Back to results
US 2006/0135591 A1Published application
Modulators of CRTH2 activity
AssigneeMicrobia, Inc.
InventorsYueh-Tyng Chien, G. Milne, Mark Currie, John Talley, Brian Cali, Barbara Chen, Craig Zimmerman, Jing Yang
Life of this patent
Estimating the term…
Abstract
Modulators of the CRTH2 receptor and their use in the treatment of various disorders, including asthma are described.
Claims68
A compound having the formula:
- wherein:
- A is
- R is H, a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- n is 1, 2, 3 or 4;
- R1 is H;
- a C1-C6 alkyl, optionally independently substituted with one or more —OH, —NH2, or halogen;
- or a C1-C6 alkenyl optionally independently substituted with one or more —OH, —NH2 or halogen;
- R2 is H;
- a C1-C6 alkyl, optionally independently substituted with one or more halogen;
- or a C1-C6 alkenyl optionally independently substituted with one or more halogen;
- R3 is a halogen;
- —CN;
- —OH;
- —SH;
- a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- —OR3A;
- —SR3A;
- —SOR3A;
- or —S(O)2R3A, wherein R3A is a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- m is 0, 1, 2, 3, 4 or 5;
- R4 is H or a halogen;
- R5 is H or a halogen;
- Y and Y′ are both H or Y and Y′ taken together are O or Y and Y′ taken together are S;
- X is O, S, or —NR6, wherein R6 is a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- and
- R7 is —OH, —OR7A;
- or R7A, wherein R7A is:
- H or a C1 to C6 (C1, C2, C3, C4, C5, C6) alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or arylalkyl optionally independently substituted with one or more halogen —OH, —C(O)OH, or —NH3.
25 more elements
The compound of claim, 1, 2 or 6 wherein Y and Y′ are both H.
A compound having the formula:
- wherein:
- A is
- R is H, a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- n is 1, 2, 3 or 4;
- R1 is H;
- a C1-C6 alkyl, optionally independently substituted with one or more —OH, —NH2, or halogen;
- or a C1-C6 alkenyl optionally independently substituted with one or more —OH, —NH2 or halogen;
- R2 is H;
- a C1-C6 alkyl, optionally independently substituted with one or more halogen;
- or a C1-C6 alkenyl optionally independently substituted with one or more halogen;
- R3 is a halogen;
- —CN;
- —OH;
- —SH;
- a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- —OR3A;
- —SR3A;
- —SOR3A;
- or —S(O)2R3A, wherein R3A is a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- m is 0, 1, 2, 3, 4, or 5;
- R4 is H or a halogen;
- R5 is H or a halogen;
- Y and Y′ are both H or Y and Y′ taken together are O or Y and Y′ taken together are S;
- X is O, S, or —NR6, wherein R6 is a C1-C3 alkyl, optionally independently substituted with one or more halogen;
- and
- R7 is —OH, —OR7A;
- or R7A, wherein R7A is:
- H or a C1 to C6 (C1, C2, C3, C4, C5, C6) alkyl, alkenyl, alkynyl, aryl, cycloalkyl, or arylalkyl optionally independently substituted with one or more halogen —OH, —C(O)OH, or —NH3;
- provided that if A is
- n is 1, R1 is H, Y is O, R2 is —CH3, R4 is H, R5 is H and R is —CH3, then R3 is not:
- Cl, H, F or —CF3;
- further provided that if A is
- n is 1, R1 is H, Y is O, R2 is —CH3, R4 is H, R5 is H, R is H, then R3 is not H;
- further provided that
- when A is
- n is 1, R1 is H, Y is O, R2 is —CH3, R4 is F, R5 is H, R is —CH3, R3 is not H;
- and further provided that when A is
- n is 1, R1 is H, Y is O, R2 is —CH3, R4 is H, R5 is H, then R is not H.
35 more elements
Dependencies are inferred from the claim text.