Novartis Ag

Schering Aktiengesellschaft

Other

Stefano Ferrari

Pascal Furet

Andreas Huth

Paul William Manley

Guido Bold

Dieter Seidelmann

Karl-Heinz Thierauch

Andreas Menrad

Jeanette Marjorie Wood

Martin Haberey

Karl-Heinz Altmann

Jürgen Mestan

Martin Krüger

Francesco Hofmann

Eckhard Ottow

Michael Schirner

Martin Kr&uuml;ger

J&uuml;rgen Mestan

Jose Brüggen

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

Described are compounds of formula (I), wherein W is O or S; X is NR ; Y is CR R &mdash;(CH )n wherein R and R 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 S0 ; R is aryl; R is a mono- or bicyclic heteroaryl group comprising one or more ring nitrogen atoms with the exception that R cannot represent 2-phthalimidyl, and in case of Y&equals;SO cannot represent 2,1,3-benzothiadiazol-4-yl; any of R , R , R and R , independently of the other, is H or a substituent other than hydrogen; and R and 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.

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Muttenz, Switzerland

Stefano Ferrari