# US 12,178,808 B2 · Amorphous solid dispersion comprising 6-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide

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- Number: US 12,178,808 B2
- Document ID: US12178808B2
- Status: Granted
- Kind: B2
- Application number: 17/241,906
- Filed: 2021-04-27
- Published: 2021-08-26
- Granted: 2024-12-31
- Earliest claimed: 2018-11-06
- Assignees: Beijing Innocare Pharma Tech Co., Ltd.
- Applicants: Beijing Innocare Pharma Tech Co., Ltd.
- Inventors: Xiangyang Chen; Zuopeng Wang; Liqin Yu
- Web page: https://patentgrep.com/patent/US12178808B2

## CPC

- A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)}
- A61K 31/4545: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
- A61K 9/14: Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)}
- A61K 9/1635: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates}
- A61K 9/1652: {Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin (homeopathic globules A61K9/1623)}
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- A61K 9/48: Preparations in capsules, e.g. of gelatin, of chocolate {(A61K9/0004 takes precedence; bite capsules A61K9/0056)}
- A61K 31/455: Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
- A61P 35/00: Antineoplastic agents
- 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 present invention relates to an amorphous solid dispersion comprises 6-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)nicotinamide (Compound I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable polymer. The present invention also relates to pharmaceutical compositions comprising the amorphous solid dispersion. The amorphous solid dispersion of the present invention is stable upon storage and provides a better dissolution rate and bioavailability when comparing with a crystalline form.

## Claims

### Claim 1

An amorphous solid dispersion comprising 20-40% w/w of compound I or a pharmaceutically acceptable salt thereof, and 60-80% w/w of hydroxypropylmethylcellulose-acetate succinate (HPMC-AS),

### Claim 2 (depends on 1)

The amorphous solid dispersion according to claim 1, comprising 20% w/w or 40% w/w of compound I.

### Claim 3 (depends on 1)

The amorphous solid dispersion according to claim 1, prepared by spray-drying or hot-melt extrusion.

### Claim 4 (depends on 1)

A pharmaceutical composition comprises a pharmaceutically acceptable carrier and a therapeutically effective amount of the amorphous solid dispersion according to claim 1.

### Claim 5 (depends on 4)

The pharmaceutical composition of claim 4, in a tablet form or a capsule form.

### Claim 6 (depends on 1)

A method for preparing the amorphous solid dispersion of claim 1, comprising the steps:
(a) dissolving compound I or a pharmaceutically acceptable salt thereof and HPMC-AS in an organic solvent to form a solution, wherein the solution comprises 20-40% w/w of compound I or the pharmaceutically acceptable salt thereof and 60-80% w/w of HPMC-AS; and
(b) spraying drying the solution to form the amorphous solid dispersion.