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N - ((6-amino-pyridin-3-yl) methyl) -heteroaryl-carboxamides as inhibitors of plasma kallikrein
专利权人:
NOVARTIS AG
发明人:
BRANDL, TRIXI,FLOHR, STEFANIE,KOPEC, SEBASTIAN,LACHAL, JULIE,MARKERT, CHRISTIAN,NAMOTO, KENJI,NGANGA, PERLE,PIRARD, BERNARD,RENATUS, MARTIN,SEDRANI, RICHARD,ZOLLER, THOMAS
申请号:
ES11745519
公开号:
ES2542764T3
申请日:
2011.08.03
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of the formula I ** Formula ** wherein R1 is hydrogen; halogen; cyano; nitro; hydroxy; Not me; -C (O) H; -C (O) OH; -C (O) NH2; C1-6 alkyl; C1-6 halogenoalkyl; C1-6 hydroxyalkyl; C1-4-C1-6 alkoxy; C1-6 aminoalkyl; C2-6 alkenyl; C2-6 halogenoalkenyl; C2-6 alkynyl; C2-6 halogenoalkynyl; C1-6 alkoxy; C1-6 halogenoalkoxy; C1-4 alkoxy-C1-6 alkoxy; C1-6 alkylamino; di (C1-6 alkyl) amino; or C3-7 cycloalkyl, where a carbon atom can be replaced by an oxygen atom, where the C3-7 cycloalkyl can be attached directly to the pyridine ring or through a C1-2 alkylene or an oxygen, and in where C3-7 cycloalkyl can be substituted once or more than once by halogen, C1-4 alkyl or C1-4 alkoxy; R2 is hydrogen or fluoro; R3 is hydrogen; halogen; cyano; nitro; hydroxy; Not me; -C (O) H; -C (O) OH; -C (O) NH2; or -X1-R6; X1 is selected from the link; carbonyl; oxygen; sulfur; -SW)-; -S (O) 2-; amino, which can be substituted by C1-4 alkyl; -NH-C (O) -; - C (O) -NH-; -NH-S (O) 2-; and -S (O) 2-NH-; R6 is C1-6 alkyl; C1-6 halogenoalkyl; C1-6 cyanoalkyl; C1-6 carboxyalkyl; C1-6 hydroxyalkyl; C1-4-C1-6 alkoxy; C1-4 C1-4 alkoxy C1-6 alkoxy; C1-4 alkylcarbonyl-C1-6 alkyl; C1-4 alkoxycarbonyl-C1-6 alkyl; C1-4 alkylcarbonyloxy-C1-6 alkyl; C1-6 aminoalkyl; C1-4 alkylamino-C1-6 alkyl; di (C1-4 alkyl) amino-C1-6 alkyl; aminocarbonyl-C1-6 alkyl; C1-4 alkylaminocarbonyl-C1-6 alkyl; di (C1-4 alkyl) aminocarbonyl-C1-6 alkyl; C1-4 alkylcarbonylamino-C1-6 alkyl; C 1-4 alkylaminosulfonyl-C 1-6 alkyl; di (C1-4 alkyl) aminosulfonyl-C1-6 alkyl; C2-6 alkenyl; C2-6 halogenoalkenyl; C2-6 alkynyl; C2-6 halogenoalkynyl; or R6 is a three to seven membered monocyclic ring system that may be aromatic, saturated or unsaturated unsaturated and may contain 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, where the ring system may contain no more of 2 oxygen atoms and not more than 2 sulfur atoms, where the ring system can be attached directly to the group X1 or through a C1-2 alkylene, where the r
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