Patents Represented by Attorney Lydia T. McNally
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Patent number: 7749698Abstract: Provided are biomarkers for determining the sensitivity of proliferative diseases such as cancer to therapeutic agents, in particular mTOR inhibitors in combination with a cytotoxic agent, in particular a cytotoxic agent which damages or affects the integrity of DNA.Type: GrantFiled: February 22, 2005Date of Patent: July 6, 2010Assignee: Novartis AGInventors: Iwan Beuvink, Anne Boulay, Heidi Lane, Terence O'Reilly, George Thomas
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Patent number: 7569566Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: GrantFiled: April 2, 2008Date of Patent: August 4, 2009Assignee: Novartis AGInventors: Werner Breitenstein, Pascal Furet, Sandra Jacob, Paul W Manley
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Patent number: 7192980Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: September 28, 2004Date of Patent: March 20, 2007Assignee: Novartis AGInventors: Frederick R Kinder, Jr., Kenneth W Bair, Timothy M Ramsey, Michael L Sabio
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Patent number: 7169791Abstract: The invention relates to compounds of formula wherein the substituents R1, R2 and R4 have the meaning as set forth and explained in the description of the invention, to processes for the preparation of these compounds, pharmaceutical compositions containing same, the use thereof optionally in combination with one or more other pharmaceutically active compounds for the therapy of a disease which responds to an inhibition of protein kinase activity, especially a neoplastic disease, in particular leukaemia, and a method for the treatment of such a disease.Type: GrantFiled: July 4, 2003Date of Patent: January 30, 2007Assignee: Novartis AGInventors: Werner Breitenstein, Pascal Furet, Sandra Jacob, Paul William Manley
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Patent number: 7148218Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: September 29, 2004Date of Patent: December 12, 2006Assignee: Novartis AGInventors: Frederick R Kinder, Jr., Kenneth W Bair, Timothy M Ramsey, Michael L Sabio
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Patent number: 7138432Abstract: ?-Amino hydroxamic acid derivative of formula (I), in which R is C2–C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C4-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3–C7-alkenyl or C3–C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasi n) and pulmonary disorders (e.g. emphysema, COPD).Type: GrantFiled: August 7, 2000Date of Patent: November 21, 2006Assignee: Novartis AGInventors: Werner Breitenstein, Kenji Hayakawa, Genji Iwasaki, Takanori Kanazawa, Tatsuhiko Kasaoka, Shinichi Koizumi, Shinichiro Matsunaga, Motowo Nakajima, Junichi Sakaki
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Patent number: 7112611Abstract: The invention relates to ?-amino-N-hydroxy-acetamide derivatives of formula (I), wherein R is di-lower alkyl amino, 1,2,3-triazol-2yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof; to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.Type: GrantFiled: February 8, 2002Date of Patent: September 26, 2006Assignee: Novartis AGInventors: Kenji Hayakawa, Genji Iwasaki, Shinichi Koizumi, Ichiro Umemura
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Patent number: 7091224Abstract: The invention relates to anthranilic acid amide derivatives of formula (I), wherein R1 represents H or lower alkyl, R2 represents H or lower alkyl, R3 represents perfluoro lower alkyl, and X is O or S, or an N-oxide or a tautomer thereof, to salts of such anthranilic acid amides, their N-oxides and their tautomers; processes for the preparation thereof, the application thereof for the treatment of the human or animal body, the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age—related macular degeneration; a method for the treatment of such a disease in animals, especially in humans, and the use of such a compound—alone or in combination with one or more other pharmaceutically active compounds—for the manufacture of a pharmaceutical preparation for the treatment of a neoplastic disease, of retinopathy or age-related macular degeneration.Type: GrantFiled: November 7, 2002Date of Patent: August 15, 2006Assignee: Novartis AGInventors: Guido Bold, Pascal Furet, Paul W Manley
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Patent number: 7091346Abstract: 2-Amino-6-anilino-purine derivatives of the formula 1 in which the symbols are as defined in claim 1 are described. These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and can be used for treatment of hyperproliferative diseases, for example tumour diseases.Type: GrantFiled: October 22, 1996Date of Patent: August 15, 2006Assignee: Novartis AGInventors: Jürg Zimmermann, Hans-Georg Capraro, Patricia Imbach, Pascal Furet
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Patent number: 7067543Abstract: The invention relates to anthranilic acid amide derivatives of formula (I), wherein Ar is represented by the subformula (Ia), wherein Ra represents H or lower alkyl, and R1 represents H or perfluoro lower alkyl, R2 represents H, halogen, C2–C7alkyl, C2–C7alkenyl or lower aklynyl; or Ar is represented by the subformula (Ib) and R1 represents perfluoro lower alkyl, and R2 represents bromo, iodo, C2–C7alkyl, C2–C7alkenyl or lower alkynyl, or R1 represents H, and R2 represents fluoro, bromo, iodo, ethyl, C5–C7alkyl, C2–C7alkenyl or lower alkynyl; to N-oxides and tautomers thereof, and to salts of such anthranilic acid amides, its N-oxides and tautomers; to processes for their preparation; to their application in the treatment of the human or animal body, to the use thereof—alone or in combination with one or more other pharmaceutically active compounds—for the treatment especially of a neoplastic disease, such as a tumor disease, of retinopathy or age-related macular degeneration; to a method for the treatment ofType: GrantFiled: November 7, 2002Date of Patent: June 27, 2006Assignee: Novartis AGInventors: Guido Bold, Pascal Furet, Paul W Manley
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Patent number: 7067551Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: GrantFiled: November 9, 2004Date of Patent: June 27, 2006Assignee: Novartis AGInventors: Stacy W Remiszewski, Kenneth W Bair, Richard W Versace, Lawrence B Perez, Michael A Green, Lidia C Sambucetti, Sushil Sharma
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Patent number: 7002022Abstract: Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R2 is aryl; R2 is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R2 cannot represent 2-phthalimidyl, and in case of Y=SO2 cannot represent 2,1,3-benzothiadiazol-4-yl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.Type: GrantFiled: April 21, 2004Date of Patent: February 21, 2006Assignees: Novartis AG, Schering AktiengesellschaftInventors: Karl-Heinz Altmann, Guido Bold, Pascal Furet, Paul William Manley, Jeanette Marjorie Wood, Stefano Ferrari, Francesco Hofmann, Jürgen Mestan, Andreas Huth, Martin Krüger, Dieter Seidelmann, Andreas Menrad, Martin Haberey, Karl-Heinz Thierauch
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Patent number: 6974875Abstract: The invention relates to a process for the preparation of a substituted alkene of formula (I) wherein R1, R2 and R3 are independently of each other a protecting group for a hydroxy group or hydrogen and R4 is phenyl which is unsubstituted or mono- or disubstituted by alkoxy, which alkene constitutes an intermediate for the preparation of discodermolide and discodermolide analogues.Type: GrantFiled: January 21, 2002Date of Patent: December 13, 2005Assignee: Novartis AGInventors: Guido Koch, Olivier Loiseleur, Gottfried Sedelmeier
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Patent number: 6933290Abstract: Disclosed are derivatives of 2-{[N-(2-amino-3-(heteroaryl or aryl)propionyl)-aminoacyl]-amino}-alkylboronic acid, processes for the preparation of such compounds, pharmaceutical preparations, and the use of such derivatives in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humansType: GrantFiled: May 29, 2002Date of Patent: August 23, 2005Assignee: Novartis AGInventors: Pascal Furet, Vito Guagnano, Patricia Imbach, Marc Lang
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Patent number: 6911440Abstract: The invention relates to the treatment of an inflammatory disease, especially an inflammatory rheumatoid or rheumatic disease, and/or pain with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the specification; as well as to new phthalazine derivatives; processes for the preparation thereof, the application thereof in a process for the treatment of the human or animal body; the use thereof for the treatment of a disease, especially a disease caused by ocular neovascularization, such as age-related macula degeneration or diabetic retinopathy, or other diseases that respond to the inhibition of tyrosine kinases, such as a proliferative disease; a method for the treatment of such disease in mammals; and the use of such a compound for the manufacture of a pharmaceutical preparation for the treatment especially of a disease as mentioned above.Type: GrantFiled: November 26, 2003Date of Patent: June 28, 2005Assignee: Novartis AGInventors: Guido Bold, Janet Dawson King, Jörg Frei, Richard Heng, Paul William Manley, Bernhard Wietfeld, Jeanette Marjorie Wood
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Patent number: 6878720Abstract: Described are compunds of formula (I), wherein W is O or S; X is NR8; Y is CR9R10—(CH2)n wherein R9 and R10 are independently of each other hydrogen or lower alkyl, and n is an integer of from and including 0 to and including 3; or Y is SO2; R1 is aryl; R2 is a bicyclic heteroaryl group comprising one ring nitrogen atom with the exception that R2 cannot represent 2-phthalimidyl; any of R3, R4, R5 and R6, independently of the other, is H or a substituent other than hydrogen; and R7 and R8, independently of each other, are H or lower alkyl; or a N-oxide or a pharmaceutically acceptable salt thereof for the preparation of a pharmaceutical product for the treatment of a neoplastic disease which responds to an inhibition of the VEGF receptor tyrosine kinase activity. The compounds of formula (I) can be used for the treatment e.g. of a neoplastic disease, such as a tumor disease, of retinopathy and age-related macular degeneration.Type: GrantFiled: June 26, 2002Date of Patent: April 12, 2005Assignees: Novartis AG, Schering AktiengesellschaftInventors: Karl-Heinz Altmann, Guido Bold, Pascal Furet, Paul William Manley, Jeanette Marjorie Wood, Stefano Ferrari, Francesco Hofmann, Jürgen Mestan, Andreas Huth, Martin Krüger, Dieter Seidelmann, Andreas Menrad, Martin Haberey, Karl-Heinz Thierauch
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Patent number: 6858404Abstract: Nucleic acid molecules are isolated from Sorangium cellulosum that encode polypeptides necessary for the biosynthesis of epothilone. Disclosed are methods for the production of epothilone in recombinant hosts transformed with the genes of the invention. In this manner, epothilone can be produced in quantities large enough to enable their purification and use in pharmaceutical formulations such as those for the treatment of cancer.Type: GrantFiled: November 13, 2001Date of Patent: February 22, 2005Assignee: Novartis AGInventors: Thomas Schupp, James Madison Ligon, Istvan Molnar, Ross Zirkle, Devon Dawn Cyr, Jörn Görlach
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Patent number: 6833367Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B and C are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: November 12, 2002Date of Patent: December 21, 2004Assignee: Novartis ACInventors: Frederick R. Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6833384Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: GrantFiled: November 19, 2002Date of Patent: December 21, 2004Assignee: Novartis AGInventors: Stacy William Remiszewski, Kenneth Walter Bair, Richard William Versace, Lawrence Blas Perez, Michael Alan Green, Lidia Cristina Sambucetti, Sushil Sharma
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Patent number: 6818661Abstract: The invention relates to substituted anthranylalkyl and cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.Type: GrantFiled: May 9, 2003Date of Patent: November 16, 2004Assignee: Novartis AGInventors: Dieter Seidelmann, Martin Krüger, Eckhard Ottow, Andreas Huth, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey