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: 20130116204Abstract: Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed.Type: ApplicationFiled: December 21, 2010Publication date: May 9, 2013Applicant: Celgene CorporationInventors: Peter H. Schafer, Anthony J. Frank, Hon-Wah Man, Sai L. Shankar
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Publication number: 20130102626Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.Type: ApplicationFiled: September 14, 2012Publication date: April 25, 2013Inventors: Peter Wipf, Marie Celine Frantz
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Publication number: 20130072519Abstract: Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein.Type: ApplicationFiled: May 9, 2011Publication date: March 21, 2013Inventors: Edward Lee Conn, David Hepworth, Yingmei Qi, Benjamin Neil Rocke, Roger Benjamin Ruggeri, Yan Zhang
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Publication number: 20130059853Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.Type: ApplicationFiled: April 28, 2011Publication date: March 7, 2013Applicant: LEO PHARMA A/SInventors: Simon Feldbaek Nielsen, Anne Marie Horneman, Jesper Lau, Jens Christian Hojland Larsen
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Patent number: 8372864Abstract: The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof.Type: GrantFiled: January 26, 2010Date of Patent: February 12, 2013Assignee: SanofiInventors: Bernard Baudoin, Michel Evers, Arielle Genevois-Borella, Andreas Karlsson, Jean-Luc Malleron, Magali Mathieu
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Patent number: 8349885Abstract: The present invention relates to a composition for preserving cells, tissues and organs, comprising as an active ingredient indole and indazole compounds of formula (1), or a pharmaceutically acceptable salt or isomer thereof, which are effective for preventing injury of organs, isolated cell systems or tissues caused by cold storage, transplant operation or post-transplantation reperfusion; a preservation method; and a preparation method of the composition.Type: GrantFiled: June 27, 2012Date of Patent: January 8, 2013Assignee: LG Life Sciences Ltd.Inventors: Soon Ha Kim, Hyoung Jin Kim, Chul Woong Chung, Heui Sul Park, Hyo Shin Kwak, Sung Ho Kim, Jin Gu Park
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Patent number: 8314140Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.Type: GrantFiled: July 18, 2007Date of Patent: November 20, 2012Assignee: Antibe Therapeutics Inc.Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
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Publication number: 20120289505Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: December 30, 2010Publication date: November 15, 2012Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Publication number: 20120276087Abstract: Methods of treating, preventing, or managing autoimmune inflammatory diseases and disorders including but not limited to spondylitis, juvenile rheumatoid arthritis, psoriasis, psoriatic arthritis, osteoarthritis, ankylosing spondylitis, and rheumatoid arthritis by the administration of phosphodiesterase 4 (PDE4) inhibitors in combination with other therapeutics are disclosed. Pharmaceutical compositions, dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: April 27, 2012Publication date: November 1, 2012Inventors: Peter H. SCHAFER, Anita GANDHI, Lori CAPONE
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Patent number: 8288406Abstract: 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: GrantFiled: September 22, 2010Date of Patent: October 16, 2012Assignee: Gruenenthal GmbHInventors: Sven Frormann, Saskia Zemolka, Klaus Linz, Werner Englberger, Fritz Theil
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Patent number: 8283374Abstract: The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I via 3-hydroxy-2,3-dihydro-1H-isoindol-1-one derivatives or 3-(2-carbamoylphenyl)-acrylic ester derivatives as intermediates, to a process for optical resolution, and to intermediates of the process according to the invention.Type: GrantFiled: April 2, 2009Date of Patent: October 9, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Gerrit Schubert, Joerg Rieke-Zapp, Johannes Keil, Heinz-Werner Kleemann, Reda Hanna, Bao-Guo Huang, Xiao-Dong Wu, Yves Gouraud
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Publication number: 20120251545Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.Type: ApplicationFiled: October 12, 2011Publication date: October 4, 2012Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueron Navarro, Alison Jo-Anne Woolford
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Patent number: 8277807Abstract: 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: GrantFiled: October 12, 2007Date of Patent: October 2, 2012Assignee: Astex Therapeutics LimitedInventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Publication number: 20120245142Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: July 6, 2010Publication date: September 27, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto
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Publication number: 20120238567Abstract: The present invention relates to compounds having pharmacological activity towards the sigma (?) receptor, and more particularly to some 4, 5, 6, 7 tetrahydrobenzo[b]thiophene derivatives, wherein n is selected from 0, 1, 2, 3 or 4; m is selected from 0, 1 or 2; the dotted line represents either a single or a double bond; to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis.Type: ApplicationFiled: May 30, 2012Publication date: September 20, 2012Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Jordi CORBERA-ARJONA, Daniel MARTINEZ-OLMO, David VANO-DOMENECH
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Patent number: 8268878Abstract: 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 11, 2011Date of Patent: September 18, 2012Assignee: Oxagen LimitedInventors: Richard Edward Armer, Graham Michael Wynne, Colin Richard Dorgan, Peter David Johnson
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Patent number: 8258175Abstract: A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; R1 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; R2 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; R3 is hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R4-R7, is used to represent groups R4, R5, R6 and R7 which are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, hType: GrantFiled: August 26, 2005Date of Patent: September 4, 2012Assignee: Cancer Research Technology LimitedInventors: Hendrika Maria Gerarda Willems, Per Kallblad, Ian Robert Hardcastle, Roger John Griffin, Bernard Thomas Golding, John Lunec, Martin E. M. Noble, David R. Newell, Alan H. Calvert
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Patent number: 8217041Abstract: The present invention makes reference to new indene derivatives with general formula (I), as well as to their preparation procedures, their application as medicament and the pharmaceutical compositions containing them. The new compounds of formula (I) show affinity for 5-HT6 receptors and are, therefore, effective for treating diseases mediated by these receptors.Type: GrantFiled: November 7, 2006Date of Patent: July 10, 2012Assignee: Laboratories del Sr. Esteve, S.A.Inventors: Maria de las Ermitas Alcalde-Pais, Jordi Frigola-Constansa, Joerg Holenz, Ramon Merce-Vidal, Maria de les Neus Mesquida-Estevez, Sara Lopez-Perez
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Publication number: 20120172392Abstract: Compositions and methods are disclosed for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1). The compounds disclosed are amine-containing and amide-containing compounds. The compounds and compositions are useful for treatment of diseases, including inflammation, inflammatory diseases and autoimmune disorders.Type: ApplicationFiled: March 7, 2012Publication date: July 5, 2012Inventors: LUISA M. SALTER-CID, ERIC Y. WANG, MARY T. MACDONALD, JINGJING ZHAO
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Publication number: 20120157494Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Inventors: Ralph New Harris, III, David Bruce Repke, Keith A.M. Walker
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Publication number: 20120149716Abstract: Methods of treating, preventing, and managing tuberculosis and other related disorders are disclosed. The methods comprise the administration of a PDE4 modulator, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, stereoisomer, or prodrug thereof, optionally in combination with a second active agent and/or other conventional therapies. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in such methods are also disclosed.Type: ApplicationFiled: February 9, 2010Publication date: June 14, 2012Inventor: Jerome B. Zeldis
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Publication number: 20120141491Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.Type: ApplicationFiled: August 9, 2010Publication date: June 7, 2012Applicant: University of Florida Research Foundation Inc.Inventors: William A. Dunn, Debra Everton Akin, Brian Keith Law
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Patent number: 8188139Abstract: The present invention relates to compounds of formula I wherein R1, R2, and are defined in the specification and to pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: April 13, 2009Date of Patent: May 29, 2012Assignee: Hoffman-La Roche Inc.Inventors: Synese Jolidon, Robert Narquizian, Roger David Norcross, Emmanuel Pinard
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Patent number: 8183279Abstract: 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: GrantFiled: July 28, 2008Date of Patent: May 22, 2012Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
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Publication number: 20120122842Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: Abbott LaboratoriesInventors: Michael L. Curtin, Bryan K. Sorensen, Howard R. Heyman, Richard F. Clark, Kevin R. Woller, Omar J. Shah, Michael Michaelides, Chris Tse, Anil Vasudevan, Helmut Mack, Todd M. Hansen, Ramzi Sweis, Marina A. Pliushchev
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Patent number: 8158672Abstract: 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 20, 2011Date of Patent: April 17, 2012Assignee: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Publication number: 20120088790Abstract: The present invention relates to phenalkylamine derivatives of the formula (I) or (II) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 10, 2011Publication date: April 12, 2012Applicants: Abbott GmbH & Co. KG, Abbott LaboratoriesInventors: Frauke Pohlki, Udo Lange, Wilhelm Amberg, Michael Ochse, Berthold Behl, Charles W. Hutchins, Wilfried Hornberger, Mario Mezler
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Patent number: 8153638Abstract: 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: August 23, 2010Date of Patent: April 10, 2012Assignee: 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: 20120083495Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: ApplicationFiled: December 5, 2011Publication date: April 5, 2012Applicants: SCIENCE APPLICATIONS INTERNATIONAL INC. (SAIC), ALBANY MOLECULAR RESEARCH, INC., DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Publication number: 20120071503Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.Type: ApplicationFiled: March 18, 2011Publication date: March 22, 2012Applicant: Sanford-Burnham Medical Research InstituteInventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique
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Patent number: 8133914Abstract: The invention relates to novel compounds containing a carboxylic acid head group. The invention further provides compositions containing the novel compounds, a particulate solid and an organic medium or water.Type: GrantFiled: September 7, 2007Date of Patent: March 13, 2012Assignee: Lubrizol LimitedInventor: Dean Thetford
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Publication number: 20120052118Abstract: The present invention provides an apparatus and process for making softgel capsules having incorporated therein other solid dosage forms selected from the group consisting of pellets, smaller capsules, smaller tablets, sustained release solid dosage forms, immediate release solid dosage forms, extended release solid dosage forms and zero order release solid dosage forms, said apparatus comprising: (a) two spreader boxes; (b) two casting drums; (c) a pair of rotary dies having means for suction; (d) a liquid fill system; (e) a wedge for heating gelatine ribbons and feeding said fill; and (f) two lateral dispensing devices said lateral dispensing devices including hoppers having said solid dosage forms, channelguides for transporting said solid dosage forms and a grasping claw for dispensing said solid dosage form into the softgel pocket formed in the rotary dies.Type: ApplicationFiled: July 18, 2011Publication date: March 1, 2012Inventors: Carlos Salazar Altamar, Gustavo Anaya, Braulio Teran, Newman Aguas Navarro, Willmer Herrera
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Publication number: 20120040986Abstract: This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: August 11, 2011Publication date: February 16, 2012Inventors: Bernd RIEDL, Jacques DUMAS, Uday KHIRE, Timothy B. LOWINGER, William J. SCOTT, Roger A. SMITH, Jill E. WOOD, Mary-Katherine MONAHAN, Reina NATERO, Joel RENICK, Robert N. SIBLEY
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Publication number: 20120034321Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: ApplicationFiled: October 18, 2011Publication date: February 9, 2012Inventor: David S. Garvey
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Publication number: 20120034270Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.Type: ApplicationFiled: October 16, 2009Publication date: February 9, 2012Applicant: Akaal Pharma Pty LtdInventors: Damian W. Grobelny, Gurmit S. Gill
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Patent number: 8110681Abstract: Compounds of Formula (I) or (II) useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: GrantFiled: March 13, 2007Date of Patent: February 7, 2012Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Albany Molecular Research, Inc., Science Applications International Inc. (SAIC)Inventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Publication number: 20120028955Abstract: In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: October 10, 2011Publication date: February 2, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20120028971Abstract: The present application relates to novel alkylcarboxylic acids having an oxo-substituted azaheterocyclic partial structure, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: February 24, 2010Publication date: February 2, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Thomas Lampe, Michael Hahn, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Stefan Heitmeier, Nils Griebenow, Sherif El Sheikh, Volkhart Min-Jian Li, Eva-Maria Becker, Friederike Stoll, Andreas Knorr
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Patent number: 8101648Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydrogen; R2 is hydroxy or methoxy; 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 oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.Type: GrantFiled: April 13, 2006Date of Patent: January 24, 2012Assignee: Astex Therapeutics, Ltd.Inventors: Gianni Chessari, Miles Stuart Congreve, Eva Figueroa Navarro, Martyn Frederickson, Christopher Murray, Alison Jo-Anne Woolford, Maria Grazia Carr, Michael Alistair O'Brien, Andrew James Woodhead, Robert Downham, Theresa Rachel Phillips
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Publication number: 20110319411Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: December 8, 2009Publication date: December 29, 2011Applicant: Sirtis Pharmaceuticals, Inc.Inventors: Chi B. Vu, Lauren Mcpherson, Pui Yee Ng, Charles Blum
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Publication number: 20110306624Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: February 3, 2010Publication date: December 15, 2011Inventors: Songnian Lin, Xibin Liao, Edward Metzger, Emma R. Parmee, Sheryl D. Debenham
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Patent number: 8076369Abstract: 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: GrantFiled: February 12, 2010Date of Patent: December 13, 2011Assignee: Celgene CorporationInventors: Hon-Wah Man, George W. Muller
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Publication number: 20110301208Abstract: Novel classes of viral and fungal inhibitors are disclosed. These compounds are useful in treating, preventing, and/or ameliorating viral infections such as, for example, Hepatitis C Virus, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus, and fungal infections such as, for example, candidiasis.Type: ApplicationFiled: September 23, 2009Publication date: December 8, 2011Applicants: WICHITA STATE UNIVERSITY, GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, William C. Groutas, Brent E. Korba
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Publication number: 20110275630Abstract: Compounds having the formula: are useful for inhibiting protein kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: November 3, 2010Publication date: November 10, 2011Applicant: ABBOTT LABORATORIESInventors: Mark Matulenko, Tammie Jinkerson, Brian S. Brown, Wilfried Braje, Michael Curtin, Howard Robin Heyman, Victoria Scott, Karen Kage, Steven Cassar, Anil Vasudevan
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Publication number: 20110269716Abstract: The invention relates to antioxidant substituted isoindoline nitroxide compounds and their use in methods of treating or preventing diseases or disorders related to oxidative stress, methods of reducing oxidative stress and methods of protecting a subject from oxidative stress upon exposure to ionising radiation. Pharmaceutical compositions comprising the antioxidant compounds are also described.Type: ApplicationFiled: September 30, 2009Publication date: November 3, 2011Applicant: Queensland University of TechnologyInventors: Steven Bottle, Kathryn Fairfull-Smith, Farina Schill
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Patent number: 8044089Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: GrantFiled: November 1, 2010Date of Patent: October 25, 2011Assignee: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
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Patent number: 8039506Abstract: The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.Type: GrantFiled: December 17, 2007Date of Patent: October 18, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata
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Patent number: 8034806Abstract: In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: October 31, 2008Date of Patent: October 11, 2011Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20110245210Abstract: Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-?) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.Type: ApplicationFiled: June 3, 2011Publication date: October 6, 2011Inventors: Nigel H. Greig, Harold Holloway, Arnold Brossi, Xiaoxiang Zhu, Tony Giordano, Qian-sheng Yu, William D. Figg
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Patent number: 8030343Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with an ?-(3,4-disubstituted phenyl)alkyl group and in the 4- and/or 5-position with a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF? and phosphodiesterase. A typical embodiment is 2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4,5-diaminoisoindoline-1,3-dione.Type: GrantFiled: October 14, 2003Date of Patent: October 4, 2011Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller