The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
  • Patent number: 8207178
    Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: June 26, 2012
    Assignee: Ardea Biosciences, Inc.
    Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
  • Publication number: 20120157430
    Abstract: The present invention provides N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: December 19, 2011
    Publication date: June 21, 2012
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Thomas P. Maduskuie, JR., Richard B. Sparks
  • Publication number: 20120157443
    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, Julio H. Cuervo, Daniel A. Erlanson, Junfa Fan, Bing Guan, Brian T. Hopkins, Tracy J. Jenkins, Gnanasambandam Kumaravel, Alexey A. Lugovskoy, Doug Marcotte, Noel Powell, Daniel Scott, Laura Silvian, Art Taveras, Deping Wang, Min Zhong
  • Publication number: 20120149701
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.
    Type: Application
    Filed: February 23, 2012
    Publication date: June 14, 2012
    Inventors: Pingda REN, Yi LIU, Troy Edward WILSON, Liansheng LI, Katrina CHAN, Christian ROMMEL
  • Publication number: 20120142712
    Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
    Type: Application
    Filed: January 9, 2012
    Publication date: June 7, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Peter Sieger
  • Patent number: 8193182
    Abstract: Chemical entities of Formula I: 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 P13 kinase activity are described herein.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: June 5, 2012
    Assignee: Intellikine, Inc.
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • Patent number: 8193199
    Abstract: Substituted bicyclic heteroaryls having the structures: 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 Leukemi
    Type: Grant
    Filed: March 24, 2008
    Date of Patent: June 5, 2012
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Patent number: 8193200
    Abstract: The present invention relates to method for treating inflammatory bowel disease that includes administration of an effective amount of an antagonist of A2B adenosine receptors (ARs).
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: June 5, 2012
    Assignees: University of Virginia Patent Foundation, Emory University
    Inventors: Shanthi V. Sitaraman, Joel M. Linden, Guoquan Wang, Robert Douglas Thompson, Jayson M. Rieger
  • Publication number: 20120129807
    Abstract: 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 scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.
    Type: Application
    Filed: October 20, 2011
    Publication date: May 24, 2012
    Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
  • Patent number: 8183238
    Abstract: 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: Grant
    Filed: June 16, 2010
    Date of Patent: May 22, 2012
    Assignee: Pfizer Inc.
    Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
  • Publication number: 20120122776
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in paediatric patients.
    Type: Application
    Filed: January 29, 2010
    Publication date: May 17, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Eva Ulrike Graefe-Mody, Dietmar Neubacher, Thomas Rauch, Hans-Juergen Woerle
  • Publication number: 20120122840
    Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
    Type: Application
    Filed: September 23, 2011
    Publication date: May 17, 2012
    Applicant: Myrexis, Inc.
    Inventors: Dange Vijay Kumar, Ian A. McAlexander, Matthew Gregory Bursavich, Christophe Hoarau, Paul M. Slattum, David A. Gerrish, Jeffrey W. Lockman, Weston R. Judd, Michael Saunders, Daniel P. Parker, Daniel Feodore Zigar, In Chul Kim, J. Adam Willardsen, Kraig M. Yager, Mark D. Shenderovich, Brandi L. Williams, Keith D. Tardif
  • 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: 20120122858
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: January 20, 2012
    Publication date: May 17, 2012
    Applicant: Incyte Corporation
    Inventors: Wenqing Yao, Chunhong He, David M. Burns, Jincong Zhuo, Meizhong Xu, Colin Zhang, Ding-Quan Qian, Brian Metcalf
  • Publication number: 20120108614
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: May 14, 2009
    Publication date: May 3, 2012
    Inventor: Jayhong A. Chong
  • Patent number: 8163754
    Abstract: Compounds of formula I in free or salt form, wherein 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: Grant
    Filed: October 21, 2005
    Date of Patent: April 24, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Harinder Pal Singh
  • Publication number: 20120094999
    Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.
    Type: Application
    Filed: May 5, 2010
    Publication date: April 19, 2012
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
  • Publication number: 20120094972
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Application
    Filed: June 25, 2010
    Publication date: April 19, 2012
    Applicant: AMGEN INC.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Patent number: 8153628
    Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected from the group consisting of oxazoyl, isoxazoyl, thiazolyl, and isothiazoyl; and Z1 is a 5-14 member substituted or unsubstituted heteroaryl ring; which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: July 22, 2009
    Date of Patent: April 10, 2012
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Guoquan Wang, Jayson M Rieger, Robert D Thompson
  • Publication number: 20120077826
    Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n2, n3, n4, A, B, D, E, G, J, Y, R1 and R2 are defined herein.
    Type: Application
    Filed: November 30, 2011
    Publication date: March 29, 2012
    Inventors: John M. Fevig, Dean A. Wacker
  • 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
  • Patent number: 8143249
    Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists of the formula: wherein R1 and R2 are independently lower alkyl; R4 is optionally substituted phenyl; X is hydrogen or methyl; and Y is —C(O)R, in which R is optionally substituted aryl or optionally substituted heteroaryl or a pharmaceutically acceptable salt thereof, and their use in treating mammals for various disease states.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: March 27, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
  • Publication number: 20120071490
    Abstract: The present invention provides p70 S6 kinase inhibitors of the formula: pharmaceutical formulations comprising them, and methods for their use.
    Type: Application
    Filed: November 30, 2011
    Publication date: March 22, 2012
    Applicant: ELI LILLY AND COMPANY
    Inventors: Robert Dean Dally, Jianping Huang, Sajan Joseph, Timothy Alan Shepherd, Christian L. Holst
  • Publication number: 20120059000
    Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
    Type: Application
    Filed: May 20, 2011
    Publication date: March 8, 2012
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
  • Publication number: 20120040982
    Abstract: 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: Application
    Filed: October 25, 2011
    Publication date: February 16, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Patent number: 8114877
    Abstract: Compounds of formula I in free or salt form, wherein 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: Grant
    Filed: January 12, 2006
    Date of Patent: February 14, 2012
    Assignee: Novartis AG
    Inventors: Robin A Fairhurst, Roger J Taylor
  • Publication number: 20120035193
    Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Application
    Filed: October 13, 2011
    Publication date: February 9, 2012
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Publication number: 20120035192
    Abstract: The present invention provides compounds of formulae Ia and Ib: wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.
    Type: Application
    Filed: July 25, 2011
    Publication date: February 9, 2012
    Inventors: Anthony BEAUGLEHOLE, Jayson M. RIEGER, Robert D. THOMPSON
  • Publication number: 20120035158
    Abstract: 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: Application
    Filed: October 25, 2011
    Publication date: February 9, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Patent number: 8106060
    Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
    Type: Grant
    Filed: July 30, 2006
    Date of Patent: January 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Peter Sieger
  • Publication number: 20120004212
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 5, 2012
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120004247
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 5, 2012
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20110319433
    Abstract: 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: Application
    Filed: December 22, 2010
    Publication date: December 29, 2011
    Inventors: Antoni Krasinski, Sreenivas Punna, Solomon Ungashe, Qiang Wang, Yibin Zeng
  • Publication number: 20110312979
    Abstract: The present invention provides fused pyrrole derivatives of Formula I: wherein V, W, X, Y, L, Q, Ar, Z, R1 and R6 are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: June 21, 2011
    Publication date: December 22, 2011
    Inventors: Yun-Long Li, Andrew P. Combs
  • Patent number: 8071565
    Abstract: 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: Grant
    Filed: July 11, 2007
    Date of Patent: December 6, 2011
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Publication number: 20110294803
    Abstract: Methods for treating CNS disorders such as schizophrenia, psychosis and cognitive disorders using specific inhibitors of phosphatidylinositol-3-kinase p110 delta (PIK3CD) expression and/or activity are described. Methods of determining risk of CNS disorders and methods of determining treatment response are also described. An integrative systems biology approach to identify a signaling mechanism and genetic network associated with schizophrenia and with schizophrenia-associated risk variation in ErbB4. A risk pathway associated with ErbB4 genetic variation involving increased expression of a PI3K-linked ErbB4 receptor CYT-1 and a specific PI3K enzyme, PIK3CD has been identified.
    Type: Application
    Filed: December 4, 2009
    Publication date: December 1, 2011
    Inventors: Amanda J. Law, Daniel R. Weinberger
  • Patent number: 8067426
    Abstract: Compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Grant
    Filed: August 7, 2009
    Date of Patent: November 29, 2011
    Assignee: GlaxoSmithKline LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Patent number: 8067411
    Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: November 29, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Tobias Mochel, Stephen Thom
  • Publication number: 20110281884
    Abstract: The present invention provides fused derivatives that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Application
    Filed: April 13, 2011
    Publication date: November 17, 2011
    Inventors: Andrew P. Combs, Richard B. Sparks, Eddy W. Yue
  • Patent number: 8058281
    Abstract: The present invention is directed to a method of treating systemic lupus erythematosus comprising administering a compound of formula (I) wherein R1 is selected from the group consisting of CF3, a C1-C5 alkyl, and (CH2)nR4, wherein n is between 0 and 4; R2 is selected from the group consisting of (CH2)mR4 and (CH2)mAr, wherein m is between 0 and 5; R3 is selected from the group consisting of hydrogen and methyl; R4 is selected from the group consisting of phenyl, OH, a C1-C3 alkoxy, a C1-C3 dialkylamino, piperidino, and N-methylpiperazino; Ar represents ?wherein X is selected from the group consisting of F, C1, a C1-C3 alkoxy, and CF3. The compounds can be used in combination with a second compound used in the treatment of systemic lupus erythematosus.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: November 15, 2011
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Claire Renée Jeanne Lugnier, Sylviane Paule Ghislaine Muller, Fanny Sylvie Michèle Monneaux, Jean-Jaques Bourguignon
  • Publication number: 20110275561
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients with insufficient glycemic control despite a therapy with an oral and/or a non-oral antidiabetic drug.
    Type: Application
    Filed: October 15, 2009
    Publication date: November 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Eva Ulrike Graefe-Mody, Thomas Klein, Michael Mark, Hans-Juergen Woerle
  • Publication number: 20110263493
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.
    Type: Application
    Filed: August 5, 2009
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Patent number: 8044056
    Abstract: A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrogen-containing heterocycle containing 1 to 2 hetero atom(s) selected from 1 to 2 nitrogen(s), 0 to 1 oxygen and 0 to 1 sulfur, etc., A2 is substituted or unsubstituted 6- to 10-membered aryl, etc., L1 and L2 are independently a straight chain or branched chain alkylene, etc.], or a pharmaceutically acceptable salt thereof, which is useful as a medicament.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: October 25, 2011
    Assignees: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca Aktiebolag
    Inventors: Yoshiaki Isobe, Tomoaki Nakamura
  • Publication number: 20110251172
    Abstract: The invention encompasses purine derivatives as gamma secretase modulators, useful for treating diseases associated with the deposition of beta-amyloid peptide in the brain, such as Alzheimer's disease, or of preventing or delaying the onset of dementia associated with such diseases. Pharmaceutical compositions and methods of use are included.
    Type: Application
    Filed: July 31, 2009
    Publication date: October 13, 2011
    Inventors: Alexey A. Rivkin, Sean P. Ahearn, Stephanie M. Chichetti, Christohpher L. Hamblett, Yudith Garcia, Michelle Martinez, Benito Munoz
  • Publication number: 20110236348
    Abstract: The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Application
    Filed: June 3, 2011
    Publication date: September 29, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • Publication number: 20110237532
    Abstract: The present invention provides a pharmaceutical composition comprising 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine or a pharmaceutically acceptable form thereof as pharmaceutically active compound for the therapy of a metabolic disorder or metabolic disease of a predominantly carnivorous non-human animal. It is especially useful for the therapy of diabetes and related diseases of predominantly carnivorous mammals like cats or dogs. The invention further provides respective uses of such compositions and of 1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[3-(R)-amino-piperidin-1-yl]-xanthine or pharmaceutically acceptable forms thereof.
    Type: Application
    Filed: March 25, 2011
    Publication date: September 29, 2011
    Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBH
    Inventors: Frerich DE VRIES, Dirk HOERSTERMANN, Ingo LANG, Michael MARK, Randolph SEIDLER, Leo THOMAS
  • Patent number: 8026244
    Abstract: There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: September 27, 2011
    Assignee: AstraZeneca AB
    Inventors: Anna-Karin Tiden, Jenny Viklund
  • Publication number: 20110230479
    Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
    Type: Application
    Filed: October 22, 2010
    Publication date: September 22, 2011
    Inventors: Frank M. Longo, Stephen M. Massa
  • Publication number: 20110230480
    Abstract: Compounds of the formula are disclosed as Mnk2 inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.
    Type: Application
    Filed: May 27, 2011
    Publication date: September 22, 2011
    Inventors: Andrew G. Cole, Marc-Raleigh Brescia, Joan J. Zhang, Zahid Hussain, David J. Diller, Axel Metzger, Gulzar Ahmed, Ian Henderson
  • Publication number: 20110229500
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Application
    Filed: August 7, 2009
    Publication date: September 22, 2011
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi