Adenosine Or Derivative Patents (Class 514/46)
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Patent number: 7199110Abstract: 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: December 30, 2003Date of Patent: April 3, 2007Assignees: Purdue Research Foundation, Indiana University Research & Technology Corp.Inventors: Richard B. Borgens, Scott A. Shapiro
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Patent number: 7199127Abstract: Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: wherein X is sulfur or oxygen; R1 is hydrogen, alkyl, benzyl, halobenzyl, or phenylalkyl; R2 is hydrogen, halogen, alkoxy, alkenyl, alkynyl, alkylthio, or thio; R3 and R3? are hydrogen, hydroxyalkyl, alkoxycarbonyl, or alkylaminocarbonyl, whereas R3 and R3? do not have identical substituents simultaneously; and R4 is hydrogen or alkyl. Also disclosed are a pharmaceutical composition comprising a compound of formula (I), an isomer, or its pharmacologically acceptable salt as an active ingredient and a method for preventing or treating various diseases, state, or condition, including asthma, inflammation, cerebral ischemia, heart diseases, and cancer.Type: GrantFiled: October 24, 2003Date of Patent: April 3, 2007Assignees: United States of America, Represented by the Secretary, Department of Health and Human Services, Ewha Womans UniversityInventors: Lak Shin Jeong, Kenneth A. Jacobson, Hyung Ryong Moon, Hea Ok Kim
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Patent number: 7196071Abstract: Methods of providing pain relief by administering a water-soluble derivative of spicamycin. Methods of using pain mediation agents are also provided.Type: GrantFiled: September 20, 2001Date of Patent: March 27, 2007Assignee: The General Hospital CorporationInventor: David Borsook
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Patent number: 7189706Abstract: The present invention concerns novel C2,5?-disubstituted and N6,C2,5?-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.Type: GrantFiled: September 3, 2003Date of Patent: March 13, 2007Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.Inventors: Erica Van Tilburg, Ad Ijzerman
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Patent number: 7183264Abstract: 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart are disclosed.Type: GrantFiled: August 29, 2003Date of Patent: February 27, 2007Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
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Patent number: 7173016Abstract: Compositions and methods are provided for prevention and clinical treatment of various forms of graft-versus-host disease (GVHD) by using inhibitors of adenosine deaminase (ADA). In particular, various formulations and dosing regimens of ADA inhibitors such as pentostatin are provided for the treatment of all forms of GVHD, especially steroid-refractory acute and chronic GVHD.Type: GrantFiled: August 18, 2005Date of Patent: February 6, 2007Assignee: Mayne Pharma (USA) Inc.Inventors: Jorge DiMartino, John Tippett Nelson
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Patent number: 7169765Abstract: The invention relates to compositions comprising acyl derivatives of 2?-deoxyribonucleosides. The invention also relates to methods of treating or preventing radiation, mutagen and sunlight-induced biological damage, and methods for improving wound healing and tissue repair, comprising administering the compositions of the present invention to an animal.Type: GrantFiled: January 31, 2000Date of Patent: January 30, 2007Assignee: Wellstat Therapeutics CorporationInventors: Reid W. Von Borstel, Michael K. Bamat
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Patent number: 7163928Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: February 2, 2004Date of Patent: January 16, 2007Assignee: CV Therapeutics, Inc.Inventors: Gloria Cristalli, Venkata Palle, Jeff Zablocki
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Patent number: 7157441Abstract: 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: GrantFiled: June 20, 2003Date of Patent: January 2, 2007Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi Di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: 7157449Abstract: The present invention relates to the use of an inhibitor of CTP synthetase, such as a glutamine analogue, and a substance capable of suppressing toxic effects thereof in vivo, in the manufacture of a medicament for the treatment of a disease caused by a parasitic protozoa. More specifically, said substance capable of suppressing toxic effects may be a nucleobase, such as a purine base or a nucleoside, while the glutamine analogue advantageously is 6-diazo-5-oxo-L-norleucine (DON). The invention also relates to a pharmaceutical composition as such for the treatment and/or prevention of a disease caused by a parasitic protozoa, wherein the disease is selected from the group consisting of malaria, leishmaniasis and trypanosomiasis, e.g. American trypanosomiasis (Chaga's disease), or African trypanosomiasis (African sleeping sickness).Type: GrantFiled: April 20, 2001Date of Patent: January 2, 2007Inventors: Anders Hofer, Lars Thelander
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Patent number: 7157440Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction.Type: GrantFiled: May 27, 2004Date of Patent: January 2, 2007Assignee: CV Therapeutics, Inc.Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Patent number: 7153840Abstract: This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg/mL and about 50 mg/mL. The pH of the composition may be between about 5.5 and about 7.1.Type: GrantFiled: May 23, 2003Date of Patent: December 26, 2006Assignee: Sicor, Inc.Inventors: Dorla Mirejovsky, Peter Lindsay Macdonald
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Patent number: 7153877Abstract: A method for preventing and or reducing the symptoms of insulin resistance and a related syndrome in persons comprises identifying persons having or at risk for having such symptoms, and administering to them an effective amount of a composition comprising niacin-bound chromium that prevents or reduces the symptoms. Compositions incorporating niacin-bound chromium and additional compounds also are disclosed that are particularly effective in synergistically preventing or reducing these symptoms.Type: GrantFiled: December 9, 2004Date of Patent: December 26, 2006Assignee: Interhealth Nutraceuticals IncorporatedInventors: Debasis Bagchi, Harry G. Preuss, Shil C. Kothari
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Patent number: 7150978Abstract: A translation template comprising an ORF region coding for a protein, a 5? untranslated region comprising a transcription promoter and a translation enhancer and locating on the 5? side of the ORF region, and a 3? end region comprising a poly-A sequence and locating on the 3? side of the ORF region, is expressed in a translation system in the presence of an agent for modifying a C-terminal of a protein, which comprises an acceptor portion having a group capable of binding to a protein through a transpeptidation reaction in a protein translation system and a modifying portion comprising a nonradioactive modifying substance linked to the acceptor portion via a nucleotide linker, to cause protein synthesis and the synthesized protein is purified. Thus, the yield of modified protein in a method of modifying C-terminal of protein is improved and detection of protein interaction based on various intermolecular interaction detection methods is realized at an improved level.Type: GrantFiled: June 6, 2003Date of Patent: December 19, 2006Assignee: Keio UniversityInventors: Hiroshi Yanagawa, Nobuhide Doi, Etsuko Miyamoto, Hideaki Takashima, Rieko Oyama
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Patent number: 7148206Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: GrantFiled: June 20, 2003Date of Patent: December 12, 2006Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi Di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: 7144871Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, myocardial infarction and hyperlipidemia.Type: GrantFiled: February 19, 2003Date of Patent: December 5, 2006Assignee: CV Therapeutics, Inc.Inventors: Prabha Ibrahim, Elfatih Elzein, Kevin Shenk, Robert Jiang, Jeff Zablocki, Xiaofen Li, Christopher Morrison, Thao Perry, Dengming Xiao
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Patent number: 7144872Abstract: This specification discloses 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.Type: GrantFiled: October 18, 2005Date of Patent: December 5, 2006Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata Palle, Luiz Belardinelli
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Patent number: 7141553Abstract: The present invention concerns a method for the treatment of inflammatory arthritis, and in particular rheumatoid arthritis, by administering to the subject specific low dosages of N6-(3-iodobenzyl)-adenosine 5?-N-methyl-uronamide (IB-MECA) and 2-chloro-N6-(3-iodobenzyl)-adenosine-5?-N-methyl-uronamide (CL-IB-MECA).Type: GrantFiled: November 19, 2003Date of Patent: November 28, 2006Assignee: Can-Fite Biopharma Ltd. IsraelInventor: Pnina Fishman
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Patent number: 7132409Abstract: 2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5?-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and protecting optic nerve failure and are highly soluble in water. Owing to these characteristics, the compounds are useful as drugs such as remedies for glaucoma and ocular hypertension.Type: GrantFiled: January 11, 2005Date of Patent: November 7, 2006Assignees: Toa Eiyo Ltd., Yamasa CorporationInventors: Takashi Konno, Kazuhiro Uemoto, Shinya Onuma, Yoshikazu Kato
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Patent number: 7132408Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5?-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5?-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5?-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.Type: GrantFiled: March 30, 2004Date of Patent: November 7, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North CarolinaInventors: José L. Boyer, James G. Douglass, III, Sammy R. Shaver, Krzysztof Bednarski, Benjamin R. Yerxa, Gillian M. Olins
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Patent number: 7119110Abstract: A method for preventing and or reducing the symptoms of insulin resistance and a related syndrome in persons comprises identifying persons having or at risk for having such symptoms, and administering to them an effective amount of a composition comprising niacin-bound chromium that prevents or reduces the symptoms. Compositions incorporating niacin-bound chromium and additional compounds also are disclosed that are particularly effective in synergistically preventing or reducing these symptoms.Type: GrantFiled: October 4, 2002Date of Patent: October 10, 2006Assignee: Interhealth Nutraceuticals IncorporatedInventors: Debasis Bagchi, Harry G. Preuss, Shil C. Kothari
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Patent number: 7115585Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides.Type: GrantFiled: February 27, 2002Date of Patent: October 3, 2006Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, James G. Douglass, III, Sammy Ray Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean
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Patent number: 7112574Abstract: Novel C2,8-disubstituted adenosine derivatives disclosed herein have been found to be potent adenosine receptor agonists, in particular for the A2A receptor. The said compounds have biological activity against conditions such as hypertension, ischemic heart disease, ischemic brain disease, psychosis and wound healing. Further, the invention also discloses a process for the preparation of such compounds and pharmaceutical compositions comprising them.Type: GrantFiled: March 3, 2002Date of Patent: September 26, 2006Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.Inventors: Erica Van Tilburg, Ad Ijzerman
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Patent number: 7107985Abstract: The present invention relates to a combination comprising (a) an adenosine A2a receptor agonist as define herein and (b) an adrenergic ?2 receptor agonist, for simultaneous, sequential or separate administration by the inhaled route in the treatment of an obstructive airways or other inflammatory disease.Type: GrantFiled: September 2, 2005Date of Patent: September 19, 2006Assignee: Pfizer, Inc.Inventor: Michael Yeadon
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Patent number: 7109180Abstract: 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heartType: GrantFiled: March 30, 2004Date of Patent: September 19, 2006Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Patent number: 7105497Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: GrantFiled: June 14, 2005Date of Patent: September 12, 2006Assignee: Hôpital Sainte-JustineInventors: Ernest G. Seidman, Yves Theoret
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Patent number: 7105499Abstract: The present invention provides nucleoside derivatives which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside derivatives alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside derivatives of the present invention.Type: GrantFiled: January 18, 2002Date of Patent: September 12, 2006Assignees: Merck & Co., Inc., Isis Pharmaceuticals, Inc.Inventors: Steven S. Carroll, David B. Olsen, Malcolm MacCoss, Balkrishen Bhat, Phillip Dan Cook, Anne B. Eldrup, Thazha P. Prakash
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Patent number: 7105493Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: GrantFiled: June 20, 2003Date of Patent: September 12, 2006Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: 7101860Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutically effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside polyphosphates and dinucleoside polyphosphates of general Formula I, or salts thereof The present invention also provides compositions comprising mononucleoside polyphosphates and dinucleoside polyphosphates according to Formula Ia and Ib.Type: GrantFiled: August 21, 2001Date of Patent: September 5, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North CarolinaInventors: Jose L. Boyer, Gillian M. Olins, Benjamin R. Yerxa, James G. Douglass
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Patent number: 7094769Abstract: The present invention relates to compounds of the formula: and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such compounds.Type: GrantFiled: October 1, 2003Date of Patent: August 22, 2006Assignee: Pfizer IncInventors: Simon J. Mantell, Peter T. Stephenson
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Patent number: 7091190Abstract: The present invention is related to antiviral compositions comprising long-chain aliphatic compounds in combination with a nucleoside analog or phosphonoformic acid, in a pharmaceutically acceptable carrier. Methods for treating viral infections using such compositions are also disclosed.Type: GrantFiled: July 16, 2002Date of Patent: August 15, 2006Assignee: Avanir PharmaceuticalsInventors: John F. Marcelletti, Laura E. Pope, Mohammed H. Khalil, David H. Katz, Lee R. Katz
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Patent number: 7087587Abstract: The present invention provides a process for the preparation of tablets comprising S-adenosylmethionine and/or a pharmaceutically and/or dietarily acceptable derivative thereof by blending that active component with specified additives, compressing the blend, followed by coating.Type: GrantFiled: October 18, 2002Date of Patent: August 8, 2006Assignee: Gnosis SRLInventor: Giuseppe Cianfarani
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Patent number: 7084127Abstract: The present invention concerns novel C2,5?-disubstituted and N6?,C2,5?-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.Type: GrantFiled: March 3, 2002Date of Patent: August 1, 2006Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.Inventors: Erica Van Tilburg, Ad Ijzerman
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Patent number: 7084128Abstract: The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a purinerginic receptor ligand, which is a mononucleoside polyphosphate or dinucleoside polyphosphate defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with other therapeutic agents or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure.Type: GrantFiled: January 15, 2003Date of Patent: August 1, 2006Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Robert Plourde, Jr., Edward G. Brown, Ward M. Peterson
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Patent number: 7081449Abstract: A purine nucleoside analog includes a pyrido[2,3-d]pyrimidine or a pyrimido[4,5-d]pyrimidine and further has a sugar moiety that is optionally modified at the C2?, C3?, C4? and/or C5? position. Particularly contemplated compounds also include prodrug forms of the purine nucleoside analogs, and both purine nucleoside analogs and the corresponding prodrugs are employed in the reduction of growth of neoplastic cells.Type: GrantFiled: July 3, 2001Date of Patent: July 25, 2006Assignee: Valeant Research & DevelopmentInventors: Zbigniew Pietrzkowski, Guangyi Wang, Johnson Lau, Zhi Hong, Jean-Luc Girardet, Esmir Gunic
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Patent number: 7064112Abstract: Adenosine receptor agonists, particularly an agonist which binds to the A3 adenosine receptor, are used for induction of production or secretion of G-CSF within the body, prevention or treatment of toxic side effects of a drug or prevention or treatment of leukopenia, particularly drug-induced leukopenias; and inhibition of abnormal cell growth and proliferation.Type: GrantFiled: September 8, 2000Date of Patent: June 20, 2006Assignee: Can-Fite Biopharma Ltd.Inventor: Pina Fishman
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Patent number: 7056894Abstract: The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: January 4, 2002Date of Patent: June 6, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauve, Vern L. Schramm
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Patent number: 7053064Abstract: The invention provides methods for treating or suppressing tobacco or nicotine usage or dependence involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal.Type: GrantFiled: November 6, 2003Date of Patent: May 30, 2006Assignee: The McLean Hospital CorporationInventor: Scott Lukas
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Patent number: 7049303Abstract: Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula I or II as herein defined, in admixture with a physiologically acceptable excipient diluent or carrier.Type: GrantFiled: July 30, 2002Date of Patent: May 23, 2006Assignee: Medical Research CouncilInventors: David Loakes, Daniel M. Brown, Kazuo Negishi, Kei Moriyama, Jan Balzarini
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Patent number: 7034011Abstract: It is an object of the present invention to provide a method of stabilizing reduced nicotinamide adenine dinucleotide or reduced nicotinamide adenine dinucleotide phosphate [hereinafter abbreviated as NAD(P)H] and a preparation containing NAD(P)H stabilized by the method. As the method of stabilizing NAD(P)H, a method of adding astaxanthin to NAD(P)H is provided.Type: GrantFiled: December 3, 2003Date of Patent: April 25, 2006Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hideo Kawabe, Hideki Murata, Hiroshi Nagano
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Patent number: 7022681Abstract: Disclosed are A1 adenosine receptor agonists of the formula: wherein: R1 is optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl; R2 is hydrogen, halo, trifluoromethyl, or cyano; R3 is hydrogen, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl, R4 and R5 are independently hydrogen or optionally substituted acyl; X is a covalent bond or lower alkylene optionally substituted by cycloalkyl; X1 is a covalent bond or alkylene; Y is a covalent bond or lower alkylene optionally substituted by hedroxy or cycloalkyl; and Z is —C?C—, —R6C?CR7—, or —CHR6CHR7—, in which R6 and R7 at each occurrence are hydrogen or lower alkyl.Type: GrantFiled: August 15, 2003Date of Patent: April 4, 2006Assignee: CV Therapeutics, Inc.Inventors: Jeff Zablocki, Venkata Palle, Elfatih Elzein, Xiaofen Li
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Patent number: 7022830Abstract: Aspects of the present invention relate to the discovery of a novel hepatitis C virus (HCV) isolate. Embodiments include HCV peptides, nucleic acids encoding said HCV peptides, antibodies directed to said peptides, compositions containing said nucleic acids and peptides, as well as methods of making and using the aforementioned compositions including, but not limited to, diagnostics and medicaments for the treatment and prevention of HCV infection.Type: GrantFiled: November 26, 2002Date of Patent: April 4, 2006Assignee: Tripep ABInventor: Matti Sallberg
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Patent number: 7022680Abstract: The present invention provides compounds having the formula: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contributing moiety; B is hydrogen, or a halogen, amino, or thiol group; C is hydrogen, or a halogen, amino, or thiol group; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: May 30, 2002Date of Patent: April 4, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauvé, Vern L. Schramm
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Patent number: 7018985Abstract: The present invention provides novel compounds of dinucleotide polyphosphates and the method of preventing or treating diseases or conditions associated with platelet aggregation. The method comprises administering systemically to a patient a pharmaceutical comprising a purinergic P2? receptor antagonist, in an amount effective to elevate its extracellular concentration to bind to P2? receptors and inhibit P2? receptor-mediated platelet aggregation. Methods of systemic administration include injection by intravenous, intramuscular, intrasternal and intravitreal routes, infusion, transdermal administration, oral administration, rectal administration and intra-operative instillation.Type: GrantFiled: August 21, 2000Date of Patent: March 28, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North Carolina at Chapel HillInventors: José L. Boyer, Gillian M. Olins, Benjamin R. Yerxa, James G. Douglass, III
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Patent number: 7005425Abstract: Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a beta blocker, calcium channel blocker, or a cardiac glycoside.Type: GrantFiled: April 18, 2003Date of Patent: February 28, 2006Assignee: CV Therapeutics, Inc.Inventors: Luiz Belardinelli, Arvinder Dhalla
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Patent number: 6995148Abstract: The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor agonists and ganglionic blocking agents. To achieve this functionality, the compounds of the present invention, preferably contain a ganglionic blocking motif, is inserted into the adenosine molecule. The ganglionic blocking motif preferably includes an elongated carbon chain that, in a particularly preferred embodiment, contains two terminal amino groups. The ganglionic blocking motif preferably includes a carbon along the elongated carbon chain that is integral to a cyclic ketal that is part of the adenosine molecule. In presently-preferred embodiments, the elongated carbon chain ranges from two to sixteen carbons in length. The compounds of the present invention will be useful for treatment of a variety of conditions including, but not limited to, hypertension, vasodilation, and ischemia.Type: GrantFiled: April 5, 2001Date of Patent: February 7, 2006Assignee: University of PittsburghInventors: Garth S. Jones, Edwin K. Jackson
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Patent number: 6995145Abstract: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing agent such as paclitaxel, and a telomerase inhibitory agent such as AZT. The invention also provides methods for identifying other agents with telomere damage-inducing activity and/or telomerase inhibitory activity (as well as and compositions having such activity), for use in the treatment of cancer.Type: GrantFiled: June 5, 2000Date of Patent: February 7, 2006Inventors: Jessie L.-S. Au, M. Guillaume Wientjes
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Patent number: 6992071Abstract: The invention relates to methods for modulating photodamage via the use of collagen derived molecules which either enhance or inhibit damage caused by ultraviolet light.Type: GrantFiled: April 17, 2003Date of Patent: January 31, 2006Assignee: Board of Regents on Behalf of the University of ArizonaInventors: Georg T. Wondrak, Michael J. Roberts, Moonsun Kim, Myron K. Jacobson, Elaine L. Jacobson
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Patent number: 6987097Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: GrantFiled: November 6, 2003Date of Patent: January 17, 2006Assignee: Hospital Sainte-JustineInventors: Ernest G. Seidman, Yves Théorêt
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Patent number: RE39573Abstract: A method of improving DNA repair and reducing DNA damage and for reducing mutation frequency in skin for the purpose of reducing consequences of exposure to solar or ultraviolet radiation is disclosed. The methods comprise administering to the skin a composition containing deoxyribonucleosides in concentrations sufficient to enhance DNA repair or reduce mutation frequency in a vehicle capable of delivering effective amounts of deoxyribonucleosides to the necessary skin cells.Type: GrantFiled: July 9, 2004Date of Patent: April 17, 2007Assignee: Wellstat Therapeutics CorporationInventors: Reid W. von Borstel, Fedor Romantsev