Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/277)
  • Publication number: 20120329809
    Abstract: A compound of the formula (I) and pharmaceutical compositions for the treatment of pain.
    Type: Application
    Filed: March 30, 2011
    Publication date: December 27, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventor: Sean Patrick Hollinshead
  • Publication number: 20120329776
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 27, 2012
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
  • 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
  • Publication number: 20120330009
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: July 16, 2012
    Publication date: December 27, 2012
    Inventors: Weiwen Ying, David James, Shijie Zhang, Teresa Przewloka, Junghyun Chae, Dinesh U. Chimmanamada, Chi-Wan Lee, Elena Kostik, Howard P. Ng, Kevin Foley, Zhenjian Du, James Barsoum
  • Patent number: 8338593
    Abstract: The present application provides for a compound of Formula (I) or (II): or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: December 25, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Lee S. Chong, Manoj C. Desai, Brian Gallagher, Michael Graupe, Randall L. Halcomb, Hong Yang, Jennifer R. Zhang
  • Publication number: 20120322815
    Abstract: The present invention relates to a pharmaceutical composition for preventing or treating inflammatory disease, colorectal cancer and prostate cancer, which contains an A3 adenosine receptor agonist, 2-chloro-N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-Cl-IB-MECA), N6-(3-iodobenzyl)-4?-thioadenosine-5?-N-methyluronamide (thio-IB-MECA), or a pharmaceutically acceptable salt thereof. The pharmaceutical composition of the invention is significantly less toxic than conventional A3 adenosine agonists, and thus is useful for prevention or treatment of inflammatory disease. In addition, it more selectively inhibits the growth of androgen receptor-dependent or independent prostate cancer cells than other A3 adenosine receptor agonists and thus is useful for prevention or treatment of colorectal cancer or prostate cancer.
    Type: Application
    Filed: December 16, 2010
    Publication date: December 20, 2012
    Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Lak Shin Jeong, Sang Kook Lee, Hwa Jin Chung, Hyuk Woo Lee
  • Publication number: 20120316185
    Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).
    Type: Application
    Filed: January 31, 2011
    Publication date: December 13, 2012
    Applicant: NOVARTIS AG
    Inventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
  • Publication number: 20120316124
    Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: February 17, 2011
    Publication date: December 13, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
  • Patent number: 8329926
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: December 11, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
  • Patent number: 8318750
    Abstract: 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: Grant
    Filed: August 26, 2011
    Date of Patent: November 27, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Patent number: 8318700
    Abstract: Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.
    Type: Grant
    Filed: January 18, 2012
    Date of Patent: November 27, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Patent number: 8318718
    Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: November 27, 2012
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
  • Publication number: 20120295283
    Abstract: Assay methods may generally comprise forming homogeneous assay mixtures comprising target SAM-utilizing protein, fluorescent detection analyte, and test compound, incubating, and measuring FP or TR-FRET signal emitted in order to determine a measure of test compound-SAM-utilizing protein binding. Assay mixtures comprise a SAM-utilizing protein, and a fluorescent detection analyte that binds with the SAM-utilizing protein in the absence of test compound. Assay mixtures may further comprise a test compound. Assay mixture embodiments may generate FP or TR-FRET signal properties that are a function of the inherent binding interactions of both the test compound and the detection analyte with the SAM-utilizing protein. Fluorescent detection analytes comprise a fluorophore moiety, a covalent linker moiety, and a SAM-utilizing protein ligand moiety and could be utilized in FP or TR-FRET assays to measure test compound binding.
    Type: Application
    Filed: May 18, 2012
    Publication date: November 22, 2012
    Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, CAYMAN CHEMICAL COMPANY, INCORPORATED
    Inventors: Stephen Douglas Barrett, Daniel Austin Bochar, Levi Lynn Blazer, Fred Lawrence Ciske, Gregory William Endres, Jeffrey Keith Johnson, Gregory Scott Keyes, Ranjinder Singh Sidhu, Raymond C. Trievel, Margaret Lynn Collins
  • Publication number: 20120295915
    Abstract: Disclosed are compounds having Formula (I), wherein R1, R2, R3, R4, Ra, Rb, X, Y, m, and n are defined herein and methods of using the same.
    Type: Application
    Filed: November 22, 2010
    Publication date: November 22, 2012
    Inventors: Amita M. Chaudhari, Jason Hallman, Christopher P. Laudeman, David Lee Musso, Cynthia A. Parrish
  • Publication number: 20120289496
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Application
    Filed: May 4, 2012
    Publication date: November 15, 2012
    Applicant: Rhizen Pharmaceuticals SA
    Inventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
  • Patent number: 8309555
    Abstract: The present invention provides 2,6-disubstituted purine compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional 2,6-disubstituted purine compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: November 13, 2012
    Assignee: The Scripps Research Institute
    Inventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
  • Publication number: 20120270842
    Abstract: The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.
    Type: Application
    Filed: April 27, 2012
    Publication date: October 25, 2012
    Applicant: Metabasis Therapeutics, Inc.
    Inventors: K. RAJA REDDY, Jeff Stebbins, Serge H. Boyer, Mark D. Erion, Scott J. Hecker, Nicholas Brian Raffaele, Brett C. Bookser, Venkat Reddy Mali
  • Patent number: 8293682
    Abstract: The invention provides a growth regulator for gramineous weeds, particularly those growing in turf, which comprises, as an active ingredient, cytokinin and/or an ethylene-producing substance in combination with cytokinin; and a method for regulating the growth of gramineous weeds with the relevant growth regulator more economically with ease.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: October 23, 2012
    Assignees: Rikengreen Co., Ltd., Kumiai Chemical Industry Co., Ltd.
    Inventor: Shinichi Iori
  • Publication number: 20120264769
    Abstract: Disclosed are (N)-methanocarba adenine nucleosides, e.g., of the formula (I): as A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein A, a, R2, and R3 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. Also disclosed are conjugates comprising a dendrimer and one or more ligands, which are functionalized congeners of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily. Such conjugates are have the potential of being used as dual agonists, dual antagonists, or agonist/antagonist combinations.
    Type: Application
    Filed: December 2, 2010
    Publication date: October 18, 2012
    Applicant: The United States of Americia, as represented by the Secretary, Department of Health and Human Serv
    Inventors: Kenneth A. Jacobson, Dilip K. Tosh
  • Patent number: 8288397
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: October 16, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • Publication number: 20120258950
    Abstract: The present invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine, in particular as Trk antagonists.
    Type: Application
    Filed: April 4, 2012
    Publication date: October 11, 2012
    Applicant: PFIZER LIMITED
    Inventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
  • Publication number: 20120258927
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Applicant: Millenium Pharmaceuticals, Inc.
    Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
  • Publication number: 20120252823
    Abstract: Disclosed are A3 adenosine receptor antagonists and/or partial agonists and A1 adenosine receptor agonists 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 A3 AR antagonists or partial agonists find use in treating a number of diseases such as cancer, glaucoma, and inflammatory diseases, 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. The A1 AR agonists and partial agonists find use in treating diseases such as seizures, convulsion, stroke, diabetes, pain, arrhythmias, depression, and anxiety and in cardioprotection or neuroprotection.
    Type: Application
    Filed: May 24, 2012
    Publication date: October 4, 2012
    Applicants: Services
    Inventors: Kenneth A. Jacobson, Dilip K. Tosh
  • Publication number: 20120245169
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: January 13, 2012
    Publication date: September 27, 2012
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • Publication number: 20120244211
    Abstract: A composition and method for the treatment of the side-effects associated with the administration of cancer chemotherapeutic agents involves the oral ingestion of a slow release capsule containing adenine and orotate. The administration of a protein pump inhibitor decreases systemic absorption of orotate and the administration of allopurinol decreases the formation of 2,8-dihydroxy adenine from adenine. In an alternative embodiment, cationic liposomes contain purine/pyrimidine precursors. The cationic liposomes bind to the cells lining the mucosa of the intestinal tract and then the contents of the cationic liposome are then taken up in the interior of the cells to prevent the metabolism of the cancer treatment drug 5-FU into a toxic species.
    Type: Application
    Filed: April 13, 2012
    Publication date: September 27, 2012
    Applicant: ASYMMETRIC THERAPEUTICS, LLC
    Inventor: John P. Ford
  • Publication number: 20120238566
    Abstract: Use of cell autophagy (type II cell apoptosis) inhibitors for preventing and/or treating avian influenza, injury of lungs caused by avian influenza virus or nanometer materials. The cell autophagy (type II cell apoptosis) inhibitors are selected from 3-methyladenine, SB203580, LY294002, and or wortmannin. The injury of lungs includes acute respiratory distress syndrome. The avian influenza virus is H5N1, H5N2 or H9N2 avian influenza virus. The nanometer materials include PAMAM G3, G4, G5, G5.5, G6, G7, or G8.
    Type: Application
    Filed: April 27, 2010
    Publication date: September 20, 2012
    Inventors: Chengyu Jiang, Shuan Rao, Haolin Liu, Feng Guo, Hongliang Wang, Yang Sun, Chenggang Li
  • Patent number: 8268838
    Abstract: Provided are substituted purinyl-pyrazol derivatives of the following formula (I), or a pharmaceutically acceptable salt thereof, and their use as potassium channel modulating agents, as well as pharmaceutical compositions having such derivatives that are useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels: wherein R1 represents hydrogen or alkyl; one of R2, R3 and R4 represents alkyl, hydroxy-alkyl, alkoxy-alkyl, halo, trifluoromethyl, trifluoromethoxy, hydroxy or alkoxy; and the other two of R2, R3 and R4, independently of each other, represent hydrogen, alkyl, hydroxy-alkyl, alkoxy-alkyl, halo, trifluoromethyl, trifluoromethoxy, hydroxy or alkoxy; R5 represents phenyl optionally substituted with one or more substituents selected from the group consisting of alkyl, halo, trifluoromethyl, trifluoromethoxy, alkoxy and cyano; and R6 represents R?OC(?O)—, wherein R? represents alkyl, alkoxy, alkoxy-alkyl or adamantanyl.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: September 18, 2012
    Assignee: Neurosearch A/S
    Inventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
  • Publication number: 20120232090
    Abstract: A novel arylpiperazine-containing purine derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating depressive disorders, are provided.
    Type: Application
    Filed: November 5, 2010
    Publication date: September 13, 2012
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Eun-Jung Park, Suk Youn Kang, Younggyu Kong, Junwon Lee, Hyun Jung Kim, Myung Eun Jung, Ki-Nam Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • Patent number: 8258141
    Abstract: 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: Grant
    Filed: April 19, 2007
    Date of Patent: September 4, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120220585
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho
    Type: Application
    Filed: May 10, 2012
    Publication date: August 30, 2012
    Applicant: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20120220586
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho
    Type: Application
    Filed: May 10, 2012
    Publication date: August 30, 2012
    Applicant: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Patent number: 8252798
    Abstract: A compound of the formula: and pharmaceutical compositions for the treatment of pain.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: August 28, 2012
    Assignee: Eli Lilly and Company
    Inventors: Peter Charles Astles, Rossella Guidetti, Sean Patrick Hollinshead, Michael Wade Tidwell
  • Patent number: 8252791
    Abstract: The present invention relates to purine-based cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, inflammatory disorders, hepatic disorders, and a combination thereof.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: August 28, 2012
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20120214815
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 23, 2012
    Applicant: UCB Pharma, S.A.
    Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
  • Patent number: 8247549
    Abstract: The present invention discloses a novel method for preparing and purifying 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester. The preparation started from cheap and easily available L-malic acid, which was transformed to intermediate I after simultaneous protection of the groups of 1-carboxyl and 2-hydroxyl. The intermediate I was selectively reduced to intermediate alcohol II, whose hydroxyl group was further transformed to an easily leaving group to afford intermediate III. The intermediate III was nucleophilically substituted with adenine to afford intermediate IV. The intermediate IV was deprotected and methyl-esterified simultaneously in methanol in the presence of an acid or a base to afford crude 4-(6-Amino-purin-9-yl)-2(S)-hydroxy-butyric acid methyl ester, which was purified by recrystallization to afford the purified product.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: August 21, 2012
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Min Gu, Wei Tang
  • Publication number: 20120208806
    Abstract: The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.
    Type: Application
    Filed: October 7, 2010
    Publication date: August 16, 2012
    Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Gabriela Chiosis, Tony Taldone, Weilin Sun
  • Publication number: 20120202287
    Abstract: The invention provides methods for reversibly inhibiting stem cell differentiation wherein a compound of formula (I) is contacted with a stem cell. The invention further provides a method for preparing a culture medium, a culture medium supplement and a composition comprising a compound of formula (I).
    Type: Application
    Filed: January 7, 2010
    Publication date: August 9, 2012
    Inventors: David Roger Adams, Peter Burton, Miles Douglas Houslay, Graeme Milligan, Joanne Mountford
  • Publication number: 20120202785
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 8, 2012
    Publication date: August 9, 2012
    Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
  • Publication number: 20120196845
    Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. 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 mediated by the M1 receptor.
    Type: Application
    Filed: October 1, 2010
    Publication date: August 2, 2012
    Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
  • Publication number: 20120196866
    Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 6, 2012
    Publication date: August 2, 2012
    Applicant: UCB PHARMA, S.A.
    Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
  • Publication number: 20120190697
    Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted
    Type: Application
    Filed: March 2, 2012
    Publication date: July 26, 2012
    Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20120190679
    Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
    Type: Application
    Filed: December 13, 2011
    Publication date: July 26, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Paul David Johnson, Andrew Leach, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris
  • Publication number: 20120184568
    Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: January 10, 2012
    Publication date: July 19, 2012
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Publication number: 20120184569
    Abstract: Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V): 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: Application
    Filed: February 10, 2012
    Publication date: July 19, 2012
    Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human Services
    Inventors: Kenneth A. Jacobson, Dilip K. Tosh
  • Publication number: 20120184516
    Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.
    Type: Application
    Filed: June 30, 2011
    Publication date: July 19, 2012
    Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian
  • Patent number: 8222257
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
  • Patent number: 8221737
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: July 17, 2012
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Xiaowen Peng, Lu Ying, Ce Wang, Yao-Ling Qiu
  • Publication number: 20120178716
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: December 5, 2011
    Publication date: July 12, 2012
    Applicant: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
  • Patent number: 8217050
    Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: July 10, 2012
    Assignee: Chroma Therapeutics Limited
    Inventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
  • Publication number: 20120171730
    Abstract: Methods for the synthesis of N-substituted pyridinium compounds by using an N-heteroaryl substituted pyridinium salt (Zincke salt) and reacting it with a nucleophilic amine are provided. Novel purine-substituted pyridyl compounds, which may be useful reagents in the above reaction, are also disclosed.
    Type: Application
    Filed: January 27, 2012
    Publication date: July 5, 2012
    Applicant: ROCHE DIAGNOSTICS OPERATIONS, INC.
    Inventors: Dieter Heindl, Heribert Maerz, Axel Schmidt