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US 2016/0096826 A1Published application
Co-crystals of lapatinib monoacid salts
AssigneeF.I.S.—Fabrica Italiana Sintetici S.p.A.
InventorsNicolas TESSON, Antonio SEGADE RODRÍGUEZ
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Abstract
The present invention refers to co-crystals of monoacid salts of the pharmaceutical active ingredient named Lapatinib and to processes for the preparation thereof and medical uses.
Claims16
Co-crystal of Lapatinib selected from the group consisting of:
- (a) Lapatinib monotosylate:caproic acid (1:2) of formula (Form I):
- (b) Lapatinib monotosylate:caprylic acid (1:2) of formula (Form II):
- and
- (c) Lapatinib monohydrochloride:adipic acid (1:1) of formula (Form III):
1 more element
Process for the preparation of the co-crystal of Lapatinib being
- (a) Lapatinib monotosylate:caproic acid (1:2) of formula (Form I):
- or being
- (b) Lapatinib monotosylate:caprylic acid (1:2) of formula (Form II):
- comprising:
- (a) reacting Lapatinib of formula (I) with paratoluensulfonic acid to provide Lapatinib monotosylate of formula (I-TsOH):
- and
- (b) treatment of treating the Lapatinib monotosylate with caproic acid or caprylic acid.
4 more elements
Process for the preparation of the co-crystal of Lapatinib being Lapatinib monohydrochloride:adipic acid (1:1) of formula (Form III):
- comprising:
- (a) reaction of reacting Lapatinib of formula (I) with hydrochloric acid to provide Lapatinib monohydrochloride of formula (I-HCl):
- and
- (b) treatment of treating the Lapatinib monohydrochloride with adipic acid.
1 more element
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Dependencies are inferred from the claim text.