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US 6,221,870 B1Granted
Ergoline derivatives and their use as somatostatin receptor antagonists
AssigneeNovartis AG
InventorsPaul Pfaeffli, Peter Neumann, Robert Swoboda, Peter Stütz
Life of this patent
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Abstract
The invention provides compounds of formula I wherein R1 to R6 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
Claims7
A compound of formula I
- wherein
- R1 is hydrogen, (C1-4)alkyl or a group of formula
- wherein n is 1 to 4 and R7 is fluorine, chlorine, hydroxy, (C1-4)alkyl or (C1-4)alkoxy,
- R2 is hydrogen, chlorine, bromine, iodine, (C1-4)alkyl or (C1-4) alkylthio,
- R3 is hydrogen or (C1-4)alkyl,
- R4 is (i) a group of formula
- wherein R8 is fluorine, chlorine, nitro or cyano and R11 is (C1-4)alkyl or (C2-5)alkenyl, or (ii) a group of formula
- wherein each X independently is O or S, and
- R5 and R6 are each hydrogen or form together a further bond between the two carbon atoms on which they are located,
- in free base or acid addition salt form.
7 more elements
A compound of formula Ia
- wherein R1 is hydrogen or a group of formula a)
- where n is 1 to 3 and R7 is fluoro or (C1-4) alkyl;
- R2 is hydrogen, chloro, bromo, (C1-4) alkyl or (C1-4) alkylthio;
- R3 is hydrogen or (C1-4) alkyl;
- and
- R4 is a group of formula
- where R8 is hydrogen, and R11 is (C1-4) alkyl;
- in free base or acid addition salt form.
5 more elements
Dependencies are inferred from the claim text.