Nitrogen Bonded Directly To Ring Carbon Of The 1,3-diazine Ring Of The Bicyclo Ring System Patents (Class 514/264.11)
  • Publication number: 20120258975
    Abstract: Certain aspects of the invention relates to small molecule autophagy inhibitors of the formula (I), and their use for treatment and prevention of cancers and acute pancreatitis. As disclosed herein, a small molecule inhibitor of autophagy was been identified from an image-based screen in a known bioactive library. It was found that this autophagy inhibitor functions by promoting the degradation of type III PI3 kinase complex which is required for initiating autophagy. Medicinal chemistry studies led to small molecular autophagy inhibitors with improved potency and selectivity.
    Type: Application
    Filed: July 21, 2010
    Publication date: October 11, 2012
    Applicants: Shanghai Institute of Organic Chemistry, President and Fellows of Harvard College
    Inventors: Junying Yuan, Dawei Ma, Junli Liu, Lihong Zhang
  • Publication number: 20120245139
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 27, 2012
    Applicant: EXELIXIS PATENT COMPANY LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
  • Publication number: 20120245166
    Abstract: Methods for enhancing memory and/or learning and prevent neurodegeneration by administration of certain heterocyclic and aromatic compounds are described. The methods are particularly useful for treating patients suffering from a neurodegenerative disease such as (without limitation) Alzheimer's, Parkinsons's, Lou Gehrig's (ALS) disease or memory or learning impairment. A neuronal human cell-based assay that assess NF-kB gene up-regulation using a luciferase reporter is also provided that screens for compounds useful in methods for enhancing memory or learning.
    Type: Application
    Filed: October 14, 2010
    Publication date: September 27, 2012
    Applicant: Southern Research Institute
    Inventors: Maurizio Grimaldi, Judith Varady Hobrath, Subramaniam Ananthan, Joseph A. Maddry
  • Patent number: 8273755
    Abstract: The present invention is directed to novel 4-methylpyridopyrimidinone compounds of Formula (I), and to salts thereof, their synthesis, and their use as inhibitors of phosphoinositide 3-kinase alpha (PI3-K?).
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: September 25, 2012
    Assignee: Pfizer Inc
    Inventors: Hengmiao Cheng, Dilip Bhumralkar, Klaus Ruprecht Dress, Jacqui Elizabeth Hoffman, Mary Catherine Johnson, Robert Steven Kania, Phuong Thi Quy Le, Mitchell David Nambu, Mason Alan Pairish, Michael Bruno Plewe, Khanh Tuan Tran
  • Publication number: 20120238570
    Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 20, 2012
    Applicant: EXELIXIS PATENT COMPANY LLC
    Inventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
  • Publication number: 20120219550
    Abstract: A pharmaceutical combination comprising an Hsp90 inhibitor and an HER2 inhibitor, and methods of using the combination to treat proliferative disorders.
    Type: Application
    Filed: May 8, 2012
    Publication date: August 30, 2012
    Applicant: NOVARTIS AG
    Inventors: Carlos Garcia-Echeverria, Michael Rugaard Jensen
  • Patent number: 8252803
    Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: August 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Alexey A. Rivkin
  • Patent number: 8247408
    Abstract: The invention is directed to Compounds of Formula I and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Grant
    Filed: October 9, 2006
    Date of Patent: August 21, 2012
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Longcheng Wang, Bryan K. S. Yeung
  • Publication number: 20120202831
    Abstract: The invention relates to a pharmaceutical formulation including, as an active principle, the compound of formula (I) or a salt of said compound with a pharmaceutically acceptable acid.
    Type: Application
    Filed: January 30, 2012
    Publication date: August 9, 2012
    Applicant: SANOFI
    Inventors: Tsiala Benard, Jean-Pierre Burnouf
  • Publication number: 20120202832
    Abstract: The invention provides kinase inhibitors of Formula I: wherein either: (1) R1 is H, and (a) R2 is (3-chlorobenzyl)oxy- and R3 is chloro; (b) R2 and R3, together with the carbon atoms to which they are attached, form 1-(3-fluorobenzyl)-1H-pyrazole; (c) R2 is 2-pyridinylmethoxy and R3 is chloro; (d) R2 and R3 are both chloro; (e) R2 is chloro and R1 is bromo; (f) R2 and R3 are both bromo; (g) R2 is fluoro and R3 is ethynyl; (h) R2 is chloro and R3 is ethynyl; (i) R2 is bromo and R3 is ethynyl; (j) other than when R1 is in the 3-position in combination with R3, in the 4-position, R2 is bromo and R3 is fluoro; (k) R2 is 2-pyridinylmethoxy and R3 is fluoro; or (l) R2 is 2-pyridinylmethoxy and R1 is bromo; or (2) at least one of R1, R2 and R3 is selected from benzyloxy, 3-chlorobenzyloxy and 2-pyridinylmethoxy and when at least one of R1, R2 and R3 is not benzyloxy, 3-chlorobenzyloxy or 2-pyridinylmethoxy, each of the others is independently selected from H, halogen, and C2-C4 alkynyl, with the proviso tha
    Type: Application
    Filed: September 2, 2010
    Publication date: August 9, 2012
    Applicant: Auckland Uniservices Limited
    Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Guo-Liang Lu, Ho Huat Lee, Amir Ashoorzadeh, Robert Forbes Anderson, William Robert Wilson, William Alexander Denny, Huai-Ling (Annie) Hsu, Andrej Maroz, Stephen Michael Frazer Jamieson, Alexandra Marie Mowday, Kendall Marie Carlin
  • Patent number: 8236811
    Abstract: The disclosure relates to methods of treating leukaemia, in particular myeloid leukaemia, comprising administering the compound N-[2-(2,1,3-benzothiadiazol-5-ylamino)-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-N?-(1,1-dimethylethyl)-urea or a hydrate, a pharmaceutically acceptable salt or a solvate thereof.
    Type: Grant
    Filed: June 16, 2009
    Date of Patent: August 7, 2012
    Assignee: Sanofi
    Inventors: Bernard Bourrie, Pierre Casellas
  • Patent number: 8232283
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Grant
    Filed: May 12, 2011
    Date of Patent: July 31, 2012
    Assignee: Forma Therapeutics, Inc.
    Inventors: Andreas Schoop, Alexander Backes, Joachim Vogt, Lars Neumann, Jan Eickhoff, Stefan Hannus, Kerrin Hansen, Peter Amon, Igor Ivanov, Matthias Borgmann, Chase Smith, Arthur F. Kluge, Krishan Murthi, Rebecca Casaubon
  • Publication number: 20120184542
    Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 19, 2012
    Inventors: Kevin Anderson, Yi Chen, Zhi Chen, Kin-Chun Luk, Pamela Loreen Rossman, Hongmao Sun, Peter Michael Wovkulich
  • Publication number: 20120184547
    Abstract: Provided herein are PAK inhibitors. Also provided herein are compositions and methods for treating an individual suffering from schizophrenia.
    Type: Application
    Filed: July 16, 2010
    Publication date: July 19, 2012
    Applicant: aFRAXis, Inc.
    Inventors: Jay Lichter, David Campbell, Benedikt Vollrath, Sergio G. Durón
  • Publication number: 20120172321
    Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Application
    Filed: March 1, 2012
    Publication date: July 5, 2012
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Young K. Chen, Erick Co, Prasuna Guntupalli, John D. Lawson, Wolfgang Reinhard Ludwig Notz, Jeffrey A. Stafford, Huong-Thu Ton-Nu
  • Publication number: 20120165313
    Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).
    Type: Application
    Filed: March 1, 2012
    Publication date: June 28, 2012
    Applicant: Genentech, Inc.
    Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Kevin Hon Luen Lau, Coung Ly, Joseph P. Lyssikatos, Daniel Ortwine, Zhonghua Pei, Xianrui Zhao
  • Publication number: 20120157442
    Abstract: The present invention provides compounds useful as inhibitors of Btk, compositions thereof, and methods of using the same.
    Type: Application
    Filed: September 3, 2010
    Publication date: June 21, 2012
    Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.
    Inventors: Minna Bui, Patrick Conlon, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Alexey Ishchenko, Tracy J. Jenkins, Gnanasambandam Kumaravel, Doug Marcotte, Noel Powell, Daniel Scott, Art Taveras, Deping Wang, Min Zhong
  • Publication number: 20120149700
    Abstract: Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Application
    Filed: December 12, 2011
    Publication date: June 14, 2012
    Inventors: Zhi-Liang WEI, Donogh John Roger O'MAHONY, Matthew DUNCTON, John KINCAID, Michael G. KELLY, Zhan WANG
  • Publication number: 20120149684
    Abstract: The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.
    Type: Application
    Filed: October 20, 2010
    Publication date: June 14, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventors: Douglas Wade Beight, Timothy Paul Burkholder, Joshua Ryan Clayton, MariJean Eggen, Kenneth James Henry, JR., Deidre Michelle Johns, Saravanan Parthasarathy, Huaxing Pei, Mark Edward Rempala, Jason Scott Sawyer
  • Publication number: 20120136012
    Abstract: The present invention is directed to amino tetrahydro-pyridopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: August 5, 2010
    Publication date: May 31, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
  • Publication number: 20120130144
    Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.
    Type: Application
    Filed: February 4, 2010
    Publication date: May 24, 2012
    Applicant: BiPar Sciences, Inc.
    Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
  • Publication number: 20120122838
    Abstract: Compounds and pharmaceutical compositions 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 PI3 kinase activity, are described herein.
    Type: Application
    Filed: November 10, 2011
    Publication date: May 17, 2012
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20120114639
    Abstract: We describe herein compositions and methods related to inferring with microbial infection. Generally, the compositions include an infection antagonist that inhibits formation of a heparin sulfonated proteoglycan (HSPG)-containing infection complex. Generally, the methods include administering to a subject an amount of a composition as described herein effective to inhibit infection by a microorganism that that infects a host through interactions that involve HSPG.
    Type: Application
    Filed: November 4, 2011
    Publication date: May 10, 2012
    Inventors: MICHELLE ADAIR OZBUN, Zurab Surviladze
  • Publication number: 20120115870
    Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.
    Type: Application
    Filed: January 11, 2012
    Publication date: May 10, 2012
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shepard, Mark R. Hellberg, Peter G. Klimko, Abbot F. Clark
  • Publication number: 20120101115
    Abstract: The present invention provides isoquinoline, tetrahydroisoquinoline and tetrahydropyridopyrimidine compounds that induce cell death by apoptosis and uses of the compounds in medicine, especially their use for treating cancer and other diseases.
    Type: Application
    Filed: April 28, 2010
    Publication date: April 26, 2012
    Applicant: QUEEN MARY AND WESTFIELD COLLEGE
    Inventor: Finbarr Edward Cotter
  • Publication number: 20120077815
    Abstract: A series of amino-substituted fused pyridine and pyrazine derivatives, in particular amino-substituted quinoline and quinoxaline derivatives, being selective inhibitors of PI3 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: Application
    Filed: February 11, 2010
    Publication date: March 29, 2012
    Applicant: UCB PHARMA S.A.
    Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
  • Publication number: 20120077811
    Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.
    Type: Application
    Filed: March 11, 2010
    Publication date: March 29, 2012
    Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
  • Publication number: 20120065189
    Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.
    Type: Application
    Filed: May 27, 2010
    Publication date: March 15, 2012
    Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
  • Publication number: 20120053179
    Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.
    Type: Application
    Filed: November 4, 2011
    Publication date: March 1, 2012
    Inventors: Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Chunguang Wang, Hans Pluempe, Achim Feurer, Samir Bennabi
  • Publication number: 20120046270
    Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R4, X1, X2, X3, X4, X5, Q, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, as well as pharmaceutical preparations and formulations of these compounds.
    Type: Application
    Filed: February 17, 2010
    Publication date: February 23, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Peter Ettmayer, Andreas Mantoulidis, Steffen Steurer
  • Publication number: 20120046283
    Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of neuropsychiatric conditions.
    Type: Application
    Filed: December 18, 2009
    Publication date: February 23, 2012
    Applicant: AFRAXIS INC.
    Inventors: David Campbell, Sergio G. Durón, Benedikt Vollrath, Warren Wade
  • Publication number: 20120035181
    Abstract: A method of controlling proliferation of fish parasites comprising the administration of 1 to 50 mg/kg fish body weight/day of an inhibitor of folate synthesis and/or an inhibitor of folate activation to fish continuously for 1 to 2 weeks. Using a combination preparation composed of an inhibitor of folate synthesis and an inhibitor of folate activation is preferable, and a sulfonamide is preferable for the inhibitor of folate synthesis. A dihydrofolate reductase inhibitor, a folate antagonist, etc., can be used as the inhibitor of folate activation. The antiparasitic agent is able to exterminate fish parasites via oral administration. It is particularly effective against parasites belonging to the ciliate group among fish parasites.
    Type: Application
    Filed: April 26, 2010
    Publication date: February 9, 2012
    Applicant: NIPPON SUISAN KAISHA, LTD.
    Inventors: Fumi Kawano, Noritaka Hirazawa
  • Patent number: 8101622
    Abstract: The invention is directed to Compounds of Formula I: optionally as a single stereoisomer or mixture of stereoisomers thereof, and additionally optionally as a pharmaceutically acceptable salt thereof; as well as methods of making and using the compounds.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: January 24, 2012
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Sunghoon Ma, Chris A. Buhr, John M. Nuss
  • Publication number: 20110319409
    Abstract: The present invention is directed to 7-aza-quinazoline compounds of general structural formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10).
    Type: Application
    Filed: June 23, 2010
    Publication date: December 29, 2011
    Inventors: Christopher D. Cox, Izzat T. Raheem, Broc A. Flores, David B. Whitman
  • Patent number: 8076345
    Abstract: Fused heterocyclic compounds are provided according to formula 1: where R1, R2, R3, and m are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: December 13, 2011
    Assignee: Evotec AG
    Inventors: Zhi-Liang Wei, Donogh John Roger O'Mahony, Matthew Duncton, John Kincaid, Michael G. Kelly, Zhan Wang
  • Patent number: 8071766
    Abstract: The invention relates to HSP90 inhibiting compounds consisting of the formula: wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: December 6, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Young K. Chen, Erick Co, Prasuna Guntupalli, John D. Lawson, Wolfgang Reinhard Ludwig Notz, Jeffrey A. Stafford, Huong-Thu Ton-Nu
  • Publication number: 20110287069
    Abstract: A solid oral dosage pharmaceutical formulation of (R)-2-Amino-7-[4-fluoro-2-(6-methoxy-pyridin-2-yl)-phenyl]-4-methyl-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one or its salt; and a surfactant or an acid.
    Type: Application
    Filed: January 28, 2010
    Publication date: November 24, 2011
    Inventors: Daya Verma, Yue (Helen) Teng, Rajinder Singh, Dan Thompson
  • Publication number: 20110281867
    Abstract: Compositions and methods are provided for using tyrosine kinase inhibitors to treat pathogenic infection. In particular, methods for using Abl-family tyrosine kinase inhibitors to treat pathogenic infection are provided. Infections to be treated according to the present invention include, particularly, those caused by microbial pathogens such as bacteria and viruses.
    Type: Application
    Filed: December 16, 2010
    Publication date: November 17, 2011
    Inventors: Daniel KALMAN, William Gerard Bornmann, Patrick Michael Reeves, Alyson Irene Swimm
  • Patent number: 8058283
    Abstract: Objects of the present invention are the compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: November 15, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Honold, Jane Paul, Carl Roeschlaub, Wolfgang Schaefer, Stefan Scheiblich, Thomas Von Hirschheydt, Alan Whittle
  • Patent number: 8058282
    Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: November 15, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
  • Publication number: 20110269739
    Abstract: The present invention provides a new group of protein kinase inhibitors, pyrido[4,3,-d]pyrimidin-5-one derivatives, and pharmaceutically acceptable salts thereof that are useful for intreating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrido[4,3,-d]pyrimidin-5-one derivatives.
    Type: Application
    Filed: October 29, 2010
    Publication date: November 3, 2011
    Applicants: Oscotec, Inc., Genosco
    Inventors: Hong Woo Kim, Jong Sung Koh, Jaekyoo Lee, Ho-Juhn Song, Youngsam Kim, Hee Kyu Lee, Jang-Sik Choi, Sun-Hee Lim, Sunhwa Chang
  • Publication number: 20110269758
    Abstract: Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
    Type: Application
    Filed: June 29, 2009
    Publication date: November 3, 2011
    Applicant: MERCK PATENT GMBH
    Inventors: Yufang Xiao, Bayard R. Huck, Amanda E. Sutton, Xiaoling Chen, Srinivasa R. Karra, Andreas Goutopoulos
  • Publication number: 20110263561
    Abstract: Compounds of the formula (I), in which R, X, Y, Z, R3 and R4 have the meanings indicated in claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: May 13, 2009
    Publication date: October 27, 2011
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Mireille Krier, Thorsten Knoechel, Alfred Jonczyk, Frank Zenke, Holger Enderle
  • Patent number: 8044062
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Grant
    Filed: October 9, 2006
    Date of Patent: October 25, 2011
    Assignee: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K. S. Yeung
  • Publication number: 20110257207
    Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are inhibitors or kinases such as Raf, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.
    Type: Application
    Filed: May 12, 2011
    Publication date: October 20, 2011
    Applicants: Agennix USA Inc, Agennix AG
    Inventors: Alexander BACKES, Joachim VOGT, Peter AMON, Igor IVANOV, Stefan HANNUS, Matthias BORGMANN, Kerrin HANSEN, Rebecca CASAUBON, Chase SMITH, Krishna MURTHI, Arthur KLUGE, Andreas SCHOOP, Lars NEUMANN, Jan EICKHOFF
  • Patent number: 8030317
    Abstract: Compounds of the following formula are provided for use with MEK: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: October 4, 2011
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Qing Dong, Stephen W. Kaldor
  • Patent number: 8030318
    Abstract: Substituted fused bicyclic pyrimidine compounds having an amide-substituted pyridylamine group at C-4 of the pyrimidine ring are useful in the treatment of conditions associated with HCV.
    Type: Grant
    Filed: March 27, 2006
    Date of Patent: October 4, 2011
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Kenneth Alan Simmen, Dominique Louis Nestor Ghislain Surleraux, Tse-I Lin, Oliver Lenz, Pierre Jean-Marie Bernard Raboisson, Sarvajit Chakravarty, Barry Patrick Hart
  • Publication number: 20110237608
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof, as well as methods of making and using the compounds.
    Type: Application
    Filed: June 2, 2011
    Publication date: September 29, 2011
    Applicant: Exelixis, Inc.
    Inventors: Tae-Gon Baik, Chris A. Buhr, Katherine Lara, Sunghoon Ma, Morrison Mac, John M. Nuss, Longcheng Wang, Yong Wang, Bryan K.S. Yeung
  • Publication number: 20110237583
    Abstract: The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.
    Type: Application
    Filed: November 3, 2009
    Publication date: September 29, 2011
    Inventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle, Ingo Kober, Dirk Wienke, Mireille Krier
  • Publication number: 20110230444
    Abstract: A pharmaceutical combination comprising an Hsp90 inhibitor and an mTOR inhibitor, and methods of using the combination to treat or prevent proliferative disorders.
    Type: Application
    Filed: November 25, 2009
    Publication date: September 22, 2011
    Applicant: NOVARTIS AG
    Inventors: Carlos Garcia-Echeverria, Michael Rugaard Jensen