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US 2024/0190911 A1Published application
Analogs of celastrol
AssigneeERX Pharmaceuticals Corporation
InventorsRalph Mazitschek, Yanbing Ding, Kaisheng Shen
Life of this patent
Estimating the term…
Abstract
Described herein, inter alia, are compositions and methods for treating or preventing obesity and using the same.
Claims18
A compound of Formula (I):
- wherein
- the dotted lines between C1 and C2, C2 and R3, C3 and R4, C5 and C6, C5 and C7, C1 and C6, and C3 and C4 indicate that a single or double bond may be present, as valence permits;
- R1 is —CN, —COOH, —COOCH2CH3, —CONHR5, —CONR5R5, —COOR5, —COOCH3, —CH2NR5R5, —CH2OCONR5R5, —CH2NR5COOR5, —CH2R5, —CH2NR5CONR5R5, —CH2OH, —CH2OR5, alkylsulfate, alkylsulfonate, alkylphosphate, —CH2OSO3R5, —CH2OSO2R5, —CH2OPO3R5R5, —CH2OPO3HR5, —CH2OPO3H2—C(═NR5)NR5R5, —NR5C(═NR5)NR5R5, —CONH2, —CH2CONR5R5, —SR5, —SO3R5, —SO2R5, —CH2NHCOR5, —CH2NHCNR5NR5R5, —CH2COSR5, CH2NR5COR5, —CH2NR5CNR5NR5R5, —CH2NR5COSR5, —CH2NHSO2R5, —CH2N R5SO2R5, —CHNR5, —CHNOR5, —H, —NH2, —NHR5, —NR5R5, —OH, —OR5, phosphate, —OPO3R5R5, —OPO3HR5, —OPO3H2, —NCO, —NCS, —N3, —R5, —C≡CR5, —(CH═CH)R5, —SH, —SR5, —SO2H, —SO3H, —SO2NR5R5, —SO3R5, —NHCOR5, -, NHCNR5NR5R5, —NHCOSR5, secondary amide, tertiary amide, —NR5COR5, —NR5C(═NH)NR5R5, —NR5COSR5, —NHC(═NR5)R5, —NR5C(═NR5)R5, —NHSO2(NH2), —NHSO2R5, —NR5SO2R5, —NR5SO2NR5R5, —OCOR5, —OCONR5R5, —O(C═O)OR5, —SCOR5, —O(C═NH)NR5R5, —OCSNHR5, —OS(═O2)R5, —OS(═O2)NR5R5, —SCONR5R5, —CH2-aryl, —CH2-heteroaryl,
- R2 is —H, —CH3, —SCH(CH3)2, —SC(═O)CH3, —SC(═O)R5, —SCH2CH2OCOCH3, —SR5, —SOR5, —SOOR5, —SCONR5R5,
- R3 is —OCOCH3, —OCOOCH2CH3, —OR7, or —R7 when a double bond is present between C1 and C2, C3 and C4, and C5 and C6;
- R4 is —OCOCH3, —OCOOCH2CH3, —OR7, or —R7 when a double bond is present between C1 and C2, C3 and C4, and C5 and C6;
- R3 is O when R4 is O and a double bond is present between C2 and R3 and C3 and R4;
- R4 is —OCH3, —OH, —OCOOCH2CH3, —OCONHCH2CH3, —OCOOCH(CH3)2, —OR7, —R7, or —NR5R5 when R3 is O and a double bond is present between C2 and R3;
- R3 and R4 may also be combined to form a heterocylic or carbocyclic ring;
- R5 is independently selected for each occurrence hydrogen, an alkyl, cycloalkyl, alkoxy, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, amine, or heteroaryl, optionally substituted with substituents individually selected from alkyl, alkoxy, cycloalkyl, ether, amine optionally substituted with one or more alkyl, halogen, hydroxyl, ether, cyano, nitrile, CF3, ester, amide, cycloalkyl amide, sugar, heteroarylamide optionally substituted with alkyl and/or alkoxy, urea, carbamate, thioether, sulfate, sulfonyl, sulfonic acid carboxylic acid, and aryl or two R5 groups taken together to form a cycloalkyl, heterocycloalkyl, aryl or heteraryl group, optionally substituted with substituents individually selected from alkyl, cycloalkyl, alkoxy, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, heteroaryl, amine, halogen, hydroxyl, ether, nitrile, cyano, nitro, CF3, ester amide, urea, carbamate, thioether, or carboxylic acid group;
- and
- R7 is hydrogen, an alkyl, cycloalkyl, heterocycloalkyl, alkylaryl, alkenyl, alkynyl, aryl, or heteroaryl, optionally substituted with substituents individually selected from alkyl, cycloalkyl, ether, amine, halogen, hydroxyl, ether, nitrile, cyano, nitrile, CF3, ester, amide, urea, carbamate, thioether, or carboxylic acid,
- or a pharmaceutically acceptable salt or prodrug thereof.
10 more elements
-47. (canceled)
Dependencies are inferred from the claim text.