Cyano Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/330)
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Publication number: 20130197013Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.Type: ApplicationFiled: July 27, 2011Publication date: August 1, 2013Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
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Publication number: 20130136794Abstract: Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.Type: ApplicationFiled: April 21, 2011Publication date: May 30, 2013Applicant: PEKING UNIVERSITYInventors: Runtao Li, Zemei Ge, Jingrong Cui, Xingyl Sun, Zhongqing Wang, Xu Yan
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Publication number: 20130040993Abstract: The present invention relates to hydroximoyl-heterocycle derivatives, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: December 28, 2010Publication date: February 14, 2013Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20120329786Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.Type: ApplicationFiled: August 31, 2012Publication date: December 27, 2012Applicant: Myrexis, Inc.Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup
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Patent number: 8338601Abstract: A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture: R1—B-T??(I); where R1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pKB of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.Type: GrantFiled: September 25, 2009Date of Patent: December 25, 2012Assignee: Board of Trustees of the University of IllinoisInventors: Martin D. Burke, David M. Knapp, Eric P Gillis
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Publication number: 20120316195Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 16, 2010Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
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Publication number: 20120283094Abstract: The present invention provides bis-organosulfur compounds of formulae (I) and (II) and compositions comprising the compounds that are effective against animal pests, including parasites. The compounds and compositions may be used for combating parasites in or on birds and mammals and for combating pests that damage crops, plants and plant propagation material. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.Type: ApplicationFiled: December 5, 2010Publication date: November 8, 2012Inventors: Charles Q. Meng, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Ralph Paulini, Sebastian Soergel
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Patent number: 8288589Abstract: The invention disclosed in this document is related to field of pesticides and their use in controlling pests. In particular compounds having the following formula are disclosed.Type: GrantFiled: July 11, 2008Date of Patent: October 16, 2012Assignee: Dow AgroSciences, LLCInventors: Benjamin M. Nugent, Ann M. Buysse, Jonathan M. Babcock, Matthias S. Ober, Timothy P. Martin
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Patent number: 8278338Abstract: Saturated and unsaturated 3-pyridyl-benzocycloalkylmethyl-amines=compounds corresponding to formula (I), wherein the various substituents have the meaning provided in the description, and pharmaceutical formulations containing these compounds and methods for producing these compounds and related pharmaceutical formulation, and to methods for treating or inhibiting pain, depression and/or anxiety states.Type: GrantFiled: December 22, 2006Date of Patent: October 2, 2012Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Klaus Schiene, Petra Bloms-Funke, Werner Englberger, Sven Frormann, Derek Saunders
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Patent number: 8269016Abstract: N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 16, 2010Date of Patent: September 18, 2012Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers, Yuanming Zhu, James M. Renga, Vidyadhar B. Hegde, Joseph J. DeMark
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Publication number: 20120220463Abstract: The present invention relates to crystalline complexes of 4-hydroxy benzoic acid and selected pesticides. It also relates to agriculturally useful compositions of the complexes.Type: ApplicationFiled: October 28, 2010Publication date: August 30, 2012Applicant: BASF SEInventors: Heidi Emilia Saxell, Rafel Israels, Ansgar Schaefer, Matthias Bratz, Hans Wolfgang Hoeffken, Ingo Brode, Elisa Nauha, Maija Nissinen
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Publication number: 20120220590Abstract: Compounds of formula (I) and pharmaceutical compositions containing them are described. The use of the compounds and compositions are also described.Type: ApplicationFiled: July 30, 2010Publication date: August 30, 2012Inventors: Pravin S. Thombare, Amitgiri Goswami, Edouard Zamaratski, Tomas Hansson, Thomas Norin
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Publication number: 20120209007Abstract: The present invention relates to titanium catalysts for synthesis reactions produced by bringing a reaction mixture comprising a titanium alkoxide and a ligand in contact with water, wherein the ligand is represented by the general formula (e): wherein R1, R2, R3, and R4 are independently a hydrogen atom, an alkyl group, or the like, and (A) represents a group with two or more carbon atoms. The titanium catalysts may be isolated in solid form and may be stored. The invention further relates to a process for cyanation of imines, wherein the process comprises reacting an imine with a cyanating agent in the presence of the titanium catalyst.Type: ApplicationFiled: February 11, 2010Publication date: August 16, 2012Applicants: Agency for Science, Technology and Research, Mitsui Chemicals Inc.Inventors: Abdul Majeed Seayad, Balamurugam Ramalingam, Christina Chai, Takushi Nagata, Kazuhiko Yoshinaga, Manabu Wadamoto
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Publication number: 20120189537Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.Type: ApplicationFiled: November 22, 2011Publication date: July 26, 2012Inventor: Krishna Menon
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Publication number: 20120165538Abstract: Cyano-substituted sulfilimines and sulfoximines are produced efficiently and in high yield from the corresponding sulfides by reaction with cyanamide and hypochlorite.Type: ApplicationFiled: December 21, 2011Publication date: June 28, 2012Applicant: Dow AgroSciences LLCInventors: Douglas C. Bland, Timothy J. Adaway, David E. Podhorez
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Publication number: 20120149738Abstract: Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Applicant: Board of Regents, The University of Texas SystemInventors: Waldemar Priebe, Stanislaw Skora, Timothy Madden, Izabela Fokt, Charles Conrad
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Patent number: 8193364Abstract: N-Substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximines are effective at controlling insects.Type: GrantFiled: February 16, 2010Date of Patent: June 5, 2012Assignee: Dow AgroSciences, LLC.Inventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang, Richard B. Rogers, Yuanming Zhu, James M. Renga, Vidyadhar B. Hegde, Joseph J. DeMark
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Patent number: 8163735Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.Type: GrantFiled: December 1, 2005Date of Patent: April 24, 2012Assignee: Virobay, Inc.Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
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Publication number: 20120077806Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: September 23, 2011Publication date: March 29, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
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Patent number: 8143412Abstract: Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders.Type: GrantFiled: June 26, 2009Date of Patent: March 27, 2012Inventors: Waldemar Priebe, Stanislaw Skora, Timothy Madden, Izabela Fokt, Charles Conrad
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Publication number: 20120041036Abstract: An object of the present invention is to provide an excellent agent for treating or preventing dementia, schizophrenia based on serotonin 5-HT5A receptor modulating action. It was discovered that acylguanidine derivatives, in which the guanidine is bonded to one ring of a naphthalene via a carbonyl group and a cyclic group is bonded to the other ring thereof, exhibit potent the 5-HT5A receptor modulating action and excellent pharmacological actions based on the action. The present invention is useful as an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder or attention deficit hyperactivity disorder.Type: ApplicationFiled: February 8, 2010Publication date: February 16, 2012Inventors: Isao Kinoyama, Yohei Koganemaru, Takehiro Miyazaki, Takuya Washio
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Publication number: 20120004417Abstract: This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.Type: ApplicationFiled: October 20, 2009Publication date: January 5, 2012Inventor: Stephen Dimagno
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Publication number: 20110319629Abstract: The present invention relates to titanium catalysts for synthesis reactions produced by bringing a reaction mixture comprising a titanium alkoxide and a ligand in contact with water, wherein the ligand is represented by the general formula (e): wherein R1, R2, R3, and R4 are independently a hydrogen atom, an alkyl group, or the like, and (A) represents a group with two or more carbon atoms. The titanium catalysts may be isolated in solid form and may be stored. The invention further relates to a process for cyanation of imines, wherein the process comprises reacting an imine with a cyanating agent in the presence of the titanium catalyst.Type: ApplicationFiled: February 11, 2010Publication date: December 29, 2011Applicants: Agency for Science, Technology and Research, Mitsui Chemicals Inc.Inventors: Abdul Majeed Seayad, Balamurugam Ramalingam, Christina Chai, Takushi Nagata, Kazuhiko Yoshinaga, Manabu Wadamoto
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Publication number: 20110306493Abstract: The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such sulfoximine compounds. The sulfoximinamid compounds of the present invention are defined by the following formula I: wherein Q, Het, R1, R2, R3, R4 and n are defined as in the description.Type: ApplicationFiled: June 19, 2009Publication date: December 15, 2011Applicant: BASF SEInventors: Ralph Paulini, Delphine Breuninger, Wolfgang Von Deyn, Henricus Maria Martinus Bastiaans, Carsten Beyer, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Faraneh Oloumi
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Publication number: 20110281879Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 12, 2011Publication date: November 17, 2011Applicant: ViroBay, Inc.Inventor: Craig Mossman
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Publication number: 20110278512Abstract: Unconventional twisted ?-electron system electro-optic (EO) chromophores/compounds, compositions and related device structures. Crystallographic analysis of several non-limiting chromophores reveals, for instance, large ring-ring dihedral twist angles and a highly charge-separated zwitterionic structure in the ground state, in both solution phase and solid-state.Type: ApplicationFiled: June 27, 2011Publication date: November 17, 2011Applicant: Northwestem UniversityInventors: Tobin J. Marks, Hu Kang
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Publication number: 20110281894Abstract: The present invention relates to a hemifumarate salt of the compound (1S)-1-(2-(difluoromethyl)pyridin-4-yl)-4-fluoro-1-(3-(pyrimidin-5-yl)phenyl)-1H-isoindol-3-amine, Form A thereof and its pharmaceutical compositions. In addition, the present invention relates to therapeutic methods for the treatment and/or prevention of A?-related pathologies such as Downs syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer Disease, memory loss, attention deficit symptoms associated with Alzheimer disease, neurodegeneration associated with diseases such as Alzheimer disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.Type: ApplicationFiled: May 11, 2011Publication date: November 17, 2011Applicant: ASTRAZENECA ABInventors: Per-Olov Bergström, Anna Minidis, Robert Ulf Johan Stranne, Mikael Wernersson
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Patent number: 8057712Abstract: The present invention relates to radialene compounds as well as to their use as doping agent for doping an organic semiconductive matrix material, as blocker material, as charge injection layer, as electrode material as well as organic semiconductor, as well as electronic components and organic semiconductive materials using them.Type: GrantFiled: November 4, 2008Date of Patent: November 15, 2011Assignee: Novaled AGInventors: Olaf Zeika, Steffen Willmann, Sascha Dorok, Ansgar Werner, Christine Bachmann
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Publication number: 20110193022Abstract: Provided is a liquid crystal compound having general physical properties necessary for a compound, stability to heat, light or the like, a wide liquid crystal phase temperature range, a high clearing point, an excellent compatibility with other liquid crystal compounds, a large refractive index anisotropy and a large dielectric anisotropy. Provided are a liquid crystal composition including the liquid crystal compound, and a liquid crystal display device containing the liquid crystal composition. The compound is represented by formula (1): wherein, for example, R1 is alkyl having 1 to 20 carbons; at least one of the rings A1 to A6 is pyrimidine-2,5-diyl or pyridine-2,5-diyl and the others are 1,4-cyclohexylene or 1,4-phenylene; Z1 to Z6 are a single bond; L1 to L4 is hydrogen or halogen; X1 is hydrogen, halogen, —C?N or alkyl having 1 to 10 carbons; and l, m, n, o, p and q are 0 or 1 and l+m+n+o+p+q=3.Type: ApplicationFiled: October 14, 2009Publication date: August 11, 2011Applicants: JNC CORPORATION, CHISSO PETROCHEMICAL CORPORATIONInventors: Hiroyuki Tanaka, Kouki Sagou
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Publication number: 20110190505Abstract: This disclosure relates to compounds, reagents, and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. For example, this disclosure provides universal “locked” aryl substituents that result in StereoElectronic Control of Unidirectional Reductive Elimination (SECURE) from diaryliodonium salts. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.Type: ApplicationFiled: February 4, 2011Publication date: August 4, 2011Inventor: Stephen DiMagno
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Patent number: 7981324Abstract: The present invention relates to oxocarbon-, pseudooxocarbon- and radialene compounds as well as to their use as doping agent for doping an organic semiconductive matrix material, as blocker material, as charge injection layer, as electrode material as well as organic semiconductor, as well as electronic components and organic semiconductive materials using them.Type: GrantFiled: April 29, 2008Date of Patent: July 19, 2011Assignee: Novaled AGInventors: Horst Hartmann, Olaf Zeika, Andrea Lux, Steffen Willmann
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Publication number: 20110152322Abstract: The present invention relates to aminopropenoate derivatives, the process of their preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: October 18, 2010Publication date: June 23, 2011Applicant: Bayer CropScience AGInventors: Christophe DUBOST, Jacky Vidal, Philippe Rinolfi, Marie-Claire Grosjean-Cournoyer, Mazen Es-Sayed, Jürgen Benting, Ulrike Wachendorff-Neumann, Shinichi Narabu, Koichi Ishikawa, Hiroyuki Hadano, Pierre Genix, Jean-Pierre Vors, Angela Becker, Ulrich Görgens
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Publication number: 20110130540Abstract: There are disclosed high yield and high productivity processes for preparing 3-hydroxyglutaronitrile by reacting allyl cyanide epoxide with a basic aqueous solution of a cyanide source.Type: ApplicationFiled: August 14, 2008Publication date: June 2, 2011Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventor: Jelena Cirakovic
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Patent number: 7943803Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: GrantFiled: May 4, 2010Date of Patent: May 17, 2011Assignee: Nippon Soda Co., Ltd.Inventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Patent number: 7935826Abstract: N-Substituted (heteroaryl)cycloalkyl sulfoximines are effective at controlling insects.Type: GrantFiled: September 10, 2009Date of Patent: May 3, 2011Assignee: Dow AgroSciences LLCInventors: Michael R. Loso, Benjamin M. Nugent, Jim X. Huang
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Publication number: 20110092544Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein each W and Y is independently CH2, O, C(?O), S(?O)n, NR8 or a direct bond; R4 is H, halogen, cyano, hydroxy, C1-C2 alkyl, C1-C2 haloalkyl, C2 alkenyl, C2 haloalkenyl or C2 alkynyl; m is an integer selected from 0, 1, 2, 3, 4 and 5; and R1, R2, R3, R5, R8 and n 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: June 18, 2009Publication date: April 21, 2011Applicant: E.I. DU PONT DE nemours and companyInventor: Bruce Lawrence Finkelstein
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Patent number: 7902233Abstract: Compounds useful to control pests are provided.Type: GrantFiled: May 29, 2009Date of Patent: March 8, 2011Assignee: Dow AgroSciences LLCInventors: Zoltan L. Benko, David A. Demeter, Carl Deamicis, Lowell Markley, Jack Geno Samaritoni, Carrie Schmidt, Yuanming Zhu, W. Randal Erickson, Peter B. Anzeveno, James Todd Pechacek, Gerald B. Watson, Gerrit Deboer, Joel J. Sheets, Susan Zabik, Carla N. Yerkes, Christian Schobert, James E. Dripps, Leonard Dintenfass, Laura L. Karr, Paul A. Neese, Jim X. Huang, James M. Gifford
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Publication number: 20110053992Abstract: Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders.Type: ApplicationFiled: June 26, 2009Publication date: March 3, 2011Inventors: Waldemar Priebe, Stanislaw Skora, Timothy Madden, Izabela Fokt, Charles Conrad
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Patent number: 7893093Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: March 22, 2006Date of Patent: February 22, 2011Assignee: ViroBay, Inc.Inventor: Craig J. Mossman
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Publication number: 20110039705Abstract: A method of producing a granular agrochemical composition having excellent handling properties, wherein a powdered agrochemical wettable composition or powdered agrochemical water-soluble composition is converted in form to a granular agrochemical composition, without altering the formulation thereof. The method of producing a granular agrochemical composition includes: treating a powdered agrochemical wettable composition or powdered agrochemical water-soluble composition by (1) a step of adding water, kneading, extruding and drying, (2) a step of adding water, granulating by stirring and drying, (3) a step of adding water, kneading and spray-drying, (4) a step of adding water and performing fluidized bed granulation, or (5) a step of pressure molding the powdered agrochemical wettable composition or powdered agrochemical water-soluble composition; followed by (a) a step of performing microgranulation by grinding, and if necessary, (b) a step of performing grain size regulation by sieving.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Inventors: Yoshihisa Endo, Satoru Yamamura
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Patent number: 7888377Abstract: Monocyclic and bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt or solvate of said compound wherein represents an optional double bond and wherein Gn, Jn, R3, R8, R9, R10, R11, R32, R33, B and Het are herein defined are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other agents is also claimed.Type: GrantFiled: March 27, 2007Date of Patent: February 15, 2011Assignee: Schering CorporationInventors: Mariappan V. Chelliah, Samuel Chackalamannil, Yan Xia
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Patent number: 7872022Abstract: The present invention relates to trans-derivatives of formula wherein R1, R2, R3, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.Type: GrantFiled: March 23, 2007Date of Patent: January 18, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Christophe Grundschober, Patrick Schnider
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Publication number: 20100331549Abstract: There is described compounds of Formulæ I, II, III, IV and V. The compounds of Formulæ I, II, III, IV and/or V are useful: in therapeutic methods and compositions for modulating cell proliferation, in diagnostic assays and as research tools.Type: ApplicationFiled: August 26, 2010Publication date: December 30, 2010Inventors: Chaim Roifman, Peter Demin, Olga Rounova, Tom Grunberger
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Publication number: 20100305056Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, strongyloidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.Type: ApplicationFiled: November 26, 2008Publication date: December 2, 2010Applicant: Merck Frosst Canada Ltd.Inventors: Elise Isabel, Christophe Mellon, Christian Beaulieu
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Publication number: 20100298374Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.Type: ApplicationFiled: May 14, 2010Publication date: November 25, 2010Applicant: CELLCEUTIX CORPORATIONInventor: Krishna MENON
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Publication number: 20100292229Abstract: The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.Type: ApplicationFiled: July 2, 2007Publication date: November 18, 2010Applicant: The Board of Regents of the University of Texas SystemInventors: Nicholas J Donato, David Maxwell, Moshe Talpaz, William Bornmann, Zhenghong PENG, Ashutosh Pal, Dongmei Han, Shimei Wang, Geoffrey Bartholomeusz, Vaibhav Kapuria
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Publication number: 20100279340Abstract: Charged and neutral small fluorescent molecules based upon the styryl scaffold are useful as imaging agents for misfolded proteins such as amyloid plaque. Charged molecules are prepared using pyrrolidine catalyzed reactions by solution-phase synthesis. Neutral styryl molecules are prepared using acetic anhydride catalyzed reactions, Horner-Emmons reactions or Wittig reactions.Type: ApplicationFiled: February 11, 2008Publication date: November 4, 2010Applicant: NYUInventors: Thomas Wisniewski, Jaeki Min, Qian Li, Young-Tae CHANG
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Publication number: 20100273919Abstract: Unconventional twisted ?-electron system electro-optic (EO) chromophores/compounds, compositions and related device structures. Crystallographic analysis of several non-limiting chromophores reveals, for instance, large ring-ring dihedral twist angles and a highly charge-separated zwitterionic structure in the ground state, in both solution phase and solid-state.Type: ApplicationFiled: June 14, 2010Publication date: October 28, 2010Inventors: Tobin J. Marks, Hu Kang
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Publication number: 20100274006Abstract: A clathrate compound containing a polymolecular host compound as a host compound and an agricultural chemical active ingredient having a saturated solubility in water at 25° C. of not less than 500 ppm as a guest compound.Type: ApplicationFiled: May 4, 2010Publication date: October 28, 2010Applicant: NIPPON SODA CO., LTDInventors: Natsuki Amanokura, Tetsuya Sahara, Hiroshi Suzuki, Yuichi Maekawa, Kiyoshi Katsuura, Yoshihiro Enomoto
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Publication number: 20100240900Abstract: The carbon nanomaterials and methods relate to methods for causing carbon nanospheres to be readily dispersible in a material. The carbon nanospheres are rendered dispersible using a cationic surfactant. The surfactant includes one or more cationic group that can bond to the surface of the carbon nanospheres, without detrimentally affecting the unique properties of carbon nanospheres. The dispersible carbon nanospheres can be dried (i.e., solvent is driven off) while maintaining their dispersibility in solvents and other materials.Type: ApplicationFiled: March 23, 2009Publication date: September 23, 2010Applicant: HEADWATERS TECHNOLOGY INNOVATION, LLCInventors: Cheng Zhang, Gaurang Bhargava, Bing Zhou