NZ796683A - Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan - Google Patents
Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentanInfo
- Publication number
- NZ796683A NZ796683A NZ796683A NZ79668318A NZ796683A NZ 796683 A NZ796683 A NZ 796683A NZ 796683 A NZ796683 A NZ 796683A NZ 79668318 A NZ79668318 A NZ 79668318A NZ 796683 A NZ796683 A NZ 796683A
- Authority
- NZ
- New Zealand
- Prior art keywords
- bromo
- sulfamide
- phenyl
- pyrimidinyloxy
- pyrimidinyl
- Prior art date
Links
Abstract
The present invention concerns novel crystalline forms of {5-(4-bromo-phenyl)-6-[2-(5-bromo- pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, processes for the preparation thereof, pharmaceutical compositions comprising said crystalline forms, pharmaceutical compositions prepared from such crystalline forms, and their use as endothelin receptor antagonists. It also relates to new uses of {5-(4-bromo-phenyl)-6-[2- (5-bromo-pyrimidin-2-yloxy)-ethoxy]-pyrimidin-4-yl}-sulfamide, either alone or in combination with other active ingredients or therapeutic agents.
Claims (14)
1. Use of the compound bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide: S Br H2N NH N O or of a pharmaceutically able salt thereof, for the manufacture of a ment for the treatment of chronic kidney disease (CKD), diabetes, diabetic nephropathy, diabetic 5 retinopathy, diabetic vasculopathy, c heart failure or diastolic dysfunction, wherein said medicament is used in combination with an Angiotensin Converting Enzyme (ACE) inhibitor, or an Angiotensin Receptor Blocker (ARB), or with a pharmaceutically able salt of one of these.
2. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- 10 pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to claim 1, wherein said medicament is for the treatment of chronic kidney disease (CKD) or diabetic nephropathy.
3. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to 15 claim 1, wherein said ment is for the treatment of chronic kidney disease (CKD).
4. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to claim 1, wherein said medicament is for the treatment of chronic kidney disease (CKD) of stages 1 to 4 as defined by the Kidney Disease Improving Global es (KDIGO) 20 ines, caused by essential hypertension.
5. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to claim 1, wherein said ment is for the treatment of diabetic nephropathy.
6. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to claim 1, wherein said medicament is for the treatment of chronic heart failure with preserved on on. 5
7. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to claim 1, wherein said medicament is for the treatment of chronic diastolic heart failure.
8. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to 10 claim 1, n said medicament is for the treatment of diastolic dysfunction.
9. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt f, according to any one of claims 1 to 8, wherein said medicament is used in combination with an
10. Angiotensin Receptor Blocker (ARB), or with a pharmaceutically acceptable salt thereof. 15 10. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)- ethoxy]-pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt f, according to claim 9, wherein said Angiotensin Receptor Blocker (ARB), or ceutically acceptable salt thereof, is valsartan, losartan, telmisartan, rtan, candesartan, olmesartan, or azilsartan, or a pharmaceutically able salt of one of 20 these.
11. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)- ]-pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to claim 9, wherein said Angiotensin Receptor Blocker (ARB) is valsartan or a pharmaceutically acceptable salt thereof. 25
12. Use of the nd {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)- ]-pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 11, wherein said medicament is in the form of a tablet, wherein said tablet consists of a pharmaceutical composition comprising: • the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- 30 pyrimidinyl}-sulfamide in a total amount from 5 to 25% in weight based on the total weight of the pharmaceutical composition, • microcrystalline cellulose in a total amount from 20 to 30% in weight based on the total weight of the pharmaceutical composition, • lactose in a total amount from 40 to 65% in weight based on the total weight of the pharmaceutical composition, 5 • hydroxypropylcellulose in a total amount from 1 to 3% in weight based on the total weight of the pharmaceutical composition, • croscarmellose sodium in a total amount from 2 to 8% in weight based on the total weight of the pharmaceutical composition, and • ium stearate in a total amount from 0.2 to 2% in weight based on the total 10 weight of the pharmaceutical composition; wherein the total percent in weight of the solid pharmaceutical composition is 100.
13. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)- ethoxy]-pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 12, wherein the compound {5-(4-bromo-phenyl)- 15 5-bromo-pyrimidinyloxy)-ethoxy]-pyrimidinyl}-sulfamide is administered in a pharmaceutical unit dosage form suitable for the oral administration of 10 to 50 mg per day of {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]-pyrimidinyl}- sulfamide.
14. Use of the compound {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)- 20 ethoxy]-pyrimidinyl}-sulfamide, or of a pharmaceutically acceptable salt f, according to any one of claims 1 to 13, wherein the compound is comprised in said medicament as {5-(4-bromo-phenyl)[2-(5-bromo-pyrimidinyloxy)-ethoxy]- pyrimidinyl}-sulfamide in free base form; wherein said free base form is a crystalline form characterized by the ce of peaks in the X-ray powder diffraction diagram at the 25 ing angles of refraction 2θ: 17.8°, 18.6°, 20.0°, 23.2° and 23.5°; wherein said X-ray powder diffraction diagram is obtained by using combined Cu Kα1 and Kα2 radiation, t Kα2 stripping; and the accuracy of the 2θ values is in the range of 2θ +/ 0.2°. WO 54101 - [/10-
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EPPCT/EP2017(EPO)/054489 | 2017-02-27 | ||
| EPPCT/EP2017(EPO)/061487 | 2017-05-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ796683A true NZ796683A (en) | 2023-01-27 |
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