Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 544/277)
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Patent number: 8362244Abstract: The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.Type: GrantFiled: July 25, 2007Date of Patent: January 29, 2013Assignee: Ajinomoto Co., Inc.Inventors: Satoji Takahashi, Mitsuhiko Kojima, Shouichi Kondou, Tatsuya Ishikawa, Yoshinori Ogawa
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Patent number: 8362024Abstract: This invention relates to novel purinyl derivatives of formula Ia or Ib Wherein the symbols are as defined in the Specification and of pharmaceutically acceptable salts thereof useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.Type: GrantFiled: March 27, 2008Date of Patent: January 29, 2013Assignee: NeuroSearch A/SInventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Publication number: 20130012526Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 18, 2011Publication date: January 10, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
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Publication number: 20130012515Abstract: A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: November 11, 2010Publication date: January 10, 2013Applicant: UCB PHARMA S.A.Inventors: Gilles Raphy, Roland Bürli, Alan Findlay Haughan
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Publication number: 20130005677Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.Type: ApplicationFiled: November 16, 2010Publication date: January 3, 2013Applicant: University of Georgia Research Foundation, Inc.Inventors: Chung K. Chu, Jianing Wang
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Publication number: 20130005687Abstract: 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: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
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Patent number: 8343961Abstract: The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2010Date of Patent: January 1, 2013Assignee: ArQule, Inc.Inventors: Robert Nicewonger, Audra Dalton, Chris Brassard, Mark A. Ashwell, Rocio Palma
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Publication number: 20120329809Abstract: A compound of the formula (I) and pharmaceutical compositions for the treatment of pain.Type: ApplicationFiled: March 30, 2011Publication date: December 27, 2012Applicant: ELI LILLY AND COMPANYInventor: Sean Patrick Hollinshead
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NOVEL HYDRAZONE DERIVATIVES HAVING POTENT ANTITUMOR ACTIVITY TOWARD MULTI-DRUG RESISTANT TUMOR CELLS
Publication number: 20120329747Abstract: 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: ApplicationFiled: June 21, 2012Publication date: December 27, 2012Inventors: Hiremagular N. JAYARAM, Praveen KUSUMANCHI, Mario GRIFANTINI, Palmarisa FRANCHETTI, Loredana CAPPELLACCI, Riccardo PETRELLI -
Publication number: 20120330009Abstract: 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: ApplicationFiled: July 16, 2012Publication date: December 27, 2012Inventors: 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
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Publication number: 20120329776Abstract: 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: ApplicationFiled: November 4, 2011Publication date: December 27, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
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Patent number: 8338593Abstract: 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: GrantFiled: July 6, 2007Date of Patent: December 25, 2012Assignee: Gilead Sciences, Inc.Inventors: Lee S. Chong, Manoj C. Desai, Brian Gallagher, Michael Graupe, Randall L. Halcomb, Hong Yang, Jennifer R. Zhang
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Publication number: 20120322815Abstract: 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: ApplicationFiled: December 16, 2010Publication date: December 20, 2012Applicant: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATIONInventors: Lak Shin Jeong, Sang Kook Lee, Hwa Jin Chung, Hyuk Woo Lee
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Publication number: 20120316124Abstract: 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: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20120316185Abstract: There are described cyclohexyl amide derivatives useful as corticotropin releasing factor (CRF) receptor antagonists Formula (I).Type: ApplicationFiled: January 31, 2011Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: David Beattie, Ian Bruce, Anny-Odile Colson, Andrew James Culshaw, Thomas Sharp
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Patent number: 8329926Abstract: 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: GrantFiled: July 27, 2005Date of Patent: December 11, 2012Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
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Patent number: 8318750Abstract: 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: GrantFiled: August 26, 2011Date of Patent: November 27, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Patent number: 8318700Abstract: 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: GrantFiled: January 18, 2012Date of Patent: November 27, 2012Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle
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Patent number: 8318718Abstract: 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: GrantFiled: November 16, 2009Date of Patent: November 27, 2012Assignee: 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
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Publication number: 20120295283Abstract: 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: ApplicationFiled: May 18, 2012Publication date: November 22, 2012Applicants: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, CAYMAN CHEMICAL COMPANY, INCORPORATEDInventors: 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
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Publication number: 20120295915Abstract: 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: ApplicationFiled: November 22, 2010Publication date: November 22, 2012Inventors: Amita M. Chaudhari, Jason Hallman, Christopher P. Laudeman, David Lee Musso, Cynthia A. Parrish
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Publication number: 20120289496Abstract: 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: ApplicationFiled: May 4, 2012Publication date: November 15, 2012Applicant: Rhizen Pharmaceuticals SAInventors: Dhanapalan NAGARATHNAM, Swaroop Kumar V.S. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
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Patent number: 8309555Abstract: 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: GrantFiled: September 21, 2009Date of Patent: November 13, 2012Assignee: The Scripps Research InstituteInventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
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Publication number: 20120270842Abstract: 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: ApplicationFiled: April 27, 2012Publication date: October 25, 2012Applicant: 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
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Patent number: 8293682Abstract: 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: GrantFiled: October 15, 2009Date of Patent: October 23, 2012Assignees: Rikengreen Co., Ltd., Kumiai Chemical Industry Co., Ltd.Inventor: Shinichi Iori
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Publication number: 20120264769Abstract: 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: ApplicationFiled: December 2, 2010Publication date: October 18, 2012Applicant: The United States of Americia, as represented by the Secretary, Department of Health and Human ServInventors: Kenneth A. Jacobson, Dilip K. Tosh
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Patent number: 8288397Abstract: 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: GrantFiled: December 16, 2008Date of Patent: October 16, 2012Assignee: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
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Publication number: 20120258927Abstract: 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: ApplicationFiled: June 19, 2012Publication date: October 11, 2012Applicant: Millenium Pharmaceuticals, Inc.Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
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Publication number: 20120258950Abstract: 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: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: PFIZER LIMITEDInventors: Mark David Andrews, Sharanjeet Kaur Bagal, Karl Richard Gibson, Kiyoyuki Omoto, Thomas Ryckmans, Sarah Elizabeth Skerratt, Paul Anthony Stupple
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Publication number: 20120252823Abstract: 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: ApplicationFiled: May 24, 2012Publication date: October 4, 2012Applicants: ServicesInventors: Kenneth A. Jacobson, Dilip K. Tosh
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Publication number: 20120245169Abstract: 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: ApplicationFiled: January 13, 2012Publication date: September 27, 2012Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Publication number: 20120244211Abstract: 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: ApplicationFiled: April 13, 2012Publication date: September 27, 2012Applicant: ASYMMETRIC THERAPEUTICS, LLCInventor: John P. Ford
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Publication number: 20120238566Abstract: 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: ApplicationFiled: April 27, 2010Publication date: September 20, 2012Inventors: Chengyu Jiang, Shuan Rao, Haolin Liu, Feng Guo, Hongliang Wang, Yang Sun, Chenggang Li
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Patent number: 8268838Abstract: 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: GrantFiled: September 22, 2009Date of Patent: September 18, 2012Assignee: Neurosearch A/SInventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
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Publication number: 20120232090Abstract: 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: ApplicationFiled: November 5, 2010Publication date: September 13, 2012Applicant: GREEN CROSS CORPORATIONInventors: 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
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Patent number: 8258141Abstract: 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: GrantFiled: April 19, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
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Publication number: 20120220586Abstract: 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 LymphoType: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Applicant: 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
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Publication number: 20120220585Abstract: 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 LymphoType: ApplicationFiled: May 10, 2012Publication date: August 30, 2012Applicant: 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
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Patent number: 8252791Abstract: 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: GrantFiled: August 13, 2009Date of Patent: August 28, 2012Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
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Patent number: 8252798Abstract: A compound of the formula: and pharmaceutical compositions for the treatment of pain.Type: GrantFiled: December 9, 2009Date of Patent: August 28, 2012Assignee: Eli Lilly and CompanyInventors: Peter Charles Astles, Rossella Guidetti, Sean Patrick Hollinshead, Michael Wade Tidwell
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Publication number: 20120214815Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 23, 2012Applicant: UCB Pharma, S.A.Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
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Patent number: 8247549Abstract: 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: GrantFiled: November 6, 2008Date of Patent: August 21, 2012Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jianping Zuo, Yangming Zhang, Min Gu, Wei Tang
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Publication number: 20120208806Abstract: The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.Type: ApplicationFiled: October 7, 2010Publication date: August 16, 2012Applicant: SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Gabriela Chiosis, Tony Taldone, Weilin Sun
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Publication number: 20120202287Abstract: 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: ApplicationFiled: January 7, 2010Publication date: August 9, 2012Inventors: David Roger Adams, Peter Burton, Miles Douglas Houslay, Graeme Milligan, Joanne Mountford
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Publication number: 20120202785Abstract: 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: ApplicationFiled: February 8, 2012Publication date: August 9, 2012Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
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Publication number: 20120196845Abstract: 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: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Publication number: 20120196866Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: UCB PHARMA, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
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Publication number: 20120190679Abstract: 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: ApplicationFiled: December 13, 2011Publication date: July 26, 2012Applicant: ASTRAZENECA ABInventors: Paul David Johnson, Andrew Leach, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris
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Publication number: 20120190697Abstract: 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; substitutedType: ApplicationFiled: March 2, 2012Publication date: July 26, 2012Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
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Publication number: 20120184568Abstract: 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: ApplicationFiled: January 10, 2012Publication date: July 19, 2012Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp