Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 546/94)
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Publication number: 20110160243Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: ApplicationFiled: August 26, 2009Publication date: June 30, 2011Applicant: Arena Pharmaceuticals ,Inc.Inventors: Robert M. Jones, Daniel J. Buzard, Andrew M. Kawasaki, Sun Hee Kim, Lars Thoresen, Juerg Lehmann, Xiuwen Zhu
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Patent number: 7968564Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: April 15, 2010Date of Patent: June 28, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph P. Vacca, Linda S. Payne, Richard C. A. Isaacs
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Publication number: 20110135958Abstract: Disclosed are a compound that emits fluorescence, particularly in its solid state, and is suited to provide a color converting material with various improved performance properties over prior art and a light emitter, a color conversion filter, a color conversion device, and a photoelectric device each containing the compound; particularly a Schiff base type compound of formula (I) and a coloring material, a color conversion layer, a light absorbing layer, a color conversion filter, a light absorbing filter, a color-converting light-emitting device, and a photoelectric device each containing the compound. The definition of the symbols in formula (I) is the same as in the specification.Type: ApplicationFiled: June 30, 2010Publication date: June 9, 2011Applicant: ADEKA CORPORATIONInventors: Mitsuhiro Okada, Koichi Shigeno
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Patent number: 7947704Abstract: The invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I), in which CKE, W, X and Y are as defined above, to a plurality of processes and intermediates for their preparation and to their use as pesticides and/or herbicides, and also to selective herbicidal compositions comprising firstly the 2,4,6-phenyl-substituted cyclic ketoenols and secondly at least one compound which improves crop plant tolerance.Type: GrantFiled: March 11, 2005Date of Patent: May 24, 2011Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Reiner Fischer, Oliver Gaertzen, Klaus Kunz, Stefan Lehr, Dieter Feucht, Peter Lösel, Olga Malsam, Guido Bojack, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne, Chris Rosinger
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Publication number: 20110118241Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: ApplicationFiled: May 5, 2009Publication date: May 19, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110118301Abstract: The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to ?7 nicotinic acetylcholine receptors also are described.Type: ApplicationFiled: January 24, 2011Publication date: May 19, 2011Applicant: ABBOTT LABORATORIESInventors: Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Diana L. Nersesian
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Publication number: 20110112067Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Publication number: 20110092535Abstract: The present invention resides in the use of a 5-HT3 receptor antagonist as medicament for the treatment of temporal lobe epilepsy associated with hippocampal sclerosis (TLE-HS) in a human patient. Tropisetron or Dolasetro are the preferred compounds.Type: ApplicationFiled: July 21, 2006Publication date: April 21, 2011Inventor: Nicholas Mark Barnes
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Patent number: 7915282Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) in which W, X, Y, Z and CKE are as defined in the description, to processes for their preparation and to their use as pesticides and herbicides.Type: GrantFiled: March 21, 2001Date of Patent: March 29, 2011Assignee: Bayer AktiengesellschaftInventors: Michael Ruther, Hermann Hagemann, Udo Schneider, Markus Dollinger, Peter Dahmen, Ulrike Wachendorff-Neumann, Reiner Fischer, Alan Graff, Thomas Bretschneider, Christoph Erdelen, Mark Wilhelm Drewes, Dieter Feucht, Folker Lieb
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Publication number: 20110061723Abstract: The present invention pertains to an electrode layer comprising a porous film made of oxide semiconductor fine particles sensitized with certain methin dyes. Moreover the present invention pertains to a photoelectric conversion device comprising said electrode layer, a dye sensitized solar cell comprising said photoelectric conversion device and to novel methin dyes.Type: ApplicationFiled: February 26, 2009Publication date: March 17, 2011Applicant: BASF SEInventors: Kazuhiko Kunimoto, Hiroshi Yamamoto, Shinji Nakamichi, Ryuichi Takahashi, Junichi Tanabe
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Publication number: 20110053162Abstract: The invention provides compounds and compositions of Formulas I-VII, and methods of using the compounds. The compounds can be used to prepare dye conjugates that are uniformly and substantially more fluorescent on proteins, nucleic acids or other biopolymers, than conjugates labeled with structurally similar known carbocyanine dyes. In addition to having more intense fluorescence emission than structurally similar dyes at virtually identical wavelengths, and decreased artifacts in their absorption spectra upon conjugation to biopolymers, the compounds can have greater photostability and/or higher absorbance (extinction coefficients) at the wavelength(s) of peak absorbance than such structurally similar dyes.Type: ApplicationFiled: August 31, 2010Publication date: March 3, 2011Applicant: PROMEGA CORPORATIONInventors: Cesear Corona, Dieter Klaubert, Mark McDougall
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Publication number: 20110039832Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-a]isoquinoline and pyrrolo[2,1-a]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: February 6, 2009Publication date: February 17, 2011Applicant: N.V. OrganonInventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lar Anders van der Veen, Willem Frederik Johan Karstens
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Patent number: 7875215Abstract: The invention provides a near-infrared-absorbing material comprising at least one first compound selected from the group consisting of a singlet oxygen scavenger, a radical trapping agent and an antioxidant and at least one second compound represented by the following formula (II-1) or (II-2).Type: GrantFiled: September 21, 2007Date of Patent: January 25, 2011Assignee: FUJIFILM CorporationInventors: Keizo Kimura, Katsuyoshi Yamakawa, Osama Uchida
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Publication number: 20110003824Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2-X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.Type: ApplicationFiled: September 16, 2010Publication date: January 6, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORDTEDInventors: Jean-Damien Charrier, Guy Brenchley
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Publication number: 20100311977Abstract: To provide a method whereby a 2-azaadamantane can easily be obtained in good yield. A method for producing a 2-azaadamantane represented by the formula (1), which comprises cyclizing a compound represented by the following formula (2) in the presence of an acid.Type: ApplicationFiled: November 20, 2008Publication date: December 9, 2010Applicants: Nissan Chemical Industries, Ltd., Tohoku Techno Arch Co., Ltd.Inventors: Toshimasa Hamada, Noriaki Nagahama, Masami Kozawa, Yoshiharu Iwabuchi, Masatoshi Shibuya, Masaki Tomizawa, Yusuke Sasano
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Publication number: 20100273824Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: January 18, 2008Publication date: October 28, 2010Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Philippe Meyer, Peteris Alberts, Mainkar S. Prathama
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Publication number: 20100256698Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: ApplicationFiled: April 2, 2010Publication date: October 7, 2010Applicant: MERCK & CO., INC.Inventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
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Publication number: 20100240648Abstract: Certain hexahydro-pyrrolo-isoquinoline compounds are histamine H3 receptor and serotonin transporter modulators useful in the treatment of histamine H3 receptor- and serotonin-mediated diseases.Type: ApplicationFiled: June 2, 2010Publication date: September 23, 2010Inventors: Richard Apodaca, Ann J. Barbier, Nicholas I. Carruthers, Leslie A. Gomez, John M. Keith, Timothy W. Lovenberg, Ronald L. Wolin
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Publication number: 20100234415Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: ApplicationFiled: February 19, 2010Publication date: September 16, 2010Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey Methot
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Publication number: 20100228008Abstract: The present invention provides dyes, reactive dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins and nucleic acids. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes are also provided that comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been modified by the addition of charged and polar groups to provide beneficial properties.Type: ApplicationFiled: June 17, 2009Publication date: September 9, 2010Applicant: ENZO LIFE SCIENCES, INC. C/O ENZO BIOCHEM, INC.Inventors: Yuejun Xiang, Praveen Pande, Rajesh Khazanchi, Elazar Rabbani, Dakai Liu, Wei Cheng
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Patent number: 7790712Abstract: The application relates to compounds of formula Ia and analogues thereof wherein R1 to R13 and X are as defined herein. The invention also relates to the use of the compounds of formula Ia as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.Type: GrantFiled: March 17, 2006Date of Patent: September 7, 2010Assignee: Boehringer Ingelheim Pharmaceutical, Inc.Inventors: Derek Cogan, Donghong A. Gao, Daniel R. Goldberg, Craig Andrew Miller, Neil Moss, Matthew Russell Netherton, Philip Dean Ramsden, Zhaoming Xiong
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Publication number: 20100216988Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.Type: ApplicationFiled: December 22, 2009Publication date: August 26, 2010Applicant: SANOFI-AVENTISInventors: Jorge ALONSO, Andreas LINDENSCHMIDT, Marc NAZARE, Omar RKYEK, Matthias URMANN, Nis HALLAND
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Publication number: 20100210622Abstract: In one aspect, the present invention provides for a compound of Formula I in which the variable X1a, X1b, X1c, X1d, Q, A, R1, B, L, E, and the subscripts m and n have the meanings as described herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: December 17, 2009Publication date: August 19, 2010Inventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Peter Czabotar, Danette A. Dudley, Wayne J. Fairbrother, John A, Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Lisa A. Hasvold, Andrew M. Petros, Andrew J. Souers, Zhi-Fu Tao, Le Wang, Xilu Wang, Kurt Deshayes
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Publication number: 20100202033Abstract: A naphthopyran compound represented by the formula (I): wherein: n1, n2, p, q is an integer comprised from 0 to 5 inclusive; m is an integer comprised from 0 to 4 inclusive; R1 and R2 represent a group selected from halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —NRbRc, —CO—Ra, and —CO2Ra1, wherein Ra, Ra1, Rb and Rc, are as defined in the description; R3 represents a group selected from halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, and —NRaRa1; R4 represents a group selected from halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —CO—Ra, and —CO2Ra1; R5 represents a group selected from: halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, and —NRaRa1, wherein Ra and Ra1 are as defined hereinbefore, or when q is equal to 2, then two R5 together represent further a group —O—(CH2)q1—O— wherein q1 represents an integer comprised from 1 to 3 inclusive.Type: ApplicationFiled: September 6, 2006Publication date: August 12, 2010Applicant: Essilor International (Compagnie Generale D' Optique)Inventors: Stuart Aiken, Jean-Paul Cano, Christopher David Gabbutt, Bernard Mark Heron, Tamas Kosa, Linli Su, Ludmila Sukhomlinova, Bahman Taheri
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Publication number: 20100183603Abstract: The present invention relates to pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound or pyrrolidine-2,5-dione compound of the present invention.Type: ApplicationFiled: June 19, 2008Publication date: July 22, 2010Applicant: ARQULE, INC.Inventors: Neil Westlund, Jason Hill, Mark A. Ashwell, Nivedita Namdev, Jianqiang Wang, Syed Ali
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Publication number: 20100178291Abstract: The present invention relates to pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosucciniroide compounds of formulae (I)-(IV), and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a compound of pyrrolidin-2-one, pyrrolidin-2,5-dione, pyrrolidine and thiosuccinimide compound of the present invention.Type: ApplicationFiled: June 19, 2008Publication date: July 15, 2010Applicant: ARQULE, INC.Inventors: Jianqiang Wang, Syed M. Ali, Eugene Kelleher, Yanbin Liu, Jason Hill, Mark A. Ashwell
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Patent number: 7750160Abstract: The invention provides methods and compositions for treating conditions mediated by various kinases wherein derivatives of urea compounds are employed. The invention also provides methods of using the compounds and/or compositions in the treatment of a variety of diseases and unwanted conditions in subjects.Type: GrantFiled: November 15, 2004Date of Patent: July 6, 2010Assignee: Ambit Biosciences CorporationInventors: Zdravko V. Milanov, Hitesh K. Patel, Robert M. Grotzfeld, Shamal A. Mehta, Andiliy G. Lai, David J. Lockhart
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Patent number: 7745628Abstract: The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.Type: GrantFiled: June 26, 2006Date of Patent: June 29, 2010Assignee: Inke, S.A.Inventors: Juan Antonio Perez Andres, Pere Dalmases Barjoan
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Publication number: 20100137353Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: April 17, 2008Publication date: June 3, 2010Applicant: GLAXO GROUP LIMITEDInventor: Neil David Pearson
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Patent number: 7723352Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: September 17, 2004Date of Patent: May 25, 2010Assignee: Merck Sharp & DohmeInventors: B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
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Patent number: 7713969Abstract: The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.Type: GrantFiled: February 9, 2006Date of Patent: May 11, 2010Assignee: ArQule, Inc.Inventors: Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
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Patent number: 7696222Abstract: Compounds according to formula (I) wherein the radicals R1, R2 and R3 are as herein defined, and wherein Ar represents an aryl group or heteroaryl group, preferably phenyl, n is 1 or 2, and the radical X represents a group selected from —C(Ra)(Rb)—, —C(Ra)(Rb)—C(Ra)(Rb)—, —C(Ra)?C(Ra)—, OC(Ra)(Rb)— or SC(Ra)(Rb)—. These compounds and their pharmaceutical acceptable salts are used in pharmaceutical compositions as prostaglandine D2 receptor antagonists useful in the treatment of CRTH2-mediated diseases such as respiratory, inflammatory or allergic conditions among others.Type: GrantFiled: August 7, 2006Date of Patent: April 13, 2010Assignee: Merck Frosst Canada LtdInventor: Zhaoyin Wang
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Publication number: 20100087424Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: April 17, 2008Publication date: April 8, 2010Inventors: Pamela Brown, Steven Dabbs
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Patent number: 7691491Abstract: Novel monoaminofluorene compounds are provided, and organic light-emitting devices which exhibit good luminescence hue of extremely high purity and have optical output with high luminescence efficiency, high luminance and longer operating life are provided using the compounds.Type: GrantFiled: August 12, 2003Date of Patent: April 6, 2010Assignee: Canon Kabushiki KaishaInventors: Akihito Saitoh, Mizuho Hiraoka, Koichi Suzuki, Akihiro Senoo, Hiroshi Tanabe, Naoki Yamada, Chika Negishi
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Publication number: 20100081823Abstract: The azo dyes relate to thiophene azo dyes of the general formula: where R1 is Cyano or C1-C5 alkoxy carbonyl; R2 is hydrogen, halogene, C1-C2 alkyl, phenyl, or substituted phenyl; and R3 is C1-C5 alkoxy carbonyl, C1-C4 alkanoyl, benzoyl, phenyl, alkyl substituted phenyl, or alkoxy phenyl; or R2 and R3 are fused cycloalkane with C3-C5.Type: ApplicationFiled: September 29, 2008Publication date: April 1, 2010Inventor: Abdullah Mohamed Asiri
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Publication number: 20100056502Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: March 20, 2008Publication date: March 4, 2010Applicant: GLAXO GROUP LIMITEDInventors: Pamela Brown, Steven Dabbs, David Thomas Davies, Neil David Pearson
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Publication number: 20100056511Abstract: The invention provides compounds of formula (I), and pharmaceutically acceptable salts thereof wherein: R1, R2, R3, R4, R5, R6, R7, X and X1 are as defined herein. These compounds are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.Type: ApplicationFiled: November 21, 2007Publication date: March 4, 2010Inventors: Robert Downham, Edward Sibley Morris, Lloyd James Payne, Philip Neil Edwards, Gareth Morse Davies
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Publication number: 20100039688Abstract: A naphthopyran compound represented by the formula (I) wherein: n1, n2, p, m and q represent an integer; R1, R2 and R4, represent a group selected from halogen, —Ra, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —NRbRc, —CO—Ra, —CO2Ra1, —OC(O)—Rd, —X—(Re)—Y, linear or branched (C1-C18) perfluoroalkyl group, wherein Ra, Ra1, Rb, Rc, X, Y, Re, and Rd are as defined in the description; Z represents a group selected from CO, CS, SO, SO2, CO2, C(O)S, CS2, C(O)NH, C(O)NRa, C(S)NH, C(S)NRa and C?NRa; R3 represents a group selected from halogen, —Ra, linear or branched (C1-18) perfluoroalkyl group —OH, —ORa, —SH, —SRa, —NH2, and —NRaRa1; R6 represents a group selected from —Ra which may be optionally substituted, linear or branched (C1-18) perfluoroalkyl, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl, which may be optionally substituted; R5 represents a group selected from: halogen, —Ra, linear or branched (C1-18) perfluoroalkyl group, —OH, —ORa, —SH, —SRa, —NH2, —NRaRa1, —CO—Ra, —O—C(O)—Ra and —CO2Ra1; or when q is equaType: ApplicationFiled: September 5, 2007Publication date: February 18, 2010Inventors: Stuart Aiken, Jean-Paul Cano, Christopher David Gabbutt, Bernard Mark Heron
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Publication number: 20100035869Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.Type: ApplicationFiled: July 17, 2009Publication date: February 11, 2010Inventors: Peter Wipf, Marie Coline Frantz
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Publication number: 20100009985Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 7, 2009Publication date: January 14, 2010Applicant: ALLERGAN, INC.Inventors: Santosh C. SINHA, Smita S. BHAT, Ken CHOW, Richard L. BEARD, John E. DONELLO, Michael E. GARST
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Publication number: 20090306122Abstract: Compound of the formula (I), in which X, R1, R2 and R3 have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: February 13, 2006Publication date: December 10, 2009Inventors: Wolfgang Staehle, Timo Heinrich, Maria Kordowicz, Andree Blaukat, Lars Thore Burgdorf
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Publication number: 20090295274Abstract: The present invention discloses deuterated semiconducting organic compounds. The deuterated semiconducting organic compounds comprise at least one partially or fully deuterated non-conjugated portion linked to the conjugated portion. The mentioned deuterated semiconducting organic compounds can be used in optoelectronic devices, such as light-emitting devices and photodiodes, with enhanced performance and lifetime. The deuterated semiconducting organic compounds of this application can be employed as emissive layer, charge-transporting layer, or energy transfer material in organic light-emitting devices.Type: ApplicationFiled: February 4, 2008Publication date: December 3, 2009Inventors: Kuo-Chu Hwang, Chun-Chih Tong, Tzu-Hao Yeh
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Publication number: 20090286825Abstract: Compounds according to formula (I) wherein the radicals R1, R2 and R3 are as herein defined, and wherein Ar represents an aryl group or heteroaryl group, preferably phenyl, n is 1 or 2, and the radical X represents a group selected from —C(Ra)(Rb)—, —C(Ra)(Rb)—C(Ra)(Rb)—, —C(Ra)?C(Ra)—, OC(Ra)(Rb)— or SC(Ra)(Rb)—. These compounds and their pharmaceutical acceptable salts are used in pharmaceutical compositions as prostaglandine D2 receptor antagonists useful in the treatment of CRTH2-mediated diseases such as respiratory, inflammatory or allergic conditions among others.Type: ApplicationFiled: August 7, 2006Publication date: November 19, 2009Inventor: Zhaoyin Wang
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Publication number: 20090281322Abstract: Disclosed herein are compounds represented by the structural formula: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: May 1, 2009Publication date: November 12, 2009Applicant: ALLERGAN, INC.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Richard L. Beard, John E. Donello
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Patent number: 7608714Abstract: The present invention provides an improved process for the preparation of Dolasetron salts, in particularly Dolasetron mesylate. Also provided are intermediates for the process and methods of preparing the intermediates.Type: GrantFiled: January 5, 2007Date of Patent: October 27, 2009Assignee: TEVA Gyógyszergyár Zártkörúen Müködö RészvénytársaságInventors: Janos Hajko, Tivadar Tamas, Adrienne Kovacsne-Mezei, Erika Magyar Molnarne, Csaba Peto, Csaba Szabo
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Publication number: 20090218039Abstract: An dye compound of the following formula (1): wherein D represents a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group; L represents ?CR2—, ?N—, or ?N—NH—; R1 represents a monovalent substituent; R2 represents a hydrogen atom or a cyano group; n indicates an integer of from 0 to 4; when n is 2 or more, then plural R1's may be the same or different.Type: ApplicationFiled: February 27, 2009Publication date: September 3, 2009Applicant: FUJIFILM CorporationInventors: Yoshihiko FUJIE, Tetsuya WATANABE, Hisashi MIKOSHIBA
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Publication number: 20090211038Abstract: The present disclosure relates to a novel dye composition for the dyeing and/or lightening of keratin materials, such dye comprising a hemicyanin styryl chromophore thiol or disulfide dye of formula (I) or (II): the organic or mineral acid salts thereof, optical isomers and geometric isomers thereof, and the solvates thereof such as hydrates. The present disclosure further relates to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, including human keratin fibers such as the hair, using said composition. This composition makes it possible to obtain a coloring with a lightening effect which is particularly resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: August 27, 2009Inventors: Andrew GREAVES, Nicolas DAUBRESSE
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Publication number: 20090192147Abstract: The invention relates to [a]-fused indole compounds of the Formula II, or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein. The invention also relates to compositions comprising the compounds of Formula II, and methods for making and using the compounds.Type: ApplicationFiled: January 30, 2009Publication date: July 30, 2009Applicant: WyethInventors: Semiramis Ayral-Kaloustian, Nan Zhang, Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Thai Hiep Nguyen, James Thomas Anderson
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Publication number: 20090142618Abstract: The invention provides an OLED device containing certain alkali metal cluster compounds with mixed ligands, such compounds, and methods of making them. In particular, the cluster compound is a neutrally charged mixed cluster compound comprising first and second subunits with the first subunit comprising an alkali metal salt of a nitrogen containing a heterocyclic ligand bearing a anionic hydroxy group and the second subunit consisting of an organic alkali metal salt different than the first subunit.Type: ApplicationFiled: November 29, 2007Publication date: June 4, 2009Inventors: William J. Begley, Manju Rajeswaran, Tukaram K. Hatwar, Natasha Andrievsky
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Publication number: 20090126125Abstract: The present disclosure relates to the dyeing of keratin materials using thiol/disulfide styryl tetrahydroquinolinium fluorescent dyes. Disclosed herein is a dye composition comprising a thiol/disulfide styryl tetrahydroquinolinium fluorescent dye and a dyeing process with, for instance, a lightening effect on keratin materials such as hair, using said composition. Disclosed herein are thiol fluorescent dyes and the uses thereof in lightening keratin materials. This composition can be used to obtain a lightening effect which can be resistant and visible on dark keratin fibers.Type: ApplicationFiled: September 19, 2008Publication date: May 21, 2009Inventors: Andrew GREAVES, Nicolas DAUBRESSE, Franco MANFRE