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Oxaborol esters and their uses
专利权人:
ANACOR PHARMACEUTICALS; INC.
发明人:
申请号:
ARP170101250
公开号:
AR108450A1
申请日:
2017.05.11
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
1. Claim 1: a formula compound (1),or a pharmaceutically acceptable salt thereof, wherein: R¹ is hydrogen or C₁₋₆ aliphatic; R¹ᵃ is hydrogen or C₁₋₆ aliphatic; or R¹ and R¹ᵃ are taken together with the carbon atom to which they are attached to form an optionally substituted 3- to 6-membered carbocyclic spiro ring; each R² is independently hydrogen, -halogen, -OR, -NO₂,-Cn, - Mr, - n (R) 8322,-C (O) R, -C (O) OR, -S (O) R, -S (O) ₂R, -C (O) N (R) ₂,-SO N (R)-OC (O) R, -N (R) C (O) R, -N (R) C (O) OR, -N (R) SO₂R, -OC (O) N (R) ₂,or an optionally substituted group selected from the group consisting of aliphatic C₁₋₆ and 3- to 6-membered saturated or partially unsaturated monocyclic carbocyclyl; R³ is hydrogen or optionally substituted aliphatic C₁₋₆; R⁴ is hydrogen, a natural or unnatural amino acid side chain group, or an optionally substituted group selected from the group consisting of C₁₋₆ aliphatic, 3- to 7-membered saturated or partially unsaturated monocyclic carbocyclyl, and phenyl;or R³ and R⁴ are taken together with the carbon atom attached to R⁴ and the nitrogen atom attached to R³ to form an optionally substituted 3- to 6-membered heterocyclyl ring having 0-1 additional heteroatoms selected from oxygen, nitrogen or sulfur; R⁵ is hydrogen or optionally substituted aliphatic C₁₋₆; or R⁴ and R⁵ are taken together with the carbon atom to which they are attached to form an optionally substituted ring selected from a 3- to 6-membered heterocyclic spiro ring having 1-2 hetero atoms selected from oxygen,nitrogen or sulfur and a 3-6 membered saturated or partially unsaturated monocyclic spiro carbocyclic ring; L is a covalent bond or a straight or branched hydrocarbon chain, saturated or unsaturated bivalent C₁₋₁₀, where one, two or three methylene units of L are optionally and independently replaced by -Cy-,- that is...-So...-SO₂-,-C (O) --C (O) N (R) -- yes.-N (R) --That's it.-OC (o)..-N (R) C (O) --N (R) SO -o -SO N (R) -Among them, each ring is a selective biva
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