C07D239/95

Kinase inhibitors and their uses

The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

Kinase inhibitors and their uses

The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein kinase and treat and/or prevent diseases associated with inappropriate kinase activity.

Preparation method for morpholinquinazoline compound and intermediates thereof

The present disclosure relates to a preparation method morpholinquinazoline compound and a midbody thereof. The preparation method for morpholinquinazoline compound comprises the following steps: S1, performing a Suzuki reaction of compound S and compound IV as represented by the following formula, so as to obtain compound V; step S2, performing a reaction of methylsufonyl chloride and compound V in an organic solvent as represented by the following formula, so as to obtain compound VI; and S3, performing a coupled reaction of compound VII and compound VI in a solvent as represented by the following formula, so as to obtain compound YY-20394. The preparation method has the advantages of higher yield, better selectivity, simple operation and mild reaction condition, and is applicable to industrial production. ##STR00001##

Preparation method for morpholinquinazoline compound and intermediates thereof

The present disclosure relates to a preparation method morpholinquinazoline compound and a midbody thereof. The preparation method for morpholinquinazoline compound comprises the following steps: S1, performing a Suzuki reaction of compound S and compound IV as represented by the following formula, so as to obtain compound V; step S2, performing a reaction of methylsufonyl chloride and compound V in an organic solvent as represented by the following formula, so as to obtain compound VI; and S3, performing a coupled reaction of compound VII and compound VI in a solvent as represented by the following formula, so as to obtain compound YY-20394. The preparation method has the advantages of higher yield, better selectivity, simple operation and mild reaction condition, and is applicable to industrial production. ##STR00001##

Small molecules for the treatment of autoimmune diseases and cancer

Disclosed herein are quinazolinyl compounds, compositions, and methods of use thereof. The compounds may be used in the treatment of autoimmune disorders or cancer.

S-substituted quinazolines and their therapeutic applications for the treatment of diseases mediated by PDE7

The present invention relates to a family of S-substituted quinazoline derivatives that inhibitors of the enzyme phosphodiesterase 7 (PDE7), useful for the treatment or prevention of diseases mediated by said enzyme, especially inflammatory, neurodegenerative, neurological, psychiatric and/or autoimmune diseases.

S-substituted quinazolines and their therapeutic applications for the treatment of diseases mediated by PDE7

The present invention relates to a family of S-substituted quinazoline derivatives that inhibitors of the enzyme phosphodiesterase 7 (PDE7), useful for the treatment or prevention of diseases mediated by said enzyme, especially inflammatory, neurodegenerative, neurological, psychiatric and/or autoimmune diseases.

Quinazolines as potassium ion channel inhibitors

A compound of formula I ##STR00001##
wherein A, X, Y, Z, R.sub.1 and R.sub.24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I.sub.Kur-associated disorders, and other disorders mediated by ion channel function.

Quinazolines as potassium ion channel inhibitors

A compound of formula I ##STR00001##
wherein A, X, Y, Z, R.sub.1 and R.sub.24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, I.sub.Kur-associated disorders, and other disorders mediated by ion channel function.

METHODS AND COMPOSITIONS FOR INHIBITION OF RAS

Inhibitors of Ras protein, methods to modulate the activity of Ras protein, and methods of treatment of disorders mediated by Ras protein are provided. A method for regulating activity of a K-Ras, H-Ras or N-Ras mutant protein with a compound is described. Disorders that can be treated include cancer, such as hematological cancer, pancreatic cancer, MYH associated polyposis, colorectal cancer, or lung cancer.