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US 10,308,629 B2Granted
1H-pyrrol-3-amines
AssigneeBayer Pharma Aktiengesellschaft
InventorsKeith Graham, Ulrich Klar, Hans Briem, Gerhard Siemeister, Ursula Mönning
Life of this patent
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Abstract
Compounds of formula (I) as described herein, processes for their production and their use as pharmaceuticals.
Claims8
A compound of formula (I),
- wherein:
- G is a group selected from the group consisting of:
- wherein * indicates the points of attachment of said group with the rest of the molecule;
- X is CH2, CHORx, or C═O;
- Rx is hydrogen or C1-C6-alkyl;
- R1 is hydrogen or C1-C6-alkyl;
- R2 is hydrogen, C1-C6-alkyl, R10—O—C(O)— or R7R8N—C(O)—;
- R3 is hydrogen or C1-C6-alkyl;
- A is a group selected from the group consisting of:
- wherein * indicates the point of attachment of said group to the rest of the molecule and said group is optionally substituted, one or more times, independently from each other, with R4;
- R4 is halogen, hydroxy, nitro, cyano, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1- C4-haloalkoxy, C1-C4-hydroxyalkyl, C1-C4-alkyl-C(O)—, R10—O—C(O)—, R7R8N—C(O)—, C1-C4-alkyl-C(O)—NH—, R7R8N—, or R7R8N—SO2—;
- E is a group
- wherein * indicates the point of attachment of said group to the rest of the molecule;
- each R5 is independently halogen, hydroxy, nitro, cyano, R9R10N—, (R13—C(O)—)(R14—C(O)—)N—, C1-C4-alkyl, C3-C6-cycloalkyl, C1-C6-alkoxy, C1-C4-haloalkyl, C1-C6-haloalkoxy, R6—C(O)—NR9—, R6—O—C(O)—NR9—, R6—SO2—NR9— or R7R8N—C(O)—NR9—;
- Q is O or N—OH;
- each R6 is independently C1-C6-alkyl, C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl or heteroaryl,
- wherein said C1-C6-alkyl is optionally substituted, one or more times, independently from each other, with halogen, hydroxy, nitro, cyano, C1-C4-alkoxy, C1-C4-haloalkoxy, C3-C6-cycloalkyl, R7R8N— or phenyl optionally substituted, one or more times, independently from each other, with R4,
- wherein said C3-C6-cycloalkyl, 4- to 6-membered heterocycloalkyl, phenyl or heteroaryl groups are optionally substituted, one or more times, independently from each other, with halogen, hydroxy, nitro, cyano, C1-C6-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, R10—O—C(O)— or C1-C4-haloalkoxy;
- R7 and R8 are independently hydrogen, C1-C6-alkyl, C3-C6-cycloalkyl, R10—O—C(O)— or phenyl,
- wherein said C1-C6-alkyl is optionally substituted, one or more times, independently from each other, with halogen, hydroxy, C1-C4-alkoxy, C1-C4-haloalkoxy, C3-C6-cycloalkyl optionally substituted one time with hydroxy, 4- to 6-membered heterocycloalkyl, heteroaryl, or R9R10N—,
- wherein said phenyl group is optionally substituted, one or more times, independently from each other, with R4;
- or,
- R7 and R8 together with the nitrogen atom to which they are attached form a 4- to 7-membered nitrogen containing heterocyclic ring, optionally containing one additional heteroatom selected from the group consisting of O, NR9 and S, and which may be optionally substituted one or more times, independently from each other, with R12;
- whereby when two R12 substituents are attached to the same ring carbon atom, together with the carbon atom to which they are attached, can be linked to one another in such a way that they jointly form a cyclobutane, azetidine, or oxetane group;
- said azetidine being optionally substituted one time with C1-C3-alkyl,
- or,
- R7 and R8 together with the nitrogen atom to which they are attached form a group selected from:
- wherein * indicates the point of attachment of said group to the rest of the molecule,
- R9 is hydrogen, or C1-C6-alkyl;
- R10 is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl;
- R12 is halogen, hydroxy, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl, C1-C4-haloalkoxy, or R9R10N—;
- R13 and R14 are independently C1-C4-alkyl, or C3-C6-cycloalkyl,
- wherein said C3-C6-cycloalkyl is optionally substituted, one or more times, independently from each other, with halogen;
- and
- m is 0, 1 or 2,
- or an N-oxide, a salt, a tautomer or a stereoisomer of said compound, or a salt of said N-oxide, tautomer or stereoisomer.
33 more elements
Dependencies are inferred from the claim text.