摘要:
The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.
摘要:
This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use. In particular, the compounds include embodiments in which Ring T is an imidazo[1,2-b]pyridazine ring system, Rings A and B are each aryl and L1 is —C(O)NR1— or —NR1C(O)—. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases.
摘要:
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
摘要:
This invention relates to compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.
摘要:
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of formula I: wherein the variables are as defined herein.
摘要:
This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which:A is absent or is —O—, —S— or —NR2—;Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M′ moiety may be saturated or unsaturated; each occurrence of x is independently an integer from 1-6; and the other variables are as defined herein.