Chalcogen Attached Indirectly To The Diazole Ring By Acyclic Nonionic Bonding [e.g., 1-(2-hydroxyethyl)-3-amino-4(para-chlorophenyl)-pyrazole, Etc.] Patents (Class 548/372.5)
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Patent number: 11242321Abstract: A salt compound of 4-(2-((4-bromophenyl)thio)acetamido)-1-phenethyl-1H-pyrazole-3-carboxylic acid is disclosed. Also disclosed are methods for making the salt compound and formulations of the salt compound into dosage forms for clinical use.Type: GrantFiled: January 30, 2019Date of Patent: February 8, 2022Assignee: Kainos Medicine Inc.Inventors: Jae Moon Lee, Sungeun Yoo, Sunmi Shin
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Patent number: 10315999Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: May 8, 2018Date of Patent: June 11, 2019Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Belgin Canturk, Elisabeth J. Kane, Yu Zhang, Joseck M. Muhuhi
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Patent number: 9670164Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: August 22, 2016Date of Patent: June 6, 2017Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Greg Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
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Patent number: 9433215Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: September 9, 2015Date of Patent: September 6, 2016Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Carl DeAmicis, Joseck M. Muhuhi
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Patent number: 9255082Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: May 20, 2015Date of Patent: February 9, 2016Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory Whiteker, Gary Roth, Carl DeAmicis, Thomas Clark, Kaitlyn Gray, Belgin Canturk, Elisabeth J. Kane, Yu Zhang, Joseck M. Muhuhi
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Patent number: 9199942Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: March 24, 2015Date of Patent: December 1, 2015Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory T. Whiteker, Carl DeAmicis, Joseck M. Muhuhi
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Patent number: 9180192Abstract: Pyrazole compounds 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.Type: GrantFiled: October 22, 2010Date of Patent: November 10, 2015Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti
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Patent number: 9085564Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: October 17, 2014Date of Patent: July 21, 2015Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory T. Whiteker, Carl DeAmicis, Kaitlyn Gray, Yu Zhang, Joseck M. Muhuhi
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Patent number: 9044017Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: October 17, 2014Date of Patent: June 2, 2015Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Gregory T. Whiteker, Carl DeAmicis, Joseck M. Muhuhi
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Publication number: 20150141465Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: November 14, 2014Publication date: May 21, 2015Inventors: Calvin W. YEE, Zhe Li
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Patent number: 9035071Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: GrantFiled: December 19, 2012Date of Patent: May 19, 2015Assignee: Allergan, Inc.Inventors: Jussi J. Kangasmetsa, William R. Carling, Jose L. Martos, David F. Woodward, Jenny W. Wang
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Patent number: 9029554Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: GrantFiled: October 17, 2014Date of Patent: May 12, 2015Assignee: Dow AgroSciences LLCInventors: Qiang Yang, Beth Lorsbach, Ronald Ross, Jr., Kaitlyn Gray, Yu Zhang, Gary Roth
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Publication number: 20150112075Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Carl DeAMICIS, Kaitlyn GRAY, Yu ZHANG, Joseck M. MUHUHI
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Publication number: 20150111938Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Carl DeAMICIS, Joseck M. MUHUHI
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Publication number: 20150112073Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Qiang YANG, Beth LORSBACH, Ronald ROSS, JR., Kaitlyn GRAY, Yu ZHANG, Gary ROTH
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Publication number: 20150112076Abstract: The present application provides processes for making pesticidal compounds and compounds useful both as pesticides and in the making of pesticidal compounds.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Inventors: Qiang YANG, Beth LORSBACH, Gregory T. WHITEKER, Gary ROTH, Carl DeAMICIS, Thomas P. CLARK, Kaitlyn GRAY, Belgin CANTURK, Elisabeth J. KANE, Yu ZHANG, Joseck M. MUHUHI
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Publication number: 20150031736Abstract: Use of 3-[5-amino-4-(3-cyanobenzoyl)-pyrazol-1-yl]-N-cyclopropyl-4-methylbenzamide or a pharmaceutically acceptable derivative thereof in the manufacture of a medicament for the treatment of acute exacerbations of chronic obstructive pulmonary disease. Treatment may involve a single dose of the active ingredient by oral administration.Type: ApplicationFiled: March 19, 2013Publication date: January 29, 2015Inventor: Paul Andrew Ford
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Patent number: 8901153Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: March 7, 2013Date of Patent: December 2, 2014Assignee: Dow AgroSciences, LLC.Inventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, Akshay Patny, Negar Garizi, Paul Renee LePlae, Jr., Frank Wessels, Ronald Ross, Jr., Carl DeAmicis, Peter Borromeo
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Publication number: 20140323485Abstract: A compound of Formula I and pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, Ra, A, B, D and E are all as defined herein. The compounds modulate the activity of CFTR and are useful in the treatment of inflammatory or obstructive airways diseases or mucosal hydration, including, for example cystic fibrosis. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 14, 2012Publication date: October 30, 2014Applicant: NOVARTIS AGInventors: Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Darren Mark LeGrand, Roger John Taylor
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Patent number: 8859605Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.Type: GrantFiled: December 10, 2010Date of Patent: October 14, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jonsson, Pia Kahnberg, Bjorn Klasson, Peter Lind, Lourdes Oden, Kevin Parkes, Daniel Wiktelius
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Patent number: 8853281Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.Type: GrantFiled: December 18, 2009Date of Patent: October 7, 2014Assignee: Medivir UK LtdInventors: Susana Ayesa, Anna Karin Belfrage, Bjorn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Patent number: 8829034Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: February 8, 2011Date of Patent: September 9, 2014Assignee: Boehringer Ingerlheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Parke, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
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Publication number: 20140200215Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: March 12, 2013Publication date: July 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20140142156Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.Type: ApplicationFiled: December 12, 2013Publication date: May 22, 2014Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Helen E. BLACKWELL, Christine E. McINNIS
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Publication number: 20130336921Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: January 4, 2013Publication date: December 19, 2013Applicant: ARDELYX, INC.Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
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Publication number: 20130324557Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formula (I) and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.Type: ApplicationFiled: November 4, 2011Publication date: December 5, 2013Applicant: SENOMYX, INC.Inventors: Chad Priest, Alain Noncovich, Andrew Patron, Jane Ung
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Publication number: 20130267543Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 8, 2011Publication date: October 10, 2013Applicants: CHAPERONE THERAPEUTICS, INC., DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
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Publication number: 20130253023Abstract: Described herein is the LPA1 antagonist 1-{4?-[3-methyl-4-((R)-1-phenyl-ethoxycarbonylamino)-isoxazol-5-yl]-bi-phenyl-4-yl}-cyclopropanecarboxylic acid (Compound 1), or pharmaceutically acceptable salts thereof. Also described are methods of preparing the LPA1 antagonist, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions suitable for administration to a mammal that include the LPA1 antagonist, or pharmaceutically acceptable salt thereof, and methods of using such pharmaceutical compositions for treating LPA-dependent or LPA-mediated diseases or conditions.Type: ApplicationFiled: December 7, 2011Publication date: September 26, 2013Inventors: Jason Edward Brittain, Thomas Jon Seiders, Christopher David King, Victor W. Rosso
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Publication number: 20130217658Abstract: The present invention relates to pyrazole amide derivatives pharmaceutical compositions containing these compounds and to their use in therapy.Type: ApplicationFiled: October 19, 2011Publication date: August 22, 2013Applicant: GLAXO GROUP LIMITEDInventors: Anthony William James Cooper, Paul Martin Gore, David House
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Publication number: 20130203705Abstract: The present invention relates to a pyrazole amide derivative, pharmaceutical compositions containing this compound and to its use in therapy.Type: ApplicationFiled: October 19, 2011Publication date: August 8, 2013Applicant: Glaxo Group LimitedInventors: Anthony William James Cooper, Paul Martin Gore, David House
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Publication number: 20130184315Abstract: Compounds of formula (I) and formula (II) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: July 18, 2011Publication date: July 18, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Eugene Richard Hickey, Doris Riether, Monika Ermann
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Publication number: 20130165666Abstract: The present invention provides a compound that is represented by the following general formula wherein R1, R2, R4, R5, R6, R7, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: ApplicationFiled: December 19, 2012Publication date: June 27, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Publication number: 20130045938Abstract: A method of treating cancer in which a compound that inhibits the expression, production or release of IL-10 by immune cells is combined with a compound that stimulates the production of IL-12 when given in combination with, or in the presence of TNFa. Said method is effective when provided in addition to standard therapies, notably chemotherapy using cytotoxic drugs and other forms of immune therapy including therapeutic vaccines.Type: ApplicationFiled: August 15, 2012Publication date: February 21, 2013Applicant: Synovo GmbHInventors: Michael W. Burnet, Jan-Hinrich Guse, Christiane Bauerlein, Ulrike Hahn
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Publication number: 20120283305Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10 alkyl chain, C2-C4haloalkyl or —CH2C3-C7 cycloalkyl; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkylamino or C1-C6dialkylamino; for use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cathepsin S.Type: ApplicationFiled: December 10, 2010Publication date: November 8, 2012Applicant: Medivir UK LTDInventors: Susana Ayesa, Peter Carlqvist, Karolina Ersmark, Urszula Grabowska, Ellen Hewitt, Daniel Jönsson, Pia Kahnberg, Björn Klasson, Peter Lind, Lourdes Odén, Kevin Parkes, Daniel Wiktelius
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Patent number: 8288428Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 26, 2010Date of Patent: October 16, 2012Assignee: Abbott LaboratoriesInventors: Xueqing Wang, Jennifer M. Frost, Michael J. Dart, Bo Liu
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Publication number: 20120214782Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Heike NEUBAUER, Bernd NOSSE
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Patent number: 8236824Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, Alk and D 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: GrantFiled: September 9, 2008Date of Patent: August 7, 2012Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Ulrich Emde, Christine Charon, Denis Carniato
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Patent number: 8236822Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.Type: GrantFiled: March 26, 2010Date of Patent: August 7, 2012Assignee: Abbott LaboratoriesInventors: Xueqing Wang, Michael J. Dart, Bo Liu
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Publication number: 20120190673Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 19, 2011Publication date: July 26, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio BERDINI, Maria Grazia CARR, Adrian Liam GILL, Steven HOWARD, Eva Figueroa NAVARRO, Gary TREWARTHA, David Charles REES, Mladen VINKOVIC, Paul Graham WYATT
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Publication number: 20120178765Abstract: The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present invention activates glucokinase remarkably, and therefore they can be usefully applied for treating glucokinase-mediated diseases, such as hyperglycemia and diabetes.Type: ApplicationFiled: September 17, 2010Publication date: July 12, 2012Applicant: YUHAN CORPORATIONInventors: Won-Hui Yi, Tae-Dong Han, Koo-Yeon Lee, Young-Hwan Kim, Eun-Hye Jung, Dong-Hoon Lee, Yoo-Hoi Park, Kyung-Nan Min, Jae-Gyu Kim, Byung-Kyu Lee
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Patent number: 8188135Abstract: Disclosed herein are cannabinoid receptor ligands of formula (I) wherein A1, A5, Rx, X4, and z are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: September 16, 2009Date of Patent: May 29, 2012Assignee: Abbott LaboratoriesInventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Teodozyj Kolasa, Tongmei Li, Sridhar Peddi, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Derek W. Nelson
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Publication number: 20120129844Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: January 26, 2012Publication date: May 24, 2012Inventors: David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
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Publication number: 20120058893Abstract: Ketosultams and diketopyridines of the formula (I) and use thereof as herbicides are described. In this formula (I), G, X, Y and Z are each radicals such as hydrogen and organic radicals such as alkyl. W represents organic radicals such as alkyl. A represents a heterocycle.Type: ApplicationFiled: August 31, 2011Publication date: March 8, 2012Applicant: BAYER CROPSCIENCE AGInventors: Stefan LEHR, Christian WALDRAFF, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Ines HEINEMANN, Christopher Hugh ROSINGER
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Publication number: 20120053150Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: ApplicationFiled: April 22, 2010Publication date: March 1, 2012Inventors: David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
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Publication number: 20120004227Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.Type: ApplicationFiled: March 5, 2010Publication date: January 5, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
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Publication number: 20110312964Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic painType: ApplicationFiled: December 18, 2009Publication date: December 22, 2011Applicant: Medivir UK LTDInventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Patent number: 7960588Abstract: Sphingosine-1-phosphate analogs that are potent, and selective agonists at one or more S1P receptors, specifically the S1P1 receptor type are provided. The disclosed compounds include an optional phosphate moiety as well as compounds with hydrolysis-resistant phosphate surrogates such as phosphonates, alpha-substituted phosphonates, and phosphothionates.Type: GrantFiled: March 29, 2010Date of Patent: June 14, 2011Assignee: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald