IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
|
| 국제특허분류(IPC7판) |
|
| 출원번호 |
US-0347922
(2012-09-27)
|
| 등록번호 |
US-9630979
(2017-04-25)
|
| 국제출원번호 |
PCT/US2012/057533
(2012-09-27)
|
| 국제공개번호 |
WO2013/049332
(2013-04-04)
|
|
발명자
/ 주소 |
- Castro, Alfredo C.
- Peluso, Stephane
- Snyder, Daniel A.
- Tibbitts, Thomas T.
|
| 출원인 / 주소 |
- Infinity Pharmaceuticals, Inc.
|
| 대리인 / 주소 |
|
| 인용정보 |
피인용 횟수 :
0 인용 특허 :
64 |
초록
▼
Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical compositio
Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein.
대표청구항
▼
1. A compound of formula (II′): or a pharmaceutically acceptable form thereof, wherein:R10 is halogen or an optionally substituted (C1-C6)alkyl;R11 is hydrogen, halogen or an optionally substituted (C1-C6)alkyl;R12 is —C(O)NH2 or —(CH2)n—NHR14 and R13 is hydrogen; orR14 is an optionally substituted
1. A compound of formula (II′): or a pharmaceutically acceptable form thereof, wherein:R10 is halogen or an optionally substituted (C1-C6)alkyl;R11 is hydrogen, halogen or an optionally substituted (C1-C6)alkyl;R12 is —C(O)NH2 or —(CH2)n—NHR14 and R13 is hydrogen; orR14 is an optionally substituted (C1-C6)alkyl, —SO2R16 or —C(O)R17;R15, R16 and R17 are each independently an optionally substituted (C1-C6)alkyl or an optionally substituted amino; andn is 0, 1, 2 or 3. 2. A compound selected from: or a pharmaceutically acceptable form thereof. 3. The compound of claim 1, wherein the compound is selected from: or a pharmaceutically acceptable form thereof. 4. A pharmaceutical composition comprising a compound of claim 1 and one or more pharmaceutically acceptable carriers or excipients. 5. A method for inhibiting monoacylglycerol lipase (MAGL) in a patient in need thereof, wherein the patient has disorder or condition mediated by monoacylglycerol lipase (MAGL), and the method comprises administering to the patient a therapeutically effective amount of a compound of claim 1. 6. The method of claim 5, wherein the disorder or condition is a CNS disorder. 7. The method of claim 6, wherein the CNS disorder is neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, epilepsy, a learning disorder or schizophrenia. 8. The method of claim 7, wherein the stroke is ischemic stroke. 9. The method of claim 7, wherein the learning disorder is attention deficit disorder. 10. A compound of formula (II): or a pharmaceutically acceptable form thereof,wherein:R10 is hydrogen;R11 is halogen or an optionally substituted (C1-C6)alkyl;R12 is —C(O)NH2 or —(CH2)n—NHR14 and R13 is hydrogen; orR12 and R13 taken together can form a 5 to 7 membered ring containing one or more heteroatoms selected from N, S and O, wherein one or more carbon or sulfur atoms on the ring can optionally be substituted with one or more oxo group;R14 is an optionally substituted (C1-C6)alkyl, —SO2R16 or —C(O)R17;R16 and R17 are each independently an optionally substituted (C1-C6)alkyl or an optionally substituted amino; andn is 0, 1, 2 or 3. 11. The compound of claim 10, wherein the compound is selected from: 12. The compound of claim 1, wherein R11 is hydrogen. 13. The compound of claim 12, wherein R10 is hydrogen or F. 14. The compound of claim 1, wherein the compound is: or a pharmaceutically acceptable salt thereof. 15. A pharmaceutical composition comprising a compound of claim 14 and one or more pharmaceutically acceptable carriers or excipients. 16. A method for treating a condition selected from NSAID-induced gastric hemorrhage, peptic ulcer and gastritis in a patient, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of claim 14. 17. A method for treating a condition selected from neuropathic and inflammatory pain in a patient, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of claim 14. 18. A method for reducing pain or providing an analgesic effect in a patient, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of claim 14. 19. A method for treating allodynia in a patient, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of claim 14. 20. A compound of formula (II′): or a pharmaceutically acceptable form thereof, wherein:R10 is halogen or an optionally substituted (C1-C6)alkyl;R11 is hydrogen, halogen or an optionally substituted (C1-C6)alkyl;R12 is —C(O)NH2 or —(CH2)n—NHR14 and R13 is hydrogen; orR12 and R13 taken together can form a 5 to 7 membered ring containing one or more heteroatoms selected from N, S and O, wherein one or more carbon or sulfur atoms on the ring can optionally be substituted with one or more oxo group;R14 is an optionally substituted (C1-C6)alkyl, —SO2R16 or —C(O)R17;R16 and R17 are each independently an optionally substituted (C1-C6)alkyl or an optionally substituted amino; andn is 0, 1, 2 or 3. 21. A method for treating a condition selected from NSAID-induced gastric hemorrhage, peptic ulcer, gastritis, neuropathic pain, inflammatory pain, allodynia and a painful condition, in a patient, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of claim 1. 22. A method for reducing pain or providing an analgesic effect in a patient, wherein the method comprises administering to the patient a therapeutically effective amount of a compound of claim 1.
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