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US 9,067,881 B2Granted
4-tolyl-ethynyl-octahydro-indole-1-ester derivatives
AssigneeNovartis AG
InventorsJoachim Nozulak, Dieter Oser
Life of this patent
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Abstract
The invention relates to compounds of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them.
Claims6
A compound of formula I
- wherein
- R1 is C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkyl-C1-4alkyl;
- R2 and R3 independently are halogen, cyano, hydroxy, amino, C1-4alkyl;
- C1-4halogenalkyl;
- C1 -4hydroxyalkyl;
- C1-4aminoalkyl;
- C1-4alkylamino-C1-4alkyl;
- di-(C1-4alkyl)amino-C1-4alkyl;
- C1 -4alkoxy-C1-4alkyl;
- C2-4alkenyl;
- C2-4halogenalkenyl;
- C2-4alkinyl;
- C2-4halogenalkinyl;
- C1-4alkoxy;
- C1-4halogenalkoxy;
- C1-4alkyl-amino;
- di-(C1-4alkyl)amino or C3-6cycloalkyl, wherein one carbon atom of the C3-6cycloalkyl may be replaced by an oxygen atom and wherein the C3-6cycloalkyl may be attached directly to the ring system or via a C1-2alkylene or an oxygen;
- m is 0, 1, 2, 3, 4, 5 or 6;
- n is 0, 1, 2, 3 or 4;
- R4 and R5 independently are hydrogen, halogen or methyl;
- R6 is halogen, hydroxy, amino, cyano, methyl or methoxy;
- p is 0, 1, 2, 3 or 4;
- R7 is —C(O)R8;
- and
- R8 is C1-6alkyl which is substituted once or more than once by R12;
- and wherein each R12 is amino, morpholino, pyrrolidino, C1-6alkylamino or aminocarbonyl;
- in free form or in salt form.
24 more elements
A compound selected from the group consisting of:
- (3aR,4S,7aR)-1-(methoxycarbonyl)-4-(m-tolylethynyl)octahydro-1H-indol-4-yl methyl glutarate;
- (3aR,4S,7aR)-methyl 4-(4-(methylamino)-4-oxobutanoyloxy)-4-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate;
- ((3aR,4S,7aR)-1-(methoxycarbonyl)-4-(m-tolylethynyl)octahydro-1H-indol-4-yl methyl succinate;
- (3aR,4S,7aR)-1-(methoxycarbonyl)-4-(m-tolylethynyl)octahydro-1H-indol-4-yl methyl malonate;
- (3aR,4S,7aR)-methyl 4-(4-(ethylamino)-4-oxobutanoyloxy)-4-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate and
- (3aR,4S,7aR)-methyl 4-(5-(ethylamino)-5-oxopentanoyloxy)-4-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate;
- or a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.