Cyclopentathiophene carboxamide derivatives as platelet activating factor receptor antagonists
AssigneeBoehringer Ingelheim International GmbH
InventorsMatthias Eckhardt, Marina Kristina Willwacher, Juergen Prestle, Ferenc Kontes, Leo Thomas, Christofer Siegfried Tautermann, Dieter Wiedenmayer
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Abstract
The invention relates to cyclopentathiophene carboxamides of formula (I.0) wherein R1, R2, R3, R4, and n are as defined herein, and pharmaceutically acceptable salts thereof. The invention also relates to the use of the cyclopentathiophene carboxamides of formula (I.0) for the treatment of diseases which can be influenced by antagonizing the activity mediated by the platelet activating factor receptor.
Claims34
A compound of formula (I.1)
- wherein
- R1 is selected from the group consisting of C1-4-alkyl optionally substituted with 1 to 3 F and of C3-4-cycloalkyl;
- R2 is selected from the group consisting of F, Cl, Br, I, C1-4-alkyl, C3-4-cycloalkyl, —CN, —CONH2, —CONH(C1-4-alkyl), —CON(C1-4-alkyl)2, —COOH, —COO—C1-4-alkyl, OH, —O—C1-4-alkyl, and S(O)r—C1-4-alkyl with r=0, 1, or 2;
- wherein
- the C1-4-alkyl R2 group may be optionally substituted with 1 to 3 F or optionally substituted with 1 —CN, with 1 OH, or with 1 —O—C1-4-alkyl, and
- the —O—C1-4-alkyl R2 group may be optionally substituted with 1 to 3 F;
- n is selected from the group consisting of 0, 1, 2, and 3;
- R3 and R4, together with the amide N atom they are attached to, form a heterocyclyl selected from the group consisting of
- or a pharmaceutically acceptable salt thereof.
A compound selected from the group consisting of:
- 2
- 4
- 5
- 6
- 26
- 27
- 64
- 69
- and
- 76
- or a pharmaceutically acceptable salt thereof.
Compound
Compound
Compound
Compound
Compound
A pharmaceutically acceptable salt of compound
A pharmaceutically acceptable salt of compound
A pharmaceutically acceptable salt of compound
A pharmaceutically acceptable salt of compound
A pharmaceutically acceptable salt of compound
Dependencies are inferred from the claim text.