Disclosed are macrocyclic compounds having the general Formula (I) or (II) and their tautomeric forms, stereoisomers, pharmaceutically acceptable salts, hydrates, solvates and prodrugs thereof, and their combination with suitable medicament, corresponding processes for the synthesis and pharmaceutical compositions and uses of compounds disclosed herein.

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The present invention relates to methods of preparing substituted indole derivatives of general formula (I):

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in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A and L are as defined herein, and intermediate compounds useful for preparing said compounds. These compounds are useful for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

The present invention relates to methods of preparing substituted indole derivatives of general formula (I):

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in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, A and L are as defined herein, and intermediate compounds useful for preparing said compounds. These compounds are useful for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

Disclosed are a compound as shown in formula (I), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.

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Disclosed are a compound as shown in formula (I), an optical isomer thereof and a pharmaceutically acceptable salt thereof, and the use of the compound as a KRAS inhibitor.

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Compounds having the formula I wherein R.sup.1, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders. ##STR00001##

Compounds having the formula I wherein R.sup.1, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders. ##STR00001##

The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.

The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to oxygen linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other disorders or conditions related to or associated with kinases.

An oxaazaquinazolin-7(8H)-ketone compound with a selective inhibition effect on KRAS gene mutation and pharmaceutically acceptable salts thereof, stereoisomers, solvent compounds or prodrugs (as shown in formula I or formula II, see the details of the definition to each group in the formulas in the specification), as well as the pharmaceutical composition containing the compound, and the application thereof in preparation of cancer medicine.

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