1,2,4-benzothiadiazines Patents (Class 544/12)
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Patent number: 11198689Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: GrantFiled: August 26, 2019Date of Patent: December 14, 2021Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
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Patent number: 10421752Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: GrantFiled: June 29, 2017Date of Patent: September 24, 2019Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
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Patent number: 9381202Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: GrantFiled: March 18, 2013Date of Patent: July 5, 2016Assignee: ESSENTIALIS, INC.Inventors: Neil M. Cowen, Khaled A. Yamout
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Patent number: 9315478Abstract: The invention relates to compounds of Formula I: and its pharmaceutical acceptable salts, solvates, enantiomers, stereoisomers and hydrates thereof. Compounds of Formula I and and compositions comprising Formula I are used to treat patients with metabolic syndrome and may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, or parenteral administration, as a syrup, or for injection.Type: GrantFiled: February 3, 2013Date of Patent: April 19, 2016Assignee: CELLIX BIO PRIVATE LIMITEDInventor: Mahesh Kandula
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Patent number: 9156832Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: June 10, 2014Date of Patent: October 13, 2015Assignee: Anadys Pharmaceuticals, Inc.Inventors: Peter Dragovich, Douglas E. Murphy
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Publication number: 20150126497Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of metabolic syndrome may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection.Type: ApplicationFiled: February 3, 2013Publication date: May 7, 2015Inventor: Mahesh Kandula
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Publication number: 20150126498Abstract: The disclosures herein relate to novel compounds of formula wherein W, X and Y1, Y2, Y3 and Y4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.Type: ApplicationFiled: July 3, 2013Publication date: May 7, 2015Inventors: Miles Stuart Congreve, John Andrew Christopher, Benjamin Gerald Tehan, Sukhbinder Singh Klair, Sarah Joanne Aves
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Publication number: 20140364414Abstract: Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.Type: ApplicationFiled: June 9, 2014Publication date: December 11, 2014Applicant: JANSSEN PHARMACEUTICA, NVInventors: Mark R. Player, Sanath K. Meegalla, Carl R. Illig, Jinsheng Chen, Kenneth J. Wilson, Yu-Kai Lee, Daniel J. Parks, Hui Huang, Sharmila Patel, Tianbao Lu
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Publication number: 20140357626Abstract: Inhibitors of HCV replication of formula I, including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: December 27, 2012Publication date: December 4, 2014Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8815848Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.Type: GrantFiled: January 25, 2013Date of Patent: August 26, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
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Patent number: 8815849Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: GrantFiled: July 26, 2011Date of Patent: August 26, 2014Assignee: Janssen R&D IrelandInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20130343992Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 21, 2012Publication date: December 26, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130338151Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.Type: ApplicationFiled: October 21, 2010Publication date: December 19, 2013Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Patent number: 8586578Abstract: The invention is directed to deuterated 5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: October 27, 2010Date of Patent: November 19, 2013Assignee: Anadys Pharmaceuticals, Inc.Inventor: Stephen E. Webber
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Publication number: 20130225806Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: Essentialis, Inc.Inventors: Neil M. Cowen, Khaled A. Yamout
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Publication number: 20130123244Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: July 26, 2011Publication date: May 16, 2013Applicant: JANSSEN R&D IRELANDInventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20120270863Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.Type: ApplicationFiled: October 21, 2010Publication date: October 25, 2012Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Publication number: 20120238554Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: ApplicationFiled: February 27, 2012Publication date: September 20, 2012Inventor: Neil M. Cowen
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Patent number: 8236948Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and compounds used to synthesize the compounds of Formula I.Type: GrantFiled: January 23, 2012Date of Patent: August 7, 2012Assignee: Anadys Pharmaceuticals, Inc.Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich
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Patent number: 8222405Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: November 22, 2010Date of Patent: July 17, 2012Assignee: Ajinomoto Co., Inc.Inventors: Shingo Makino, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Patent number: 8222404Abstract: The invention is directed to a [7-methanesulfonylamino-methyl)-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-3-yl]-acetic acid compound and to methods of making the same.Type: GrantFiled: January 13, 2012Date of Patent: July 17, 2012Assignee: Anadys Pharmaceuticals, Inc.Inventors: Peter Dragovich, Douglas Eric Murphy
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Publication number: 20120165321Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: ApplicationFiled: March 5, 2012Publication date: June 28, 2012Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerrard Darcy, Carla A. Donatelli, Steven David Knight, Kenneth Allen Newlander, Lance Ridgers, Martha A. Sarpong, Stanley J. Schmidt
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Patent number: 8138347Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.Type: GrantFiled: May 16, 2008Date of Patent: March 20, 2012Assignee: GlaxoSmithKline LLCInventors: Steven David Knight, Stanley J. Schmidt
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Patent number: 8101800Abstract: The invention is directed to a 5,6-dihydro-1H-pyridin-2-one compound selected from:Type: GrantFiled: March 8, 2011Date of Patent: January 24, 2012Assignee: Anadys Pharmaceuticals, Inc.Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera, Fritz Blatter, Martin Viertelhaus
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Patent number: 8097613Abstract: The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds of formula I wherein A is B is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: June 9, 2009Date of Patent: January 17, 2012Assignee: Anadys Pharmaceuticals, Inc.Inventors: Frank Ruebsam, Peter Dragovich, Stephen E. Webber, Douglas Eric Murphy, Chinh Viet Tran
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Patent number: 8022066Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.Type: GrantFiled: November 15, 2007Date of Patent: September 20, 2011Assignee: High Point Pharmaceuticals, LLCInventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
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Patent number: 7939524Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I wherein X is N, and A is and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.Type: GrantFiled: April 2, 2008Date of Patent: May 10, 2011Assignee: Anadys Pharmaceuticals, Inc.Inventors: Chinh V. Tran, Frank Ruebsam, Douglas E. Murphy, Peter Dragovich, Yuefen Zhou, Lijian Chen, David Kucera
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Publication number: 20110065918Abstract: Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: Ajinomoto Co., Inc.Inventors: Shingo MAKINO, Tatsuya Okuzumi, Toshihiko Yoshimura, Yuko Satake, Nobuyasu Suzuki, Hiroyuki Izawa, Kazuyuki Sagi, Akira Chiba, Eiji Nakanishi, Masahiro Murata, Takashi Tsuji
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Patent number: 7902203Abstract: The present invention provides an HCV polymerase inhibiting compound having the formula (I) and a composition comprising a therapeutically effective amount of said compound. The present invention also provides a method for inhibiting hepatitis C virus (HCV) polymerase, a method for inhibiting HCV viral replication, and a method for treating or preventing HCV infection. Processes for making said compounds, and synthetic intermediates employed in said processes, are also provided.Type: GrantFiled: October 31, 2003Date of Patent: March 8, 2011Assignee: Abbott Laboratories, Inc.Inventors: John K. Pratt, David A. Betebenner, Pamela L. Donner, Brian E. Green, Dale J. Kempf, Keith F. McDaniel, Clarence J. Maring, Vincent S. Stoll, Rong Zhang, Hui-Ju Chen, William J. Flosi, Larry L. Klein, Allan C. Krueger, Dachun Liu, Darold L. Madigan, Laura M. Maymon, Todd W. Rockway, Kent D. Stewart, Ming C. Yeung, Qinghua Xie
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Publication number: 20100324029Abstract: The invention encompasses 2-[4-(imidazolyl)-phenyl]vinyl-heterocycle derivatives which selectively attenuate production of Abeta(1-42) and are useful in the treatment of Alzheimer's disease. Pharmaceutical compositions and methods of use are also encompassed.Type: ApplicationFiled: February 5, 2008Publication date: December 23, 2010Inventors: Christian Fischer, Benito Munoz, Alexey A. Rivkin
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Patent number: 7834009Abstract: The invention is directed to 4-hydroxy-5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R6 is X is N, Ring A is a 5- or 6-membered aryl, optionally substituted by 1-3 R8 moieties, n is 2, and R1-R6 and R8 are defined herein.Type: GrantFiled: August 27, 2007Date of Patent: November 16, 2010Assignee: Anadys Pharmaceuticals, Inc.Inventors: David Ellis, Liansheng Li, Chinh V. Tran, Frank Ruebsam, Yuefen Zhou
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Publication number: 20100273784Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides quinazolinone, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.Type: ApplicationFiled: April 9, 2010Publication date: October 28, 2010Applicant: Icagen, Inc.Inventors: Grant Andrew McNaughton-Smith, George Salvatore Amato, James Barnwell Thomas, JR.
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Patent number: 7799777Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: GrantFiled: December 20, 2006Date of Patent: September 21, 2010Assignee: Essentialis, Inc.Inventors: Neil M. Cowen, Khaled A. Yamout
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Publication number: 20100160300Abstract: Methods for treatment of depression-related mood disorders in mammals, particularly humans are disclosed. The methods of the invention include administration of compounds capable of enhancing glutamate transporter activity in the brain of mammals suffering from depression. ATP-sensitive K+ channel openers and ?-lactam antibiotics are used to enhance glutamate transport and to treat depression-related mood disorders and depressive symptoms.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Applicant: Brookhaven Science Associates, LLCInventor: Fritz Henn
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Patent number: 7741320Abstract: Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.Type: GrantFiled: July 9, 2009Date of Patent: June 22, 2010Assignee: Les Laboratoires ServierInventors: Pierre Francotte, Pascal De Tullio, Bernard Pirotte, Laurence Danober, Pierre Lestage, Daniel-Henri Caignard
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Publication number: 20100035866Abstract: The present invention relates to compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones acting as a 5HT6 receptor antagonist, a preparation method thereof, and a pharmaceutical composition containing the same for treatment of the central nervous system disorders. The compounds of substituted-1,1-dioxo-benzo[1,2,4]thiadiazin-3-ones according to the present invention have excellent binding affinity for the 5HT6 receptor and excellent selectivity for the 5HT6 receptor over other receptors. Also, the compounds reverse a disruption of PPI by apomorphine and don't show rotatod deficit in mice. Therefore the compounds according to the present invention may be valuably used for treatment of a 5HT6 receptor relating disorders.Type: ApplicationFiled: March 28, 2006Publication date: February 11, 2010Applicant: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGYInventors: Churlmin Seong, Jinil Choi, Chul Min Park, Wookyu Park, Jaeyang Kong, Sunhee Kang, Chimin Park
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Publication number: 20100009974Abstract: Compounds of formula (I): wherein: RCy represents an unsubstituted or substituted cycloalkyl group or cycloalkylalkyl group, R1, R2, R3 and R4, which may be the same or different, each represent a hydrogen or halogen atom or a nitro group; a cyano group; a hydroxy group; an alkoxy group; an alkyl group; an unsubstituted or substituted amino group; a carboxy group; an alkoxycarbonyl group; an aryloxycarbonyl group; an unsubstituted or substituted aminocarbonyl group. Medicinal products containing the same which are useful in treating or preventing conditions treatable by an AMPA receptor modulator.Type: ApplicationFiled: July 9, 2009Publication date: January 14, 2010Applicant: LES LABORATOIRES SERVIERInventors: Pierre FRANCOTTE, Pascal De Tullio, Bernard Pirotte, Laurence Danober, Pierre Lestage, Daniel-Henri Caignard
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Patent number: 7642253Abstract: Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: wherein the variables are as defined herein.Type: GrantFiled: May 10, 2006Date of Patent: January 5, 2010Assignee: Takeda San Diego, Inc.Inventors: Jerome C. Bressi, Jason W. Brown, Anthony R. Gangloff, Jeffrey A. Stafford, Phong H. Vu
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Publication number: 20090325941Abstract: The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.Type: ApplicationFiled: November 15, 2007Publication date: December 31, 2009Inventors: Anders Klarskov Petersen, Preben Houlberg Olesen, Lise Brown Christiansen, Holger Claus Hansen, Flemming Elmelund Nielsen
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Publication number: 20090257979Abstract: The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: April 14, 2009Publication date: October 15, 2009Applicant: INTERMUNE, INC.Inventors: Leonid Beigelman, Guangyi Wang, Brad O. Buckman, Antitsa Dimitrova Stoycheva
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Patent number: 7582626Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating hepatitis C virus infections: wherein Z is X is N or CR9; Y is ā(CR4R5)nā; n is 2, 3, 4, or 5; and R1 through R9 are defined herein.Type: GrantFiled: December 12, 2007Date of Patent: September 1, 2009Assignee: Anadys Pharmaceuticals, Inc.Inventors: Chinh V. Tran, Frank Ruebsam, Yuefen Zhou, Peter Dragovich, Alan X. Xiang
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Patent number: 7572789Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: GrantFiled: February 24, 2009Date of Patent: August 11, 2009Assignee: Essentialis, Inc.Inventors: Neil M. Cowen, Kenneth B. Kashkin, Khaled A. Yamout
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Publication number: 20090148526Abstract: Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.Type: ApplicationFiled: February 24, 2009Publication date: June 11, 2009Inventors: Neil M. Cowen, Kenneth B. Kashkin, Khaled A. Yamout
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Patent number: 7541459Abstract: The present invention provides a method of producing a compound represented by the following formula (1) or a compound represented by the following formula (4) or a tautomer thereof, the method including reacting a compound represented by the following formula (2) or a compound represented by the following formula (5) or a tautomer thereof with a compound represented by the following formula (3) or a compound represented by the following formula (6) in the presence of an aluminum alkoxide compound.Type: GrantFiled: September 27, 2005Date of Patent: June 2, 2009Assignee: Fujifilm CorporationInventors: Keizo Kimura, Katsuyoshi Yamakawa
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Patent number: 7524841Abstract: The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides 4,4-(disubstituted)piperidine derivatives represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.Type: GrantFiled: April 16, 2003Date of Patent: April 28, 2009Assignee: Teijin LimitedInventors: Yoshiyuki Matsumoto, Minoru Imai, Yoshiyuki Sawai, Susumu Takeuchi, Akinobu Nakanishi, Kunio Minamizono, Tomonori Yokoyama
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Patent number: 7517875Abstract: The invention provides low molecular compounds having activity which inhibits binding of CCR3 ligands to CCR3 on target cells, i.e. CCR3 antagonists. The invention also provides compounds represented by formula (I) below, pharmaceutically acceptable acid adducts thereof, or pharmaceutically acceptable C1-C6 alkyl adducts thereof, as well as pharmaceutical compositions comprising them as effective ingredients, which are useful for treatment or prevention of diseases associated with CCR3, such as asthma and allergic rhinitis.Type: GrantFiled: April 16, 2003Date of Patent: April 14, 2009Assignee: Teijin LimitedInventors: Yoshiyuki Matsumoto, Minoru Imai, Yoshiyuki Sawai, Susumu Takeuchi, Akinobu Nakanishi, Kunio Minamizono, Tomonori Yokoyama
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Patent number: 7517876Abstract: Compounds having the formula are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.Type: GrantFiled: February 27, 2006Date of Patent: April 14, 2009Assignee: Abbott LaboratoriesInventors: Larry L. Klein, Peggy P. Huang, John T. Randolph, Douglas K. Hutchinson, Ming C. Yeung, Charles A. Flentge
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Patent number: 7498325Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.Type: GrantFiled: April 29, 2004Date of Patent: March 3, 2009Assignee: Karl Thomas GmbHInventors: Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
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Patent number: 7462611Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R4 is selected from Ring A is 5 or 6- membered aryl or heterocyclyl, and the remaining substituents are defined herein.Type: GrantFiled: June 21, 2007Date of Patent: December 9, 2008Assignee: Anadys Pharmaceuticals, Inc.Inventors: Frank Ruebsam, Martin Tran, Stephen E. Webber, Peter Dragovich, Liansheng Li, Douglas Murphy, David Kucera, Zhongxiang Sun, Chinh Viet Tran