Abstract: The present invention provides a synthesis for the preparation of epothilone derivatives of formula 9 wherein R1 is methyl, and R2 is an unsubstituted or substituted aryl; an unsubstituted or substituted heteroaryl; or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus; and salts thereof, and intermediates for the synthesis of a compound of formula 9.
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 tumor therapy.
Type:
Grant
Filed:
July 16, 1998
Date of Patent:
May 17, 2005
Assignee:
Novartis AG
Inventors:
Jürg Zimmermann, Bertrand Sutter, Hans Michael Bürger
Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
Type:
Grant
Filed:
November 19, 2002
Date of Patent:
December 21, 2004
Assignee:
Novartis AG
Inventors:
Stacy William Remiszewski, Kenneth Walter Bair, Richard William Versace, Lawrence Blas Perez, Michael Alan Green, Lidia Cristina Sambucetti, Sushil Sharma
Abstract: 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:
Grant
Filed:
May 9, 2003
Date of Patent:
November 16, 2004
Assignee:
Novartis AG
Inventors:
Dieter Seidelmann, Martin Krüger, Eckhard Ottow, Andreas Huth, Karl-Heinz Thierauch, Andreas Menrad, Martin Haberey
Abstract: The present invention relates to methods for treating multidrug resistant cells, preferably multidrug resistant cancer cells with discodermolide. Discodermolide is found to be effective in limiting the growth of otherwise growth unregulated cells having tubulin mutations and in promoting phosphorylation of the oncogene RAF-1.
Type:
Grant
Filed:
April 10, 2003
Date of Patent:
August 10, 2004
Assignee:
Novartis AG
Inventors:
Peter Lassota, Christopher Turchik Jagoe
Abstract: This application discloses 2-amino-6-anilino-purine derivatives of the formula I
in which
q is 1-5, and
R1 is
&agr;) —S(═O)k—NR6R7, in which
k is 1 or 2,
wherein under the proviso that R6 and R7 cannot be simultaneously hydrogen
&agr;1) R6, R7 can be identical or different from one another and represent an aliphatic, carbocyclic, heterocyclic, carbocyclic-aliphatic or heterocyclic-aliphatic radical; hydrogen or lower aliphatic acyl; or
&agr;2) R6 and R7 together are an alkylene or alkenylene radical having from 3 up to and including 9 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen,
&bgr;) N-(aryl lower alkyl)carbamoyl, or
&ggr;) a radical of the formula —NH—S(═O)i—R8, in which
i is 1 or 2,
R8 is an aliphatic, carbocyclic or heterocyclic radical; or
&dgr;) a radical of the formula —NH—C(═O)—R9,
and the other variable substituents are as defined herein.
Type:
Grant
Filed:
August 10, 2001
Date of Patent:
July 27, 2004
Assignee:
Novartis AG
Inventors:
Patricia Imbach, Hans-Georg Capraro, Jürg Zimmermann, Giorgio Caravatti, Pascal Furet, Wolfgang Karl-Diether Brill
Abstract: There are provided membrane-associated polypeptides having the sequence shown in SEQ ID Nos. 1 and 9. Also provided are immunogenic determinants derived from said polypeptides and antibodies raised thereto. The polypeptides, their derived antigenic determinants and the antibodies are useful for the diagnosis and treatment of metastatic potential in tumors.
Abstract: The invention relates to pyridine derivatives of formula I:
wherein the substituents and symbols are defined as indicated in the description, processes for the preparation thereof, their usage in the preparation of a pharmaceutical composition for the treatment of a disease which responds to an inhibition of angiogenesis, and pharmaceutical compositions containing such compounds.
Abstract: Pharmaceutical formulations comprising an epothilone in the form of an infusion concentrate or a lyophilised composition, and methods of administration of an epothilone in suitable form for parenteral administration.
Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.
Type:
Grant
Filed:
January 29, 2002
Date of Patent:
December 2, 2003
Assignee:
Novartis AG
Inventors:
Hans Hofmann, Marion Mahnke, Klaus Memmert, Frank Petersen, Thomas Schupp, Ernst Küsters, Michael Mutz
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:
August 9, 2001
Date of Patent:
October 21, 2003
Assignee:
Novartis AG
Inventors:
Terence O'Reilly, Markus Wartmann, Manuel Litchman, Pamela Cohen
Abstract: The invention relates to the use of 2 amino-nicotinamide derivatives of formula I
wherein n is from 1 up to and including 6;
W is O or S;
R1 and R3 represent independently of each other hydrogen, lower alkyl or lower acyl;
R2 represents a cycloalkyl group, an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted;
R and R′ are independently of each other hydrogen or lower alkyl;
X represents an aryl group, or a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms and 0, 1 or 2 heteroatoms independently from each other selected from the group consisting of oxygen and sulfur, which groups in each case are unsubstituted or mono- or polysubstituted;
or a N-oxide, a possible tautomer thereof or a pharmaceutically acceptable salt of such a
Abstract: A novel crystal form of ,&agr;-dimethyl-4-{1-hydroxy-4-{4-(hydroxydiphenylmethyl)-1-piperidinyl}butyl}benzeneacetic acid hydrochloride, processes for its preparation and its pharmaceutical use are disclosed.
Abstract: Disclosed are compounds of the formula
in free or salt form, wherein X, R1, R2, R3, and R4 are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of inflammatory or obstructive airways disease.
Type:
Grant
Filed:
March 19, 2002
Date of Patent:
July 8, 2003
Assignee:
Novartis AG
Inventors:
Stephen Paul Collingwood, Judy Hayler, Darren Mark Le Grand, Henri Mattes, Keith Allan Menear, Clive Victor Walker, Xiao-Ling Cockcroft
Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
Type:
Grant
Filed:
August 31, 2001
Date of Patent:
April 22, 2003
Assignee:
Novartis AG
Inventors:
Stacy William Remiszewski, Kenneth Walter Bair, Richard William Versace, Lawrence Blas Perez, Michael Alan Green, Lidia Cristina Sambucetti, Sushil Sharma
Abstract: The invention provides Drosophila melanogaster p70S6K, as well as nucleic acids encoding this kinase. The sequence of Drosophila p70S6K and the gene encoding it are represented in SEQ ID No. 2 and 1 respectively. The invention moreover provides mutated forms of Drosophila p70S6K, including constitutively active and dominant negative forms thereof, which are useful in the study of p70S6K activity. Furthermore, the invention provides expression systems which produce Drosophila p70S6K in Drosophila and other organisms, and in particular systems in which expression of Drosophila p70S6K has been modulated so as to facilitate the study of its activity.
Type:
Grant
Filed:
March 26, 2001
Date of Patent:
March 18, 2003
Assignee:
Novartis AG
Inventors:
Mary Stewart, Sara Kozma, George Thomas
Abstract: A process is presented for producing spherical particles containing microorganism cells having desired enzyme activity. The process comprises the steps of mixing the cells directly with a primary or secondary amine-containing polymer, combining the resulting mixture with an organic solvent to form a two-phase system, and then adding a bifunctional cross-linking agent to yield the spherical particles. The preferred enzyme activities are D-amino acid oxidase and glutarylacylase activities.
Type:
Grant
Filed:
April 3, 2000
Date of Patent:
October 15, 2002
Assignee:
Biochemie Gesellschaft m.b.H.
Inventors:
Arno Reichert, Waander Riethorst, Franz Knauseder, Norbert Palma
Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.
Type:
Grant
Filed:
July 12, 2000
Date of Patent:
October 1, 2002
Assignee:
Geneva Pharmaceuticals, Inc.
Inventors:
Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
Abstract: Described are compounds 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 S02; R1 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.
Inventors:
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