Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/153)
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Patent number: 8440694Abstract: The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X?, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.Type: GrantFiled: September 13, 2012Date of Patent: May 14, 2013Assignee: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Wilfried Braje, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer, Andrea Hager-Wernet
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Publication number: 20130116249Abstract: The invention relates to compounds corresponding to formula (I): in which R3 and R4 together form, with the carbon atoms of the phenyl nucleus to which they are attached, a 6-membered nitrogenous heterocycle corresponding to one of formula (A), (B) or (C) below: in which the wavy lines represent the phenyl nucleus to which R3 and R4 are attached. Preparation process and therapeutic use.Type: ApplicationFiled: July 4, 2011Publication date: May 9, 2013Applicant: SANOFIInventors: Chantal Alcouffe, Corentin Herbert, Gilbert Lassalle
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Publication number: 20130116216Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.Type: ApplicationFiled: November 12, 2010Publication date: May 9, 2013Inventors: Celia Dominguez, John Wityak, Michael Prime, Stephen Martin Courtney, Christopher Yarnold, Frederick Brookfield, Richard Marston, Douglas Macdonald
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Patent number: 8431706Abstract: The present invention provides a compound of the formula below or a pharmaceutical salt thereof, methods of treating diabetes using the compound and a process for preparing the compound.Type: GrantFiled: August 9, 2012Date of Patent: April 30, 2013Assignee: Eli Lilly and CompanyInventor: Chafiq Hamdouchi
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Publication number: 20130102631Abstract: The present invention provides compounds of formula (I) wherein R1, A1, X, Y6, Y7, Y8, G1, G2, G3 and p are as defined in the claims. The invention further provides intermediates used in the preparation of these compounds, to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: June 29, 2011Publication date: April 25, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Kurt Nebel, Daniel Stierli, Werner Zambach, Andrea Bortolato
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Patent number: 8426585Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: August 17, 2012Date of Patent: April 23, 2013Assignees: Sunshine Lake Pharma Co., Ltd.Inventor: Ning Xi
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Patent number: 8426586Abstract: An improved process for preparing 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline and related aminocrotonyl compounds and the preparation of a suitable salt of 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline for use as a pharmaceutically active substance.Type: GrantFiled: July 14, 2006Date of Patent: April 23, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Rainer Soyka, Werner Rall, Juergen Schnaubelt, Peter Sieger, Christian Kulinna
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Patent number: 8410109Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: GrantFiled: July 28, 2006Date of Patent: April 2, 2013Assignee: Resverlogix Corp.Inventors: Norman C. W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
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Publication number: 20130065922Abstract: Compounds of the general formula (I), wherein the substituents are as defined in claim 1, are useful as fungicides.Type: ApplicationFiled: May 4, 2011Publication date: March 14, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Stephan Trah, Laura Quaranta, Renaud Beaudegnies, Fiona Murphy Kessabi, Guillaume Berthon, Clemens Lamberth
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Patent number: 8394959Abstract: The present invention relates to maleate salt forms of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, methods of preparing crystalline maleate salt forms, the associated compounds, and pharmaceutical compositions containing the same. The maleate salts are useful in treating cancers, particularly those affected by kinases of the epidermal growth factor receptor family.Type: GrantFiled: April 6, 2012Date of Patent: March 12, 2013Assignee: Wyeth LLCInventors: Qinghong Lu, Mannching Sherry Ku, Warren Chew, Gloria Cheal, Anthony F. Hadfield, Mahmoud Mirmehrabi
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Patent number: 8389728Abstract: This disclosure relates, inter alia, to stimulants of pollen tube germination and growth of pollen tubes, and methods of their use to stimulate in vitro and in vivo pollen germination and pollen tube growth.Type: GrantFiled: March 26, 2010Date of Patent: March 5, 2013Assignee: The Arizona Board of RegentsInventors: Yuan Qin, Ravishankar Palanivelu, Ronald J. Wysocki, Jr., Arpad Somogyi, Yelena Feinstein
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Publication number: 20130045989Abstract: An objective of the present invention is to provide a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate having stable physicochemical properties. The objective is attained by a crystal of 2-ethyl-3,7-dimethyl-6-(4-(trifluoromethoxy)phenoxy)quinoline-4-yl methyl carbonate that exhibits a diffraction peak pattern shown in FIG. 1 as determined by powder X-ray diffractometry.Type: ApplicationFiled: February 22, 2011Publication date: February 21, 2013Inventors: Kouki Tanigakiuchi, Mikio Sekiguchi, Hiroki Hotta, Shizuo Shimano, Akinori Morikawa, Kazumi Yamamoto, Nozomu Nakanishi, Nobuto Minowa, Takashi Watanabe
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Patent number: 8362035Abstract: This invention relates to novel crystalline forms of the following Compound (1), and the sodium salt thereof, and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of Hepatitis C Viral (HCV) infection:Type: GrantFiled: July 3, 2012Date of Patent: January 29, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Thilo Berkenbusch, Carl Alan Busacca, Burkhard Jaeger, Richard J. Varsolona
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Patent number: 8357700Abstract: The present invention is directed to 2,3-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors 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 orexin receptors are involved.Type: GrantFiled: October 15, 2009Date of Patent: January 22, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Broc Flores, John D. Schreier
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Publication number: 20130018043Abstract: The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.Type: ApplicationFiled: July 11, 2012Publication date: January 17, 2013Inventors: Joseph A. Bilotta, Adrian Wai-Hing Cheung, Fariborz Firooznia, Kevin Richard Guertin, Stuart Hayden, Nancy-Ellen Haynes, Christine M. Lukacs-Lesburg, Nicholas Marcopulos, Eric Mertz, Lida Qi, Yimin Qian, Sung-Sau So, Jenny Tan, Kshitij C. Thakkar
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Patent number: 8354413Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP-ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.Type: GrantFiled: August 21, 2008Date of Patent: January 15, 2013Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti, S.R.L.Inventors: Philip Jones, Olaf Kinzel, Uwe Koch, Jesus Maria Ontoria Ontoria, Giovanna Pescatore, Rita Scarpelli, Caterina Torrisi
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Patent number: 8349829Abstract: The invention relates to antibacterial compounds of formula I wherein R1 represents alkoxy or halogen; U, V and W each represent CH, or one of U, V and W represents N and the others each represent CH; A represents CH2 or O; G is CH?CH-E wherein E represents a phenyl group mono- or di-substituted with halogen, or G is a group of one of the formulae hereafter wherein Z represent CH or N, Q represents O or S and K represents O or S; and salts of such compounds.Type: GrantFiled: June 2, 2009Date of Patent: January 8, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Patent number: 8349867Abstract: A kind of quinoline compounds as formula A, pharmaceutical accepted solvates, optical isomers or polymorphisms thereof. The intermediates of formula D. in which, R1, R2 and R3 is independently H, halo or the subustitents of formula H, in which, R is H, halo, C1˜C4alkyl, C1˜C4alkoxyl. The preparation methods and the uses for the manufacture of a medicament of inhibiting the HMG CoA reductase and treating the diseases relating to the high blood fat. Compared with the fluvastatin, rosuvatatin, pitavastatin disclosed in the prior arts, present quinoline compounds have better activity of inhibiting HMG CoA reductase. Present quinoline compounds can be used for treating the diseases relating to the high blood fat.Type: GrantFiled: December 6, 2007Date of Patent: January 8, 2013Assignee: Shanghai Institute of Pharmaceutical IndustryInventors: Zhengyan Cai, Weicheng Zhou, Qun Hao
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Patent number: 8349868Abstract: Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: GrantFiled: May 17, 2011Date of Patent: January 8, 2013Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Roland Burli, Marian C. Bryan, Guo-Qiang Cao, Susana C. Neira, Anthony B. Reed
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Publication number: 20130005709Abstract: The present invention relates to novel sulfone compounds as 5-HT6 receptor ligands of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment/prevention of various disorders that are related to 5-HT6 receptor functions.Type: ApplicationFiled: March 24, 2010Publication date: January 3, 2013Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Rama Sastri Kambhampati, Rajesh Kumar Badange, Veena Reballi, Anil Kashinath Chindhe, Rambabu Namala, Mohamad Sadik Abdulhamid Mulla, Ishtiyaque Ahmad, Renny Abraham, Venkateswarlu Jasti
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Publication number: 20130005760Abstract: A heterocyclic compound of formula (I) or a salt thereof: wherein R1 is an optionally protected amino group or an optionally substituted C1-6 alkyl group; R2 and R3 are each independently a C1-2 alkyl group; X is a hydrogen atom or a halogen atom; Z1 is N or C—R4; Z2 is N or C—R5; Z3 is N or C—R6; Z4 is N or C—R7; R4, R5, R6, and R7 are each independently a hydrogen atom, a halogen atom, an optionally protected amino group, or a C1-6 alkylsulfonyl group; Z is CH or N; and A is a methylene group or a bond, which has an excellent anti-HIV activity and is useful as an anti-HIV agent.Type: ApplicationFiled: January 20, 2011Publication date: January 3, 2013Applicant: Toyama Chemical Co., Ltd.Inventors: Yuji Oonishi, Kenichiro Awasaguchi, Nobuhiko Nomura, Keisuke Tohdo, Hyouei Kawai, Tomomi Wakatsuki
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Publication number: 20130005759Abstract: MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.Type: ApplicationFiled: January 21, 2011Publication date: January 3, 2013Inventors: Alexander Deiters, Douglas D. Young
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Publication number: 20130005767Abstract: Disclosed herein are compounds of the formula or salts or bioisosteres thereof. Therapeutic methods, medicaments, and compositions related thereto are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: Allergan, Inc.Inventors: David W. Old, Vinh X. Ngo
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Publication number: 20130005675Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.Type: ApplicationFiled: September 14, 2012Publication date: January 3, 2013Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Takahito YAMAUCHI, Yuji OCHI
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Publication number: 20120315247Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: August 17, 2012Publication date: December 13, 2012Applicants: SUNSHINE LAKE PHARMA CO., LTD.Inventor: Ning Xi
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Publication number: 20120316168Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.Type: ApplicationFiled: August 21, 2012Publication date: December 13, 2012Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Kenji OTSUBO, Yuji OCHI, Masami NAKAI, Atsushi MORI
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Patent number: 8329619Abstract: 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: October 29, 2010Date of Patent: December 11, 2012Assignee: 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: 20120309786Abstract: Compounds represented by the general formula (I): pharmaceutically acceptable salts or solvates thereof, a process for their manufacture; pharmaceutical compositions containing them; and use of the compounds in the treatment of metabolic disorders related to insulin resistance or hyperglycemia are described.Type: ApplicationFiled: August 13, 2012Publication date: December 6, 2012Inventors: Nabajyoti DEKA, Kamlesh Jyotindra Padiya, Swapnil Ramesh Bajare, Rhushikesh Arun Kulkarni, Taj Usman Khan, Sivaramakrishnan Hariharan, Rosalind Adaikalasamy Marita
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Patent number: 8324245Abstract: An objective of the present invention is to provide compounds having potent antitumor activity. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein X?CH or N; Z?O or S; L=O or S; M=CR10R11, wherein R10 and R11?H, alkyl, or alkoxy, NR12 wherein R12?H or alkyl; R1, R2, and R3?H or optionally substituted alkoxy; R4?H; R5-8?H, halogen, alkoxy or the like; and R9=alkyl optionally substituted by —R14, -T-R15, or —NR16R17 wherein T=O, S, or NH; R14=an optionally substituted carbocyclic or heterocyclic ring; and R15-17=alkyl or an optionally substituted carbocyclic or heterocyclic ring, or —NR18R19 wherein R18 and R19?H, optionally substituted alkyl, or an optionally substituted carbocylic or heterocyclic ring, or optionally substituted carbocyclic or heterocyclic ring.Type: GrantFiled: January 10, 2011Date of Patent: December 4, 2012Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Yasunari Fujiwara, Terufumi Senga, Tsuyoshi Nishitoba, Tatsushi Osawa, Atsushi Miwa, Kazuhide Nakamura
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Patent number: 8318769Abstract: Substituted sulfonamide compounds corresponding to formula I: processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor.Type: GrantFiled: April 8, 2009Date of Patent: November 27, 2012Assignee: Gruenethal GmbHInventors: Stefan Oberboersch, Melanie Reich, Stefan Schunk, Michael Franz-Martin Engels, Ruth Jostock, Tieno Germann, Jean De Vry, Klaus Schiene, Sabine Hees
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Patent number: 8314087Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: February 15, 2008Date of Patent: November 20, 2012Assignee: Amgen Inc.Inventors: Brian K. Albrecht, Steven Bellon, Shon Booker, Alan C. Cheng, Derin D'Amico, Noel D'Angelo, Jean-Christophe Harmange, Tae-Seong Kim, Longbin Liu, Mark H. Norman, Aaron C. Siegmund, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20120289702Abstract: Provided is an agricultural fungicide that contains at least one selected from the group consisting of a novel nitrogen-containing heterocyclic compound represented by Formula (I), a salt thereof, or an N-oxide compound thereof. In Formula (I), R represents a group represented by CR1R2R3 or a cyano group. R1 to R3 each independently represents a hydrogen atom, an unsubstituted or substituted C1-8 alkyl group, an unsubstituted or substituted hydroxyl group, or the like. R4 or R5 represents a halogeno group or the like. Y or Z represents a carbon atom or the like, and A or D represents a benzene ring or the like. X represents an oxygen atom or a nitrogen atom or the like.Type: ApplicationFiled: December 28, 2010Publication date: November 15, 2012Applicant: Nippon Soda Co., Ltd.Inventors: Kotaro Shibayama, Jun Inagaki, Yuto Saiki, Akira Mitani, Raito Kuwahara, Motoaki Sato, Satoshi Nishimura, Mami Kuboki
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Publication number: 20120283216Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is O or S; Z1 and Z2 are each independently CR9 or N; and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 22, 2010Publication date: November 8, 2012Inventors: Alvin Donald Crews, JR., Amy X. Ding, Chi-Ping Tseng
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Publication number: 20120283260Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: ApplicationFiled: July 24, 2012Publication date: November 8, 2012Applicants: ASTELLAS PHARMA INC., ALCON RESEARCH, LTD.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120277185Abstract: To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.Type: ApplicationFiled: July 10, 2010Publication date: November 1, 2012Applicant: BAYER CROPSCIENDE AGInventors: Jun Mihara, Koichi Araki, Takuma Mori, Tetsuya Murata, Yasushi Yoneta, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya, Ulrich Görgens
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Publication number: 20120277150Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: April 11, 2012Publication date: November 1, 2012Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Munetaka OHKOUCHI
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Publication number: 20120277231Abstract: The present invention relates to quinolinyloxyphenylsulfonamides and stereoisomeric forms, solvates, hydrates and/or pharmaceutically acceptable salts of these quinolinyloxyphenylsulfonamide compounds as well as pharmaceutical compositions containing at least one of these compounds together with at least one pharmaceutically acceptable carrier, excipient and/or diluent. Said quinolinyloxyphenylsulfonamides are useful for prophylaxsis, treatment and/or after-treatment of hyperproliferative disorders, such as cancer, tumors and particularly cancer metastases.Type: ApplicationFiled: October 16, 2010Publication date: November 1, 2012Inventors: Axel Ullrich, Robert Torku, Yixiang Zhang, György Kéri, László Örfi, István Szabadkai
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Patent number: 8299094Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: GrantFiled: December 13, 2010Date of Patent: October 30, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Patent number: 8299254Abstract: A process for making 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid, and therapeutically acceptable salts thereof, and intermediates used in the process are disclosed.Type: GrantFiled: August 18, 2009Date of Patent: October 30, 2012Assignee: Abbott LaboratoriesInventors: Anthony Haight, David M. Barnes, Geoff G. Z. Zhang
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Patent number: 8293913Abstract: The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X?, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.Type: GrantFiled: August 6, 2008Date of Patent: October 23, 2012Assignee: Abbott GmbH & Co. KGInventors: Sean Colm Turner, Wilfried Braje, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Wolfgang Wernet, Andrea Hager-Wernet, legal representative, Matthias Mayrer
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Patent number: 8293732Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: GrantFiled: December 4, 2007Date of Patent: October 23, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Ismet Dorange, Magali Madeleine Simone Motte, Koenraad Jozef Lodewijk Marcel Andries, Anil Koul
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Patent number: 8293897Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter—and/or intra—cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: GrantFiled: October 9, 2009Date of Patent: October 23, 2012Assignees: Sunshine Lake Pharma Co., Ltd.Inventor: Ning Xi
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Patent number: 8288410Abstract: The present invention relates to quinolinium antiinfective agents in which the qunolinium nucleus is fused to an indole ring or the qunolinium nucleus is linked to a cyclic structure through an opened indole or a benzothiophene or benzofuran ring. The compound is further substituted with various substituent groups. The compounds are represented by formula (I), (II) and (III): Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: July 8, 2008Date of Patent: October 16, 2012Assignee: Florida Agricultural and Mechanical UniversityInventor: Seth Y. Ablordeppey
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Publication number: 20120259094Abstract: The present invention relates generally to affinity ligands and chemical affinity ligand-matrix conjugates for use as chromatographic adsorbents and methods which utilise the adsorbents in the purification of proteins by affinity chromatography. The affinity ligand-matrix conjugates of the present invention comprise ligands of general formula (I): wherein m represents an integer from 0-2, n represents an integer from 0-6, p represents an integer from 0-4, R1 represents H or C1-3 alkyl, R2 is an optional substituent, and X is the position at which the ligand is immobilized, optionally via a linker.Type: ApplicationFiled: October 15, 2010Publication date: October 11, 2012Inventors: Milton TW Hearn, Anjali Makarand Bhagwat, William Roy Jackson, Simon John Mountford
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Publication number: 20120237874Abstract: According to one embodiment, an actinic-ray- or radiation-sensitive resin composition includes any of the compounds (A) of general formula (I) below that when exposed to actinic rays or radiation, generates an acid and a resin (B) whose rate of dissolution into an alkali developer is increased by the action of an acid. (The characters used in general formula (I) have the meanings mentioned in the description.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Applicant: FUJIFILM CORPORATIONInventors: Shuhei Yamaguchi, Akinori Shibuya
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Patent number: 8269011Abstract: The present invention provides a quinolone compound represented by General Formula (1) or a salt thereof, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; R3 represents a phenyl group optionally being substituted with one or more substituents, etc.; R4 represents a halogen atom; R5 represents a hydrogen atom or halogen atom; R6 represents a hydrogen atom; and R7 represents a hydroxyl group, etc. The quinolone compound have a functional improvement effect, which suppresses progression of neurological dysfunction by inhibiting the chronic progression of Parkinson's disease or protecting dopamine neurons from the disease etiology, thereby prolonging the period before first administration begins.Type: GrantFiled: June 6, 2008Date of Patent: September 18, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Kenji Otsubo, Yuji Ochi, Masami Nakai, Atsushi Mori
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Patent number: 8258293Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y—X is C(O)—O, S(O)2-O, NHC(O)—O, NHC(S)—O, OC(O)—O, bond-O, C(O)—NH, S(O)2-NH, NHC(O)—NH, NHC(S)—NH, OC(O)—NH, bond-NH, NH—C(O), O—C(O), NH—S(O)2, or O—S(O)2 or Y—X is a bond; R6 is H, trifluoromethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8,R9-aminocarbonyl(1-4C)alkyl, R8,R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro, hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4CType: GrantFiled: October 7, 2011Date of Patent: September 4, 2012Assignee: MSD OSS B.V.Inventors: Nicole Corine Renee Van Straten, Rudolf Gijsbertus Van Someren, Jurgen Schulz
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Publication number: 20120219522Abstract: The present invention provides novel substituted quinoline compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: February 21, 2012Publication date: August 30, 2012Inventor: Ning XI
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Publication number: 20120220775Abstract: A process for preparing 8-substituted oxy-5-((R)-2-halo-1-hydroxy-ethyl)-(1H)-quinolin-2-ones or acceptable solvates thereof. The process involves reacting a 5-(?-haloacetyl)-8-substituted oxy-(1H)-quinolin-2-one with a reducing agent in the presence of a chiral agent and a base to form a 8-(substituted oxy)-5-((R)-2-halo-1-hydroxy-ethyl)-(1H)-quinolin-2-one, said chiral agent having a formula I or II wherein M, L, X, R1, R2 and R3 have the meanings as indicated in the specification.Type: ApplicationFiled: May 1, 2012Publication date: August 30, 2012Inventors: Olivier Lohse, Caspar Vogel, Gerhard Penn
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Patent number: 8252932Abstract: Chemically reactive carbocyanine dyes incorporating an indolium ring moiety that is substituted at the 3-position by a reactive group or by a conjugated substance, and their uses, are described. Conjugation through this position results in spectral properties that are uniformly superior to those of conjugates of spectrally similar dyes wherein attachment is at a different position. The invention includes derivative compounds having one or more benzo nitrogens.Type: GrantFiled: October 18, 2010Date of Patent: August 28, 2012Assignee: Life Technologies CorporationInventors: Wai-Yee Leung, Ching-Ying Cheung, Stephen Yue