# US 10,117,870 B2 · Stable pharmaceutical compositions comprising a pyrimidine-sulfamide

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- Number: US 10,117,870 B2
- Document ID: US10117870B2
- Status: Granted
- Kind: B2
- Application number: 15/002,255
- Filed: 2016-01-20
- Published: 2016-05-19
- Granted: 2018-11-06
- Earliest claimed: 2005-09-12
- Assignees: Actelion Pharmaceuticals Ltd.
- Applicants: Actelion Pharmaceuticals Ltd.
- Inventors: Charles Tokunbo Adesuyi; Bruce Hamilton Lithgow; Olivier Lambert; Lovelace Holman
- Web page: https://patentgrep.com/patent/US10117870B2

## CPC

- A61K 31/506: not condensed and containing further heterocyclic rings
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/205: {Polysaccharides, e.g. alginate, gums; Cyclodextrin}
- A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin}
- A61K 9/2077: {Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets}
- A61K 9/2846: {Poly(meth)acrylates}
- A61K 9/2866: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose}
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/00: Drugs for disorders of the respiratory system
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to stable pharmaceutical compositions comprising the compound of the below formula, or pharmaceutically acceptable salts, solvates, hydrates or morphological forms thereof.

## Claims

### Claim 1

A pharmaceutical composition comprising:
a) the compound of the formula I as drawn below
or a pharmaceutically acceptable salt, solvate, hydrate or morphological form thereof,
b) a filler, consisting of lactose monohydrate with microcrystalline cellulose,
c) a disintegrant, consisting of sodium starch glycolate or a combination of sodium starch glycolate and polyvinylpyrrolidone,
d) a surfactant, consisting of sodium lauryl sulphate, in a total amount of 0.1 to 3% in weight based on the total weight of the pharmaceutical composition, and
e) a lubricant, consisting of magnesium stearate.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the disintegrant is consisting of a combination of sodium starch glycolate and polyvinylpyrrolidone.

### Claim 3 (depends on 2)

The pharmaceutical composition according to claim 2, wherein the combination of sodium starch glycolate and polyvinylpyrrolidone is present in a total amount of 2 to 10% in weight based on the total weight of the pharmaceutical composition.

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the magnesium stearate is present in a total amount of between 0.1 to 1% in weight based on the total weight of the pharmaceutical composition.

### Claim 5 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the sodium lauryl sulphate is present in a total amount of 0.1 to 1% in weight based on the total weight of the pharmaceutical composition.

### Claim 6 (depends on 1)

The pharmaceutical composition according to claim 1, which is in the form of a capsule.

### Claim 7 (depends on 1)

The pharmaceutical composition according to claim 1, which is in the form of a tablet.

### Claim 8 (depends on 1)

A method of treating pulmonary arterial hypertension comprising the administration to a patient in need thereof a pharmaceutical composition according to claim 1.

### Claim 9 (depends on 1)

The pharmaceutical composition according to claim 1, comprising:
a) the compound of the formula I as drawn below
or a pharmaceutically acceptable salt, solvate, hydrate or morphological form thereof, in a total amount of up to 50% in weight based on the total weight of the pharmaceutical composition,
b) a filler, consisting of lactose monohydrate with microcrystalline cellulose, in a total amount of 10 to 95% in weight based on the total weight of the pharmaceutical composition,
c) a disintegrant, consisting of sodium starch glycolate or a combination of sodium starch glycolate and polyvinylpyrrolidone, in a total amount of 1 to 20% in weight based on the total weight of the pharmaceutical composition,
d) a surfactant, consisting of sodium lauryl sulphate, in a total amount of 0.1 to 3% in weight based on the total weight of the pharmaceutical composition, and
e) a lubricant, consisting of magnesium stearate, in a total amount of 0.05 to 10% in weight based on the total weight of the pharmaceutical composition.

### Claim 10 (depends on 9)

The pharmaceutical composition according to claim 9, wherein the disintegrant is consisting of a combination of sodium starch glycolate and polyvinylpyrrolidone.

### Claim 11 (depends on 10)

The pharmaceutical composition according to claim 10, wherein the combination of sodium starch glycolate and polyvinylpyrrolidone is present in a total amount of 2 to 10% in weight based on the total weight of the pharmaceutical composition.

### Claim 12 (depends on 9)

The pharmaceutical composition according to claim 9, wherein the magnesium stearate is present in a total amount of between 0.1 to 1% in weight based on the total weight of the pharmaceutical composition.

### Claim 13 (depends on 9)

The pharmaceutical composition according to claim 9, wherein the sodium lauryl sulphate is present in a total amount of 0.1 to 1% in weight based on the total weight of the pharmaceutical composition.

### Claim 14 (depends on 9)

The pharmaceutical composition according to claim 9, which is in the form of a capsule.

### Claim 15 (depends on 9)

The pharmaceutical composition according to claim 9, which is in the form of a tablet.

### Claim 16 (depends on 9)

A method of treating pulmonary arterial hypertension comprising the administration to a patient in need thereof a pharmaceutical composition according to claim 9.

### Claim 17 (depends on 1)

The pharmaceutical composition according to claim 1, comprising the compound of formula I shown below

### Claim 18 (depends on 7)

The pharmaceutical composition according to claim 7, comprising the compound of formula I shown below

### Claim 19 (depends on 9)

The pharmaceutical composition according to claim 9, comprising the compound of formula I shown below

### Claim 20 (depends on 15)

The pharmaceutical composition according to claim 15, comprising the compound of formula I shown below