Plural Chalcogens Bonded Directly To Ring Carbons Of The Five-membered Hetero Ring (e.g., Isatins, Etc.) Patents (Class 548/485)
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Patent number: 9987251Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.Type: GrantFiled: November 21, 2016Date of Patent: June 5, 2018Assignee: Oncternal Therapeutics, Inc.Inventor: Jean-Michel Vernier
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Patent number: 9604927Abstract: Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.Type: GrantFiled: October 7, 2015Date of Patent: March 28, 2017Assignee: Oncternal Therapeutics, Inc.Inventor: Jean-Michel Vernier
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Patent number: 9242934Abstract: The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above ?65° C.Type: GrantFiled: June 12, 2013Date of Patent: January 26, 2016Assignee: BAYER CROPSCIENCE AGInventors: Mark James Ford, Gunter Karig
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Publication number: 20150051260Abstract: Compounds, compositions and methods relating to EWS-FLI1 protein inhibitors are provided. The compounds have utility in the treatment of cancers including the Ewing's sarcoma family of tumors.Type: ApplicationFiled: April 11, 2013Publication date: February 19, 2015Applicant: GEORGETOWN UNIVERSITYInventors: Jeffrey A. Toretsky, Milton Lang Brown, Perrer N. Tosso, Aykut Uren, Yali Kong
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Patent number: 8957225Abstract: Compounds and methods for controlling the surface properties are described. Compounds of the invention can form radicals upon exposure to irradiation, which can then react with nearby molecules to alter the surface properties of various substrates. The invention can provide surfaces that are resistant to dewetting, surfaces that have immobilized molecules such as carbohydrates and polymers immobilized, and surfaces that have metals deposited on the surface. The invention can be utilized in a wide range of application, such as sensors, microreactors, microarrays, electroless deposition of metals, and the like.Type: GrantFiled: March 9, 2012Date of Patent: February 17, 2015Assignee: The Trustees of Columbia University in the City of New YorkInventors: Gregory T. Carroll, Jeffrey T. Koberstein, Denong Wang, Nicholas J. Turro
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Publication number: 20150045562Abstract: The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1?R,3?S)-5,7?-dichloro-6?-fluoro-3?-methyl-2?,3?,4?,9?-tetrahydrospiro[indoline-3,1?-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof.Type: ApplicationFiled: March 22, 2013Publication date: February 12, 2015Applicant: Novartis AGInventors: Michael Crowe, Michael Foulkes, Giancarlo Francese, Dominique Grimler, Ernst Kuesters, Kurt Laumen, Yunzhong Li, Changxue Lin, Jovana Nazor, Thomas Ruch, Derek Smith, Shiwei Song, Shangjun Teng
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Patent number: 8933248Abstract: The present invention relates to expedient method for synthesis of 3-substituted-3-hydroxy-oxindole derivatives, which are useful as synthetic precursors to valuable pharmaceutical compounds. These are synthesized by reacting nitromethane with the corresponding isatins of formula (I). The reaction process of isatins was carried using water as a solvent at room temperature to form the corresponding 3-hydroxy-3-nitromethylindolin-2-ones of formula (II).Type: GrantFiled: June 19, 2013Date of Patent: January 13, 2015Assignee: Council of Scientific & Industrial ResearchInventors: Mandapati Mohan Rao, Parvathaneni Sai Prathima
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Publication number: 20140275075Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.Type: ApplicationFiled: March 13, 2013Publication date: September 18, 2014Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
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Patent number: 8822702Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: GrantFiled: May 2, 2011Date of Patent: September 2, 2014Assignee: BASF SEInventors: Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
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Patent number: 8785627Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methane compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.Type: GrantFiled: August 5, 2013Date of Patent: July 22, 2014Assignee: Abbott Medical Optics Inc.Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
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Patent number: 8710093Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: GrantFiled: April 30, 2012Date of Patent: April 29, 2014Assignee: BASF SE LudwigshafenInventors: Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
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Publication number: 20130345438Abstract: The present invention relates to expedient method for synthesis of 3-substituted-3-hydroxy-oxindole derivatives, which are useful as synthetic precursors to valuable pharmaceutical compounds. These are synthesized by reacting nitromethane with the corresponding isatins of formula (I). The reaction process of isatins was carried using water as a solvent at room temperature to form the corresponding 3-hydroxy-3-nitromethylindolin-2-ones of formula (II).Type: ApplicationFiled: June 19, 2013Publication date: December 26, 2013Inventors: Mandapati Mohan RAO, Parvathaneni Sai PRATHIMA
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Publication number: 20130281711Abstract: The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above ?65° C.Type: ApplicationFiled: June 12, 2013Publication date: October 24, 2013Inventors: Mark James Ford, Gunter Karig
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Publication number: 20130225637Abstract: One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations.Type: ApplicationFiled: February 25, 2013Publication date: August 29, 2013Inventors: David A. Horne, Richard Jove, Christopher Lincoln, Sangkil Nam, Larry Overman, Jun Xie
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Publication number: 20130217884Abstract: An object of the present invention is to provide a novel fungicide having an excellent fungicidal activity. The compound used as the fungicide of the present invention is an ethynylphenylamidine compound or a salt thereof, the compound being represented by Formula (1): wherein R1 and R2 are each hydrogen or C1-12 alkyl, or R1 and R2 may be bonded together to form C1-7 alkylene; R3 is hydrogen or C1-4 alkylthio; R4, R5, R6, and R7 are each hydrogen, halogen, etc.; and R8 is hydrogen, C1-20 alkyl, C3-8 cycloalkyl, C1-4 haloalkyl, phenyl, a heterocyclic group, or —(CH2)n-Si(R9)(R10)(R11) wherein R9, R10, and R11 are each C1-6 alkyl, and n is an integer of 0 or 1.Type: ApplicationFiled: November 2, 2011Publication date: August 22, 2013Applicant: OTSUKA AGRITECHNO CO., LTD.Inventors: Satoru Masumoto, Hitoshi Mutsutani, Sachi Kimura
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Patent number: 8426541Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.Type: GrantFiled: April 9, 2012Date of Patent: April 23, 2013Assignee: Alltech, Inc.Inventors: Alexandros Yiannikouris, Stefan Kwiatkowski, Manoj Bojappa Kudupoje, Clayton Matney
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Patent number: 8343986Abstract: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metalloproteinase enzymes (MMPs).Type: GrantFiled: September 1, 2009Date of Patent: January 1, 2013Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Patent number: 8258175Abstract: A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; R1 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; R2 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; R3 is hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R4-R7, is used to represent groups R4, R5, R6 and R7 which are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, hType: GrantFiled: August 26, 2005Date of Patent: September 4, 2012Assignee: Cancer Research Technology LimitedInventors: Hendrika Maria Gerarda Willems, Per Kallblad, Ian Robert Hardcastle, Roger John Griffin, Bernard Thomas Golding, John Lunec, Martin E. M. Noble, David R. Newell, Alan H. Calvert
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Publication number: 20120220782Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: April 30, 2012Publication date: August 30, 2012Inventors: Ulrich BERENS, Oliver DOSENBACH, Daniel SPRENGER
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Patent number: 8153737Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.Type: GrantFiled: August 27, 2010Date of Patent: April 10, 2012Assignee: Alltech, Inc.Inventors: Alexandros Yiannikouris, Stefan Kwiatkowski, Manoj Bojappa Kudupoje, Clayton Matney
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Publication number: 20120034270Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.Type: ApplicationFiled: October 16, 2009Publication date: February 9, 2012Applicant: Akaal Pharma Pty LtdInventors: Damian W. Grobelny, Gurmit S. Gill
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Publication number: 20110311813Abstract: Nanostructures are formed from alkylated derivatives of aromatic acids of the formula: wherein at least one of R1 to R6 represents a carboxylic acid group, a primary amide group, an ester group, an amidine group, or a salt thereof, at least one other of R1 to R6 is X—Rc, and the remaining of R1 to R6 independently represent H or substituted or unsubstituted organic groups; X represents a linking group; and Rc represents a substituted or unsubstituted alkyl group.Type: ApplicationFiled: June 22, 2010Publication date: December 22, 2011Applicants: NATIONAL RESEARCH COUNCIL OF CANADA, XEROX CORPORATIONInventors: Darren Andrew MAKEIFF, Rina Carlini
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Publication number: 20110286995Abstract: Administering an effective dose of a tTGase inhibitor to a Celiac or dermatitis herpetiformis patient reduces the toxic effects of toxic gluten oligopeptides, thereby attenuating or eliminating the damaging effects of gluten.Type: ApplicationFiled: June 13, 2011Publication date: November 24, 2011Inventors: CHAITAN KHOSLA, KIHANG CHOI
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Patent number: 8058269Abstract: There is provided compounds of the formula wherein R6, V, W, X, Y, Q and n are as described. The compounds exhibit activity as anticancer agents.Type: GrantFiled: September 17, 2007Date of Patent: November 15, 2011Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Song Yang, Jing Zhang, Zhuming Zhang
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Publication number: 20110275645Abstract: The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity.Type: ApplicationFiled: May 5, 2010Publication date: November 10, 2011Inventors: Renee Desai, Ketan Desai
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Publication number: 20110207941Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: May 2, 2011Publication date: August 25, 2011Inventors: ULRICH BERENS, OLIVER DOSENBACH, DANIEL SPRENGER
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Patent number: 7968730Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: GrantFiled: December 7, 2009Date of Patent: June 28, 2011Assignee: BASF SEInventors: Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
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Publication number: 20110130361Abstract: The present invention relates to a novel class of Silicon derivatives. The Silicon compounds can be used to treat cancer. The Silicon 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: ApplicationFiled: August 5, 2008Publication date: June 2, 2011Inventors: Jonathan Grimm, Richard W. Heidebrecht, JR., Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Scott Peterson, Phieng Siliphaivanh, Kevin J. Wilson, David J. Witter
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Publication number: 20110118478Abstract: The present invention relates to processes for the preparation of oxindoles and ortho-substituted anilines and their use as intermediates for syntheses. The invention further relates to a process for the preparation of compounds of formula (4): where a mixture of an aniline (compound of formula Q) is reacted with a thioether (compound of formula W): in the presence of a chlorinating agent and an organic solvent at a reaction temperature in the range above ?65° C.Type: ApplicationFiled: April 28, 2010Publication date: May 19, 2011Applicant: Bayer CropScience AGInventors: Mark James Ford, Gunter Karig
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Publication number: 20110112307Abstract: Solid forms comprising (+)-2-[1-(3-Ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their use are disclosed. The methods include methods of treating and/or preventing disorders ameliorated by the reduction of levels of TNF-? or the inhibition of PDE4.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Inventors: George W. MULLER, Peter H. Schafer, Hon-Wah Man, Chuansheng Ge, Jean Xu
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Patent number: 7915430Abstract: A method of producing a phenolphthalein comprises reacting a phenolic compound of the formula: wherein R1 is a hydrogen or a C1-C12 hydrocarbyl group, with a phthalic anhydride compound of the formula: wherein R2 is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen, in the presence of a heterogeneous catalyst and a promoter to form a reaction mixture comprising a phenolphthalein compound of the formula: wherein each R1 is independently a hydrogen or a C1-C12 hydrocarbyl group, and R2 is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen; wherein the heterogeneous catalyst comprises a metal oxide composition in combination with a porous support, wherein the metal is molybdenum, tungsten, or a combination comprising at least one of the foregoing metals.Type: GrantFiled: September 29, 2008Date of Patent: March 29, 2011Assignee: Sabic Innovative Plastics IP B.V.Inventors: Venkata Rama Narayanan Ganapathy Bhotla, Shivappa Basappa Halligudi, Gurram Kishan, Salkod Parameshwar Mallika, Bhaskar Veldurthy
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Publication number: 20110054132Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.Type: ApplicationFiled: August 27, 2010Publication date: March 3, 2011Applicant: Alltech, Inc.Inventors: Alexandros Yiannikouris, Stefan Kwiatkowski, Manoj Bojappa Kudupoje, Clayton Matney
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Publication number: 20110009379Abstract: [Problems] A compound, which is useful as an active ingredient for a pharmaceutical composition, for example a pharmaceutical composition for treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder, is provided. [Means for Solution] The present inventors have extensively studied compounds having TRPA1 channel activation activity, and confirmed that an indolinone compound has a TRPA1 channel activation activity, and thus completed the present invention. The indolinone compound of the present invention has a TRPA1 channel activation activity and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating constipation-type irritable bowel syndrome, atonic constipation and/or functional gastrointestinal disorder or the like.Type: ApplicationFiled: March 30, 2009Publication date: January 13, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hidetaka Kaku, Tomofumi Takuwa, Michihito Kageyama, Katsura Nozawa, Hitoshi Doihara
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Patent number: 7825155Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: GrantFiled: September 13, 2006Date of Patent: November 2, 2010Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Publication number: 20100197676Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].Type: ApplicationFiled: April 1, 2010Publication date: August 5, 2010Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
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Publication number: 20100184768Abstract: Among other things, the present invention provides novel isoprenyl compounds capable of effectively modulating inflammatory responses and pharmaceutical, cosmetic, cosmeceutical and topical compositions comprising these isoprenyl compounds. Anti-inflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with inflammation. Proinflammatory compounds of the present invention are useful in treating or preventing diseases or conditions associated with suppression of inflammatory responses. Thus, the present invention also provides methods useful in the treatment or prevention of diseases or conditions associated with inflammation as well as methods useful in the treatment or prevention of diseases or conditions associated with suppression of inflammatory responses.Type: ApplicationFiled: November 12, 2009Publication date: July 22, 2010Applicant: SIGNUM BIOSCIENCES, INC.Inventors: Jeffry B. Stock, Maxwell Stock, Keshava Rapole, Seung-Yub Lee, Michael Voronkov, Eduardo Perez, Joel Gordon, Shuyi Chen, Jinglong Chen
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Publication number: 20100167994Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: GEORGETOWN UNIVERSITYInventors: Jeffrey A. Toretsky, Aykut Üren, Milton Lang Brown, Yali Kong
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Publication number: 20100087660Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, or especially of amides of the formula II, wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: ApplicationFiled: December 7, 2009Publication date: April 8, 2010Inventors: ULRICH BERENS, OLIVER DOSENBACH, DANIEL SPRENGER
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Publication number: 20100087505Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.Type: ApplicationFiled: March 14, 2008Publication date: April 8, 2010Applicant: Bracco Imaging S.p.A.Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tziano Tuccinardi
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Publication number: 20100081828Abstract: A method of producing a phenolphthalein comprises reacting a phenolic compound of the formula: wherein R1 is a hydrogen or a C1-C12 hydrocarbyl group, with a phthalic anhydride compound of the formula: wherein R2 is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen, in the presence of a heterogeneous catalyst and a promoter to form a reaction mixture comprising a phenolphthalein compound of the formula: wherein each R1 is independently a hydrogen or a C1-C12 hydrocarbyl group, and R2 is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen; wherein the heterogeneous catalyst comprises a metal oxide composition in combination with a porous support, wherein the metal is molybdenum, tungsten, or a combination comprising at least one of the foregoing metals.Type: ApplicationFiled: September 29, 2008Publication date: April 1, 2010Inventors: Venkata Rama Narayanan Ganapathy BHOTLA, Shivappa Basappa HALLIGUDI, Gurram KISHAN, Salkod Parameshwar MALLIKA, Bhaskar VELDURTHY
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Publication number: 20100081829Abstract: A method for producing a phenolphthalein compound comprises: reacting a phenolic compound of the formula: wherein R1 is a hydrogen or a C1-C12 hydrocarbyl group, with a phthalic anhydride compound of the formula: wherein R2 is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen, in the presence of a heterogeneous catalyst and a promoter to form a reaction mixture comprising a phenolphthalein compound of the formula: wherein each R1 is independently a hydrogen or a C1-C12 hydrocarbyl group; and R2 is a hydrogen, a C1-C12 hydrocarbyl group, or a halogen; wherein the heterogeneous catalyst comprises, on a porous support, a calcination product of a heteropolyacid composition.Type: ApplicationFiled: September 29, 2008Publication date: April 1, 2010Inventors: Venkata Rama Narayanan Ganapathy BHOTLA, Shivappa Basappa HALLIGUDI, Gurram KISHAN, Salkod Parameshwar MALLIKA, Bhaskar VELDURTHY
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Publication number: 20100029699Abstract: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metallproteinase enzymes (MMPs).Type: ApplicationFiled: September 1, 2009Publication date: February 4, 2010Inventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Setphen Paul Watson
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Patent number: 7645886Abstract: The invention relates in a first embodiment to a method for the manufacture of esters of the formula (I), or especially of amides of the formula (II), wherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.Type: GrantFiled: December 12, 2003Date of Patent: January 12, 2010Assignee: Ciba Specialty CorporationInventors: Ulrich Berens, Oliver Dosenbach, Daniel Sprenger
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Publication number: 20100004179Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.Type: ApplicationFiled: June 29, 2009Publication date: January 7, 2010Inventors: Jeffrey A. Toretsky, Aykut Uren, Milton Lang Brown, Yali Kong
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Publication number: 20090291991Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.Type: ApplicationFiled: August 4, 2009Publication date: November 26, 2009Inventors: George W. MULLER, Hon-Wah Man
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Publication number: 20090181971Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: August 13, 2007Publication date: July 16, 2009Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Publication number: 20090182153Abstract: To provide a novel process for producing an optically active allyl compound which is useful as an intermediate raw material for e.g. pharmaceutical products.Type: ApplicationFiled: February 8, 2006Publication date: July 16, 2009Applicant: Nissan Chemical Industries, LTDInventor: Yoshikazu Ootsuka
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Publication number: 20090176851Abstract: The present invention relates to a new use of spiro-hydantoin derivatives of formula (I), or salts, solvates or solvated salts thereof, as well as to new compounds, a process for their preparation and new intermediates used in the preparation thereof, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds in therapy.Type: ApplicationFiled: February 6, 2007Publication date: July 9, 2009Applicant: AstraZeneca ABInventors: Lucy Horoszok, Carmen Leung, Miroslaw Tomaszewski, Christopher Walpole
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Publication number: 20090131398Abstract: Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.Type: ApplicationFiled: September 13, 2006Publication date: May 21, 2009Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Teruhisa Tokunaga, Tsuyoshi Takasaki, Kozo Yoshida, Ryu Nagata
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Patent number: RE45274Abstract: The present invention relates generally to molecularly imprinted polymers (MIPs). In particular, the present invention relates to reusable, ecologically friendly MIPs that can be produced in relatively large quantities, methods of producing the same, and methods of utilizing the same (e.g., to sequester and/or adsorb target compounds (e.g., mycotoxins)). Compositions and methods of the invention find use in a variety of applications including dietary therapeutic, prophylactic, food and beverage processing and manufacture, as well as research, quality control and traceability applications.Type: GrantFiled: April 8, 2014Date of Patent: December 2, 2014Assignee: Alltech, Inc.Inventors: Alexandros Yiannikouris, Stefan Kwiatkowski, Manoj Bojappa Kudupoje, Clayton Matney