The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same.

The present invention provides a salt form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibits desirable characteristics for the same.

A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture. ##STR00001##

A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoroanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture. ##STR00001##

Disclosed are compounds of general formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.

A sulfonate composition obtainable by a process in which a naphthalene ring-containing sulfonic acid is reacted with an amine in the presence of a base oil at a temperature in the range of from 20-80 C. The molar ratio of the sulfonic acid to the amide is in the range of from 0.2-3 (S/A). The invention also provides a preservative composition comprising the present sulfonate composition; a metal article having a coating thereon which coating comprises the present preservative composition; a process for preparing the sulfonate composition; the use of the present sulfonate composition to prevent and/or reduce corrosion in a roll bearing system; and the use of the present preservative composition to prevent and/or reduce corrosion in a roll bearing system.

A sulfonate composition obtainable by a process in which a naphthalene ring-containing sulfonic acid is reacted with an amine in the presence of a base oil at a temperature in the range of from 20-80 C. The molar ratio of the sulfonic acid to the amide is in the range of from 0.2-3 (S/A). The invention also provides a preservative composition comprising the present sulfonate composition; a metal article having a coating thereon which coating comprises the present preservative composition; a process for preparing the sulfonate composition; the use of the present sulfonate composition to prevent and/or reduce corrosion in a roll bearing system; and the use of the present preservative composition to prevent and/or reduce corrosion in a roll bearing system.

The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

The present invention provides processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as intermediates and processes for making the intermediates. Also provided are crystalline forms of the compound and the intermediates.

Disclosed are compounds of general formula (I):

##STR00001##

and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.