Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 548/152)
  • Patent number: 10329481
    Abstract: New composition of polymeric scintillator was revealed, which can be used particularly in medical diagnostics especially in productions of CT scanners, PET scanners and SPECT scanners.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: June 25, 2019
    Assignees: UNIWERSYTET JAGIELLONSKI, UNIWERSYTET ROLNICZY IM. HUGONA KOLLATAJA W KRAKOWIE
    Inventors: Anna Wieczorek, Andrzej Danel, Tomasz Uchacz, Pawel Moskal
  • Patent number: 10209568
    Abstract: A display panel and a display device, the display panel includes an array substrate; wherein the array substrate includes a common electrode, a first insulation layer, a plurality of pixel electrodes and an alignment layer; the common electrode, first insulation layer, plurality of pixel electrodes and alignment layer are successively arranged; at least one first through hole is defined in the first insulation layer, and the alignment layer contacts with the common electrode via the at least one first through hole. By arranging in such a manner, although a thin-film transistor stays in a turn-on state for an extremely short time, however, since the common electrode is always in a conductive state, so that the electrostatic charge remaining on the alignment layer can be conducted away by the common electrode, thereby reducing the electrostatic charge remaining on the alignment layer, and thus improving display quality of display panel.
    Type: Grant
    Filed: October 25, 2017
    Date of Patent: February 19, 2019
    Assignee: XIAMEN TIANMA MICRO-ELECTRONICS CO., LTD.
    Inventor: Hongbo Zhou
  • Patent number: 9187467
    Abstract: The present invention provides 2-phenyl benzothiazole linked imidazole compounds of formula A as anti cancer agent against fifty three human cancer cell lines.
    Type: Grant
    Filed: February 15, 2012
    Date of Patent: November 17, 2015
    Assignee: Council of Scientific and Industrial Research
    Inventors: Kamal Ahmed, Ratna Reddy Challa, Prabhakar Singaraboina
  • Patent number: 9040714
    Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts there-of. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.
    Type: Grant
    Filed: April 5, 2011
    Date of Patent: May 26, 2015
    Assignee: MannKind Corporation
    Inventors: Qingping Zeng, Andras Toro, John Bruce Patterson, Warren Stanfield Wade, Zoltan Zubovics, Yun Yang, Zhipeng Wu
  • Publication number: 20150141657
    Abstract: The present invention provides 2-phenyl benzothiazole linked imidazole compounds of formula A as anti cancer agent against fifty three human cancer cell lines.
    Type: Application
    Filed: February 15, 2012
    Publication date: May 21, 2015
    Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH
    Inventors: Kamal Ahmed, Ratna Reddy Challa, Prabhakar Singaraboina
  • Patent number: 8993777
    Abstract: The present invention is a method for producing a phenyl-substituted heterocyclic derivative represented by general formula (1), which has a step wherein a heteroaromatic compound represented by general formula (2) is reacted with a phenol derivative represented by general formula (3) in the presence of a nickel compound, 1,2-bis(dicyclohexylphosphino)ethane, and a base.
    Type: Grant
    Filed: October 10, 2012
    Date of Patent: March 31, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kenichiro Itami, Junichiro Yamaguchi, Kei Muto
  • Patent number: 8987314
    Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: March 24, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
  • Patent number: 8927584
    Abstract: The present invention provides a photodynamic therapy to a patient having at least one tumor comprising the steps of: administering a compound of formula 6 (wherein R1 and R2 are defined as the above) in a pharmaceutically acceptable carrier to the patient; waiting for a sufficient time to allow the administered compound to be taken up by a target tissue having the at least one tumor; and irradiating a region of the patient containing the target tissue, wherein growth of the tumor is inhibited.
    Type: Grant
    Filed: October 18, 2013
    Date of Patent: January 6, 2015
    Assignee: Kaohsiung Medical University
    Inventors: Jeh-Jeng Wang, Chao-Cheng Liao, Wan-Ping Hu, Ho-Chuan Shen
  • Patent number: 8927709
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with the compounds.
    Type: Grant
    Filed: September 10, 2010
    Date of Patent: January 6, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
  • Publication number: 20150005505
    Abstract: A process for the production of a compound of formula (III) which comprises a step of reacting a compound of formula (I) with an excess amount of a compound of formula (II) in absence of aromatic solvent, wherein n is 0, 1, 2, 3 or 4; X is NH, O or S; each R1 group may be the same or different, and is independently selected from the group consisting of hydrogen, hydroxyl, alkoxy, alkyl, carbonyl, carboxyl, carboxylic acid ester, amido, cyano, halogenated aliphatic, nitro, and amino; and R2 group is selected from the group consisting of hydroxyl, Cl, F, Br, amino, and alkoxy.
    Type: Application
    Filed: February 20, 2012
    Publication date: January 1, 2015
    Applicant: RHODIA OPERATIONS
    Inventors: Tao Zhang, Claude Mercier, Olivier Buisine
  • Patent number: 8916563
    Abstract: The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like.
    Type: Grant
    Filed: January 16, 2013
    Date of Patent: December 23, 2014
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Andrew Wasmuth, Donald W. Landry, Shi Xian Deng, Banavara L. Mylari
  • Publication number: 20140348753
    Abstract: The development of a series of fluorescent materials including heterocycle-functionalized luminogens with aggregation-induced/enhanced emission (AIE/AEE), long wavelength emission, and high solid state fluorescence quantum efficiency is contemplated. The described fluorescent materials are promising candidates in selective luminescence-based chemosensor for Hg2+ or ATP, fluorescent staining for mitochondria in living cells with high photostability, stimuli-responsive luminescent materials, and materials for optical waveguides. In addition, these heterocycle-functionalized luminogens are particularly useful as fluorescent labels for biopolymers such as peptides, antibodies, or nucleic acids, making them useful as AIE-active biocompatible probes for clinical cancer imaging and diagnostics.
    Type: Application
    Filed: May 24, 2013
    Publication date: November 27, 2014
    Inventors: Benzhong TANG, Wing Yip LAM, Na ZHAO, Min LI, Bin LIU, Haibin SHI, Dan DING
  • Patent number: 8889881
    Abstract: Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPAR? and PPAR? activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: November 18, 2014
    Assignee: Pusan National University Industry —University Cooperation Foundation
    Inventors: Hae Young Chung, Min Hi Park, Young Mi Ha, Yu Kyeong Han, Ji Young Park, Yun Jung Park, Jin Ah Kim, Ji Yeon Lee, Yu Min Song, Hyung Ryong Moon
  • Patent number: 8883833
    Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.
    Type: Grant
    Filed: November 20, 2008
    Date of Patent: November 11, 2014
    Assignee: Decode Genetics EHF
    Inventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8859814
    Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: October 14, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
  • Publication number: 20140288105
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, OSCAR MIGUEL MORADEI
  • Publication number: 20140275549
    Abstract: The present invention is a method for producing a phenyl-substituted heterocyclic derivative represented by general formula (1), which has a step wherein a heteroaromatic compound represented by general formula (2) is reacted with a phenol derivative represented by general formula (3) in the presence of a nickel compound, 1,2-bis(dicyclohexylphosphino)ethane, and a base.
    Type: Application
    Filed: October 10, 2012
    Publication date: September 18, 2014
    Applicant: National University Corporation Nagoya University
    Inventors: Kenichiro Itami, Junichiro Yamaguchi, Kei Muto
  • Publication number: 20140235867
    Abstract: The present invention relates to a specific thiazolium salt used for producing an ?-hydroxy ketone compound, and a method for producing an ?-hydroxy ketone compound by carrying out a coupling reaction of an aldehyde compound in the presence of a base compound and the specific thiazolium salt.
    Type: Application
    Filed: August 27, 2012
    Publication date: August 21, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Koji Hagiya, Akio Tanaka, Toshihiro Hodai
  • Patent number: 8759382
    Abstract: Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis.
    Type: Grant
    Filed: September 29, 2011
    Date of Patent: June 24, 2014
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Eliezer Falb, Jeffrey Sterling, Yaacov Herzig, Raphael Nudelman, Konstantin Ulanenko
  • Publication number: 20140171502
    Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl] 2-methylthiopropionate which is useful as a pharmaceutically active compound.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 19, 2014
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans-Juergen Mair, Reinhard Reents, Michelangelo Scalone, Shaoning Wang, Andreas Zogg
  • Patent number: 8754113
    Abstract: A compound represented by the formula: or its pharmaceutically acceptable salt. Ring A is aromatic carbocycle or aromatic heterocycle, Z is —O— or —S—, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n—R8, R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, and m is an integer of 0 to 3.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: June 17, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Shiro Kida, Naoki Yoshikawa, Manabu Katou, Terukazu Kato, Mado Nakajima, Eiichi Kojima, Mitsuhiro Yonehara
  • Patent number: 8735528
    Abstract: Two-photon absorbing (2PA), cross-linked polyurethanes were prepared from bis(isocyanato) monomers, tris(isocyanato) monomers or a mixture thereof, in conjunction with novel polyol molecules with donor-acceptor octupolar geometry, whose generic structure is comprised of an electron-accepting 1,3,5-triazine hub with three spokes constituted by electron-donating triarylalkylamine end-groups, which are polyfunctionalized with thermally reactive alcohol functions. The resulting neat glassy or rubbery solids are applicable in a wide range of linear and nonlinear optical applications.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: May 27, 2014
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Matthew J Dalton, Ramamurthi Kannan
  • Patent number: 8703962
    Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: April 22, 2014
    Assignee: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Laykea Tafesse
  • Patent number: 8664403
    Abstract: The present invention relates to a process for the preparation of S-[2-[1-(2-ethylbutyl)cyclohexylcarbonylamino]-phenyl]2-methylthiopropionate which is useful as a pharmaceutically active compound.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: March 4, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans-Juergen Mair, Reinhard Reents, Michelangelo Scalone, Shaoning Wang, Andreas Zogg
  • Patent number: 8648081
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Grant
    Filed: May 8, 2012
    Date of Patent: February 11, 2014
    Assignee: Eli Lilly and Company
    Inventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
  • Publication number: 20130331413
    Abstract: Disclosed are compositions and methods for treating and/or preventing infections in mammals, by administering to a mammal a therapeutically effective amount of at least one defensin-like molecule, e.g., in a composition that includes such molecule. Also disclosed are kits that include such molecules, or compositions that include such molecules, as well as instructions for using such molecules to treat a mammal.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 12, 2013
    Inventors: Erik DE LEEUW, Alexander D. MACKERELL, JR.
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8592467
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
    Type: Grant
    Filed: June 22, 2009
    Date of Patent: November 26, 2013
    Assignee: Abbvie Inc.
    Inventors: Marlon D. Cowart, Minghua Sun, Chen Zhao, Guo Zhu Zheng
  • Patent number: 8592603
    Abstract: The present invention provides a method of preparing a compound of formula 6 comprising: (a) reacting a compound of formula 1 with a compound of formula 2 to form a compound of formula 3 wherein X of formula 2 is Cl or OH; (b) treating the compound formula 3 with Lawesson's reagent to form a compound of formula 4 (c) reacting a compound of formula 4 with potassium ferricyanide to produce a compound of formula 5 and (d) performing catalytic reduction of nitro group of the compound of formula 5 with palladium on charcoal to generate the compound of formula 6, wherein R1 of formulae 1-6 is H, C1-10 alkyl, C1-10 alkoxy or C1-10 haloalkyl, and R2 of formulae 1-6 is H or C1-10 alkyl.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: November 26, 2013
    Assignee: Kaohsiung Medical University
    Inventors: Jeh-Jeng Wang, Chao-Cheng Liao, Wan-Ping Hu, Ho-Chuan Shen
  • Patent number: 8586205
    Abstract: Disclosed herein are compounds represented by a formula: Wherein Ar1, Cb, Ph1, Het1, and A are described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Grant
    Filed: September 15, 2010
    Date of Patent: November 19, 2013
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, David T. Sisk, Brett T. Harding, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae, Sazzadur Rahman Khan, Liping Ma, Rebecca Bottger
  • Patent number: 8586325
    Abstract: Enzyme substrates and associated technology of the present invention are provided. An enzyme substrate of the invention may comprise a biologically functional fluorescent dye and an enzyme-specific substrate moiety attached in such a way that the functionality of the functional dye is diminished. An enzymatic reaction may cleave at least a portion of the substrate moiety from the enzyme substrate to provide a more functional product dye. This product dye may be nonfluorescent or weakly fluorescent, in general, and relatively fluorescent, in a particular condition, such as when bound to a partner biological molecule or an assembly of partner biological molecules. An enzyme substrate of the present invention may thus be useful in fluorescence detection, and/or in any of a variety of useful applications, such as the detection of enzymatic activity in a cell-free system or in a living cell, the screening of drugs, or the diagnosis of disease.
    Type: Grant
    Filed: May 10, 2013
    Date of Patent: November 19, 2013
    Assignee: Biotium, Inc.
    Inventors: Fei Mao, Hui Cen
  • Publication number: 20130217699
    Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
    Type: Application
    Filed: May 8, 2012
    Publication date: August 22, 2013
    Applicant: ELI LILLY AND COMPANY
    Inventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
  • Patent number: 8513291
    Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
    Type: Grant
    Filed: June 1, 2011
    Date of Patent: August 20, 2013
    Assignee: Angion Biomedica Corp.
    Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
  • Patent number: 8481574
    Abstract: 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: Grant
    Filed: October 12, 2007
    Date of Patent: July 9, 2013
    Assignee: Abbott Laboratories
    Inventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
  • Publication number: 20130172570
    Abstract: This present invention provides a method of making benzazoles comprising a process of making aryl or alkyl benzazoles from corresponding aryl acid chlorides or alkyl acid chlorides without applying hazard condensing agent. The benzazole compounds described in this invention have following formula I: Wherein: n is an integer of from 3 to 8; Z is O, NR or S; and R and R? are individually hydrogen; alkyl of from 1 to 24 carbon atoms, for example, propyl, t-butyl, heptyl, and the like; aryl or hetero-atom substituted aryl of from 5 to 20 carbon atoms, for example, phenyl and naphthyl, furyl, thienyl, pyridyl, quinolinyl and other heterocyclic systems; or halo such as chloro, fluoro, bromo, cyano; or atoms necessary to complete a fused aromatic ring; and B is a linkage unit consisting of alkyl, aryl, substituted alkyl, or substituted aryl which conjugately or unconjugately connects the multiple benzazoles together.
    Type: Application
    Filed: February 15, 2012
    Publication date: July 4, 2013
    Applicant: US Government as Represented by the Secretary of the ARMY
    Inventors: Jianmin Shi, Eric W. Forsythe, David C. Morton
  • Patent number: 8461348
    Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: June 11, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Matsunaga, Yoshihisa Nakada, Yusuke Ohba, Hideyuki Nakagawa
  • Patent number: 8440674
    Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I wherein R1 is and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: May 14, 2013
    Assignee: Amgen Inc.
    Inventors: Frenel F. De Morin, Jian J. Chen, Elizabeth M. Doherty, Stephen A. Hitchcock, Qi Huang, Joseph L. Kim, Gang Liu, Thomas Nixey, Nick A. Paras, Jeffrey Petkus, Daniel Martin Retz, Adrian Leonard Smith, Jiawang Zhu
  • Patent number: 8399504
    Abstract: This invention relates to novel compounds of the Formula (I) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: March 19, 2013
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjie Ye, Suresh B. Singh, Colin M. Tice
  • Patent number: 8389555
    Abstract: A compound of formal (I) is described: wherein R1 and R2 are as defined in the text and wherein the compounds are intended for use in treating medical conditions characterized by an imbalance in dopamine receptor activity.
    Type: Grant
    Filed: October 28, 2008
    Date of Patent: March 5, 2013
    Assignee: Motac Neuroscience Limited
    Inventors: Holger Stark, Jukka Matti Leppanen, Britta Caroline Sasse, Oliver Saur, Tim Kottke, Michael Peter Hill
  • Patent number: 8372991
    Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1 and R4 are defined herein, 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 or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: February 12, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8372380
    Abstract: Radiolabeled tracers for sulfotransferases (SULTs), their synthesis, and their use are provided. Included are substituted phenols, naphthols, coumarins, and flavones radiolabeled with 18F, 123I, 124I, 125I, or 11C. Also provided are in vivo techniques for using these and other tracers as analytical and diagnostic tools to study sulfotransferase distribution and activity, in health and disease, and to evaluate therapeutic interventions.
    Type: Grant
    Filed: March 31, 2008
    Date of Patent: February 12, 2013
    Assignee: The Regents of the University of California
    Inventors: Jorge R. Barrio, Vladimir Kepe, Gary W. Small, Nagichettiar Satyamurthy
  • Publication number: 20130004422
    Abstract: This invention provides benzothiazole derivative compounds, compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for detecting amyloid deposit(s) and for diagnosing a disease, disorder or condition characterized by amyloid deposit(s).
    Type: Application
    Filed: July 12, 2012
    Publication date: January 3, 2013
    Inventors: William E. KLUNK, Chester A. MATHIS, JR., Yanming WANG
  • Patent number: 8329700
    Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: March 7, 2011
    Date of Patent: December 11, 2012
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Matthew Paul Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
  • Patent number: 8329706
    Abstract: The present invention relates to oxazolidinone derivatives of formula (I) wherein Y, R3 and R4 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: December 11, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Christine Brotschi, Markus Gude, Romain Siegrist, Thierry Sifferlen, Jodi T Williams
  • Patent number: 8323805
    Abstract: Disclosed herein are compounds represented by a formula: R1—O-A-C?C-D, where R1, A, and D are defined as described herein. Compositions and light-emitting devices related thereto are also disclosed.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: December 4, 2012
    Assignee: Nitto Denko Corporation
    Inventors: Shijun Zheng, Jensen Cayas, Sheng Li, Amane Mochizuki, Hyunsik Chae
  • Patent number: 8318888
    Abstract: Two-photon absorbing (2PA), cross-linked polyurethanes were prepared from bis(isocyanato) monomers, tris(isocyanato) monomers or a mixture of bis(isocyanato) and tris(isocyanato) monomers, in conjunction with a novel polyol molecules with donor-acceptor octupolar geometry, whose generic structure is comprised of an electron-accepting 1,3,5-triazine hub with three spokes constituted by electron-donating triarylalkylamine end-groups, which are polyfunctionalized with thermally reactive alcohol functions. The resulting neat glassy or rubbery solids are applicable in a wide range of linear & nonlinear optical applications.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: November 27, 2012
    Assignee: The United States of America as represented by the Secretary of the Air Force
    Inventors: Loon-Seng Tan, Matthew Dalton, Ramamurthi Kannan
  • Patent number: 8299065
    Abstract: Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, or —C(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N? or —CH?Z2 is —N? or —C(R1)?; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic ra
    Type: Grant
    Filed: December 12, 2008
    Date of Patent: October 30, 2012
    Assignee: Biota Europe Ltd.
    Inventors: David John Haydon, Lloyd George Czaplewski
  • Patent number: 8278337
    Abstract: Disclosed are compounds of the formula (I) wherein X is N or CH, and Y is N or CR5. Also disclosed are methods of treating JNK and ERK mediated diseases using the compounds of formula 1.0.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme
    Inventors: David B. Belanger, M. Arshad Siddiqui, Patrick J. Curran, Blake Hamann, Lianyun Zhao, Panduranga Adulla P. Reddy, Praveen K. Tadikonda, Gerald W. Shipps, Jr., Umar Faruk Mansoor
  • Patent number: 8273769
    Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: September 25, 2012
    Assignee: Merck Serono SA
    Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Christophe Cleva, Adeline Pretre