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US 2011/0237565 A1Published application
Heterocyclic inhibitors of histamine receptors for the treatment of disease
AssigneeKalypsys, Inc.
InventorsAllen Borchardt, Robert Davis, Stewart A. Noble
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds and methods which may be useful as inhibitors of H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.
Claims57
A compound of structural Formula (I):
- or a salt thereof, wherein:
- the ring comprising X1-X5 is aromatic;
- X1 and X5 are independently chosen from C, CH and N;
- X2 is chosen from [C(R6)(R7)], NR8, O and S;
- X3 is chosen from [C(R9)(R10)], NR11, O, and S;
- X4 is chosen from [C(R12)(R13)], NR14, O and S;
- X6 is chosen from CR18 and N;
- X7 is chosen from CR19 and N;
- Y1 is chosen from a bond, lower alkyl, lower alkoxy, OR15, NR16R17, and lower aminoalkyl;
- Y2 is chosen from a bond, lower alkyl, lower alkoxy, OR20, NR21R22, S, S(O), S(O)2, S(O)2NH2, S(O)2NHR23, S(O)2NR23R24, C(O)NH2, C(O)NHR23, C(O)NR23R24 and lower aminoalkyl;
- R1 is selected from the group consisting of:
- aryl, heterocycloalkyl, cycloalkyl, and heteroaryl, any of which may be optionally substituted, when Y1 is a bond;
- and
- null, when Y1 is chosen from OR15, NR16R17, lower alkyl, lower alkoxy, or lower aminoalkyl;
- R2 is chosen from alkyl, aryl, cycloalkyl, heterocycloalkyl and heteroaryl, any of which may be optionally substituted;
- R6, R7, R9, R10, R12, R13, R18, and R19 are independently chosen from null, hydrogen, alkyl, alkynyl, heteroalkyl, alkoxy, halogen, haloalkyl, perhaloalkyl, amino, aminoalkyl, amido, carboxyl, acyl, hydroxy, cyano, nitro, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which may be optionally substituted;
- R8, R11, and R14 are independently chosen from null, hydrogen, alkyl, heteroalkyl, alkoxy, haloalkyl, perhaloalkyl, aminoalkyl, C-amido, carboxyl, acyl, hydroxy, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which may be optionally substituted;
- R15, R16, R20, and R21 are independently chosen from aminoalkyl, alkylaminoalkyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, ether, heterocycloalkyl, lower alkylaminoheterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which may be optionally substituted;
- R17 and R22 are independently chosen from hydrogen, aminoalkyl, alkylaminoalkyl aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, ether, heterocycloalkyl, lower alkylaminoheterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which may be optionally substituted;
- and
- R23 and R24 are independently chosen from hydrogen, alkyl, alkenyl, alkynyl, heteroalkyl, alkoxy, halogen, haloalkyl, perhaloalkyl, perhaloalkoxy, amino, aminoalkyl, amido, carboxyl, acyl, hydroxy, cyano, nitro, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl, heteroaryl, and heteroarylalkyl, any of which may be optionally substituted.
18 more elements
A compound chosen from Examples 1-90.
A pharmaceutical composition comprising Example 1-90, together with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.