The invention relates to new compounds of formula (I) that are useful in medicine, specifically in treating or preventing cancerous diseases in a mammal, to pharmaceutical compositions comprising such compounds, optionally together with other pharmaceutically active compounds, or to pharmaceutical formulations comprising such compounds or pharmaceutical compositions. The invention further relates to methods of making these compounds.

The invention relates to new compounds of formula (I) that are useful in medicine, specifically in treating or preventing cancerous diseases in a mammal, to pharmaceutical compositions comprising such compounds, optionally together with other pharmaceutically active compounds, or to pharmaceutical formulations comprising such compounds or pharmaceutical compositions. The invention further relates to methods of making these compounds.

Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

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Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer.

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The present invention relates to a process for preparing C.sub.4-C.sub.15 lactams, in which a C.sub.1-C.sub.10-alkyl nitrite is reacted with a C.sub.4-C.sub.15-cycloalkane and is illuminated with a light-emitting diode during the reaction. This forms a C.sub.4-C.sub.15-cyclohexanone oxime which is then converted further to a C.sub.4-C.sub.15 lactam; the C.sub.1-C.sub.10 alcohol formed is recycled into the preparation of the C.sub.1-C.sub.10-alkyl nitrite.

The present invention relates to a process for preparing C.sub.4-C.sub.15 lactams, in which a C.sub.1-C.sub.10-alkyl nitrite is reacted with a C.sub.4-C.sub.15-cycloalkane and is illuminated with a light-emitting diode during the reaction. This forms a C.sub.4-C.sub.15-cyclohexanone oxime which is then converted further to a C.sub.4-C.sub.15 lactam; the C.sub.1-C.sub.10 alcohol formed is recycled into the preparation of the C.sub.1-C.sub.10-alkyl nitrite.

The present invention relates to a preparation method of a long-chain compound, which includes the following steps: (1) carrying out condensation reaction on HR.sub.2 and R.sub.5N-Glu(OR.sub.4)OR.sub.3, wherein, R.sub.3 is a carboxyl protecting group, R.sub.4 is a carboxyl activating group, and R.sub.5 is an amino protecting group; obtaining a compound of formula II; (2) removing carboxyl protecting group R.sub.3 and amino protecting group R.sub.5 of the compound shown in formula II to obtain a compound of formula III; (3) carrying out condensation reaction on the compound shown in formula III and

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to obtain a compound shown in formula I. The method reduces the time of deprotection, and all the reactions can be carried out in a solvent with low boiling point. The post-processing requires only simple washing and recrystallization to obtain the product with higher purity, so the method is suitable for large-scale production.

The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.

The present invention relates to novel amidoheteroaryl aroyl hydrazide ethynes as tyrosine kinase inhibitors, process of preparation thereof, and use of the compounds for preparation of pharmaceutical compositions in the therapeutic treatment of disorders related to tyrosine kinases in humans.

A process for making ixazomib citrate of formula VI comprising reacting a compound of formula V with citric acid to form ixazomib citrate of formula VI: ##STR00001## wherein R is hydrogen or an amide protecting group.