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US 9,802,947 B2Granted
3-oxo-tetrahydro-furo[3,2-b]pyrrol-4(5H)-yl) derivatives II
AssigneeGrüNenthal GmbH
InventorsAntonio Nardi, Paul Ratcliffe, Tobias Craan, Torsten Hertrampf, Bernhard Lesch, Henning Steinhagen
Life of this patent
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Abstract
The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors exhibiting a pronounced CatK-inhibition, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Claims14
A compound of the general formula (I)
- wherein
- R1 represents H or F;
- X represents S or O;
- Y1 and Y2 independently represents CH or N;
- Z1, Z2, Z3, Z4 and Z5 independently represents CH or N,
- with the proviso that 1, 2 or 3 of Z1, Z2, Z3, Z4 and Z5 represent N;
- m denotes 0, 1 or 2;
- n denotes 0, 1, 2 or 3;
- each R2 and each R3 is independently selected from the group consisting of F;
- Cl;
- Br;
- CN;
- CF3;
- CF2H;
- CFH2;
- CF2Cl;
- CFCl2;
- C1-4-alkyl;
- C(═O)—(C1-4-alkyl);
- C(═O)—NH2;
- C(═O)—N(H)(C1-4-alkyl);
- C(═O)—N(C1-4-alkyl)2;
- OH;
- O—C1-4-alkyl;
- OCF3;
- OCF2H;
- OCFH2;
- OCF2Cl;
- OCFCl2;
- NH2;
- N(H)(C1-4-alkyl);
- N(C1-4-alkyl)2;
- N(H)—C(═O)—(C1-4-alkyl);
- N(C1-4-alkyl)-C(═O)—(C1-4-alkyl);
- N(H)—S(═O)2—(C1-4-alkyl);
- N(H)—C(═O)—NH2;
- N(H)—C(═O)—N(H)(C1-4-alkyl);
- N(H)—C(═O)—N(C1-4-alkyl)(C1-4-alkyl);
- S—(C1-4-alkyl);
- S(═O)—(C1-4-alkyl);
- S(═O)2—(C1-4-alkyl);
- S(═O)2—N(H)(C1-4-alkyl);
- cyclopropyl;
- O-cyclopropyl;
- NH-cyclopropyl;
- N(H)—C(═O)-cyclopropyl;
- S(═O)-(cyclopropyl) and S(═O)2-(cyclopropyl);
- wherein the above-mentioned substituents C1-4-alkyl and cyclopropyl may in each case be unsubstituted or substituted one or more times by identical or different substituents;
- and the above-mentioned substituent C1-4-alkyl may in each case be branched or unbranched;
- in the form of an individual stereoisomer or a mixture thereof;
- in the form of a tautomer;
- of a free compound;
- of an N-oxide;
- or in the form of a solvate and/or of a physiologically acceptable salt.
51 more elements
Dependencies are inferred from the claim text.