Additional Hetero Ring Which Is Unsaturated And Is Not One Of The Cyclos Of A Purine Ring System Patents (Class 544/269)
  • Patent number: 9221821
    Abstract: Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: December 29, 2015
    Assignee: Forest Laboratories Holdings, Limited
    Inventors: Nhut Diep, Yuriy B. Kalyan
  • Publication number: 20150133475
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of periodontitis and rheumatoid arthritis may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.
    Type: Application
    Filed: May 13, 2013
    Publication date: May 14, 2015
    Inventor: Mahesh Kandula
  • Publication number: 20150087660
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of chronic diseases and inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.
    Type: Application
    Filed: February 27, 2013
    Publication date: March 26, 2015
    Inventor: Mahesh KANDULA
  • Patent number: 8969364
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: March 3, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, Scott T. Harrison, James C. Barrow, Zhijian Zhao, Jeffrey Melamed, Nathan R. Kett, Amy Zartman
  • Publication number: 20150025089
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 22, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
  • Publication number: 20150018321
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: September 25, 2014
    Publication date: January 15, 2015
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio DELCANALE, Elisabetta ARMANI, Gabriele AMARI
  • Patent number: 8883805
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
  • Publication number: 20140275528
    Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventors: Bertrand L. Chenard, Randall J. Gallaschun, Spencer David Kimball
  • Patent number: 8759361
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: June 24, 2014
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Publication number: 20140135301
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: January 22, 2014
    Publication date: May 15, 2014
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Patent number: 8697868
    Abstract: Disclosed are substituted xanthines of the formula wherein R is defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: April 15, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
  • Publication number: 20140057901
    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: February 21, 2013
    Publication date: February 27, 2014
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Patent number: 8637530
    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: January 9, 2012
    Date of Patent: January 28, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Peter Sieger
  • Publication number: 20130324724
    Abstract: Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
    Type: Application
    Filed: May 31, 2013
    Publication date: December 5, 2013
    Inventors: Nhut Diep, Yuriy B. Kalyan
  • Patent number: 8552019
    Abstract: The instant invention provides for compounds of formula A that inhibit PDK1 activity: The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting PDK1 activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: November 24, 2009
    Date of Patent: October 8, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin A. Keenan, Alan B. Northrup
  • Publication number: 20130178485
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines.
    Type: Application
    Filed: March 1, 2013
    Publication date: July 11, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Waldemar PFRENGLE, Thorsten PACHUR, Thomas NICOLA, Adil DURAN
  • Publication number: 20130165428
    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: February 21, 2013
    Publication date: June 27, 2013
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20130137648
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: January 23, 2013
    Publication date: May 30, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Publication number: 20130102576
    Abstract: Compounds, pyridine N-oxides, and pharmaceutically acceptable salts of formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and for preventing and/or treating diseases of the respiratory tract characterized by airway obstruction, such as asthma or COPD.
    Type: Application
    Filed: October 19, 2012
    Publication date: April 25, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Patent number: 8420813
    Abstract: 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. Also provided are processes for the preparation of the compounds and their intermediates such as: wherein: R2 and R21 are defined in the description.
    Type: Grant
    Filed: July 15, 2009
    Date of Patent: April 16, 2013
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Guoquan Wang, Jayson M Rieger, Robert Thompson
  • Patent number: 8362025
    Abstract: Compounds of formula (I) and compositions comprising a compound of formula (I) for treating disorders related to TRPA1 are described herein.
    Type: Grant
    Filed: December 22, 2009
    Date of Patent: January 29, 2013
    Assignee: Hydra Biosciences, Inc.
    Inventors: Howard Ng, Jianfeng Hang
  • Patent number: 8324224
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Grant
    Filed: June 27, 2011
    Date of Patent: December 4, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • Patent number: 8309543
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: May 23, 2012
    Date of Patent: November 13, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jesus E. Gonzalez, III, Andreas P. Termin, Esther Martinborough, Nicole Hilgraf
  • Publication number: 20120252783
    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: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Publication number: 20120252782
    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: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20120225812
    Abstract: The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides process of preparation of compounds of formula (I).
    Type: Application
    Filed: November 9, 2010
    Publication date: September 6, 2012
    Applicant: Advinus Therapeutics Limited
    Inventors: Vidya Ramdas, Summon Koul, Sujay Basu, Yogesh Waman, Yogesh Shejul, Dinesh Barawkar, Ventaka Poornapragnacharyulu Palle
  • Patent number: 8258142
    Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines such as the following: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: September 4, 2012
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
  • Patent number: 8252797
    Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Advinus Therapeutics Pvt. Ltd.
    Inventors: Venkata Palle, Sujay Basu, Yogesh Waman, Vidya Ramdas, Dinesh Barawkar, Meena Patel, Anil Panmand
  • Patent number: 8252798
    Abstract: A compound of the formula: and pharmaceutical compositions for the treatment of pain.
    Type: Grant
    Filed: December 9, 2009
    Date of Patent: August 28, 2012
    Assignee: Eli Lilly and Company
    Inventors: Peter Charles Astles, Rossella Guidetti, Sean Patrick Hollinshead, Michael Wade Tidwell
  • Publication number: 20120208829
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Application
    Filed: August 22, 2011
    Publication date: August 16, 2012
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Patent number: 8202861
    Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: August 9, 2004
    Date of Patent: June 19, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jesus E Gonzales, III, Andreas P Termin, Esther Martinborough, Nicole Zimmerman
  • 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: 8163479
    Abstract: The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3—CH2—X-A-R1, and L2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: April 24, 2012
    Assignee: Ecole Polytechnique Federale de Lausanne
    Inventors: Hughes Jaccard, Kai Johnsson, Maik Kindermann, India Christina Sielaff
  • 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
  • Patent number: 8143264
    Abstract: The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazol-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a pharmaceutically acceptable salt thereof, corresponding pharmaceutical formulations, combinations, preparation methods and methods or uses in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: March 27, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
  • 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
  • Patent number: 8044061
    Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 25, 2011
    Assignee: UCB Pharma GmbH
    Inventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
  • 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
  • Patent number: 8003656
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 22, 2007
    Date of Patent: August 23, 2011
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Publication number: 20110144095
    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: February 23, 2011
    Publication date: June 16, 2011
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Publication number: 20110144070
    Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.
    Type: Application
    Filed: February 22, 2011
    Publication date: June 16, 2011
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
  • Publication number: 20110144083
    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: February 23, 2011
    Publication date: June 16, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R. H. LOTZ
  • Publication number: 20110086868
    Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.
    Type: Application
    Filed: December 16, 2010
    Publication date: April 14, 2011
    Applicant: NOVA Southeastern University
    Inventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
  • Publication number: 20110082139
    Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Application
    Filed: December 14, 2010
    Publication date: April 7, 2011
    Inventors: Guoquan WANG, Robert D. Thompson, Jayson M. Rieger
  • Patent number: 7884100
    Abstract: 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: Grant
    Filed: June 12, 2007
    Date of Patent: February 8, 2011
    Assignee: PGxHealth, LLC
    Inventors: Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
  • Patent number: 7875608
    Abstract: 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: Grant
    Filed: December 17, 2008
    Date of Patent: January 25, 2011
    Inventors: Robert D. Thompson, Guoquan Wang, Anthony Beauglehole, Frank Schmidtmann
  • Publication number: 20100273780
    Abstract: 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: Application
    Filed: April 19, 2010
    Publication date: October 28, 2010
    Applicant: PGXHEALTH, LLC
    Inventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
  • Publication number: 20100249154
    Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.
    Type: Application
    Filed: December 22, 2009
    Publication date: September 30, 2010
    Inventors: Howard Ng, Jianfeng Hang