C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/517 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) A61P 37/00 (2006.01) C07D 239/70 (2006.01) C07D 405/04 (2006.01) C07D 405/06 (2006.01) C07D 409/04 (2006.01) C07D 409/06 (2006.01)
Patent
CA 2739250
Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed. These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
La présente invention concerne des composés pyrimidiques cycliques condensés, y compris leurs tautomères, et les sels, promédicaments, solvates et hydrates pharmaceutiquement acceptables de ceux-ci. Ces composés sont utiles dans des méthodes de traitement du cancer, car ils ciblent sélectivement les cellules cancéreuses via les voies du transporteur du folate couplé aux protons, du récepteur du folate alpha, et/ou du récepteur du folate bêta, ils inhibent la GARFTase dans les cellules cancéreuses, et ils ciblent sélectivement les macrophages activés chez un patient atteint d'une maladie auto-immune, telle que la polyarthrite rhumatoïde.
Gangjee Aleem
Matherly Larry H.
Bereskin & Parr Llp/s.e.n.c.r.l.,s.r.l.
Duquesne University Of The Holy Spirit
Wayne State University
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