Therapeutic morpholino-substituted compounds

Details Therapeutic morpholino-substituted compounds Therapeutic morpholino-substituted compounds

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/5377 (2006.01)

Patent

CA 2398163

Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders; neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer; and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

L'invention concerne des dérivés de pyridopyrimidine, de quinolone, et de benzopyranone, à substitution morpholino, inhibant la phosphoinositide 3-kinase (PI 3-kinase), une enzyme qui régule le processus d'adhésion plaquettaire. Les composés en question ont par conséquent une activité anti-thrombotique, ainsi que d'autres propriétés pharmaceutiques. L'invention concerne les composés représentés par les formules générales (I), (II) et (III). La PI 3-kinase génère des seconds messagers de la PI 3-phosphorylée qui stimulent l'adhésion plaquettaire dans le débit sanguin. Etant donné que l'adhésion plaquettaire est une étape nécessaire dans la formation d'un thrombus, l'inhibition par ces composés de la PI 3-kinase dans ces conditions permet d'inhiber ou d'empêcher la formation d'un thrombus. Ces composés sont utiles dans le traitement d'états dépendant de la PI 3-kinase, y compris les maladies cardio-vasculaires, telle que l'occlusion des artères coronariennes, l'accident vasculaire cérébral, le syndrome coronarien aigu, l'infarctus aigu du myocarde, la resténose vasculaire, l'athérosclérose, et l'angine instable ; les maladies des voies respiratoires, tel que l'asthme, la bronchopneumopathie chronique obstructive (BPCO), et la bronchite ; les troubles inflammatoires ; les néoplasmes, y compris les cancers, tel que le gliome, le cancer de la prostate, le cancer pulmonaire à petites cellules, et le cancer du sein ; et les maladies liées au fonctionnement désordonné des globules blancs, telles que les maladies autoimmunes et inflammatoires.

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