Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors iia and xa
Номер патента: EP2655399A1
Опубликовано: 30-10-2013
Автор(ы): Adel Rafai Far, Alexander Schulze, Andrea Schweinitz, Claudia Reichelt, Friedrich-Alexander Ludwig, Mohammed Daghish, Peter Herold, Stjepan Jelakovic, TING Kang
Принадлежит: Medicines Company Leipzig GmbH
Опубликовано: 30-10-2013
Автор(ы): Adel Rafai Far, Alexander Schulze, Andrea Schweinitz, Claudia Reichelt, Friedrich-Alexander Ludwig, Mohammed Daghish, Peter Herold, Stjepan Jelakovic, TING Kang
Принадлежит: Medicines Company Leipzig GmbH
Реферат: The invention provides methods of making and using compounds of the formula (I) or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R 1 is selected from the group consisting of -CH 2 NH 2 , and (Formula (II)); R 2 is selected from the group consisting of -H, -OH, -NH 2 and acetyl; R 3 is selected from the group consisting of -H, benzyloxycarbonyl and benzyisulfonyl;and R 4 is selected from the group consisting of -OH, (Formulae (III), (IV), (V), (VI)), wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of -0-, -S-, -S(=0)-, -S0 2 -, methylene, -CH(OH)-, -CH(NH 2 )-, -CH(CH 2 -OH)-, -CH(CH 2 - NH 2 )- or -N(R 6 )-, R 5 is selected from the group consisting of -H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of -H, a simple (C 1 -C 3 ) alkyl or a simple (C 1 -C 3 ) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.
Trypsin-like serine protease inhibitors, their preparation and use as selective inhibitors of the clotting factors iia and xa
Номер патента: US20120252743A1. Автор: TING Kang,Peter Herold,Stjepan Jelakovic,Andrea Schweinitz,Adel Rafai Far,Claudia Reichelt,Friedrich-Alexander Ludwig,Alexander Schulze,Mohammed Daghish. Владелец: Medicines Company Leipzig GmbH. Дата публикации: 2012-10-04.