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US 6,855,715 B1Granted
Serine protease inhibitors
AssigneeEli Lilly and Company
InventorsJohn Walter Liebeschuetz, Amanda Jane Lyons, Christopher William Murray, Andrew David Rimmer, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, Phillip John Morgan, Simon James Richards, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
Claims13
A compound of formula (I)
- where R2 represents
- (i) phenyl optionally being substituted in the 3 and/or 4 position by halo, nitro, thiol, haloalkoxy, hydrazido, alkylhydrazido, amino, haloalkyl, alkylthio, alkenyl, alkynyl, acylamino, tri or difluoromethoxy, carboxy, acyloxy, MeSO2— or R1, and optionally substituted at the 6 position by amino, hydroxy, halo, alkyl, carboxy, alkoxycarbonyl, cyano, amido, aminoalkyl, alkoxy or alkylthio;
- or
- (ii) naphth-2-yl optionally substituted at the 6 or 7 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1j and optionally substituted at the 3 position by amino, hydroxy, halo, alkyl, carboxy, cyano, amido, aminoalkyl, alkoxy or alkylthio;
- —X—X— is CONH;
- R1j represents hydrogen or hydroxyl, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, alkoxyalkyl, alkoxycarbonyl, alkylaminocarbonyl, alkoxycarbonylamino, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl or cycloalkyl;
- R1 is as defined for R1j, provided that R1 is not unsubstituted aminoalkyl;
- L is CO;
- Y is a CH group;
- Cy is a saturated or unsaturated, mono or poly cyclic, homocyclic group optionally substituted by groups R3a or phenyl optionally substituted by R3a;
- each R3a independently is R1c, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, triazolyl, imidazolyl, tetrazolyl, hydrazido, alkyl iymidazolyl, thiazolyl, alkyl thiazolyl, alkyl oxazolyl, oxazolyl, alkylsulphonamido, alkylaminosulphonyl, aminosulphonyl, haloalkoxy and haloalkyl;
- Lp(D)n is a lipophilic organic group selected from
- wherein R3 is as defined for R3a;
- R4 represents hydrogen, (CH2)wCOOH or (CH2)wCONH2;
- w represents an integer from 0 to 4;
- and
- when X is in the ring bonded to L, X is N and, otherwise X represents CH or N;
- and
- R1c is as defined for R1j, or a physioloqically tolerable salt thereof.
16 more elements
Dependencies are inferred from the claim text.