The present invention relates to novel crystalline forms of Neratinib maleate and the preparation method thereof. The novel crystalline forms of Neratinib maleate in the present invention have high solubility, good stability, good processability, easy post-treatment process and other favorable properties. The preparation method is simple, low cost, and has an important value for future optimization and development of the drug.

The present disclosure discloses an immobilized metalloporphyrin catalyst and its utilization in maleic acid preparation, belonging to the technical field of metalloporphyrin catalytic application. The immobilized metalloporphyrin catalyst is used for catalyzing furfural to prepare maleic acid and is good in catalytic effect, mild in reaction conditions and capable of greatly reducing the energy consumption required in the prior art. The catalyst disclosed by the present disclosure can provide a good microenvironment for a reaction, so that the yield and selectivity of maleic acid are increased; and according to a method disclosed by the present disclosure, the conversion ratio of furfural is 20.4%-95.6%, the yield of maleic acid is 10%-56.1%, and the selectivity is 43.6%-76.1%. Meanwhile, the catalyst is easy to separate and environmentally friendly and may be recycled for many times.

The present disclosure discloses an immobilized metalloporphyrin catalyst and its utilization in maleic acid preparation, belonging to the technical field of metalloporphyrin catalytic application. The immobilized metalloporphyrin catalyst is used for catalyzing furfural to prepare maleic acid and is good in catalytic effect, mild in reaction conditions and capable of greatly reducing the energy consumption required in the prior art. The catalyst disclosed by the present disclosure can provide a good microenvironment for a reaction, so that the yield and selectivity of maleic acid are increased; and according to a method disclosed by the present disclosure, the conversion ratio of furfural is 20.4%-95.6%, the yield of maleic acid is 10%-56.1%, and the selectivity is 43.6%-76.1%. Meanwhile, the catalyst is easy to separate and environmentally friendly and may be recycled for many times.

An acid addition salt of a ROCK inhibitor, and a crystal form, a composition and the pharmaceutical use thereof are provided. The acid addition salt is an acid addition salt of compound A and any one of the following acids: hydrochloric acid, p-toluenesulfonic acid, benzenesulfonic acid, maleic acid, tartaric acid, oxalic acid, fumaric acid, sulfuric acid, methanesulfonic acid, phosphoric acid, succinic acid or citric acid (A). The acid addition salt of compound A and the crystal form thereof have the characteristics of high solubility, good stability, high purity, few impurities and high bioequivalence, and are beneficial for the storage, quality control and druggability of drugs.

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An acid addition salt of a ROCK inhibitor, and a crystal form, a composition and the pharmaceutical use thereof are provided. The acid addition salt is an acid addition salt of compound A and any one of the following acids: hydrochloric acid, p-toluenesulfonic acid, benzenesulfonic acid, maleic acid, tartaric acid, oxalic acid, fumaric acid, sulfuric acid, methanesulfonic acid, phosphoric acid, succinic acid or citric acid (A). The acid addition salt of compound A and the crystal form thereof have the characteristics of high solubility, good stability, high purity, few impurities and high bioequivalence, and are beneficial for the storage, quality control and druggability of drugs.

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The invention concerns compounds of Formula (I)

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or pharmaceutically-acceptable salts thereof, wherein R.sup.1 to R.sup.5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.

The invention concerns compounds of Formula (I)

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or pharmaceutically-acceptable salts thereof, wherein R.sup.1 to R.sup.5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

The present invention relates a new process to synthesize 1-((4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxyquinolin-7-yloxy)methyl)cyclopropanamine (AL3818). A stable crystalline form of Al3818 has been prepared. Salts and their crystalline forms of AL3818 have been also prepared. Anti-cancer and optometric activities of AL3818 and its salts have been further tested. New process has been outlined in Scheme I.

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