The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
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Patent number: 7910561Abstract: The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.Type: GrantFiled: December 9, 2005Date of Patent: March 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Jeannie M. Arruda, Brian T. Campbell, Nicholas D. P. Cosford, Jacob M. Hoffman, Essa H. Hu, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Tony Siu, Brian A. Stearns, Lida R. Tehrani, Mark T. Bilodeau, Peter J. Manley
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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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: 20110046165Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: January 5, 2009Publication date: February 24, 2011Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Katrina Chan, Christian Rommel, Liansheng Li
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Patent number: 7888343Abstract: The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds and methods for the treatment of metabolic disorders such as type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerosis diseases and the like through the administration of said compositions.Type: GrantFiled: January 18, 2007Date of Patent: February 15, 2011Assignee: Sanofi-A Ventis Deutschland GmbHInventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Lothar Schwink, Holger Wagner, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7884109Abstract: The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 11, 2007Date of Patent: February 8, 2011Assignee: Wyeth LLCInventors: Michael J. Ohlmeyer, Adolph C. Bohnstedt, Celia Kingsbury, Koc-Kan Ho, Jorge Gabriel Quintero, Ming You, Haengsoon Park, Yingchun Lu
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Patent number: 7884110Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases and as controls in assays for the identification of CCR2 antagonists.Type: GrantFiled: July 11, 2008Date of Patent: February 8, 2011Assignee: ChemoCentryx, Inc.Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
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Patent number: 7884100Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: June 12, 2007Date of Patent: February 8, 2011Assignee: PGxHealth, LLCInventors: Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
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Patent number: 7879864Abstract: Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed which are inhibitors of the enzyme dipeptidyl peptidase IV (DDP-IV) and comprise novel substituted bicyclic 8-pyrrolidinoxanthines of formula I and their derivatives: wherein the various R-groups are defined herein. These compounds may be combined with other secondary active compounds which also are effective in the treatment of said disorders and the disease states or physiological manifestations arising therefrom.Type: GrantFiled: February 13, 2007Date of Patent: February 1, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Karl Schoenafinger, Gerhard Jaehne, Elisabeth Defossa, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 7875608Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines like the compound shown in the following formula: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 17, 2008Date of Patent: January 25, 2011Inventors: Robert D. Thompson, Guoquan Wang, Anthony Beauglehole, Frank Schmidtmann
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Publication number: 20100331306Abstract: 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.Type: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Applicant: AMGEN INC.Inventors: Minna Bui, Yi Chen, Timothy D. Cushing, Jason A. Duquette, Benjamín Fisher, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Michael G. Johnson, Brian Lucas
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Publication number: 20100324062Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Aurora-A, Axl, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKK?, IR, JNK2?2, Lck, Met, MKK6, MST2, p70S6K, PDGFR?, PKA, PKD2, ROCK-II, Ros, Rsk1, SAPK2?, SAPK2?, SAPK3, SAPK4, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: October 20, 2006Publication date: December 23, 2010Applicant: IRM LLCInventors: Advait Nagle, Nathanael S. Gray
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Publication number: 20100324043Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: ApplicationFiled: June 16, 2010Publication date: December 23, 2010Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20100324047Abstract: The present invention comprises a new class of compounds capable of modulating the activity of Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula (I) wherein each of A1, A2, A3, A4, A5, A6, A7, A8, A9, bond B, X, rings Z1 and Z2, R1 and R3 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: June 5, 2008Publication date: December 23, 2010Applicant: AMGEN INC.Inventors: Adrian L. Smith, Elizabeth M. Doherty, Qi Huang, Gang Liu
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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: 20100311721Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 4, 2008Publication date: December 9, 2010Applicant: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
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Patent number: 7838529Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted by R10 and R11 and R2 to R4 and R10 and R1l are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type II diabetes mellitus and obesity using these compounds.Type: GrantFiled: January 16, 2009Date of Patent: November 23, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz
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Publication number: 20100292255Abstract: The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders, such as cancer.Type: ApplicationFiled: May 14, 2010Publication date: November 18, 2010Applicant: Myriad Pharmaceuticals, Inc.Inventors: Ashok C. Bajji, Se-Ho Kim, Rajendra Tangallapally, Benjamin J. Markovitz, Richard Trovato, Mark B. Anderson, Daniel A. Wettstein, Mark D. Shenderovich
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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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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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Publication number: 20100273764Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.Type: ApplicationFiled: April 27, 2010Publication date: October 28, 2010Applicant: Amgen Inc.Inventors: Kristin Andrews, Yunxin Y. Bo, Shon Booker, Victor J. Cee, Noel D'Angelo, Bradley J. Herberich, Fang-Tsao Hong, Claire L.M. Jackson, Brian A. Lanman, Hongyu Liao, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Liping H. Pettus, Anthony B. Reed, Adrian L. Smith, Seifu Tadesse, Nuria A. Tamayo, Bin Wu, Ryan Wurz, Kevin Yang
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Publication number: 20100273780Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: ApplicationFiled: April 19, 2010Publication date: October 28, 2010Applicant: PGXHEALTH, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20100267698Abstract: This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.Type: ApplicationFiled: January 5, 2010Publication date: October 21, 2010Inventors: Guiying Li, Pamela Albaugh, Kevin S. Currie, Guolin Cai, Linda M. Gustavson, Kyungae Lee, Alan Hutchison, George D. Maynard, Jun Yuan, Ling Hong Xie, Manuka Ghosh, Nian Liu, George P. Luke, Scott Mitchell, Martin Patrick Allen, Spiros Liras
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Publication number: 20100249122Abstract: The present invention provides compositions and methods of use thereof to prevent and/or treat pathogenic infection. In particular, the present invention provides the use of kinase inhibitors to inhibit kinases that involve in pathogen-host cell interactions that are associated with or cause pathogenic infections, therefore, to effectively prevent and/or treat pathogenic infections with far less likely to engender resistance as compared to conventional antibiotics and anti-viral drugs. The present invention further provides the use of kinase inhibitors for the treatment of acute pathogenic infections for a short period of time to avoid toxicities that may caused by long term use of these kinase inhibitors.Type: ApplicationFiled: September 5, 2007Publication date: September 30, 2010Applicant: Emory UniversityInventor: Daniel Kalman
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Publication number: 20100249115Abstract: 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: ApplicationFiled: March 31, 2010Publication date: September 30, 2010Applicant: Arqule, Inc.Inventors: Robert Nicewonger, Audra Dalton, Chris Brassard, Mark A. Ashwell, Rocio Palma
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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: 20100240623Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.Type: ApplicationFiled: July 3, 2007Publication date: September 23, 2010Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
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Publication number: 20100240680Abstract: Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: July 11, 2007Publication date: September 23, 2010Inventors: Robin Alec Fairhurst, Roger John Taylor
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Publication number: 20100210598Abstract: Provided herein are small molecule conjugates that are agonists or antagonists of one or more toll-like receptors.Type: ApplicationFiled: February 11, 2010Publication date: August 19, 2010Applicant: Regents of the University of California, San DiegoInventors: Dennis A. Carson, Howard B. Cottam, Tomoko Hayashi, Michael Chan
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Publication number: 20100204249Abstract: Niacin drugs are frequently utilized as a therapeutic to treat CVD, increase HDL levels, and/or decrease TG levels. As disclosed herein, it has been found that administration of one or more sPLA2 inhibitors in combination with one or more niacin drugs unexpectedly results in a synergistic increase in HDL levels and a synergistic decrease in TG levels. Therefore, compositions, methods, and kits are provided for treating CVD, increasing HDL levels, decreasing TG levels, and improving HDL/LDL ratios.Type: ApplicationFiled: January 8, 2010Publication date: August 12, 2010Inventors: Colin HISLOP, Joaquim Trias, Debra Odink, Bernadine Fraser, Scott Chadwick
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Publication number: 20100204250Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: April 27, 2010Publication date: August 12, 2010Applicant: Boehringer Ingelheim Pharma & Co. KGInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
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Publication number: 20100204187Abstract: Purine derivatives of Formula (I), wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK3 kinase inhibitors.Type: ApplicationFiled: January 23, 2008Publication date: August 12, 2010Inventors: Jorge Salas Solana, Carmen Almansa Rosales, Robert Soliva Soliva, Montserrat Fontes Ustrell, Marina Virgili Bernadó, Josep Comelles Espuga, José Javier Pastor Porras
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Patent number: 7772226Abstract: The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein, T1 represents a 4- to 12-membered heterocyclic group containing one or two nitrogen atoms in the ring, which is a monocyclic or bicyclic structure that may have one or more substituents; X represents a C1-6 alkyl group which may have one or more substituents, or such; Z1 and Z2 each independently represent a nitrogen atom or a group represented by the formula —CR2—; R1 and R2 independently represent a hydrogen atom, a C1-6 alkyl group which may have one or more substituents, or a C1-6 alkoxy group which may have one or more substituents, or such. These are novel compounds that exhibit an excellent DPPIV-inhibiting activity.Type: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Seiji Yoshikawa, Eita Emori, Fumiyoshi Matsuura, Richard Clark, Hironori Ikuta, Kazunobu Kira, Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki
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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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Publication number: 20100179128Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7754728Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.Type: GrantFiled: September 26, 2003Date of Patent: July 13, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100173916Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
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Publication number: 20100168122Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficialType: ApplicationFiled: August 8, 2006Publication date: July 1, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
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Publication number: 20100144663Abstract: The present invention provides 2,6-dinitrogen-containing substituted purine compounds of formula (A) or salts or solvates thereof or the solvates of salts thereof, as well as pharmaceutical compositions containing such compounds. The compounds of the present invention have the characteristics of lower toxicity, broad anticancer spectrum, higher anticancer activity, good stability and the like. The compounds are useful for the manufacture of an antitumor medicament. The present invention also provides a process for preparing these compounds.Type: ApplicationFiled: April 17, 2008Publication date: June 10, 2010Inventors: Zhanggui Wu, Weidong Ye, Jianyong Yuan, Gang Chen
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Publication number: 20100143350Abstract: The present invention relates to combination comprising (i) an ErbB inhibitor; and (ii) a CDK inhibitor, or a pharmaceutically acceptable salt thereof, selected from: (a) roscovitine; (b) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-2-methyl-pentan-2-ol; (c) 3-{9-isopropyl-6-[(pyridin-3-ylmethyl)-amino]-9H-purin-2-ylamino}-pentan-2-ol; and (d) (2R,3S-3-(6-((4,6-dimethylpyridin-3-ylmethylamino)-9-isopropyl-9H-purin-2-ylamino)pentan-2-ol. Further aspects of the invention relate to pharmaceutical products and pharmaceutical compositions comprising combinations according to the invention, and methods of treatment using the same.Type: ApplicationFiled: October 5, 2009Publication date: June 10, 2010Applicant: CYCLACEL LIMITEDInventors: Simon GREEN, Sheelagh FRAME, Ian FLEMING
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Patent number: 7732455Abstract: Selective antagonists of A2B adenosine receptors like those of formula I are provided. These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 14, 2007Date of Patent: June 8, 2010Assignee: PGx Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7723340Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and 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: January 12, 2006Date of Patent: May 25, 2010Assignees: Signal Pharmaceuticals, LLC, Pharmacopeia Drug Discovery, Inc.Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
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Publication number: 20100125062Abstract: 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: ApplicationFiled: November 16, 2009Publication date: May 20, 2010Applicant: AMEN INC.Inventors: Jennifer R. Allen, Kaustav Biswas, Frank Chavez, Jr., Ning Chen, Frenel Fils Demorin, James R. Falsey, Mike Frohn, Paul Harrington, Dan Horne, Essa Hu, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Tom Nguyen, Alex Pickrell, Andreas Reichelt, Shannon Rumfelt, Rob Rzasa, Kelvin Sham, Guomin Yao
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Publication number: 20100120765Abstract: The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: ApplicationFiled: July 22, 2009Publication date: May 13, 2010Applicant: PGXHEALTH, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Publication number: 20100120798Abstract: The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R)x N * (GP1) (2) GP is a group GP2: 10 (R)r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claimsType: ApplicationFiled: December 20, 2007Publication date: May 13, 2010Applicants: ASTEX THERAPEUTICS LIMITED, CANCER RESEARCH TECHNOLOGY LIMITED, ASTRAZENECA AB, THE INSTITUTE OF CANCER RESEARCHInventors: Steven John Woodhead, Christopher Hamlett, Marinus Leendert Verdonk, Hannah Fiona Sore, David Winter Walker, Ian Collins, Kwai Ming Cheung, John Caldwell, Tatiana Faria Da Fonseca McHardy, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Gregory Richard Carr, Jeffrey James Morris
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Publication number: 20100112090Abstract: [Purpose] The present invention provides compounds useful as agents for the prevention or treatment of a sex hormone-dependent disease or the like. [Solution] The present invention provides nitrogen-containing fused ring derivatives represented by the following general formula (I) which has a GnRH antagonistic activity, prodrugs, salts, pharmaceutical compositions containing the same, medicinal uses thereof and the like. In the formula (I), rings A and B are independently aryl or heteroaryl; RA and RB are independently halogen, cyano, alkyl, alkylsulfonyl, —OW1, —SW1, —COW2, —NW3W4, —SO2NW3W4, aryl, etc.; RC is H or alkyl; E is oxygen atom, etc.; U is single bond or alkylene; and X is Y, —CO—Y, —SO2—Y, —S-(alkylene)-Y, —O-(alkylene)-Y, —SO2-(alkylene)-Y, etc.; Y is Z or amino, etc.; and Z is cycloalkyl, heterocycloalkyl, aryl, heteroaryl, etc.Type: ApplicationFiled: April 16, 2008Publication date: May 6, 2010Applicant: KISSEI PHARMACEUTICAL CO., LTDInventors: Shigeru Yonekubo, Takashi Miyagi, Kohsuke Ohno, Mikie Kambara, Nobuhiko Fushimi
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Publication number: 20100105705Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.Type: ApplicationFiled: March 27, 2008Publication date: April 29, 2010Applicant: NeuroSearch A/SInventors: Birgitte L. Eriksen, Ulrik Svane, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Publication number: 20100105652Abstract: Substituted heteroaryl nitrile salt of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.Type: ApplicationFiled: February 28, 2008Publication date: April 29, 2010Inventors: Jose Miguel Coteron-Lopez, Beatriz Diaz-Hernandez, Jose Maria Fiandor-Roman, Maria Marco-Martin
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Publication number: 20100105706Abstract: The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.Type: ApplicationFiled: October 26, 2009Publication date: April 29, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Dewan Zeng, Michael R. Blackburn, Luiz Belardinelli
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Publication number: 20100093769Abstract: The present invention relates to compounds of formula (I) wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl or cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and each R9 is other than H. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula (I), and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.Type: ApplicationFiled: October 5, 2009Publication date: April 15, 2010Applicants: CYCLACEL LIMITED, CANCER RESEARCH TECHNOLOGY LIMITEDInventors: Peter William SHELDRAKE, Butrus ATRASH, Simon GREEN, Edward MCDONALD, Sheelagh FRAME