At Least Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 548/153)
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Patent number: 9469657Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: GrantFiled: September 30, 2014Date of Patent: October 18, 2016Assignee: Merck Patent GmbHInventors: Marianne Donnelly, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
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Patent number: 9024037Abstract: Diphenylamine-benzobisthiazole-diphenylamine monomers having two-photon absorption cross-sections and high solubility in organic solvents are provided. Also provided are the corresponding organo-soluble, wholly conjugated and two-photon absorbing benzobisthiazole-triarylamine polymers.Type: GrantFiled: May 18, 2012Date of Patent: May 5, 2015Assignee: The United States of America as represented by the Secretary of the Air ForceInventors: Loon-Seng Tan, Ramamurthi Kannan, Matthew Dalton
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Patent number: 9006275Abstract: The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L2, are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: December 16, 2010Date of Patent: April 14, 2015Assignee: AbbVie Inc.Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
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Publication number: 20150065482Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Applicant: GENENTECH, INC.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Jason Burch
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Patent number: 8962664Abstract: The invention provides compounds of formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: GrantFiled: August 22, 2012Date of Patent: February 24, 2015Assignee: Simon Fraser UniversityInventors: David Vocadlo, Ernest McEachern, Keith Stubbs, Tong-Shuang Li, Garrett Whitworth, Julia Heinonen, Matthew Macauley
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Patent number: 8933040Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: GrantFiled: November 8, 2011Date of Patent: January 13, 2015Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEacher, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Patent number: 8927507Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: GrantFiled: March 16, 2012Date of Patent: January 6, 2015Inventors: Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Craig A. Coburn, Kun Liu, Harold G. Selnick
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Patent number: 8884023Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: GrantFiled: August 22, 2012Date of Patent: November 11, 2014Assignee: Merck Patent GmbHInventors: Marianne Donnely, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
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Publication number: 20140296205Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: June 27, 2012Publication date: October 2, 2014Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
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Publication number: 20140275022Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: June 27, 2012Publication date: September 18, 2014Applicants: MERCK SHARP & DOHME CORP., ALECTOS THERAPEUTICS INC.Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick
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Publication number: 20140243288Abstract: The present invention relates to a fused ring-containing oxazolidinone compound shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof, wherein R1, R2, R3, R4, R5, R6, A, B and C are as defined in the description. The present invention further relates to a method for preparing the compound, a pharmaceutical composition and a pharmaceutical formulation comprising the compound, and a use of the compound for the manufacture of a medicament for the treatment and/or prevention of infectious diseases and a use for the treatment and/or prevention of infectious diseases.Type: ApplicationFiled: September 29, 2012Publication date: August 28, 2014Inventors: Hui Zhang, Aichen Wang
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Publication number: 20140243370Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: ApplicationFiled: August 22, 2012Publication date: August 28, 2014Applicant: MERCK PATENT GmbHInventors: Marianne Donnelly, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
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Publication number: 20140213538Abstract: 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: January 15, 2014Publication date: July 31, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
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Publication number: 20140213584Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 8, 2011Publication date: July 31, 2014Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Patent number: 8779086Abstract: An electrochromic material containing a ?-electron based conjugated polymer that changes from a desired color developed state to a decolored state, and a method for producing the electrochromic material, are provided. The electrochromic material contains a?-electron based conjugated polymer as shown in chemical formula (1). In formula (1), each X is any one selected from —S—, —O—, —Se— and —Te—; each Y is any one selected from a hydrogen atom and an organic group having 1 to 20 carbon atoms; W is an arylene group or divalent heteroaromatic ring group; and n is a number of 2 to 1,000. Repetition of this structure forms a structure of random copolymers, graft copolymers, block copolymers and/or dendrimers.Type: GrantFiled: March 8, 2011Date of Patent: July 15, 2014Assignee: Kuraray Co., Ltd.Inventors: Yoshirou Kondou, Tomiaki Otake
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Patent number: 8759333Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: GrantFiled: March 13, 2013Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Patent number: 8759533Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: GrantFiled: March 13, 2013Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Patent number: 8735434Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 15, 2008Date of Patent: May 27, 2014Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Arturo Perez-Medrano, Jennifer M. Frost, Sridhar Peddi
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Patent number: 8716277Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Patent number: 8703961Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: November 9, 2010Date of Patent: April 22, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Hannes Koolman
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Patent number: 8674113Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
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Publication number: 20140034880Abstract: The invention relates to novel benzo[1,2-b:4,5-b?]dithiophene-2,6-diyl-alt-thieno[3,4-b]thiazole-4,6-diyl polymers, methods for their preparation and monomers used therein, blends, mixtures and formulations containing them, the use of the polymers, blends, mixtures and formulations as semiconductor in organic electronic (OE) devices, especially in organic photovoltaic (OPV) devices, and to OE and OPV devices comprising these polymers, blends, mixtures or formulations.Type: ApplicationFiled: March 26, 2012Publication date: February 6, 2014Applicant: MERCK PATENT GMBHInventors: Nicolas Blouin, William Mitchell, Amy Topley, Steven Tierney
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Publication number: 20140005191Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 9, 2011Publication date: January 2, 2014Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEacher, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Patent number: 8592604Abstract: The invention provides a thiazolothiazole compound represented by the following Formula (I). In Formula (I), Ar1 represents a substituted or unsubstituted aromatic group; R1 represents a hydrogen atom, an alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and n represents an integer of 0 or 1. The invention further provides a thiazolothiazole polymer having the thiazolothiazole compound as a polymerization unit thereof.Type: GrantFiled: May 16, 2012Date of Patent: November 26, 2013Assignee: Fuji Xerox Co., Ltd.Inventors: Hidekazu Hirose, Takeshi Agata, Katsuhiro Sato, Kazuaki Sato, Yoshihiro Ohba
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Publication number: 20130296301Abstract: The invention is directed to compounds for selectively inhibiting glycosidases, uses of the compounds and pharmaceutical compositions including the compounds, and methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, and/or accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 8, 2011Publication date: November 7, 2013Inventors: Jiang Chang, Kun Liu, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, Feng Shi, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou, Yongbao Zhu
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Patent number: 8524894Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: GrantFiled: June 4, 2010Date of Patent: September 3, 2013Assignee: Laboratorios Salvat, S.A.Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleo Mas
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Publication number: 20130216552Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed herein.Type: ApplicationFiled: June 24, 2011Publication date: August 22, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Takashi Nakai, James Jia, Jason Rohde, Regina Graul, Ara Mermerian
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Publication number: 20130217666Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: February 15, 2013Publication date: August 22, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
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Publication number: 20130196960Abstract: The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy.Type: ApplicationFiled: February 9, 2011Publication date: August 1, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
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Publication number: 20130196968Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Patent number: 8492403Abstract: Bicyclic derivatives useful as ion channel antagonists are disclosed herein. The compositions thereof are useful for treating or relieving pain-related conditions.Type: GrantFiled: January 21, 2013Date of Patent: July 23, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Aarti Sameer Kawatkar, Esther Ann Martinborough, Nicole Hilgraf, Andreas P. Termin, Timothy Donald Neubert
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Publication number: 20130178453Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).Type: ApplicationFiled: February 9, 2011Publication date: July 11, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
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Patent number: 8481574Abstract: The present invention relates to compounds of formula (I) wherein A, E, L2, R1, R3, R4 and R5 are as defined in the herein, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: October 12, 2007Date of Patent: July 9, 2013Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
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Publication number: 20130158011Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130150347Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130150341Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130096110Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds 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.Type: ApplicationFiled: February 11, 2011Publication date: April 18, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Patent number: 8334310Abstract: The invention provides compounds of formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAcType: GrantFiled: August 31, 2007Date of Patent: December 18, 2012Assignee: Simon Fraser UniversityInventors: David Vocadlo, Ernest McEachern, Keith Stubbs, Tong-Shuang Li, Garrett Whitworth, Julia Heinonen, Matthew Macauley
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Publication number: 20120316207Abstract: The invention provides compounds of formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: August 22, 2012Publication date: December 13, 2012Applicant: Simon Fraser UniversityInventors: David Vocadlo, Ernest McEachern, Keith Stubbs, Tong-Shuang Li, Garrett Whitworth, Julia Heinonen, Matthew Macauley
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Publication number: 20120252759Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 9, 2010Publication date: October 4, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKER HAFTINGInventors: Timo Heinrich, Hannes Koolman
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Patent number: 8263431Abstract: Provided are an organic semiconductor compound using thiazole, and an organic thin film transistor having an organic semiconductor layer formed of the organic semiconductor compound using thiazole. The novel organic semiconductor compound including thiazole has liquid crystallinity and excellent thermal stability, and thus is provided to form an organic semiconductor layer in the organic thin film transistor. To this end, a silicon oxide layer is formed on a silicon substrate, and an organic semiconductor layer including thiazole is formed on the silicon oxide layer. In addition, source and drain electrodes are formed on both edge portions of the organic semiconductor layer. The organic thin film transistor using the organic semiconductor layer has an improved on/off ratio and excellent thermal stability. Also, a solution process can be applied in its manufacture.Type: GrantFiled: January 24, 2011Date of Patent: September 11, 2012Assignee: Gwangju Institute of Sciences and TechnologyInventors: Dong-Yu Kim, Bogyu Lim, Kang-Jun Baeg, Hyung-Gu Jeong, Seung-Hwan Oh, Hong-Ju Park
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Publication number: 20120202815Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein Y is a 5-membered, fully or partially unsaturated heterocyclic ring containing 2-4 carbon atoms and 2-3 nitrogen atoms as ring members, the ring substituted with Z on a ring member atom connected through an adjacent single ring member atom to the ring member atom attaching the heterocyclic ring to the phenyl ring of Formula 1, and optionally further substituted with up to 2 substituents independently selected from R5 on carbon atom ring members and from R6 on nitrogen atom ring members; Z is an 8-, 9-, 10- or 11-membered fused heterobicyclic ring system containing ring members selected from carbon atoms and 1 to 4 heteroatoms independently selected from up to 2O, up to 2S and up to 4 N atoms, wherein up to 3 carbon atom ring members are independently selected from C(?O) and C(?S), and the sulfur atom ring members are independently selected from S(?O)u(?NR7)z, the ring system optionally substituted wiType: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Applicant: E.I.DU PONT DE NEMOURS AND COMPANYInventors: John Lawrence Andreassi II, Andrew Edmund Taggi
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Patent number: 8227504Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.Type: GrantFiled: March 15, 2010Date of Patent: July 24, 2012Assignee: SanofiInventors: Werngard Czechtizky, Zhongli Gao, William Joseph Hurst, Lothar Schwink, Siegfried Stengelin
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Patent number: 8207348Abstract: The invention provides a thiazolothiazole compound represented by the following Formula (I). In Formula (I), Ar1 represents a substituted or unsubstituted aromatic group; R1 represents a hydrogen atom, an alkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and n represents an integer of 0 or 1. The invention further provides a thiazolothiazole polymer having the thiazolothiazole compound as a polymerization unit thereof.Type: GrantFiled: May 14, 2010Date of Patent: June 26, 2012Assignee: Fuji Xerox Co., Ltd.Inventors: Hidekazu Hirose, Takeshi Agata, Katsuhiro Sato, Kazuaki Sato, Yoshihiro Ohba
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Publication number: 20120149676Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Alexander HEIM-RIETHER, Raimund KUELZER, Roland PFAU, Klaus RUDOLF, Dirk STENKAMP
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Publication number: 20120108591Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol
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Patent number: 8148540Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.Type: GrantFiled: June 7, 2007Date of Patent: April 3, 2012Assignee: AstraZenecaInventors: Joseph Aszodi, Maxime Lampilas, Branislav Musicki, David Alan Rowlands, Pascal Colette
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Publication number: 20120065196Abstract: The present invention provides compounds represented by the formula (Ie): and the formula (If): wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibitory activity and are useful for the prophylaxis, treatment or improvement of diseases or pathologies caused by high expression or high activation of DGAT.Type: ApplicationFiled: July 20, 2007Publication date: March 15, 2012Inventors: Shuji Kitamura, Thomas Daniel Aicher, Steve Gonzales, Yvan Le Huerou, Scott Alan Pratt, Yoshihisa Nakada
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Publication number: 20120058986Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Q and Z are defined herein.Type: ApplicationFiled: September 2, 2011Publication date: March 8, 2012Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
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Patent number: 8110686Abstract: The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.Type: GrantFiled: May 3, 2010Date of Patent: February 7, 2012Assignee: Chugai Seiyaki Kabushiki KaishaInventors: Thomas Arrhenius, Jie Fei Cheng, Mark E. Wilson, Rossy Serafimov, Alex M. Nadzan, Gary D. Lopaschuk, Jason R. Dyck