Thiazolones for use as pi3 kinase inhibitors
OwnerDashyant Dhanak, Steven David Knightinventors
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Abstract
Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of substituted thiazolones.
Claims15
1-13. (canceled)
A method of inhibiting one or more phosphatoinositides 3-kinases (PI3Ks) in a mammal;
- comprising administering to the mammal a therapeutically effective amount of a compound of Formula (I):
- in which
- R is C3-6 cycloalkyl or naphtyl;
- or
- R is
- in which R1 is hydrogen, halogen, —C1-6alkyl, —SC1-6alkyl, —OC1-6alkyl, —NO2, —S(═O)—C1-6alkyl, —OH, —CF3, —CN, —CO2H, —OCF3, or —CO2C1-6alkyl;
- and R2 and R3 are independently hydrogen, halogen, —C1-6 alkyl, —SC1-6alkyl, —OC1-6alkyl, —NO2, —S(═O)—C1-6alkyl, —OH, —CF3, —CN, —CO2H, —CO2C1-6alkyl, —CONH2, —NH2, —OCH2(C═O)OH, —OCH2CH2OCH3, —SO2NH2, —CH2SO2CH3, —NH(C═NH)CH3;
- or R2 and R3 can independently be a radical of the formula
- in which q is one or two;
- R4 is hydrogen, halogen, or —SO2NH2;
- or
- R is —(CH2)n—NRkRl in which n is 2 or 3, and Rk and Rl are independently —C1-6alkyl;
- or —NRkRl together form
- R is
- Q is
- in which R5 is hydrogen, phenyl optionally substituted with up to three C1-6 alkyl or halogen, or C1-6 alkyl or
- Q is
- in which Y is CH;
- and A and B together are a part of
- provided that ortho position to Y is N or O;
- or
- Q is
- in which Y is N or CH;
- J is hydrogen, NH2, OH or —OC1-6alkyl;
- and L is hydrogen, NH2, halogen, —NO2, or —OC1-6alkyl,
- and/or a pharmaceutically acceptable salt, hydrate, solvate or pro-drug thereof.
A method of treating cancer comprises co-administration a compound of formula I and/or a pharmaceutically acceptable salt, hydrate, solvate or pro-drug thereof and at least one anti-neoplastic agent, such as one selected from the group consisting of anti-microtubule agents, platinum coordination complexes, alkylating agents, antibiotic agents, topoisomerase II inhibitors, antimetabolites, topoisomerase I inhibitors, hormones and hormonal analogues, signal transduction pathway inhibitors, non-receptor tyrosine kinase angiogenesis inhibitors, immunotherapeutic agents, proapoptotic agents, and cell cycle signaling inhibitors.
A method of claim one wherein the compound of formula (I), and/or a pharmaceutically acceptable salt, hydrate, solvate or pro-drug thereof, is administered in a pharmaceutical composition.
Dependencies are inferred from the claim text.