Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: 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.
Abstract: The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity.
Type:
Grant
Filed:
August 19, 2003
Date of Patent:
February 8, 2011
Assignee:
Lorus Therapeutics Inc.
Inventors:
Raed Al-Qawasmeh, Aiping H. Young, Mario Huesca, Yoon Lee
Abstract: 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:
Application
Filed:
October 8, 2010
Publication date:
February 3, 2011
Inventors:
Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
Abstract: There is presently provided methods for delivering a neuroprotective agent to a neural cell. The methods comprise contacting a neural cell with an imidazolium or imidazolinium compound as described herein, including an imidazolium or imidazolinium salt.
Type:
Application
Filed:
March 31, 2009
Publication date:
February 3, 2011
Inventors:
Lang Zhuo, Gideon Ho, Yugen Zhang, Jackie Y. Ying
Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
Type:
Application
Filed:
August 4, 2008
Publication date:
January 13, 2011
Inventors:
Zhaoning Zhu, William J. Greenlee, John P. Caldwell, Robert D. Mazzola, JR., Brian McKittrick, Chad E. Bennett, Xianhai Huang, Hubert B. Josien, Duane A. Burnett
Abstract: 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:
Application
Filed:
July 21, 2010
Publication date:
December 30, 2010
Applicant:
Schering Corporation
Inventors:
Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
Abstract: The present invention relates to the inhibition of melanogenesis with para-aminobenzoic acid (PABA) and its use in treating melanotic cancer.
Type:
Application
Filed:
February 5, 2010
Publication date:
December 23, 2010
Applicant:
NEW YORK UNIVERSITY
Inventors:
Peter C. Brooks, Danielle Morais, Dorothy Rodriguez
Abstract: This disclosure concerns compounds which are useful as inhibitors of spleen tyrosine kinase (Syk) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of Syk. This disclosure also relates to pharmaceutical compositions containing these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Type:
Application
Filed:
June 14, 2010
Publication date:
December 16, 2010
Inventors:
Jing Zhang, Rajinder Singh, Dane Goff, Taisei Kinoshita
Abstract: The present invention relates to new cyclobutanemethanamine inhibitors of monoamine reuptake, pharmaceutical compositions thereof, and methods of use thereof.
Type:
Application
Filed:
December 4, 2009
Publication date:
December 9, 2010
Applicant:
AUSPEX PHARMACEUTICALS, INC.
Inventors:
Thomas G. Gant, Sepehr Sarshar, Manouchehr M. Shahbaz
Abstract: The present invention is directed to multiple a-lipoic acid-containing hydrophobic compounds (mALAs) capable of acting as scavengers of free radicals, metals and reactive oxygen species (ROS). Methods of synthesizing novel antioxidant mALAs, spontaneous emulsification or nanoprecipitaion thereof to produce antioxidant nanospheres and their use in preventing or treating diseases or conditions caused by oxidative stress and other free radical mediated conditions are also described. Another aspect of this invention is the use of these antioxidant nanospheres for the preparation of antioxidant particulate delivery system of therapeutic agents.
Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM 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:
Application
Filed:
December 16, 2008
Publication date:
November 11, 2010
Applicant:
PHARMINOX LIMITED
Inventors:
Malcolm Francis Graham Stevens, David Cousin, Sharon Jennings, Andrew James McCarroll, John Gareth Williams, Marc Geoffery Hummersone, Jihong Zhang
Abstract: The present invention discloses novel compounds of Formula I: (I) having 11?-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11?-HSD type 1 activity.
Type:
Grant
Filed:
April 19, 2007
Date of Patent:
October 26, 2010
Assignee:
Eli Lilly and Company
Inventors:
Ashraf Saeed, Owen Brendan Wallace, Yanping Xu, Thomas Edward Mabry, Rebecca Lynn Rezac Guenther, Nancy June Snyder
Abstract: Formula (I) compounds are described: Formula (I) where the radicals are as defined in the description, processes for their preparation, and their uses for the preparation of conjugates with radionuclides for use in human and animal therapy and diagnostics, particularly for the diagnosis and therapy of pathological conditions such as tumors.
Abstract: The present invention mainly aims to provide a drug for the prophylaxis or treatment of androgen-independent prostate cancer, which is highly useful as a pharmaceutical agent. The present invention provides a drug for the prophylaxis or treatment of androgen-independent prostate cancer, containing a steroid C17,20 lyase inhibitor, particularly, a compound represented by the formula (I): wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof or a prodrug thereof.
Abstract: 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 subs
Type:
Application
Filed:
September 17, 2009
Publication date:
September 30, 2010
Inventors:
Karl Richard Gibson, Martin Peter Green, Toby James Underwood, Florian Wakenhut
Abstract: Disclosed, is a composition for reducing the levels or level of glucose, malondialdehyde-modified LDL, homocysteine, and/or C-reactive protein in the blood. Specifically disclosed is a composition for reducing the level of at least one substance selected from the group consisting of glucose, malondialdehyde-modified LDL, homocysteine, and C-reactive protein in the blood, which comprises the following components (a) and (b): (a) at least one component selected from the group consisting of vitamin B12, vitamin B6, and folic acid; and (b) at least one component selected from the group consisting of zinc, selenium, and an antioxidant vitamin.
Abstract: There are disclosed methods and kits for treating cancer in a patient in need of such treating comprising administering temozolomide according to improved dosing schedules.
Type:
Application
Filed:
March 31, 2010
Publication date:
September 23, 2010
Inventors:
WALTER ROBERT BISHOP, PAUL KIRSCHMEIER, MING LIU
Abstract: The present invention relates to thienopyrrole compounds of formula (I); wherein A, B, Y, Ar, n, Z and X1 are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.
Type:
Grant
Filed:
September 7, 2004
Date of Patent:
August 24, 2010
Assignee:
Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
Inventors:
Barbara Attenni, Jose Ignacio Martin Hernando, Savina Malancona, Frank Narjes, Jesus Maria Ontoria Ontoria, Michael Rowley
Abstract: This invention relates to methods and drug products for treating proliferative disorders using intravenous formulations comprising temozolomide over a specific infusion time. These methods and drug products are particularly well-suited for patients who cannot swallow oral formulations. These methods and drug products also afford an added convenience to patients who are already receiving other therapeutic treatments.
Abstract: The present invention provides methods for the treatment of respiratory tract mucositis in individuals in need of such treatment, the method comprising the systemic administration to the individual of therapeutically effective amounts of at least one anti-fungal agent and at least one anti-bacterial agent, wherein the treatment does not involve the cessation of use of emollients by the individual. The present invention also provides compositions suitable for use in the treatment of respiratory tract mucositis.
Abstract: A pharmaceutical composition comprising an anticholinergic and at least one additional active ingredient selected from among corticosteroids, dopamine agonistes, PDE-IV inhibitors, NK1-antagonists, endothelin antagonists, antihistamines, and EGFR-kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.
Type:
Grant
Filed:
December 8, 2004
Date of Patent:
August 17, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Michel Pairet, Michael P. Pieper, Christopher John Montague Meade, Richard Reichl, Christel Schmelzer, Birgit Jung
Abstract: There are provided compounds according to formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia. Also provided are pharmaceutical compositions containing such compounds and processes for preparing some of the compounds of the invention. Other embodiments are also disclosed.
Type:
Grant
Filed:
October 31, 2007
Date of Patent:
August 10, 2010
Assignee:
Bristol-Myers Squibb Company
Inventors:
Chong-qing Sun, Lawrence Hamann, David Augeri, Yingzhi Bi, Jeffrey Robl, Yan-Ting Huang, Tammy Wang, Alexandra Holubec, Ligaya Simpkins, James C. Sutton, James J. Li
Abstract: 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.
Abstract: The invention features compositions and methods that are useful for the treatment of neoplasia by reducing base excision repair (BER). Such compositions are useful, for example, for enhancing the efficacy of known chemotherapeutics, such as DNA alkylating agents. In particular, the invention features agents that mimic the interaction of APC with pol-?. Such agents reduce the activity of long patch- and single nucleotide-base extension repair pathways.
Type:
Application
Filed:
February 14, 2008
Publication date:
July 29, 2010
Applicant:
University of Florida Research Foundation
Inventors:
Satya Narayan, Aruna S. Jaiswal, David A. Ostrov
Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
January 19, 2007
Date of Patent:
July 6, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula I wherein A, X, Y, Z, Ra, Rb, Rc, R1, R2, R3 and m are defined herein.
Type:
Grant
Filed:
August 14, 2006
Date of Patent:
July 6, 2010
Assignees:
Genentech, Inc., Hoffman-LaRoche, Inc. (US Only), F. Hoffman-LaRoche, AG (EX-US)
Inventors:
Thomas E. Rawson, Brian Safina, Jennafer Dotson, Aihe Zhou, Ignacio Aliagas-Martin, Jason Halladay, Jun Liang, Matthias Rueth, Bing-Yan Zhu, Frederick Brookfield, Michael Prime, Birong Zhang, Jun M. Li
Abstract: A pharmaceutical composition for transdermal delivery comprising one or more physiologically active agents; one or more dermal penetration enhancers; and a volatile pharmaceutically acceptable carrier comprising a volatile solvent; and wherein the physiologically active agent and dermal penetration enhancer form an amorphous deposit upon evaporation of the volatile carrier, said amorphous deposit forming a reservoir within the stratum corneum; and (A) wherein the composition has a release rate profile of physiologically active agent so as to provide a ratio of the maximum concentration (Cmax) to the average concentration (Cavg) for the physiologically active agent over the dosage interval within the range of 1 to 10.
Type:
Application
Filed:
December 18, 2009
Publication date:
July 1, 2010
Inventors:
Timothy Matthias Morgan, Nina Frances Wilkins, Kathryn Taci-Jane Klose, Barrie Charles Finnin, Barry Leonard Reed
Abstract: A novel therapeutic agent for hyperlipidemia, which is an ester compound represented by the formula (1?) (wherein R1 and R2 are each hydrogen atom or optionally substituted aryl, etc.; X is —COO— or —CON(R10)—; R3 and R4 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R5, R6 and R7 are each hydrogen atom, C1-C6 alkyl or C1-C6 alkoxy, etc.; R9 and R9 are each independently hydrogen atom, C1-C6 alkyl, —CON(R18) (R19) or —COO(R20), etc.; ring A, ring B and ring C are each independently aryl or heterocycle residue, etc.; Alk1 and Alk2 are each independently alkanediyl, etc.; l and m are each an integer of 0 or 1 to 3) or a prodrug thereof, or a pharmaceutically acceptable salt of either. The therapeutic agent selectively inhibits MTP in the small intestine, thus causes no such side effect as a fatty liver.
Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R1, R2, Q, T, n and p 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 aldosterone synthase inhibitors.
Type:
Application
Filed:
March 27, 2008
Publication date:
June 10, 2010
Inventors:
Peter Herold, Robert Mah, Stefan Stutz, Vincenzo Tschinke, Aleksandar Stojanovic, Nathalie Jotterand, Bibia Bennacer
Abstract: The present invention relates to new phenylalanine amide inhibitors of ATP-sensitive potassium channels, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: The present invention provides a method of treatment, prevention and/or delay of progression of neuropathic pain by a specific dosing regime of acetam derivatives.
Type:
Application
Filed:
September 24, 2009
Publication date:
May 20, 2010
Applicant:
NEUROTUNE AG
Inventors:
Carlo Farina, Carla Ghelardini, Ruggero Fariello
Abstract: Methods are provided for treating a subject for a condition. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is modulated during at least one predetermined phase of the subject's menstrual cycle to alter the parasympathetic activity/sympathetic activity ratio in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, including various disease conditions, that increase in severity and/or occurrence during one or more phases of the menstrual cycle. Also provided are systems and kits for use in practicing the subject methods.
Type:
Application
Filed:
December 24, 2009
Publication date:
May 13, 2010
Inventors:
Anthony Joonkyoo Yun, Partic Yuarn-Bor Lee
Abstract: The present disclosure provides compounds that function as modulators of aldehyde dehydrogenase (ALDH) enzymatic activity, as well as compositions and formulations comprising the compounds. The present disclosure provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition.
Type:
Application
Filed:
October 19, 2009
Publication date:
May 6, 2010
Inventors:
Daria Mochly-Rosen, Che-Hong Chen, Wenjin Yang
Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.
Type:
Application
Filed:
March 20, 2008
Publication date:
May 6, 2010
Applicant:
Givaudan SA
Inventors:
Boris Schilling, Wolf D. Woggon, Antoinette Chougnet, Thierry Granier, Georg Frater, Andreas Hanhart
Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
Type:
Grant
Filed:
September 21, 2005
Date of Patent:
May 4, 2010
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Shoujun Chen, Jun Jiang, Hao Li, David James, Dinesh Chimmanamada, Christopher Borella, Lijun Sun, Yu Xie, Mats Holmqvist, Jerome Mahiou, Zhi Qiang Xia
Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.
Type:
Application
Filed:
October 26, 2007
Publication date:
April 29, 2010
Inventors:
Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
Abstract: This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex.
Type:
Grant
Filed:
October 20, 2004
Date of Patent:
April 20, 2010
Assignees:
N. V. Organon, Neurosearch A/S
Inventors:
Niall Morton Hamilton, Susan Elizabeth Napier, Morag Ann MacCall Easson, Andrew John Cooke, Lene Teuber, Naheed Mirza, Frank Wätjen
Abstract: The present invention provides methods for discovering agents that are effective in reversing epigenetic silencing by inhibiting the interaction of methyl-binding (MBD) proteins with methylated genomic DNA. Also provided are methods for reactivating silenced genes having CpG island hypermethylation along with methods for treatment and prevention of diseases, such as cancer and sickle cell anemia, by administering an agent that modulates methyl-binding domain (MBD) protein-mediated transcriptional repression, thereby increasing gene transcription to prevent or treat disease. Additionally, compounds identified by the present invention useful for treatment and prevention of diseases, such as cancer and sickle cell anemia, are provided.
Type:
Application
Filed:
December 21, 2007
Publication date:
April 15, 2010
Inventors:
William G. Nelson, Srinivasan Yegnasubramanian, Xiaohui Lin, Traci J. Speed, Zachery Reichert