Chalcogen Or Nitrogen Attached Directly To The Other Cyclo Of The Bicyclo Ring System By Nonionic Bonding Patents (Class 548/178)
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Patent number: 10913972Abstract: Described are luciferin analogues, methods for making the analogues, kits including the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays.Type: GrantFiled: July 19, 2019Date of Patent: February 9, 2021Assignee: Promega CorporationInventors: Lance P. Encell, Mary P. Hall, Michael Killoran, Thomas A. Kirkland, Poncho Meisenheimer, Ce Shi
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Patent number: 10745365Abstract: A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided.Type: GrantFiled: August 22, 2018Date of Patent: August 18, 2020Assignee: Promega CorporationInventors: James J. Cali, William Daily, Erika Hawkins, Dieter Klaubert, Jianquan Liu, Poncho Meisenheimer, Michael Scurria, John W. Shultz, James Unch, Michael P. Valley, Keith V. Wood, Wenhui Zhou
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Patent number: 10400264Abstract: Described are luciferin analogs, methods for making the analogs, kits including the analogs, and methods of using the compounds for the detection of luminescence in luciferase-based assays.Type: GrantFiled: December 1, 2017Date of Patent: September 3, 2019Assignee: PROMEGA CORPORATIONInventors: Lance P. Encell, Mary P. Hall, Michael Killoran, Thomas A. Kirkland, Poncho Meisenheimer, Ce Shi
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Patent number: 9814787Abstract: This disclosure relates to luciferin amides of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to detect fatty acid amide hydrolase activities in vitro, in live cells, or in vivo.Type: GrantFiled: June 3, 2016Date of Patent: November 14, 2017Assignee: University of MassachusettsInventor: Stephen C. Miller
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Patent number: 9434720Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.Type: GrantFiled: May 6, 2014Date of Patent: September 6, 2016Assignee: DIRMIRA (CANADA), INC.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Publication number: 20150148546Abstract: Provided is a photosensitive resin composition having high sensitivity and storage stability.Type: ApplicationFiled: January 28, 2015Publication date: May 28, 2015Applicant: FUJIFILM CorporationInventors: Kyouhei SAKITA, Shinji FUJIMOTO, Mikio NAKAGAWA, Kenta YAMAZAKI
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Publication number: 20150141657Abstract: 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: ApplicationFiled: February 15, 2012Publication date: May 21, 2015Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Kamal Ahmed, Ratna Reddy Challa, Prabhakar Singaraboina
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Publication number: 20150099883Abstract: The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R1 represents an ethyl group or the like, R2 represents a hydrogen atom or the like, R3 and R4 represents a methyl group or the like, X1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X2 represents a methyl group or the like, m2 is an integer of 0 to 3.Type: ApplicationFiled: April 8, 2013Publication date: April 9, 2015Inventors: Hironori Furukawa, Daisuke Hanai, Tetsuo Tamai, Jun Kanazawa, Katsunori Tanaka, Asaho Nagagata
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Patent number: 8993561Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.Type: GrantFiled: November 18, 2011Date of Patent: March 31, 2015Assignee: SanofiInventor: Alain Pellet
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Patent number: 8980892Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: GrantFiled: February 18, 2010Date of Patent: March 17, 2015Assignees: Syngenta Crop Protection LLC, Syngenta LimitedInventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
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Patent number: 8969580Abstract: A diagnostic imaging agent useful for positron emission tomography (PET) imaging as well as to improved hardware for producing such imaging agents is described. Flutemetamol (18F) Injection for the imaging of b amyloid plaques in the brain and methods and devices for preparing same are described including the automated synthesis and purification of [18F]flutemetamol by means of solid phase extraction (SPE).Type: GrantFiled: October 8, 2010Date of Patent: March 3, 2015Assignee: GE Healthcare LimitedInventors: Eric Horn, Steven Fairway, Dimitrios Mantzilas, Nigel Powell
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Patent number: 8962854Abstract: An object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate. The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.Type: GrantFiled: August 22, 2012Date of Patent: February 24, 2015Assignee: The University of Electro-CommunicationsInventors: Shigeru Nishiyama, Tsuyoshi Saito, Shojiro Maki, Haruki Niwa
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Patent number: 8957219Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.Type: GrantFiled: October 15, 2009Date of Patent: February 17, 2015Assignee: Shionogi & Co., Ltd.Inventors: Koji Masuda, Shiro Kida, Kyohei Hayashi, Manabu Katou, Naoki Yoshikawa, Akira Kugimiya, Mado Nakajima, Nobuyuki Tanaka
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150038515Abstract: Pharmaceutical compositions of the invention comprise covalently closed circular DNA formation inhibitors having a disease-modifying action in the treatment of diseases associated with the formation of covalently closed circular DNA that include hepatitis B infection, and any disease involving formation of covalently closed circular DNA.Type: ApplicationFiled: February 28, 2013Publication date: February 5, 2015Inventors: Andrea Cuconati, Haitao Guo, Timothy M. Block, Ju-Tao Guo, Xiaodong Xu, Huagang Lu, Dawei Cai
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Publication number: 20140371278Abstract: Disclosed are compound of formula (I) and pharmaceutically accepted salts and prodrugs thereof, wherein each of R1, R2, R3, R4, R5, R6, X1 and X2 is as defined in the description. These compounds are protein kinases inhibitors, especially the inhibitors of Mek, which are useful in the treatment of cancers and inflammation of mammals. Disclosed are the treatment methods of cancers and inflammation of mammals as well as pharmaceutical compositions comprising the compounds described herein. The preparation of benzoheterocyclic compounds are disclosed. Disclosed are the preparation of potential drug candidates, such as benzooxazol, benzothiazol, benzothiadiazol and the like.Type: ApplicationFiled: January 16, 2013Publication date: December 18, 2014Applicant: TIANJIN BINJIANG PHARMA, INC.Inventors: Hongqi Tian, Conghui Ji, Chunlei Liu, Li Kong, Ying Cheng, Gongchao Huang
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Patent number: 8895313Abstract: Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.Type: GrantFiled: September 23, 2009Date of Patent: November 25, 2014Assignee: Wista Laboratories Ltd.Inventors: Steven John Kemp, Lynda Jane Storey, John Mervyn David Storey, Janet Rickard, Charles Robert Harrington, Claude Michel Wischik, Scott Clunas, Tobias Kerst Heinrich
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Publication number: 20140341812Abstract: Novel derivatives of imidazopyridinylbenzeneamines and novel derivatives of benzothiazolylbenzeneamines are disclosed that offer improved behavior when used as imaging agents for positron emission tomography of beta-amyloids. Also disclosed is a palladium-catalyzed reaction scheme under microwave conditions for aryl thioethers in general that provides a high ratio of substitution relative to reduction and can be used for the imidazopyridinylbenzeneamine derivatives as well as other compounds of related structure.Type: ApplicationFiled: March 24, 2014Publication date: November 20, 2014Applicant: The United States of America, as represented by the Secretary, Department of Health and Human ServInventors: Lisheng Cai, Victor W. Pike, Robert B. Innis
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Publication number: 20140343070Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof, or a prodrug theType: ApplicationFiled: August 1, 2014Publication date: November 20, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Patent number: 8883437Abstract: The invention relates to the use of a compound having formula (I) as an enzymatic substrate for the detection of a nitroreductase activity, wherein: W1, W2, W3 and W4 are independently H, Br, Cl, F, I, alkyl, alkoxy, thiomethyl, perfluoroalkyl, nitro, cyano, carboxyl (including the esters or amides thereof) or any combination of same; n=0, 1 or 2; X is NR, CZ5Z6, S or O, R being H, alkyl, aralkyl, aryl, alkanoic or alkylsulphonic, Z5 and Z6 being an alkyl; Y is N or N+R, R being alkyl, aralkyl, aryl, alkanoic or alkylsulphonic; Z1, Z2, Z3 and Z4 are independently H, Br, Cl, F, I, alkyl, aryl, alkoxy, perfluoroalkyl, nitro, cyano, carboxyl, sulphonyl, including the sulphonyl or carboxyl amides or esters thereof, and the salts of same.Type: GrantFiled: July 29, 2010Date of Patent: November 11, 2014Assignee: bioMérieux S.A.Inventors: Olivier Fabrega, Arthur James, Sylvain Orenga, John Perry, Vindhya Salwatura, Stephen Stanforth
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Publication number: 20140303171Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
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Publication number: 20140288302Abstract: A pharmaceutical composition including a compound of formula (I): its pharmaceutically acceptable salt, or a solvate thereof. Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by formula: —C(R1R2)—C(?O)—NR3R4 and a group represented by formula: —R5, a broken line represents presence or absence of a bond, Z is —NR6—, ?N—, —O—, or —S—, R6 is halogen or substituted or unsubstituted alkyl, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen or substituted or unsubstituted alkyl, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted alkynyl.Type: ApplicationFiled: March 18, 2014Publication date: September 25, 2014Applicant: Shionogi & Co., Ltd.Inventors: Koji MASUDA, Shiro KIDA, Kyohei HAYASHI, Manabu KATOU, Naoki YOSHIKAWA, Akira KUGIMIYA, Mado NAKAJIMA, Nobuyuki TANAKA
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Publication number: 20140275064Abstract: The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.Type: ApplicationFiled: August 17, 2012Publication date: September 18, 2014Applicant: DIAXONHITInventors: Bertrand Leblond, Anne-Sophie Casagrande, Laurent Desire, Alicia Foucourt, Thierry Besson
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Publication number: 20140246094Abstract: Asymmetric dyes of the D-?-A type have the Formula (1), including the valence tautomers thereof. The dyes of Formula (1) are suitable for use in dye-sensitized solar cells (DSSC), in photoelectrochemical devices or in photonic devices. A solar cell and a device for photoelectric conversion contain an asymmetric dye of Formula (1). The dyes of Formula (1) are also suitable for conjugating with optically active nanoparticles (NP).Type: ApplicationFiled: August 24, 2012Publication date: September 4, 2014Applicant: PIANETA S.R.L.Inventor: Giuseppe Caputo
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Publication number: 20140242627Abstract: Methods, kits and compositions containing a mixture of D-luciferin and L-luciferin for light generation with luciferase are disclosed that have improved stability when stored over time. The mixture of D-luciferin and L-luciferin can be used to detect the presence or amount of ATP or of luciferase in a sample.Type: ApplicationFiled: February 21, 2014Publication date: August 28, 2014Applicant: PROMEGA CORPORATIONInventors: Michael P. Valley, James J. Cali, Brock Binkowski, Christopher Todd Eggers, Keith V. Woods
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Publication number: 20140221665Abstract: An object of the present invention to provide a firefly luciferin and firefly luciferin analog that are modified to maintain luminescent activity by luciferase in a firefly bioluminescent system. In particular, it is an object of the present invention to provide a new luminescent substrate for which the emission wavelength in a firefly bioluminescent system is shifted to a longer wavelength than that of a conventional luminescent substrate. The present invention provides a luciferin in which the benzothiazole ring moiety has been modified at the 7-position, a luciferin analog in which the benzene ring moiety has been modified at the 6-position, and a luciferin analog in which the 6-(dialkylamino)-2-naphthalenyl moiety has been modified at the 5-position.Type: ApplicationFiled: August 22, 2012Publication date: August 7, 2014Applicant: THE UNIVERSITY OF ELECTRO-COMMUNICATIONSInventors: Shigeru Nishiyama, Tsuyoshi Saito, Shojiro Maki, Haruki Niwa
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Publication number: 20140221319Abstract: The invention provides methods and compositions for inhibiting CD 38 activity, and methods of treating or preventing various disorders associated with CD38 activity.Type: ApplicationFiled: April 13, 2012Publication date: August 7, 2014Applicants: Mayo Foundation for Medical Education and Research, President and Fellows of Harvard CollegeInventors: David A. Sinclair, Nathan L. Price, Eduardo N. Chini, Jon C. Clardy, Shugeng Cao
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Publication number: 20140193340Abstract: This disclosure relates to luciferin amides of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to detect fatty acid amide hydrolase activities in vitro, in live cells, or in vivo.Type: ApplicationFiled: March 15, 2013Publication date: July 10, 2014Applicant: University of MassachusettsInventor: Stephen C. Miller
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Patent number: 8772501Abstract: The present invention provides fluorescent dyes that are based on firefly luciferin structure. These dyes are optimally excited at shorter wavelengths and have Stokes shift of at least 50 nm. The fluorescent dyes of the invention are useful for preparation of dye-conjugates, which can be used in detection of an analyte in a sample.Type: GrantFiled: January 24, 2013Date of Patent: July 8, 2014Assignee: Beckman Coulter, Inc.Inventors: Hashem Akhavan-Tafti, Renuka De Silva, Guoping Wang, Robert A. Eickholt, Ravinder Gupta, Lakshmi S. Kaanumalle
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Patent number: 8765969Abstract: The invention provides compounds, compositions, methods, substrates, and kits useful for analyzing the metabolic activity in cells, tissue, and animals and for screening test compounds for their effect on cytochrome P450 activity. In particular, a one-step and two-step methods using luminogenic molecules, e.g. luciferins or coelenterazines, that are cytochrome P450 substrates and that are also bioluminescent enzyme, e.g., luciferase, pro-substrates are provided. The present method further provides a method for stabilizing and prolonging the luminescent signal in a luciferase-based assay using luciferase stabilizing agents such as reversible luciferase inhibitors.Type: GrantFiled: July 3, 2008Date of Patent: July 1, 2014Assignee: Promega CorporationInventors: James J. Cali, Dieter Klaubert, William Daily, Samuel K. Ho, Susan Frackman, Erika Hawkins, Keith V. Wood
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Publication number: 20140171438Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.Type: ApplicationFiled: December 9, 2013Publication date: June 19, 2014Applicant: CELLCEUTIX CORPORATIONInventors: Wenxi Pan, Haizhong Tang
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Patent number: 8754233Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.Type: GrantFiled: February 25, 2013Date of Patent: June 17, 2014Assignee: Dermira (Canada), Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Patent number: 8754216Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: GrantFiled: September 26, 2011Date of Patent: June 17, 2014Assignee: OPKO Health, Inc.Inventors: Sapna S. Shah, Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Neng-Yang Shih
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Publication number: 20140154716Abstract: A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided.Type: ApplicationFiled: June 10, 2013Publication date: June 5, 2014Inventors: James J. Cali, William Daily, Erika Hawkins, Dieter Klaubert, Jianquan Liu, Poncho Meisenheimer, Michael Scurria, John W. Shultz, James Unch, Michael P. Valley, Keith V. Wood, Wenhui Zhou
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Patent number: 8722887Abstract: This invention concerns compounds of the general formula (1): and derivatives thereof, which are antagonists of 5-HT6 receptors, wherein the symbols have the meanings given in the description.Type: GrantFiled: February 16, 2010Date of Patent: May 13, 2014Assignee: Abbvie Bahamas, Ltd.Inventors: Arnold Van Loevezijn, Wouter I. Iwema Bakker, Hiskias G. Keizer, Jan Zorgdrager, Martina A. W. Van Der Neut, Cornelis G. Kruse
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Publication number: 20140121371Abstract: This disclosure relates to processes and reagents for making diaryliodonium salts, which are useful for the preparation of fluorinated, iodinated, astatinated and radiofluorinated aromatic compounds.Type: ApplicationFiled: October 25, 2013Publication date: May 1, 2014Applicant: Ground Fluor Pharmaceuticals, Inc.Inventor: Stephen G. DiMagno
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Patent number: 8703938Abstract: 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: GrantFiled: September 10, 2010Date of Patent: April 22, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Ce Wang, Lu Ying, Xiaowen Peng, Yao-Ling Qiu
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Publication number: 20140018325Abstract: Compounds of Formula I are disclosed wherein R1, R2, R3A, R3B, R4A, R4B, R5A, R5B, R6A, R6B, R8 and R9 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 27, 2011Publication date: January 16, 2014Inventors: Michael John Boyd, Carmela Molinaro, Amelia Roy, Vouy Linh Truong
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Publication number: 20140018326Abstract: Compounds of Formula I are disclosed: wherein L, A, R1, R2, R3A, R3B, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 27, 2011Publication date: January 16, 2014Inventors: Oscar M. Moradei, Sheldon Crane, Daniel J. Mckay, Marie-Eve Lebrun, Vouy Linh Truong
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Patent number: 8629285Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: August 10, 2006Date of Patent: January 14, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
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Publication number: 20140005385Abstract: According to the present invention, a tetrazoyloxime derivative and a salt thereof, which are excellent in a control effect against plant disease injury, and a plant disease controlling agent containing the same as an active ingredient are provided.Type: ApplicationFiled: August 29, 2013Publication date: January 2, 2014Applicant: Nippon Soda Co., Ltd.Inventors: Takeo Kobori, Hazumi Nomura, Ichirou Urihara, Hiroyasu Hosokawa, Atsunori Isshiki, Syuichi Ito, Jun Inagaki, Kazushige Fujii
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Publication number: 20140005409Abstract: A compound represented by the following formula (I): wherein in formula (I), R1 represents a hydrogen atom, an alkyl group, an alkenyl group, an alkoxy group, an alkoxycarbonyl group, an acyl group, a carbamoyl group, a sulfamoyl group, a sulfo group, a cyano group, an aryl group or a heteroaryl group; R2 represents an alkyl group or an aryl group; each of R3 and R4 independently represents a hydrogen atom, an alkyl group, an alkenyl group, an alkoxy group, an alkoxycarbonyl group, a carbonyl group or an aryl group; X represents —O—, —S—, —NH—, —NR5—, —CH2—, —CR6H— or —CR6R7—; each of R5 to R7 independently represents an alkyl group or an aryl group; and R1 and any one of R5 to R7, or R3 and R4, may be bonded to each other to form a ring.Type: ApplicationFiled: September 5, 2013Publication date: January 2, 2014Applicant: FUJIFILM CORPORATIONInventors: Youhei ISHIJI, Masanori HIKITA
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Publication number: 20130345196Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.Type: ApplicationFiled: May 24, 2012Publication date: December 26, 2013Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
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Patent number: 8586759Abstract: Methods and systems to generate 6-amino-6-deoxy-D-luciferin precursor, 2-cyano-6-aminobenzothiazole and related compounds and derivatives.Type: GrantFiled: February 28, 2011Date of Patent: November 19, 2013Assignee: Lawrence Livermore National Security, LLCInventors: Amy L. Gryshuk, Julie Perkins, John V. LaTour
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Publication number: 20130302248Abstract: Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formula (I) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.Type: ApplicationFiled: June 25, 2013Publication date: November 14, 2013Inventors: Umesh B. Gangadharmath, Hartmuth C. Kolb, Peter J.H. Scott, Joseph C. Walsh, Wei Zhang, Anna Katrin Szardenings, Anjana Sinha, Gang Chen, Eric Wang, Vani P. Mocharla, Chul Yu, Changhui Liu, Daniel Kurt Cashion, Dhanalakshmi Kasi
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Publication number: 20130287699Abstract: The present disclosure features a condensation reaction and a luciferin-unmasking reaction that can be carried out under physiological conditions. In general, the condensation reaction involves reacting a bicyclic reactant with an aminothiol derivative, generating a luciferin or luciferin derivative. A luciferin can provide detectable luminescence. A luciferin derivative can be unmasked to provide detectable luminescence in a luciferin-unmasking reaction. The present disclosure provides bicyclic reactants and aminothiol derivatives suitable for use in the condensation reaction. The condensation and luciferin-unmasking reactions find use in a variety of applications, which are also provided.Type: ApplicationFiled: January 15, 2013Publication date: October 31, 2013Inventors: Christopher J. Chang, Carolyn R. Bertozzi, Genevieve C. van de Bittner, Elena A. Dubikovskaya
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Patent number: 8558003Abstract: The present invention relates to compounds and methods for imaging and treating Alzheimer's disease or an amyloidosis-associated pathological condition that utilize a novel amyloid imaging tracer for detecting amyloid deposits in a subject suffering from these conditions. In certain embodiments, the invention relates to [N-2[18F]fluoropropyl]-2-(4?-(methylamino)-phenyl)-6-hydroxybenzothiazole (F-18MHT) and dimers thereof.Type: GrantFiled: August 11, 2010Date of Patent: October 15, 2013Assignee: The General Hospital CorporationInventors: David R. Elmaleh, Timothy M. Shoup, Alan J. Fischman
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Patent number: 8558004Abstract: The present invention relates to reagents and methods for influenza virus detection. These reagents and methods disclosed in the present invention enable simple, rapid, specific and sensitive detection of influenza virus types A and B. These reagents are N-acetylneuraminic acid-firefly luciferin conjugates which can be cleaved by influenza virus neuraminidase.Type: GrantFiled: February 2, 2011Date of Patent: October 15, 2013Assignee: Cellex, Inc.Inventors: Xing-Xiang Li, Tianxin Wang
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Publication number: 20130245025Abstract: 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 or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 3, 2013Publication date: September 19, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20130245008Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.Type: ApplicationFiled: November 18, 2011Publication date: September 19, 2013Applicant: SANOFIInventor: Alain Pellet