Astrazeneca Ab

Albireo Ab

Anders Johansson

Tord Bertil Inghardt

Arne Svensson

Johan R Johansson

Joachim Persson

Carl-Gustav Sigfridsson

Tord Astrazeneca Inghardt

The present invention relates to new compounds of formula I, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I.

Benzamide compounds that act as NK receptor antagonists

The present invention relates to a compound of the general formula (I) wherein Het is an optionally substituted 4-, 5-, 6- or 7-membered heterocyclic ring having at least one nitrogen atom; R1 is hydrogen, hydroxy, C-Calkyl, C-Ccycloalkyl, C-Calkenyl or C-Calkynyl; R2 and R3 is each and independently selected from hydrogen, C-Calkyl, C-Ccycloalkyl, C-Calkenyl, C-Calkynyl, C-Calkoxy, halogen and cyano, provided that R2 and R3 may not both be hydrogen; R4 is C-Calkyl, C-Ccycloalkyl, C-Calkenyl or C-Calkynyl; Ar is an optionally substituted aromatic ring system selected from pyridinyl; 1-naphthyl; 5,6,7,8-tetrahydro-1-naphthyl; quinolinyl; 2,3-dihydro-1,4-benzodioxinyl; 1,3-benzodioxolyl; 5,6,7,8-tetrahydroquinolinyl; 5,6,7,8-tetrahydroisoquinolinyl; 5,6,7,8-tetrahydroquinazolin-4-yl; 1-benzo[b]thiophen-7-yl; 1-benzo[b]thiophen-4-yl; 1-benzo[b]thiophen-3-yl; isoquinolinyl; quinazolinyl; and indan-4-yl; or Ar is substituted phenyl; or an enantiomer thereof or any salt thereof; to a pharmaceutical composition containing said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I and to new intermediates used in the preparation thereof. 

Azetidine compounds

There is provided a compound of formula I wherein R, R, R, Y and Rhave meanings given in the description and pharmaceutically-acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

Mandelic acid derivatives and their use as thrombin inhibitors

There is provided a compound of formula (1) and pharmaceutically-acceptable derivatives (including prodrugs) thereof. Which compound and derivatives are useful as, or are as useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.

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Mölndal, Sweden

Anders Johansson