US 10,851,061 B2 · Crystalline solid forms of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use

Abstract

The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.

Claims8

Dependent claims

A crystalline solid form of Compound 1:

wherein said crystalline solid form is in Form XXVIII, wherein said Form XVIII is characterized by an x-ray powder diffraction pattern (CuKα) comprising peaks at 6.5, 12.3, 17.7, and 19.1 (° 2θ±0.2° 2θ), or at 9.5, 11.8, 13.0, and 22.3 (° 2θ±0.2° 2θ), or at 6.5, 9.5, 11.8, 12.3, 13.0, 17.7, 19.1, and 22.3 (° 2θ±0.2° 2θ) at room temperature.

Dependencies are inferred from the claim text.

Facts

Application

16/671,834Filed 1 Nov 2019 · division

Priority

14 Feb 2014

Published

US 2020/0190033 A118 Jun 2020

Granted

1 Dec 2020

Term ends

Not estimatedThe source records don’t support an estimate.

Classification7 codes

C07D 215/233
Attached in position 2 or 4: only one oxygen atom which is attached in position 4
A61P 35/00
Antineoplastic agents
C07D 215/22
Oxygen atoms: attached in position 2 or 4
C07B 2200/13
Indexing scheme relating to specific properties of organic compounds: crystalline forms, e.g. polymorphs

Family

Application61/939,985Us provisional application · filed 14 Feb 2014

PCT/US2015/016052Parent of this division · filed 16 Feb 2015

US 2020/0190033 A1Pre-grant publication · published 18 Jun 2020

Application15/118,738Parent of this division

US 10,501,418 B2Parent of this division

US 2017/0044106 A1Published application

US 10,851,061 B2This patent

From the US filing history. Foreign family members aren’t listed.

Crystalline solid forms of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use

Life of this patent

Crystalline solid forms of N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use

Life of this patent

Abstract

Claims8