Adenosine Or Derivative Patents (Class 514/46)
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Publication number: 20100279964Abstract: The present invention relates to methods of using 3?,4?-aromatic acyloxy substituted 7,8-pyranocoumarins compounds in reversing P-glycoprotein overexpression mediated multidrug resistance in cancer cells including uses in treating cancers.Type: ApplicationFiled: July 16, 2010Publication date: November 4, 2010Inventors: Wangfun Fong, Xiaoling Shen, Guangying Chen, Guoyuan Zhu, Chikeung Wan, Kaiwing Tse
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Publication number: 20100279971Abstract: This invention relates to compounds of the formula X) or XI) (X) (XI) wherein: each —R1, —R2 and —R3 is independently -Q1, —OH or —H, where at least one of —R1, —R2 and —R3 is not —H or —OH; each —R4 and —R5 is independently -Q2 or —H; each -Q1 is independently selected from: —F, —Cl, —RA, —ORA, —SH, —SRA, where each —RA is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; and each -Q2 is selected from: —F, —Cl, —RB, —ORB, —SH, —SRB, where each —RB is independently selected from methyl and ethyl, which may substituted by one or more fluoro or chloro groups; which are useful in the treatment of melanoma.Type: ApplicationFiled: December 18, 2008Publication date: November 4, 2010Inventors: Jose Neptuno Rodriguez-Lopez, Luis Sanchez Del Campo Ferrer, Juan Cabezas-Herrera, Alberto Tarraga Tomas, Magali Maria Saez Ayala
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Patent number: 7825096Abstract: Disclosed are prodrugs of inactivators of O6-alkylguanine-DNA alkyltransferase (AGT). The prodrugs are cleavable by the ?-glucuronidase enzyme, which is either administered to the patient or produced by necrotic tumor cells. The prodrugs are represented by the formula A-B-C, wherein A is a glucuronosyl residue linked through its 1-oxygen to the phenyl ring of B; B is a benzyloxycarbonyl group, optionally ring-substituted with one or more electron withdrawing groups; and C is an inactivator of AGT, e.g., a substituted or unsubstituted O6-benzylguanine or O6-benzyl-2?-deoxyguanosine. Also disclosed are additional inactivators of AGT, pharmaceutical compositions comprising an inactivator or prodrug and a pharmaceutically acceptable carrier, and a method of use of the inactivator or prodrug in enhancing the chemotherapeutic treatment of tumor cells in a mammal, e.g., a human, with an antineoplastic alkylating agent that causes cytotoxic lesions at the O6-position of guanine.Type: GrantFiled: March 7, 2007Date of Patent: November 2, 2010Assignees: The United States of America as represented by the Department of Health and Human Services, The Penn State Research FoundationInventors: Robert C. Moschel, Matthew Karl Moschel, legal representative, Natalia A. Loktionova, Anthony E. Pegg, Gary T. Pauly
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Patent number: 7825102Abstract: The present invention provides a method for treating dry eye condition in an individual comprising administrating to said individual an amount of A3 adenosine receptor (A3AR) agonist, the amount being effective to ameliorate symptoms of dry eye in the individual. In accordance with one embodiment, the dry eye condition is manifested by one or more ophthalmologic clinical symptoms selected from foreign body sensation, burning, itching, irritation, redness, eye pain, blurred vision, degraded vision and excessive tearing. A preferred A3RAg in accordance with the invention is N6-(3-iodobenzyl)-adenosine-5?-N-methyluronamide (IB-MECA).Type: GrantFiled: November 28, 2006Date of Patent: November 2, 2010Assignee: Can-Fite Biopharma Ltd.Inventors: Pnina Fishman, Tatiana Reitblat, Ilan Cohn
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Publication number: 20100272645Abstract: A myocardial imaging method that is accomplished by administering one or more adenosine A2A adenosine receptor agonist to a human undergoing myocardial imaging.Type: ApplicationFiled: January 27, 2010Publication date: October 28, 2010Inventor: Luiz Belardinelli
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Publication number: 20100272711Abstract: The present invention is directed to a pharmaceutical composition, and methods of use thereof, comprising at least one agent which target multiple adenosine receptors (AR) simultaneously in a stoichiometric relationship (i.e. each AR receptor is targeted to an equal extent). Aspects of the present invention relate to pharmaceutical compositions, and uses thereof, comprising at least one agent which co-activates an A1-adenosine receptor (A1-AR) and an A2A-adenosine receptor (A2A-AR) or a combination of at least one agent which activates an A1-AR and at least one agent which activates an A2A-AR, where both the A1-AR and A2A-AR are activated in a stoichiometric relationship such that the level of biological activation of A1-AR is approximately the same level of biological activation of A2A-AR.Type: ApplicationFiled: December 12, 2008Publication date: October 28, 2010Applicant: THOMAS JEFFERSON UNIVERSITYInventors: Arthur Feldman, Tung Chan
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Patent number: 7820811Abstract: The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2?-methoxy adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine receptor agonists, and to their use as therapeutic compounds, in particular as analgesic or anti-inflammatory compounds, or as disease modifying antirheumatic drugs (DMARDs), and to methods of preventing, treating or ameliorating pain or inflammation using these compounds.Type: GrantFiled: June 26, 2007Date of Patent: October 26, 2010Assignee: CBT Development LimitedInventor: Edward D. Savory
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Publication number: 20100261668Abstract: Novel mechanism-based inhibitors of S-adenosyl-L-methionine decarboxylase are provided. These compounds of formula (1) inhibit the life cycle of trypanosomes, and are useful to treat subjects infected with African trypanosomes. The invention includes pharmaceutical compositions and methods of using the compounds of formula (1).Type: ApplicationFiled: June 13, 2008Publication date: October 14, 2010Inventors: Yibin Xiang, Bradford Hirth, Cassandra Celatka
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Publication number: 20100260755Abstract: The invention contemplates methods and compositions for treating multiple sclerosis including the administration of a PDE inhibitor and at least one immunomodulator comprising mitoxantrone, natalizumab, fingolimod, laquinimod, cladribine, dimethylfumarate or a mixture comprising synthetic polypeptide analogs of myelin basic protein, including alanine, glutamic acid, lysine, and tyrosine amino acid residues, in a therapeutically effective amount. A preferred PDE inhibitor includes ibudilast.Type: ApplicationFiled: April 7, 2010Publication date: October 14, 2010Inventors: Richard E. GAMMANS, Kenneth W. Locke, Michael E. Kalafer
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Publication number: 20100260709Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: ApplicationFiled: April 7, 2010Publication date: October 14, 2010Inventors: Trixi BRANDL, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Oliver Simic
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Publication number: 20100260716Abstract: Therapeutic methods, therapeutic combinations and pharmaceutical compositions provided herein are useful for inhibiting demyelination, for delaying the clinical onset of a demylination condition, for inhibiting progression and/or reducing frequency of relapse of a demylination condition, and/or enhancing physical ability of a human subject having a demylination condition. Lacosamide is one of the active compounds.Type: ApplicationFiled: October 23, 2008Publication date: October 14, 2010Applicant: UCB PHARMA GMBHInventors: Thomas Stöhr, David Rudd
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Patent number: 7812000Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5? end.Type: GrantFiled: October 3, 2007Date of Patent: October 12, 2010Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla, Dong Yu, Lakshmi Bhagat
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Publication number: 20100256083Abstract: This application describes compositions, methods of treatment, and methods of manufacturing a medicament for reducing injury or damage to cells, tissues or organs during ischemia, reperfusion, or following ischemia or trauma. The methods for reducing damage to a cell, tissue or organ comprise administering an effective amount of a composition including (i) a potassium channel opener or agonist and/or adenosine receptor agonist; and (ii) an antiarrhythmic agent. The methods may further include postconditioning the cell, tissue or organ.Type: ApplicationFiled: July 25, 2008Publication date: October 7, 2010Applicant: HIBERNATION THERAPEUTICS LIMITEDInventor: Geoffrey P. Dobson
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Publication number: 20100254942Abstract: The present invention relates to novel compositions having anti-viral activity and in particular it relates to synergistic compositions active against Hepatitis C virus (HCV). The invention also relates to methods for retarding, reducing or otherwise inhibiting HCV growth and/or functional activity.Type: ApplicationFiled: August 4, 2008Publication date: October 7, 2010Applicant: BIOTRON LIMITEDInventors: Gary Dinneen Ewart, Carolyn Anne Luscombe, Michelle Miller
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Publication number: 20100256084Abstract: Inflammatory state in a subject is assayed by determining the level of expression of A3 adenosine receptor (A3AR) in white blood cells (WBC), e.g. circulating WBCs, from the subject. A high level of expression of A3AR is indicative of an inflammatory state in the subject. This assay can be used for determining the severity of inflammation in a subject and monitoring the efficacy of anti-inflammatory treatment. Also, the level of expression may be used for selecting patients to receive an anti-inflammatory treatment that comprises an A3AR agonist.Type: ApplicationFiled: June 21, 2010Publication date: October 7, 2010Applicant: CAN-FITE BIOPHARMA LTD.Inventors: Pnina Fishman, Sara Bar-Yehuda, Lea Madi
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Publication number: 20100249053Abstract: The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.Type: ApplicationFiled: October 22, 2008Publication date: September 30, 2010Applicant: Can-Fite Biopharma Ltd.Inventors: Pnina Fishman, Shira Cohen
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Publication number: 20100247433Abstract: The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handle” to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.Type: ApplicationFiled: October 16, 2006Publication date: September 30, 2010Applicant: California Institute of TechnologyInventors: David Tirrell, Daniela C. Dieterich, Aaron J. Link, Erin Schuman
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Publication number: 20100239668Abstract: Described is a layered or segmented controlled release pharmaceutical tablet adapted for separating one segment from another by breaking through a segment.Type: ApplicationFiled: June 19, 2007Publication date: September 23, 2010Inventors: Allan S. Kaplan, Lawrence Solomon
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Patent number: 7795236Abstract: The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.Type: GrantFiled: March 13, 2007Date of Patent: September 14, 2010Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Yoshinori Nonaka, Norihiko Kikuchi
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Publication number: 20100226980Abstract: A subject of the invention is a tablet for pharmaceutical use, particularly for veterinary use, particularly suitable for the chronic treatment of hepatic insufficiency, comprising at least one S-Adenosyl-Methionine salt. Said tablet has the advantage of being divisible and being capable of including an appetizing agent.Type: ApplicationFiled: January 8, 2010Publication date: September 9, 2010Applicant: VETOQUINOLInventor: Marinette MOREAU
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Patent number: 7792576Abstract: Injuries to the central nervous system, particularly spinal cord injuries, are treated by administering a purine nucleoside or analog to the patient and, optionally, electrically stimulating the site of injury.Type: GrantFiled: February 20, 2007Date of Patent: September 7, 2010Assignee: Purdue Research FoundationInventors: Richard B. Borgens, Scott A. Shapiro
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Patent number: 7790698Abstract: Compounds of the class of adenosines, represented by structural formula I, wherein R is C1-4 alkoxy, and X is H or OH, are useful in a method of preventing, treating, or ameliorating various conditions or disorders, e.g., inflammation, which comprises administering a compound of formula I to a subject in need of such prevention, treatment, or amelioration, for example, at a dosage which gives rise to a peak plasma concentration in the subject that is less than the EC50 value of the compound at adenosine receptors at nH 7.4.Type: GrantFiled: March 5, 2004Date of Patent: September 7, 2010Assignee: Cambridge Biotechnology LtdInventor: Peter Richardson
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Publication number: 20100222275Abstract: Provided are a pharmaceutical product capable of treating vitiligo by thickening the epidermis at a vitiligo-affected site, which has been thinned, to thereby accelerate pigmentation, and a method of accelerating pigmentation by thickening the epidermis. Vitiligo can be treated by using a compound having an epidermis thickening action, for example, a therapeutic agent for a skin ulcer which is used in the treatment of burn ulcer, crural ulcer, diabetic ulcer or post-operative ulcer, or a therapeutic agent for bedsore.Type: ApplicationFiled: October 17, 2008Publication date: September 2, 2010Inventors: Kunihiko Tamaki, Kanako Kikuchi, Mayumi Komine, Seiki Fujimoto
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Publication number: 20100222292Abstract: The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune diseases.Type: ApplicationFiled: May 7, 2010Publication date: September 2, 2010Inventor: Steven Baranowitz
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Publication number: 20100221351Abstract: In accordance with certain embodiments of the present disclosure, A method for intracellular delivery of cytotoxin in combination with cyoablation is provided. The method includes encapsulation of one or more cytotoxins in a thermally responsive nanocapsule by decreasing the temperature of the nanocapsule to increase the permeability of the nanocapsule whereby the one or more cytotoxins are sucked into or diffuse into the nanocapsule. The temperature of the nanocapsule is increased and the nanocapsule is delivered into a cell. Cryoablation is performed in proximity to the cell resulting in the release of the one or more cytotoxins from the nanocapsule into the cell.Type: ApplicationFiled: March 1, 2010Publication date: September 2, 2010Applicant: UNIVERSITY OF SOUTH CAROLINAInventor: Xiaoming He
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Publication number: 20100222257Abstract: Disclosed herein are substituted phenethylamine alpha adrenergic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: May 17, 2010Publication date: September 2, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100210579Abstract: Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.Type: ApplicationFiled: March 15, 2010Publication date: August 19, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Publication number: 20100203017Abstract: The present invention is related to the use of Cladribine for the preparation of a pharmaceutical formulation for the treatment of multiple sclerosis, especially relapsing-remitting multiple sclerosis or early secondary progressive multiple sclerosis, wherein the preparation is to be the orally administered and wherein re-treatments are possible.Type: ApplicationFiled: April 23, 2010Publication date: August 12, 2010Applicant: Merck Serono S.A.Inventors: Giampiero De Luca, Arnaud Ythier, Alain Munafo, Maria Lopez-Bresnahan
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Publication number: 20100203110Abstract: The present invention relates to methods of treating a cancerous tumor in a subject comprising administering to the subject an effective amount of 3-bromopyruvate. The 3-bromopyruvate may be administered intraarterially directly to a tumor as a continuous intraarterial infusion. The present invention also relates to methods for identifying agents that inhibit type II hexokinase activity.Type: ApplicationFiled: December 17, 2007Publication date: August 12, 2010Applicant: The Johns Hopkins UniversityInventors: Jean-Francois Geschwind, Mustafa Vali
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Patent number: 7772198Abstract: The invention concerns pharmaceutical formulas designed for the treatment of diseases related to CFTR channel dysfunction, such as cystic fibrosis, asthma or diarrhoea. These formulas contain a molecule, coming in the form of a zwitterion at physiological pH, with the general formula: where X?N or P; and Y?O or S.Type: GrantFiled: April 21, 2006Date of Patent: August 10, 2010Assignees: Centre National de la Recherche Scientifique, Universite Joseph Fourier, Universite de PoitiersInventors: Jean-Luc Decout, Christel Routaboul, Frederic Becq, Caroline Norez
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Patent number: 7772206Abstract: This invention relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof and an additional therapeutic agent to a patient in need of such treatment.Type: GrantFiled: February 27, 2009Date of Patent: August 10, 2010Assignee: Genzyme CorporationInventors: Christopher B. Wood, Stuart W. Smith
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Publication number: 20100196517Abstract: This invention generally relates to improvement of the body and skin appearance, for example enhancing the appearance of sagging, wrinkled, or cellulite-afflicted areas of the skin and body, through the local delivery of a nitric oxide donor, for example, using delivery vehicles such as lotions, creams, liquids, and/or transdermal patches. In some embodiments, a delivery vehicle containing a nitric oxide donor, for example, L-arginine (an important biological precursor) or its derivatives in a sufficient concentration to improve the appearance of a selected area of the body may be applied. In certain cases, one or more agents may also be included that aid in the transfer of the nitric oxide donor into the tissue, which may overcome the resistance to transfer into the skin. Non-limiting examples of suitable agents include agents able to create hostile biophysical environments, for instance, choline chloride, magnesium chloride, and/or sodium chloride.Type: ApplicationFiled: April 15, 2010Publication date: August 5, 2010Applicant: Strategic Science & Technologies, LLCInventor: Eric Thor Fossel
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Publication number: 20100190737Abstract: The invention comprises a composition of inosine and orotic acid or a salt thereof, and its methods of use in treating, maintaining and enhancing the health of the heart, and specifically the integrity of the myocardium. The effective combination of inosine and orotic acid/orotate effectively improves various medical parameters that are widely used to assess cardiac function and structure. These include EKG and VCG recordings, quantitative assessments of work capacity and athletic performance, clinically relevant observations, and direct biochemical, histological and ultrastructural analyses. The observations and controlled studies in mice, rats, rabbits, cardiology patients and high performance human athletes (cyclists) consistently support the effectiveness of the combination of inosine and orotic acid/orotate in both preventing and reversing damage to the myocardium resulting from physical stress.Type: ApplicationFiled: January 26, 2009Publication date: July 29, 2010Applicant: NUTRITIONAL RESEARCH GROUP LLCInventors: Yevsey Belenky, Jeffrey Shapiro
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Publication number: 20100184715Abstract: The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe.Type: ApplicationFiled: October 22, 2007Publication date: July 22, 2010Applicant: GNOSIS SPAInventors: Ermanno Valoti, Daniele Giovannone, Marco Berna
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Publication number: 20100184707Abstract: The use of a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis, for manufacturing a pharmaceutical composition for preventing or inhibiting the undesirable side-effects caused to a human or an animal organism by an active ingredient that induces a high level of extracellular GABA or increases GABA receptor activation.Type: ApplicationFiled: July 4, 2008Publication date: July 22, 2010Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Serge Picaud, Jose Alain Sahel, Jammoul Firas, Caroline Coriat, Manuel Simonutti
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Publication number: 20100183503Abstract: 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: ApplicationFiled: March 29, 2010Publication date: July 22, 2010Inventors: Luiz Belardinelli, Mitchell Rosner
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Patent number: 7759321Abstract: Compounds of the class of adenosines, represented by structural formula I, wherein R is C1-4 alkoxy, and X is H or OH, excluding 2-methoxyadenosine, are useful as analgesics, particularly in a method of preventing, treating, or ameliorating pain which comprises administering a compound of formula I to a subject in need of such prevention, treatment, or amelioration.Type: GrantFiled: March 5, 2004Date of Patent: July 20, 2010Assignee: Cambridge Biotechnology LtdInventors: Peter Richardson, Kevin Lee, Lisa Lione
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Patent number: 7749981Abstract: The present invention provides a drug-eluting stent, wherein the stent is coated with one or more non-nucleotide P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.Type: GrantFiled: November 4, 2005Date of Patent: July 6, 2010Assignee: Inspire Pharmaceuticals, Inc.Inventors: José L. Boyer, James G. Douglass, III, Sammy R. Shaver
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Patent number: 7749975Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5? end.Type: GrantFiled: July 1, 2005Date of Patent: July 6, 2010Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla, Dong Yu, Lakshmi Bhagat
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Patent number: 7749980Abstract: The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and/or pain associated with diseases. The P2X receptor antagonists useful for this invention are non-nucleotide compounds of general Formula I. Compounds of Formula I can be used alone to treat pain. Compounds of Formula I can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the therapeutic effect of pain reduction.Type: GrantFiled: October 21, 2004Date of Patent: July 6, 2010Assignee: Inspire Pharmaceuticals, Inc.Inventors: Robert Plourde, Jr., Sammy R. Shaver, Melwyn Anthony Abreo, Lorenzo Josue Alfaro-Lopez, Yangbo Feng, Tatyana V. Khasanova, Mark W. Holladay, Christopher S. Crean
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Publication number: 20100166727Abstract: The present invention relates to S-adenosylmethionine (SAMe), methylthioadenosine (MTA) for the treatment of disease. More specifically, the invention relates to SAMe and MTA methods and compositions for the chemoprevention and treatment of colon polyps and cancer.Type: ApplicationFiled: April 2, 2008Publication date: July 1, 2010Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventor: Shelly C. Lu
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Publication number: 20100168048Abstract: Provided are a process for producing a S-adenosyl-L-methionine-containing composition which is very excellent in a stability by adding at least ascorbic acids or salts thereof to a composition liquid containing S-adenosyl-L-methionine and then drying the above composition liquid or separating and drying a crystallized deposit obtained from the above composition liquid, a S-adenosyl-L-methionine-containing composition obtained by the above production process and a molding obtained from the above composition.Type: ApplicationFiled: January 16, 2007Publication date: July 1, 2010Inventors: Kentarou Takano, Shinyo Gayama
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Publication number: 20100166698Abstract: The present invention describes combinations of A2A adenosine receptor agonists and anti-inflammatory compounds for the inhibition of an inflammatory response in mammalian tissue.Type: ApplicationFiled: December 3, 2009Publication date: July 1, 2010Inventor: Jayson M. Rieger
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Publication number: 20100168049Abstract: The present invention relates to a composition, especially a cosmetic and/or dermatological composition, containing, in a physiologically acceptable medium, a combination of at least one monosaccharide chosen from mannose, rhamnose and a mixture thereof, and of at least one additional compound chosen from adenosine, an analogue thereof and a mixture thereof.Type: ApplicationFiled: December 30, 2009Publication date: July 1, 2010Applicant: L'OREALInventors: Julien LABOUREAU, Jean-Thierry Simonnet, Pascal Portes
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Patent number: 7745415Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyrimidine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: January 17, 2008Date of Patent: June 29, 2010Assignee: Anadys Pharmaceuticals, Inc.Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden
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Patent number: 7745420Abstract: The invention relates to the use of nucleotide substitutes for increasing the in vivo efficacy of nucleic acid molecules and also for inhibiting inflammation in mammals. More particularly, the present invention relates to the use of 2?6?diaminopurine (DAP) and analogs thereof per se in anti-inflammatory compositions, and also for preparing nucleic acid molecules having an increased in vivo physiological efficiency and a reduced toxicity as compared to conventional oligos. The invention is particularly useful for the preparation of antisense oligonucleotides for treating pulmonary/respiratory diseases such as cystic fibrosis, asthma, chronic bronchitis, chronic obstructive lung disease, eosinophilic bronchitis, allergies, allergic rhinitis, pulmonary fibrosis, adult respiratory distress syndrome, sinusitis, respiratory syncytial virus or other viral respiratory tract infection and cancer.Type: GrantFiled: July 8, 2002Date of Patent: June 29, 2010Assignee: Topigen Pharmaceutique, Inc.Inventors: Paolo Renzi, Mustapha Allam, Zoulfia Allakhverdi
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Publication number: 20100158797Abstract: Myocardial imaging methods that are accomplished by administering doses of a pharmaceutical composition including regadenoson—an adenosine A2A receptor agonist—to a human undergoing myocardial imaging in an amount sufficient to achieve at least a minimal increase in average coronary peak flow velocity.Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Inventors: Toufigh Gordi, Ann Walls Olmsted, Hsiao Dee Lieu, Luiz Belardinelli
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Publication number: 20100160250Abstract: This invention provides a method for inhibiting the release of interleukin-1? in a mammal. This invention also provides a method for preventing or treating pulmonary diseases, ophthalmic diseases, and autoimmune diseases that are associated with inflammation or inflammatory conditions. The invention also provides a method for preventing or treating neurodegenerative diseases, or pain in a mammal. The method comprises administering to a mammal in need thereof a therapeutically effective amount of a mononucleoside compound, which is an antagonist of P2X7 receptor.Type: ApplicationFiled: December 17, 2009Publication date: June 24, 2010Inventors: James G. Douglass, III, Sammy R. Shaver, Tomas Navratil, José L. Boyer, Carl A. Samuelson, Jonathan B. DeCamp
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Patent number: 7741296Abstract: 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: March 27, 2006Date of Patent: June 22, 2010Inventor: Igor E. Bondarev
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Patent number: 7741310Abstract: This invention relates to the novel identification of arginase as an enzymatic activity which can reverse inhibition of neuronal regeneration in the central and peripheral nervous system. Assays to monitor the effects of various agents on arginase expression and thus on neuronal regeneration and repair and to identify agents which will block or promote the inhibitory effects on neuronal outgrowth are provided. This invention also relates to compositions and methods using agents that can reverse the inhibitory effects of myelin on neural regeneration by affecting arginase activity or putrescine and derivative polyamine levels in a neuron.Type: GrantFiled: May 4, 2001Date of Patent: June 22, 2010Assignees: Research Foundation of the City University of New York, Beth Israel Deaconess Medical CenterInventors: Marie T. Filbin, Rajiv R. Ratan