The invention relates to the use of di-aspirin (bis(2-carboxyphenyl)succinate) and its derivatives in the treatment of colon and colorectal cancer. It also relates to novel derivatives of di-aspirin and to a method of synthesis of the di-aspirin and its derivatives.
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1. A compound of Formula (I) for use in the treatment of colorectal cancer: wherein Y represents H or —C(═O)—Xwherein X represents:(i)(a) C1-12alkyl optionally substituted by one or more of C1-12alkyl, halogen or —O—NO2,(b) C5-12aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH,
1. A compound of Formula (I) for use in the treatment of colorectal cancer: wherein Y represents H or —C(═O)—Xwherein X represents:(i)(a) C1-12alkyl optionally substituted by one or more of C1-12alkyl, halogen or —O—NO2,(b) C5-12aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na, or(c) C2-12alkenyl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na,each of (a)-(c) being substituted with the following structure by attachment through the carbon of the —C(O)O group of the structure (ii) C2-6alkyl substituted with one or more carboxyl group;(iii) C1-12alkyl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na;(iv) C5-10aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na;(v) C1-6alkoxy optionally substituted by one or more of halogen, —OH, OC1-6alkyl, primary, secondary or tertiary amino where the N-substituents are C1-6alkyl; or(vi) —O—C5-10aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na;wherein when Y represents —C(═O)—X, R and R1 are independently selected from —OH, —NH2 and C1-8alkoxy;wherein when Y represents H, R represents —NHC(═O)-C1-6alkyl,R2 and R3 are independently selected from halogen, C1-12alkyl, hydroxyl, carboxyl, C1-12alkoxy, —NH2, —NH(C1-6alkyl), —N(C1-6alkyl)(C1-6alkyl), C1-12alkyl-NH2, C1-12alkyl-NH(C1-6alkyl), C1-12alkyl-N(C1-6alkyl)(C1-6alkyl), C1-12alkyl-C(═O)—NH2, C1-12alkyl-C(═O)—NH(C1-6 alkyl), C1-12alkyl-C(═O)—N(C1-6alkyl)(C1-6alkyl), —NO2, —SO3H and —SO3Na;and n and m are independently selected from 0, 1, 2, 3 or 4,with the proviso that where X is CH3, then R is —NH2. 2. The compound according to claim 1 wherein X represents C1-12alkyl substituted with the following structure by attachment through the carbon of the —C(O)O group of the structure 3. The compound according to claim 2 wherein the C1-12alkyl is —CH2CH2—, —CH2(CH2)2CH2— or —CH2(CH2)6. 4. The compound according to claim 1 wherein X represents C5-12aryl substituted with the following structure by attachment through the carbon of the —C(O)O group of the structure 5. The compound according to claim 4 wherein C5-12aryl is phenyl. 6. The compound according to claim 1 wherein X represents C2-12alkenyl substituted with the following structure by attachment through the carbon of the —C(O)O group of the structure 7. The compound according to claim 6 wherein C2-12alkenyl is —CH═CH—. 8. The compound according to claim 1 wherein X represents phenyl. 9. The compound according to claim 1 wherein X represents phenyl substituted with halogen or C1-6alkyl. 10. A compound of Formula (I) wherein Y represents H or —C(═O)—X and X represents: (i)(a) C1-12alkyl optionally substituted by one or more of C1-12alkyl, halogen or —O—NO2,(b) C5-12aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na, or(c) C2-6alkenyl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na,each of (a)-(c) being substituted with the following structure by attachment through the carbon of the —C(O)O group of the structure (ii) C2-6alkyl substituted with one or more carboxyl groups,(iii) C1-12alkyl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na,(iv) C5-10aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na;(v) C1-6alkoxy optionally substituted by one or more of halogen, —OH, OC1-6alkyl, primary, secondary or tertiary amino where the N-substituents are C1-6alkyl; or(vi) —O—C5-10aryl optionally substituted by one or more of halogen, —CO2H, —CN, —OH, —NH2, —CONH2, C1-6alkyl, C1-6alkenyl, —NO2, —SO3H, or —SO3Na;wherein when Y represents —C(═O)—X, R and R1 are independently selected from —OH, —NH2 and C1-8alkoxy;wherein when Y represents H, R represents —NHC(═O)—C1-6alkyl,R2 and R3 are independently selected from halogen, C1-12alkyl, hydroxyl, carboxyl, C1-12alkoxy, —NH2, —NH(C1-6alkyl), —N(C1-6alkyl)(C1-6alkyl), C1-12alkyl-NH2, C1-12alkyl-NH(C1-6alkyl), C1-12alkyl-N(C1-6alkyl)(C1-6alkyl), C1-12alkyl-C(═O)—NH2, C1-12alkyl-C(═O)—NH(C1-6alkyl), C1-12alkyl-C(═O)—N(C1-6alkyl)(C1-6alkyl), —NO2, —SO3H and —SO3Na;and n and m are independently selected from 0, 1, 2, 3 or 4;with the proviso that one or both of R and R1 are —NH2 when X represents:C1-12alkyl or C2-6alkenyl, each substituted with the following structure by attachment through the carbon of the —C(O)O group of the structure and with the further proviso that when X is —CH3, R is —NH2. 11. Use the compound of claim 1 having Formula (I) in the treatment of colorectal cancer. 12. (canceled) 13. A pharmaceutical composition comprising the compound according to claim 1, or a pharmaceutically acceptable salt, solvate or hydrate thereof. 14. A pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutically acceptable salt, solvate or hydrate thereof for use in the treatment of colorectal cancer. 15. (canceled) 16. A method of treating colorectal cancer, comprising administering an effective amount of the compound of claim 1, or a pharmaceutically acceptable salt, solvate or hydrate thereof, to a patient in need thereof. 17. Use the compound of claim 10 having Formula (I) in the treatment of colorectal cancer. 18. A pharmaceutical composition comprising the compound according to claim 10, or a pharmaceutically acceptable salt, solvate or hydrate thereof. 19. A method of treating colorectal cancer, comprising administering an effective amount of the compound of claim 10, or a pharmaceutically acceptable salt, solvate or hydrate thereof, to a patient in need thereof.
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