The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provide
The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
대표청구항▼
1. A pharmaceutically acceptable composition, comprising a compound of formula III, a pharmaceutically acceptable salt, a stereoisomer, or tautomer thereof and a pharmaceutically acceptable excipient;wherein:each of Z1 and Z2 is —OH;L1 is a covalent bond;Ring A is an optionally substituted phenyl ri
1. A pharmaceutically acceptable composition, comprising a compound of formula III, a pharmaceutically acceptable salt, a stereoisomer, or tautomer thereof and a pharmaceutically acceptable excipient;wherein:each of Z1 and Z2 is —OH;L1 is a covalent bond;Ring A is an optionally substituted phenyl ring where n is an integer between 0 and 4, inclusive, each occurrence of R1 is, independently, halogen, —OR, —CF3, —CN, —NO2, —NC, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R′)2, —CHO, —N3, —N2R, —N(R′)2, —B(OH2), or an optionally substituted C1-8 aliphatic group, each occurrence of R is hydrogen, an optionally substituted C1-6 aliphatic group, or an optionally substituted C6-12 aliphatic aryl group, at least one R1, if present, is in an ortho position relative to the boron atom, and each occurrence of R′ is hydrogen —C(O)R, a suitable amino protecting group, or an optionally substituted C1-6 aliphatic group, or optionally substituted C6-12 aryl group;X is —O—CH2—CH2—, —CH2—O—CH2—,—CH2—CH2—CH2—, —O—CH(CH3)—CH2—, —O—CH2—CH2—CH2—, —C(═O)—CH2—CH2—, —CH2—CH2—C(═O)—, —CH2—CH2—CH2—C(═O)—, or —(CCH3═N)—O—CH2— and X is in a para position relative to the boron atom; andRing B is a phenyl ring where m is 0. 2. The composition according to claim 1, wherein X is —O—CH2—CH2—. 3. The composition according to claim 1, wherein X is —CH2—O—CH2—. 4. The composition according to claim 1, wherein at least one Rl is fluoro in the ortho position relative to the boron atom. 5. The composition according to claim 1, wherein X is —CH2—CH2—CH2—. 6. The composition according to claim 1, wherein X is —O—CH(CH3)—CH2—. 7. The composition according to claim 1, wherein X is —O—CH2—CH2—CH2—. 8. The composition according to claim 1, wherein X is —C(═O)—CH2—CH2—. 9. The composition according to claim 1, wherein X is —CH2—CH2—C(═O)—. 10. The composition according to claim 1, wherein X is —(CCH3═N)—O—CH2—. 11. The composition according to claim 1, wherein the compound of formula III comprises: 12. The composition according to claim 1, wherein n is 0. 13. The composition according to claim 1, wherein n is 1. 14. A method for treating a fatty acid amide hydrolase (FAAH)-mediated disease, disorder, or condition by administering a therapeutically effective amount of a compound of formula III, a pharmaceutically acceptable salt, stereoisomer, or tautomer thereof, or a pharmaceutically acceptable composition thereof, to a patient in need thereof;wherein:each of Z′ and Z2 is —OH;L1 is a covalent bond;Ring A is an optionally substituted phenyl ring where n is an integer between 0 and 4, inclusive, each occurrence of R′ is, independently, halogen, —OR, —CF3, —CN, —NO2, —NC, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R′)2, —CHO, —N3, —N2R, —N(R′)2, —B(OH2), or an optionally substituted C1-8 aliphatic group, at least one R1, if present, is in an ortho position relative to the boron atom, each occurrence of R is hydrogen, an optionally substituted C1-6 aliphatic group, or an optionally substituted C6-12 aryl group, and each occurrence of R′ is hydrogen, —C(O)R, a suitable amino protecting group, or an optionally substituted C1-6 aliphatic group, or optionally substituted C6-12 aryl group;X is —O—CH2—CH2—, —CH2—O—CH2—, —CH2—CH2—CH2—, —O—CH(CH3)—CH2—, —O—CH2—CH2—CH2—, —C(═O)—CH2CH2—, —CH2CH2—C(═O)—, —CH2—CH2—CH2—C(═O)—, or —(CCH3═N)—O—CH2— and X is in a para position relative to the boron atom; andRing B is a phenyl ring where m is 0,wherein the FAAH-mediated disease, disorder, or condition is a painful syndrome, disease, or disorder. 15. The method according to claim 14, wherein the painful syndrome, disease, or disorder is selected from the group consisting of neuropathic pain, central pain, deafferentation pain, chronic pain, stimulus of nociceptive receptors, acute pain, non-inflammatory pain, inflammatory pain, pain associated with cancer, preoperative pain, arthritic pain, lumbosacral pain, musculo-skeletal pain, headache, migraine, muscle ache, lower back and neck pain, and toothache. 16. The method according to claim 15, wherein the painful syndrome, disease, or disorder is neuropathic pain.
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