The Ring Nitrogen Is Bonded Directly To Nonshared Ring Carbons Of The Five-membered Hetero Ring (e.g., Isoindole, Etc.) Patents (Class 514/416)
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Publication number: 20110217301Abstract: The present invention relates to a method for treating and screening for compounds for the treatment of sepsis. More specifically, the treatment and screening methods are based on the discovery that granzyme B containing platelets (GzmB-platelet) causes apoptosis by direct contact with cells.Type: ApplicationFiled: April 6, 2011Publication date: September 8, 2011Applicant: THE CHILDREN'S RESEARCH INSTUTEInventor: ROBERT J. FREISHTAT
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Publication number: 20110213005Abstract: The present invention relates to compounds that modulate ribosomal frameshifting and nucleic acid constructs for use in methods for identifying or validation such compounds. In particular, the present invention relates to the use of nucleic acid constructs to identify or validate compounds capable of modulating the efficiency of programmed ribosomal frameshifting and the use of said compounds to inhibit the replication or infectivity of viruses that employ programmed ribosomal frameshifting.Type: ApplicationFiled: August 13, 2009Publication date: September 1, 2011Inventors: Sergey V. Paushkin, Nikolai A. Naryshkin, Ellen Welch
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Patent number: 7999119Abstract: Compounds of general formula (I) wherein R is phenyl optionally substituted with one or more halo substituents; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.Type: GrantFiled: July 20, 2007Date of Patent: August 16, 2011Assignee: Oxagen LimitedInventors: Richard Edward Armer, Graham Michael Wynne, Colin Richard Dorgan, Peter David Johnson
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Patent number: 7981401Abstract: Described herein are diuretic condensation aerosols and methods of making and using them. Kits for delivering a condensation aerosol are also described. The diuretic aerosols typically comprise diuretic condensation aerosol particles that comprise a diuretic compound. In some variations the diuretic compound is selected from the group consisting of bumetanide, ethacrynic acid, furosemide, muzolimine, spironolactone, torsemide, triamterene, tripamide, BG 9928, and BG 9719. Methods of treating edema using the described aerosols are also provided. In general, the methods typically comprise the step of administering a therapeutically effective amount of diuretic condensation aerosol to a person with edema. The diuretic condensation aerosol may be administered in a single inhalation, or may be administered in more than one inhalation. Methods of forming a diuretic condensation aerosol are also described.Type: GrantFiled: February 2, 2007Date of Patent: July 19, 2011Assignee: Alexza Pharmaceuticals, Inc.Inventors: Nathan R. Every, Ron L. Hale, Amy T. Lu, Joshua D. Rabinowitz
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Patent number: 7981922Abstract: This invention relates to a process for synthesizing an amino acid derivative of a tripeptidomimetic, such as lisinopril. The invention also relates to a derivative of lisinopril, incorporating a amino acid moeity such as tryptophan at the P2? position.Type: GrantFiled: May 29, 2006Date of Patent: July 19, 2011Assignee: University of Cape TownInventors: Edward Sturrock, Aloysius Nchinda, Kelly Chibale
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Publication number: 20110172284Abstract: Described herein are methods for the identification or validation of compounds capable of causing ribosomal frameshifting and the use of said compounds to produce a stabilized SMN?Ex7 protein and treat Spinal Muscular Atrophy.Type: ApplicationFiled: August 13, 2009Publication date: July 14, 2011Inventors: Sergey V. Paushkin, Nikolai A. Naryshkin, Ellen Welch
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Publication number: 20110166155Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: January 6, 2011Publication date: July 7, 2011Inventors: Bradford VAN WAGENEN, Radhakrishnan UKKIRAMAPANDIAN, Joshua CLAYTON, Ian EGLE, James R. EMPFIELD, Methvin ISAAC, Fupeng MA, Abdelmalik SLASSI, Gary STEELMAN, Rebecca URBANEK, Sally WALSH
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Patent number: 7968578Abstract: The invention is directed to indole amide derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: April 23, 2007Date of Patent: June 28, 2011Assignee: Merck Frosst Canada Ltd.Inventors: Michael Boyd, John Colucci, Zhaoyin Wang
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Patent number: 7964628Abstract: This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.Type: GrantFiled: June 8, 2010Date of Patent: June 21, 2011Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Ashok Kumar Gangopadhyay, Vadlamudi V. S. V. Rao, Ravindra Dattatraya Gupte, Gopal Vishnu Gole, Asha Kulkarni-Almeida, Sridevi Krishnan, Radha Bhaskar Panicker, Eleanor Pinto De Souza
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Publication number: 20110144146Abstract: The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; X is a covalent bond or N—R2, CHR2, CHR2CH2, N or C—R2; Y is N—R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond oType: ApplicationFiled: October 14, 2005Publication date: June 16, 2011Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel
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Publication number: 20110144037Abstract: The presently disclosed and claimed inventive concepts include inhibitors of antiplasmin cleaving enzyme (APCE) and fibroblast activation protein alpha (FAP) which can be used in various therapies related to disorders of fibrin and ?2-antiplasmin and abnormal cell proliferation. The presently disclosed and claimed inventive concepts also include substrates of APCE and FAP, which may be used, for example, in screening methods for identifying such inhibitors. The presently disclosed and claimed inventive concepts further include, but are not limited to, methods of treating or inhibiting atherosclerosis and thrombus disorders by altering the ratios of types of plasma ?2-antiplasmin and to methods of treating conditions involving abnormal cell proliferation such as cancers.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Inventors: Patrick A. McKee, Kenneth W. Jackson, Kyung N. Lee, Victoria J. Christiansen
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Publication number: 20110130383Abstract: Use of compounds of general formula (1) and pharmacologically acceptable salts and prodrugs thereof: Formula (1) wherein A and B are CH2 or CH2CH2, R1 is hydrogen, alkyl, cycloalkyl, aryl, aralkyl or heteroaralkyl, R2, R3 and R4 are selected from hydrogen, alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl or cyano; X is R5CO, R5SO2, R5R7NCO, R5R7NSO2, R5SO2NR7CO or CO2R8, Y is R6CO, R6SO2, R6R7NCO, R6R7NSO2, R6SO2NR7CO or CO2R8, R5 and R6 are hydrogen, alkyl, aryl, aralkyl, heteroaryl or heteroaralkyl, R7 is hydrogen, alkyl, aryl or aralkyl, and R8 is alkyl, aryl, aralkyl, alkoxyalkyl, heteroaryl or heteroarylalkyl, provided that when X is R5CO or R5SO2, then Y is not R6CO, R6SO2 or R6R7NCO, in the manufacture of a medicament for the prophylaxis or treatment of inflammatory or immunological disease.Type: ApplicationFiled: September 28, 2007Publication date: June 2, 2011Applicant: LECTUS THERAPEUTICS LIMITEDInventors: Geoff Lawton, Roland Kozlowski, Dayle Hogg
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Publication number: 20110130436Abstract: This invention provides novel compounds, and pharmaceutically acceptable derivatives thereof, that are useful as caspase inhibitors. These compounds have the general formula I: where R1, R2, and R3 are as described herein, Ring A contains zero to two double bonds, each X is independently selected from nitrogen or carbon, at least one X in Ring A is a nitrogen, Ring A is optionally substituted as described, and may be fused to a saturated or unsaturated five to seven membered ring containing zero to three heteroatoms, and provided that when X3 is a carbon, a substituent on X3 is attached by an atom other than nitrogen.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Julian M. C. Golec, Paul S. Charifson, Jean-Damien Charrier, Hayley Binch
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Publication number: 20110124679Abstract: Methods of treating or suppressing oxidative stress diseases including mitochondrial diseases, impaired energy processing disorders, neurodegenerative diseases and diseases of aging are disclosed, as well as compounds useful in the methods of the invention, such as 2-substituted-p-quinone derivatives as disclosed herein.Type: ApplicationFiled: March 4, 2009Publication date: May 26, 2011Inventors: Andrew W. Hinman, Kieron E. Wesson, Orion D. Jankowski, Paul Mollard, William D. Shrader, Christpher R. Cornell
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Publication number: 20110124622Abstract: The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: July 1, 2009Publication date: May 26, 2011Applicant: Genentech, Inc.Inventors: Emanuela Gancia, Robert Andrew Heald, Philip Jackson, Stephen Price
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Publication number: 20110124645Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.Type: ApplicationFiled: January 20, 2011Publication date: May 26, 2011Inventors: George W. MULLER, Hon-Wah Man, Weihong Zhang
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Publication number: 20110124702Abstract: Provided are compositions and methods for preparation and administration of an oral nanosuspension of a poorly soluble drug with improved bioavailability. The method is optimized through microfluidization process with water soluble polymeric excipients in the absence of surfactants.Type: ApplicationFiled: November 9, 2010Publication date: May 26, 2011Inventors: Ming J. CHEN, Ho-Wah Hui, Thomas Lee, Paul Kurtulik, Sekhar Surapaneni
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Publication number: 20110118303Abstract: The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity. In a first embodiment, the present invention relates to compounds derived from taurine, in which taurine is bound directly by means of an amide bond or through an spacing group, to a compound selected from the group of non-steroidal anti inflammatory compounds, cited as derived from taurine presenting the Formula (I): in which R means the component with non-steroidal anti inflammatory activity. In a second embodiment, the invention provides a process for obtaining the compounds of Formula (I) by reaction of taurine with a compound belonging to the group of non-steroidal anti inflammatory (NSAIs), in order to obtain a compound derived from taurine by direct bond or through a spacing group of the taurine to the NSAI. The invention also relates to the pharmaceutical compositions comprising at least one compound derived from taurine presenting non-steroidal anti inflammatory activity.Type: ApplicationFiled: April 9, 2009Publication date: May 19, 2011Applicants: EMS S.A., Universidade Estadual Paulista Julio De Mesquita Filho - UNESPInventors: Ednir de Oliveira Vizioli, Chung Man Chin, Renato Farina Menegon, Lorena Blau, Jean Leandro Dos Santos, Maria do Carmo Longo
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Patent number: 7943657Abstract: Imidoalkancarboxylic acids of formula: are described, wherein A, X and M are as defined in the application, said acids being in a crystalline form which in contact with water gives rise to crystals having sizes lower than 30 micron.Type: GrantFiled: February 29, 2008Date of Patent: May 17, 2011Assignee: Solvay Solexis S.p.A.Inventors: Ugo Piero Bianchi, Roberto Garaffa
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Patent number: 7939557Abstract: The present application describes isoindoles and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful inhibitors of VEGFR.Type: GrantFiled: April 19, 2007Date of Patent: May 10, 2011Assignee: Nova Southeastern UniversityInventors: Appu Rathinavelu, Nagarajan Pattabiraman, Jayalakshmi Sridhar, Sivanesan Dakshanamurthy
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Publication number: 20110105501Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: ApplicationFiled: October 12, 2007Publication date: May 5, 2011Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Publication number: 20110104144Abstract: Methods of treating cutaneous lupus in a human are disclosed. Specific methods encompass the administration of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, 4-(amino)-2-(2,6-dioxo(3-piperidyl))-isoindoline-1,3-dione (ACTIMID™), 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione (REVLIMID®), or cyclopropyl 2-[(1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl]-3-oxoisoindolin-4-yl}carboxamide, alone or alternatively, in combination with a second active agent.Type: ApplicationFiled: January 11, 2011Publication date: May 5, 2011Applicant: CELGENE CORPORATIONInventors: Jerome B. Zeldis, Patricia E.W. Rohane, Peter H. Schafer
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Patent number: 7935832Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl-; and any of said C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R3 represents hydrogen, fluorine or methyl; or R2 and R3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor.Type: GrantFiled: March 20, 2008Date of Patent: May 3, 2011Assignee: Glaxo Group LimitedInventors: Robert James Gleave, David George Hubert Livermore, Daryl Simon Walter
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Patent number: 7915249Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.Type: GrantFiled: January 25, 2006Date of Patent: March 29, 2011Assignee: Janssen Pharmaceutical NVInventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20110059992Abstract: This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.Type: ApplicationFiled: November 11, 2010Publication date: March 10, 2011Applicants: ASTRAZENECA AB, ASTEX THERAPEUTICS LTD.Inventors: James Arnold, Phil Edwards, Mark Sylvester, Stefan Berg, Jörg Holenz, Annika Kers, Karin Kolmodin, Laszlo Rakos, Liselotte Öhberg, Rotticci Didier, Gianni Chessari, Miles Congreve, Christopher Murray, Sahil Patel
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Publication number: 20110059999Abstract: The invention relates to compounds which have an affinity for the ? opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.Type: ApplicationFiled: September 22, 2010Publication date: March 10, 2011Applicant: GRÜNENTHAL GMBHInventors: Sven Frormann, Saskia Zemolka, Klaus Linz, Werner Englberger, Fritz Theil
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Patent number: 7897601Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, is useful in treating diseases, disorders, or conditions such as obesity, metabolic disorders, addiction, diseases of the central nervous system, cardiovascular disorders, respiratory disorders, and gastrointestinal disorders.Type: GrantFiled: January 16, 2007Date of Patent: March 1, 2011Assignees: Intervet, Inc., Intervet International B.V.Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Martin C. Clasby, Keith A. Eagen, Jack D. Scott, Yuguang Wang, Yan Xia, William J. Greenlee
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Patent number: 7893102Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.Type: GrantFiled: January 30, 2009Date of Patent: February 22, 2011Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Publication number: 20110039827Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: June 21, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
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Patent number: 7888382Abstract: For controlling the condition of type 2 diabetes, a pharmaceutical including a combination of mitiglinide, a pharmacologically acceptable salt thereof or a hydrate thereof and an ?-glucosidase inhibitor such as voglibose or acarbose, and a therapeutic method using the pharmaceutical are provided. The pharmaceutical according to the present invention has an extremely strong effect of decreasing a morning fasting blood glucose level, a postprandial blood glucose level and HbA1C of a patient with type 2 diabetes, and can improve glucose spike, insulin resistance and lipid metabolism.Type: GrantFiled: April 18, 2006Date of Patent: February 15, 2011Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Yuji Kiyono, Yoshio Okubo, Katsumi Hontani, Imao Mikoshiba, Kazuma Ojima
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Publication number: 20110034440Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: April 10, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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Publication number: 20110034461Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: sanofi-aventisInventors: Uwe HEINELT, Volkmar WEHNER, Matthias HERRMANN, Karl SCHOENAFINGER, Henning STEINHAGEN
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Publication number: 20110021505Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.Type: ApplicationFiled: March 30, 2010Publication date: January 27, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Karl RUDOLPHI, Martin MICHAELIS, Hans GUEHRING
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Patent number: 7863315Abstract: Provided herein are isolated compounds of formula I: processes for their preparation and isolation, as well as pharmaceutical compositions which comprise these therapeutic agents, and methods of use therefore the treatment and/or control of conditions associated with or mediated by effects of histone deacetylase.Type: GrantFiled: January 14, 2009Date of Patent: January 4, 2011Assignee: Shenzhen Chipscreen Biosciences, Ltd.Inventors: Xian-Ping Lu, Zhi-bin Li, Zhi-Qiang Ning
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Patent number: 7855223Abstract: The present invention is directed to a method for treating inflammatory arthritis in a mammal. The method typically comprises administering to an animal a therapeutically effective amount of at least one compound selected from indigo, isoindigo, indirubin or derivatives thereof, such as NATURA-? or NATURA. The present invention is further directed to pharmaceutical compositions that include a therapeutically effective amount of at least one compound of the invention, an anti-inflammatory arthritis agent and a pharmaceutically acceptable carrier.Type: GrantFiled: July 26, 2006Date of Patent: December 21, 2010Assignee: Natrogen Therapeutics International, Inc.Inventors: Ruihuan Chen, Simon K. Mencher, Allen Tsao, Xiao Mei Liu, Longgui Wang
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Publication number: 20100317674Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Inventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20100311745Abstract: Novel 1,3-dihydroisoindole derivatives of the formula (I), in which R1-R3 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: July 28, 2008Publication date: December 9, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
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Publication number: 20100298392Abstract: There is provided compounds of formula I, wherein R1 to R7 have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.Type: ApplicationFiled: July 12, 2007Publication date: November 25, 2010Applicant: ASTRAZENECA ABInventors: Annika Bjore, Jonas Bostrom, Ojvind Davidsson, Hans Emtenas, Ulrik Gran, Tommy Iliefski, Johan Kajanus, Roine Olsson, Lars Sandberg, Gert Strandlund, Johan Sundell, Zhong-Qing Yuan
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Publication number: 20100273853Abstract: A compound of formula (1) or a pharmaceutically acceptable derivative thereof, where R1, R2, R3, R4, R5, X and Y are as defined in the specification; corresponding processes for preparing; pharmaceutical compositions comprising; and medicinal uses of such compounds.Type: ApplicationFiled: August 16, 2007Publication date: October 28, 2010Inventors: Gerard Martin Paul Giblin, Mark Patrick Healy, David George Livermore, Helen Susanne Price, Martin Edward Swarbrick
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Publication number: 20100273772Abstract: Disclosed are compounds of Formula I: pharmaceutical compositions containing compounds of Formula I, and the use of compounds of Formula I to treat diseases and disorders including schizophrenia, paranoia, depression, manic-depressive illness and anxiety wherein W1-W5, X1-X4, Y, Z1-Z5, m, n, p, and R1-R6 in Formula I are defined in the specification.Type: ApplicationFiled: April 22, 2010Publication date: October 28, 2010Applicant: Wyeth LLCInventors: Steven Victor O'Neil, Benjamin Miller Zegarelli, Dane Mark Springer, David Zenan Li
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Patent number: 7820711Abstract: Described herein are methods for treating a subject suffering from a T-cell lymphoma by administering to the subject a pharmaceutical composition containing a therapeutically effective amount of a selective inhibitor of histone deacetylase 8. Also described herein are methods for treating a subject suffering from a T-cell lymphoma by administering to the subject a population of autologous T-cells that have been exposed to a selective HDAC8 inhibitor composition ex vivo.Type: GrantFiled: July 18, 2007Date of Patent: October 26, 2010Assignee: Pharmacyclics Inc.Inventors: Joseph J. Buggy, Sriram Balasubramanian
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Publication number: 20100267800Abstract: The invention encompasses novel N-alkyl-hydroxamic acid-isoindolyl compounds, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions for treatment or prevention of various diseases and disorders, for example, diseases associated with PDE4.Type: ApplicationFiled: February 12, 2010Publication date: October 21, 2010Inventors: Hon-Wah MAN, George W. Muller
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Publication number: 20100256114Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: June 17, 2010Publication date: October 7, 2010Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20100256161Abstract: This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.Type: ApplicationFiled: June 8, 2010Publication date: October 7, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi Lal, Ashok Kumar Gangopadhyay, Vadlamudi V.S.V Rao, Ravindra Dattatraya Gupte, Radha Bhaskar Panicker, Eleanor Pinto De Souza, Gopal Vishnu Gole, Asha Kulkarni-Almeida, Sridevi Krishnan
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Patent number: 7807706Abstract: Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.Type: GrantFiled: February 15, 2006Date of Patent: October 5, 2010Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James R. Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Publication number: 20100222363Abstract: New bicyclic derivatives of formula (I); wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as p38 kinase inhibitors.Type: ApplicationFiled: June 28, 2006Publication date: September 2, 2010Applicant: PALAU PHARMA, S.A.Inventors: Carmen Almansa Rosales, Marina Virgili Bernadó
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Publication number: 20100216782Abstract: This invention provides methods for treating, alleviating or reducing the incidence of a disease or condition comprising or arising from abnormal cell growth in a mammal, which comprise administering to the mammal a compound, salt, hydrate, tautomer or N-oxide according to formula (I): wherein R1 is hydroxy or hydrogen; R2 is hydroxyl, methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n.Type: ApplicationFiled: February 17, 2010Publication date: August 26, 2010Inventors: Gianni CHESSARI, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
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Patent number: 7781429Abstract: A vehicle for topical delivery which contains a liquid eutectic mixture of hydrophobic compounds.Type: GrantFiled: May 18, 2006Date of Patent: August 24, 2010Assignee: Alpharx Inc.Inventors: Joseph Schwarz, Michael Weisspapir
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Publication number: 20100210705Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl-; and any of said C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R3 represents hydrogen, fluorine or methyl; or R2 and R3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor.Type: ApplicationFiled: March 20, 2008Publication date: August 19, 2010Inventors: Robert James Gleave, David George Hubert Livermore, Daryl Simon Walter