Nitrogen Attached Directly Or Indirectly To The Purine Ring System By Nonionc Bonding Patents (Class 544/272)
  • Patent number: 10253026
    Abstract: This invention relates to a method for preparation of a xanthine-based compound of formula (I): as well as to intermediates useful in such preparation.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: April 9, 2019
    Assignee: Boenringer Ingelheim International GmbH
    Inventors: Weitong Dong, Yao Huang, Shengmin Su, Yongfen Sun, Pengtao Zhang
  • Publication number: 20150139903
    Abstract: Tracers targeting phosphodiesterase1 for use in gamma radiation detection-based diagnostic techniques, particularly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.
    Type: Application
    Filed: September 22, 2014
    Publication date: May 21, 2015
    Inventors: Peng LI, Lawrence WENNOGLE, Jun ZHAO, Hailin ZHENG
  • 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: 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: 20140073656
    Abstract: Novel compounds for the treatment of estrogen receptor-mediated disorders, including breast cancer, and methods of treatment using the novel compounds. The novel compounds, when administered in a safe and effective amount, present extended binding to estrogen receptors in breast tissue without activating the estrogen receptors. Estrogen is blocked from binding to the estrogen receptors for an extended period of time, effectively hindering growth of breast cancer cells.
    Type: Application
    Filed: October 10, 2013
    Publication date: March 13, 2014
    Applicant: Florida A&M University
    Inventor: John S. Cooperwood
  • 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
  • Publication number: 20140031375
    Abstract: This invention relates to compounds of formula (I), Wherein R1-R4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.
    Type: Application
    Filed: December 19, 2008
    Publication date: January 30, 2014
    Inventor: Constance Neely Wilson
  • Publication number: 20130303761
    Abstract: The present invention relates to novel protein modulators capable of altering function of the mutant CFTR protein and their use for treating diseases associated with CFTR protein malfunction. The invention provides compositions, pharmaceutical preparations and methods of correcting the cellular alteration of a mutant CFTR protein wherein the CFTR mutation is a mutation AF508-CFTR, or another mutation of class II.
    Type: Application
    Filed: June 20, 2011
    Publication date: November 14, 2013
    Applicant: INSTYTUT BIOCHEMII I BIOFIZYKI PAN
    Inventors: Norbert Odolczyk, Piotr Zielenkiewicz, Grzegorz Wieczorek, Aleksander Edelman, Danielle Tondelier, Janine Fritsch
  • Patent number: 8569489
    Abstract: The invention relates to a range of original xanthine derivatives substituted in 1 -and 7-positions with benzhydryl-4-piperazinyl-1-alkane fragments. A method for obtaining 3-methyl-7-[4-(benzhydryl-4-piperazinyl-1)butyl]xanthine and the salts thereof with organic and inorganic acids by alkylating the 7-potassium salt of 3-methylxanthine by 1,4-dibromobutane, by subsequently interacting the thus formed 7-(4-bromobutyl)-3-methylxanthine with 1-benzhydrylpiperazinyl and by neutralising the thus obtained radical 7-/4-(4-benzhydrylpiperazinyl-1) butyl/-3-methylxanthine by an organic or inorganic acid is also disclosed.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: October 29, 2013
    Assignee: A.B. Intelpharm Limited
    Inventors: Robert G. Glushkov, Sergei D. Juzhakov, Olga S. Fominova, Nelli M. Sazonova, Elena M. Dolginova, Vadim A. Shorr, Mikhail V. Borovkov, Valentina V. Asnina
  • Patent number: 8492390
    Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: July 23, 2013
    Assignee: Santaris Pharma A/S
    Inventors: Mads Detlef Sorensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
  • 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
  • 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
  • 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: 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: 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: 8222257
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
  • Patent number: 8207175
    Abstract: The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular the inhibition of those enzymes.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: June 26, 2012
    Assignee: University Court of the University of Dundee
    Inventors: Daniel Marinus Ferdinand Van Aalten, Ian Michael Eggleston
  • 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
  • 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
  • Publication number: 20120022086
    Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 26, 2012
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 8084458
    Abstract: Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.
    Type: Grant
    Filed: August 3, 2009
    Date of Patent: December 27, 2011
    Assignee: Santaris Pharma A/S
    Inventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
  • Publication number: 20110282031
    Abstract: This invention relates to a diagnostic probe comprising a compound of formula (I): such as 3-[2-[4-(5-aminopentyl-3-amidocarboxypropanoyl)]aminophenyl]ethyl]-8-benzyl-7-[2-ethyl(2-hydroxyethyl)amino]ethyl-1-propylxanthine, with one or more label moieties attached thereto. The compounds of the present invention are useful as diagnostic probes, including probes for diagnostic assays and imaging. Accordingly, the invention provides A1 adenosine receptor antagonist compounds with radioactive or non-radioactive labels suitable for executing such assays and imaging measurements. Labeled compounds are useful to obtain quantitative measurements of the A1 adenosine receptor antagonist compounds. They may be employed as an imaging agent in diagnostic procedures such as MRI and PET as well as cell or receptor based assays.
    Type: Application
    Filed: January 20, 2011
    Publication date: November 17, 2011
    Inventors: Constance N. Wilson, John J. Partridge
  • 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: 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: 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: 20110118464
    Abstract: The halogenated xanthine derivatives and the precursors thereof for anti-cancer and anti-metastasis activity and the preparation method thereof are provided. The halogenated xanthine derivatives can further be radio-labeled with the radioactive halide group. The growth of human prostate carcinoma, tongue squamous cell carcinoma, colon adenocarcinoma and lung carcinoma can be inhibited and arrested in G0/G1 phase by KMUP-2Cl (7-[2-[4-(chlorophenyl)-piperazinyl]ethyl]-1,3-dimethyl-8-chloroxanthine). In addition, the growth of human prostate carcinoma LNCaP can be inhibited by KMUP-1 (7-[2-[4-(2-chlorobenzene)-piperazinyl]-ethyl]-1,3-dimethyl-xanthine), and the LNCaP prostate cancer xenograft growth in nude mice is effectively inhibited by the intraperitoneal injection and per oral administration of KMUP-1.
    Type: Application
    Filed: November 18, 2009
    Publication date: May 19, 2011
    Inventor: Ing-Jun Chen
  • 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
  • Patent number: 7902360
    Abstract: wherein R3 is Alk14ArR16, and wherein Alk14 is C1-8 straight or branched alkylene or alkenylene. The present invention provides novel adenosine receptor antagonists, more particularly, A1 adenosine receptor antagonists of formula (I). Pharmaceutical compositions comprising an A1 adenosine receptor antagonist of formula (I) and a pharmaceutically acceptable carrier are further provided. Compositions also include diagnostic assay-type probes comprising a novel A1 adenosine receptor antagonist of formula (I) that is labeled or conjugated with radioactive or non-radioactive material. Methods for treating A1 adenosine receptor related disorders comprising administering an A1 adenosine receptor antagonist of formula I are also disclosed. The novel A1 adenosine receptor antagonist compositions of formula (I) find further use in diagnostic and imaging methods.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: March 8, 2011
    Inventors: Constance N. Wilson, John J. Partridge
  • Patent number: 7875603
    Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.
    Type: Grant
    Filed: September 21, 2007
    Date of Patent: January 25, 2011
    Assignee: Nova Southeastern University
    Inventors: Appu Rathinavelu, Sivanesan Dakshanamurthy, Nagarajan Pattabiraman
  • Publication number: 20100317671
    Abstract: A pharmaceutical composition for a treatment of an interstitial lung disease is provided. The pharmaceutical composition comprises an effective amount of an active component being one selected from a group consisting of a KMUP compound, a KMUP monoquaternary ammonium salt and a KMUP monoquaternary ammonium complex salt, wherein the KMUP monoquaternary ammonium complex salt is synthesized by the KMUP compound and a carboxylic acid derivative of one selected from a group consisting of a statin, a non-steroid anti-inflammatory (NSAIDs) and an anti-asthmatic drug.
    Type: Application
    Filed: July 7, 2010
    Publication date: December 16, 2010
    Applicant: KAOHSIUNG MEDICAL UNIVERSITY
    Inventor: Ing-Jun Chen
  • Patent number: 7838523
    Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.
    Type: Grant
    Filed: September 11, 2007
    Date of Patent: November 23, 2010
    Assignee: CGI Pharmaceuticals, Inc.
    Inventors: Peter A. Blomgren, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Jeffrey E. Kropf, Kevin S. Currie
  • Patent number: 7820815
    Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof where X is a leaving group selected from halogens and sulphonic ester acid residues, and R1 to R3 are as defined herein, to obtain a compound of the formula (II) and deprotecting the obtained compound of the formula (II) to obtain the product xanthines.
    Type: Grant
    Filed: November 4, 2005
    Date of Patent: October 26, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Thorsten Pachur, Thomas Nicola, Adil Duran
  • Patent number: 7799524
    Abstract: The invention relates to compounds of formula 1 wherein R1-R2 is a guanine derivative; X is oxygen or sulfur; R3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH2; R4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R4 to R1 forming a cyclic substrate, or a further group —R3—CH2—X—R1-R2. The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O6-alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.
    Type: Grant
    Filed: October 1, 2003
    Date of Patent: September 21, 2010
    Assignee: Ecole Polytechnique Ferdeale de Lausanne
    Inventors: Maik Kindermann, Kai Johnsson, Christoph Bieri
  • Patent number: 7786301
    Abstract: A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9.
    Type: Grant
    Filed: May 8, 2006
    Date of Patent: August 31, 2010
    Assignee: Schering Corporation
    Inventors: Vilas A. Dahanukar, Hoa N. Nguyen, Cecilia A. Orr, Fucheng Zhang, Ilia Zavialov
  • Publication number: 20100204250
    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: April 27, 2010
    Publication date: August 12, 2010
    Applicant: Boehringer Ingelheim Pharma & Co. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Patent number: 7772226
    Abstract: 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: Grant
    Filed: August 28, 2008
    Date of Patent: August 10, 2010
    Assignee: 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
  • Patent number: 7759355
    Abstract: The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a patient in need thereof. More preferably the adenosine A2A receptor antagonist is a xanthine derivative or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 27, 2003
    Date of Patent: July 20, 2010
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Hiroshi Kase, Naoki Seno, Akihisa Mori, Dayao Zhao
  • Publication number: 20100173916
    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: March 16, 2010
    Publication date: July 8, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20100168425
    Abstract: The invention relates to a range of original xanthine derivatives substituted in 1- and 7-positions with benzhydryl-4-piperazinyl-1-alkane fragments. A method for obtaining 3-methyl-7-[4-(benzhydryl-4-piperazinyl-1)butyl]xanthine and the salts thereof with organic and inorganic acids by alkylating the 7-potassium salt of 3-methylxanthine by 1,4-dibromobutane, by subsequently interacting the thus formed 7-(4-bromobutyl)-3-methylxanthine with 1-benzhydrylpiperazinyl and by neutralising the thus obtained radical 7-/4-(4-benzhydrylpiperazinyl-1) butyl/-3-methylxanthine by an organic or inorganic acid is also disclosed.
    Type: Application
    Filed: September 29, 2009
    Publication date: July 1, 2010
    Applicant: OOO 'FARMVING'
    Inventors: Robert G. Glushkov, Sergei D. Juzhakov, Olga S. Fominova, Nelli M. Sazonova, Elena M. Dolginova, Vadim A. Shorr, Mikhail V. Borovkov, Valentina V. Asnina
  • Patent number: 7713982
    Abstract: The present invention relates to a therapeutically active xanthine derivative compound of formula (I): corresponding pharmaceutical formulations containing, manufacture processes for, methods or uses of such compounds in therapy, in particular for treatment of diseases where under-activation of the HM74A receptor contributes to such diseases or where activation of the HM74A receptor will be beneficial.
    Type: Grant
    Filed: February 10, 2005
    Date of Patent: May 11, 2010
    Assignee: Smithkline Beecham Corporation
    Inventor: Ivan Leo Pinto
  • Publication number: 20100016329
    Abstract: The present invention provides a pharmaceutical composition including a compound of 7-[2-[4-(2-chlorophenyl)piperazinyl]-ethyl]-1,3-dimethylxanthine (KMUP-1), wherein the compound is a Rho-kinase inhibitor, and the pharmaceutical composition inhibits a physiological activity of a lung epithelial cell.
    Type: Application
    Filed: July 21, 2008
    Publication date: January 21, 2010
    Applicant: KAOHSIUNG MEDICAL UNIVERSITY
    Inventor: Ing-Jun Chen
  • Patent number: 7645763
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 and R2 are defined as in the claims, 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: February 22, 2005
    Date of Patent: January 12, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
  • Patent number: 7569574
    Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: August 4, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
  • Patent number: 7569575
    Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilizing intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.
    Type: Grant
    Filed: May 8, 2003
    Date of Patent: August 4, 2009
    Assignee: Santaris Pharma A/S
    Inventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
  • Patent number: 7560450
    Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: July 14, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co., KG
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
  • Patent number: 7550455
    Abstract: The present invention relates to substituted xanthines of the general formula in which R1 to R3 and n are as defined in claims 1 to 8, their tautomers, their enantiomers, their diastereomers, their mixtures, their prodrugs and their salts, which have valuable pharmacological properties, in particular an inhibitory action on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: June 23, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
  • Publication number: 20090137801
    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: Application
    Filed: January 27, 2009
    Publication date: May 28, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Mohammad TADAYYON, Leo THOMAS
  • Patent number: 7501426
    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: February 17, 2005
    Date of Patent: March 10, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
  • Patent number: 7495002
    Abstract: The present invention relates to new substituted xanthines of general formula wherein R1, R2 and X are defined as in the claims, the tautomers, the enantiomers, the diastereomers, 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: September 1, 2005
    Date of Patent: February 24, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Elke Langkopf, Matthias Eckhardt, Frank Himmelsbach, Mohammad Tadayyon, Leo Thomas, Ralf R. H. Lotz
  • Patent number: 7495003
    Abstract: The application relates to new substituted xanthines of general formula wherein R1 and R2 are defined as in claims 1 to 11, the tautomers, the enantiomers, the diastereomers, 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: September 1, 2005
    Date of Patent: February 24, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Mohammad Tadayyon, Leo Thomas