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Last Updated: December 12, 2025

Claims for Patent: 8,324,232

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Summary for Patent: 8,324,232

Title:	4-pyrimidinesulfamide derivative
Abstract:	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.
Inventor(s):	Martin Bolli, Christoph Boss, Alexander Treiber
Assignee:	Idorsia Pharmaceuticals Ltd
Application Number:	US12/673,413
Patent Claims:	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-2B with a compound of formula I-3 wherein G1 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-1B obtained in step a) using, BCl3 or BBr3. 8. The process of claim 7, which comprises the additional step of reacting a compound of formula I-4 wherein PG represents benzyl and G2 represents a halogen atom with ethylene glycol in the presence of a base to obtain the compound of formula I-2B.

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