Bicyclo Ring System Which Is Isoindole (including Hydrogenated) Patents (Class 546/277.1)
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Publication number: 20110318266Abstract: Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.Type: ApplicationFiled: August 24, 2009Publication date: December 29, 2011Inventor: John A. McCauley
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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: 20110319426Abstract: The present invention relates to novel compounds of formula (I) and their pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Downs syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: September 6, 2011Publication date: December 29, 2011Applicant: ASTRAZENECA ABInventors: Jörg HOLENZ, Sofia KARLSTRÖM, Karin KOLMODIN, Johan LINDSTRÖM, Laszlo RAKOS, Didier ROTTICCI, Peter SÖDERMAN, Britt-Marie SWAHN, Stefan VON BERG
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Publication number: 20110312976Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2010Publication date: December 22, 2011Applicant: MSD K.K.Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
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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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Publication number: 20110281894Abstract: The present invention relates to a hemifumarate salt of the compound (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Downs syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: May 11, 2011Publication date: November 17, 2011Applicant: ASTRAZENECA ABInventors: Per-Olov Bergström, Anna Minidis, Robert Ulf Johan Stranne, Mikael Wernersson
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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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Patent number: 8053039Abstract: The present invention is directed towards polymerizable dichroic azo dyes comprising azo-chromophores having at least one standard mesogenic ring system attached to said chromophores and at least one polymerizable group leading to dyes having sufficient solubilty and a very high order parameter.Type: GrantFiled: March 23, 2004Date of Patent: November 8, 2011Assignee: Rolic AGInventors: Thomas Peglow, Franco Moia, Zoubair Mohammed Cherkaoui, Mario Schwab
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Publication number: 20110245247Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: March 28, 2011Publication date: October 6, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker
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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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Publication number: 20110243844Abstract: Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.Type: ApplicationFiled: August 24, 2009Publication date: October 6, 2011Inventor: John A. McCauley
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Publication number: 20110245232Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: March 25, 2011Publication date: October 6, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker, Jayne Froggett
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Patent number: 8030334Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.Type: GrantFiled: June 26, 2009Date of Patent: October 4, 2011Assignee: Novartis AGInventors: Christopher Adams, Qi-Ying Hu, Leslie Wighton McQuire, Julien Papillon
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Publication number: 20110237802Abstract: The present application relates to lenalidomide salts and solvates, and processes for the preparation thereof.Type: ApplicationFiled: May 17, 2011Publication date: September 29, 2011Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Srinivasulu Rangineni, Nagakiran Duggirala, Vamsi Krishna Mudapaka, Rajasekhar Kadaboina, Veerender Murki, Amarendhar Manda, Venkata Rao Badisa, Naresh Vemula, Rama Seshagiri Rao Pulla
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Publication number: 20110223611Abstract: Novel conjugates and immunogens derived from lenalidomide and antibodies generated by these immunogens are useful in immunoassays for the quantification and monitoring of thalidomide and lenalidomide in biological fluids.Type: ApplicationFiled: March 12, 2010Publication date: September 15, 2011Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Alexander Volkov, Howard Sard, Vishnumurthy Hegde
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Patent number: 8008324Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: March 6, 2008Date of Patent: August 30, 2011Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20110201643Abstract: Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors.Type: ApplicationFiled: March 12, 2009Publication date: August 18, 2011Applicant: 4SC AGInventors: Thomas Maier, Thomas Beckers, Christian Hesslinger
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Publication number: 20110196150Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: February 10, 2011Publication date: August 11, 2011Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Patent number: 7989453Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: December 20, 2007Date of Patent: August 2, 2011Assignee: AEterna Zentaris GmbHInventors: Peter Emig, Gerald Bacher, Dietmar Reichert, Silke Basner, Beate Aue, Bernd Nickel, Eckhard Gunther
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Publication number: 20110124663Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. 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: November 23, 2010Publication date: May 26, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
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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: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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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: 20110060010Abstract: The present invention provides a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione, a solvate thereof, a process for preparing the same and use in the preparation of a medicament for treating diseases or physiological abnormities by inhibiting inflammatory factors or angiogenesis. The water-solubility of the pharmaceutically acceptable strong acid salts of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione is quite higher than that of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione. The present invention also provides polymorphs of a pharmaceutically acceptable strong acid salt of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)piperidine-2,6-dione and a solvate thereof.Type: ApplicationFiled: September 13, 2010Publication date: March 10, 2011Applicants: TIANJIN HEMAY BIO-TECH CO., LTD, TIANJIN MICHELE SCI-TECH DEVELOPMENT CO., LTDInventor: Hesheng Zhang
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Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Publication number: 20110009428Abstract: The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C-4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH?NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Applicant: N.V. OrganonInventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
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Publication number: 20100331346Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: December 23, 2008Publication date: December 30, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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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: 20100305162Abstract: The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): and salts thereof. The invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.Type: ApplicationFiled: August 12, 2010Publication date: December 2, 2010Inventors: Raja Khalifah, Roland Keilitz, Christoph Koellner, Thorsten Degenhardt, Stephen Robert Brand
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Publication number: 20100298378Abstract: The invention relates to aryl-substituted polycyclic amines of formula I, especially bicyclic amines, and to the physiologically tolerated salts and physiologically functional derivatives thereof; where the symbols and radicals are explained in the description, as well as to pharmaceutical compositions containing them and to methods of treatment using them.Type: ApplicationFiled: July 29, 2010Publication date: November 25, 2010Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Lothar SCHWINK, Siegfried STENGELIN, Matthias GOSSEL, Gerhard HESSLER, Petra LENNIG
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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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Publication number: 20100267712Abstract: Disclosed is a compound of Formula (I) in which W and R1-R6 are defined herein. Also disclosed is a method of treating spinal muscular atrophy, 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 directly or indirectly by mutation or frameshift.Type: ApplicationFiled: September 26, 2008Publication date: October 21, 2010Applicants: Human Services, Science Applications International Coporation Saic, Albany Molecular Research, Inc.,Inventors: Jill E. Heemskerk, John M. McCall, Keith D. Barnes
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Publication number: 20100261758Abstract: Compounds of Formula (I) wherein R1 is aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R2 is defined heterocyclyl, R3 is alkyl, aryl, cyclohexyl or heterocyclyl, or (C1-4)alkyl substituted by aryl, cyclohexyl or heterocyclyl, R4 is H or alkyl, or R3 and R4 together with the carbon atom to which they are attached are cycloalkyl fused with aryl, and their use as pharmaceuticals.Type: ApplicationFiled: March 28, 2007Publication date: October 14, 2010Applicant: NOVARTIS AGInventors: Luca Arista, Klemens Hogenauer, Niko Schmiedeberg, Gudrun Werner, Herbert Jaksche
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Publication number: 20100256144Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.Type: ApplicationFiled: June 26, 2008Publication date: October 7, 2010Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Adreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Publication number: 20100234350Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 14, 2009Publication date: September 16, 2010Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Wolin Huang, Charles K. Marlowe, Kim A. Kane-McGuire, Hans-Michael Jantzen, David M. Sedlock
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Publication number: 20100222358Abstract: Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: ApplicationFiled: March 2, 2010Publication date: September 2, 2010Applicant: ABBOTT LABORATORIESInventors: Marlon D. Cowart, Chen Zhao, Minghua Sun, Lawrence A. Black, Guo Zhu Zheng, Robert J. Gregg, Geoff G.Z. Zhang, Ahmad Y. Sheikh, Xiaochun Lou, Rodger F. Henry, David M. Barnes, Lawrence Kolaczkowski, Anthony R. Haight, Sou-Jen Chang, Steven J. Wittenberger, Michael G. Fickes
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Publication number: 20100184762Abstract: The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, —C1-20-alkyl, —C2-20-alkenyl, —C2-20-alkinyl, —C5-6-cykloalkyl, aryl, aralkyl, adamantyl, heterocyclic, hydroxyl, hydroxyalkyl, Or —N—(R1, R2) group; n is 0, 1, 2, 3, or 4; R1 and R2 may each be independently hydrogen, straight or branching alkyl, cyclo-alkyl, aryl, aralkyl, heterocyclic group, wherein each is un-substituted or halogen substituted; or R1 and R2 together with the nitrogen in between them form a 5 or 6 member ring; A is a single bond, —O—, —S—, —CH2-, or —NH—; Y is O or S; Z is O or S; R? and R? are each independently methyl, ethyl, isopropyl, isobuthyl, sec-butyl or terc-butyl; with the restriction that: X(n) cannot all be fluorine, and A be a single bond, and Y, as well as Z be O, and R?, as well as R? bType: ApplicationFiled: June 20, 2008Publication date: July 22, 2010Applicant: AVIDIN KFTInventors: Laszlo Puskas, Liliana Feher, Eszter Molnar
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Publication number: 20100119479Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.Type: ApplicationFiled: October 14, 2009Publication date: May 13, 2010Applicant: INTERMUNE, INC.Inventors: BRAD BUCKMAN, VLADIMIR SEREBRYANY, SCOTT SEIWERT, LEONID BEIGELMAN, ANTITSA STOYCHEVA
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Publication number: 20100111900Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: October 30, 2009Publication date: May 6, 2010Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
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Patent number: 7696231Abstract: The present invention is related to the use of oxindole hydrazide derivatives of formula (I) for the treatment and/or prevention of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of oxindole hydrazide derivatives of formula (I) to modulate, notably to inhibit the activity of PTPs, in particular of PTP1B, TC-PTP, SHP and GLEPP-1. The present invention is furthermore related to novel oxindole hydrazide derivatives and method of preparation thereof.(I).Type: GrantFiled: October 24, 2002Date of Patent: April 13, 2010Assignee: Laboratoires Serono SAInventors: Agnes Bombrun, Patrick Gerber, Denis Church
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Publication number: 20100081610Abstract: The present invention relates to ?-hydroxy and amino substituted carboxylic acids, which act as matrix metalloprotease inhibitors, particularly diastereomerically pure ?-hydroxy carboxylic acids, corresponding processes for the synthesis of and pharmaceutical compositions containing the compounds of the present invention. Compounds of the present invention are useful in the treatment of various inflammatory, autoimmune and allergic diseases, such as methods of treating asthma, rheumatoid arthritis, COPD, rhinitis, osteoarthritis, psoriatic arthritis, psoriasis, pulmonary fibrosis, wound healing disorders, pulmonary inflammation, acute respiratory distress syndrome, perodontitis, multiple sclerosis, gingivitis, atherosclerosis, neointimal proliferation, which leads to restenosis and ischemic heart failure, stroke, renal diseases, tumor metastasis, and other inflammatory disorders characterized by the over-expression and over-activation of a matrix metalloproteinase using the compounds.Type: ApplicationFiled: August 21, 2007Publication date: April 1, 2010Inventors: Viswajanani J. Sattigeri, Venkata P. Palle, Manoj Kumar Khera, Ranaheer Reddy, Manoj Kumar Tiwari, Ajay Soni, Abdul Rehman Abdul Rauf, Sony Joseph, Arpita Musib, Sunanda G. Dastidar, Punit Kumar Srivastava
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Patent number: 7683068Abstract: The present invention is directed to certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: GrantFiled: June 23, 2006Date of Patent: March 23, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Jinlong Jiang, Robert J. DeVita, Sanjeev Kumar, Sander G. Mills, Richard A. Tschirret-Guth
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Publication number: 20100069404Abstract: The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising a compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced bones mass, osteoporosis, osteopenia, or reduced muscle mass or strength, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof. X-17142.Type: ApplicationFiled: November 6, 2007Publication date: March 18, 2010Inventors: Konstantinos Gavardinas, Jonathan Edward Green, Prabhakar Kondaji Jadhav, Donald Paul Matthews
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Patent number: 7671208Abstract: An acetone solvate of phthaloyl amlodipine, as well as a process for its preparation including dissolving phthaloyl amlodipine in acetone and cooling the mixture. The present invention also comprises a method for the synthesis of amlodipine, its salts or solvates, which comprises the use of an acetone solvate of phthaloyl amlodipine.Type: GrantFiled: May 31, 2007Date of Patent: March 2, 2010Assignee: Esteve Quimica, S.A.Inventors: Ramón Berenguer Maimó, Jorge Medrano Rupérez, Juan Francisco Merodio Cabanillas
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Publication number: 20100022514Abstract: The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.Type: ApplicationFiled: December 17, 2007Publication date: January 28, 2010Inventors: Young Shin Cho, Lei Jiang, Michael Shultz
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Publication number: 20090318499Abstract: The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.Type: ApplicationFiled: January 25, 2006Publication date: December 24, 2009Inventors: Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
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Patent number: 7635694Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.Type: GrantFiled: February 24, 2005Date of Patent: December 22, 2009Assignee: Schering CorporationInventors: Stephane L. Bogen, Weidong Pan, Sumie Ruan, F. George Njoroge