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US 8,309,596 B2Granted
Kallikrein 7 modulators
AssigneeNovartis AG
InventorsStefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
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Abstract
The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
Claims6
A modulator of kallikrein 7 which is a compound of formula
- Or a salt thereof wherein
- R1 is cyano, (C1-8)alkyl, (C2-8)alkenyl, (C2-8)alkynyl, halogen, (C1-8)alkylamino, (C1-8)alkylamino(C1-8)alkyl, (C1-8)alkoxy, or halo(C1-8)alkyl,
- X is CH═CH, NH, N═CH, O or S,
- Y is a group of formula
- wherein
- the N-containing ring system is optionally annelated with (C3-8)cycloalkyl, (C6-18)aryl or heterocyclyl having 5 to 6 ring members and 1 to 4 heteroatoms selected from N, O, S,
- n is 1, 2 or 3,
- R2 is
- (C1-8)alkyl, (C1-8)alkylamino, (C1-8)alkylamino(C1-8)alkyl, di(C1-8)alkylamino(C1-8)alkyl, halo(C1-8)alkyl, (C1-8)alkoxy, (C1-8)alkoxy(C1-8)alkyl, or
- (CH2)m—Z, wherein Z is unsubstituted or substituted (C3-8)cycloalkyl, (C6-18)aryl or heterocyclyl having 5 to 6 ring members and 1 to 4 heteroatoms selected from N, O, S;
- and
- m is 1 or 2,
- R3 is hydrogen, (C1-8)alkyl, (C1-8)alkoxy, (C6-18)aryl or heterocyclyl having 5 to 6 ring members and 1 to 4 heteroatoms selected from N, O, S.
10 more elements
Dependencies are inferred from the claim text.