N.v. Organon

Msd Oss B.v.

Robert Gilfillan

Simon James Anthony Grove

Julia Adam-Worrall

Mingqiang Zhang

David Jonathan Bennett

Julia Adam-Worall

Minggiang Zhang

The invention relates to the compound N-(2-oxo-2-propoxyethyl)-&#x3b2;-phenyl-D-phenyl-alanyl-N-[(1-amino-6-iso-quinolinyl)methyl]-L-prolinamide or a pharmaceutically acceptable salt thereof, to a pharmaceutical composition comprising said compound, as well as to the use of the compound for the manufacture of a medicament for treating or for preventing thrombin mediated diseases.

Aminoisoquinoline thrombin inhibitor with improved bioavailability

The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R, Rand Rare independently H or (C)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, CF, halogen, nitro, cyano, NRR, NRCOR, and CONRR; Rand Rare independently H or (C)-alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)-alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

(Pyrido/thieno)-[f]-oxazepine-5-one derivatives

The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula I wherein R, Rand Rare independently H or (C)alkyl; Ar represents a fused thiophene or pyridine ring optionally substituted with one or more substituents selected from (C)alkyl, (C)alkyloxy, (C)alkyloxy(C)alkyl, CF, halogen, nitro, cyano, NRR, NRCOR, and CONRR; Rand Rare independently H or (C)alkyl; or Rand Rform together with the nitrogen atom to which they are bound a 5- or 6-membered saturated heterocyclic ring, optionally containing a further heteroatom selected from O, S or NR; Ris (C)alkyl; A represents the residue of a 4-7 membered saturated heterocyclic ring, optionally containing an oxygen atom, the ring being optionally substituted with 1-3 substituents selected from (C)alkyl, (C)alkyloxy, hydroxy, halogen and oxo; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

The present invention relates to (pyrido/thieno)-[f]-oxazepine-5-one derivatives having the general Formula (I) or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these (pyrido/thieno)-[f]-oxazepine-5-one derivatives in the treatment of neurological diseases and psychiatric disorders which are responsive to enhancement of synaptic responses mediated by AMPA receptors in the central nervous system.

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Newhouse, United Kingdom

Robert Gilfillan