Quinoxalines (including Hydrogenated) Patents (Class 544/353)
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Publication number: 20140239269Abstract: A pyrene-based compound, and an organic light-emitting diode including the pyrene-based compound are provided.Type: ApplicationFiled: August 5, 2013Publication date: August 28, 2014Inventors: Eun-Jae Jeong, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Jun-Ha Park, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Soo-Yon Kim, Jong-Hyuk Lee
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Patent number: 8815412Abstract: An object is to provide a novel quinoxaline derivative, a light-emitting element with low driving voltage, and a light-emitting element which consumes low power. Another object is to provide a light-emitting device and an electronic appliance which consume low power by using the above light-emitting element. A quinoxaline derivative represented by a general formula (G11) is provided, in which at least one of carbon at a 2-position and carbon at a 3-position of quinoxaline, and carbon at a 2-position of a 1H-benzimidazole ring are bonded to each other via an arylene group.Type: GrantFiled: December 17, 2008Date of Patent: August 26, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Hiroshi Kadoma, Sachiko Kawakami, Satoko Shitagaki, Satoshi Seo
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Patent number: 8809333Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: GrantFiled: March 27, 2012Date of Patent: August 19, 2014Assignee: Pfizer Inc.Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20140228566Abstract: To provide a new bipolar organic compound. In particular, to provide a bipolar organic compound having excellent heat resistance and to provide a bipolar organic compound which is electrochemically stable. Further, to provide a light emitting element and a light emitting device of which a driving voltage and power consumption are reduced by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have excellent heat resistance by using a new bipolar organic compound. Further, to provide a light emitting element and a light emitting device which have a long life by using a new bipolar organic compound.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Semiconductor Energy Laboratory Co., Ltd.Inventors: Masakazu Egawa, Satoshi Seo, Nobuharu Ohsawa
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Patent number: 8802675Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.Type: GrantFiled: January 31, 2010Date of Patent: August 12, 2014Assignees: Technion Research and Development Foundation Ltd, Yeda Research and Development Company Ltd.Inventors: Moussa B. H. Youdim, Mati Fridkin, Hailin Zheng
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Publication number: 20140221345Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: August 7, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
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Publication number: 20140213580Abstract: Provided are compounds with the following structure, formula (I) pharmaceutically acceptable salts thereof, use of those compounds for treating cancer and pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: June 18, 2012Publication date: July 31, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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Publication number: 20140209872Abstract: A compound having an electron injection capability and/or electron transport capability represented by Formula 1, an organic light emitting device including the compound; and a flat display device including the organic light emitting device. The descriptions of substituents are referred to in the detailed description.Type: ApplicationFiled: July 26, 2013Publication date: July 31, 2014Inventors: Jun-Ha Park, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
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Patent number: 8785639Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: December 1, 2010Date of Patent: July 22, 2014Assignee: AbbVie Inc.Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
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Patent number: 8785643Abstract: The present invention is directed to novel substituted bicyclic aromatic compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: GrantFiled: December 16, 2011Date of Patent: July 22, 2014Assignee: N30 Pharmaceuticals, Inc.Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20140179921Abstract: A compound of formula I wherein Y is a single bond, C?O, C?S or S(O)m where m is 0, 1 or 2; the ring is a 6-membered aromatic or is a 5 or 6 membered heteroaromatic ring; Z and Z? are joined by a single or a double bond and are ?C— or —N— provided that both are not N; Ra, R1, R2, R3, R3a, R4 and R8 are specified organic groups; n is 2, 3 or 4 and p is 0-4; or salts or N-oxides thereof.Type: ApplicationFiled: January 6, 2014Publication date: June 26, 2014Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jerome Cassayre, Peter Maienfisch, Fredrik Cederbaum, Louis-Pierre Molleyres
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Patent number: 8758905Abstract: A quinoxaline derivative represented by a formula (1) is provided. In the formula (1), R9 and R10 and R11 and R12 are bonded to each other to form an aromatic ring, and Ar1 to Ar4 each independently represents an aryl group or a heterocyclic group.Type: GrantFiled: July 25, 2012Date of Patent: June 24, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Satoko Shitagaki, Atsushi Tokuda, Hiroko Abe, Ryoji Nomura, Satoshi Seo
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Publication number: 20140171639Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: February 24, 2014Publication date: June 19, 2014Applicant: AMGEN INC.Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
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Patent number: 8748431Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: GrantFiled: November 25, 2011Date of Patent: June 10, 2014Assignee: Syngenta Participations AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
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Publication number: 20140148461Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: November 22, 2013Publication date: May 29, 2014Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
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Publication number: 20140142307Abstract: Singly and multiply charged imidazolium cations (ICs) have been identified as a class of chemical compositions that possess potent antineoplastic, antibacterial and antimicrobial properties. The imidazolium cations disclosed demonstrate greater or equivalent potency towards cancerous cells as the current clinical standard, cisplatin. These imidazolium cations, however, achieve this efficacy without any of the known toxic side effects caused by heavy metal-based antineoplastic drugs such as cisplati.Type: ApplicationFiled: April 30, 2012Publication date: May 22, 2014Inventors: Wiley Youngs, Matthew Panzner, Claire Tessier, Michael Deblock, Brian Wright, Patrick Wagers, Nikki Robishaw
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Publication number: 20140128392Abstract: Disclosed herein are new heterocyclic compounds of Formula IIa: and compositions thereof, and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: March 19, 2010Publication date: May 8, 2014Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
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Patent number: 8716289Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or oType: GrantFiled: November 13, 2009Date of Patent: May 6, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
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Patent number: 8716473Abstract: The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O?); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.Type: GrantFiled: May 26, 2010Date of Patent: May 6, 2014Assignee: Sentinel Oncology LimitedInventors: Robert George Boyle, David Winter Walker
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Publication number: 20140100213Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.Type: ApplicationFiled: November 4, 2013Publication date: April 10, 2014Applicant: GlaxoSmithKline LLCInventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20140088080Abstract: [Problem] An excellent drug for treating or preventing cardiovascular diseases, based on cGMP production enhancing action due to soluble guanylate cyclase activating action, is provided. [Means for Solution] It was found that imidazopyridine compounds having a carbamoyl group at the 3-position and a substituent bonded at the 8-position via an oxygen atom in an imidazo[1,2-a]pyridine skeleton exhibits a cGMP production enhancing action by a potent soluble guanylate cyclase activating action, and is useful as a drug for treating or preventing various soluble guanylate cyclase-related cardiovascular diseases, thereby completing the present invention.Type: ApplicationFiled: November 26, 2013Publication date: March 27, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Yuji KOGA, Kyoichi MAENO, Ippei SATO, Yoshimasa IMAMURA, Takeshi HANAZAWA, Maiko IIDA, Kazuhiko OHNE, Kenichiro IMAMURA, Tsubasa WATANABE, Eisuke NOZAWA, Hiroshi SHIBATA
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Publication number: 20140088029Abstract: Provided is a novel therapeutic means for Alzheimer's disease. In particular, provided is a compound represented by the following general formula (I): [wherein Ar1 represents 2-methoxy-4-(2-pyridylmethoxy)phenyl etc. and Ar2 represents a 1H-indol-6-yl group etc.] or a salt thereof.Type: ApplicationFiled: April 11, 2012Publication date: March 27, 2014Applicant: PHARMA EIGHT CO., LTD.Inventors: Hachiro Sugimoto, Michiaki Okuda, Takashi Takahashi, Ichiro Hijikuro, Hidetaka Suzuki, Shinichi Nakayama
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Publication number: 20140088306Abstract: Provided is a compound effective as a diagnostic imaging probe targeting amyloid and an agent for Alzheimer's disease diagnosis including the compound.Type: ApplicationFiled: August 26, 2013Publication date: March 27, 2014Applicants: Nihon Medi-Physics Co., Ltd., KYOTO UNIVERSITYInventors: Hideo Saji, Masahiro Ono, Masafumi Ihara, Ikuya Seki
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Publication number: 20140088079Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.Type: ApplicationFiled: June 1, 2012Publication date: March 27, 2014Applicant: GREEN CROSS CORPORATIONInventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
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Publication number: 20140081019Abstract: The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.Type: ApplicationFiled: May 21, 2012Publication date: March 20, 2014Applicant: SANOFIInventors: Jens Atzrodt, Volker Derdau, Wolfgang Holla, Matthias Beller, Lorenz Neubert, Dirk Michalik
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Patent number: 8674099Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.Type: GrantFiled: August 16, 2012Date of Patent: March 18, 2014Assignee: Novartis AGInventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
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Patent number: 8658569Abstract: Substituted quinolinones of the formula I in which the variables are defined according to the description, their agriculturally suitable salts, processes and intermediates for preparing the compounds of the formula I, compositions comprising them and their use as herbicides, i.e. for controlling harmful plants, and also a method for controlling unwanted vegetation which comprises allowing a herbicidally effective amount of at least one compound of the formula I to act on plants, their seed and/or their habitat.Type: GrantFiled: August 22, 2012Date of Patent: February 25, 2014Assignee: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska, Anja Simon, Richard Roger Evans
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Publication number: 20140051694Abstract: Oxazole derivatives are described. The inventive compounds are useful as kinase inhibitors, and may be used in the treatment of cancer, such as prostate cancer, lung cancer, breast cancer, colon cancer, leukemia, CNS cancer, melanoma, ovarian cancer, and renal cancer.Type: ApplicationFiled: September 24, 2013Publication date: February 20, 2014Applicant: NEOSOME LIFE SCIENCES, LLCInventors: Laxman S. Desai, Srinivas Chittaboina
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Publication number: 20140038965Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comparing cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 17, 2013Publication date: February 6, 2014Applicant: EnVivo Pharmaceuticals, Inc.Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
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Publication number: 20140038975Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors and, more specifically, their use to treat bacterial infections.Type: ApplicationFiled: March 27, 2012Publication date: February 6, 2014Inventors: Matthew Frank Brown, Jinshan Michael Chen, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20140031368Abstract: This disclosure is related to compounds having the structure wherein Ar1, Ar2, R1-R6, Z, m, n, o, and p are defined herein. This disclosure also relates to pharmaceutical compositions comprising the above compounds and methods for their use.Type: ApplicationFiled: July 8, 2013Publication date: January 30, 2014Applicants: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCHInventors: Ronald Breslow, Paul A. Marks, K. G. Abhilash, Jianing Wang
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Patent number: 8637515Abstract: A polymorph of brimonidine pamoate having the formula exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.Type: GrantFiled: March 14, 2013Date of Patent: January 28, 2014Assignee: Bausch & Lomb IncorporatedInventors: Hongna Wang, Stephen R. Davio, Gregory L. McIntire, Michael Hall, Shazad Suchit, Jon Summersett, Brent Whitehead
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Patent number: 8637513Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: GrantFiled: October 23, 2008Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
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Patent number: 8637514Abstract: A polymorph of brimonidine pamoate having the formula exhibits characteristics disclosed herein. The polymorph is included in a composition, device, or implant for use in the treatment or control of elevated intraocular pressure or in the neuroprotection of components of a neurological tissue to prevent progressive degeneration of such components. In particular, such a composition, device, or implant can be used to provide neuroprotection to cells and components of the optic nerve system.Type: GrantFiled: March 14, 2013Date of Patent: January 28, 2014Assignee: Bausch & Lomb IncorporatedInventors: Hongna Wang, Stephen R. Davio, Gregory L. McIntire, Michael Hall, Shazad Suchit, Jon Summersett, Brent Whitehead
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Patent number: 8623523Abstract: A quinoxaline derivative expressed by the general formula (1) is provided. (Each of R1 to R12 represents one of a hydrogen atom, a halogen atom, an alkyl group, an alkoxyl group, an acyl group, a dialkyl amino group, a diarylamino group, a substituted or unsubstituted vinyl group, a substituted or unsubstituted aryl group, and a substituted or unsubstituted heterocycle group. Ar1 represents one of a substituted or unsubstituted biphenyl group and a substituted or unsubstituted terphenyl group, and Ar2 represents one of a substituted or unsubstituted phenyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted terphenyl group, and a substituted or unsubstituted monocyclic heterocycle group.Type: GrantFiled: May 3, 2012Date of Patent: January 7, 2014Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Masakazu Egawa, Sachiko Kawakami, Nobuharu Ohsawa, Hideko Inoue, Satoshi Seo, Ryoji Nomura
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Publication number: 20140005382Abstract: There are provided compounds represented by the following general formula (I) or pharmaceutically acceptable salts of thereof, which have a superior monoacylglycerol acyltransferase 2 inhibitory action: wherein Ring A represents a partially saturated heteroaryl group, an aryl group or a heteroaryl group, RB represents a C4-18 alkyl group, a C3-8 cycloalkyl group, a partially saturated aryl group, an aryl group, or the following formula (II): wherein V represents the formula —CR11R12—, —CO—, —CO—O—, or —CO—NH—, W represents a single bond or a C1-3 alkylene group, and Ring B represents a C3-8 cycloalkyl group, a C3-8 cycloalkenyl group, a partially saturated heteroaryl group, a saturated heterocyclyl group, an aryl group, or a heteroaryl group, Y represents a nitrogen atom or the formula N+(RF), RF represents a C1-4 alkyl group, and m and n, which may be the same or different, each represent an integer of 0 or 1.Type: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Tsuyoshi Busujima, Takahiro Oi, Hiroaki Tanaka, Yoshihisa Shirasaki, Kanako Iwakiri, Nagaaki Sato, Shigeru Tokita
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Publication number: 20130345222Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: May 17, 2013Publication date: December 26, 2013Inventors: Donald S. Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
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Patent number: 8609690Abstract: The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: GrantFiled: August 21, 2009Date of Patent: December 17, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Stefan Peters
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Patent number: 8604040Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG, and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: GrantFiled: May 26, 2011Date of Patent: December 10, 2013Assignee: Bayer CropScience AGInventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Nicola Rahn, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
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Publication number: 20130324519Abstract: The invention relates to compounds of formula (I) wherein the substituents are as defined in the specification, in free form or in the form of a pharmaceutically acceptable salt, solvate, ester, N-oxide thereof; processes for the preparation thereof; to pharmaceuticals containing such compounds, in particular for the use in one or more Protein tyrosine kinase mediated diseases.Type: ApplicationFiled: August 8, 2013Publication date: December 5, 2013Applicant: Novartis AGInventors: Pascal Furet, Diana Graus Porta, Vito Guagnano
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Publication number: 20130324544Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.Type: ApplicationFiled: November 25, 2011Publication date: December 5, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
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Publication number: 20130317213Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.Type: ApplicationFiled: August 1, 2013Publication date: November 28, 2013Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
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Publication number: 20130317223Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.Type: ApplicationFiled: November 6, 2012Publication date: November 28, 2013Applicant: The Board of Trustees of the University of IllinoisInventors: Martin D. Burke, David M. Knapp, Eric P. Gillis
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Publication number: 20130317218Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 24, 2012Publication date: November 28, 2013Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
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Patent number: 8592415Abstract: The present invention relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I: or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present invention further provides novel compounds and compositions as well as their methods of preparation and use of the same as JAK3 inhibitors in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.Type: GrantFiled: February 11, 2010Date of Patent: November 26, 2013Assignees: Reaction Biology Corp., Synerga LimitedInventors: Haiching Ma, Sorin Vasile Filip, Matthew Alexander Henry, James Alexander Dolan, Bartosz Dietrich
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Patent number: 8586739Abstract: Substituted bicyclic heteroaryls having the general structure: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: GrantFiled: May 10, 2012Date of Patent: November 19, 2013Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20130303517Abstract: The invention provides certain quinoxalines and aza-quinoxalines of the Formula (I), and their pharmaceutically acceptable salts, wherein J1, J2, R1, R2, R3, R22, Ra, Rb, Rc, Rd, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTH2 function.Type: ApplicationFiled: December 19, 2011Publication date: November 14, 2013Inventors: Christopher W. Boyce, Sylvia Joanna Degrado, Xiao Chen, Jun Qin, Robert D. Mazzola, JR., Younong Yu, Kevin D. McCormick, Anandan Palani, Dong Xiao, Robert George Aslanian, Jie Wu, Ashwin Umesh Rao, Phieng Siliphaivanh, Joey L. Methot, Hongjun Zhang, Elizabeth Helen Kelley, William Colby Brown, Qin Jiang, Jolicia Polivina Gauuan, Andrew J. Leyhane, Purakkattle Johny Biju, Pawan K. Dhondi, Li Dong, Salem Fevrier, Xianhai Huang, Henry M. Vaccaro
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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: 20130303370Abstract: The present invention provides a compound of formula (I) wherein R4 is of sub-formula (a) or (b) and wherein the other substituents are as defined in the specification. The compounds of formula (I) are potentially useful as herbicides.Type: ApplicationFiled: October 14, 2011Publication date: November 14, 2013Applicants: SYNGENTA LIMITED, SYNGENTA PARTICIPATIONS AGInventors: Alaric James Avery, Alain De Mesmaeker, Nicholas Phillip Mulholland, Nigel James Willetts, Paul Anthony Worthington
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Publication number: 20130303525Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.Type: ApplicationFiled: July 19, 2011Publication date: November 14, 2013Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach