Halogen, Chalcogen, Or Cyano Bonded Directly To The 2-position Of The Purine Ring System Patents (Class 536/27.63)
  • Patent number: 9018371
    Abstract: Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases.
    Type: Grant
    Filed: March 7, 2007
    Date of Patent: April 28, 2015
    Assignees: FM Therapeutics Co., Ltd., The United States of America, As Represented by the Secretary, Department of Health and Human Services, The Office of Technology Transfer, National Institutes of Health
    Inventors: Lak Shin Jeong, Hea Ok Kim, Kenneth A. Jacobson, Seung Ah Choe
  • Patent number: 8658616
    Abstract: Compounds having the general formula (I): are provided which have enhanced inhibitory potency and are thus useful in methods of prophylaxis or treatment of a viral infection such as hepatitis C virus. The compounds are phosphoramidate derivatives of nucleoside compounds derived from bases such as adenine and guanine. The glycoside moiety of the nucleoside compound can be substituted at the ss-2? position with methyl and the phosphoramidate group can be 1-naphthyl linked by —O— to the P atom. These compounds can be administered as pharmaceutical compositions, and methods for their preparation are also provided.
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: February 25, 2014
    Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and Development
    Inventors: Christopher McGuigan, Plinio Perrone, Johan Neyts
  • Publication number: 20140005138
    Abstract: The present invention relates to the compounds of the formulae (I) and (I-1) and the process for preparing the same, uses of the compounds for the treatment of diseases associated with platelet aggregation and in the manufacture of a medicament for the treatment of diseases associated with platelet aggregation, and relates to a pharmaceutical composition and a pharmaceutical formulation containing the compounds, wherein the definitions of R1, R2, R3 and R2a in the formulae are the same as those in the description.
    Type: Application
    Filed: January 20, 2012
    Publication date: January 2, 2014
    Applicants: BEIJING KBD PHARMACEUTICALS CO., LTD., BEIJING UNIVERSITY OF CHEMICAL TECHNOLOGY
    Inventors: Hongguang Du, Guocheng Liu, Zhongren Ding, Shuming Wang
  • Patent number: 8609339
    Abstract: An embodiment of a method for extracting biological material from an emulsion is described that comprises the steps of a) breaking an emulsion comprising a plurality of aqueous droplets in a continuous phase of an oil using a solvent to produce a combined aqueous-oil mixture, where the solvent disrupts the aqueous droplets which release a plurality of biological elements each immobilized on a substrate into the combined aqueous-oil mixture; b) introducing an inorganic salt to the combined aqueous-oil mixture causing a phase separation of the mixture into a first phase comprising an aqueous solution and the biological elements and a second phase comprising the solvent and the oil; c) extracting the first phase from the second phase; and d) collecting the substrate immobilized biological elements from the first phase.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: December 17, 2013
    Assignee: 454 Life Sciences Corporation
    Inventor: Yue Suo
  • Patent number: 8569260
    Abstract: 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: Grant
    Filed: August 29, 2012
    Date of Patent: October 29, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
  • Patent number: 8470800
    Abstract: 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: Grant
    Filed: April 30, 2010
    Date of Patent: June 25, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Shikha Barman, Rudolf A. Baumgartner
  • Patent number: 8470801
    Abstract: 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: Grant
    Filed: January 30, 2012
    Date of Patent: June 25, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Mitchell Rosner
  • Patent number: 8455457
    Abstract: 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: Grant
    Filed: March 18, 2011
    Date of Patent: June 4, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
  • Patent number: 8440639
    Abstract: Provided herein is a pharmaceutical composition or a kit comprising a combination of a carbonic anhydrase inhibitor analog 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 dorzolamide marketed under the brand Trusopt™ and Compound A.
    Type: Grant
    Filed: March 18, 2011
    Date of Patent: May 14, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley
  • Patent number: 8334364
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: December 18, 2012
    Assignee: Nipon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20120252751
    Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.
    Type: Application
    Filed: May 7, 2012
    Publication date: October 4, 2012
    Inventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
  • Patent number: 8268988
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: April 22, 2011
    Date of Patent: September 18, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein
  • Patent number: 8188222
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: May 29, 2012
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Patent number: 7956179
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.
    Type: Grant
    Filed: January 13, 2010
    Date of Patent: June 7, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein
  • Patent number: 7863253
    Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for treating or preventing an ischemic condition, reperfusion injury, a cellular proliferative disorder, a cardiovascular disease, a neurological disorder, a skin disorder, a radiation-induced injury, a wound, or an inflammatory disease comprising administering an effective amount of a Purine Derivative to a subject in need thereof.
    Type: Grant
    Filed: September 19, 2005
    Date of Patent: January 4, 2011
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Andrew L. Salzman, Csaba Szabo
  • Patent number: 7807653
    Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: October 5, 2010
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
  • Patent number: 7790698
    Abstract: 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: Grant
    Filed: March 5, 2004
    Date of Patent: September 7, 2010
    Assignee: Cambridge Biotechnology Ltd
    Inventor: Peter Richardson
  • Patent number: 7759321
    Abstract: 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: Grant
    Filed: March 5, 2004
    Date of Patent: July 20, 2010
    Assignee: Cambridge Biotechnology Ltd
    Inventors: Peter Richardson, Kevin Lee, Lisa Lione
  • Patent number: 7732595
    Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph. The A2A-adenosine receptor agonist has the following formula: This compound is prepared by reacting the ethyl ester with methylamine in a sealed pressure reactor.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: June 8, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein
  • Patent number: 7732424
    Abstract: The present invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's core body temperature, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, an ophthalmic condition, an ischemic condition, a reperfusion injury, obesity, a wasting disease, or diabetes, comprising administering an effective amount of a Purine Derivative to an animal in need thereof.
    Type: Grant
    Filed: November 30, 2006
    Date of Patent: June 8, 2010
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Andrew L. Salzman
  • Patent number: 7691825
    Abstract: The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, methods for their preparation, and pharmaceutical compositions containing them. The compounds of formula (I) are adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases. Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack. The present invention also provides methods for the induction of pharmacological stress to facilitate coronary imaging of areas of ischemia by employing compounds of formula (I). The compounds of formula (I) may be labeled, e.g., with radioactive isotopes, and therefore are useful in kinetic binding experiments.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: April 6, 2010
    Assignee: King Pharmaceuticals Research and Development, Inc.
    Inventors: Pier Giovanni Baraldi, Pier Andrea Borea, Allan R. Moorman, Delia Preti
  • Patent number: 7671192
    Abstract: Synthesis methods suitable for large scale manufacture of the A2A-adenosine receptor agonist (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide and precursors thereof.
    Type: Grant
    Filed: May 17, 2007
    Date of Patent: March 2, 2010
    Assignee: Gilead Palo Alto, Inc.
    Inventors: Jeff Zablocki, Elfatih Elzein
  • Publication number: 20090286971
    Abstract: The present invention for the stereoselective preparation of 2-deoxy-?-D-adenine nucleosides wherein a blocked 2-deoxy-?-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative.
    Type: Application
    Filed: May 4, 2009
    Publication date: November 19, 2009
    Inventors: William E. Bauta, Brian D. Burke, Brian E. Schulmeier, William R. Cantrell, JR., Dennis P. Lovett, Jose Puente
  • Patent number: 7605143
    Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described herein.
    Type: Grant
    Filed: August 2, 2005
    Date of Patent: October 20, 2009
    Assignee: University of Virginia Patent Foundation
    Inventors: Jayson M. Rieger, Joel M. Linden, Timothy L. Macdonald, Gail W. Sullivan, Lauren J. Murphree, Robert Alan Figler
  • Patent number: 7470784
    Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: December 30, 2008
    Assignee: Southern Research Institute
    Inventors: John A. Montgomery, Anita T. Fowler, John A. Secrist, III
  • Patent number: 7425547
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula IB as follows: and pharmaceutically acceptable prodrugs and salts thereof, where R, R1, R13, R14, W, W2, W3, Y and Z are as defined herein.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: September 16, 2008
    Assignee: Genelabs Technologies, Inc.
    Inventors: Christopher Don Roberts, Natalia B. Dyatkina
  • Patent number: 7342003
    Abstract: Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
    Type: Grant
    Filed: June 16, 2005
    Date of Patent: March 11, 2008
    Assignee: King Pharmaceuticals Research and Development, Inc.
    Inventors: Allan R. Moorman, Michael Scannell, Thiagarajan Balasubramanian, Russell Outcalt, Edward Leung
  • Patent number: 7199127
    Abstract: 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: Grant
    Filed: October 24, 2003
    Date of Patent: April 3, 2007
    Assignees: United States of America, Represented by the Secretary, Department of Health and Human Services, Ewha Womans University
    Inventors: Lak Shin Jeong, Kenneth A. Jacobson, Hyung Ryong Moon, Hea Ok Kim
  • Patent number: 7189706
    Abstract: 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: Grant
    Filed: September 3, 2003
    Date of Patent: March 13, 2007
    Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.
    Inventors: Erica Van Tilburg, Ad Ijzerman
  • Patent number: 7141553
    Abstract: 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: Grant
    Filed: November 19, 2003
    Date of Patent: November 28, 2006
    Assignee: Can-Fite Biopharma Ltd. Israel
    Inventor: Pnina Fishman
  • Patent number: 7112574
    Abstract: 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: Grant
    Filed: March 3, 2002
    Date of Patent: September 26, 2006
    Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.
    Inventors: Erica Van Tilburg, Ad Ijzerman
  • Patent number: 7084127
    Abstract: 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: Grant
    Filed: March 3, 2002
    Date of Patent: August 1, 2006
    Assignees: Universiteit Leiden, Can-Fite Biopharma Ltd.
    Inventors: Erica Van Tilburg, Ad Ijzerman
  • Patent number: 6949640
    Abstract: 2-Chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy-2-fluoro-?-D-arabinofuranosyl)-9H-purin-6-amine. When the purine reactant is substituted in the 6 position with a halogen, a reaction step with an alkoxide is carried out prior to the reaction with ammonia.
    Type: Grant
    Filed: February 16, 2001
    Date of Patent: September 27, 2005
    Assignee: Southern Research Institute
    Inventors: John A. Montgomery, Anita T. Fowler, John A. Secrist, III
  • Patent number: 6946449
    Abstract: 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: Grant
    Filed: July 11, 2002
    Date of Patent: September 20, 2005
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
  • Patent number: 6921753
    Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.
    Type: Grant
    Filed: June 19, 2001
    Date of Patent: July 26, 2005
    Assignee: Pfizer Inc
    Inventors: Simon John Mantell, Sandra Marina Monaghan, Peter Thomas Stephenson
  • Patent number: 6914053
    Abstract: Disclosed are novel adenosine A3 receptor agonists of Formula I: wherein: R is hydrogen or lower alkyl; R1 is optionally substituted lower alkoxy or optionally substituted cycloalkyloxy; R2 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted trialkylsilyl; and R3 is hydroxymethyl or R4R5NC(Q)—; in which R4 and R5 are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclyl, optionally substituted aryl, or optionally substituted heteroaryl.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: July 5, 2005
    Assignee: CV Therapeutics, Inc.
    Inventor: Gloria Cristalli
  • Patent number: 6900309
    Abstract: 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 as adenosine A2a receptor agonists.
    Type: Grant
    Filed: June 8, 2000
    Date of Patent: May 31, 2005
    Assignee: Pfizer Inc
    Inventors: Simon J. Mantell, Sandra M. Monaghan
  • Patent number: 6803457
    Abstract: A3 agonists, methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists. The A3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia.
    Type: Grant
    Filed: August 17, 2000
    Date of Patent: October 12, 2004
    Assignee: Pfizer, Inc.
    Inventors: Michael P. DeNinno, Hiroko Masamune, Robert W. Scott
  • Patent number: 6680382
    Abstract: The present invention provides for the preparation &bgr;-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and solvent. The present invention also provides for the stereoselective preparation of 2-deoxy-&bgr;-D-adenine nucleosides wherein a blocked 2-deoxy-&agr;-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. The forgoing aspects of the present invention are utilized in the preparation of a clofarabine composition wherein the ratio of &bgr; to &agr;-anomer is at least 99:1.
    Type: Grant
    Filed: August 1, 2002
    Date of Patent: January 20, 2004
    Assignee: Ilex Products, Inc.
    Inventors: William E. Bauta, Brian D. Burke, Brian E. Schulmeier, William R. Cantrell, Jr., Dennis P. Lovett, Jose Puente
  • Patent number: 6677316
    Abstract: A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: January 13, 2004
    Assignee: SmithKline Beecham Corporation
    Inventors: David Edmund Bays, Richard Peter Charles Cousins, Hazel Joan Dyke, Colin David Eldred, Brian David Judkins, Martin Pass, Andrew Michael Kenneth Pennell
  • Patent number: 6642210
    Abstract: N-pyrazole substituted 2-adenosine compounds and methods for using the compounds as A2A-adenosine receptor agonists useful to stimulate mammalian coronary vasodilation for therapeutic purposes and as adjuncts in cardiological imaging.
    Type: Grant
    Filed: April 12, 2002
    Date of Patent: November 4, 2003
    Assignee: CV Therapeutics, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
  • Patent number: 6576620
    Abstract: The present invention provides a method for identifying partial adenosine A1 receptor agonists that are useful in the treatment of arrhythmias. Partial adenosine A1 receptor agonists and methods for using partial adenosine A1 receptor agonists to treat arrhythmias in mammals.
    Type: Grant
    Filed: December 1, 2000
    Date of Patent: June 10, 2003
    Assignee: CV Therapeutics, Inc.
    Inventors: Luiz Belardinelli, Zhenhai Gao
  • Patent number: 6544960
    Abstract: A compound of formula (I), wherein R2 represents C1-3alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3alkyl, R2 represents C1-3alkyl, R1 cannot represent phenyl optionally substituted by one or more substituents selected from halogen, C1-3alkyl, trifluoromethyl, nitro, cyano, —CO2Rc, —CONRcRd, —CORc, —SORe, SO2Re, —SO3H, —SO2NRcRd, —ORc, —NHSO2Re, —NHCORc and —NRcRd; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists at the Adenosine Al receptor.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: April 8, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Colin David Eldred, Andrew Michael Kenneth Pennell
  • Patent number: 6498241
    Abstract: 2′-Deoxyisoguanosine, isosteric analogues and isoguanosine derivatives of formulae I-V, processes for their production via compounds of the general formulae a or b and reaction with aroyl isocyanates or from compounds of the general formulae VI-IX by photochemical irradiation. A further production process is the conversion of deoxyguanosines or guanosines by means of persilylation, reaction with ammonia and deamination in the 2 position. The compounds are suitable as pharmaceutical agents with antiviral efficacy.
    Type: Grant
    Filed: November 13, 2000
    Date of Patent: December 24, 2002
    Assignee: Roche Diagnostics GmbH
    Inventors: Frank Seela, Zigmunt Kasimierczuk, Klaus Mühlegger, Herbert Von Der Eltz
  • Patent number: 6492348
    Abstract: A compound of formula (I) which is an agonist at the adenosine Al receptor, wherein Y, Z, and W represent heteroatoms, and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof for use in therapy.
    Type: Grant
    Filed: March 6, 2001
    Date of Patent: December 10, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: David Edmund Bays, Richard Peter Charles Cousins, Hazel Joan Dyke, Colin David Eldred, Brian David Judkins, Martin Pass, Andrew Michael Kenneth Pennell
  • Patent number: 6407076
    Abstract: A compound of formula (I) wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists of the Adenosine A1 receptor.
    Type: Grant
    Filed: June 27, 2000
    Date of Patent: June 18, 2002
    Assignee: SmithKline Beecham Corporation
    Inventors: Philip Charles Box, Brian David Judkins, Andrew Michael Kenneth Pennell
  • Patent number: 6403567
    Abstract: 2-adenosine N-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
    Type: Grant
    Filed: June 22, 1999
    Date of Patent: June 11, 2002
    Assignee: CV Therapeutics, Inc.
    Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
  • Publication number: 20020052492
    Abstract: A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific combination of aprotic polar and nonpolar organic solvents to give the corresponding halogenated derivatives.
    Type: Application
    Filed: March 12, 2001
    Publication date: May 2, 2002
    Applicant: Reliable Biopharmaceutical, Inc.
    Inventors: Sampath UmaShanker, Bartlett Lawrence
  • Patent number: 6355787
    Abstract: This invention discloses a method for the preparation of 2′-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the novel pyrimidines and purines that can be prepared according to the method of the invention and oligonucleotides containing said modified pyrimidines and purines.
    Type: Grant
    Filed: January 31, 2000
    Date of Patent: March 12, 2002
    Assignee: Gilead Sciences, Inc.
    Inventors: Jeffrey T. Beckvermit, Chi Tu
  • Patent number: RE38090
    Abstract: The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may be substituted by a group represented by the formula: in which Ra, Rb and Rc are individually a lower alkyl group or a phenyl group, or an oxiranyl group which may have at least one lower alkyl group, R1 and R2 individually represent H or an ester-forming residue capable of easily leaving in a living body, and R3 is H, a mono- or polyphosphoric acid residue, or an ester-forming residue capable of easily leaving in a living body, with the proviso that the sugar moiety is ribose, or a pharmaceutically acceptable salt thereof. The 3′-substituted nucleoside derivative according to the invention has an excellent antitumor activity and is hence useful for treatment for and prevention of cancers.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: April 22, 2003
    Assignees: Taiho Pharmaceutical Co., Ltd.
    Inventors: Akira Matsuda, Takuma Sasaki