Neatinib maleate and crystalline forms

• Main Authors: CHEW WARREN, LU QINGHONG, CHEAL GLORIA K, MIRMEHRABI, MAHMOUD, KU MANNCHING SHERRY, HADFIELD ANTHONY F
• Format: Patent
• Language: Chinese; English
• Published: 01.12.2023
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention relates to maleate forms of (E)-N-{4-[3-chloro-4-(2-pyridylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide, to a process for the preparation of the crystalline maleate forms, and to related compounds, and to pharmaceutical compositions comprising the same. The present invention also relates to a pharmaceutical composition comprising the maleate forms of (E)-N-{4-[3-chloro-4-(2-pyridylmethoxy) anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide. The maleate salts are useful in the treatment of cancers, in particular those affected by kinases of the epidermal growth factor receptor family. 本发明涉及(E)-N-{4-[3-氯-4-(2-吡啶基甲氧基)苯胺基]-3-氰基-7-乙氧基-6-喹啉基}-4-(二甲基氨基)-2-丁烯酰胺的马来酸盐形式，制备结晶马来酸盐形式的方法，和有关的化合物，以及包含它们的药物组合物。所述马来酸盐可用于治疗癌、特别是受表皮生长因子受体家族激酶影响的那些癌。