former, and (d) an organic solvent.Type: GrantFiled: June 29, 2009Date of Patent: October 29, 2013Assignee: Almirall Hermal GmbHInventors: Manfred Melzer, Carmen Matthies, Klaus Treudler, Christoph Willers, Henning Mallwitz
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Patent number: 8569322Abstract: Lamivudine oxalate, preparation method and crystalline forms thereof are disclosed. A preparation method of Lamivudine is also disclosed.Type: GrantFiled: December 23, 2010Date of Patent: October 29, 2013Assignee: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.Inventors: Yanlong Liu, Fei Liu, Xiquan Zhang
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Publication number: 20130280337Abstract: The present invention relates to methods and kits for the treatment of breast cancer based on hormone receptor status of progesterone receptor and estrogen receptor comprising the administration of a taxane alone, in combination with at least one other and other therapeutic agents, as well as other treatment modalities useful in the treatment of breast cancer. In particular, the invention relates to the use of nanoparticles comprising paclitaxel and albumin (such as Abraxane®) either alone or in combination with other chemotherapeutic agents or radiation, which may be used for the treatment of breast cancer which does not express estrogen receptor and/or progesterone receptor.Type: ApplicationFiled: February 27, 2013Publication date: October 24, 2013Inventors: Neil P. DESAI, Patrick SOON-SHIONG
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Publication number: 20130280245Abstract: Disclosed are 3-aryl-6-aryl-[1,2,4]triazolo[4,3-?]pyridines thereof, represented by the Formula (I) wherein Ar1, Ar2, R1—R3 are defined herein. Compounds having Formula (I) are inhibitors of cell proliferation. Therefore, compounds of the invention may be used to treat clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: November 16, 2011Publication date: October 24, 2013Applicant: IMPACT Therapeutics, Inc.Inventors: Suixiong Cai, Ye Edward Tian, Haijun Dong, Lei Chen, Zenghui Yu, Feng Yin, Sheng Bi, Lijun Liu, Lizhen Wu
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Publication number: 20130281366Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.Type: ApplicationFiled: December 26, 2011Publication date: October 24, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Patent number: 8563565Abstract: A compound and/or pharmacologically acceptable salt thereof represented by the formula (I) has PDE9 inhibitory action, so that the intracerebral cGMP concentration is anticipated to be elevated. The PDE9 inhibitory action and the increase in cGMP lead to the improvement of learning and memory behaviors, and the compound (I) has a potential use of a therapeutic agent for cognitive dysfunctions in Alzheimer's disease. wherein R1 is a hydrogen atom; R2 is an aromatic ring group, etc.; R3 is a hydrogen atom, etc; R4 is a hydrogen atom; R5 is an oxepanyl group, etc.; R6 is a hydrogen atom.Type: GrantFiled: October 4, 2012Date of Patent: October 22, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Yoshihiko Norimine, Kunitoshi Takeda, Koji Hagiwara, Yuichi Suzuki, Yuki Ishihara, Nobuaki Sato
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Publication number: 20130273183Abstract: 2-Pyrimidine thioesters and thiocarbonates are disclosed as effective skin brightening agents. These compounds may be formulated with dermatologically acceptable carriers to form skin brightening compositions. Methods for brightening skin and for inhibiting melanogenesis using these agents are also disclosed.Type: ApplicationFiled: April 13, 2012Publication date: October 17, 2013Applicant: EASTMAN CHEMICAL COMPANYInventors: Stephanie Kay Clendennen, Liu Deng, Neil Warren Boaz
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Publication number: 20130274227Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
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Publication number: 20130273034Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: October 17, 2013Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
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Patent number: 8557833Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: September 30, 2010Date of Patent: October 15, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Damien Fraysse, Alistair Rutherford
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Patent number: 8557834Abstract: The invention described herein relates to certain pyrimidinetrione 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: GrantFiled: November 2, 2012Date of Patent: October 15, 2013Assignee: GlaxoSmithKline LLCInventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
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Publication number: 20130267510Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.Type: ApplicationFiled: December 6, 2011Publication date: October 10, 2013Applicant: AUTIFONY THERAPEUTICS LIMITEDInventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
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Publication number: 20130267547Abstract: Prodrugs comprising a lipophilic drug linked to a transport moiety that can be taken up by a fatty acid transporter are provided. The transport moiety comprises a lipid chain connected to a hydrophilic group (e.g. a carboxylic acid, a phosphate, or a sphingosine-like moiety). Due to the presence of the transport moiety, the prodrugs are substrates for endogenous fatty acid transporter systems. The transport moiety thus serves as a carrier or targeting moiety to facilitate uptake of the entire prodrug complex by endogenous fatty acid transporter systems, thereby moving the prodrug into cells and tissues where drug distribution and effects are desired. Hydrolysis of the chemical linkage between the lipid-like moiety and the lipophilic drug releases the drug in an active form within the cells or tissues.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Inventors: Phillip M. GERK, Scott W. Walsh, Meng WANG, Andrew K. LANDSBERG
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Publication number: 20130267546Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.Type: ApplicationFiled: April 2, 2013Publication date: October 10, 2013Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of AriInventors: Sidney HECHT, Omar KHDOUR, Jun LU, Pablo ARCE
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Publication number: 20130267544Abstract: The present invention provides compositions and methods useful for treating and preventing ocular diseases by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing diseases and disorders such as but not limited to, macular edema, uveitis and diabetic retinopathy.Type: ApplicationFiled: December 16, 2011Publication date: October 10, 2013Inventors: Peter Adamson, Daniel Lee
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Patent number: 8552020Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: August 5, 2010Date of Patent: October 8, 2013Assignee: Dow AgroSciences, LLC.Inventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Patent number: 8552184Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof, and compositions comprising the same, that are useful in modulating lyn kinase activity, treating obesity, type II diabetes, metabolic syndrome, and in reducing blood glucose level, weight gain, or fat depot level, or treating a disease or condition associated with the same.Type: GrantFiled: July 1, 2009Date of Patent: October 8, 2013Assignee: Melior Pharmaceuticals I, Inc.Inventors: Andrew G. Reaume, Michael S. Saporito, Alexander R. Ochman, Christopher K. Lipinski
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Patent number: 8552021Abstract: Compounds of formula I: including any possible stereoisomers thereof, wherein: R1 is hydrogen, —C(?O)R6 or —C(?O)CHR7—NH2; R2 is hydrogen; or C1-C6alkyl or phenyl, either of which is optionally substituted with 1, 2 or 3 substituents each independently selected from halo, C1-C6alkyl, C2-C6-alkenyl and C1-C6alkoxy, hydroxy or amino, or R2 is naphtyl; or R2 is indolyl, R3 is hydrogen, C1-C6alkyl, benzyl; R4 is hydrogen, C1-C6alkyl, benzyl; or R3 and R4 together with the carbon atom to which they are attached form C3-C7cycloalkyl; R5 is C1-C10alkyl, C3-C7-cycloalkyl, benzyl, or phenyl, any of which being optionally substituted with 1, 2 or 3 substituents each independently selected from hydroxy, C1-C6alkoxy, amino, mono- and diC1-C6alkylamino; R6 is C1-C6 alkyl; R7 is C1-C6 alkyl; R8 is hydrogen or halogen; or a pharmaceutically acceptable salt or solvate thereof are useful in the prophylaxis or treatment of HCV infections.Type: GrantFiled: September 29, 2010Date of Patent: October 8, 2013Assignees: Janssen Products, L.P., Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Michael Pelcman, Bengt Christian Sund, Horst Jurgen Wahling, Pedro Manuel Passos Pinho, Anna Winqvist, Karl Magnus Nilsson
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Patent number: 8551524Abstract: A pharmaceutical composition comprising a dipeptidyl peptidase IV inhibitor and a slow release biguanide is provided. A method for treating diabetes in a patient in need thereof including administering an anti-diabetic combination comprising a DPP inhibitor and a slow release biguanide is also provided.Type: GrantFiled: September 15, 2009Date of Patent: October 8, 2013Assignee: IYCUS, LLCInventor: Ramesh Sesha
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Publication number: 20130261128Abstract: This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 16, 2011Publication date: October 3, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Osamu Sakurai, Kunio Saruta, Norimitsu Hayashi, Takashi Goi, Kenji Morokuma, Hidekazu Tsujishima, Hiroaki Sawamoto, Hiroaki Shitama, Ritsuo Imashiro