Adenosine Or Derivative Patents (Class 514/46)
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Patent number: 8580763Abstract: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.Type: GrantFiled: April 17, 2008Date of Patent: November 12, 2013Assignees: Zhanggui Wu, Zhe Jiang Medicine Co., LtdInventors: Zhanggui Wu, Weidong Ye, Jianyong Yuan, Gang Chen
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Patent number: 8580762Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 2, 2011Date of Patent: November 12, 2013Assignee: Epizyme, Inc.Inventors: Edward James Olhava, Richard Chesworth, Kevin Wayne Kuntz, Victoria M. Richon, Roy Macfarlane Pollock, Scott Richard Daigle
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Patent number: 8580753Abstract: Induction of telomere shortening, G2 arrest and apoptosis in telomerase positive cancer cells using acyclic nucleoside analogs has been disclosed. In addition, methods for impairment or prevention of tumorigenic telomerase positive cells from having a chance to grow into a tumor and methods for promoting tumor regression (decrease in size of an established tumor) using acyclic nucleoside analogs has been disclosed.Type: GrantFiled: January 6, 2012Date of Patent: November 12, 2013Assignee: ALT Solutions Inc.Inventor: Igor E. Bondarev
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Patent number: 8580296Abstract: Compositions and methods to improve the pharmacokinetic profile of S-Adenosylmethionine (SAMe) are provided, as are methods of treating various disorders using SAMe formulations with improved pharmacokinetic profiles. More specifically, the invention is directed to methods of treating a disease or disorder in a subject and/or improving the nutritional status of a subject by administering formulations exhibiting improved pharmacokinetic profiles of exogenous SAMe. The method also includes the step of orally administering compositions of the invention to the subject once per day after overnight fast; that is prior to food intake in the morning.Type: GrantFiled: December 13, 2012Date of Patent: November 12, 2013Assignee: Methylation Sciences International SRLInventors: Nancy Harrison, I. David MacDonald, Aniko Takacs-Cox, Robert Miller
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Patent number: 8575127Abstract: The invention features compounds of formula I and methods of their use as antiplatelet and antithrombotic compounds: H/N=Q?2OOOO?Q2-N, HR6/NIf)(^XMO-M??OM°?X1MQ?)r(^rfHOOHHOOQHiN?iR2 Formula (I).Type: GrantFiled: November 20, 2009Date of Patent: November 5, 2013Assignee: GLSynthesis Inc.Inventors: Ivan Borissov Yanachkov, George Edward Wright
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Publication number: 20130287767Abstract: The invention discloses 4-(arylamino)selenophenopyrimidine derivatives of formula (I), hydrates, solvates, isomers, or pharmaceutically acceptable salts thereof; process for their preparation and methods of treating or inhibiting or controlling a cell proliferative disorders, particularly cancer using said compounds. Pharmaceutical compositions comprising 4-(arylamino)selenophenopyrimidine derivatives of formula (I) are useful for the treatment, inhibition, or control of cancer.Type: ApplicationFiled: June 7, 2013Publication date: October 31, 2013Inventors: Ganga Raju GOKARAJU, Sudhakar KASINA, Venkateswarlu SOMEPALLI, Rama Raju GOKARAJU, Venkata Kanaka Ranga Raju GOKARAJU, Kiran BHUPHATIRAJU, Trimurtulu GOLAKOTI, Krishanu SENGUPTA, Venkata Krishna Raju ALLURI
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Patent number: 8569260Abstract: The present disclosure provides a process for the preparation of 2-adenosine N-pyrazole compounds exemplified by the structure shown below that are potent and selective agonists for A2A adenosine receptor, compositions comprising these compounds, and methods for using these compounds to stimulate mammalian coronary vasodilation for imaging the heart.Type: GrantFiled: August 29, 2012Date of Patent: October 29, 2013Assignee: Gilead Sciences, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
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Publication number: 20130281400Abstract: The present provides a system and method of maintaining and/or increasing cell viability by downregulating cellular metabolic rate under hypoxic conditions. The present invention also relates to a system and method of prolonging the survival of implanted cells that are under hypoxic condition until host neovascularization is achieved.Type: ApplicationFiled: November 10, 2011Publication date: October 24, 2013Applicant: Wake Forest University Health SciencesInventors: James J. Yoo, Sang Jin Lee, Jaehyun Kim, Anthony Atala
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Publication number: 20130274220Abstract: The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5?-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.Type: ApplicationFiled: November 28, 2011Publication date: October 17, 2013Applicants: Industrial Research Limited, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Keith Clinch, Peter Charles Tyler, Gary Brian Evans, Richard Hubert Furneaux
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Patent number: 8557790Abstract: The present disclosure provides the use of an A3R agonist, such as IB-MECA, for reducing in a subject, preferably, human subject, intra ocular pressure (IOP). Similarly, the invention provides a pharmaceutical composition and a method for reducing IOP in a subject making use of the A3R agonist.Type: GrantFiled: May 16, 2010Date of Patent: October 15, 2013Assignee: Can-Fite Biopharma Ltd.Inventors: Pnina Fishman, Mordechai Farbstein
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Publication number: 20130266563Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.Type: ApplicationFiled: May 17, 2013Publication date: October 10, 2013Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
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Patent number: 8551515Abstract: Compositions and methods to improve the pharmacokinetic profile of S-Adenosylmethionine (SAMe) are provided, as are methods of treating various disorders using SAMe formulations with improved pharmacokinetic profiles. More specifically, the invention is directed to methods of treating a disease or disorder in a subject and/or improving the nutritional status of a subject by administering formulations exhibiting improved pharmacokinetic profiles of exogenous SAMe. The method also includes the step of orally administering compositions of the invention to the subject once per day after overnight fast; that is prior to food intake in the morning.Type: GrantFiled: December 13, 2012Date of Patent: October 8, 2013Assignee: Methylation Sciences International SRLInventors: Nancy Harrison, I. David MacDonald, Aniko Takacs-Cox, Robert Miller
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Patent number: 8551972Abstract: The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A2A adenosine receptors (ARs).Type: GrantFiled: November 5, 2010Date of Patent: October 8, 2013Assignee: Adenosine Therapeutics, LLCInventors: Onno Kranenburg, Jarmila van der Bilt, Inne Borel Rinkes, Jayson M. Rieger
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Publication number: 20130251790Abstract: The present invention provides a pharmaceutical composition comprising a low dose of zanamivir and a process for preparing the pharmaceutical composition comprising a low dose of zanamivir. The pharmaceutical composition comprising a low dose zanamivir may be used in the treatment and/or prophylaxis of influenza. The present invention also provides a method of treatment and/or prophylaxis of influenza which comprises administering a dry powder inhaler composition comprising a low dose zanamivir. The pharmaceutical composition of the present invention comprises zanamivir and one or more pharmaceutically acceptable excipients, wherein the total daily dose of the zanamivir is less than 10 mg, preferably for administration at least once a day, and preferably wherein the composition delivers from 3 mg to 8 mg of zanamivir per administered dose.Type: ApplicationFiled: September 26, 2011Publication date: September 26, 2013Applicant: CIPLA LIMITEDInventors: Geena Malhotra, Shrinivas Madhukar Purandare
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Patent number: 8541391Abstract: The invention relates to novel crystalline forms of 5,6-dichloro-2-(isopropylamino)-1-(?-L-ribofuranosyl)-1H-benzimidazole (Maribavir), pharmaceutical compositions thereof and their use in medical therapy.Type: GrantFiled: October 27, 2011Date of Patent: September 24, 2013Assignee: ViroPharma IncorporatedInventors: Eugene C. Amparo, Cristina Stoica, Mihaela Pop, Jaroslaw Mazurek
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Patent number: 8536150Abstract: The present invention provides a method of myocardial perfusion imaging using reduced doses of (1-{9-[(4S,2R,3R,5R)3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide.Type: GrantFiled: June 15, 2012Date of Patent: September 17, 2013Assignee: Gilead Sciences, Inc.Inventors: Luiz Belardinelli, Brent K. Blackburn, Zhenhai Gao
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Publication number: 20130237491Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: April 12, 2013Publication date: September 12, 2013Applicant: Roche Palo Alto LLCInventors: Rene Robert Devos, Christopher John Hobbs, Wen-Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
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Publication number: 20130230542Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicants: CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER, UNIVERSITY OF CINCINNATIInventors: Edward J. Merino, James C. Mulloy, Guorui Li, Tiffany Bell-Horwath
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Patent number: 8524248Abstract: The present invention provides isolated or substantially purified polypeptides, nucleic acids, and virus-like particles (VLPs) derived from a Merkel cell carcinoma virus (MCV), which is a newly-discovered virus. The invention further provides monoclonal antibody molecules that bind to MCV polypeptides. The invention further provides diagnostic, prophylactic, and therapeutic methods relating to the identification, prevention, and treatment of MCV-related diseases.Type: GrantFiled: December 15, 2008Date of Patent: September 3, 2013Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Patrick S. Moore, Yuan Chang, Huichen Feng, Christopher Brian Buck, Diana V. Pastrana
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Publication number: 20130224239Abstract: The present invention relates to an alcoholic extract of fungi of the genus Cunninghamella; a method for its preparation and use thereof.Type: ApplicationFiled: February 16, 2012Publication date: August 29, 2013Applicant: KING SAUD UNIVERSITYInventors: Amani S. Awaad, Gamal A. Soliman, Nabila A. Aljaber, Tahani A. Al-Hamad
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Publication number: 20130224170Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.Type: ApplicationFiled: March 26, 2013Publication date: August 29, 2013Applicant: The University of Kentucky Research FoundationInventor: The University of Kentucky Research Foundation
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Publication number: 20130217643Abstract: Provided herein are compounds of Formula I, compositions comprising an effective amount of a compound of Formula I, and methods for reducing intraocular pressure comprising administering an effective amount of compounds of Formula I to a subject in need thereof.Type: ApplicationFiled: April 3, 2013Publication date: August 22, 2013Applicant: INOTEK PHARMACEUTICALS CORPORATIONInventor: INOTEK PHARMACEUTICALS CORPORATION
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Patent number: 8513205Abstract: The present invention relates to compounds, in particular, dual antagonists comprising a nucleoside reverse transcriptase inhibitor (NRTI) or a nucleoside competitive reverse transcriptase inhibitor and a non-nucleoside reverse transcriptase inhibitor (NNRTI), linked together using a chemical linker, which may be used to inhibit HIV (HIV-1) reverse transcriptase and in the treatment of HIV infections, more severe cases of HIV infections, including ARC and AIDS, including reducing the likelihood of these infections and disease states.Type: GrantFiled: April 9, 2009Date of Patent: August 20, 2013Assignees: Yale University, University of Cape TownInventors: Karen S. Anderson, Roger Hunter
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Patent number: 8512690Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: April 7, 2010Date of Patent: August 20, 2013Assignee: Novartis AGInventors: Trixi Brandl, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
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Patent number: 8513214Abstract: The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4?-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.Type: GrantFiled: November 10, 2008Date of Patent: August 20, 2013Assignee: The United States of America as Represented by the Secretary of the Dept. of Health and Human ServicesInventors: Bao-Han C. Vu, Maqbool A. Siddiqui, Victor E. Marquez, Stephen H. Hughes, Paul L. Boyer
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Patent number: 8507459Abstract: The present invention relates to the novel use of an adenosine aspartate product for the formulation of a drug intended to prevent the development of preneoplastic lesions and to reverse some types of cancer, particularly liver cancer, providing chemoprotection, preventing myelotoxic effects.Type: GrantFiled: August 21, 2008Date of Patent: August 13, 2013Assignee: Universidad Nacional Autonnoma de MexicoInventors: Victoria-Eugenia Chagoya-Hazas, Rolando-Efraín Hernandez Muñoz, Saúl Villa-Treviño
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Patent number: 8507710Abstract: The invention relates to pharmaceutical compositions comprising alkylphosphocholines and antimetabolite antitumor substances. The pharmaceutical compositions of the invention are useful for the treatment of benign and malignant oncoses in humans and animals. Preferred alkylphosphocholines are described by the Formula II. One such preferred alkylphosphocholine is perifosine.Type: GrantFiled: March 31, 2010Date of Patent: August 13, 2013Assignee: AEterna Zentaris GmbHInventors: Jurgen Engel, Eckhard Gunther, Herbert Sindermann
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Patent number: 8501708Abstract: Provided herein are a class of purine nucleoside compounds, particularly substituted adenosine compounds, such as benzyloxy cyclopentyladenosine (BCPA) compounds, as well as methods of using these compounds as selective A1 adenosine receptor agonists, particularly for reducing and/or controlling elevated or abnormally fluctuating intraocular pressure (IOP) in the treatment of glaucoma or ocular hypertension (OHT).Type: GrantFiled: March 25, 2011Date of Patent: August 6, 2013Assignee: Inotek Pharmaceuticals CorporationInventor: Prakash Jagtap
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Publication number: 20130190264Abstract: The invention provides a method of reducing injury to cells, tissues or organs of a body following trauma by administering a composition to the body following trauma, including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) a local anaesthetic. Also provided is a composition for reducing injury to cells, tissues or organs of a body following trauma including: (i) and (ii). The composition may be hypertonic.Type: ApplicationFiled: January 24, 2013Publication date: July 25, 2013Applicant: Hibernation Therapeutics LimitedInventor: Geoffrey Phillip Dobson
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Patent number: 8491927Abstract: A pharmaceutical composition for induction therapy which has a hypomethylating agent and a histone deacetylase inhibitor (“HDAC inhibitor”); wherein the hypomethylating agent is a DNA and histone methylation inhibitor such as cladribine and the HDAC inhibitor is, for example, entinostat, panobinostat, vorinostat, and/or romedepsin; further wherein the hypomethylating agent and the HDAC inhibitor are combined in formulations for various administrations including e.g., a continuous delivery system such as a transdermal patch of at least one reservoir or a plurality of reservoirs, oral, a fixed-dose oral combination, intravenous, and combinations thereof. This pharmaceutical composition for induction therapy is used with a monoclonal antibody in the treatment of various cancers, sarcomas, and other malignancies.Type: GrantFiled: April 29, 2010Date of Patent: July 23, 2013Assignee: Nimble Epitech, LLCInventors: Elliot M. Epner, Luke M. Vaughan
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Publication number: 20130184231Abstract: The present invention relates to a method for arresting, protecting and/or preserving an organ which includes administering effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) local anaesthetic to a subject in need thereof. The present invention also relates to a method for arresting, protecting and/or preserving an organ which comprises adding a composition which includes effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) a local anaesthetic to the organ. The present invention further provides a pharmaceutical or veterinary composition which includes effective amounts of (i) a potassium channel opener or agonist and/or an adenosine receptor agonist and (ii) a local anaesthetic.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: Hibernation Therapeutics LimitedInventor: Hibernation Therapeutics Limited
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Publication number: 20130172285Abstract: The disclosure provides linked purine pterin compounds and analogues thereof that are novel HPPK inhibitors. The HPPK inhibitors described herein are compounds and the pharmaceutically acceptable salts thereof of general Formula I The variables, e.g. A1 to A3, R1 to R4, L1, L2, B1, and B2 are described herein. Compounds and salts of Formula I bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing an HPPK inhibitor of Formula I and methods of treating a bacterial infection in a patient by providing one or more HPPK inhibitors of Formula I to the patient are also provided. Processes and intermediates useful for preparing compounds of Formula I are also provided. Methods of using the disclosed compounds to guide the development of additional novel anti-bacterial agents are also provided.Type: ApplicationFiled: June 1, 2011Publication date: July 4, 2013Inventors: Genbin Shi, Gary X. Shaw, Xinhua Ji
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Patent number: 8476247Abstract: Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).Type: GrantFiled: March 25, 2011Date of Patent: July 2, 2013Assignee: Inotek Pharmaceuticals CorporationInventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley, Prakash Jagtap
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Publication number: 20130165399Abstract: The present invention has an object to provide an effective and safe therapeutic agent for inflammatory diseases such as sepsis, hepatitis, and inflammatory bowel disease, and solves the above object by providing a therapeutic agent for inflammatory diseases containing adenosine N1-oxide or a derivative thereof as an effective ingredient.Type: ApplicationFiled: June 16, 2011Publication date: June 27, 2013Applicant: HAYASHIBARA CO., LTD.Inventors: Keizo Kohno, Emiko Ohashi, Hajime Kusano, Shigeharu Fukuda, Tatsuya Ishihara
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Patent number: 8470801Abstract: A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging as well as pharmaceutical compositions comprising at least one A2a receptor agonist, at least one liquid carrier, and at least one co-solvent.Type: GrantFiled: January 30, 2012Date of Patent: June 25, 2013Assignee: Gilead Sciences, Inc.Inventors: Luiz Belardinelli, Mitchell Rosner
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Patent number: 8470800Abstract: Provided herein are compounds, compositions, and methods for reducing intraocular pressure. Also provided herein are compounds, compositions and methods for the treatment of glaucoma or ocular hypertension.Type: GrantFiled: April 30, 2010Date of Patent: June 25, 2013Assignee: Inotek Pharmaceuticals CorporationInventors: Shikha Barman, Rudolf A. Baumgartner
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Publication number: 20130157971Abstract: 2?-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy; R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 2, 2012Publication date: June 20, 2013Inventors: RAYMOND F. SCHINAZI, Dennis C. Liotta, Chung K. Chu, J. Jeffrey McAtee
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Publication number: 20130156872Abstract: The present invention is an ingestable blended formulation which will cause a series of distinct biochemical changes in-vivo; initiate desirable psychological consequences in that person; and induce an observable increase in cognitive functions for that living human subject. In particular, the initiated psychological events will generate a positive change in one's personal perceptions, evoke optimism as the subjective state of mind, and elicit a more sociable attitude and favorable mood as the observable behavior of the affected human person. Moreover, in addition to the initiation of a more positive state of mind, another major result and effect of ingesting the blended formulation is an observable amplification of human brain functions and a substantive increase of human concentration, focus and memory.Type: ApplicationFiled: November 30, 2012Publication date: June 20, 2013Applicant: INVIVO BEVERAGES LLCInventor: InVivo Beverages LLC
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Publication number: 20130149283Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: December 28, 2012Publication date: June 13, 2013Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.Inventors: IDENIX PHARMACEUTICALS, INC., UNIVERSITA DEGLI STUDI DI CAGLIARI
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Publication number: 20130149350Abstract: Compositions and methods to improve the pharmacokinetic profile of S-Adenosylmethionine (SAMe) are provided, as are methods of treating various disorders using SAMe formulations with improved pharmacokinetic profiles. More specifically, the invention is directed to methods of treating a disease or disorder in a subject and/or improving the nutritional status of a subject by administering formulations exhibiting improved pharmacokinetic profiles of exogenous SAMe. The method also includes the step of orally administering compositions of the invention to the subject once per day after overnight fast; that is prior to food intake in the morning.Type: ApplicationFiled: December 5, 2012Publication date: June 13, 2013Applicant: Methylation Sciences International SRLInventor: Methylation Sciences International SRL
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Patent number: 8461128Abstract: Many pathogens, including Mycobacterium tuberculosis and Yersinia pestis, rely on an iron acquisition system based on siderophores, secreted iron-chelating compounds with extremely high Fe(III) affinity. The compounds of the invention are inhibitors of domain salicylation enzymes, which catalyze the salicylation of an aroyl carrier protein (ArCP) domain to form a salicyl-ArCP domain thioester intermediate via a two-step reaction. The compounds include the intermediate mimic 5?-O—[N-(salicyl)sulfamoyl]-adenosine (salicyl-AMS) and analogs thereof. These compounds are inhibitors of the salicylate activity of MbtA, YbtE, PchD, and other domain salicylation enzymes involved in the biosynthesis of siderophores. Therefore, these compounds may be used in the treatment of infection caused by microorganisms which rely on siderphore-based iron acquisition systems.Type: GrantFiled: April 14, 2006Date of Patent: June 11, 2013Assignees: Sloan-Kettering Institute for Cancer Research, Cornell Research Foundation, Inc.Inventors: Derek Shieh Tan, Luis E. N. Quadri, Jae-Sang Ryu, Justin Scott Cisar, Julian Alberto Ferreras, Xuequan Lu
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Patent number: 8461124Abstract: Conformationally locked 2?,4?-carbocylic nucleosides with improved thermal and nuclease stability are disclosed. Oligonucleotides incorporating the locked nucleosides, and methods of treating disease states, are also disclosed.Type: GrantFiled: March 11, 2008Date of Patent: June 11, 2013Inventor: Jyoti Chattopadhyaya
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Publication number: 20130142847Abstract: Provided herein are compositions and methods to enhance the absorption of S-adenosylmethionine (SAMe) and methods of treating various disorders or diseases using non-parenteral SAMe formulations with enhanced-absorption and improved bioavailability. In certain embodiments, the enhanced bioavailability formulations provided herein may be used to treat a variety of diseases or disorders, such as for example, psychiatric disorders including, generalized anxiety disorder, obsessive compulsive disorder, post traumatic stress disorder, panic disorder, depressive disorders (e.g. major clinical depression) and dysthymia; as well as treating liver disorders, cancer, autoimmune disorders, inflammatory disorders, joint disorders, gastrointestinal disorders and cardiovascular disease.Type: ApplicationFiled: July 27, 2011Publication date: June 6, 2013Applicant: Methylation Sciences, Inc.Inventors: I. David MacDonald, Nancy Harrison, Aniko Takacs-Cox, Admir Purac, Almira Blazek-Welsh
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Publication number: 20130143833Abstract: The present invention relates to a method of reducing injury to cells, a tissue or organ to be explanted from a body and upon implantation into a body by administering a composition to the cell, tissue or organ, including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) an antiarrhythmic agent. The invention also provides a composition for reducing injury to vasculature ex vivo including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) an antiarrhythmic agent.Type: ApplicationFiled: November 13, 2012Publication date: June 6, 2013Applicant: Hibernation Therapeutics LimitedInventor: Hibernation Therapeutics Limited
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Patent number: 8455457Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a non-selective beta-adrenergic receptor blocker and an adenosine A1 receptor agonist. Also provided herein is a method of reducing intraocular pressure (IOP) in a subject using such a combination or kit. In a particular embodiment, provided herein is a combination of timolol marketed under the brand Timoptic™ and Compound A.Type: GrantFiled: March 18, 2011Date of Patent: June 4, 2013Assignee: Inotek Pharmaceuticals CorporationInventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
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Publication number: 20130136693Abstract: The present invention provides novel crystalline polymorphic forms of 2-cyclohexylmethylidenehydrazino adenosine, also known as binodenoson, methods of making the same, and methods for the manufacture of a pharmaceutical composition by employing such crystal forms, in particular, for the use of binodenoson in a subject, in need thereof, as a pharmacological stress agent to produce coronary vasodilation.Type: ApplicationFiled: July 11, 2012Publication date: May 30, 2013Applicant: King Pharmaceuticals Research and Development, IncInventors: Allan R. Moorman, Michael H. O'Neal
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Publication number: 20130131006Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.Type: ApplicationFiled: April 28, 2011Publication date: May 23, 2013Applicant: Gachon University of Industry-Academic Cooperation FoundationInventors: Bong Hee Lee, Kyung Hee Byun
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Publication number: 20130131005Abstract: The invention provides a method of reducing infarct size and/or limiting, decreasing and/or inhibiting reperfusion injury and/or ameliorating heart failure in a patient comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to the patient. The compound capable of inhibiting AC5 is particularly effective when administered during or after reperfusion in patients suffering from an ischemic injury.Type: ApplicationFiled: November 5, 2012Publication date: May 23, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventor: University of Medicine and Dentistry of New Jersey
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Publication number: 20130129792Abstract: Compositions and methods to improve the pharmacokinetic profile of S-Adenosylmethionine (SAMe) are provided, as are methods of treating various disorders using SAMe formulations with improved pharmacokinetic profiles. More specifically, the invention is directed to methods of treating a disease or disorder in a subject and/or improving the nutritional status of a subject by administering formulations exhibiting improved pharmacokinetic profiles of exogenous SAMe. The method also includes the step of orally administering compositions of the invention to the subject once per day after overnight fast; that is prior to food intake in the morning.Type: ApplicationFiled: December 13, 2012Publication date: May 23, 2013Applicant: METHYLATION SCIENCES INTERNATIONAL SRLInventor: METHYLATION SCIENCES INTERNATIONAL SRL
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Publication number: 20130121986Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.Type: ApplicationFiled: December 26, 2012Publication date: May 16, 2013Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY