# US 8,771,648 B2 · (Trimethoxyphenylamino) pyrimidinyl formulations

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- Number: US 8,771,648 B2
- Document ID: US8771648B2
- Status: Granted
- Kind: B2
- Application number: 13/559,805
- Filed: 2012-07-27
- Published: 2013-03-07
- Granted: 2014-07-08
- Earliest claimed: 2011-07-28
- Assignees: Rigel Pharmaceuticals, Inc.
- Applicants: Bindhumadhavan Gururajan; Farhan Abdul Karim Alhusban; Ian Paul Gabbott; David Bradley Brook Simpson; Dawn Sievwright
- Inventors: Bindhumadhavan Gururajan; Farhan Abdul Karim Alhusban; Ian Paul Gabbott; David Bradley Brook Simpson; Dawn Sievwright
- Web page: https://patentgrep.com/patent/US8771648B2

## CPC

- A61K 9/0007: {Effervescent (A61K9/0065 takes precedence)}
- A61K 31/5383: ortho- or peri-condensed with heterocyclic ring systems
- A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
- A61P 7/00: Drugs for disorders of the blood or the extracellular fluid
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 35/00: Antineoplastic agents
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- 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

There are provided pharmaceutical compositions comprising greater than 15% w/w of a compound of Formula (I) as defined herein and/or hydrate thereof and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.

## Claims

### Claim 1

A solid pharmaceutical composition comprising greater than 15% w/w of the compound of Formula (I):
wherein each X+ represents a monovalent cation;
and/or a hydrate thereof;
and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution at low pH;
and further comprising one or more pharmaceutically acceptable ingredients.

### Claim 2 (depends on 1)

The solid pharmaceutical composition according to claim 1 comprising greater than or equal to 25% w/w of the compound of Formula (I) and/or hydrate thereof.

### Claim 3 (depends on 1)

The solid pharmaceutical composition according to claim 1 comprising less than or equal to 20% w/w of the effervescent agent.

### Claim 4 (depends on 1)

The solid pharmaceutical composition according to claim 1 wherein the effervescent agent is sodium hydrogen carbonate.

### Claim 5 (depends on 1)

The solid pharmaceutical composition according to claim 1 wherein each X+ in the compound of Formula (I) represents a sodium cation (Na+).

### Claim 6 (depends on 1)

The solid pharmaceutical composition according to claim 1 wherein the compound of Formula (I) is in the form of an hexahydrate.

### Claim 7 (depends on 1)

The solid pharmaceutical composition according to claim 1 wherein the compound of Formula (I) is in the form of Formula (II):

### Claim 8

A unit dosage form comprising greater than or equal to 60 mg of the compound of Formula (I):
wherein each X+ represents a monovalent cation; and/or a hydrate thereof;
and less than or equal to 110 mg of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution at low pH;
and further comprising one or more pharmaceutically acceptable ingredients.