At 2- And 6-positions (e.g., Theophyllines, Etc.) Patents (Class 544/267)
  • Patent number: 9133062
    Abstract: Methods of firing a cordierite green body to form a fired cordierite body. The green body comprises cordierite-forming raw materials and organic material, the body having a core portion and a skin portion. The green body is pre-heated to a pre-heat temperature that is less than a thermal decomposition temperature of the organic material. The green body is maintained at the pre-heat temperature for a period of time sufficient to minimize a temperature differential between the core portion and the skin portion. The green body is heated to a low firing temperature in a firing atmosphere sufficient to reduce a content of the organic material and to substantially remove chemically bound water from hydrous alumina. The green body is heated to a high firing temperature in a firing atmosphere sufficient to reduce the content of the organic material prior to a substantial removal of chemically bound water from clay.
    Type: Grant
    Filed: November 21, 2012
    Date of Patent: September 15, 2015
    Assignee: Corning Incorporated
    Inventors: Robert Joseph Castilone, Sriram Rangarajan Iyer, Mark Allen Spetseris, Jonathan Mark Stalker
  • Patent number: 9035050
    Abstract: This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: wherein the values of R1, R2, R3, R4, R5, Y1 and Y2 are described herein.
    Type: Grant
    Filed: July 24, 2013
    Date of Patent: May 19, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
  • Publication number: 20150119409
    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 treating or preventing inflammatory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of intermittent claudication resulting from obstructed arteries in the limbs, and vascular dementia, improves blood flow through peripheral blood vessels and therefore helps with blood circulation in the arms and legs (e.g.
    Type: Application
    Filed: February 2, 2013
    Publication date: April 30, 2015
    Inventor: Mahesh KANDULA
  • Patent number: 8987442
    Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.
    Type: Grant
    Filed: April 17, 2012
    Date of Patent: March 24, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
  • Patent number: 8952016
    Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. The compound of the invention are represented by one of the following structural formulas: The variables for these structural formulas are described herein. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.
    Type: Grant
    Filed: September 1, 2010
    Date of Patent: February 10, 2015
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
  • Publication number: 20150017151
    Abstract: The present invention relates to pharmaceutical formulations comprising xanthine or xanthine derivatives, kits thereof, and methods for treating fibrotic diseases by local administration.
    Type: Application
    Filed: June 18, 2014
    Publication date: January 15, 2015
    Inventor: Matthew J. Buderer
  • Patent number: 8871520
    Abstract: The invention provides a method of detecting uracil. The method comprises reacting uracil with a compound represented by the formula (I) in the presence of an oxidant and a base to produce a fluorescent compound represented by the formula (II).
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: October 28, 2014
    Assignee: Nagasaki University
    Inventors: Masaaki Kai, Takayuki Shibata
  • Patent number: 8865731
    Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.
    Type: Grant
    Filed: May 29, 2009
    Date of Patent: October 21, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Jun Ouchi, Shunji Kunori, Yozo Kojima, Katsumi Shinoda, Katsutoshi Sasaki, Shiro Shirakura
  • Publication number: 20140296263
    Abstract: The present invention in one embodiment relates to a compound of Formula (I); or a pharmaceutically acceptable salt thereof, wherein: each of R1 and R2 is independently selected from —CH3 and —CD3; R3 is hydrogen or deuterium; each of Z1, Z2 and Z3 is independently selected from hydrogen and deuterium; each Z4 is hydrogen or deuterium; each Z5 is hydrogen or deuterium; and each Z6 is hydrogen or deuterium.
    Type: Application
    Filed: July 19, 2012
    Publication date: October 2, 2014
    Applicant: CONCERT PHARMACEUTICALS, INC.
    Inventors: Ara Aslanian, Dolly Parasrampuria, Kristine Hogan, Virginia Braman, Changfu Cheng
  • 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
  • Publication number: 20140271527
    Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 18, 2014
    Applicant: Serina Therapeutics, Inc.
    Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
  • Publication number: 20140275071
    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
  • Publication number: 20140235656
    Abstract: The present invention relates to a stable pharmaceutical composition for sublingual administration comprising a therapeutically effective quantity of an antihistamine agent, in particular Dimenhydnnate and a process for the preparation thereof.
    Type: Application
    Filed: October 25, 2011
    Publication date: August 21, 2014
    Applicant: EXPERMED S.A.
    Inventors: Evangelos Karavas, Efthimios Koutris, Vicky Samara, Amalia Diakidou, Aggelos Karatzas
  • Publication number: 20140194447
    Abstract: Compounds and their pharmaceutically acceptable salts for treatment of ?-amyloid diseases, such as observed in Alzheimer's disease and synucleinopathies, such as Parkinson's disease.
    Type: Application
    Filed: October 10, 2012
    Publication date: July 10, 2014
    Inventors: Luke Esposito, Kelsey Hanson, Marisa C. Yadon, Thomas Lake, Alan D. Snow, Joel Cummings, Anil Kumar
  • 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: 20130324564
    Abstract: The present invention provides individual crystalline polymorphs of (S)-1-(4,4,6, 6,6-pentadeutero-5-hydroxy-hexyl)-3,7-dimethyl-1H-purine-2,6(3H,7H)-dione designated Form 1, Form 2, Form 3 and Form 4. Each polymorph disclosed herein is characterized according to one or more of (a) powder X-ray diffraction data (“XRPD”); (b) differential scanning calorimetry (“DSC”); and (e) thermo gravimetric analysis (TGA).
    Type: Application
    Filed: September 1, 2011
    Publication date: December 5, 2013
    Applicant: CONCERT PHARMACEUTICALS, INC.
    Inventors: Joanna A. Bis, David H. Igo, David J. Turnquist
  • Publication number: 20130310347
    Abstract: High throughput methods for identifying novel inhibitors of Hsp90 chaperone protein folding are disclosed. The inhibitors so identified disrupt the binding of p23 to either Hsp90? or Hsp90? and have selective activity against the proliferation of cancer cells. In particular are provided embodiments of therapeutic compositions that comprise at least one inhibitor of an Hsp90 chaperone activity, the inhibitor being any of the compounds designated as CP1-CP19 as shown in FIGS. 1A-1D or a 2-(trifluoromethyl)pyrimidin-2-yl)thio)acetamide derivatives.
    Type: Application
    Filed: May 21, 2013
    Publication date: November 21, 2013
    Applicant: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Carmel Chan, Sanjiv S. Gambhir, David E. Solow-Cordero, Aileen Hoehne, Ramasamy Paulmurugan
  • Publication number: 20130202549
    Abstract: The disubstituted piperazine analogs (DPAs) derivative compound and DPAs amine complex compound disclosed in the present aspects have characterized by presented pharmaceutics having functions to improve lipolysis, such as inhibiting obesity hyperlipidemia, and atherosclerosis.
    Type: Application
    Filed: September 6, 2012
    Publication date: August 8, 2013
    Inventor: Ing-Jun Chen
  • Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • Patent number: 8471009
    Abstract: The invention relates to substituted 2-alkylamino-3-(arylsulfonyl)cycloalkyl[e or d]pyrazolo[1,5-a]pyrimidines, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions comprising the said compounds as active ingredients, and to novel medicaments and method for treatment and prophylaxis of various CNS diseases. 2-Alkylamino-3-arylsulfonylcycloalkyl[e]pyrazolo[1,5-a]pyrimidines of general formula 1 and 2-alkylamino-3-arylsulfonylcycloalkyl[d]pyrazolo[1,5-a]pyrimidines of general formula 2, wherein: R1 is hydrogen or C1-C3 alkyl; R2 is C1-C3 alkyl; R3 is hydrogen, one or more optionally identical halogen atoms, C1-C3 alkyl or hydroxyl group optionally substituted with C1-C3 alkyl; n is the whole numbers 1, 2 or 3.
    Type: Grant
    Filed: January 23, 2009
    Date of Patent: June 25, 2013
    Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko
  • Patent number: 8440678
    Abstract: The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 14, 2013
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Hiroshi Kase, Minoru Kobayashi, Shizuo Shiozaki, Akihisa Mori, Naoki Seno
  • Patent number: 8409593
    Abstract: The invention relates to a composition containing, preferably in a physiologically acceptable medium, at least one xanthine base or a plant extract containing it, at least one polyurethane powder, and at least one non-ionic dimethicone copolyol. The invention also relates to a cosmetic method for combating cellulite and/or “orange-peel” skin and/or slimming the figure, comprising the application of the composition to the skin. The composition applied to the skin exhibits good cosmetic properties of softness and of non-tackiness.
    Type: Grant
    Filed: June 9, 2008
    Date of Patent: April 2, 2013
    Assignee: L'Oreal
    Inventors: Angeles Fonolla Moreno, Bertrand Piot
  • Publication number: 20130052678
    Abstract: The invention provides a method of detecting uracil. The method comprises reacting uracil with a compound represented by the formula (I) in the presence of an oxidant and a base to produce a fluorescent compound represented by the formula (II).
    Type: Application
    Filed: March 1, 2011
    Publication date: February 28, 2013
    Applicant: NAGASAKI UNIVERSITY
    Inventors: Masaaki Kai, Takayuki Shibata
  • Publication number: 20120309705
    Abstract: The present invention includes novel 3?-deoxy-3?-methylidene-?-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections.
    Type: Application
    Filed: December 14, 2010
    Publication date: December 6, 2012
    Applicant: NOVADEX PHARMACEUTICALS AB
    Inventors: Xiao Xiong Zhou, Staffan Torssell, Olov Wallner, Piaoyang Sun
  • 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: 8263601
    Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by one of the following structural formulas: wherein the values of R1, R2, Y1 and Y2 are described herein.
    Type: Grant
    Filed: September 2, 2010
    Date of Patent: September 11, 2012
    Assignee: CoNCERT Pharmaceuticals, Inc.
    Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
  • 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
  • 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: 8236951
    Abstract: There is disclosed the use of a compound of formula (Ia) or (Ib) wherein R1, R2, R3, R4, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of the enzyme myeloperoxidase (MPO) is beneficial. Certain novel compounds of formula (Ia) or (Ib) and pharmaceutically acceptable salts thereof are disclosed, together with processes for their preparation. The compounds of formulae (Ia) and (Ib) are MPO inhibitors and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders.
    Type: Grant
    Filed: August 4, 2008
    Date of Patent: August 7, 2012
    Assignee: AstraZeneca AB
    Inventors: Sverker Hanson, Gunnar Nordvall, Anna-Karin Tiden
  • Publication number: 20120088771
    Abstract: This invention relates generally to the field of mineralization, and specifically to the role of TNAP in regulating the levels of extracellular inorganic pyrophosphate. The invention provides methods for modulating the activity of TNAP activity; methods for screening for modulators of TNAP activity; modulators of TNAP activity; and methods for treating pathologic conditions known of suspected to be affected by modulation of TNAP activity.
    Type: Application
    Filed: October 11, 2011
    Publication date: April 12, 2012
    Inventor: Jose Luis Millan
  • 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: 20110251218
    Abstract: The present invention relates to a tris salt of 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione of Formula (A) or a pharmaceutically acceptable salt thereof: corresponding pharmaceutical formulations, manufacture processes and uses of the aforementioned compound in therapy, particularly 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: Application
    Filed: December 7, 2009
    Publication date: October 13, 2011
    Inventors: Holly Esken, Beth Adams Norton
  • Patent number: 8034820
    Abstract: The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, a monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.
    Type: Grant
    Filed: July 22, 2004
    Date of Patent: October 11, 2011
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiroshi Kase, Minoru Kobayashi, Shizuo Shiozaki, Akihisa Mori, Naoki Seno
  • 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
  • Patent number: 7981901
    Abstract: Methods and compositions for targeting cerebral circulation and treatment of headache include formulations comprising a pharmacologically active substance in a transdermal formulation, which is topically applied to an area of skin superficial to a carotid artery, a temporal artery, a vertebral artery, or to a tender spot associated with a headache. Particularly preferred formulations include a xanthine derivative (e.g., theophylline, caffeine, aminophylline), and may further comprise ketoprofen. Contemplated methods further include methods of advertising use of contemplated compositions.
    Type: Grant
    Filed: August 20, 2002
    Date of Patent: July 19, 2011
    Inventor: Bruce Frome
  • 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
  • Patent number: 7943625
    Abstract: The present invention relates to a compound according to Formula (I) wherein R1 is selected from C1-C6 alkyl, and said C1-C6 alkyl is substituted with C1-C6 alkoxy; and at least one of said C1-C6 alkyl or said C1-C6 alkoxy is branched; or a pharmaceutically acceptable salt thereof, solvate or solvate of a salt thereof, as well as, to compositions containing at least one compound according to Formula (I) and methods of treating at least one disease or condition therewith.
    Type: Grant
    Filed: June 1, 2007
    Date of Patent: May 17, 2011
    Assignee: AstraZeneca AB
    Inventor: Anna-Karin Tidén
  • Publication number: 20110077255
    Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. For example, this invention relates to novel substituted xanthine derivatives that are derivatives of pentoxifylline. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial.
    Type: Application
    Filed: September 2, 2010
    Publication date: March 31, 2011
    Inventors: Roger D. Tung, Julie F. Liu, Scott L. Harbeson
  • Patent number: 7884202
    Abstract: Nucleobases are perfluoroalkylated in a one step process with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound. Compounds so produced are useful as medicinal drugs, intermediates for medicinal drugs and agricultural chemicals.
    Type: Grant
    Filed: November 6, 2006
    Date of Patent: February 8, 2011
    Assignees: Tosoh Corporation, Tosoh F-Tech, Inc., Sagami Chemical Research Center
    Inventors: Tetsu Yamakawa, Kyoko Yamamoto, Daisuke Uraguchi, Kenji Tokuhisa
  • Publication number: 20110009623
    Abstract: Methods and an apparatus for producing stable crystal polymorphs are provided. Inner surfaces of glass vials with a concave bottom topography are coated with nonstick compounds to select for nucleation of stable polymorphs.
    Type: Application
    Filed: March 20, 2007
    Publication date: January 13, 2011
    Applicant: Worcester Polytechnic Institute
    Inventors: Jason R. Cox, Marta Dabros, Venkat R. Thalladi
  • Publication number: 20100304418
    Abstract: Latently detectable tracers for use in fluid conducting and containment systems wherein the interaction between the tracer and a biomacromolecule produces a detectable signal. More specifically, the latently detectable tracers monitor flow through such systems. Methods for monitoring the flow of fluid using the tracers, and a kit for use in monitoring the flow of fluid in such systems, including the tracers are also disclosed.
    Type: Application
    Filed: December 17, 2008
    Publication date: December 2, 2010
    Inventors: Artin Moussavi, Catherine Rowley-Williams, Cameron MacKenzie, Fiona MacKay, Anne-Marie Fuller, Vjera Magdalenic, Emma Perfect
  • Publication number: 20100256082
    Abstract: The present invention is directed to methods for screening for metallohydrolase inhibitors using metal binding moieties in combination with targeting moieties.
    Type: Application
    Filed: June 12, 2007
    Publication date: October 7, 2010
    Applicant: Viamet Pharmaceuticals, Inc.
    Inventor: Robert J. Schotzinger
  • Patent number: 7795427
    Abstract: The invention provides methods and compositions for modulating osteoclastogenesis and for treating bone diseases characterized by bone loss or a decrease in bone mass or density, by administering a compound or agent that modulates the adenosine A1 receptor, in particular, an inhibitor or antagonist of the A1 receptor.
    Type: Grant
    Filed: February 13, 2007
    Date of Patent: September 14, 2010
    Assignee: New York University
    Inventors: Bruce N. Cronstein, Firas Mohamed Kara
  • 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
  • Publication number: 20100179128
    Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial
    Type: Application
    Filed: August 8, 2006
    Publication date: July 15, 2010
    Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
  • Publication number: 20100168122
    Abstract: The present invention relates to compounds of formula (I) which are xanthine derivatives, processes for manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial
    Type: Application
    Filed: August 8, 2006
    Publication date: July 1, 2010
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Richard Jonathan Daniel Hatley, Andrew McMurtrie Mason, Ivan Leo Pinto
  • Publication number: 20100144703
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, 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: Application
    Filed: February 17, 2010
    Publication date: June 10, 2010
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Publication number: 20100099690
    Abstract: The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing the active compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
    Type: Application
    Filed: August 8, 2006
    Publication date: April 22, 2010
    Inventors: Jag Paul Heer, Ian Edward David Smith
  • Publication number: 20100087455
    Abstract: The present invention relates to new substituted xanthine-based agents, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: October 6, 2009
    Publication date: April 8, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Thomas G. Gant
  • Publication number: 20100010021
    Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly 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: Application
    Filed: September 2, 2009
    Publication date: January 14, 2010
    Inventors: Ivan Leo Pinto, Shahzad Sharooq Rahman, Neville Hubert Nicholson