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US 10,370,338 B2Granted
Benzazepine dicarboxamide compounds with tertiary amide function
AssigneeHoffmann-La Roche Inc.
InventorsLisha Wang, Hongying Yun, Weixing Zhang, Wei Zhu, Zhiwei Zhang
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Abstract
This invention relates to new benzazepine dicarboxamide compounds of the formula wherein R1 to R3 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are TLR agonists and may therefore be useful as medicaments for the treatment of diseases such as cancer, autoimmune diseases, inflammation, sepsis, allergy, asthma, graft rejection, graft-versus-host disease, immunodeficiencies, and infectious diseases.
Claims21
A benzazepine-4-carboxamide compound of the formula
- wherein
- R1 is C3-7-alkyl;
- R2 is C3-7-alkyl or C3-7-cycloalkyl-C1-7-alkyl;
- R3 is a heterocycle selected from
- wherein
- X1 is (CH2)m wherein m is 1 or 2;
- X2 is (CH2)n wherein n is 1 or 2;
- X3 is (CH2)o wherein o is 1 or 2;
- X4 is (CH2)p wherein p is 1 or 2;
- and
- Z1 is phenyl, wherein phenyl is unsubstituted or substituted by one or two groups selected from the group consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkyl-amino-C1-7-alkyl and di-C1-7-alkyl-amino-C1-7-alkyl;
- or
- wherein
- X5 is (CH2)q wherein q is 1 or 2;
- X6 is (CH2)r wherein r is 1 or 2;
- Y1 is a carbon or nitrogen atom and
- Z2 is hydrogen and
- Z3 is selected from the group consisting of hydrogen, C1-7-alkoxy, C2-7-alkenyloxy, phenyl, phenyl-C1-7-alkyl, phenyl-C1-7-alkyloxy, phenyl-C1-7-alkylamino, phenylamino-C1-7-alkyl, phenylamino, wherein phenyl is unsubstituted or substituted by one or two groups selected from the group consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkyl-amino-C1-7-alkyl and di-C1-7-alkyl-amino-C1-7-alkyl;
- wherein
- X7 is (CH2)s wherein s is 1 or 2;
- and
- Z4 is phenyl, wherein phenyl is unsubstituted or substituted by one or two groups selected from the group consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkyl-amino-C1-7-alkyl and di-C1-7-alkyl-amino-C1-7-alkyl;
- or
- wherein
- X8 is (CH2)t wherein t is 1 or 2;
- and
- Z5 is phenyl, wherein phenyl is unsubstituted or substituted by one or two groups selected from the group consisting of C1-7-alkyl, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, hydroxy-C1-7-alkyl, amino-C1-7-alkyl, C1-7-alkyl-amino-C1-7-alkyl and di-C1-7-alkyl-amino-C1-7-alkyl,
- or a pharmaceutically acceptable salt thereof.
25 more elements
Dependencies are inferred from the claim text.