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US 6,187,776 B1Granted
Heterocyclic compounds and their use
AssigneeEli Lilly and Company
InventorsLeander Merritt, John S. Ward
Life of this patent
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Abstract
The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.
Claims21
A compound of the formula:
- wherein
- W is oxygen or sulphur;
- R is selected from the group consisting of —OR4, —SR4, —SOR4, —SO2R4, —Z—C3-10-cycloalkyl, —Z—C4-12-(cycloalkylalkyl), —O—R5—Z—R4 and —S—R5—Z—R4;
- R4 is selected from the group consisting of C1-15-alkyl, C2-15-alkenyl, or C2-15-alkynyl, each of which is optionally substituted with one or more substituents independently selected from the group consisting of halogen(s), —CF3, —CN, phenyl and phenoxy wherein phenyl or phenoxy is optionally substituted with one or more selected from the group consisting of halogen, —CN, C1-4-alkyl, C1-4-alkoxy, —OCF3, —CF3, —CONH2 and —CSNH2;
- Z is oxygen or sulphur;
- R5 is selected from the group consisting of C1-15-alkyl, C2-15-alkenyl, and C2-15-alkynyl;
- G is the azacyclic ring system selected from the group consisting of:
- R1 and R2 independently are selected from the group consisting of hydrogen, C-1-15-alkyl, C2-5-alkenyl, C2-5-alkynyl, C1-10-alkoxy, and C1-5-alkyl substituted with a substituent independently selected from the group consisting of —OH, —COR6′, CH2—OH, halogen, —NH2, carboxy, and phenyl;
- R6′ is hydrogen or C1-6-alkyl;
- R3 is selected from the group consisting of hydrogen, C1-5-alkyl, C2-5-alkenyl, and C2-5-alkynyl;
- r is 0, 1 or 2;
- is a single or double bond;
- or a pharmaceutically acceptable salt thereof.
10 more elements
Dependencies are inferred from the claim text.