Nitrogen, Chalcogen, Or Additional Carbon Bonded Directly To The 6-position Nitrogen (e.g., 6-position Nitrogen Is Substituted, Etc.) Patents (Class 536/27.62)
  • Patent number: 10174033
    Abstract: The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: January 8, 2019
    Assignee: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Jiangong Shi, Jianjun Zhang, Zhenggang Yue, Min Li, Chenggen Zhu, Ying Zhang, Jiachen Zi, Yafang Wang, Xiaona Fan, Ruiming Xu, Sheng Lin, Yan Li, Yongchun Yang, Li Sheng
  • Patent number: 9186369
    Abstract: This invention is directed to a method for treating a host, especially a human, infected with hepatitis C, flavivirus and/or pestivirus, comprising administering to that host an effective amount of an anti-HCV biologically active pentofuranonucleoside where the pentofuranonucleoside base is an optionally substituted 2-azapurine. The optionally substituted pentofuranonucleoside, or a salt or prodrug thereof, may be administered alone or in combination with one or more optionally substituted pentofuranonucleosides or other anti-viral agents.
    Type: Grant
    Filed: May 2, 2014
    Date of Patent: November 17, 2015
    Assignee: Idenix Pharmaceuticals, LLC
    Inventors: Richard Storer, Gilles Gosselin, David Dukhan, Frederic Leroy
  • Publication number: 20150126726
    Abstract: The invention relates to the development of drugs intended for the prophylaxis and/or treatment of viral diseases caused, in particular, by herpes viruses. What are proposed are complex compounds of germanium having the general structural formula: Gex[AD][CA]y[AA]z??(I), where AD is a derivative of a nitrogenous base of the purine series that has antiviral activity and can be selected from guanine derivatives, such as acyclovir, valacyclovir, gancyclovir and pencyclovir, or from adenine derivatives, such as vidarabine; CA is a hydroxycarboxylic acid which can be selected from acids such as (but not limited to) citric acid, lactic acid and malic acid; AA is an amino acid which can be selected from various a-amino acids, such as arginine, glycine, lysine and threonine, and where x=1-2, y=2-4 and z=0-2. Complex compounds of germanium have a high level of antiviral and immune-stimulating activity and are readily soluble in water.
    Type: Application
    Filed: November 1, 2012
    Publication date: May 7, 2015
    Applicant: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTYU "WDS FARMA"
    Inventors: Alexandr Dmitrievich Isaev, Igor Valerievich Ambrosov, Tamaz Omarovich Manasherov, Svetlana Konstantinovna Matelo
  • 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: 8895530
    Abstract: Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).
    Type: Grant
    Filed: June 4, 2013
    Date of Patent: November 25, 2014
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley, Prakash Jagtap
  • Patent number: 8748593
    Abstract: Orthogonally protected 3?-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3?-amino group in the presence of the unprotected nucleoside base.
    Type: Grant
    Filed: December 22, 2008
    Date of Patent: June 10, 2014
    Assignee: Geron Corporation
    Inventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
  • 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
  • Patent number: 8637485
    Abstract: The crystal structure of the complex of S-adenosylmethionine methyl ester with h?doMetDC F223A, a mutant where the stacking of the aromatic rings of F7, adenine and F223 would be eliminated. The structure of this mutant with the ester shows that the ligand still maintains a syn conformation aided by pi-pi interactions to F7, hydrogen bonds to the backbone of Glu67, and electrostatic interactions. Several series of AdoMet substrate analogues with a variety of substituents at the 8 position of adenine were synthesized and analyzed for their ability to inhibit hAdoMetDC. To understand these results, virtual modeling of the enzyme inhibitor complexes and the crystal structures of human AdoMetDC with 5?-deoxy-5?-[N-methyl-N-[2-(aminooxy)ethyl]amino-8-methyl]adenosine (MAOEMA) and 5?-deoxy-5?-[N-methyl-N-[4-(aminooxy)butyl]amino-8-ethyl]adenosine (MAOBEA) at the active site have been determined experimentally.
    Type: Grant
    Filed: August 1, 2008
    Date of Patent: January 28, 2014
    Assignees: Southern Research Institute, Cornell University, H. Lee Moffitt Cancer and Research Institute, The Penn State Research Foundation
    Inventors: John A. Secrist, III, Steven Ealick, Shridhar Bale, Anthony E. Pegg, Diane E. McCloskey, Wayne C. Guida
  • 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: 8501708
    Abstract: Provided herein are a class of purine nucleoside compounds, particularly substituted adenosine compounds, such as benzyloxy cyclopentyladenosine (BCPA) compounds, as well as methods of using these compounds as selective A1 adenosine receptor agonists, particularly for reducing and/or controlling elevated or abnormally fluctuating intraocular pressure (IOP) in the treatment of glaucoma or ocular hypertension (OHT).
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: August 6, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventor: Prakash Jagtap
  • Publication number: 20130196940
    Abstract: The present invention provides novel anhydrous polymorph forms of 2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl nitrate (Compound A). The present invention also provides processes for preparation of the anhydrous polymorphic forms of compound A.
    Type: Application
    Filed: January 25, 2013
    Publication date: August 1, 2013
    Applicant: INOTEK PHARMACEUTICALS CORPORATION
    Inventor: Inotek Pharmaceuticals Corporation
  • Patent number: 8476247
    Abstract: Provided herein is a method of reducing intraocular pressure (IOP) in humans using N6-cyclopentyladenosine (CPA), CPA derivatives or prodrugs or enhanced cornea permeability formulations of CPA. In one embodiment, the invention is directed to CPA derivatives or prodrugs that are permeable to the cornea. In another embodiment, the invention is directed to uses of certain compounds in human subjects for reducing and/or controlling elevated or abnormally fluctuating IOPs in the treatment of glaucoma or ocular hypertension (OHT).
    Type: Grant
    Filed: March 25, 2011
    Date of Patent: July 2, 2013
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Norman N. Kim, William K. McVicar, Thomas G. McCauley, Prakash Jagtap
  • 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: 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: 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
  • Publication number: 20130045942
    Abstract: The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
    Type: Application
    Filed: December 10, 2009
    Publication date: February 21, 2013
    Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Jiangong Shi, Jianjun Zhang, Zhenggang Yue, Min Li, Chenggen Zhu, Ying Zhang, Jiachen Zi, Yafang Wang, Xiaona Fan, Ruiming Xu, Sheng Lin, Yan Li, Yongchun Yang, Li Sheng
  • Publication number: 20120329747
    Abstract: A patentable new class of hydrazone derivative compounds is described, as are methods for synthesizing such compounds. The hydrazones of the invention can be used, for example, as potent anti-cancer agents, including to inhibit the growth of cancer cells that exhibit multidrug resistance.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: Hiremagular N. JAYARAM, Praveen KUSUMANCHI, Mario GRIFANTINI, Palmarisa FRANCHETTI, Loredana CAPPELLACCI, Riccardo PETRELLI
  • 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: 20120296076
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 22, 2012
    Inventors: Richard Hung Chiu Yu, Brandon Heath Brown, Richard P. Polniaszek, Benjamin R. Graetz, Keiko Sujino, Duong Duc-Phi Tran, Alan Scott Triman, Kenneth M. Kent, Steven Pfeiffer
  • Publication number: 20120232029
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Patent number: 8252919
    Abstract: The present invention relates to a method for producing a 2?-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating or a carbamoylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2?-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2?,3?-hydroxy groups are not protected.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Kaneka Corporation
    Inventors: Hirofumi Maeda, Akio Fujii, Masaru Mitsuda
  • Patent number: 8193339
    Abstract: This invention relates to a process of stereoselectively synthesizing a ?-nucleoside compound of formula (I): wherein R1, R2, and B are as defined in the specification; each of R3 and R4, independently, is H or fluoro. The process includes reacting, in the presence of a transition metal salt, a tetrahydrofuran compound of formula (II): wherein R1, R2, and L are as defined in the specification, with a nucleobase derivative; and each of R3 and R4, independently, is H or fluoro.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: June 5, 2012
    Assignee: Pharmaessentia Corp.
    Inventors: Chi-Yuan Chu, Wei-Der Lee, Wensen Li, Chan Kou Hwang
  • 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
  • Publication number: 20120071433
    Abstract: The invention relates to 2-substituted-6-(substituted benzylamino)purine riboside derivatives of the general formula I. These compounds possess antiapoptotic, anti-inflammatory and differentiating activities. The invention relates also to the compositions, which contain these derivatives as active ingredients.
    Type: Application
    Filed: May 12, 2010
    Publication date: March 22, 2012
    Inventors: Lucie Szucova, Viadimir Krystof, Marek Zatloukal, Karel Dolezal, Miroslav Strnad, Lukas Spichal
  • Publication number: 20120071641
    Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least one nucleoside of formula (2): Another aspect of the invention relates to a method of inhibiting the expression of a gene in cell, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
    Type: Application
    Filed: March 2, 2010
    Publication date: March 22, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Alexander V. Kelin, Sudhakar Rao Takkellapati, Shigeo Matsuda
  • Publication number: 20120071646
    Abstract: There is a demand for a convenient production method of an NC type purine nucleoside. The present invention relates to a method of producing a purine nucleoside represented the formula (I?) or a salt thereof, which comprising reacting a pyrimidine nucleoside represented by the formula (I) or a salt thereof with a purine nucleobase represented by the formula B?H in the presence of a Lewis acid.
    Type: Application
    Filed: March 30, 2010
    Publication date: March 22, 2012
    Inventors: Tadashi Umemoto, Yoji Hayase, Shumpei Murata, Kenichi Miyata
  • Patent number: 8119614
    Abstract: The invention concerns novel substitution derivatives of N6-benzyladenosine having anticancer, mitotic, immunosuppressive and antisenescent properties for plant, animal and human cells. This invention also relates to the methods of preparation of these N6-benzyladenosine derivatives and their use as drugs, cosmetic preparations and growth regulators comprising these derivatives as active compound and use of these derivatives for preparation of pharmaceutical compositions, in biotechnological processes, in cosmetics and in agriculture.
    Type: Grant
    Filed: December 29, 2003
    Date of Patent: February 21, 2012
    Assignee: Ustav Experimentalni Botaniky Akademie Ved Ceske Republiky
    Inventors: Karel Dolezal, Igor Popa, Marek Zatloukal, René Lenobel, Dana Hradecká, Borivoj Vojtesek, Stjepan Uldrijan, Petr Mlejnek, Stefaan Werbrouck, Miroslav Strnad
  • Publication number: 20110294122
    Abstract: Methods for preparation of 2?,3?-dideoxynucleotides support structures, such as 2?,3?-dideoxyguanosine, 2?,3?-dideoxyadenosine, and 3?-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as their use for automated DNA synthesis and pyrophosphorolysis activated polymerization.
    Type: Application
    Filed: May 26, 2011
    Publication date: December 1, 2011
    Applicant: Life Technologies Corporation
    Inventors: Zhaochun Ma, Khairuzzaman Bashar Mullah, Robert Eason
  • Publication number: 20110178284
    Abstract: A protective group represented by the following general formula (I) (the oxygen atom attached with * represents oxygen atom of 2?-hydroxyl group of a ribonucleoside, a ribonucleotide or a derivative thereof; R1 and R2 both represent hydrogen atom, or represent a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; R3 and R4 represent hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 halo-substituted alkyl group; and R5 and R6 represent a halogen atom, a C1-6 halo-substituted alkyl group, cyano group, nitro group, or the like), which is stable under the reaction conditions of the nucleic acid synthetic cycles and has little steric hindrance, and can be removed under mild conditions using fluoride ions as a base.
    Type: Application
    Filed: September 15, 2010
    Publication date: July 21, 2011
    Applicant: CHIRALGEN, LTD.
    Inventors: Takeshi WADA, Mamoru SHIMIZU
  • Patent number: 7915232
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof which inhibit HCV polymerase and are useful for treating a patient suffering from a HCV infection and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: March 29, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Nobuo Shimma, Takuo Tsukuda
  • Publication number: 20110015382
    Abstract: This invention relates to synthesis of novel -N-FMOC protected nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides and RNA oligonucleotide synthesis. Our discovery using N-FMOC as nucleoside base protecting group, which is highly base labile protecting group is a novel approach to obtain highest purity oligonucleotides. This approach is designed to lead to very high purity and very clean oligonucleotide, after efficient removal of the protecting groups and to produce high purity therapeutic grade DNA oligonucleotides, RNA oligonucleotides, diagnostic DNA, diagnostic RNA for microarray platform. The deprotection of FMOC protecting groups of the natural deoxy and ribonucleosides occurs under very mild deprotection conditions such as mild bases, secondary and tertiary amines for removal of such groups under such conditions would allows synthesis of various DNA and RNA of highest purity for diagnostics and therapeutic application.
    Type: Application
    Filed: November 30, 2009
    Publication date: January 20, 2011
    Applicant: ChemGenes Corporation
    Inventors: Suresh C. Srivastava, Naveen P. Srivastava
  • 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: 7772198
    Abstract: 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: Grant
    Filed: April 21, 2006
    Date of Patent: August 10, 2010
    Assignees: Centre National de la Recherche Scientifique, Universite Joseph Fourier, Universite de Poitiers
    Inventors: Jean-Luc Decout, Christel Routaboul, Frederic Becq, Caroline Norez
  • Patent number: 7741473
    Abstract: The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles (Formula I). The process comprises the steps of: (a) obtaining a compound of Formula II, which is a mixture of cis and trans-diastereomers, and (b) chemically decomposing the compound of Formula II in a solution comprising a solvent and an acid that is a hydrogen donor or an electron pair acceptor, whereby the cis diastereomer is decomposed and the compound of Formula I is obtained. The compounds prepared by the present invention are useful in treating diseases or conditions associated with platelet aggregation and/or platelet activation.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: June 22, 2010
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: Paul S. Watson, James G. Douglass, III, Bob Suchozak, Subramanian Pandiaraju, Craig E. Dixon, Daniel Levin
  • Patent number: 7737127
    Abstract: The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here.
    Type: Grant
    Filed: March 26, 2007
    Date of Patent: June 15, 2010
    Assignee: University of Virginia Patent Foundation
    Inventors: Joel M. Linden, Jayson M. Rieger, Timothy L. Macdonald, Gail W. Sullivan, Lauren Jean Murphree, Robert Alan Figler
  • 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: 7696181
    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, myocardial infarction and hyperlipidemia. The structure of the compounds is given by Formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z, and T are as described herein.
    Type: Grant
    Filed: August 24, 2006
    Date of Patent: April 13, 2010
    Assignee: CV Therapeutics, Inc.
    Inventors: Prabha Ibrahim, Elfatih Elzein, Kevin Shenk, Robert Jiang, Jeff Zablocki, Xiaofen Li, Christopher Morrison, Thao Perry, Dengming Xiao
  • 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
  • Publication number: 20100062994
    Abstract: The present application discloses locked nucleoside compounds of the Formula I which act as antagonists of adenosine receptors, in particular the adenosine A3 receptor, and the use of such adenosine A3 receptor compounds in medicine, e.g.
    Type: Application
    Filed: July 6, 2007
    Publication date: March 11, 2010
    Applicant: SANTARIS PHARMA A/S
    Inventors: Jacob Ravn, Christoph Rosenbohm, Katrine Qvortrup, Troels Koch
  • 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
  • Publication number: 20090240045
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2, R3, R4 and W are as defined herein.
    Type: Application
    Filed: April 19, 2007
    Publication date: September 24, 2009
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 7544794
    Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, this invention relates to compositions that allow the sequencing of oligonucleotides by synthesis, and processes for sequencing by synthesis that exploit these compositions. Most specifically, the instant invention discloses compositions of matter that are 5?-triphosphates of ribo- and 2?-deoxyribonucleosides wherein the 3?-OH group is replaced by a 3?-ONHR group in the alpha configuration, wherein R is either a H or CH3 group. Also disclosed are these triphosphates where the nucleobase carries, via a linker, a reporter groups, such as a fluorescent species that can be used in single- or multi-copy DNA sequencing, or a tag that can be visualized by ultramicroscopy. Also disclosed are processes that use these compositions to do sequencing by synthesis.
    Type: Grant
    Filed: March 11, 2006
    Date of Patent: June 9, 2009
    Inventor: Steven Albert Benner
  • Publication number: 20090093001
    Abstract: A high content screening (HCS) assay for rapidly screening one or more compounds to determine functional response or pharmacological properties thereof, comprising: i) priming a cell or cell material with a sensor for a biological response; ii) contacting the compound(s) to be tested with the primed cell or cell material or contacting a cell or cell material which has been contacted with the compound(s) with the primed cell or cell material; iii) simultaneously or subsequently contacting with a fluorescent agonist or a fluorescent neutral antagonist wherein the binding of the fluorescent agonist or antagonist and its associated biological response are detected or monitored in the same cell and are distinct allowing separate readout.
    Type: Application
    Filed: September 26, 2005
    Publication date: April 9, 2009
    Inventors: Stephen John Hill, Barrie Kellam, Stephen John Briddon
  • Patent number: 7511133
    Abstract: The compounds of the following formula: wherein Ar, R and R1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the 5? position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido derivatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: March 31, 2009
    Assignee: King Pharmaceuticals Research and Development, Inc.
    Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Pier A. Borea
  • Publication number: 20090054369
    Abstract: Novel compositions of silicon-containing anti-metabolite compounds, their preparation and use in methods for treating cancer are described. The silyl group confers lipophilicity that can enhance the penetration of the compounds across the gut wall, cell membranes and blood brain barrier, thus improving therapeutic properties including bioavailability, metabolism, and/or pharmacokinetics. The triorganosilyl group provides compounds having improved pharmacokinetics and anti-tumor activity. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for treatment of diseases and other maladies or conditions involving cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: August 2, 2006
    Publication date: February 26, 2009
    Applicant: RND PHARMACEUTICALS, INC.
    Inventor: Stephen Gately
  • Patent number: 7488720
    Abstract: Disclosed are novel compounds that are A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, diseases related to release of nonesterified fatty acids, and myocardial infarction.
    Type: Grant
    Filed: October 11, 2006
    Date of Patent: February 10, 2009
    Assignee: CV Therapeutics, Inc.
    Inventors: Elfatih Elzein, Xiaofen Li, Jeff Zablocki
  • Patent number: 7479485
    Abstract: 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: Grant
    Filed: October 28, 2005
    Date of Patent: January 20, 2009
    Assignee: CV Therapeutics, Inc.
    Inventors: Luiz Belardinelli, Arvinder Dhalla
  • Patent number: 7423144
    Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, 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: May 25, 2005
    Date of Patent: September 9, 2008
    Assignee: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Csaba Szabo, Andrew L. Salzman