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

US7002022B2 · kind B2 · utility

Assignees

• Novartis AG · CH
• SCHERING CORPORATION · US

Inventors

• Karl-Heinz Altmann · Reinach, CH
• Guido Bold · Gipf-Oberfrick, CH
• Pascal Furet · Basel, CH
• Paul W. Manley · Arlesheim, CH
• Jeanette Marjorie Wood · Biel-Benken, CH
• Stefano Ferrari · Muttenz, CH
• Francesco Hofmann · Bottmingen, CH
• Jurgen Mestan · Denzlingen, DE
• Andreas Huth · Berlin, DE
• Martin Kruger · Berlin, DE
• Dieter Seidelmann · Berlin, DE
• Andreas Menrad · Berlin, DE
• Martin Haberey · Berlin, DE
• Karl-Heinz Thierauch · Berlin, DE

Key dates

• Filing date: Apr 21, 2004
• Grant date: Feb 21, 2006
• Expiry date: Apr 21, 2024

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D405/12
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.