Nitrogen Bonded Directly To Ring Carbon Of The Purine Ring System (e.g., Adenine, Etc.) Patents (Class 514/263.4)
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Patent number: 7985754Abstract: The present invention provides compounds of formulae Ia and Ib: wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.Type: GrantFiled: July 16, 2007Date of Patent: July 26, 2011Assignee: Trovis Pharmaceuticals, LLCInventors: Anthony Beauglehole, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20110171130Abstract: Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.Type: ApplicationFiled: July 31, 2009Publication date: July 14, 2011Applicant: The United States of America, as represented by the Secretary ,Deptment of Health and HumanServiceInventors: Kenneth A. Jacobson, Artem Melman, Ben Bih-Ren Wang
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Publication number: 20110160228Abstract: The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 represent, independently of one another, a hydrogen atom or a methoxy group optionally substituted by one or more fluorine atoms, —A represents a ring chosen from the group comprising aryl and heteroaryl groups, said ring possibly being substituted by or fused to a heterocycle, —X represents a nitrogen atom or a CH group, and —Z1 represents a hydrogen atom or a halogen atom, preferably fluorine, and —Z2 represents a hydrogen atom, a halogen atom, preferably fluorine, a C1 to C4 alkyl group, an aryl group or a —CN, —SO2NR12R13, —SO2R9, —COOR15 or —COR15 group, and also to the pharmaceutically acceptable salts thereof, the isomers thereof and the prodrugs thereof.Type: ApplicationFiled: June 4, 2009Publication date: June 30, 2011Inventors: Mouâd Alami, Samir Messaoudi, Abdallah Hamze, Olivier Provot, Jean-Daniel Brion, Jian-Miao Liu, Jérôme Bignon, Joanna Bakala
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Publication number: 20110160229Abstract: The present invention is directed to AHCY inhibitors of formula (I): which are useful in the treatment of diseases characterized by high homocysteine levels, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases characterized by high homocysteine levels.Type: ApplicationFiled: August 31, 2009Publication date: June 30, 2011Inventors: Antonella Converso, Timothy J. Hartingh, Mark E. Fraley
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Publication number: 20110152213Abstract: It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural “riboswitches” (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies.Type: ApplicationFiled: February 23, 2011Publication date: June 23, 2011Inventors: Ronald R. Breaker, Ali Nahvi, Narasimhan Sudarsan, Margaret S. Ebert, Wade Winkler, Jeffrey E. Barrick, John K. Wickiser
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Publication number: 20110152215Abstract: It has been discovered that certain natural mRNAs serve as metabolite-sensitive genetic switches wherein the RNA directly binds a small organic molecule. This binding process changes the conformation of the mRNA, which causes a change in gene expression by a variety of different mechanisms. Modified versions of these natural “riboswitches” (created by using various nucleic acid engineering strategies) can be employed as designer genetic switches that are controlled by specific effector compounds. Such effector compounds that activate a riboswitch are referred to herein as trigger molecules. The natural switches are targets for antibiotics and other small molecule therapies.Type: ApplicationFiled: February 23, 2011Publication date: June 23, 2011Inventors: Ronald R. Breaker, Ali Nahvi, Narasimhan Sudarsan, Margaret S. Ebert, Wade Winkler, Jeffrey E. Barrick, John K. Wickiser
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Patent number: 7960397Abstract: Certain 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts of the following general formula are provided wherein R6 and R9 are as defined in the specification. These 6,9-disubstituted purine derivatives and their pharmaceutically acceptable salts are useful in compositions for application to mammalian cells, and especially human skin cells, in order to improve the cosmetic appearance of the mammalian cells, especially human skin.Type: GrantFiled: December 28, 2007Date of Patent: June 14, 2011Assignee: Institute of Experimental Botany, Academy of Sciences of the Czech RepublicInventors: Lucie Szucova, Marek Zatloukal, Lukas Spichal, Jiri Voller, Karel Dolezal, Miroslav Strnad, Frank J. Massino
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Patent number: 7951803Abstract: Compounds of the formula wherein R1 represents optionally substituted C1-C10 alkyl, aryl or heteroaryl, and R3 represents alkoxy-substituted aryl or optionally substituted heteroaryl, are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.Type: GrantFiled: March 9, 2007Date of Patent: May 31, 2011Assignee: Pharmacopeia, LLCInventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
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Publication number: 20110104065Abstract: Described herein are progenitor cancer cells and cell lines isolated from human breast ductal carcinoma in situ (DCIS) lesions and the uses of these cells or cell lines in drug design, drug screening, and monitoring in vivo therapy. The DCIS malignant precursor cells or cell lines are epithelial in origin, are positive for markers of autophagy, show at least one genetic difference from normal cells of said fragment, form 3-D tube-like structures or ball aggregates, or are inhibited in formation of 3-D structures and migration by treatment with chloroquine. In one embodiment, there is a loss of heterozygosity (LOH) that is narrowly confined to a region of chromosome 6p (6p21.1-6p12.3) that contains the SUPT3H gene.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: Virginia Espina, Lance Liotta
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Publication number: 20110104054Abstract: Hsp90 inhibitors having are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.Type: ApplicationFiled: November 4, 2010Publication date: May 5, 2011Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Huazhong He, Laura Llauger-bufi, Joungnam Kim, Steven M. Larson, Peter Smith-Jones
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Patent number: 7932263Abstract: A combination comprising candesartan and rosuvastatin for the prevention or treatment of arteriosclerosis and for the prevention of cardiovascular events is described.Type: GrantFiled: September 22, 2004Date of Patent: April 26, 2011Assignee: AstraZeneca ABInventor: Jay Lal Mehta
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Publication number: 20110092521Abstract: The invention relates to treating a disease or condition in which it is desirable to inhibit 5?-methylthioadenosine phosphorylase (MTAP) and/or 5?-methylthioadenosine nucleosidase (MTAN). The invention particularly relates to the co-administration of 5?-methylthioadenosine (MTA), or a prodrug of MTA, with one or more MTAP/MTAN inhibitors. Included among the diseases treatable are prostate cancer and head and neck cancer.Type: ApplicationFiled: February 23, 2007Publication date: April 21, 2011Inventors: Richard Hubert Furneaux, Peter Charles Tyler, Gary Brian Evans, Vern L. Schramm
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Publication number: 20110092522Abstract: The invention provides compositions and methods that employ compounds that can stimulate proliferation of fibroblasts or keratinocytes and/or stimulate production of collagen by fibroblasts. These compositions and methods are useful for treating gum- and skin-related conditions.Type: ApplicationFiled: November 23, 2010Publication date: April 21, 2011Applicant: KIMBERLY-CLARK WORLDWIDE, INC.Inventor: Sohail Malik
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Publication number: 20110092523Abstract: The present invention provides a method for lowering intraocular pressure and providing neuroprotection to a patient in need thereof by administering a therapeutically effective amount of at least one non-nucleotide or non-protein agent that inhibits expression and/or signaling of connective tissue growth factor (CTGF).Type: ApplicationFiled: December 16, 2010Publication date: April 21, 2011Applicant: ALCON RESEARCH, LTD.Inventors: Debra L. Fleenor, Allan Shepard, Nasreen Jacobson, Iok-Hou Pang, Abbot F. Clark
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Publication number: 20110059921Abstract: The invention relates to (among other things) oligomer-nitrogenous base conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over unconjugated nitrogenous base compounds.Type: ApplicationFiled: March 27, 2009Publication date: March 10, 2011Applicant: Ektar TherapeuticsInventor: Jennifer Riggs-Sauthier
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Publication number: 20110053883Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect c-Jun NH2-terminal kinase; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a c-Jun NH2-terminal kinase in a reaction system in which the c-Jun NH2-terminal kinase contacts with a test substance, and the like.Type: ApplicationFiled: June 23, 2006Publication date: March 3, 2011Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Yasutaka Shimokawatoko, Mar Van De Craen, Irene Nooren, Sandra Turconi, Annelies Roobrouck, Wendy Maddelein
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Publication number: 20110046131Abstract: A chemical genus of purines, which are useful as PKC? inhibitors, is disclosed.Type: ApplicationFiled: October 19, 2007Publication date: February 24, 2011Inventors: Irina Neagu, Andrew Laird Roughton, Koc-Kan Ho, David Diller, Jui-Hsiang Chan, Michael Ohlmeyer, Celia Kingsbury, Johannes Petrus Maria Lommerse, Neeltje Miranda, Jacobus Cornelis Henricus Maria Wijkmans
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Publication number: 20110046166Abstract: Disclosed are (N)-methanocarba adenine nucleosides, e.g., of formula (I) as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.Type: ApplicationFiled: March 24, 2009Publication date: February 24, 2011Applicant: Office of Technology Transfer, NIHInventors: Kenneth A. Jacobson, Artem Melman
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Publication number: 20110046164Abstract: Provided herein are methods of treatment of a cystic disease by administering a compound of Formula I. In certain embodiments, the compound for use in the methods provided herein is roscovitine or an analog thereof.Type: ApplicationFiled: October 19, 2007Publication date: February 24, 2011Inventors: Nikolay O. Bukanov, Oxana Beskrovnaya
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Publication number: 20110021524Abstract: This invention provides a combination of ATP-competitive BCR-ABL inhibitor and a non-ATP competitive BCR-ABL inhibitor. The combination of the present invention may be used for treating cancers known to be associated with BCR-ABL.Type: ApplicationFiled: December 18, 2008Publication date: January 27, 2011Applicant: IRM LLCInventors: Francisco Adrian, Christine Dierks, Nathanael S. Gray, Markus Warmuth
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Publication number: 20110009351Abstract: The present invention relates to a novel assay or screen for identifying compounds with potential therapeutic value for the treatment of protein trafficking diseases such as Cystic Fibrosis (CF) and nephrogenic diabetes insipidus (NDI). The usual approach involves expressing the mutant form of the gene in cells and assaying function in a multiwell format when cells are exposed to libraries of compounds. Although such functional assays are useful, they do not directly test the ability of a compound to correct defective trafficking of the protein. To address this a novel corrector screening assay for CF has been developed in which the appearance of the mutant protein at the cell surface is measured as the assay output. This assay was used to screen more than 3100 compounds. This novel screening approach to protein trafficking diseases is robust and general, and may enable the selection of molecules that can be translated rapidly to a clinical setting.Type: ApplicationFiled: May 9, 2008Publication date: January 13, 2011Inventors: David Y. Thomas, John Hanrahan, Graeme Carlile, Renaud Robert
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Publication number: 20110009475Abstract: The invention relates to methods and products for treating emotional disorders such as stress induced emotional disorders, as well as related assays and kits. Methods include administering to a subject an effective amount of an agent for targeting the Rac1, Cdk5, p35, PAK-1 pathway to treat the emotional disorder. The agent for targeting the Rac1, Cdk5, p35, PAK-1 pathway may be, for instance a Rac-1 inhibitor, a Cdk5 inhibitor, a PAK-1 activator, or p35 mobilizing agent.Type: ApplicationFiled: July 11, 2008Publication date: January 13, 2011Applicant: Massachusetts Institute of TechnologyInventors: Andre Fischer, Li-Huei Tsai
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Patent number: 7868011Abstract: The present invention provides methods for suppressing autoimmunity in a patient in need of treatment for systemic lupus erythematosus by administering to the patient an effective amount of methyl 4-(Adenin-9-yl)-2-hydroxybutanoate or pharmaceutically acceptable salts thereof. In some embodiments, the claimed methods include co-administering an effective amount of an immunosuppressant.Type: GrantFiled: January 5, 2007Date of Patent: January 11, 2011Assignee: General AtomicsInventor: Chong-Sheng Yuan
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Publication number: 20110003764Abstract: The present invention relates to a drug combination capable of conferring therapeutic benefits in the treatment of both AIDS and malaria. In particular, it relates to a drug combination including at least one quinolinic antimalarial compound such as chloroquine or hydroxychloroquine, and at least one inhibitor of the Human Immunodeficiency Virus (HIV) protease enzyme. This drug combination is capable of inhibiting the replication of both HIV and Plasmodium sp. It also relates to the direct antimalarial effects of the HIV PIs.Type: ApplicationFiled: May 26, 2009Publication date: January 6, 2011Inventor: Andrea Savarino
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Publication number: 20100311768Abstract: The invention relates to the use of purine derivatives in the manufacture of a medicament for treating pathological conditions in which an imbalance between cell division and apoptosis is involved, and more particularly in which excessive apoptosis is responsible for the pathological condition. According to the invention, a purine derivative of formula I is used. The invention finds use in the pharmaceutical field.Type: ApplicationFiled: September 12, 2008Publication date: December 9, 2010Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE RENNES 1, UNIVERSITE PARIS DESCARTES, UNIVERSITE DE BRETAGNE OCCIDENTALE, CENTRE HOSPITALIER UNIVERSITAIRE DE BRESTInventors: Laurent Meijer, Karima Bettayeb, Herve Galons, Nassima Oumata, Christian Berthou, Karine Lester
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Publication number: 20100311767Abstract: The present invention relates to a method for the treatment of an amyloidosis such as Alzheimer's disease in a subject in need thereof, characterized in that it comprises administering an agonist of the P/Q type voltage-gated presynaptic calcium channel to said subject.Type: ApplicationFiled: February 27, 2008Publication date: December 9, 2010Applicant: ABBOTT GMBH & CO. KGInventors: Volker Nimmrich, Stefan Barghorn, Ulrich Ebert, Heinz Hillen, Gerhard Gross, Andreas Draguhn, Claus Bruhl, Christine Grimm, Carsten Krantz
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Publication number: 20100298352Abstract: A method of inhibiting a carcinoma in a subject, comprising administering to the subject at least one therapeutic agent that selectively targets carcinoma stem cells. Illustrative carcinoma stem cell-selective therapeutic agents include CGP74514A, rottlerin, and A-77636.Type: ApplicationFiled: May 6, 2010Publication date: November 25, 2010Inventors: Edward V. Prochownik, John S. Lazo
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Publication number: 20100298354Abstract: Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C1-C4)-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.Type: ApplicationFiled: January 21, 2009Publication date: November 25, 2010Applicant: ESTEVE QUIMICA, S.A.Inventors: Marti Bartra Sanmarti, Ramón Berenguer Maimó, Jordi Benet-Buchholz, Luis Sola I Carandell
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Publication number: 20100298353Abstract: A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.Type: ApplicationFiled: July 1, 2010Publication date: November 25, 2010Inventors: Stephan Anthony Billstein, Robert Charnas, Spotswood Spruance
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Publication number: 20100298209Abstract: The invention which is the subject of the present application relates to a compound of structure I: A-B-C for use in the prophylaxis and/or treatment of a viral infection, and in particular for preventing and/or inhibiting viral replication, in which A is a quinoline or a quinoline-type group, B is a single amino acid or a peptide or polypeptide having a given amino acid sequence, C is an O-phenoxy group and the symbol “-” indicates that the entities A, B and C are chemically bonded within the compound I. According to a particular embodiment, said compound is a protease inhibitor, in particular a caspase inhibitor, and more particularly the inhibitor Q-VD-OPh (N-(2(quinolyl)valyl-aspartyl-(2,6-difluorophenoxy)methyl ketone), optionally in an O-methylated form.Type: ApplicationFiled: October 31, 2008Publication date: November 25, 2010Inventors: Jérôme Estaquier, Mireille Laforge, Anna Senik
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Publication number: 20100284959Abstract: The present invention provides specific double-stranded DNA/RNA binding compounds having a polymeric structure, which are in fact, triplex forming molecules capable of binding tightly and specifically to predetermined sequences in the major groove of double stranded nucleic acid molecules; as well as pharmaceutical compositions comprising thereof. The triplex forming molecules and the pharmaceutical compositions of the invention can be used for various therapeutic applications such as site-specific modulation of gene expression and targeting of DNA or RNA damage, as well as for diagnostic applications in vitro.Type: ApplicationFiled: July 22, 2010Publication date: November 11, 2010Applicant: GENE ARREST LTD.Inventors: ANWAR RAYAN, MIZIED FALAH
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Publication number: 20100284970Abstract: The present invention relates to new benzimidazole modulators of H1 receptor activity and/or inhibitors of NS4B protein activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 9, 2010Publication date: November 11, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20100286126Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.Type: ApplicationFiled: April 19, 2007Publication date: November 11, 2010Applicant: NOVARTIS AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20100280052Abstract: The invention provides for the use of compounds active against cytomegalovirus (CMV) in the preparation of medicaments for improving the immune response of a CMV-seropositive, immunocompetent individual, or for the amelioration of certain other medical conditions. Suitable compounds include the nucleoside analogues acyclovir, famciclovir, and valacyclovir. Infection with cytomegalovirus is widespread and commonly believed to be both asymptomatic in immunocompetent individuals and unbeatable without the use of highly cytotoxic drugs. It is suggested herein that, in fact, CMV infection produces a disproportionately large immune response, thereby weakening the ability of the immune system to respond to other infections (and hence is not asymptomatic).Type: ApplicationFiled: May 30, 2008Publication date: November 4, 2010Inventor: Paul Austin Henry Moss
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Patent number: 7825126Abstract: Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.Type: GrantFiled: September 2, 2005Date of Patent: November 2, 2010Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Bhalchandra V. Joshi, Susanna Tchilibon
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Patent number: 7820636Abstract: An object of the invention is to provide a substance that activates saccharide uptake in epidermal cells and is thus expected to be effective in promoting skin cell neogenesis and metabolism. The invention provides a promoter for saccharide uptake in epidermal keratinocytes which comprises a purine base or a salt thereof as an active ingredient. The present invention further provides a method of promoting saccharide uptake in epidermal keratinocytes, comprising applying a purine base or a salt thereof to the skin.Type: GrantFiled: March 20, 2002Date of Patent: October 26, 2010Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiromichi Okuda, Chie Morimoto, Kenji Kameda, Fumiki Harano
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Publication number: 20100249066Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: ApplicationFiled: May 13, 2010Publication date: September 30, 2010Inventors: Brydon L. Bennett, Kate Blease, Brian Edwin Cathers
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Publication number: 20100239657Abstract: The inventive composite having a nanoscale particle size can specifically deliver therapeutic nucleic acids or drugs to the liver and selectively release them into hepatic cells to manifest potent therapeutic effects without inducing any enzymatic abnormalities or pathological damage to the normal liver function, when administered together with the therapeutic agents.Type: ApplicationFiled: June 1, 2010Publication date: September 23, 2010Applicant: MOGAM BIOTECHNOLOGY RESEARCH INSTITUTEInventors: Meehyein KIM, Soo In Kim, Duckhyang Shin, Mahnhoon Park
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Publication number: 20100239563Abstract: The invention relates to the use of at least one active substance for producing a pharmaceutical composition for the prophylaxis and/or treatment of at least one viral disease. It is characterized by active substance(s) which inhibit(s) either at least two kinases or at least one SEK kinase of a cellular signal transmission path such that virus multiplication is inhibited.Type: ApplicationFiled: December 23, 2008Publication date: September 23, 2010Inventors: Stephan Ludwig, Oliver Planz, Hans-Harald Sedlacek, Stephan Pleschka
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Publication number: 20100222298Abstract: The invention relates to novel spill resistant formulations comprising either a weak base or a weak acid as the pharmaceutical ingredient, a liquid base, a clay and a water soluble cellulose ether. The clay and cellulose ether allow for a broader pH range into which the pharmaceutically active agent may be dispersed or dissolved, and therefore allows for easier preparation and formulation of the pharmaceutical composition.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Applicant: Taro Pharmaceuticals U.S.A., Inc.Inventors: Satish ASOTRA, Xiaoli WANG, Zoltan BODOR
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Publication number: 20100222289Abstract: Methods for diagnosing and treating chronic fatigue syndrome in a patient comprise, for example, testing tissue of the patient for the presence of nucleic acid molecules of one or more CFS-causing herpesviruses and one or more non-herpesvirus infectious agents, and diagnosing the patient's CFS as (a) caused by one or more herpesvirus and no non-herpesvirus infectious agent; (b) caused by one or more herpesviruses and at least one non-herpesvirus infectious agent; (c) not caused by a herpesvirus and caused by at least one non-herpesvirus infectious agent; and (d) not caused by a herpesvirus and not caused by at least one non-herpesvirus infectious agent. In some embodiments, the methods of treating comprise administering a therapeutically effective amount of at least one pharmaceutical composition for each herpesvirus and/or non-herpesvirus infectious agent present found in the patient.Type: ApplicationFiled: October 22, 2008Publication date: September 2, 2010Applicant: CFS Research LLCInventor: Albert Martin Lerner
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Publication number: 20100216822Abstract: (R)-9-[2-bis[pivaloyloxymeihoxy]phosphinoylmethoxypropyl]adenine (being abbreviated bis-POMPMPA, TD), the derivative and the use thereof. Also including the synthetic process of TD and the procedure for manufacturing solid TD, as well as the composition containing TD and the procedure for manufacturing the composition.Type: ApplicationFiled: June 9, 2006Publication date: August 26, 2010Applicants: BRIGHTGENE BIO-MEDICAL TECHNOLOGY CO., LTD., JIANGSU CHIA TAI TIANQING PHARMACEUTICAL CO., LTD.Inventor: Jiandong Yuan
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Publication number: 20100204162Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.Type: ApplicationFiled: June 26, 2008Publication date: August 12, 2010Inventors: Mary Frances Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
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Patent number: 7772207Abstract: A first aspect of the invention relates to a combination comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.Type: GrantFiled: December 3, 2004Date of Patent: August 10, 2010Assignee: Cyclacel LimitedInventors: Simon Richard Green, Roger Neil Sleigh
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Publication number: 20100190788Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims. In particular, the present invention relates to more specifically ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.Type: ApplicationFiled: July 11, 2006Publication date: July 29, 2010Inventors: Olivier Defert, Philippe Van Rompaey, Petra Blom, Dirk Leysen, Gert De Wilde, Thomas Brown
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Publication number: 20100190806Abstract: The invention relates to substituted 6-anilinopurine derivatives of the general formula I, wherein R denotes one to five substituents independently selected from the group consisting of hydrogen, halogen, hydroxyl, amino, alkyloxy and alkyl group, and R2 denotes amino, halogen, nitro, thio, alkylthio or alkyl group for use as inhibitors of cytokinin oxidase/dehydrogenase. The invention also relates to the compositions containing these derivatives.Type: ApplicationFiled: July 2, 2008Publication date: July 29, 2010Inventors: Lukas Spichal, Marketa Gemrotova, Marek Zatloukal, Jitka Frebortova, Petr Galuszka, Tomas Werner, Thomas Schmulling, Karel Dolezal, Miroslav Strnad
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Publication number: 20100190787Abstract: The invention relates to compounds of Formula (I), a prodrug, a polymorph, a tautomer, an enantiomer, a stereoisomer, a solvate, an N-oxide, or a pharmaceutically acceptable salt thereof: (formula should be inserted here) which have inhibitory effect on one or more protein kinases that are involved in cell mitosis.Type: ApplicationFiled: January 30, 2008Publication date: July 29, 2010Inventors: Srinivas Rao Kasibhatla, Kevin Hong, Lin Zhang, Marcus F. Boehm, Junhua Fan, Jean-Yves LeBrazidec
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Publication number: 20100183564Abstract: The present invention relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. The invention further relates to a cell population comprising expanded hematopoietic stem cells (HSCs) and its use in autologous or allogeneic transplantation for the treatment of patients with inherited immunodeficient and autoimmune diseases and diverse hematopoietic disorders to reconstitute the hematopoietic cell lineages and immune system defense.Type: ApplicationFiled: October 29, 2009Publication date: July 22, 2010Applicant: IRM LLCInventors: Anthony E. Boitano, Michael Cooke, Shifeng Pan, Peter G. Schultz, John Tellew, Yongqin Wan, Xing Wang
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Patent number: 7759342Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: GrantFiled: February 15, 2007Date of Patent: July 20, 2010Assignee: Signal Pharmaceuticals, LLCInventors: Brydon L. Bennett, Kate Blease, Brian Edwin Cathers
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Publication number: 20100178340Abstract: Disclosed are compressed tablets containing atazanavir sulfate, optionally with another active agents, e.g., anti-HIV agents, granules that contain atazanavir sulfate and an intragranular lubricant that can be used to make the tablets, compositions comprising a plurality of the granules, processes for making the granules and tablets, and methods of treating HIV.Type: ApplicationFiled: June 20, 2008Publication date: July 15, 2010Inventors: Otilia May Koo, Faranak Nikfar, Steven Diaz