The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.

The present invention relates to enzyme inhibitors. More specifically, the present invention relates to ligand-directed covalent modification of proteins; method of designing same; pharmaceutical formulation of same; and method of use.

Compounds and methods for treating diseases mediated by a P2X.sub.3 and/or a P2X.sub.2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined herein.

Compounds and methods for treating diseases mediated by a P2X.sub.3 and/or a P2X.sub.2/3 receptor antagonist, the methods comprising administering to a subject in need thereof an effective amount of a compound of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, solvate or prodrug thereof, wherein X is O, D, Y, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are as defined herein.

Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I through IV are disclosed.

Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I through IV are disclosed.

The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

The present invention relates to diazine and triazine compounds having activity as Interleukin inhibitors, particularly Interleukin-1 beta, 2, 4, 6, 8, 13 and 17, and to the compounds for use in the treatment of associated disorders, particularly Alzheimer's Disease, Parkinson's Disease, Asthma, and solid organ transplant rejection.

The present invention relates to diazine and triazine compounds having activity as Interleukin inhibitors, particularly Interleukin-1 beta, 2, 4, 6, 8, 13 and 17, and to the compounds for use in the treatment of associated disorders, particularly Alzheimer's Disease, Parkinson's Disease, Asthma, and solid organ transplant rejection.