Tetrazole derivatives as TRPA1 inhibitors
AssigneeBoehringer Ingelheim International GmbH
InventorsFlorian Paul Christian Binder, Martin Thomas Fleck, Jens Willwacher
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Abstract
The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.
Claims34
A compound according to formula (I)
- wherein
- A is selected from the group consisting of phenyl, thiophenyl, benzothiophenyl or benzofuranyl, unsubstituted or substituted with one, two or three members of the group R3 consisting of halogen, C1-4-alkyl, C1-4-fluoroalkyl, C3-4-cycloalkyl, C3-4-cyclofluoroalkyl, O—C1-4-alkyl, O-cyclopropyl and NC—;
- or
- A is selected from the group consisting of
- R1 is selected from the group consisting of C1-4-alkyl, C1-4-fluoroalkyl, C3-6-cycloalkyl, R4—(H2C)m— and R5—(H2C)n—;
- wherein
- m is 1 or 2;
- n is 2;
- R4 is C3-6-cycloalkyl;
- R5 is —O—C1-4-alkyl or —O—C1-4-fluoroalkyl;
- R2 is selected from the group consisting of H, C1-4-alkyl, C3-6-cycloalkyl, C3-6-cyclofluoroalkyl, HO—C1-4-alkyl-, C1-4-fluoroalkyl, R6—(H2C)p—, R7—(H2C)q—, R6—(H(R8)C)p— and R7—(H(R9)C)q—;
- wherein
- p is 1 or 2;
- q is 2;
- R6 is selected from the group consisting of HO—C1-2-alkyl-, C3-6-cycloalkyl, C-morpholinyl, C-imidazolyl and C-pyrazolyl;
- wherein said C-pyrazolyl, C-imidazolyl and C-morpholinyl is unsubstituted or substituted with C1-4-alkyl or C1-4-fluoroalkyl;
- R7 is selected from the group consisting of C1-4-alkyl-O—, C1-4-fluoroalkyl-O—, C1-4-alkyl-S(O)2—, N-morpholinyl, N-imidazolyl and N-pyrazolyl;
- wherein said N-pyrazolyl, N-imidazolyl, N-morpholinyl is unsubstituted or substituted with C1-4-alkyl or C1-4-fluoroalkyl;
- R8 and R9 are independently selected from H or C1-4-alkyl;
- or a salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
- or a pharmaceutically acceptable salt thereof.
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
A compound having the following formula:
Dependencies are inferred from the claim text.