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US 12,338,214 B2Granted
Bexarotene derivatives and their use in treating cancer
AssigneeDJ Therapeutics LLC
InventorsDonald Tsai, David Kaelin
Life of this patent
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Abstract
Compounds of the invention, such as compounds of formula (I): where R, R1, R2, R3, R4, R5, R6, and R7 are defined herein, are useful for treating cancer, autoimmune disorders, and/or skin dermatitis, and/or methods for increasing peripheral blood counts and/or improving immune system function. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
Claims24
A compound of formula:
- or pharmaceutically acceptable salts thereof, wherein
- two R groups and the carbon atom to which they are attached form ═CH2 or cyclopropyl ring;
- R1 is —CO2H;
- R2 is halogen or methyl;
- R3 is halogen;
- R4 and R5 are independently C1-C6 alkyl or C1-C6 haloalkyl, or R4 and R5 are together with the carbon atoms to which they are attached form C3 cycloalkyl optionally substituted with one or more R8;
- R6 and R7 are independently C1-C6 alkyl or C1-C6 haloalkyl, or R6 and R7 are together with the carbon atoms to which they are attached form C3 cycloalkyl optionally substituted with one or more R8;
- wherein each R8 is independently halogen, —NO2, —CN, C1-C6 alkyl, C1-C6 haloalkyl, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, —OH, C1-C6 alkoxy, or C1-C6 haloalkoxy.
5 more elements
A compound having the formula:
- or pharmaceutically acceptable salts thereof, wherein
- X is CH2, O, or NH;
- y is CH2, O, or NH;
- m is 1;
- n is 1;
- R1 is —CO2H;
- R2 is halogen or methyl;
- R3 is halogen;
- R4 and R5 are independently C1-C6 alkyl or C1-C6 haloalkyl, or R4 and R5 are together with the carbon atoms to which they are attached form C3 cycloalkyl optionally substituted with one or more R8;
- R6 and R7 are independently C1-C6 alkyl or C1-C6 haloalkyl, or R6 and R7 are together with the carbon atoms to which they are attached form C3 cycloalkyl optionally substituted with one or more R8;
- wherein each R8 is independently halogen, —NO2, —CN, C1-C6 alkyl, C1-C6 haloalkyl, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl) 2, —OH, C1-C6 alkoxy, or C1-C6 haloalkoxy.
8 more elements
Dependencies are inferred from the claim text.