Serine protease inhibitors

A serine protease inhibitor compound of formula (I)

• wherein:
• R2 is:
• (i) phenyl optionally being substituted in the 3 and/or 4 position by halo, nitro, thiol, haloalkoxy, hydrazido, alkylhydrazido, amino, cyano, 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;
• (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;
• (iii) isoquinolin-7-yl, indol-5-yl, indol-6-yl, indazol-5-yl, indazol-6-yl, benzothiazol-6-yl or benzisoxazol-5-yl optionally substituted at the 3 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1j;
• (iv) benzimidazol-5-yl or benzothiazol-6-yl optionally substituted at the 2 position by amino;
• (v) thien-2-yl or thien-3-yl optionally substituted at the 4 or 5 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1;
• (vi) 3,4-methylenedioxyphenyl, 2,3-dihydroindol-6-yl, 3,3-dichloro-2-oxo-indol-6-yl or 1-methyl-3-aminoindazol-5-yl;
• (vii) benzothiazol-2-yl, imidazo[1,2-a]pyrimidin-2-yl or tetrahydroimidazo[1,2-a]pyrimidin-2-yl;
• (viii) pyrazol-2-yl optionally substituted at the 5 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1;
• (ix) pyrid-2-yl optionally substituted at the 5 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1;
• (x) pyrid-3-yl optionally substituted at the 6 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1;
• (xi) benzofur-2-yl optionally substituted at the 3 position by amino, hydroxy, halo, alkyl, carboxy, cyano, amido, aminoalkyl, alkoxy or alkylthio and at the 5 or 6 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1j;
• (xii) indol-2-yl optionally substituted on the indole nitrogen atom by alkyl and optionally substituted at the 5 or 6 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1j;
• (xiii) indol-6-yl substituted at the 5 position by amino, hydroxy, halo, alkyl, carboxy, alkoxycarbonyl, cyano, amido, aminoalkyl, alkoxy or alkylthio and optionally substituted at the 3 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1j;
• or
• (xiv) benzo[b]thiophen-2-yl optionally substituted at the 3 position by amino, hydroxy, halo, alkyl, carboxy, cyano, amido, aminoalkyl, alkoxy or alkylthio and at the 5 or 6 position by halo, haloalkoxy, haloalkyl, cyano, nitro, amino, hydrazido, alkylthio, alkenyl, alkynyl or R1j;
• with the proviso that R2 cannot be aminoisoquinolyl;
• R1 is hydrogen;
• hydroxy;
• alkoxy;
• alkyl;
• alkylaminoalkyl;
• alkanoyl;
• hydroxyalkyl;
• alkoxyalkyl;
• alkoxycarbonyl;
• alkylaminocarbonyl;
• alkylamino;
• carboxyl;
• carboxymethyl;
• amido (CONH2) or amidomethyl;
• R1j is:
• hydrogen;
• hydroxy;
• alkoxy;
• alkyl;
• alkanol;
• hydroxyalkyl;
• alkoxyalkyl;
• alkoxycarbonyl;
• alkylamino;
• carboxyl;
• carboxymethyl;
• amido (CONH2) or amidomethyl;
• —X—X— is —CONH—;
• Y (the α-atom) is CH;
• Cy is an optionally R3a substituted:
• phenyl, pyridyl, thienyl, thiazolyl, naphthyl, piperidinyl, furanyl, pyrrolyl, isoxazolyl, isothiazolyl, pyrazolyl, oxazolyl, imidazolyl, 1,2,4-thiadiazolyl, 1,3,4-thiadiazolyl, pyrimidinyl, pyridazinyl, quinoloyl, isoquinolyl, benzofuryl, benzothienyl or cycloalkyl group, or a phenyl group substituted by R3ixi in which x1 is a bond, O, NH or CH2 and R3i is phenyl, pyridyl or pyrimidinyl optionally substituted by R3a;
• each R3a independently is hydrogen;
• hydroxyl;
• alkoxy;
• alkyl;
• alkylaminoalkyl;
• hydroxymethyl;
• carboxy;
• alkoxyalkyl;
• alkoxycarbonyl;
• alkylaminocarbonyl;
• aminomethyl;
• CONH2;
• CH2CONH2;
• (1-6C)alkanoylamino;
• alkoxycarbonylamino;
• amino;
• halo;
• cyano;
• nitro;
• thiol;
• alkylthio;
• alkylsulphonyl;
• alkylsulphenyl;
• alkylsulphonamido;
• alkylaminosulphonyl;
• aminosulphonyl;
• haloalkoxy;
• haloalkyl;
• a group of the formula —C(X3)N(R11)R12 (wherein X3 is O or S and R11 and R12 are independently selected from hydrogen, methyl, ethyl, or together with the nitrogen atom to which they are attached form a pyrrolidin-1-yl, piperidin-1-yl or morpholino group;
• or —OCH2O— which is bonded to two adjacent ring atoms in Cy and
• —L—Lp(D)n is
• q is 1 or 2;
• Q is methylene;
• and Rq is NRaRb in which each of Ra and Rb independently is hydrogen or C1-3alkyl;
• or one of Ra and Rb is hydrogen or methyl and the other of Ra and Rb is (3-6C)cycloalkyl, pyrid-4-yl, —CH2—Rc or —CH2—Rd in which Rc is pyridyl or phenyl (which phenyl may bear a fluoro, chloro, methyl, CONH2, SO2NH2, methylaminosulphonyl, dimethylaminosulphonyl, methylsulphonylamino, methoxy or methylsulphonyl substituent) and in which Rd is isopropyl or cyclopentyl, or NRaRb is azetidino, pyrrolidino, piperidino, morpholino, thiomorpholino, piperazino, or tetrahydro-1,4-diazepino [in which a pyrrolidino or piperidino may be a 3,4-didehydro derivative and in which a azetidino, pyrrolidino, piperidino, morpholino, thiomorpholino, piperazino, or tetrahydro-1,4-diazepino may be optionally substituted on a ring carbon atom by hydroxy, amino, (1-3C)alkoxy, (1-3C)hydroxyalkyl, (1-3C)alkyl, carboxy, methoxycarbonyl or ethoxycarbonyl (provided that the amino, hydroxy or alkoxy substituent is not on a ring carbon atom which is included in a double bond, or adjacent to a ring oxygen, sulfur or nitrogen atom) and in which the piperazino or tetrahydro-1,4-diazepino may bear a methyl group at the 4-position];
• or a physiologically-tolerable salt thereof.