IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0263324
(2010-04-07)
|
등록번호 |
US-8541581
(2013-09-24)
|
국제출원번호 |
PCT/US2010/030276
(2010-04-07)
|
§371/§102 date |
20111223
(20111223)
|
국제공개번호 |
WO2010/118159
(2010-10-14)
|
발명자
/ 주소 |
- Castro, Alfredo C.
- Evans, Catherine A.
- Grenier, Louis
- Grogan, Michael J.
|
출원인 / 주소 |
- Infinity Pharmaceuticals, Inc.
|
대리인 / 주소 |
|
인용정보 |
피인용 횟수 :
0 인용 특허 :
87 |
초록
▼
Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2, R3, R4, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula
Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2, R3, R4, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating an FAAH-mediated disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention.
대표청구항
▼
1. A compound of formula III: or a pharmaceutically acceptable salt, solvate or prodrug thereof, or mixture thereof, wherein: is selected from a single bond and a double bond;m is 1 when is a single bond;m is 0 when is a double bond;Z1 is —OR14;Z2 is —OR15;R1, R2, R3, R4, R6, R7, R12 and R13 each
1. A compound of formula III: or a pharmaceutically acceptable salt, solvate or prodrug thereof, or mixture thereof, wherein: is selected from a single bond and a double bond;m is 1 when is a single bond;m is 0 when is a double bond;Z1 is —OR14;Z2 is —OR15;R1, R2, R3, R4, R6, R7, R12 and R13 each independently is selected from H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 perhaloalkyl, —CN, —OR16, NR17R18, —C(O)R19, C3-10 carbocyclyl, C6-10 aryl, C7-12 aralkyl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R8 is selected from C2-6 alkenyl, C2-6 alkynyl, —C(O)R20, —C(O)NR22R23, S(O)2R24, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, 5-10 membered heteroaryl, and —(CH2)p—R25;R14 and R15, at each occurrence, each independently is selected from H, C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl;R16, at each occurrence, each independently is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, C7-12 aralkyl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R17 and R18, at each occurrence, each independently is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, —C(O)R26, —C(O)OR27, C3-10 carbocyclyl, C6-10 aryl, C7-12 aralkyl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R19, at each occurrence, each independently is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, C7-12 aralkyl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R20 is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, 5-10 membered heteroaryl, and —(CH2)q—R28;R22 and R23 each independently is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, 5-10 membered heteroaryl, and —(CH2)r—R29;R24 is selected from C1-6 alkyl, C2-6 alkenyl, alkynyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, 5-10 membered heteroaryl, and —(CH2)t—R30;R25 is selected from C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R26 and R27 each independently is selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, C7-12 aralkyl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R28, R29, and R30, at each occurrence, each independently is selected from —OR31, —NR32R33, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl;R31, R32 and R33, at each occurrence, each independently is selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-10 carbocyclyl, C6-10 aryl, C7-12 aralkyl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl; andp, q, r, and t, at each occurrence, each independently is selected from 1, 2, 3, 4, 5 and 6. 2. The compound of claim 1, wherein R8 is selected from —C(O)R20, —C(O)NR22R23, S(O)2R24, and —(CH2)p—R25. 3. The compound of claim 1, wherein R8 is —C(O)R20, and R20 is selected from C1-6 alkyl, C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, 5-10 membered heteroaryl, and —(CH2)q—R28. 4. The compound of claim 3, wherein R20 is —(CH2)q—R28, and R28 is selected from C3-10 carbocyclyl, C6-10 aryl, 3-10 membered cycloheteroalkyl, and 5-10 membered heteroaryl. 5. The compound of claim 3, wherein R20 is —(CH2)q—R28, and R28 is —NR32R33. 6. The compound of claim 5, wherein R32 and R13 each independently is selected from H, C1-6 alkyl, and C7-12 aralkyl. 7. The compound of claim 1, wherein R8 is —C(O)NR22R23. 8. The compound of claim 7, wherein R22 and R23 each independently is selected from H, C1-6 alkyl, and —(CH2)r—R29. 9. The compound of claim 8 wherein R29 is selected from C6-10 aryl and 5-10 membered heteroaryl. 10. The compound of claim 1, wherein R8 is —S(O)2R24. 11. The compound of claim 10, wherein R24 is selected from C1-6 alkyl, C6-10 aryl, 5-10 membered heteroaryl, and —(CH2)t—R30. 12. The compound of claim 1, wherein R8 is —(CH2)p—R25. 13. The compound of claim 12, wherein R25 is selected from C6-10 aryl and 5-10 membered heteroaryl. 14. The compound of claim 1, wherein R12 is H and R13 is H. 15. The compound of claim 1, wherein R6 is H and R7 is H. 16. The compound of claim 1, wherein is a double bond and m is 0. 17. The compound of claim 1, wherein is a single bond and m is 1. 18. The compound of claim 17, wherein R2 is H. 19. The compound of claim 1, wherein R1 is H. 20. The compound of claim 1, wherein R3 is H and R4 is H. 21. The compound of claim 1, wherein R14 is H and R15 is H. 22. The compound of claim 1, wherein the compound is selected from: or a pharmaceutically acceptable salt, solvate or prodrug thereof, or mixture thereof. 23. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof, or mixture thereof and a pharmaceutically acceptable excipient. 24. The compound of claim 1, wherein the compound is of the formula IIIa: or a pharmaceutically acceptable salt, solvate or prodrug thereof, or mixture thereof. 25. The compound of claim 1, wherein the compound is of the formula IIIb: or a pharmaceutically acceptable salt, solvate or prodrug thereof, or mixture thereof.
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