3- substituted quinoline or quinoxaline derivatives and...

C - Chemistry – Metallurgy – 07 – D

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C07D 401/12 (2006.01) A61K 31/4709 (2006.01) A61K 31/506 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2680853

Substituted bicyclic heteroaryls having the structure: (I) or any pharmaceutically-acceptable salt thereof, wherein: X1 is C(R9) or N; X2 is C(R10) or N; Y is N(R11), O or S; which are useful to inhibit the biological activity of human PI3K.delta. and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110.delta. activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo- dysplastic syndrome (MDS) myeloproliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia ( T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

L'invention concerne des hétéroaryles bicycliques substitués et des compositions les contenant, pour le traitement d'une inflammation générale, de l'arthrite, des maladies rhumatoïdes, de l'arthrose, des troubles intestinaux inflammatoires, des troubles inflammatoires de l'AEil, des troubles de la vessie inflammatoires ou instables, du psoriasis, des troubles de la peau avec des composantes inflammatoires, d'infections inflammatoires chroniques y compris, sans s'y limiter, des maladies auto-immunitaires telles que le lupus érythémateux dissémine (LED), la myasthénie grave, la polyarthrite rhumatoïde, l'encéphalomyélite disséminée aiguë, le purpura thrombopénique idiopathique, la sclérose en plaques, le syndrome de Sjögren et l'anémie hémolytique auto-immune, les affections allergiques y compris toute forme d'hypersensibilité. La présente invention concerne également des procédés de traitement du cancer qui sont véhiculés, dépendent de ou sont associés à une activité de p110, y compris, sans s'y limiter, les leucémies, la leucémie myéloïde aiguë (AML), le syndrome myélo-dysplasique (SDM), les maladies myélo-prolifératives (MPD), la leucémie myéloïde chronique (CML), la leucémie lymphoblastique aiguë de lymphocyte T (T-ALL), la leucémie lymphoblastique aiguë de lymphocyte B (B-ALL), le lymphome non hodgkinien (NHL), le lymphome de lymphocyte B et les tumeurs solides, telles que le cancer du sein.

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