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US 2006/0135550 A1Published application
Rapamycin derivatives and the uses thereof in the treatment of neurological disorders
AssigneeWyeth
InventorsEdmund Graziani, Kevin Pong, Jerauld Skotnicki
Life of this patent
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Abstract
The present invention provides compounds of the following structure, wherein R1-R9, R15, and n are defined herein. These compounds are useful in treating neurological disorders or complications due to stroke or head injury, and as neuroprotective and neuroregenerative agents.
Claims22
A compound of the formula I:
- wherein:
- R1 and R2 are the same or different and are selected from the group consisting of CR16R17 and CR18R19;
- R3 and R4 are:
- (a) independently selected from the group consisting of H, OH, O(C1 to C6 alkyl), O(substituted C1 to C6 alkyl), O(acyl), O(aryl), O(substituted aryl), and halogen;
- or
- (b) taken together to form a double bond to O;
- R5, R6, and R7 are independently selected from the group consisting of H, OH, and OCH3;
- R8 and R9 are connected through a (i) single bond and are CH2 or (ii) double bond and are CH;
- R15 is selected from the group consisting of C═O, CHOH, and CH2;
- R16 and R17 are independently selected from the group consisting of H, C1 to C6 alkyl, C1 to C6 substituted alkyl, aryl, substituted aryl, acyl, CF3, CN, and NO2;
- R18 and R19 are independently selected from the group consisting of H, C1 to C6 alkyl, C1 to C6 substituted alkyl, aryl, substituted aryl, acyl, CF3, CN, and NO2;
- or
- R17 and R18 are taken together to form a carbon-based or heterocyclic 5- to 7-membered ring;
- n is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
12 more elements
The compound according to claim 11, wherein R15 is C═O.
A compound of the formula Ia:
- wherein:
- R1 and R2 are the same or different and are selected from the group consisting of CR16R17 and CR18R19;
- R6 is selected from the group consisting of H, OH, and OCH3;
- R8 and R9 are connected through a (i) single bond and are CH2 or (ii) double bond and are CH;
- R16 and R17 are independently selected from the group consisting of H, C1 to C6 alkyl, C1 to C6 substituted alkyl, aryl, substituted aryl, acyl, CF3, CN, and NO2;
- R18 and R19 are independently selected from the group consisting of H, C1 to C6 alkyl, C1 to C6 substituted alkyl, aryl, substituted aryl, acyl, CF3, CN, and NO2;
- or
- R18 and R19 are taken together to form a 5- to 7-membered ring;
- or a pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.