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US 2006/0148879 A1Published application
1-Phenyl-2-oxo-3-sulfonylamino-pyrrolidine derivatives and related compounds as factor xa inhibitors for the treatment of acute vascular diseases
AssigneeGlaxo Group Limited
InventorsAlan Borthwick, Chuen Chan, Henry Kelly, Savvas Kleanthous, Andrew Mason, Nigel Watson
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Abstract
The invention relates to compounds of formula (I): wherein substituents are as defined.
Claims11
A compound of formula (I):
- wherein:
- R1 represents a group selected from:
- each ring of which optionally contains a further heteroatom N,
- Z represents an optional substituent halogen,
- alk represents alkylene or alkenylene,
- T represents S, O or NH;
- R2 represents —C1-6alkyl, —C1-3alkylCN, —C0-3alkylRc, —C1-3alkylRf, —C2-3alkylNRaRb, —C2-3alkylOC1-6alkyl, —C2-3alkylOC1-3alkylCONRaRb, with the proviso that R2 does not represent C2-3alkylmorpholino;
- Ra and Rb independently represent hydrogen, —C1-6alkyl, or together with the N atom to which they are bonded form a 5-, 6- or 7-membered non-aromatic heterocyclic ring optionally containing an additional heteroatom selected from O, N or S optionally substituted by —C1-4alkyl, and optionally the S heteroatom is substituted by 0 i.e. represents S(O)n;
- Rc represents —C1-4cycloalkyl;
- Rf represents phenyl or a 5- or 6-membered aromatic heterocyclic ring, containing at least one heteroatom selected from O, N or S, optionally substituted by 0 to 2 groups selected from —C1-4alkyl or —NH2, and optionally the S or N heteroatom is substituted by 0, i.e. represents S(O), or N-oxide;
- n represents 0-2;
- X represents phenyl or a 5- or 6-membered aromatic heterocyclic group containing at least one heteroatom selected from O, N or S, each of which is optionally substituted by 0-2 groups selected from:
- halogen, —C1-4alkyl, —C2-4alkenyl, —CN, —CF3, —NRaRb, —C1-4alkylORa, —C(O)Rd and —C(O)NRaRb;
- R represents hydrogen or —C1-4alkyl;
- Y represents a substituent selected from hydrogen, halogen, —C1-4alkyl, —C2-4alkenyl, —NRaRb, —NO2, —C(O)NRaRb, —N(C1-4alkyl)(CHO), —NHCOC1-4alkyl, —NHSO2RC0-4alkylRO, —C(O)Rd, —S(O)nRd, or —S(O)2NRaRb;
- Rd represents —C1-6alkyl;
- and/or pharmaceutically acceptable derivative thereof.
14 more elements
A compound according to any one of claims 14 wherein Y represents a substituent selected from —C(O)NRaRb, —S(O)nRd, —S(O)2NRaRb, —N(C1-4alkyl)(CHO) or —NHSO2Rd and/or pharmaceutically acceptable derivative thereof.
A process for preparing a compound of formula (I) which comprises, reacting a compound of formula (II) with a compound of formula (III):
- where R2 is —C1-6alkyl, —C1-3alkylCN, —C0-3alkylRc, —C1-3alkylRf, —C2-3alkylNRaRb, —C2-3alkylOC1-6alkyl, —C2-3alkylOC1-3alkylCONRaRb, with the proviso that R2 does not represent C2-3alkylmorpholino, and T is a suitable leaving group.
Dependencies are inferred from the claim text.