The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/263.23)
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Publication number: 20100222369Abstract: 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: ApplicationFiled: May 6, 2010Publication date: September 2, 2010Applicant: CAN-FITE BIOPHARMA LTD.Inventors: Pnina FISHMAN, Tatiana REITBLAT, Ilan COHN
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Publication number: 20100210579Abstract: 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: ApplicationFiled: March 15, 2010Publication date: August 19, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Patent number: 7772226Abstract: 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: GrantFiled: August 28, 2008Date of Patent: August 10, 2010Assignee: 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
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Publication number: 20100196443Abstract: 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: ApplicationFiled: July 4, 2008Publication date: August 5, 2010Applicant: A P NUTRIPHARM PTE. LTD.Inventor: Yue Xu
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Publication number: 20100183564Abstract: 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: ApplicationFiled: October 29, 2009Publication date: July 22, 2010Applicant: IRM LLCInventors: Anthony E. Boitano, Michael Cooke, Shifeng Pan, Peter G. Schultz, John Tellew, Yongqin Wan, Xing Wang
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Publication number: 20100179128Abstract: 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 beneficialType: ApplicationFiled: August 8, 2006Publication date: July 15, 2010Inventors: Richard Jonathan Daniel Hatley, Jag Paul Heer, John Liddle, Andrew McMurtrie Mason, Ivan Leo Pinto, Shahzad Sharooq Rahman, Ian Edward David Smith
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Patent number: 7754728Abstract: 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: GrantFiled: September 26, 2003Date of Patent: July 13, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Yoshiaki Isobe, Haruo Takaku, Haruhisa Ogita, Masanori Tobe, Ayumu Kurimoto, Tetsuhiro Ogino, Hitoshi Fujita
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Publication number: 20100160262Abstract: 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: ApplicationFiled: December 23, 2008Publication date: June 24, 2010Inventors: Melanie Ott, Eric M. Verdin, Manfred Jung
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Publication number: 20100144685Abstract: 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: ApplicationFiled: October 10, 2007Publication date: June 10, 2010Inventors: Rodger E. Tiedemann, Alexander Keith Stewart, Aaron David Schimmer, Xinliang Mao
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Publication number: 20100144738Abstract: 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: ApplicationFiled: August 29, 2007Publication date: June 10, 2010Inventors: William Bornmann, David Maxwell, Yunming Ying, Dongmei Han, Zhenghong Peng, Varsha Gandhi, Christine Stellrecht
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Patent number: 7723340Abstract: 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: GrantFiled: January 12, 2006Date of Patent: May 25, 2010Assignees: 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
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Publication number: 20100120799Abstract: 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: ApplicationFiled: February 15, 2008Publication date: May 13, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Publication number: 20100105706Abstract: 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: ApplicationFiled: October 26, 2009Publication date: April 29, 2010Applicant: Gilead Palo Alto, Inc.Inventors: Dewan Zeng, Michael R. Blackburn, Luiz Belardinelli
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Publication number: 20100105652Abstract: 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: ApplicationFiled: February 28, 2008Publication date: April 29, 2010Inventors: Jose Miguel Coteron-Lopez, Beatriz Diaz-Hernandez, Jose Maria Fiandor-Roman, Maria Marco-Martin
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Publication number: 20100093737Abstract: 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: ApplicationFiled: January 17, 2008Publication date: April 15, 2010Applicant: INSTITUT DE RECHERCHES CLINIQUES DE MONTREALInventor: Yvan Guindon
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Publication number: 20100093770Abstract: 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: ApplicationFiled: April 14, 2008Publication date: April 15, 2010Inventors: Atsushi Shimazaki, Noriko Kawabata, Tomoko Kirihara, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7645763Abstract: 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: GrantFiled: February 22, 2005Date of Patent: January 12, 2010Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas
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Publication number: 20090258887Abstract: 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: ApplicationFiled: September 14, 2006Publication date: October 15, 2009Inventors: Raphael Beumer, Jochen Klock, Stefan Martin Stoeckli
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Publication number: 20090253665Abstract: 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: ApplicationFiled: June 16, 2009Publication date: October 8, 2009Inventors: Lauren Otsuki, Kenneth Widder, Howard C. Dittrich
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Publication number: 20090253718Abstract: 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 saturType: ApplicationFiled: April 25, 2007Publication date: October 8, 2009Applicants: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Technology LimitedInventors: Thomas Glanmor Davies, Michelle Dawn Garrett, Robert George Boyle, Ian Collins
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Publication number: 20090247557Abstract: 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: ApplicationFiled: April 2, 2009Publication date: October 1, 2009Inventors: Arvinder Dhalla, Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Vaibhav Varkhedkar, Jeff Zablocki
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Publication number: 20090233922Abstract: 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: ApplicationFiled: October 13, 2006Publication date: September 17, 2009Inventor: Min Zhuo
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Publication number: 20090233947Abstract: 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: ApplicationFiled: May 10, 2006Publication date: September 17, 2009Inventors: Tracy Bayliss, Rebecca Elizabeth Brown, Gregory John HollingWorth, A. Brian Jones
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Patent number: 7589075Abstract: 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: GrantFiled: January 13, 2002Date of Patent: September 15, 2009Assignee: Can-Fite Biopharma Ltd.Inventors: Pnina Fishman, Kamel Khalili
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Publication number: 20090203638Abstract: 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: ApplicationFiled: April 7, 2009Publication date: August 13, 2009Applicant: VDF FUTURECEUTICALS, INC.Inventors: Dusan Miljkovic, Jovan Hranisavljevic, Zbigniew Pietrzkowski
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Patent number: 7572800Abstract: 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: GrantFiled: February 25, 2003Date of Patent: August 11, 2009Assignee: Gilead Sciences, Inc.Inventors: Phillip A. Furman, George R. Painter, III, David W. Barry, Franck Rousseau
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Patent number: 7569575Abstract: 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: GrantFiled: May 8, 2003Date of Patent: August 4, 2009Assignee: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Patent number: 7569574Abstract: 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: GrantFiled: August 4, 2003Date of Patent: August 4, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
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Patent number: 7560450Abstract: 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: GrantFiled: November 18, 2003Date of Patent: July 14, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
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Publication number: 20090131458Abstract: 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: ApplicationFiled: February 15, 2008Publication date: May 21, 2009Applicant: SmithKline Beecham CorporationInventors: Linos Lazarides, Stephen Allan Smith, Richard Stocker, Colin Jack Theobald
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Publication number: 20090111836Abstract: 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: ApplicationFiled: October 31, 2007Publication date: April 30, 2009Inventors: Wangfun Fong, Xiaoling Shen, Guangying Chen, Guoyuan Zhu, Chikeung Wan, Kaiwing Tse
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Publication number: 20090099213Abstract: 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 gType: ApplicationFiled: October 25, 2005Publication date: April 16, 2009Applicants: Astex Therapeutics Limited, The Institute of Cancer Research: Royal Cancer Hospital, Cancer Research Techology LimitedInventors: 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
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Publication number: 20090069289Abstract: 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: ApplicationFiled: August 22, 2008Publication date: March 12, 2009Applicant: PHARMACOPEIA, INC.Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Ansari Nasrin
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8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
Patent number: 7501426Abstract: 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: GrantFiled: February 17, 2005Date of Patent: March 10, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Mohammad Tadayyon, Leo Thomas -
Publication number: 20090062314Abstract: 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: ApplicationFiled: August 4, 2008Publication date: March 5, 2009Applicant: Inotek Pharmaceuticals CorporationInventors: Prakash Jagtap, Csaba Szabo, Andrew L. Salzman
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Patent number: 7495004Abstract: 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: GrantFiled: May 20, 2003Date of Patent: February 24, 2009Assignee: Glaxo Group LimitedInventors: Sharon Davis Boggs, Jon Loren Collins, Adam Fivush, Eugene Lee Stewart, Timothy Mark Willson
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Patent number: 7495006Abstract: 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: GrantFiled: December 8, 2005Date of Patent: February 24, 2009Assignee: Emory UniversityInventors: Dennis C. Liotta, Shuli Mao, Michael Hager
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Publication number: 20090048275Abstract: 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: ApplicationFiled: August 28, 2008Publication date: February 19, 2009Inventors: Marie G. Beauchamps, Louise Michelle Cameron, Robert Hilgraf, Mohit Atul Kothare, Manohar T. Saindane, Jean Xu
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Publication number: 20090048203Abstract: This invention relates to compounds of Formula (I): and their use in the treatment of bacterial infections.Type: ApplicationFiled: October 13, 2005Publication date: February 19, 2009Inventors: Marta Cavero-Tomas, Madhu Gowravaram, Hoan Huynh, Haihong Ni, Suzanne Stokes
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Publication number: 20090028895Abstract: 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: ApplicationFiled: November 29, 2007Publication date: January 29, 2009Inventor: Walter P. Smith
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Patent number: 7452894Abstract: 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 proType: GrantFiled: January 10, 2002Date of Patent: November 18, 2008Assignee: Vernalis Research LimitedInventors: Roger John Gillespie, Joanne Lerpiniere, Claire Elizabeth Dawson, Suneel Gaur, Robert Mark Pratt, Gemma Caroline Stratton, Scott Murray Weiss
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Publication number: 20080262002Abstract: 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: ApplicationFiled: January 26, 2006Publication date: October 23, 2008Applicant: UNIVERSITY OF MANITOBAInventors: Wilfred Wayne Lautt, Zhi Ming
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Publication number: 20080262003Abstract: 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: ApplicationFiled: April 14, 2008Publication date: October 23, 2008Applicant: Southern Research Institute Office of Commercialization and intellectual PropInventor: Bo Xu
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Publication number: 20080262001Abstract: 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: ApplicationFiled: April 14, 2008Publication date: October 23, 2008Applicant: Adenosine Therapeutics, LLCInventors: Onno Kranenburg, Jarmila van der Bilt, Inne Borel Rinkes, Jayson M. Rieger
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Publication number: 20080242683Abstract: 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: ApplicationFiled: March 13, 2006Publication date: October 2, 2008Inventors: Robin Alec Fairhurst, Roger John Taylor
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Patent number: 7423041Abstract: 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: GrantFiled: March 23, 2007Date of Patent: September 9, 2008Assignee: Endacea, Inc.Inventors: Constance Wilson, John J. Partridge
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Patent number: 7420056Abstract: 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: GrantFiled: March 14, 2007Date of Patent: September 2, 2008Assignee: Gruenenthal GmbHInventors: Sven Kuehnert, Stefan Oberboersch, Corinna Sundermann, Michael Haurand, Ruth Jostock, Klaus Schiene, Thomas Tzschentke, Thomas Christoph, Dagmar Kaulartz, Saskia Zemolka
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Publication number: 20080187561Abstract: 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: ApplicationFiled: December 21, 2007Publication date: August 7, 2008Inventors: Mona DHALIWAL, Girish Karanth, Romi Barat Singh
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Patent number: 7407955Abstract: 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: GrantFiled: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
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Patent number: 7388002Abstract: 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: GrantFiled: November 9, 2005Date of Patent: June 17, 2008Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Yahya El-Kattan, Minwan Wu