Composition comprising tetracyclic compound

Patent metadata

Field	Value
Publication number	US-10646468-B2
Application number	US-201615151601-A
Country	US
Kind code	B2
Filing date	May 11, 2016
Priority date	Aug 20, 2010
Publication date	May 12, 2020
Grant date	May 12, 2020

Abstract

A composition which comprises substance represented by Formula (I),

[Meanings of the symbols that are included in the formula are given in the specification as definitions]

a pharmaceutically acceptable carrier, and a dissolution aid.is useful for improving solubility, oral absorbability and/or absorbability in blood of a poorly water-soluble or water insoluble tetracyclic compounds having an ALK inhibitory activity that are useful as a prophylactic and/or therapeutic agent for cancer, depression, and cognitive function disorder.

First claim

The invention claimed is:

1. A composition comprising 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile,
or a salt thereof, a pharmaceutically acceptable carrier, and a dissolution aid,
wherein the dissolution aid is selected from the group consisting of citric acid, hydroxypropylmethyl cellulose, methacrylic acid copolymer LD, methyl cellulose, purified shellac, sodium dehydroacetate, fumaric acid, DL-malic acid, L-aspartic acid, adipic acid, propylene glycol alginate ester, sodium caseinate, carboxymethylethyl cellulose, succinic acid, copolyvidone, dioctyl sodium sulfosuccinate, lactic acid, aluminum lactate, hydroxyethylmethyl cellulose, hydroxypropylmethyl cellulose acetate succinate, sodium polystyrene sulfonate, polyvinylacetal diethylaminoacetate, methacrylic acid copolymer S, sulfuric acid, aluminum sulfate, a vinyl pyrrolidone×vinyl acetate copolymer, and sodium decyl sulfate.

2. The composition according to claim 1 , wherein the composition further comprises an organic polymer which is selected from the group consisting of hydroxypropyl cellulose, powdered agar, guar gum, zein, a carboxyvinyl polymer, polyvinyl alcohol, a vinyl acetate resin, casein, amino alkylmethacrylate copolymer E, cellulose acetate phthalate, and a mixture thereof.

3. The composition according to claim 1 , wherein said 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-yl-piperidin-1-yl)-11-oxo-6,11-dihydro-5H-benzo[b]carbazole-3-carbonitrile or salt thereof has a water solubility less than 100 μg/mL at 25° C.

4. An orally administrable formulation comprising the composition of claim 1 .

Assignees

• Chugai Pharmaceutical Co Ltd

Inventors

• Furumoto Kentaro
• Shiraki Koji
• Hirayama Tomoaki

Classifications

• C07D209/56

  Ring systems containing three or more rings · CPC title

• C07D405/14

  containing three or more hetero rings · CPC title

• A61K47/20

  containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids · CPC title

• A61K47/02

  Inorganic compounds · CPC title

• A61K31/4439

  containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465) · CPC title