1,2-thiazoles (including Hydrogenated) Patents (Class 546/271.1)
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Publication number: 20110218101Abstract: A compound of the formula I or where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as as pesticidal agents.Type: ApplicationFiled: October 27, 2009Publication date: September 8, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Ottmar Franz Hueter, Peter Renold, Werner Zambach, Thomas Pitterna, Peter Maienfisch
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Publication number: 20110190255Abstract: Disclosed are compounds of Formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: A is Q is a substituted 5-membered monocyclic heteroaryl group; W is CH2, O, or NH; and R1, R2, R3, R4, R5, R6, m, n, t, and x are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: August 5, 2010Publication date: August 4, 2011Inventors: John L. Gilmore, James E. Sheppeck
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Publication number: 20110166162Abstract: The present invention relates to sulfonamide compounds of formula (I) wherein R1 is H, halogen, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, C1-C6-alkylthio, C2-C6-alkenylthio, C2-C6-alkynylthio, C1-C6-haloalkyl or C1-C6-haloalkoxy; R2 and R3 are H, halogen, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C4-alkyl, C1-C6-alkoxy, C2-C6-alkenyloxy, C2-C6-alkynyloxy, C1-C6-alkylthio, C2-C6-alkenylthio, C2-C6-alkynylthio, C1-C6-haloalkyl or C1-C6-haloalkoxy; or R2 together with R3 form a fused 5 or 6-membered carbocycle or heterocycle; R4 is halogen, CN, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, C1-C6-haloalkyl, C1-C6-haloalkoxy, C1-C6-haloalkylthio, C1-C6-haloalkylsulfinyl or C1-C6-haloalksulfonyl; n is 0, 1, 2 or 3; R5 is phenyl or a 5- or 6-membered heterocycle; X is O or NRx, wherein Rx is H, C1-C6Type: ApplicationFiled: June 17, 2009Publication date: July 7, 2011Applicant: BASF SEInventors: Wolfgang von Deyn, Michael Puhl, Matthias Pohlman, Michael Rack, Liliana Parra Rapado, Jürgen Langewald, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Gale F. Matt Hews, Deborah L. Culbertson, Nancy B. Rankl, Hennicke Kamp, Bennard van Ravenzwaay
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Patent number: 7968572Abstract: It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.Type: GrantFiled: October 2, 2006Date of Patent: June 28, 2011Assignee: Ono Pharmaceuticals Co., Ltd.Inventors: Hisao Nakai, Shingo Yamamoto, Shingo Nakatani, Tomomi Hirosaki
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Publication number: 20110144068Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: July 23, 2009Publication date: June 16, 2011Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Chiara Marchionni, Michele Modugno
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Patent number: 7932274Abstract: The present invention provides 3-indazoyl-4-pyridylisothiazoles or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and methods of using the same, as well as processes for preparing the same, and intermediates thereof.Type: GrantFiled: March 18, 2009Date of Patent: April 26, 2011Assignee: Eli Lilly and CompanyInventors: Thomas Charles Britton, Veronique Dehlinger, Adam Michael Fivush, Sean Patrick Hollinshead, Benjamin Paul Vokits
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Patent number: 7872033Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: April 10, 2008Date of Patent: January 18, 2011Assignee: Abbott LaboratoriesInventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Patent number: 7871773Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: June 1, 2007Date of Patent: January 18, 2011Assignee: Life Technologies CorporationInventors: Richard Haugland, Stephen Yue
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Patent number: 7868014Abstract: The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.Type: GrantFiled: October 13, 2005Date of Patent: January 11, 2011Assignee: Eli Lilly and CompanyInventors: Thomas Charles Britton, Veronique Dehlinger, Colin Peter Dell, Bruce Anthony Dressman, Jason Kenneth Myers, Eric Samuel Nisenbaum
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Publication number: 20100311741Abstract: This invention pertains generally to the field of therapeutic compounds, and more particularly, to certain bicyclosulfonyl acid (BCSA) compounds which act as inhibitors of Tumour Necrosis Factor-? Converting Enzyme (TACE). The compounds are useful in the treatment of conditions mediated by TNF-?, such as rheumatoid arthritis; inflammation; psoriasis; septic shock; graft rejection; cachexia; anorexia; congestive heart failure; post ischaemic reperfusion injury; inflammatory disease of the central nervous system; inflammatory bowel disease; insulin resistance; HIV infection; cancer; chronic obstructive pulmonary disease (COPD); and asthma. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in the inhibition of TACE, and in the treatment of conditions that are ameliorated by the inhibition of TACE.Type: ApplicationFiled: May 16, 2008Publication date: December 9, 2010Applicant: INHIBOX LTD.Inventors: Aigars Jirgensons, Gundars Leitis, Ivars Kalvinsh, Daniel Robinson, Paul Finn, Nagma Khan
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Patent number: 7838523Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof is described herein. Pharmaceutical compositions comprising at least one chemical entity of the invention, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: GrantFiled: September 11, 2007Date of Patent: November 23, 2010Assignee: CGI Pharmaceuticals, Inc.Inventors: Peter A. Blomgren, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Jeffrey E. Kropf, Kevin S. Currie
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Publication number: 20100273830Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: ApplicationFiled: July 14, 2008Publication date: October 28, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
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Patent number: 7816354Abstract: The present invention is directed to compounds of Formula I: Wherein R1, R2, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: December 6, 2006Date of Patent: October 19, 2010Assignee: AstraZeneca ABInventors: Abdelmalik Slassi, Methvin Isaac, Ian Egle, Fupeng Ma, Babu Joseph, Joshua Clayton, Krzysztof Swierczek
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Publication number: 20100249179Abstract: The present invention provides novel isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.Type: ApplicationFiled: June 13, 2008Publication date: September 30, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: David Norman Deaton, Frank Navas, III, Paul Kenneth Spearing
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Publication number: 20100234345Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: November 4, 2009Publication date: September 16, 2010Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Patent number: 7781591Abstract: The present teachings provide compounds of formula I and their pharmaceutically acceptable salts, hydrates, and esters, wherein R1, R2, and X are as defined herein. The present teachings also provide methods of making the compounds of formula I, and methods of treating autoimmune and inflammatory diseases by administering a therapeutically effective amount of a compound or compounds of formula I to a mammal including a human.Type: GrantFiled: June 13, 2007Date of Patent: August 24, 2010Assignee: Wyeth LLCInventors: Derek Cecil Cole, Diane Harris Boschelli, Yanong Daniel Wang, Magda Asselin, Diane Marie Joseph-McCarthy, Amarnauth Shastrie Prashad, Allan Wissner, Russell Dushin, Biqi Wu, Lawrence Nathan Tumey, Chuan S. Niu, Joan Chen
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Patent number: 7737281Abstract: The present invention provides novel purine-based fluorescent dyes that may be used for staining, localizing and otherwise labeling target molecules, such as nucleic acids, for detection, amplification and quantification.Type: GrantFiled: July 7, 2005Date of Patent: June 15, 2010Assignee: Enzo Life Sciences, Inc. c/o Enzo Biochem, Inc.Inventor: Maciej Szczepanik
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Publication number: 20100111900Abstract: Compounds having the formula I wherein R1, R2, R3a, R3b, R3c, R4, R5 and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: October 30, 2009Publication date: May 6, 2010Inventors: Jim Li, Alfred Sui-Ting Lui, Kristen Lynn McCaleb, Francisco Xavier Talamas
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Publication number: 20100009848Abstract: The invention provides 3-amino-1,2-benzisothiazole compounds of formula (I) wherein n, R1, R2, R3, R4 and A are defined as in the description.Type: ApplicationFiled: January 14, 2008Publication date: January 14, 2010Applicant: BASF SEInventors: Wolfgang von Deyn, Matthias Pohlman, Florian Kaiser, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
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Patent number: 7615570Abstract: Compounds having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein L, A, G, R1, R2 and R3 are as defined herein. These compounds are particularly useful in the treatment of pain, inflammatory hyperalgesia, and urinary dysfunctions, such as bladder overactivity and urinary incontinence.Type: GrantFiled: December 5, 2005Date of Patent: November 10, 2009Assignee: Abbott LaboratoriesInventors: Brian S. Brown, Tammie K. Jinkerson, Ryan G. Keddy, Chih-Hung Lee
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Publication number: 20090253750Abstract: The present invention provides 3-indazoyl-4-pyridylisothiazoles or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and methods of using the same, as well as processes for preparing the same, and intermediates thereof.Type: ApplicationFiled: March 18, 2009Publication date: October 8, 2009Inventors: Thomas Charles Britton, Veronique Dehlinger, Adam Michael Fivush, Sean Patrick Hollinshead, Benjamin Paul Vokits
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Publication number: 20090240057Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.Type: ApplicationFiled: July 6, 2007Publication date: September 24, 2009Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD. AND IHARA CHEMICAL INDUSTRY CO., LTD.Inventors: Toshihiro Nagata, Atsushi Kogure, Isao Kaneko, Norihisa Yonekura, Ryo Hanai
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Publication number: 20090227592Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: ApplicationFiled: February 2, 2009Publication date: September 10, 2009Applicant: AstraZeneca ABInventors: Scott BOYD, Peter William Rodney CAULKETT, Rodney Brian HARGREAVES, Suzanne Saxon BOWKER, Roger JAMES, Clifford David JONES, Darren McKERRECHER, Michael Howard BLOCK, Craig JOHNSTONE
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Publication number: 20090192154Abstract: A sultam derivative of Formula (1) described below having inhibitory action for aggrecanase activity is provided. The sultam derivative of Formula (1) and a salt thereof exhibit strong inhibitory action for aggrecanase activity in a living body of a mammalian animal including human, and is useful, for example, as an active ingredient of a pharmaceutical agent for preventing and/or treating various diseases caused by degradation of aggrecan.Type: ApplicationFiled: December 23, 2008Publication date: July 30, 2009Applicant: Asahi Kasei Pharma CorporationInventors: Naomi MAEKAWARA, Masakazu Atobe, Masashi Kawanishi, Eiichi Tanaka
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Patent number: 7560563Abstract: The present invention provides a method of producing a pyridine derivative having a substituent at the 2-position of a heterocyclic structure conveniently and with fine selectivity. The present invention relates to a production method of a pyridine derivative having a substituent at the 2-position of a heterocyclic structure, which is represented by the formula (III), which includes reacting a 2-sulfonylpyridine derivative of the formula (I) with an organometallic compound of the formula (II) and the like, and the like: wherein each symbol is as defined in the Description.Type: GrantFiled: July 23, 2003Date of Patent: July 14, 2009Assignee: Kuraray Co., Ltd.Inventors: Kenichi Koyakumaru, Yoshimi Fukunaga
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Publication number: 20090005353Abstract: The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) ? (NR1H3) and/or ? (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 9, 2006Publication date: January 1, 2009Applicant: AstraZeneca ABInventors: Anders Broo, Robert Judkins, Lanna Li, Eva-Lotte Lindstedt-Alstermark, Pernilla Sandberg, Marianne Swanson, Lars Weidolf, Kay Brickmann, Patrik Holm
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Publication number: 20080269267Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof aType: ApplicationFiled: April 18, 2008Publication date: October 30, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20080261961Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.Type: ApplicationFiled: April 18, 2008Publication date: October 23, 2008Applicant: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Patent number: 7429667Abstract: The invention concerns compounds which inhibit MEK and which have activity as anti-neoplastic agents. These compounds include N-substituted-3-hydroxy-5-arylamino-isothiazole-4-carboxamidines. Also included are the tautomeric isothiazol-3(2H)-ones.Type: GrantFiled: January 20, 2006Date of Patent: September 30, 2008Assignee: Ardea Biosciences, Inc.Inventors: Hassan Abdellaoui, Robert Tam, Huanming Chen, Varaprasad Chamakura, Dinesh Barawkar, Andreas Maderna, Zhi Hong, Stanley Lang
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, 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, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080125466Abstract: Aryl-substituted benzo[d]isothiazol-3-ylamine analogues) are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: July 9, 2004Publication date: May 29, 2008Applicant: NEUROGEN CORPORATIONInventors: Charles A. Blum, Xiaozhang Zheng
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Publication number: 20080125429Abstract: A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided. The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.Type: ApplicationFiled: November 1, 2005Publication date: May 29, 2008Applicant: BANYU PHARMACEUTICAL CO., LTD.Inventors: Noriaki Hashimoto, Keiji Takahashi, Chisato Nakama, Yoshio Ogino, Fumiko Sakai, Teruyuki Nishimura, Jun-ichi Eiki
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Patent number: 7276602Abstract: The invention relates to compounds of the formula 1 or pharmaceutically acceptable salts, prodrugs, solvates or hydrates thereof, wherein wherein X, R1, and R2 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula 1.Type: GrantFiled: July 24, 2003Date of Patent: October 2, 2007Assignee: Pfizer IncInventors: Blaise Lippa, Tricia Ann Kwan, Joel Morris, Susan D. LaGreca, Matthew David Wessel
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Patent number: 7256291Abstract: This invention provides for labeling reagents, labeled targets and processes for preparing labeling reagents. The labeling reagents can take the form of cyanine dyes, xanthene dyes, porphyrin dyes, coumarin dyes or composite dyes. These labeling reagents are useful for labeling probes or targets, including nucleic acids and proteins. These reagents can be usefully applied to protein and nucleic acid probe based assays. They are also applicable to real-time detection processes.Type: GrantFiled: January 22, 2004Date of Patent: August 14, 2007Assignee: Enzo Life Sciences, Inc.Inventors: Jannis G. Stavrianopoulos, Elazar Rabbani
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Patent number: 7253187Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein Z1 and Z2 are each independently nitrogen or CH and Ring A, TmR1, QR2, UnR3, and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.Type: GrantFiled: February 3, 2004Date of Patent: August 7, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jingrong Cao, Jeremy Green, Michael Hale, Francois Maltais, Judy Straub, Qing Tang, Alex Aronov
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Patent number: 7226740Abstract: Unsymmetrical cyanine dyes that incorporate an aza-benzazolium ring moiety are described, including cyanine dyes substituted by a cationic side chain, monomeric and dimeric cyanine dyes, chemically reactive cyanine dyes, and conjugates of cyanine dyes. The subject dyes are virtually non-fluorescent when diluted in aqueous solution, but exhibit bright fluorescence when associated with nucleic acid polymers such as DNA or RNA, or when associated with detergent-complexed proteins. A variety of applications are described for detection and quantitation of nucleic acids and detergent-complexed proteins in a variety of samples, including solutions, electrophoretic gels, cells, and microorganisms.Type: GrantFiled: October 13, 2003Date of Patent: June 5, 2007Assignee: Invitrogen CorporationInventors: Richard P. Haugland, Stephen T. Yue
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Patent number: 7214678Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.Type: GrantFiled: June 1, 2006Date of Patent: May 8, 2007Assignee: Allergan, Inc.Inventors: Robert M. Burk, Sophie Beauchemin
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Patent number: 7183303Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.Type: GrantFiled: November 5, 2004Date of Patent: February 27, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Ian James Collins, Timothy Harrison
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Patent number: 7141596Abstract: The present invention provides compounds that can modulate the activity of a target protein, such as a phosphatase, that selectively binds phosphorylated peptides or proteins. The present compounds can be useful in treating diseases or disorders, including, for example, diabetes and obesity, that are connected directly or indirectly to the activity of the target protein.Type: GrantFiled: October 7, 2004Date of Patent: November 28, 2006Assignee: Incyte CorporationInventors: Andrew P. Combs, Eddy Wai Tsun Yue, Michael J. Bower, Wenyu Zhu, Matthew L. Crawley, Richard B. Sparks, James R. Pruitt, Amy Takvorian
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Patent number: 7132425Abstract: The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.Type: GrantFiled: December 10, 2003Date of Patent: November 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
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Patent number: 7105556Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.Type: GrantFiled: May 22, 2002Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. Cheng, Yoon Jeon, Wei Wang
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Patent number: 7022650Abstract: A description is given of 4-trifluoromethylpyrazolyl-substituted pyridines and pyrimidines of formula (I) and of their use as herbicides. In this formula (I) R1, R2, R3 and R4 are various radicals, A is an aromatic or heteroaromatic radical, and Z is a nitrogen or carbon atom.Type: GrantFiled: July 24, 2003Date of Patent: April 4, 2006Assignee: Bayer CropScience GmbHInventors: Michael Gerhard Hoffmann, Hendrik Helmke, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
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Patent number: 6989398Abstract: Benzanilides are provided which are voltage-dependent potassium channel openers. Methods of using the benzanilides of the invention are also provided.Type: GrantFiled: February 2, 2004Date of Patent: January 24, 2006Assignee: ICAgen, Inc.Inventors: Grant A. McNaughton-Smith, Michael F. Gross, Alan D. Wickenden
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Patent number: 6987189Abstract: A method of making a compound of Formula VI: wherein Tr is a triphenyl group; R1, R2 and R3 are each independently selected from the group consisting of H, C1–C4 alkyl, C1–C4 alkoxy, aryl, heteroaryl, and arylalkyl; R4 is C2–C6 alkyl, and R5 and R6 are each independently H or C1–C4 alkyl, involves the step of reacting a compound of Formula V: with Tr-OH to produce a compound of Formula VI. The compounds of Formula VI are useful as intermediates in the manufacture of antibiotic agents. Methods of making compounds of Formula V, and intermediates made or used in the foregoing methods, are also described.Type: GrantFiled: September 28, 2004Date of Patent: January 17, 2006Assignee: North Carolina State UniversityInventors: Daniel L. Comins, Shenlin Huang
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Patent number: 6987184Abstract: Isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein R0 is —CH2—, —SO—, —O—, —SO2—, or —S—; compositions comprising the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.Type: GrantFiled: February 7, 2002Date of Patent: January 17, 2006Assignee: Signal Pharmaceuticals, LLCInventors: Steven T. Sakata, Heather K. Raymon
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Patent number: 6939882Abstract: Use of compounds of general formula (I) or salts thereof as phytopathogenic fungicides wherein the various radicals and substituents are as defined in the description, pesticidal compositions containing them and method for combatting pests which comprises applying these.Type: GrantFiled: August 11, 2000Date of Patent: September 6, 2005Assignee: Aventis Cropsciences GmbHInventors: Tracey Cooke, David Hardy, Brian Anthony Moloney, Mary Josephine O'Mahony, Michael George Pettett, Gita Patel, Stefan Schnatterer
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Patent number: 6927216Abstract: The present application describes novel cyclic sulfonyl derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.Type: GrantFiled: September 17, 2001Date of Patent: August 9, 2005Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Robert J. Cherney, Bryan W. King
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley