The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/263.23)
  • Publication number: 20100222369
    Abstract: The present invention provides a method for treating dry eye condition in an individual comprising administrating to said individual an amount of A3 adenosine receptor (A3AR) agonist, the amount being effective to ameliorate symptoms of dry eye in the individual. In accordance with one embodiment, the dry eye condition is manifested by one or more opthalmologic clinical symptoms selected from foreign body sensation, burning, itching, irritation, redness, eye pain, blurred vision, degraded vision and excessive tearing. A preferred A3RAg in accordance with the invention is N6-(3-iodobenzyl)-adenosine-5?-N-methyluronamide (IB-MECA).
    Type: Application
    Filed: May 6, 2010
    Publication date: September 2, 2010
    Applicant: CAN-FITE BIOPHARMA LTD.
    Inventors: Pnina FISHMAN, Tatiana REITBLAT, Ilan COHN
  • Publication number: 20100210579
    Abstract: Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
    Type: Application
    Filed: March 15, 2010
    Publication date: August 19, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
  • 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: 20100196443
    Abstract: A dietary supplement or animal feed includes at least one Cordyceps species or extract thereof. The dietary supplement and/or animal feed is preferably for oviparous animals and in particular for the production of eggs.
    Type: Application
    Filed: July 4, 2008
    Publication date: August 5, 2010
    Applicant: A P NUTRIPHARM PTE. LTD.
    Inventor: Yue Xu
  • Publication number: 20100183564
    Abstract: The present invention relates to compounds and compositions for expanding the number of CD34+ cells for transplantation. The invention further relates to a cell population comprising expanded hematopoietic stem cells (HSCs) and its use in autologous or allogeneic transplantation for the treatment of patients with inherited immunodeficient and autoimmune diseases and diverse hematopoietic disorders to reconstitute the hematopoietic cell lineages and immune system defense.
    Type: Application
    Filed: October 29, 2009
    Publication date: July 22, 2010
    Applicant: IRM LLC
    Inventors: Anthony E. Boitano, Michael Cooke, Shifeng Pan, Peter G. Schultz, John Tellew, Yongqin Wan, Xing Wang
  • 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
  • Patent number: 7754728
    Abstract: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.
    Type: Grant
    Filed: September 26, 2003
    Date of Patent: July 13, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
  • Publication number: 20100160262
    Abstract: The present invention provides treatment methods involving modulating a sirtuin activity and/or a sirtuin mRNA and/or a sirtuin polypeptide level. In some embodiments, the present invention provides treatment methods involving modulating SIRT1 activity and/or SIRT mRNA and/or polypeptide level. The present invention provides methods of inhibiting SIRT1 Tat deacetylase activity. Methods of inhibiting SIRT1 Tat deacetylase activity are useful for treating immunodeficiency virus infections, particularly human immunodeficiency virus (HIV) infection. Thus, the present invention provides methods of treating an immunodeficiency virus infection, generally involving inhibiting SIRT1 Tat deacetylase activity. The present invention further provides methods of identifying agents that modulate sirtuin activity (e.g., SIRT1 activity), particularly ability of sirtuins to interact with (e.g., bind and/or deacetylate) a substrate, e.g., a viral substrate such as a Tat polypeptide.
    Type: Application
    Filed: December 23, 2008
    Publication date: June 24, 2010
    Inventors: Melanie Ott, Eric M. Verdin, Manfred Jung
  • Publication number: 20100144685
    Abstract: This document involves methods and materials related to inhibiting cyclin D polypeptide activity. For example, this document provides methods and materials that can be used to (1) identify mammals or cells in need of cyclin D polypeptide inhibition and (2) administer an agent capable of inhibiting cyclin D polypeptide activity.
    Type: Application
    Filed: October 10, 2007
    Publication date: June 10, 2010
    Inventors: Rodger E. Tiedemann, Alexander Keith Stewart, Aaron David Schimmer, Xinliang Mao
  • Publication number: 20100144738
    Abstract: The present invention relates to compounds and methods use as inhibitors of c-Met. Certain compounds of the subject invention have the following structural formula (I). Other compounds of the subject invention have structural formulas as defined herein. Also disclosed herein are pharmaceutical compositions comprising the compounds of the subject invention.
    Type: Application
    Filed: August 29, 2007
    Publication date: June 10, 2010
    Inventors: William Bornmann, David Maxwell, Yunming Ying, Dongmei Han, Zhenghong Peng, Varsha Gandhi, Christine Stellrecht
  • Patent number: 7723340
    Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: May 25, 2010
    Assignees: Signal Pharmaceuticals, LLC, Pharmacopeia Drug Discovery, Inc.
    Inventors: Ronald J. Albers, Leticia Ayala, Steven S. Clareen, Maria Mercedes Delgado Mederos, Robert Hilgraf, Sayee G. Hegde, Kevin Hughes, Adam Kois, Veronique Plantevin-Krenitsky, Meg McCarrick, Lisa Nadolny, Moorthy S. S. Palanki, Kiran Sahasrabudhe, John Sapienza, Yoshitaka Satoh, Marianne K. Sloss, Elise Sudbeck, Jonathan Wright, Ian Henderson, Andrew G. Cole
  • Publication number: 20100120799
    Abstract: Compounds of formula (I): wherein R1 is C1-8alkylamino, C1-8alkoxy, C3-7cycloalkylC1-6alkylamino, C3-7cycloalkylC1-6alkoxy, C1-3alkoxyC2-3alkoxy, or Hetb-C1-3alkoxy; Hetb is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen atom; R2 is —(CH2)n-Het; n is an integer having a value of 1 to 4; Het is a 5- or 6-membered saturated aliphatic heterocycle containing one oxygen heteroatom, which heterocycle may be substituted by one or two C1-4alkyl groups, and salts and solvates thereof, are inducers of human interferon and may be useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.
    Type: Application
    Filed: February 15, 2008
    Publication date: May 13, 2010
    Applicant: SMITHKLINE BEECHAM CORPORATION
    Inventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
  • Publication number: 20100105706
    Abstract: The present invention relates to methods of preventing airway remodeling using A2B adenosine receptor antagonists. This invention finds utility in the treatment and prevention of asthma, COPD, pulmonary fibrosis, emphysema, and other pulmonary diseases. The invention also relates to pharmaceutical compositions for use in the method.
    Type: Application
    Filed: October 26, 2009
    Publication date: April 29, 2010
    Applicant: Gilead Palo Alto, Inc.
    Inventors: Dewan Zeng, Michael R. Blackburn, Luiz Belardinelli
  • Publication number: 20100105652
    Abstract: Substituted heteroaryl nitrile salt of Formula I, processes for their preparation, pharmaceutical compositions comprising such compounds and use of the compounds as cysteine protease inhibitors are provided.
    Type: Application
    Filed: February 28, 2008
    Publication date: April 29, 2010
    Inventors: Jose Miguel Coteron-Lopez, Beatriz Diaz-Hernandez, Jose Maria Fiandor-Roman, Maria Marco-Martin
  • Publication number: 20100093737
    Abstract: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3? position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.
    Type: Application
    Filed: January 17, 2008
    Publication date: April 15, 2010
    Applicant: INSTITUT DE RECHERCHES CLINIQUES DE MONTREAL
    Inventor: Yvan Guindon
  • Publication number: 20100093770
    Abstract: A method for treating glaucoma or ocular hypertension comprising administering to a patient a pharmacologically effective amount of a compound represented by the following (1) or a salt thereof: wherein X represents CH or N; R1 represents a hydrogen atom, a hydroxy group, a halogen atom, an alkyl group, an alkoxy group, a cycloalkyl group, a cycloalkoxy group, a (cycloalkyl)methoxy group, or ?R2 represents a hydrogen atom, an alkyl group, a cycloalkyl group, an alkylcarbonyl group or an alkyloxycarbonyl group; and Ra and Rb are the same or different and represent a hydrogen atom, a hydroxy group, a halogen atom, an alkyl group, an alkoxy group, a cycloalkyl group or a cycloalkoxy group.
    Type: Application
    Filed: April 14, 2008
    Publication date: April 15, 2010
    Inventors: Atsushi Shimazaki, Noriko Kawabata, Tomoko Kirihara, Jayson M. Rieger, Robert D. Thompson
  • 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
  • Publication number: 20090258887
    Abstract: The present invention is concerned with novel arylalkyl carboxylic acid derivatives, more specifically, with acylates of arylalkyl carboxylic acids with naturally occurring, non-toxic hydroxy, sulfhydryl, amino or imino compounds, and to compositions containing them. The compositions are preferably cosmetic preparations.
    Type: Application
    Filed: September 14, 2006
    Publication date: October 15, 2009
    Inventors: Raphael Beumer, Jochen Klock, Stefan Martin Stoeckli
  • Publication number: 20090253665
    Abstract: Pharmaceutical compositions comprising an aldosterone inhibitor and an adenosine A1 receptor antagonist (AA1RA) and methods of treating cardiovascular disease comprising identifying a patient in need of such treatment, and administering a pharmaceutical composition disclosed herein to said patient are disclosed.
    Type: Application
    Filed: June 16, 2009
    Publication date: October 8, 2009
    Inventors: Lauren Otsuki, Kenneth Widder, Howard C. Dittrich
  • Publication number: 20090253718
    Abstract: The invention provides a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a satur
    Type: Application
    Filed: April 25, 2007
    Publication date: October 8, 2009
    Applicants: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology Limited
    Inventors: Thomas Glanmor Davies, Michelle Dawn Garrett, Robert George Boyle, Ian Collins
  • Publication number: 20090247557
    Abstract: Disclosed are novel compounds a compound of Formula I that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular dyslipidemia, diabetes, decreased insulin sensitivity, Polycystic Ovarian Syndrome, Stein-Leventhal syndrome, and obesity.
    Type: Application
    Filed: April 2, 2009
    Publication date: October 1, 2009
    Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
  • Publication number: 20090233922
    Abstract: A method for the combined treatment of neuronal and non-neuronal pain in mammals is provided comprising administration of adenylyl cyclase 1 inhibitors having the following general formula (1): (1) wherein: G, H, J and M are each N, or H and J are each C, and G and M are each N, S or O, or H, J and M are each C and G is N, S or O.
    Type: Application
    Filed: October 13, 2006
    Publication date: September 17, 2009
    Inventor: Min Zhuo
  • Publication number: 20090233947
    Abstract: Compounds of formula (I) which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1, also known as TRPV1).
    Type: Application
    Filed: May 10, 2006
    Publication date: September 17, 2009
    Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John HollingWorth, A. Brian Jones
  • Patent number: 7589075
    Abstract: The present invention concerns the use of an active ingredient selected from the group consisting of agonists of the adenosine receptor system, for inhibiting viral replication in cells. In particular, the invention provides a composition and method for inhibiting viral replication in cells, the method comprising presenting to the cells an effective amount of the active ingredient. According to one embodiment, the adenosine agonist is an A3 receptor agonist (A3RAg). The invention is particularly useful, for although not limited to, inhibiting the replication of HIV virus in human cells.
    Type: Grant
    Filed: January 13, 2002
    Date of Patent: September 15, 2009
    Assignee: Can-Fite Biopharma Ltd.
    Inventors: Pnina Fishman, Kamel Khalili
  • Publication number: 20090203638
    Abstract: Pharmaceutical compositions include compounds with cytokinin activity to modulate glucose and/or lipid metabolism in a mammal. Especially preferred compounds include those comprising a purine scaffold, and it is further preferred that contemplated compositions are employed to prevent and/or treat various diseases, including pre-diabetes, insulin resistance, type-2 diabetes, Syndrome X, and dyslipidemia. In still further preferred aspects, compounds with cytokinin activity are used to activate AMPK and/or Akt. Consequently, various diseases associated with dysregulation of AMPK and/or Akt may be treated using the compounds of the present inventive subject matter.
    Type: Application
    Filed: April 7, 2009
    Publication date: August 13, 2009
    Applicant: VDF FUTURECEUTICALS, INC.
    Inventors: Dusan Miljkovic, Jovan Hranisavljevic, Zbigniew Pietrzkowski
  • Patent number: 7572800
    Abstract: The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B virus activity in combination or alternation. Specifically, the invention is directed to a method for treating hepatitis B virus infection comprising administering FTC in combination or alternation with penciclovir, famciclovir or Bis-POM-PMEA. Additionally, the invention is directed to a method for treating hepatitis B virus infection comprising administering L-FMAU in combination or alternation with DAPD, penciclovir or Bis-POM-PMEA. The invention is further directed to a method for treating hepatitis B virus infection comprising administering DAPD in combination or alternation with Bis-POM-PMEA.
    Type: Grant
    Filed: February 25, 2003
    Date of Patent: August 11, 2009
    Assignee: Gilead Sciences, Inc.
    Inventors: Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
  • 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: 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: 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
  • Publication number: 20090131458
    Abstract: The present invention includes novel compounds useful in the treatment of various disorders in particular infectious diseases, cancer, and allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, and as vaccine adjuvants.
    Type: Application
    Filed: February 15, 2008
    Publication date: May 21, 2009
    Applicant: SmithKline Beecham Corporation
    Inventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
  • Publication number: 20090111836
    Abstract: The present invention relates to compounds, compositions for use in reversing multidrug resistance in cancer cells, process for the preparation thereof and their uses in treating cancers. More particularly, the present invention relates to 3?,4?-aromatic acyloxy substituted 7,8-pyranocoumarins compounds for use in reversing P-glycoprotein overexpression mediated multidrug resistance in cancer cells, pyranocoumarins containing compositions, process for the preparation thereof and their uses in treating cancers.
    Type: Application
    Filed: October 31, 2007
    Publication date: April 30, 2009
    Inventors: Wangfun Fong, Xiaoling Shen, Guangying Chen, Guoyuan Zhu, Chikeung Wan, Kaiwing Tse
  • Publication number: 20090099213
    Abstract: The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N?C(R6), (R7)C?N, (R8)N—C(O), (R8)2C—C(O), N?N or (R7)C?C(R6); A is an optionally substituted saturated C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole g
    Type: Application
    Filed: October 25, 2005
    Publication date: April 16, 2009
    Applicants: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Techology Limited
    Inventors: Valerio Berdini, Robert George Boyle, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Hannah Fiona Sore, John Caldwell, Ian Collins, Tatiana Faria Da Fonseca, Alastair Donald
  • Publication number: 20090069289
    Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 12, 2009
    Applicant: PHARMACOPEIA, INC.
    Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Ansari Nasrin
  • 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
  • Publication number: 20090062314
    Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, an ischemic condition, a reperfusion injury, obesity, a wasting disease, or diabetes, comprising administering an effective amount of a Purine Derivative to an animal in need thereof.
    Type: Application
    Filed: August 4, 2008
    Publication date: March 5, 2009
    Applicant: Inotek Pharmaceuticals Corporation
    Inventors: Prakash Jagtap, Csaba Szabo, Andrew L. Salzman
  • Patent number: 7495004
    Abstract: The invention relates to methods for the treatment or prevention of an LXR mediated disease or condition, including cardiovascular disease and atherosclerosis, novel compounds of formula (I) for use in such methods and pharmaceutical compositions comprising compounds for use in such methods.
    Type: Grant
    Filed: May 20, 2003
    Date of Patent: February 24, 2009
    Assignee: Glaxo Group Limited
    Inventors: Sharon Davis Boggs, Jon Loren Collins, Adam Fivush, Eugene Lee Stewart, Timothy Mark Willson
  • Patent number: 7495006
    Abstract: Provided are cyclobutyl nucleosides and methods for their use in treatment of infections including Retroviridae (including HIV), Hepadnaviridae (including HBV), or Flaviviridae (including BVDV and HCV) infection, or conditions related to abnormal cellular proliferation, in a host, including animals, and especially humans.
    Type: Grant
    Filed: December 8, 2005
    Date of Patent: February 24, 2009
    Assignee: Emory University
    Inventors: Dennis C. Liotta, Shuli Mao, Michael Hager
  • Publication number: 20090048275
    Abstract: Solid forms comprising 4-[9-(tetrahydro-furan-3-yl)-8-(2,4,6-trifluoro-phenylamino)-9H-purin-2-ylamino]-cyclohexan-1-ol, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders are disclosed.
    Type: Application
    Filed: August 28, 2008
    Publication date: February 19, 2009
    Inventors: Marie G. Beauchamps, Louise Michelle Cameron, Robert Hilgraf, Mohit Atul Kothare, Manohar T. Saindane, Jean Xu
  • Publication number: 20090048203
    Abstract: This invention relates to compounds of Formula (I): and their use in the treatment of bacterial infections.
    Type: Application
    Filed: October 13, 2005
    Publication date: February 19, 2009
    Inventors: Marta Cavero-Tomas, Madhu Gowravaram, Hoan Huynh, Haihong Ni, Suzanne Stokes
  • Publication number: 20090028895
    Abstract: A dietary supplement composition comprising a therapeutically effective amount of at least one sirt 1 activating agent, a therapeutically effective amount of at least one Qi activating agent, and a therapeutically effective amount of at least one adaptogen is disclosed. An optional herbal treatment for stress-related deep wrinkles comprises chronic oral administration for at least two weeks of a beverage containing an effective amount of a valerian root extract sufficient to provide a desired reduction in the appearance of the deep wrinkles. A photoprotective agent may also be included. Also included are a microcirculation increasing agent. Also optional are an herbal toner and topical cellulite product.
    Type: Application
    Filed: November 29, 2007
    Publication date: January 29, 2009
    Inventor: Walter P. Smith
  • Patent number: 7452894
    Abstract: Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11, is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or pro
    Type: Grant
    Filed: January 10, 2002
    Date of Patent: November 18, 2008
    Assignee: Vernalis Research Limited
    Inventors: Roger John Gillespie, Joanne Lerpiniere, Claire Elizabeth Dawson, Suneel Gaur, Robert Mark Pratt, Gemma Caroline Stratton, Scott Murray Weiss
  • Publication number: 20080262002
    Abstract: The present invention provides antioxidant compositions comprising S-adenosylmethionine (SAMe), vitamin E and vitamin C and uses thereof for the treatment of liver injury and insulin resistance.
    Type: Application
    Filed: January 26, 2006
    Publication date: October 23, 2008
    Applicant: UNIVERSITY OF MANITOBA
    Inventors: Wilfred Wayne Lautt, Zhi Ming
  • Publication number: 20080262003
    Abstract: Methods for treating neoplasia with a chemotherapeutic agent and radiation are provided. Radiation therapies used in conduction with a compound described herein presents a synergistic effect in the treatment of cancers. A compound of formula (I): wherein X, Y, Z, R1 and R2 are defined herein, sensitize cells making them more susceptible to radiation therapy.
    Type: Application
    Filed: April 14, 2008
    Publication date: October 23, 2008
    Applicant: Southern Research Institute Office of Commercialization and intellectual Prop
    Inventor: Bo Xu
  • Publication number: 20080262001
    Abstract: The present invention relates to a method for treating recurrent tumor metastases following liver resection that includes administration of an effective amount of an agonist of A2A adenosine receptors (ARs).
    Type: Application
    Filed: April 14, 2008
    Publication date: October 23, 2008
    Applicant: Adenosine Therapeutics, LLC
    Inventors: Onno Kranenburg, Jarmila van der Bilt, Inne Borel Rinkes, Jayson M. Rieger
  • Publication number: 20080242683
    Abstract: Compounds of (I) or stereoisomers or pharmaceutically acceptable salts thereof, where W, R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Application
    Filed: March 13, 2006
    Publication date: October 2, 2008
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 7423041
    Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.
    Type: Grant
    Filed: March 23, 2007
    Date of Patent: September 9, 2008
    Assignee: Endacea, Inc.
    Inventors: Constance Wilson, John J. Partridge
  • Patent number: 7420056
    Abstract: Substituted bicyclic imidazo-3-yl-amine compounds are provided, as well as processes for the production thereof and pharmaceutical formulations containing these compounds. The use of these compounds for the production of pharmaceutical formulations and related methods of treatment are also provided.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: September 2, 2008
    Assignee: Gruenenthal GmbH
    Inventors: Sven Kuehnert, Stefan Oberboersch, Corinna Sundermann, Michael Haurand, Ruth Jostock, Klaus Schiene, Thomas Tzschentke, Thomas Christoph, Dagmar Kaulartz, Saskia Zemolka
  • Publication number: 20080187561
    Abstract: The present invention relates to enteric coated didanosine compositions having a subcoat comprising hydroxypropyl methylcellulose, and process for preparation thereof. The enteric coating ranges from 19-25% w/w of the composition. The compositions are stable and have acceptable acid resistance and release profile.
    Type: Application
    Filed: December 21, 2007
    Publication date: August 7, 2008
    Inventors: Mona DHALIWAL, Girish Karanth, Romi Barat Singh
  • Patent number: 7407955
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs 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: August 12, 2003
    Date of Patent: August 5, 2008
    Assignee: Boehringer Ingelheim Pharma GmbH & Co., KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
  • Patent number: 7388002
    Abstract: Compounds represented by the formula: A is (CH2)nR2, —CH?CH2, CH2—CH?CH2, O(CH2)nR2, CH(OH)CH3, CH(OH)CH2OH, CH2—CH(OH)CH3, CH2CH(OH)CH2OH, or CH(OH)CH(OH)CH3, R,R1 individually is H, NH2OH, Cl, Br, I, aryl, substituted aryl, heterocycle, NR3R4, OR3 or SR3, R2 is H, OH, F, N3, NH2, CO2H, SH, alkyl, substituted alkyl, S-alkyl, O-acyl, CONH2, or CONH-alkyl, n is 1-3, y is O, S or NH, W is O or S, Z, Z? individually is OR3, OR4, O(CH2)m—O—(CH2)xCH3, NH—CH(alkyl)CO2R3, alkyl, substituted alkyl, OCH2CH2S—C(O)CH3, OCH2CH2S—C(O)CH(CH3)2, OCH2CH2S—C(O)C(CH3)3, OCH2CH2—SC(O)aryl, OCH2CH2—S—S—OCH2CH2OH, OCH2OC(O)C(CH3)3, OCH2—O—C(O)OCH(CH3)2, or OCH2—O—C(O)CH(CH3)2 R3, R4 individually is H, alkyl, substituted alkyl, aryl, or substituted aryl; Both R3 and R4 can form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring; m is 1-3, x is 0-19; and pharmaceutically acceptable salts thereof and prodrugs thereof are provided.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: June 17, 2008
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu