Deazapurines and uses thereof

Assignee: Eisai R&D Management Co., Ltd.

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Quick Facts

Patent No.: US 7,868,002
App. No.: 11/906,056
Granted: Jan 11, 2011
Kind: B2

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Abstract

As discussed above, there remains a need for the development of novel therapeutic agents useful for treating inflammatory or autoimmune and proliferative diseases. The present invention provides novel compounds of general formula (I), and pharmaceutical compositions thereof, as described generally and in classes and subclasses herein, as well as methods of making and using such compounds.

Claims (834)

1. A pharmaceutical composition comprising a compound having the structure (I):

or a pharmaceutically acceptable salt, ester or salt of such ester thereof;

wherein n is an integer from 0-4;

R 1 is hydrogen, —NH 2 , —NHMe, —NHAc, —OH, F, —OMe, —CN, or —NH(C═O)OEt;

R 2 is hydrogen, —NR A R B , —OR A , an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, wherein R A and R B are each independently hydrogen or an aliphatic, heteroaliphatic, aryl or heteroaryl moiety;

each occurrence of R 3 is independently hydrogen, halogen, cyano, or an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or a group —G-R C , wherein G is absent or is —CH 2 —, —NR D —, —O—, or (C═O), and wherein R C is hydrogen, —NR F R G , —OR F , —SR F , or an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, wherein R D , R F and R G are each independently hydrogen, —NR x R y , an aliphatic, cycloaliphatic, heteroaliphatic, cycloheteroaliphatic, aryl, or heteroaryl moiety, an acyl moiety substituted with an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or wherein R D and R C or R F and R G taken together are a 3-, 4-, 5-, 6-, 7- or 8-membered substituted or unsubstituted cycloaliphatic or cycloheteroaliphatic moiety; wherein each occurrence of R x and R y is independently hydrogen, an aliphatic, cycloaliphatic, heteroaliphatic, cycloheteroaliphatic, aryl, or heteroaryl moiety, an acyl moiety substituted with an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or wherein R x and R y taken together are a 4-, 5- or 6-membered substituted or unsubstituted, saturated or unsaturated cycloaliphatic or cycloheteroaliphatic moiety;

whereby each of the foregoing aliphatic or heteroaliphatic moieties may be independently substituted or unsubstituted, cyclic or acyclic, linear or branched, saturated or unsaturated and wherein each of the foregoing aryl or heteroaryl moieties may be independently substituted or unsubstituted; and

a pharmaceutically acceptable carrier or diluent; and optionally further comprising an additional therapeutic agent.

2. The pharmaceutical composition of claim 1 , wherein the compound has the structure:

wherein R 3a and R 3b are each independently hydrogen, halogen, cyano, or an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or a group —G-R C , wherein G is absent, —CH 2 —, —NR D —, —O—, or (C═O), and wherein R C is hydrogen, —NR F R G , —OR F , —SR F , or an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, wherein R D , R F and R G are each independently hydrogen, —NR x R y , an aliphatic, cycloaliphatic, heteroaliphatic, cycloheteroaliphatic, aryl, or heteroaryl moiety, an acyl moiety substituted with an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or wherein R D and R C or R F and R G taken together are a 3-, 4-, 5-, 6-, 7- or 8-membered substituted or unsubstituted cycloaliphatic or cycloheteroaliphatic moiety: wherein each occurrence of R x and R y is independently hydrogen, an aliphatic, cycloaliphatic, heteroaliphatic, cycloheteroaliphatic, aryl, or heteroaryl moiety, an acyl moiety substituted with an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or wherein R x and R y taken together are a 4-, 5- or 6-membered substituted or unsubstituted, saturated or unsaturated cycloaliphatic or cycloheteroaliphatic moiety;

whereby each of the foregoing aliphatic or heteroaliphatic moieties may be independently substituted or unsubstituted, cyclic or acyclic, linear or branched, saturated or unsaturated; and wherein each of the foregoing aryl or heteroaryl moieties may be independently substituted or unsubstituted.

3. The pharmaceutical composition of claim 1 , wherein the compound has the structure:

wherein R 3a and R 3b are each independently hydrogen, halogen, cyano, or an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or a group —G-R C , wherein G is absent, —CH 2 —, —NR D —, —O—, or (C═O), and wherein R C is hydrogen, —NR F R G , —OR F , —SR F , or an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, wherein R D , R F and R G are each independently hydrogen, —NR x R y , an aliphatic, cycloaliphatic, heteroaliphatic, cycloheteroaliphatic, aryl, or heteroaryl moiety, an acyl moiety substituted with an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or wherein R D and R C or R F and R G taken together are a 3-, 4-, 5-, 6-, 7- or 8-membered substituted or unsubstituted cycloaliphatic or cycloheteroaliphatic moiety; wherein each occurrence of R x and R y is independently hydrogen, an aliphatic, cycloaliphatic, heteroaliphatic, cycloheteroaliphatic, aryl, or heteroaryl moiety, an acyl moiety substituted with an aliphatic, heteroaliphatic, aryl or heteroaryl moiety, or wherein R x and R y taken together are a 4-, 5- or 6-membered substituted or unsubstituted, saturated or unsaturated cycloaliphatic or cycloheteroaliphatic moiety;

whereby each of the foregoing aliphatic or heteroaliphatic moieties may be independently substituted or unsubstituted, cyclic or acyclic, linear or branched, saturated or unsaturated; and wherein each of the foregoing aryl or heteroaryl moieties may be independently substituted or unsubstituted.

4. The pharmaceutical composition of claim 1 , wherein the compound has the structure: