4-pyrimidinesulfamide derivative
View Patent ↗The invention relates to the compound of structural formula (I) and the salts thereof. Said compound is useful as endothelin receptor antagonist. The invention further relates to a process for preparing said compound.
1. The compound having the formula I
or a salt thereof.
2. A compound of formula I as defined in claim 1 , or a pharmaceutically acceptable salt thereof.
3. A pharmaceutical composition containing, as active principle, the compound of formula I as defined in claim 1 or a pharmaceutically acceptable salt thereof, and at least one therapeutically inert excipient.
4. A method for the treatment of hypertension comprising administering to a patient in need thereof, a pharmaceutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt form.
5. A method for the treatment of pulmonary hypertension comprising administering to a patient in need thereof, a pharmaceutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt form.
6. A method for the treatment of pulmonary arterial hypertension comprising administering to a patient in need thereof, a pharmaceutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt form.
7. A process for the preparation of the compound of formula I according to claim 1 , which process comprises the following steps:
a) reacting a compound of formula I-2 B
with a compound of formula I-3
wherein G 1 represents a chlorine or bromine atom or a methylsulfonyl or ethylsulfonyl group, in the presence of a strong base; and
b) cleaving the benzyl group of the compound of formula I-1 B obtained in step a)
using, BCl 3 or BBr 3 .
8. The process of claim 7 , which comprises the additional step of reacting a compound of formula I-4
wherein PG represents benzyl and G 2 represents a halogen atom
with ethylene glycol in the presence of a base to obtain the compound of formula I-2 B .