Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
Type:
Grant
Filed:
November 3, 2005
Date of Patent:
June 12, 2012
Assignee:
Novartis AG
Inventors:
Pascale Hoehn, Bernd Koch, Michael Mutz
Abstract: The present invention relates to the use of the combination of tyrosine phosphate inhibitors AMN107 and PKC412 for the preparation of a drug for the treatment of a mast cell-related proliferative disease. The present invention is also drawn to a combination treatment of a tyrosine phosphate inhibitor and a TK-inhibitor that is effective against a mast cell-related proliferative disease, including especially systemic mastocytosis (SM) including aggressive SM (ASM) and mast cell leukemia (MCL).
Abstract: The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.
Type:
Grant
Filed:
August 28, 2009
Date of Patent:
August 30, 2011
Assignee:
Novartis AG
Inventors:
TianLing Chen, Diane Greeley, John David Rothermel, Markus Wartmann, Jeanette Marjorie Wood
Abstract: The present invention relates to the use of staurosporines derivatives for the preparation of a drug for the treatment of diseases involving deregulated FLT3 receptor tyrosine kinase activity, especially for the curative and/or prophylactic treatment of leukemias and myelodysplastic syndromes, and to a method of treating diseases involving deregulated FLT3 receptor tyrosine kinase activity.
Type:
Grant
Filed:
October 29, 2002
Date of Patent:
July 5, 2011
Assignees:
Novartis AG, Dana-Farber Cancer Institute Inc
Inventors:
James Douglas Griffin, Paul William Manley
Abstract: This invention relates to staurosporine derivatives are effective when used in combination with ionizing radiation for the delay of progression or treatment of a proliferative disease, especially a disease associated with a PAX/FKHR translocation including a PAX3/FKHR translocation and a PAX7/FKHR translocation, more especially a solid tumor disease such as a Sarcoma, most especially an Alveolar Rhabdomyosarcoma.
Type:
Grant
Filed:
November 13, 2006
Date of Patent:
July 5, 2011
Assignee:
University of Zurich
Inventors:
Marco Wachtel, Beat W. Schäfer, Ralf Amstutz
Abstract: 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:
Grant
Filed:
June 22, 2009
Date of Patent:
June 7, 2011
Assignee:
Novartis AG
Inventors:
Werner Breitenstein, Pascal Furet, Sandra Jacob, Paul W Manley
Abstract: The invention relates to the F-crystal form, G-crystal form, H-crystal form, I-crystal form and K-crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide, certain processes for their preparation, pharmaceutical compositions containing these crystal forms, their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.
Abstract: The present invention pertains to a combination for simultaneous, separate or sequential use which comprises (a) a cyclin-dependent kinase inhibitor and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide and to its use for the treatment of cancer, especially of Bcr/Abl+ leukemia resistant to compound of formula I.
Type:
Grant
Filed:
April 4, 2003
Date of Patent:
February 15, 2011
Assignees:
The United States of America as represented by the Department of Veterans Affairs, Virginia Commonwealth University
Inventors:
Paul Dent, Steven Grant, Geoffrey Krystal, Chunrong Yu
Abstract: The invention relates to the delta and epsilon crystal form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)pyrimidin-2 -ylamino)phenyl]-benzamide (the compound of formula I, see below), certain processes for their preparation, pharmaceutical compositions containing these crystal forms, and their use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, and their use as an intermediate or for the preparation of pharmaceutical preparations for use in diagnostic methods or for the therapeutic treatment of warm-blooded animals, especially humans.
Abstract: The invention relates to the treatment of a proliferative disease, especially according to certain treatment regimens, with an epothilone, especially with epothilone A and more preferably epothilone B; as well as to the treatment of certain cancers with such an epothilone.
Type:
Grant
Filed:
April 19, 2006
Date of Patent:
January 25, 2011
Assignee:
Novartis AG
Inventors:
Terence O'Reilly, Markus Wartmann, Manuel Litchman, Pamela Cohen
Abstract: The invention relates to a pharmaceutical combination which comprises (a) a vasculostatic compound, (b) an alkylating agent and (c) optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use for the treatment of a tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a tumor disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.
Abstract: The present invention relates to a combination comprising N-{5-[4-(4-methyl-piperazino-methyl) -benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine and an epothiione derivative; pharmaceutical composition comprising said combination; method of treatment comprising said combination; and commercial packages comprising said combination.
Type:
Grant
Filed:
February 26, 2002
Date of Patent:
May 25, 2010
Assignee:
Novartis AG
Inventors:
Ralf Brandt, Elisabeth Buchdunger, Carl-Henrik Heldin, Arne Östman, Kristian Pietras, Terence O'Reilly, John D Rothermel, Peter Traxler, Markus Wartmann
Abstract: The invention relates to a combination which comprises (a) a bisphosphonate, a platinum compound or a vasculostatic compound and (b) an epothilone derivative of formula I wherein A represents O or NRN, wherein RN is hydrogen or lower alkyl, R is hydrogen or lower alkyl, and Z is O or a bond, in which the active ingredients (a) and (b) are present in each case in free form or in the form of a pharmaceutically acceptable salt and optionally at least one pharmaceutically acceptable carrier for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition, a commercial package or product comprising such a combination; the use of such a combination for the preparation of a medicament for the delay of progression or treatment of a proliferative disease and to a method of treatment of a warm-blooded animal.
Type:
Grant
Filed:
January 24, 2008
Date of Patent:
November 3, 2009
Assignee:
Novartis AG
Inventors:
John David Rothermel, Markus Wartmann, Jeanette Marjorie Wood
Abstract: The invention relates to a desorption process for epothilones, especially epothilone A and/or epothilone B, from resins and new production, work-up or purification processes or manufacturing methods for epothilones comprising said desorption process, as well as the use of certain solvents for the desorption of epothilones from resins.
Abstract: The invention relates to N-phenyl-2-pyrimidine-amine derivatives in which at least one nitrogen atom carries an oxygen atom to form the corresponding N-oxides, to processes for the preparation thereof, to pharmaceutical compositions comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.
Type:
Grant
Filed:
January 22, 2003
Date of Patent:
July 7, 2009
Assignee:
Novartis AG
Inventors:
Klaus Olaf Börnsen, Peter End, Gerhard Gross, Ulrike Pfaar, Paul William Manley, Jürg Zimmermann
Abstract: The invention relates to a new crystalline form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide of formula 1, which may be used for example for tumour therapy.
Type:
Grant
Filed:
September 5, 2006
Date of Patent:
June 9, 2009
Assignee:
Novartis AG
Inventors:
Jürg Zimmermann, Bertrand Sutter, Hans M Bürger