IP Library Granted Patent US 9,238,571
Granted Patent B2
US 9,238,571 · App. 13/498,600 · Granted Jan 19, 2016

Formulations for c-Met kinase inhibitors

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Quick Facts
Patent No.
US 9,238,571
App. No.
13/498,600
Granted
Jan 19, 2016
Kind
B2
Abstract

The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.

Claims (7)

1. A pharmaceutical composition comprising from 30% to 35% by weight of 1-[3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2- ylmethyl)methanesulfonamide or a pharmaceutically acceptable salt thereof, 40% to 45% by weight of an acidulant, 20% to 25% by weight of a diluent, 1.0% to 5.0% by weight of a disintegrant and from 0.5% to 2.0% by weight of a lubricant, wherein the weight ratio of 1-[3-(1-Methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide to acidulant is selected from within a range of 0.3 to 5.0.

2. The pharmaceutical composition of claim 1 wherein the acidulent is selected from the group consisting of acetic, adipic, benzenesulphonic, benzoic, caprylic, cinnamic, citric, ethanedisulphonic, tartaric, ascorbic, maleic, glutamic, lactic, oxalic, L-Aspartic, 2-hydroxyethanesulfonic, pamoic, malonic, gentisic, salicylic, fumaric, glucoheptoic, gluconic, glucuronic, hippuric, lactobionic, laurylsulfuric, malic, malonic, mandelic, methanesulphonic, propionic, stearic, toluenesulphonic, undecylenic, camphorsulfonic and oleic acid.

3. The pharmaceutical composition of claim 1 wherein the diluent is selected from the group consisting of microcrystalline cellulose, lactose, mannitol, calcium phosphate, calcium carbonate, magnesium carbonate, sucrose, glucose, sorbitol, calcium sulfate, powdered cellulose, silicified microcrystalline cellulose, cellulose acetate, compressible sugar, dextrates, dextrin, dextrose, ethylcelluose, fructose, glyceryl palmitostearate, kaolin, lactitol, magnesium carbonate, magnesium oxide, maltodextrin, maltose, medium-chain triglycerides, polydextrose, polymethacrylates, simethicone, sodium alginate, sodium chloride, tragacanth, trehalose, xylitol and starch.

4. The pharmaceutical composition of claim 1 wherein the disintegrant is selected from the group consisting of croscarmellose sodium, starch, crospovidone, sodium starch glycolate, calcium carbonate, sodium carbonate, magnesium carbonate, alginic acid, tribasic calcium phosphate, calcium carboxymethylcellulose, sodium carboxymethylcellulose, powdered cellulose, chitosan, colloidal silicon dioxide, guar gum, hydroxypropyl cellulose, magnesium aluminium silicate, methylcellulose, povidone, and sodium alginate.

5. The pharmaceutical composition of claim 1 wherein the lubricant is selected from the group consisting of magnesium stearate, stearic acid, sodium stearyl fumerate, talc, calcium stearate, glycerin monostearate, glyceryl behenate, glyceryl palmitostearate, magnesium lauyl sulfate, medium chain triglycerides, poloxamer, sodium benzoate, sodium chloride, sodium lauryl sulfate and zinc stearate.

6. The pharmaceutical composition of claim 1 wherein the acidulant is citric acid, the diluent is microcrystalline cellulose, the disintegrant is croscarmellose sodium and the lubricant is magnesium stearate.

7. A method of improving the absorption of a c-Met kinase inhibitor by administering to a patient the pharmaceutical composition of claim 1 .

Assignments (3)
CHANGE OF ADDRESS Recorded May 10, 2022
From: MERCK SHARP & DOHME (UK) LIMITED
To: MERCK SHARP & DOHME (UK) LIMITED
Reel/Frame 060110/0121 →
NUNC PRO TUNC ASSIGNMENT Recorded Aug 5, 2021
From: MERCK SHARP & DOHME LIMITED
To: MERCK SHARP & DOHME (UK) LIMITED
Reel/Frame 057089/0263 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 28, 2012
From: WARD, ROBERT
To: MERCK SHARP & DOHME LIMITED
Reel/Frame 027943/0586 →