Phosphorus imidazoquinoline amine derivatives, pharmaceutical compositions and therapeutic methods thereof
AssigneeCanWell Biotech Limited
InventorNinghui Yu
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Abstract
The invention provides novel phosphorus imidazoquinoline amine derivatives, having agonistic activities to Toll-like receptors (TLRs), in particular TLR7 and/or TLR8, pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by or associated with TLR7 and/or TLR8, e.g., cancer, graft rejection, autoimmunity, inflammation allergy, asthma, infection, sepsis, and immunodeficiency.
Claims14
A unit dosage form comprising a compound having the structural formula of (I):
- or a pharmaceutically acceptable form or an isotope derivative thereof, wherein,
- R1 is a C1-C8 alkyl group;
- R2 is (CH2)m, wherein m is an integer selected from 1 to 8;
- L is a linking moiety;
- R3 is a H, or C1-C32 alkyl group;
- and
- each of R4 and R5 is independently a C1-C6 aliphatic group;
- provided that R4 and R5, together with atoms to which they are bonded to, may optionally form a 5- to 7-membered aliphatic ring.
A method for treating or reducing a condition or disorder treatable by modulation of TLR7- and/or TLR8-mediated cellular activities, comprising administering to a subject in need thereof a pharmaceutical composition comprising a compound having the structural formula of (I):
- or a pharmaceutically acceptable form or an isotope derivative thereof, wherein,
- R1 is a C1-C8 alkyl group;
- R2 is (CH2)m, wherein m is an integer selected from 1 to 8;
- L is a linking moiety;
- R3 is a H, or C1-C32 alkyl group;
- and
- each of R4 and R5 is independently a C1-C6 aliphatic group;
- provided that R4 and R5, together with atoms to which they are bonded to, may optionally form a 5- to 7-membered aliphatic ring.
Dependencies are inferred from the claim text.