Novartis Ag

Schering Aktiengesellschaft

University of Texas System

Ciba-geigy Corporation

Novartis Corporation

Gsf-international Research Institute for Environment and Health

Novartis Pharma Gmbh

Jürgen Mestan

Paul William Manley

Guido Bold

Doriano Fabbro

Pascal Furet

Andreas Huth

Dieter Seidelmann

Shripad S Bhagwat

Marc Lang

Karl-Heinz Thierauch

Hans-Georg Capraro

Andreas Menrad

Satish Chandra Khanna

Jeanette Marjorie Wood

Alexander Fassler

Martin Krüger

Stefano Ferrari

Janis Karlis Lazdins

Martin Haberey

Michael Hallek

Karl-Heinz Altmann

Markus Warmuth

Moshe Talpaz

Nicholas J Donato

Francesco Hofmann

Ji Wu

Eckhard Ottow

Michael Schirner

Leila Alland

Jose Brüggen

The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of systemic mastocytosis.

Pyrimidylaminobenzamide derivatives for systemic mastocytosis

The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine or the monomethanesulfonate salt thereof; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukaemia, especially chronic myelogenous leukaemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, alone or in combination with a Bcr-Abl inhibitor, in particular N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine.

Use of c-Src inhibitors alone or in combination with STI571 for the treatment of leukaemia

The present invention relates to the use of pyrimidylaminobenzamide derivatives for the preparation of a drug for the treatment of FIP1L1-PDGFR&#x3b1;-induced or TEL-PDGFR&#x3b2;-induced myeloproliferative diseases, especially for the curative and/or prophylactic treatment of hypereosinophilic syndrome and hypereosinophilic syndrome with resistance to imatinib, and to a method of treating hypereosinophilic syndrome, chronic eosinophilic leukemia and hypereosinophilic syndrome with resistance to imatinib, or other diseases associated with FIP1L1-PDGFR&#x3b1;, TEL-PDGFR&#x3b2; or similar mutations that activate PDGFR.

Pyrimidylaminobenzamide derivatives for hypereosinophilic syndrome

The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.

Anthranilic acid amides and the use thereof as medicaments

Described are compunds of formula (I), wherein W is O or S; X is NR; Y is CRR&#x2014;(CH)n wherein Rand Rare 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 SO; Ris aryl; Ris a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that Rcannot represent 2-phthalimidyl, and in case of Y=SOcannot represent 2,1,3-benzothiadiazol-4-yl; any of R, R, Rand R, independently of the other, is H or a substituent other than hydrogen; and Rand R, 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.

N-Aryl (thio) anthranilic acid amide derivatives, their preparation and their use as VEGF

Described are compunds of formula (I), wherein W is O or S; X is NR; Y is CRR&#x2014;(CH)n wherein Rand Rare 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 SO; Ris aryl; Ris a bicyclic heteroaryl group comprising one ring nitrogen atom with the exception that Rcannot represent 2-phthalimidyl; any of R, R, Rand R, independently of the other, is H or a substituent other than hydrogen; and Rand R, 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.

VEGF receptor tyrosine kinase inhibitors

Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.1 is an acyl radical lower-alkoxy-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amino, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl;

Antiviral ethers of aspartate protease substrate isosteres

Antiretroviral compounds (which are effective, for example, against HIV) of the formula I ##STR1## in which R.sub.1 is an acyl radical lower-alkoxyl-lower-alkanoyl whose lower alkoxy radical is unsubstituted or is substituted by halogen, phenyl, lower alkoxy or a heterocyclic radical selected from piperidinyl, pyrrolidinyl, tetrahydropyranyl, tetrahydrofuranyl, thiazolidinyl, thiazolyl, indolyl or 4H-1-benzopyranyl which is unsubstituted or substituted by oxo, hydroxyl, amine, lower alkyl, lower-alkoxycarbonyl and/or phenyl-lower-alkoxycarbonyl; lower alkanoyl which is unsubstituted or is substituted by one of the said unsubstituted or substituted heterocyclic radicals; arylcarbonyl or heterocyclylcarbonyl which are substituted by heterocyclyl or heterocyclyl-lower-alkyl; phenyl-lower-alkanoyl which is substituted by hydroxyl and lower alkyl; or arylsulfonyl; or the residue of an amino acid which is defined in accordance with the description (and which may be acylated on the amino nitrogen by one of the abovementioned acyl radicals);

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Denzlingen, Germany

Jürgen Mestan