Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Patent number: 8263615Abstract: Heterocyclic compounds of the general formula (I) are provided in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldostereone synthase inhibitors,Type: GrantFiled: October 8, 2010Date of Patent: September 11, 2012Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
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Publication number: 20120220640Abstract: The present invention relates to computer-implemented methods and system for analysing a biomarker which cycles in a subject. In some other aspects, the present invention relates to analysing a biomarker which at least initially increases or decreases in amount in a subject following a treatment for a disease. In further aspects, the present invention relates to computer-implemented methods and systems for determining a preferred time to administer a therapy to treat a disease in a subject. The present invention also relates to computer program product to implement the methods. Further, the present invention relates to methods of determining the timing of treating a disease in a subject in which the immune system is cycling.Type: ApplicationFiled: May 27, 2010Publication date: August 30, 2012Applicant: IMMUNAID PTY LTDInventors: Martin Leonard Ashdown, Andrew Robinson
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Publication number: 20120219541Abstract: This invention provides a compositions for transport of a therapeutic agent. The compositions contain a therapeutic agent and a monoterpene or an analog thereof. In one aspect, the monoterpene is perillyl alcohol (POH) or an analog thereof. In one aspect, the therapeutic agent is provided in an amount effective to treat the disease or subject of choice.Type: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Inventors: Thomas C. Chen, Clovis O. da Fonseca, Thereza Quirico dos Santos, Gilberto Schwartsmann
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Patent number: 8242155Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available ALDARA 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for ALDARA 5% imiquimod cream to treat actinic keratosis are also disclosed and described.Type: GrantFiled: July 13, 2011Date of Patent: August 14, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
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Publication number: 20120202834Abstract: The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.Type: ApplicationFiled: February 7, 2012Publication date: August 9, 2012Applicant: PFIZER INC.Inventors: Gary Erik Aspnes, Mary Theresa Didiuk, Kevin James Filipski, Angel Guzman-Perez, Esther Cheng Yin Lee, Jeffrey Allen Pfefferkorn, Benjamin Dawson Stevens, Meihua Mike Tu
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Patent number: 8236816Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available ALDARA 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for ALDARA 5% imiquimod cream to treat actinic keratosis are also disclosed and described.Type: GrantFiled: July 12, 2011Date of Patent: August 7, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
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Patent number: 8232269Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein, R1 and R2 each independently represent H, halogen, CF3, C1-3 alkyl or C1-3 alkoxy; R3 represents C1-6 alkyl, C3-6 cycloalkyl, phenyl (optionally substituted by one or more substituents each independently selected from Ra) or Het (optionally substituted by one or more substituents each independently selected from OH, oxo, or C1-4 alkyl); R4 represents H or C1-3 alkyl; R5 represents C1-6 alkyl (optionally substituted by one or more substituents each independently selected from Rb), C3-6 cycloalkyl (optionally substituted by one or more substituents each independently selected from oxo or OH), or Het2 (optionally substituted by one or more substituents each independently selected from Rd); oxygen atom or 1 sulphur atom, or (c) 1 oxygen atom or 1 sulphur atom, (optionally substituted by one or more substituents each independently selected from OH, oxo or C1-4 alkyl); and R6 represents C1-3 alkyl (optionally substituType: GrantFiled: September 17, 2009Date of Patent: July 31, 2012Assignee: Pfizer Inc.Inventors: Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
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Patent number: 8222287Abstract: 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: GrantFiled: March 29, 2010Date of Patent: July 17, 2012Assignee: National Defense Medical CenterInventor: Hsu-Shan Huang
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Patent number: 8221799Abstract: The invention is directed to a method for administering antioxidant micronutrient formulations comprising multiple dietary and endogenous antioxidants, B-vitamins, vitamin D and minerals at appropriate dosages and dose schedules particularly chosen to produce long-term ‘optimal health’ effects in individuals of various age groups and occupations, with particular emphasis on reducing and/or eliminating acute and/or long term effects of environmental and physical stressors and toxic chemicals to which current Operating Forces and veterans of military service are or have been exposed.Type: GrantFiled: February 5, 2007Date of Patent: July 17, 2012Assignee: Premier Micronutrient CorporationInventors: Kedar N. Prasad, Gerald M. Haase, William C. Cole
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Patent number: 8222277Abstract: The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders comprising administration of novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent.Type: GrantFiled: December 28, 2010Date of Patent: July 17, 2012Assignee: NiCox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Patent number: 8222270Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1-isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine or 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine, i.e., imiquimod, to treat actinic keratosis with short durations of therapy, than currently prescribed for the commercially available ALDARA 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating actinic keratosis with an acceptable safety profile and dosing regimens that are short and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for ALDARA 5% imiquimod cream to treat actinic keratosis are also disclosed and described.Type: GrantFiled: July 8, 2011Date of Patent: July 17, 2012Assignee: Medicis Pharmaceutical CorporationInventors: Michael T. Nordsiek, Sharon F. Levy, James H. Lee, James H. Kulp, Kodumudi S. Balaji, Tze-Chiang Meng, Jason J. Wu, Valyn S. Bahm, Robert Babilon
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Patent number: 8211906Abstract: Disclosed is a method of inhibiting the growth of neoplastic tumors and lesions and localized infections by administering an Immune Response Modifier (IRM) drug to human patients suffering from such tumors, lesions or infections. IRMs act by stimulating cellular immunity and have been found to have both anti-viral and anti-tumor effects. By administering IRM drugs directly into a tumor, lesion or infection, the cells of the tumor, lesion or infection, as well as those surrounding the tumor, lesion or infection can be stimulated to increase their cellular response, thereby inhibiting the growth of such tumors, lesions or infections.Type: GrantFiled: August 4, 2004Date of Patent: July 3, 2012Inventor: Lawrence C. Scherrer
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Publication number: 20120164103Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: March 9, 2012Publication date: June 28, 2012Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Patent number: 8193228Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: October 16, 2007Date of Patent: June 5, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: David Chen, Christopher L. Franklin, Peter R. Guzzo, Linus S. Lin, Michael M. C. Lo, Ravi P. Nargund, Iyassu K. Sebhat
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Patent number: 8193214Abstract: Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase.Type: GrantFiled: September 27, 2007Date of Patent: June 5, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Stéphane De Lombaert, Michel Jose Emmanuel
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Publication number: 20120129854Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the yield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: April 27, 2010Publication date: May 24, 2012Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Patent number: 8183275Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: GrantFiled: October 16, 2007Date of Patent: May 22, 2012Assignees: Merck Sharp & Dohme Corp., Albany Molecular Research, Inc.Inventors: Peter H. Dobbelaar, Christopher L. Franklin, Allan Goodman, Cheng Guo, Peter R. Guzzo, Mark Hadden, Shuwen He, Alan J. Henderson, Tianying Jian, Linus S. Lin, Jian Liu, Ravi P. Nargund, Megan Ruenz, Bruce J. Sargent, Iyassu K. Sebhat, Larry Yet
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Publication number: 20120121534Abstract: The invention relates to a composition that can be subcutaneously or intradermally injected, comprising: a filling agent; and a fibroblast growth medium.Type: ApplicationFiled: July 6, 2010Publication date: May 17, 2012Applicant: Jean-Noel ThorelInventors: Jean-Noel Thorel, Hugues Gatto
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Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120108613Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: May 14, 2009Publication date: May 3, 2012Inventor: Jayhong A. Chong
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Patent number: 8168668Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.Type: GrantFiled: October 14, 2009Date of Patent: May 1, 2012Assignee: AstraZeneca ABInventors: Yevgeni Besidski, Martin Nylof, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
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Patent number: 8168665Abstract: The present invention relates to derivatives of 2-phenyl-benzimidazoles of the formula I, in which X, R, R1 to R3 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: March 27, 2009Date of Patent: May 1, 2012Assignee: Sanofi-AventisInventors: Gerhard Zoller, Hartmut Strobel, David William Will, Paulus Wohlfart
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Publication number: 20120083513Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and —B are as defined herein (collectively referred to herein as 38TM compounds): The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.Type: ApplicationFiled: June 23, 2010Publication date: April 5, 2012Applicant: PHARMINOX LIMITEDInventors: Marc Geoffery Hummersone, Malcolm Francis Graham Stevens, David Cousin
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Publication number: 20120076755Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B-W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 4, 2011Publication date: March 29, 2012Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
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Publication number: 20120077778Abstract: Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes.Type: ApplicationFiled: September 29, 2010Publication date: March 29, 2012Inventors: Andrea Bourdelais, Daniel Baden, Allan Goodman, Steven Fontana
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Publication number: 20120071499Abstract: There are provided compounds of the formula wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 and R6 are as described herein and enantiomers or a pharmaceutically acceptable salt or ester thereof. The compounds are useful as anticancer agents.Type: ApplicationFiled: August 18, 2011Publication date: March 22, 2012Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Jing Zhang, Zhuming Zhang
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Publication number: 20120071435Abstract: The present invention relates to the field of oncology and provides compositions and methods for treating specific cancers, including non small cell lung cancer, breast cancer, thyroid cancer, pancreatic cancer, colon cancer, melanoma, hepatoma and adenocarcinoma. Particularly, compositions and methods involving administration, either simultaneously or sequentially, of pharmaceutical combinations comprising (S)—N-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide with other compounds, to patients suffering from cancer are described.Type: ApplicationFiled: March 11, 2010Publication date: March 22, 2012Applicant: Ardea Biosciences, Inc.Inventor: Mark Chapman
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Publication number: 20120065145Abstract: This application provides compositions and methods useful in the treatment of certain cancers. In part, this application is based on the recognition that certain molecules that target abasic lesions or AP sites in DNA improve, augment, or potentiate the chemotherapeutic efficacy of certain anticancer agents.Type: ApplicationFiled: July 22, 2011Publication date: March 15, 2012Inventors: Stanton L. Gerson, Lili Liu
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Publication number: 20120053219Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.Type: ApplicationFiled: November 7, 2011Publication date: March 1, 2012Applicant: Schering CorporationInventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
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Patent number: 8124637Abstract: A series of novel anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, wherein said application includes a pharmaceutical composition containing said derivatives for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.Type: GrantFiled: February 25, 2010Date of Patent: February 28, 2012Assignee: National Defense Medical CenterInventor: Hsu-Shan Huang
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Publication number: 20120045519Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Applicant: Academia SinicaInventors: Lie-Fen SHYUR, Wen-Wan Chao, Ya-Wen Cheng
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Publication number: 20120040977Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: February 22, 2010Publication date: February 16, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Patent number: 8114898Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.Type: GrantFiled: November 17, 2008Date of Patent: February 14, 2012Assignee: Allergan, Inc.Inventors: Stuart D. Shanler, Andrew Ondo
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Patent number: 8106052Abstract: The present invention provides methods, compositions, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferin or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. Upon addition of the luciferin derivative or other luminogenic molecule into a P450 reaction, the P450 enzyme metabolizes the molecule into a bioluminescent enzyme substrate, e.g., luciferin and/or luciferin derivative metabolite, in a P450 reaction. The resulting metabolite(s) serves as a substrate of the bioluminescent enzyme, e.g., luciferase, in a second light-generating reaction. Luminescent cytochrome P450 assays with low background signals and high sensitivity are disclosed and isoform selectivity is demonstrated.Type: GrantFiled: April 5, 2010Date of Patent: January 31, 2012Assignee: Promega CorporationInventors: James J. Cali, Dieter Klaubert, William Daily, Samuel Kin Sang Ho, Susan Frackman, Erika Hawkins, Keith V. Wood
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Publication number: 20120020920Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: February 24, 2011Publication date: January 26, 2012Applicant: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
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Patent number: 8101637Abstract: The present invention relates to novel compounds of formula (I) wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors-subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: GrantFiled: June 17, 2005Date of Patent: January 24, 2012Assignee: Addex Pharma SAInventors: Anne-Sophie Bessis, Christelle Bolea, Béatrice Bonnet, Mark Epping-Jordan, Nicholas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Patent number: 8101633Abstract: The present disclosure is directed to modulators of GABAA receptors and pharmaceutically acceptable salts and prodrugs thereof, the chemical synthesis thereof, and the medical use of such compounds for the treatment and/or management of sleep disorders and/or for providing a patient in need with a hypnotic, anxiolytic or anti-convulsive effect are described.Type: GrantFiled: September 1, 2009Date of Patent: January 24, 2012Assignee: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 8097628Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: (relative chemistry shown) pharmaceutical compositions comprising them, their use in therapy especially against tuberculosis, and methods of preparing them are described.Type: GrantFiled: May 21, 2009Date of Patent: January 17, 2012Assignee: Glaxo Group LimitedInventors: Carlos Alemparte-Gallardo, Christopher Barfoot, David Barros-Aguirre, Monica Cacho-Izquierdo, Jose Maria Fiandor Roman, Alan Joseph Hennessy, Neil David Pearson, Modesto Jesus Remuinan-Blanco
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Patent number: 8093401Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: GrantFiled: August 4, 2006Date of Patent: January 10, 2012Assignee: Sirtris Pharmaceuticals, Inc.Inventors: Joseph J. Nunes, Jill Milne, Jean Bemis, Roger Xie, Chi B. Vu, Pui Yee Ng, Jeremy S. Disch
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Publication number: 20120003209Abstract: The invention encompasses methods and kits used in the identification of invasive glioblastoma based upon the expression of Akt1, Akt2, and Akt3. The methods and kits also allow prediction of disease outcome and staging of patients with regard to therapy.Type: ApplicationFiled: October 25, 2010Publication date: January 5, 2012Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: NHAN TRAN
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Publication number: 20110318334Abstract: Provided herein are compounds and methods for the treatment of brain cancer in a mammal, wherein the method comprises the administration to the mammal a compound that stabilizes tubulin dimers or microtubles at G2-M interface during mitosis but is not a substrate for MDR protein. In particular, the present application relates to the use of an orally effective abeo-taxane, alone or in combination with temozolomide or bevacizumab, for the treatment of brain cancer.Type: ApplicationFiled: August 20, 2010Publication date: December 29, 2011Inventors: James D. McChesney, Gilles TAPOLSKY, David L. EMERSON, John MARSHALL, Tauseef AHMED, Allen COHN, Michael KURMAN, Manuel MODIANO
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Publication number: 20110313010Abstract: The additive effect of combined intracranial carmustine (“BCNU”) with intracranial temozolomide (“TMZ”), and particularly in combination with radiation (“XRT”), in the treatment of two rat intracranial glioma models, the 9L gliosarcoma and the F98 glioma, demonstrates that local delivery of both drugs, especially in combination with radiation, is far more effective than delivery of either drug alone or one systemically and one locally, either with or without radiation. The triple therapy showed a significant improvement in survival when compared to controls (p=0.0004), local BCNU (p=0.0043), oral TMZ (p=0.0026), local TMZ (p=0.0105), and the combinations of either BCNU and XRT (p=0.0378) or oral TMZ and local BCNU (p=0.0154).Type: ApplicationFiled: June 17, 2011Publication date: December 22, 2011Inventors: Violette Renard Recinos, Betty Tyler, Sarah Brem Sunshine, Henry Brem
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Patent number: 8080560Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: February 24, 2006Date of Patent: December 20, 2011Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Publication number: 20110306584Abstract: This invention provides a novel class of substituted macrocyclic metallic compounds. The compounds are useful as peroxynitrite decomposition catalysts. Pharmaceutical compositions, and methods of making and using the compounds, or a pharmaceutically acceptable salt, hydrate, or prodrug thereof are also described.Type: ApplicationFiled: October 5, 2007Publication date: December 15, 2011Applicant: TRUSTEES OF PRINCETONInventor: John T. Groves
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Publication number: 20110305681Abstract: A topical hair care formulation and method of making includes combining herbal powders to form a herbal powder mixture. The herbal powder mixture is steeped in an amount of carrier oil for a period of time to form an infused oil. A portion of an amount of olive oil is combined with an amount of biotin and an amount of an organosulfur compound to form a natural mixture. A remainder of the amount of olive oil is combined with the infused oil. An amount of jojoba oil is combined with the infused oil. An amount of rosemary oil is combined with the infused oil. An amount of lavender oil is combined with the infused oil. The natural mixture is combined with the infused oil. The infused oil is settled for a period of time to form the topical hair care formulation.Type: ApplicationFiled: August 23, 2011Publication date: December 15, 2011Inventor: Lavonda D. Anderson
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Patent number: 8067457Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: GrantFiled: October 26, 2006Date of Patent: November 29, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20110280860Abstract: The present invention provides a process for purifying a monoterpene or sesquiterpene having a purity greater than about 98.5% (w/w). The process comprises the steps of derivatizing the monoterpene (or sesquiterpene) to produce a monoterpene (or sesquiterpene) derivative, separating the monoterpene (or sesquiterpene) derivative, and releasing the monoterpene (or sesquiterpene) from the derivative. Also encompassed by the scope of the present invention is a pharmaceutical composition comprising a monoterpene (or sesquiterpene) having a purity greater than about 98.5% (w/w). The purified monoterpene can be used to treat a disease such as cancer. The present monoterpene (or sesquiterpene) may be administered alone, or may be co-administered with radiation or other therapeutic agents, such as chemotherapeutic agents.Type: ApplicationFiled: March 3, 2011Publication date: November 17, 2011Inventors: Thomas Chen, Daniel Levin, Satish Puppali
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Publication number: 20110275680Abstract: The invention relates to novel chemical compounds, in particular oxime derivatives of 3,5-seco-4-nor-cholestane, to the application thereof as drugs, in particular cytoprotective drugs, and more particularly as neuroprotective, cardioprotective and/or hepatoprotective drugs.Type: ApplicationFiled: December 17, 2009Publication date: November 10, 2011Applicant: TROPHOSInventors: Cyrille Drouot, Abdesslame Nazih, Corinne Chaimbault
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Publication number: 20110262426Abstract: The invention encompasses methods and kits used in the identification of invasive glioblastoma based upon the expression of TROY. The methods and kits also allow prediction of disease outcome as well as therapeutic outcome.Type: ApplicationFiled: October 25, 2010Publication date: October 27, 2011Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: NHAN TRAN