# US 10,479,782 B2 · Forms of lumacaftor and processes for the preparation thereof

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- Number: US 10,479,782 B2
- Document ID: US10479782B2
- Status: Granted
- Kind: B2
- Application number: 15/763,216
- Filed: 2016-09-28
- Published: 2019-02-21
- Granted: 2019-11-19
- Earliest claimed: 2015-09-29
- Assignees: Mylan Laboratories Limited
- Applicants: Mylan Laboratories LImited
- Inventors: Ramakoteswara Rao Jetti; Hemant Malhari Mande; AnJaneyaraju Indukuri; Bommareddy Aggiramireddy; Neelima Bhagavatula; Amit Singh; Soumyajit Ghosh; Attanti Veera Venkata Srinivasarao; Umasankara Sastry Tummalapalli; Veera Venkata Satya Surya Appala Gosula
- Web page: https://patentgrep.com/patent/US10479782B2

## CPC

- C07D 405/12: linked by a chain containing hetero atoms as chain links
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

The present disclosure provides amorphous lumacaftor, amorphous solid dispersions of lumacaftor, crystalline lumacaftor acetic acid solvate, crystalline lumacaftor ethyl acetate solvate, and processes for the preparation thereof. The lumacaftor forms disclosed herein may be useful for the preparation of oral dosage forms for treating cystic fibrosis transmembrane conductance regulator (CFTR) mediated diseases.

## Claims

### Claim 1

A crystalline lumacaftor acetic acid solvate.

### Claim 2 (depends on 1)

The crystalline lumacaftor acetic acid solvate of claim 1, characterized by a 1H NMR (300 MHz, DMSO-d6) spectrum having peaks at 8.99, 7.97-7.89, 7.73-7.70, 7.69-7.67, 7.57-7.52, 7.38-7.34, 7.33-7.30, 2.22, 1.91, 1.52-1.48, and 1.16-1.13.

### Claim 3 (depends on 1)

The crystalline lumacaftor acetic acid solvate of claim 1, characterized by a PXRD pattern as shown in FIG. 3.

### Claim 4 (depends on 1)

Crystalline lumacaftor acetic acid solvate according to claim 1, with a purity of at least 99% as measured by HPLC.

### Claim 5

A process for the preparation of a crystalline lumacaftor acetic acid solvate comprising the steps of either:
a) suspending lumacaftor in acetic acid solvent; and
b) isolating the crystalline lumacaftor acetic acid solvate;
or
a) dissolving lumacaftor in acetic acid solvent to form a solution
b) cooling the solution; and
c) isolating crystalline lumacaftor acetic acid solvate.