Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase. ##STR00001##

Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase. ##STR00001##

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NRR, C.sub.1-7alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R and R are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R.sub.2 is hydrogen, NRR, C.sub.1-7alkyl, arylC.sub.1-7 alkyl or C.sub.3-10 cycloalkyl; R.sub.4 is amino, C.sub.1-7alkyl, C.sub.2-7 alkenyl, C.sub.3-10 cycloalkyl, C.sub.3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C.sub.1-7alkyl or C.sub.3-10 cycloalkyl-C.sub.1-7 alkyl; R.sub.5 is hydrogen or C.sub.1-7 alkyl, or R.sub.5 and R.sub.4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C.sub.1-7alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene; R.sub.6 is halogen, heteroaryl or aryl; R and R are each independently hydrogen, C.sub.1-7 alkyl-carbonyl or C.sub.1-7 alkyl; provided that R.sub.4 is not phenyl substituted with morpholino when R.sub.2 is H and R.sub.5 is H, and provided that when NR.sub.4R.sub.5 is piperazinyl, said NR.sub.4R.sub.5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.

The present invention provides compounds and methods for treating MKP-5 modulated disease. In certain embodiments, the MKP-5 modulated disease is a fibrotic disease.

The present invention provides compounds and methods for treating MKP-5 modulated disease. In certain embodiments, the MKP-5 modulated disease is a fibrotic disease.

Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.

Disclosed are a condensed ring derivative, and a preparation method, an intermediate, a pharmaceutical composition and a use thereof. The condensed ring derivative of the present invention has a significant inhibitive effect on URAT1, which can effectively alleviate or treat hyperuricemia and other related diseases.

The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.