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US 7,511,013 B2Granted
Cyclosporin analogues and their pharmaceutical uses
AssigneeAMR Technology, Inc.
InventorsBruce F. Molino, Zhicai Yang
Life of this patent
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Abstract
The compounds of the present invention are represented by Formula I, as shown below: or a pharmaceutically acceptable salt thereof, with X, R0, R1, and R2 defined herein.
Claims9
A compound of Formula Ia:
- wherein:
- X is OH or OAc;
- R0 is H or CH2OR3;
- R1 is H or D;
- R2 is selected from the group consisting of:
- halogen,
- C3-C6 unsubstituted cycloalkyl,
- —CH═N—OR4, and
- —CH═N—NR4R5;
- R3 is selected from the group consisting of:
- hydrogen,
- alkanoyl,
- alkenoyl,
- alkynoyl,
- aryloyl,
- arylalkanoyl,
- alkylaminocarbonyl,
- arylaminocarbonyl,
- arylalkylaminocarbonyl,
- alkyloxycarbonyl,
- aryloxycarbonyl, and
- arylalkyloxycarbonyl;
- R4 and R5 are the same or different and independently selected from the group consisting of:
- hydrogen,
- C1-C6 saturated straight or branched carbon chain,
- C3-C6 unsaturated straight or branched carbon chain,
- C3-C6-substituted and unsubstituted cycloalkyl,
- C1-C4 carbon chain containing an aryl or heteroaryl,
- substituted and unsubstituted aryl,
- substituted and unsubstituted heteroaryl,
- alkanoyl,
- alkenoyl,
- alkynoyl,
- aryloyl,
- arylalkanoyl,
- alkylaminocarbonyl,
- arylaminocarbonyl,
- arylalkylaminocarbonyl,
- alkyloxycarbonyl,
- aryloxycarbonyl,
- arylalkyloxycarbonyl,
- alkylsulfonyl, and
- arylsulfonyl;
- and
- R4 together with R5 results in the formation of a cyclic moiety of C2-C6 optionally containing heteroatom or heteroatoms,
- wherein the compound is a cis geometric isomer, a trans geometric isomer, or a mixture of the cis and the trans geometric isomers or a pharmaceutically acceptable salt thereof.
43 more elements
A compound of Formula Ia:
- wherein:
- X is OH or OAc;
- R0 is H, CH2OH, or CH2OAc;
- R1 is H or D;
- R2 is selected from the group consisting of —CH═CHF, —CH═CHCl, —CH═CHBr, and —CH═CHI,
- wherein the compound is a cis geometric isomer, a trans geometric isomer, or a mixture of the cis and the trans geometric isomers or a pharmaceutically acceptable salt thereof.
3 more elements
A compound of Formula Ib:
- wherein:
- X is OH or OAc;
- R0 is H or CH2OR3;
- R1 is halogen;
- R2 is selected from the group consisting of:
- hydrogen,
- deuterium,
- halogen,
- C2-C6 unsaturated straight or branched carbon chain, optionally containing halogen,
- C3-C6 substituted and unsubstituted cycloalkyl,
- substituted and unsubstituted aryl, and
- substituted and unsubstituted heteroaryl;
- and
- R3 is selected from the group consisting of:
- hydrogen,
- alkanoyl,
- alkenoyl,
- alkynoyl,
- aryloyl,
- arylalkanoyl,
- alkylaminocarbonyl,
- arylaminocarbonyl,
- arylalkylaminocarbonyl,
- alkyloxycarbonyl,
- aryloxycarbonyl, and
- arylalkyloxycarbonyl,
- wherein the compound is a cis geometric isomer, a trans geometric isomer, or a mixture of the cis and the trans geometric isomers or a pharmaceutically acceptable salt thereof.
24 more elements
Dependencies are inferred from the claim text.