The Additional Hetero Ring Is Five-membered Patents (Class 546/280.4)
  • Patent number: 8202894
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: June 19, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Harald Walter, Daniel Stierli, Hans Tobler
  • Publication number: 20120148955
    Abstract: A resist composition including: a base component (A) which exhibits changed solubility in a developing solution under action of acid; a nitrogen-containing organic compound component (C) containing a compound (C1) represented by general formula (c1) shown below; and an acid generator component (B) which generates acid upon exposure, provided that the compound (C1) is excluded from the acid generator component (B): wherein RN represents a nitrogen-containing heterocyclic group which may have a substituent; X0 represents a linear or branched divalent aliphatic hydrocarbon group of 1 to 10 carbon atoms, a cyclic divalent aliphatic hydrocarbon group of 3 to 20 carbon atoms or a divalent aliphatic hydrocarbon group of 3 to 20 carbon having a cyclic partial structure, or any one of these groups in which some or all of the hydrogen atoms thereof have been substituted with fluorine atoms; and M+ represents an organic cation.
    Type: Application
    Filed: December 6, 2011
    Publication date: June 14, 2012
    Applicant: TOKYO OHKA KOGYO CO., LTD.
    Inventors: Yoshiyuki Utsumi, Kenichiro Miyashita, Akiya Kawaue
  • Publication number: 20120128640
    Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.
    Type: Application
    Filed: June 4, 2010
    Publication date: May 24, 2012
    Applicant: NISSAN CHEMICAL INDUSTRIES LTD.
    Inventors: Taito Nishino, Shunsuke Iwamoto, Katsuaki Miyaji
  • Publication number: 20120129100
    Abstract: An actinic ray-sensitive or radiation-sensitive resin composition including: (PA) a compound having a proton acceptor functional group and undergoing decomposition upon irradiation with an actinic ray or radiation to generate a compound reduced in or deprived of proton acceptor property or changed to be acidic from being proton acceptor-functioning, wherein a molar extinction coefficient ? of the compound (PA) at a wavelength of 193 nm as measured in acetonitrile solvent is 55,000 or less, and a pattern forming method using the composition are provided.
    Type: Application
    Filed: August 17, 2010
    Publication date: May 24, 2012
    Applicant: FUJIFILM CORPORATION
    Inventors: Akinori Shibuya, Shuhei Yamaguchi, Shohei Kataoka, Michihiro Shirakawa, Takayuki Kato, Naohiro Tango
  • Patent number: 8168658
    Abstract: The present invention relates to a novel class of compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
    Type: Grant
    Filed: February 23, 2007
    Date of Patent: May 1, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan B. Grimm, Jed L. Hubbs, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Kevin Wilson, David Witter, Hua Zhou
  • Patent number: 8163778
    Abstract: Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof wherein the residues have the significance given in claim 1 and which can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: November 24, 2008
    Date of Patent: April 24, 2012
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Wolfgang Haap, Paul Hebeisen, Eric Argirios Kitas, Bernd Kuhn, Peter Mohr, Hans Peter Wessel
  • Publication number: 20120094980
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: October 14, 2011
    Publication date: April 19, 2012
    Inventors: Janet L. Gunzner, Daniel P. Sutherlin, Mark S. Stanley, Liang Bao, Georgette Castanedo, Rebecca Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina, Michael F.T. Koehler
  • Publication number: 20120095012
    Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
    Type: Application
    Filed: December 30, 2009
    Publication date: April 19, 2012
    Applicant: Elara Pharmaceuticals GmbH
    Inventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
  • Publication number: 20120094837
    Abstract: The present invention relates to novel heterocyclic compounds, to processes for preparation thereof and to the use thereof for controlling animal pests, which include arthropods and especially insects.
    Type: Application
    Filed: July 15, 2011
    Publication date: April 19, 2012
    Applicant: Bayer Crop Science AG
    Inventors: Friedrich August MÜHLTHAU, Thomas BRETSCHNEIDER, Reiner FISCHER, Martin FÜßLEIN, Markus HEIL, Achim HENSE, Joachim KLUTH, Adeline KÖHLER, Eva-Maria FRANKEN, Olga MALSAM, Arnd VOERSTE, Peter JESCHKE, Angela BECKER, Peter LÖSEL, Yoshitaka SATO
  • Patent number: 8158654
    Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.
    Type: Grant
    Filed: May 19, 2009
    Date of Patent: April 17, 2012
    Assignee: The University of Tennessee Research Foundation
    Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
  • Publication number: 20120071517
    Abstract: The invention discloses a compound of general formula (I) and a process for preparing this compound. The invention discloses a fungicidal composition comprising a compound of general formula (I) and a method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Application
    Filed: November 23, 2011
    Publication date: March 22, 2012
    Applicant: BAYER SAS
    Inventors: Pierre-Yves COQUERON, Philippe DESBORDES, Darren James MANSFIELD, Heiko RIECK, Marie-Claire GROSJEAN-COURNOYER, Alain VILLIER, Pierre GENIX
  • Publication number: 20120046320
    Abstract: The present invention discloses ?-diketones, ?-diketones or ?-hydroxyketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.
    Type: Application
    Filed: August 17, 2011
    Publication date: February 23, 2012
    Applicant: WINTHERIX, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
  • Publication number: 20120046317
    Abstract: The present invention relates to a new class of heterocyclic compounds and pharmaceutically acceptable salts thereof, process for preparing the same, pharmaceutical composition containing these compounds and to their use in treatment of diseases caused due to formation and accumulation of AGEs (Advanced Glycation end products). The compounds of the present invention are useful for the treatment of diabetic and aging-related complications caused by formation and accumulation of AGEs, such as neuropathy, nephropathy, microangiopathy, retinopathy, hypertension, heart failure, atherosclerosis, Alzheimer's disease & dermatological disorders.
    Type: Application
    Filed: May 6, 2010
    Publication date: February 23, 2012
    Inventors: Chaitanya Dutt, Vijay Chauthaiwale, Ramesh Chandra Gupta, Manish Patel, Jignesh Kotecha, Sachin Latad, Jaya Abraham, Sanjay Srivastava, Milin Rode, Shailesh Deshpande, Anita Chaudhary, Amit Kumar Kesarwani
  • Publication number: 20120035157
    Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R4, G1, G2, L, Y and n are as defined in the Specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of neutrophil elastase.
    Type: Application
    Filed: October 14, 2011
    Publication date: February 9, 2012
    Applicant: AstraZeneca AB
    Inventors: Marjana Andersson, Peter Hansen, Hans Lönn, Antonios Nikitidis, Petter Sjölin
  • Publication number: 20120022255
    Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
    Type: Application
    Filed: March 23, 2010
    Publication date: January 26, 2012
    Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
  • Publication number: 20120015399
    Abstract: The present invention presents a novel fluorescent solvatochromic dye that (1) has an ionic terminal that makes it easier to use in a hydrophilic surface or in polar solvents, (2) can be efficiently excited by commonly used Argon lasers (488 nm), (3) shifts the wavelength of emitted light according to the change of polarity, and (4) can effectively stain living tissues such as cells and the like. A pyridinium group was introduced to the electron attracting group of the neutral fluorescent solvatochromic dye (Japanese Patent Application Public Disclosure No. 20008-291210 A) displaying an excellent emission wavelength response and synthesized a fluorescent solvatochromic dye. Then it was found that the fluorescence wavelength of the fluorescent solvatochromic dye changed extensively when the polarity changed on a hydrophilic surface and that the fluorescent solvatochromic dye, when altered to a cationic form, stained cell membranes and could be used to observe the behavior thereof.
    Type: Application
    Filed: February 4, 2010
    Publication date: January 19, 2012
    Applicant: National University Corporation Hokkaido University
    Inventors: Koji Yamada, Yutaka Yamagishi, Tokiyoshi Ayabe, Sang-Hyun Son, Maiko Aoyagi, Toshio Taira
  • Publication number: 20120015297
    Abstract: A compound represented by general formula (b1); an acid generator including the compound; and a resist composition including a base component (A) which exhibits changed solubility in an alkali developing solution under action of acid and an acid-generator component (B) which generates acid upon exposure, the acid-generator component (B) including an acid generator (B1) including a compound represented by general formula (b1), wherein R1 represents a hydrogen atom, a linear, branched or cyclic alkyl group of 1 to 10 carbon atoms or a heterocyclic group of 1 to 10 carbon atoms; R2 represents a linear or branched alkyl group of 1 to 10 carbon atoms; x represents an integer of 0 to 6; n represents an integer of 0 to 3; and X? represents an anion.
    Type: Application
    Filed: July 7, 2011
    Publication date: January 19, 2012
    Applicant: TOKYO OHKA KOGYO.CO., LTD.
    Inventors: Yoshitaka KOMURO, Yoshiyuki Utsumi
  • Patent number: 8093241
    Abstract: The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl which may be substituted by X, a heterocyclic group which may be substituted by X, a fused heterocyclic group which may be substituted by X, indanyl (the indanyl may be substituted by halogen, alkyl or alkoxy) or tetrahydronaphthyl (the tetrahydronaphthyl may be substituted by halogen, alkyl or alkoxy), B is alkyl, cycloalkyl, phenyl which may be substituted by Y, a heterocyclic group which may be substituted by Y, or a condensed heterocyclic group which may be substituted by Y, each of R1 and R2 is alkyl, cyano or —CO2R14, or R1 and R2 may together form a 3- to 6-membered saturated carbocyclic ring, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, —COR15, —S(O)mR16 or —S(O)nNR17R18, which is useful as an active ingredient of pesticides.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: January 10, 2012
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Yuji Nakamura, Masayuki Morita, Tetsuo Yoneda, Kenji Izakura
  • Publication number: 20110318359
    Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.
    Type: Application
    Filed: December 2, 2009
    Publication date: December 29, 2011
    Inventors: Edward P. Feener, Allen Clermont
  • Publication number: 20110319616
    Abstract: An object is to provide a thiazole derivative produced from easily available raw materials by a simplified production process. Provided are a process for producing a novel thiazole derivative represented by the general formula (I), which is characterized by adding a strong base to a thioamide represented by the general formula (II) and reacting the mixture with a thioformamide represented by the general formula (III), and a novel thiazole derivative.
    Type: Application
    Filed: March 8, 2010
    Publication date: December 29, 2011
    Applicant: GIFU UNIVERSITY
    Inventor: Toshiaki Murai
  • Patent number: 8084470
    Abstract: Substituted nicotinamide compounds corresponding to formula I a process for their preparation, pharmaceutical compositions containing these compounds, and the use thereof for the treatment or inhibition conditions such as pain, epilepsy, migraine, anxiety states, or urinary incontinence.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: December 27, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Beatrix Merla, Sven Kuehnert, Robert Frank, Dagmar Kaulartz, Wolfgang Schroeder, Gregor Bahrenberg, Klaus Schiene
  • Patent number: 8071627
    Abstract: A compound of general formula (I) A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Grant
    Filed: November 24, 2008
    Date of Patent: December 6, 2011
    Assignee: Bayer SAS
    Inventors: Pierre-Yves Coqueron, Philippe Desbordes, Darren James Mansfield, Heiko Rieck, Marie-Claire Grosjean-Cournoyer, Alain Villier, Pierre Genix
  • Publication number: 20110281836
    Abstract: One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor.
    Type: Application
    Filed: November 19, 2010
    Publication date: November 17, 2011
    Applicant: PSYCHOGENICS, INC.
    Inventors: Joel R. Walker, Milton Brown, Mikell A. Paige, Yingxian Xiao, Kenneth J. Kellar
  • Patent number: 8058273
    Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: November 15, 2011
    Assignee: DAC S.R.L.
    Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Publication number: 20110251069
    Abstract: The present invention relates to thiophene, furan and pyrrole compounds of formula (I) having plant growth regulating properties, to agricultural compositions comprising them, and to the use of said compounds for regulating plant growth.
    Type: Application
    Filed: December 11, 2009
    Publication date: October 13, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Camilla Corsi, Sebastian Volker Wendeborn, Carla Bobbio, Jilali Kessabi, Peter Schneiter, Valeria Grasso, Ulrich Johannes Haas, Shy-Fuh Lee, Micah Gliedt
  • Publication number: 20110195999
    Abstract: The present invention provides an antifungal agent represented by the formula: wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(?O)—, a group represented by the formula —C(?O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents.
    Type: Application
    Filed: March 14, 2011
    Publication date: August 11, 2011
    Inventors: Kazutaka NAKAMOTO, Itaru Tsukada, Keigo Tanaka, Masayuki Matsukura, Toru Haneda, Satoshi Inoue, Norihiro Ueda, Shinya Abe, Katsura Hata, Naoaki Watanabe
  • Publication number: 20110190310
    Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: May 14, 2009
    Publication date: August 4, 2011
    Inventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
  • Publication number: 20110178129
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: January 14, 2011
    Publication date: July 21, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Michael O' Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Philip Anthony Morganelli, William J. Watkins
  • Publication number: 20110178101
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 18, 2011
    Publication date: July 21, 2011
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 7981925
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: August 26, 2009
    Date of Patent: July 19, 2011
    Assignee: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20110166159
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: March 17, 2011
    Publication date: July 7, 2011
    Applicant: CalciMedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20110160207
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 30, 2011
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 7968542
    Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Grant
    Filed: July 13, 2006
    Date of Patent: June 28, 2011
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Katsuaki Miyaji, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
  • Publication number: 20110152234
    Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Application
    Filed: December 23, 2010
    Publication date: June 23, 2011
    Inventors: Alan Faull, Craig Johnstone, Andrew Morley, Jeffrey Philip Poyser
  • Publication number: 20110130426
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating the glucocorticoid receptor in a warm blooded animal).
    Type: Application
    Filed: October 26, 2005
    Publication date: June 2, 2011
    Applicant: ASTRAZENECA AB
    Inventors: Håkan Bladh, Krister Henriksson, Vijaykumar Hulikal, Matti Lepistö
  • Patent number: 7947732
    Abstract: Disclosed herein is a compound having a formula therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: January 22, 2010
    Date of Patent: May 24, 2011
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Vinh X. Ngo
  • Patent number: 7935825
    Abstract: 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: Grant
    Filed: May 4, 2007
    Date of Patent: May 3, 2011
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Sophie Beauchemin
  • Patent number: 7932272
    Abstract: The present invention provides an antifungal agent represented by the formula: [wherein A1 represents a 3-pyridyl group which may have a substituent, a quinolyl group which may have a substituent, or the like; X1 represents a group represented by the formula —NH—C(?O)—, a group represented by the formula —C(?O)—NH—, or the like; E represents a furyl group, a thienyl group, a pyrrolyl group, a phenyl group, a pyridyl group, a tetrazolyl group, a thiazolyl group or a pyrazolyl group; with the proviso that A1 may have 1 to 3 substituents, and E has one or two substituents].
    Type: Grant
    Filed: September 27, 2004
    Date of Patent: April 26, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Kazutaka Nakamoto, Itaru Tsukada, Keigo Tanaka, Masayuki Matsukura, Toru Haneda, Satoshi Inoue, Norihiro Ueda, Shinya Abe, Katsura Hata, Naoaki Watanabe
  • Publication number: 20110092461
    Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
    Type: Application
    Filed: December 6, 2010
    Publication date: April 21, 2011
    Inventors: Janet L. GUNZNER, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
  • Publication number: 20110092496
    Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: November 29, 2010
    Publication date: April 21, 2011
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Katsuaki MIYAJI, Kazufumi Yanagihara, Yukihiro Shigeta, Shunsuke Iwamoto, Masato Horikawa, Yutaka Hirokawa, Shingo Owada, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
  • Patent number: 7902372
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
    Type: Grant
    Filed: April 2, 2008
    Date of Patent: March 8, 2011
    Assignee: Eli Lilly and Company
    Inventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
  • Publication number: 20110053939
    Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    Type: Application
    Filed: November 8, 2010
    Publication date: March 3, 2011
    Applicant: REVOTAR BIOPHARMACEUTICALS AG
    Inventors: Ewald M. AYDT, Remo Kranich
  • Publication number: 20110053905
    Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.
    Type: Application
    Filed: September 3, 2010
    Publication date: March 3, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Xialing Guo, Zhen Zhu
  • Publication number: 20110034378
    Abstract: The present invention relates to a combination, such as a combined preparation or pharmaceutical composition comprising: (a) compound of formula (I), and/or (II) or a pharmaceutically acceptable salt thereof; (b) at least one therapeutic agent selected from the group consisting of: an antihypertensive agent; an antidiabetics agent; a hypolipidemic agent; an antiplatelet agent; an antiobesity agent; an antithrombotic agent; an agent for diabetic vascular complications; and an agent for treatment of heart failure; or a pharmaceutically acceptable salts thereof, optionally in presence of a pharmaceutically acceptable carrier for separate, simultaneous or sequential use. The present invention also relates to a use of such combination for the treatment of mammal including human being. R1, R2, R3, R1, R2, R3, R4, R5, X, Y, A and B and m are as defined in the specification.
    Type: Application
    Filed: January 21, 2009
    Publication date: February 10, 2011
    Inventors: Chaitanya Dutt, Deepa Joshi, Ram Gupta, Kumarprafull Chandra
  • Publication number: 20110020278
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: July 19, 2010
    Publication date: January 27, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
  • Publication number: 20110009447
    Abstract: Substituted benzoic acid amides of formula (I) and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis as well as their intermediate products for the production of benzoic acid amides are described.
    Type: Application
    Filed: April 24, 2001
    Publication date: January 13, 2011
    Inventors: Andreas Huth, Dieter Seidelmann, Karl-Heinz Thierauch
  • Patent number: 7868023
    Abstract: Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. The compounds are of Formula I or a solvate, hydrate, pharmaceutically acceptable salt, or prodrug thereof; wherein Ra, Rb, and Rc are as defined in the specification, as are A Z, Q, R1 and R2.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: January 11, 2011
    Assignee: Janssen Pharmaceutica NV
    Inventors: Nalin L. Subasinghe, Shelley Ballentine, Jeremy M. Travins, Ehab M. Khalil, Farah Ali, Kristi A. Leonard, Joan M. Gushue, Michael Peter Winters, Heather Hufnagel, Maxwell David Cummings
  • Publication number: 20110003806
    Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: January 28, 2010
    Publication date: January 6, 2011
    Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
  • Publication number: 20100324046
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Application
    Filed: June 24, 2008
    Publication date: December 23, 2010
    Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Publication number: 20100311582
    Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.
    Type: Application
    Filed: January 23, 2009
    Publication date: December 9, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach