C07D239/72

BIARYL KINASE INHIBITORS

The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.

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Sulfoximine substituted quinazolines for pharmaceutical compositions
10167296 · 2019-01-01 · ·

The application relates to novel sulfoximine substituted quinazoline derivatives of formula ##STR00001##
wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

Sulfoximine substituted quinazolines for pharmaceutical compositions
10167296 · 2019-01-01 · ·

The application relates to novel sulfoximine substituted quinazoline derivatives of formula ##STR00001##
wherein Ar, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description and claims, and their use as MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) kinase inhibitors, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of MNK1 (MNK1a or MNK1b) and/or MNK2 (MNK2a or MNK2b) mediated disorders.

INHIBITORS OF THE FIBROBLAST GROWTH FACTOR RECEPTOR

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.

CONTROLLED RELEASE COMPOSITIONS OF AGENTS THAT REDUCE CIRCULATING LEVELS OF PLATELETS AND METHODS THEREFOR
20180153810 · 2018-06-07 ·

Provided are prophylactic and therapeutic methods of treatment of subjects for the purpose of inhibiting vaso-occlusive events, including embolism, by administering agents, including anagrelide and anagrelide derivatives, which reduce the number of circulating platelets to low normal or to below normal levels. Methods and pharmaceutical preparations comprising such agents are provided.

Substituted Pyrazole Compounds Containing Pyrimidine and Preparation Method and Use Thereof

Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I:

##STR00001##

The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity,and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.

Substituted Pyrazole Compounds Containing Pyrimidine and Preparation Method and Use Thereof

Disclosed are substituted pyrazole compounds containing pyrimidinyl as shown in Formula I:

##STR00001##

The definitions of each of the substituents can be seen in the description. The compounds of present invention have a good spectrum of bactericidal, insecticidal and acaricidal activity,and have good control effect on downy mildew of cucumber, powdery mildew of wheat, corn rust, rice blast, cucumber anthracnosis and the like. The compounds of present invention also show good insecticidal activity.

ARYLQUINAZOLINES

The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation.

ARYLQUINAZOLINES

The invention relates to novel compounds of the formula (I) which can be used for the inhibition of serine-threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation.

Process for the Preparation of Amorphous Idelalisib and its Premix

Processes for the preparation of amorphous idelalisib are provided. Processes for the preparation of a premix of amorphous idelalisib are also provided.