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US 2003/0216403 A1Published application
Serine protease inhibitors
AssigneeTularik Inc.
InventorsSarah Elizabeth Lively, Bohdan Waszkowycz, Martin James Harrison, Christopher Neil Farthing, Keith Michael Johnson
Life of this patent
Estimating the term…
Abstract
1 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.
Claims36
A tryptase inhibitor compound of formula (I)
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- where:
- R5 represents amino, hydroxy, aminomethyl, hydroxymethyl or hydrogen;
- R6a represents hydrogen or methyl;
- X—X is selected from —CH═CH—, —CONR1a—, —NH—CO—, —NR1a, —CH2—, —CH2—NR1a—, —CH2O—, —OCH2—, —COO—, —OC═O— and —CH2CH2—;
- R1a represents hydrogen, (1-6C)alkyl or phenyl(1-6C)alkyl;
- L is CO or CONR1d(CH2)m in which m is 0 or 1 and R1d is hydrogen, (1-6C)alkyl or phenyl(1-6C)alkyl;
- Cy is cycloalkyl, piperidinyl, 3,4-methylenedioxyphenyl, furyl, thienyl, imidazolyl, oxazolyl, thiazolyl, pyridyl, pyrimidinyl, pyrazinyl, naphthyl, benzofuryl or benzo[b]thienyl group, optionally substituted by R3a or R3iXi in which Xi is a bond, O, NH, CO, CONH, NHCO, SO2, NHSO2 or SO2NH, CH2 and R3i is phenyl or pyridyl optionally substituted by R3a;
- each R3a independently is hydrogen, hydroxyl, (1-6C)alkoxy, (1-6C)alkyl, (2-6C)alkenyl, (2-6C)alkynyl, (1-6C)alkanoyl, (1-6C) alkylaminoalkyl, hydroxy(1-6C)alkyl, carboxy, (1-6C)alkoxyalkyl, (1-6C)alkoxycarbonyl, (1-6C)alkylaminocarbonyl, amino(1-6C)alkyl CONH2, CH2CONH2, aminoacetyl, (1-6C)alkanoylamino, hydroxy(1-6C)alkanoylamino, amino(1-6C)alkanoylamino, (1-6C)alkylamino(1-6C)alkanoylamino, di(1-6C)alkylamino(1-6C)alkanoylamino, (1-6C)alkoxycarbonylamino, amino, halo, cyano, nitro, thiol, 1-6C)alkylthio, (1-6C)alkylsulphonyl, (1-6C)alkylsulphenyl, imidazolyl, hydrazido,(1-6C)alkylimidazolyl,(1-6C)alkylsulphonamido, (1-6C)alkylaminosulphonyl, aminosulphonyl, (1-6C)haloalkoxy, or (1-6C)haloalkyl;
- and
- Lp is a lipophilic group;
- or a physiologically tolerable salt thereof.
9 more elements
A compound as claimed in any one of claims 1 to 10, in which Cy is a group of formula
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- in which one of Xa and Xb is N and the other is NH or S, and each of R3r and R3s is as defined for R3a.
Dependencies are inferred from the claim text.