Hetero Ring Patents (Class 544/212)
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Publication number: 20120135994Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: September 28, 2011Publication date: May 31, 2012Applicant: ICOS CorporationInventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
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Publication number: 20120129862Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.Type: ApplicationFiled: May 23, 2011Publication date: May 24, 2012Inventors: Steven J. Coats, Alexey B. Dyatkin, Wei He, Joseph Lisko, Tamara A. Miskowski, Janet L. Ralbovsky, Mark J. Schulz
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Publication number: 20120122680Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 0, 1, 2 or 3; and R1, R2, R3, R4, R5a, R5b, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: August 3, 2010Publication date: May 17, 2012Applicant: E.I. Du Pont de Nemours and CompanyInventors: Caleb William Holyoke, JR., Wenming Zhang, kanu Maganbhai Patel, George Philip Lahm, My-Hanh Thi Tong
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Publication number: 20120122835Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: January 18, 2012Publication date: May 17, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Patent number: 8173808Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: May 8, 2012Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel
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Publication number: 20120104940Abstract: The present invention relates to novel compounds for organic electronic material, and organic electronic devices and organic solar cells using the same. The compounds for organic electronic material may be included in a hole transport layer, electron transport layer or hole injection layer, or may be used as host or dopant. With good luminous efficiency and excellent life property of the material, they may be used to manufacture OLEDs having very good operation life.Type: ApplicationFiled: March 19, 2010Publication date: May 3, 2012Applicant: Rohm and Haas Electronic Materials Korea Ltd.Inventors: Hyo-Nim Shin, Chi Sik Kim, Young Jun Cho, Hyuck Joo Kwon, Bong Ok Kim, Sung Min Kim, Seung Soo Yoon
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Publication number: 20120097925Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein Ar1, Ar2, X, and R1 to R5 are defined as in the specification.Type: ApplicationFiled: April 1, 2011Publication date: April 26, 2012Applicant: Samsung Mobile Display Co., Ltd.Inventors: Young-Kook KIM, Seok-Hwan Hwang, Hye-Jin Jung, Jin-O Lim, Jong-Hyuk Lee
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Publication number: 20120097899Abstract: The present invention describes novel indenofluorene derivatives which can preferably be employed as matrix materials for phosphorescent dopants or as electron-transport materials, in particular for use in the emission and/or charge-transport layer of electroluminescent devices. The invention furthermore relates to polymers which comprise these compounds as structural units and to a process for the preparation of the compounds according to the invention and to electronic devices which comprise same.Type: ApplicationFiled: June 1, 2010Publication date: April 26, 2012Inventors: Amir Hossain Parham, Christof Pflumm, Teresa Mujica-Fernaud, Arne Buesing, Holger Heil
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Publication number: 20120094999Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: May 5, 2010Publication date: April 19, 2012Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
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Publication number: 20120095005Abstract: A series of substituted pyrazolo[1,5-?][1,3,5]triazine and pyrazolo[1,5-?j-pyrimidine derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. Formula (I).Type: ApplicationFiled: May 19, 2010Publication date: April 19, 2012Applicant: UCB PHARMA S.A.Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Barry John Langham, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
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Publication number: 20120091446Abstract: A compound for an organic optoelectronic device, an organic light emitting diode, and a display device, the compound including sequentially combined substituents represented by the following Chemical Formulae 1 to 3:Type: ApplicationFiled: December 23, 2011Publication date: April 19, 2012Inventors: Sung-Hyun JUNG, Hyung-Sun Kim, Ho-Jae Lee, Eun-Sun Yu, Mi-Young Chae, Young-Hoon Kim, Ja-Hyun Kim
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Patent number: 8153788Abstract: Compounds of the formula (I) or salts thereof, in which in which R1 is an optionally substituted amino group or analogous group, and R2 to R7 are each as described herein, are suitable as herbicides and crop growth regulators. The compounds (I) can be prepared by the processes described, via intermediates including novel intermediates for example of the formula (III).Type: GrantFiled: December 14, 2007Date of Patent: April 10, 2012Inventors: Hartmut Ahrens, Hansjörg Dietrich, Thomas Auler, Martin Hills, Heinz Kehne, Dieter Feucht, Stefan Herrmann, Kristian Kather, Stefan Lehr
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Publication number: 20120080670Abstract: Disclosed are a novel-structural compound including a 5-membered heterocycle, an organic electronic device using the same, and a terminal thereof.Type: ApplicationFiled: April 30, 2010Publication date: April 5, 2012Applicants: Samsung Mobile Display Co., Ltd., Duksan High Metal Co., Ltd.Inventors: Junghwan Park, Daesung Kim, Jungcheol Park, Klwon Kim, Jinuk Ju, Jangyeol Baek, Soungyun Mun, Yongwook Park, Hwasoon Jung, Wonsam Kim, Jihun Byun, Sungjin Park, Eunkyung Kim, Daehyuk Choi, Dongha Kim, Hansung Yu, Kwanhee Lee, Taeshick Kim, Daeyup Shin, Mikyung Kim, Dongheon Kim
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Publication number: 20120077815Abstract: A series of amino-substituted fused pyridine and pyrazine derivatives, in particular amino-substituted quinoline and quinoxaline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: February 11, 2010Publication date: March 29, 2012Applicant: UCB PHARMA S.A.Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
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Publication number: 20120077814Abstract: The disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof, compositions containing these compounds, and methods of using these compounds in a variety applications, such as treatment of diseases or disorders associated with E1 type activating enzymes, and with Nedd8 activating enzyme (NAE) in particular.Type: ApplicationFiled: September 12, 2011Publication date: March 29, 2012Inventors: Zhong Wang, Emilie D. Smith, James M. Veal, Kenneth H. Huang, Robert N. Atkinson, Rong Jiang
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Publication number: 20120068170Abstract: The present invention describes indenocarbazole derivatives having electron- and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices or as matrix material. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same.Type: ApplicationFiled: May 3, 2010Publication date: March 22, 2012Applicant: MERCK PATENT GmbHInventors: Christof Pflumm, Arne Buesing, Amir Hossain Parham, Teresa Mujica-Fernaud, Holger Heil, Philipp Stoessel
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Publication number: 20120053167Abstract: A series of substituted [1,3,5]triazin-2-yl derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: March 2, 2010Publication date: March 1, 2012Applicant: UCB PHARMA, S.A.Inventors: Daniel Rees Allen, Roland Bürli, Alan Findlay Haughan, Jonathan David MacDonald, Mizio Matteucci, David John Nash, Andrew Pate Owens, Gilles Raphy, Elizabeth Anne Saville-Stones, Andrew Sharpe
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Publication number: 20120040881Abstract: The invention relates to new triazine derivatives, the use of new triazine derivatives as graying-inhibiting active substances, and washing agent compositions comprising the new triazine derivatives as graying-inhibiting active substances along with surfactant and other ingredients found in detergent compositions.Type: ApplicationFiled: September 22, 2011Publication date: February 16, 2012Applicant: Henkel AG & KGaAInventors: Thomas Eiting, Birgit Glüsen
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Patent number: 8093382Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C?NR4, and L, X, Z, R2 and R3 are as defined herein.Type: GrantFiled: December 9, 2010Date of Patent: January 10, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Michael B. Wallace, Jeffrey A. Stafford, Zhiyuan Zhang
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MATERIAL FOR PHOSPHORESCENT LIGHT-EMITTING ELEMENT AND ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME
Publication number: 20120001165Abstract: Provided is an organic electroluminescent device (organic EL device), which has improved luminous efficiency, has sufficient driving stability, and has a simple construction. The organic EL device of the present invention is an organic electroluminescent device, including a light-emitting layer and a hole-transporting layer between an anode and a cathode laminated on a substrate, in which the light-emitting layer contains a phosphorescent light-emitting dopant and an indolocarbazole compound that serves as a host material, or alternatively, the hole-transporting layer contains an indolocarbazole compound. The indolocarbazole compound is represented by the following formula (1). In the formula: A1's each represent an aromatic hydrocarbon group or an aromatic heterocyclic group, provided that at least one of A1's has a fused ring structure; and R1's each represent a hydrogen atom, an alkyl group, an alkoxy group, or an acyl group.Type: ApplicationFiled: March 25, 2010Publication date: January 5, 2012Inventors: Masaki Komori, Takahiro Kai, Toshihiro Yamamoto -
Patent number: 8088761Abstract: Compounds of formula (I), are aurora kinase inhibitors: wherein X is —N—, —CH2-N—, —CH2-CH—, or —CH—; R1 is a radical of formula (IA) wherein Z is —CH2-, —NH—, -0-, —S(O)— —S—, —S(O)2 or a divalent monocyclic carbocyclic or heterocyclic radical having 3-7 ring atoms; Alk is an optionally substituted divalent C1-C6 alkylene radical; A is hydrogen or an optionally substituted monocyclic carbocyclic or heterocyclic ring having 5-7 ring atoms; r, s and t are independently 0 or 1, provided that when A is hydrogen then at least one of r and s is 1; R2 is halogen, —CN, —CF3, —OCH3, or cyclopropyl; and R3 is a radical of formula (IB) wherein Q is hydrogen or an optionally substituted phenyl or monocyclic heterocyclic ring with 5 or 6 ring atoms; Z&It;1> is —S—, —S(O)—, —S(O)2-, —O—, —SO2NH—, —NHSO2-, NHC(?O)NH, —NH(C?S)NH—, Or —N(R4)— wherein R4 is hydrogen, C1-C3 alkyl, cycloalkyl, or benzyl; and Alk&It;1> and Alk&It;2> are, independently, optionally substituted divalent C1-C3 alkyleType: GrantFiled: December 21, 2006Date of Patent: January 3, 2012Assignee: Cancer Research Technology LimitedInventors: Vassilios Bavetsias, Edward McDonald, Spyridon Linardopoulos
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Publication number: 20110319418Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, L2, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Publication number: 20110319400Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Publication number: 20110319414Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Ra, Rb and Rc are, (a) Ra and Rb are taken together ?Z; and Rc is a group represented by R1c; or (b) Rb and Rc are taken together to form a bond; and Ra is a group represented by —Y—R1a; R1a and R1c are each independently hydrogen, substituted or unsubstituted alkyl, etc.; R2 and R3 are each independently substituted or unsubstituted aryl, etc.; R4a and R4b are each independently hydrogen, substituted or unsubstituted alkyl, etc.; X is —N(R5)—, etc.; R5 is hydrogen, substituted or unsubstituted lower alkyl, etc.; —Y— is —O—, etc.; ?Z is ?O, etc.; and n is an integer of 0 to 4.Type: ApplicationFiled: February 10, 2010Publication date: December 29, 2011Inventors: Hiroyuki Kai, Takayuki Kameyama, Tsuyoshi Hasegawa, MIho Oohara, Yukio Tada, Takeshi Endoh
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COMPOUND FOR ORGANIC ELECTROLUMINESCENT DEVICE AND ORGANIC ELECTROLUMINESCENT DEVICE HAVING THE SAME
Publication number: 20110309345Abstract: The present invention provides a compound of formula (I) for an organic electroluminescent device: wherein X and Y are each independently selected for the group consisting of an alkyl substituted, aryl substituted or unsubstituted carbazole, indolocarbazole, triphenylsilyl and diphenylphosphine oxide represented by formula (A), (B), (C), (D) or (E), in which R1, R2, and R3 are each independently selected from the group consisting of a hydrogen, an alkyl having 1 to 15 carbons atoms, an aryl group having 6 to 15 carbons atoms, an alkyl substituted, an aryl substituted or unsubstituted triphenylsilyl, and a diphenylphosphine oxide represented by the formula (D) or (E); m and n are each independently 0 or 1, provided that m+n is 1 or more; and Ar1 and Ar2 are each independently selected from the group consisting of an alkyl substituted, aryl substituted or unsubstituted phenyl, tolyl, naphthyl, fluorenyl, anthracenyl, and phenanthryl.Type: ApplicationFiled: June 16, 2011Publication date: December 22, 2011Applicant: E-RAY OPTOELECTRONICS TECHNOLOGY CO., LTD.Inventors: Banumathy Balaganesan, Yi-Huan Fu, Huang-Ming Guo -
Publication number: 20110301123Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R9a, R9b, G, W, X, Y, and Z 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: August 16, 2011Publication date: December 8, 2011Applicant: E.I. DU PONT NEMOURS AND COMPANYInventor: Paula Louise Sharpe
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Publication number: 20110294810Abstract: The present invention relates (pyridyl)-azinylamino derivatives of formula (I) wherein Q1 and p, Ra to Rc, X, Y, Z, L2 and Q2 represent various substituents, their process of preparation, 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, using these compounds or compositions.Type: ApplicationFiled: November 13, 2009Publication date: December 1, 2011Inventors: Christian Beier, Jurgen Benting, Pierre-Yves Coqueron, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Jean-Pierre Vors
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Patent number: 8063045Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.Type: GrantFiled: February 1, 2010Date of Patent: November 22, 2011Assignee: Sanofi-AventisInventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
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Publication number: 20110268903Abstract: Disclosed are methods of attaching biologically active compounds to a solid surface, comprising modifying the solid surface using triazine chloride and attaching the biologically active compound to the triazine moiety.Type: ApplicationFiled: July 11, 2011Publication date: November 3, 2011Applicant: ILLUMINA, INC.Inventors: Chanfeng ZHAO, Igor KOZLOV, Galina STEINBERG-TATMAN
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Publication number: 20110237594Abstract: The present invention relates to heterocyclyl-triazinyl-amino derivatives of formula (I) wherein Het, Y, p, Ra, Rb, X, n, L1 and L2 represent various substituents, their process of preparation, 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, using these compounds or compositions.Type: ApplicationFiled: November 12, 2009Publication date: September 29, 2011Inventors: Christian Beier, Pierre-Yves Coqueron, Ralf Dunkel, Jorg Greul, Marie-Claire Grossjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors
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Publication number: 20110230472Abstract: It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 25, 2009Publication date: September 22, 2011Applicant: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Manami Masuda, Daisuke Taniyama
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Publication number: 20110224434Abstract: The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents.Type: ApplicationFiled: May 16, 2011Publication date: September 15, 2011Applicant: Koronis Phamaceuticals, IncorporatedInventors: Richard Daifuku, Alexander Gall, Dmitri Sergueev, Dina Sologub, Kevin Harris
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Publication number: 20110218188Abstract: The present invention relates to phenyl-pyrimidinyl-amino derivatives of formula (I) wherein Q1 and p, Ra to Rc, L1, Y, L2 and Q2 represent various substituents, their process of preparation, 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, using these compounds or compositions.Type: ApplicationFiled: November 12, 2009Publication date: September 8, 2011Inventors: Christian Beier, Jurgen Benting, Isabelle Christian, Pierre-Yves Coqueron, Peter Dahmen, Ralf Dunkel, Jorg Greul, Marie-Claire Grosjean-Cournoyer, Hiroyuki Hadano, Philippe Rinolfi, Arnd Voerste, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Patent number: 8007546Abstract: The invention relates to a method of increasing the depth of shade of dyed natural or synthetic polyamide fiber materials, which comprises treating the fiber material before, during or after dyeing with a liquor comprising a compound of formula (1) wherein R is halogen, C1-C12alkyl, C5-C24aryl, C6-C36aralkyl, —OR1, or —NR1R2, R1 and R2 being, each independently of the other, hydrogen, C1-C12alkyl unsubstituted or substituted by one or more hydroxy, amino, mercapto, carboxyl, sulfo, C1-C12alkylsulfonyl, C5-C24arylsulfonyl or C6-C36aralkylsulfonyl groups, C5-C24aryl unsubstituted or substituted by one or more hydroxy, amino, carboxyl, sulfo, C1-C12 alkylsulfonyl, C5-C24arylsulfonyl or C6-C36aralkylsulfonyl groups, or C6-C36aralkyl unsubstituted or substituted by one or more hydroxy, amino, carboxyl, sulfo, C1-C12alkylsulfonyl, C5-C24arylsulfonyl or C6-C36aralkylsulfonyl groups, X and Y are, each independently of the other, mercapto, —NR3R4 or —N+R3R4R5A?, wherein R3, R4 and R5 are, each independently of the othType: GrantFiled: November 10, 2004Date of Patent: August 30, 2011Assignee: Huntsman International LLCInventors: Philippe Ouziel, Ulrich Strahm
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Publication number: 20110207736Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: December 22, 2010Publication date: August 25, 2011Inventors: Nathanael S. GRAY, Wenjun Zhou
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Patent number: 8003718Abstract: This invention relates to new polypiperidine compounds of general formula (I) which give different kinds of polymer materials, in particular polyolefins, high stability towards oxidative action and photodegradation. The invention also relates to the processes used to prepare the compounds of formula (I).Type: GrantFiled: June 13, 2008Date of Patent: August 23, 2011Assignee: 3V SIGMA S.p.A.Inventors: Ferruccio Berte', Massimo Magnoni
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Publication number: 20110201602Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: ApplicationFiled: November 22, 2010Publication date: August 18, 2011Applicant: Amgen Inc.Inventors: Stephanie D. GEUNS-MEYER, Brian L. HODOUS, Stuart C. CHAFFEE, Paul TEMPEST, Phillip R. OLIVIERI, Rebecca E. JOHNSON, Brian K. ALBRECHT, Vinod F. PATEL, Victor J. CEE, Joseph L. KIM, Steven BELLON, Xiaotian ZHU, Yuan CHENG, Ning XI, Karina ROMERO, Hanh Nho NGUYEN, Holly L. DEAK
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Publication number: 20110172230Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.Type: ApplicationFiled: August 22, 2007Publication date: July 14, 2011Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
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Publication number: 20110166137Abstract: The present invention relates to substituted naphthalenyl-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted naphthalenyl-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: December 29, 2010Publication date: July 7, 2011Applicant: ArQule, Inc.Inventors: Mark A. Ashwell, Chris Brassard, Audra Dalton, Jason Hill, Robert Nicewonger, David Vensel
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Publication number: 20110152240Abstract: The invention provides compounds that inhibit protein kinase CK2 activity (CK2 activity), and compositions containing such compounds.Type: ApplicationFiled: November 15, 2010Publication date: June 23, 2011Applicant: CYLENE PHARMACEUTICALS, INC.Inventors: Mustapha Haddach, Joe A. Tran, Fabrice Pierre, Collin F. Regan, Nicholas B. Raffaele, Suchitra Ravula, David M. Ryckman
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Patent number: 7964620Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.Type: GrantFiled: September 17, 2008Date of Patent: June 21, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Publication number: 20110144114Abstract: Triazinone derivatives represented by formula (I) wherein: Z, R1, R2, R3, R4, and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I) and their use in therapeutics.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicants: SANOFI-AVENTIS, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Alistair LOCHEAD, Mourad SAADY, Philippe YAICHE
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Patent number: 7960182Abstract: For the separation, removal, isolation, purification, characterization, identification or quantification of Factor VIII, von Willebrand's Factor or a protein that is a analogue of either, an affinity adsorbent is used that is a compound of formula (II) wherein one X is N and the other is N, C—Cl or C—CN; A is a support matrix, optionally linked to the triazine ring by a spacer; Y is O, S or NR2; Z is O, S or N—R3; R2 and R3 are each H, C1-6 alkyl, C1-6 hydroxyalkyl, benzyl or &bgr;-phenylethyl; B and W are each an optionally substituted hydrocarbon linkage containing from 1 to 10 carbon atoms; D is H, OH or a primary amino, secondary amino, tertiary amino, quaternary ammonium, imidazole, guanidino or amidino group; or B-D is —CHCOOH—(CH2)3-4—NH2; and R7 is a group bearing a positive charge at neutral pH.Type: GrantFiled: May 9, 2006Date of Patent: June 14, 2011Assignee: Prometic Biosciences Ltd.Inventors: Jason Richard Betley, Baldev Singh Baines
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Publication number: 20110124649Abstract: Described herein are novel pyrimidine-pyridine compounds, methods of inhibiting methionine aminopeptidase and treating disorders (or symptoms thereof) associated with methionine aminopeptidase, wherein a compound of the invention is administered to a subject.Type: ApplicationFiled: November 10, 2008Publication date: May 26, 2011Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Jun O. Liu, Xiaoyi Hu, Xiaochun Chen, Dawei Ma, Shridhar Bhat
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Publication number: 20110117651Abstract: The subject invention discloses an agent for promoting cell adhesion to a support, comprising a dispirotripiperazine derivative represented by Formula I below or a salt thereof; a method for promoting cell adhesion to a support comprising adding the dispirotripiperazine derivative represented by Formula I below or a salt thereof to a culture medium, or applying the same to a support; and an agonist of a heparin sulfate that comprises the dispirotripiperazine derivative represented by Formula I below or a salt thereof, and that promotes cell adhesion and/or cell growth.Type: ApplicationFiled: June 16, 2009Publication date: May 19, 2011Inventors: Motonari Uesugi, Sayumi Yamazoe
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Publication number: 20110101312Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.Type: ApplicationFiled: December 21, 2009Publication date: May 5, 2011Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Daniel David LeCloux, Kalindi Dogra, Weishi Wu, Adam Fenninmore, Eric Maurice Smith
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Publication number: 20110105508Abstract: A series of heteroaryl-substituted quinoxaline and quinoline derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: ApplicationFiled: December 17, 2008Publication date: May 5, 2011Applicant: UCB PHARMA, S.A.Inventors: Daniel Rees Allen, George Martin Buckley, Roland Bürli, John Richard Davenport, Natasha Kinsella, Christopher James Lock, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Andrew James Ratcliffe, Marianna Dilani Richard, Verity Margaret Sabin, Andrew Sharpe, Laura Jane Tait, Graham John Warrelow, Sophie Caroline Williams
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Publication number: 20110086834Abstract: Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.Type: ApplicationFiled: June 26, 2009Publication date: April 14, 2011Applicant: AMGEN INC.Inventors: Guoqing Chen, Timothy D. Cushing, Paul Faulder, Benjamin Fisher, Xiao He, Kexue Li, Zhihong Li, Wen Liu, Lawrence R. Mcgee, Vatee Pattaropong, Jennifer L. Seganish, Youngshook Shin, Zhulun Wang
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Publication number: 20110086857Abstract: The present invention provides a novel antagonist: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide: or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having unexpected dual CCR-2 and CCR-5 receptor activity. Crystalline forms, metabolites, pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases are also disclosed. The present disclosure also provides processes for preparing compounds of Formula (I) as provided herein, including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide. Compounds that are useful intermediates of the process are also provided herein.Type: ApplicationFiled: October 11, 2010Publication date: April 14, 2011Inventors: Percy H. Carter, Robert J. Cherney, Victor W. Rosso, Jun Li
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Publication number: 20110087022Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a member selected from the group consisting of: wherein E is CH or N, Q is selected from the group consisting of CO, CS, SO, SO2, or C?NR4, and L, X, Z, R2 and R3 are as defined herein.Type: ApplicationFiled: December 9, 2010Publication date: April 14, 2011Inventors: Jun Feng, Stephen L. Gwaltney, II, Jeffrey A. Stafford, Michael B. Wallace, Zhiyuan Zhang