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carboxamide compounds and their use as calpain inhibitors
专利权人:
ABBOTT LABORATORIES;ABBOTT GMBH & CO KG
发明人:
ACHIM MÖLLER,ANDREAS KLING,GISELA BACKFISCH,HELMUT MACK,KATJA JANTOS,MARJOLEEN NIJSEN,WILFRIED HORNBERGER,YANBIN LAO
申请号:
BR112012015659
公开号:
BR112012015659A2
申请日:
2010.12.21
申请国别(地区):
BR
年份:
2016
代理人:
摘要:
carboxamide compounds and their use as calpain inhibitors. The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. carboxamide compounds are calpain inhibitors (calcium dependent cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for the treatment of a disorder associated with high calpain activity. carboxamide compounds are compounds of the general formula i wherein r ^ 1 ^, r ^ 2 ^, r ^ 3 ^, r ^ 4 ^, r ^ 5 ^ and m have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically acceptable salts thereof. Of these compounds, those wherein R 1 is R 2 is phenyl-C 1 -C 2 -alkyl or optionally substituted Hetaryl C 1 -C 2 alkyl, R 2 is optionally substituted aryl are preferred. , hetaryl, aryl-C 1-6-C 6 -alkyl, aryl-C 2-2-C 6 -alkenyl or heraryl-C 1-4 C-alkyl, R 3 is C 1-1 -C 3 alkyl, C 1-1 C 3 alkyl, R 4 and R 5, independently of each other, are halogen, C 3-3, C H 2 O 2. ch 2 -f, c-1-c-2-alkyl or c-1-c-2-alkoxy, but independently of each other are 0 or 1.compostos de carboxamida e seu uso como inibidores de calpaína. a presente invenção refere-se a novos compostos de carboxamida e seu uso para a fabricação de um medicamento. os compostos de carboxamida são inibidores de calpaína (proteases de cisteína dependentes de cálcio). a invenção, portanto, também se refere á utilização destes compostos de carboxamida para o tratamento de um distúrbio associado a uma elevada atividade de calpaína. os compostos de carboxamida são compostoes da fórmula geral i em que r^ 1^, r^ 2^, r^ 3^, r^ 4^, r^ 5^, m e n tem os significados mencionados nas reivindicações e a descrição, os tautômeros do mesmos, os hidratos dos mesmos e os sais farmaceuticamente aceitáveis dos mesmos. destes compostos, são preferidos aqueles em que r^ 1^ é fenil-c~ 1~-c~ 2~-alquila ou hetaril-c~ 1~-c~ 2~alquila opcionalmente substituído, r^ 2^ é
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