Mayo Foundation for Medical Education and Research
대리인 / 주소
Fish & Richardson P.C.
인용정보
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50
초록
This disclosure relates to materials and methods for inhibiting Botulinum neurotoxin, and more particularly to materials and methods for inhibiting the zinc endopeptidase of Botulinum neurotoxin serotypes A, D and/or E (BoNTA, BoNTD and/or BoNTE).
대표청구항▼
1. A composition comprising a compound of Formula (IIA): or a pharmaceutically acceptable salt or derivative thereof, wherein:R1 is chosen from NH2, aryl, and heteroaryl;R2 is chosen from NR2aR2b;R2a and R2b are chosen from (CH2)mNH2;m is an integer from 4 to 12;R3 is chosen from thiol, imidazole, s
1. A composition comprising a compound of Formula (IIA): or a pharmaceutically acceptable salt or derivative thereof, wherein:R1 is chosen from NH2, aryl, and heteroaryl;R2 is chosen from NR2aR2b;R2a and R2b are chosen from (CH2)mNH2;m is an integer from 4 to 12;R3 is chosen from thiol, imidazole, sulfonamide, COOH, and CONHOH;R4 and R5 are independently chosen from aryl and heteroaryl;R6 is chosen from H, OH, CH2OH, NH2, aryl and heteroaryl;U and X are independently (CH2)m1V(CH2)m2;V is chosen from C, C(OH), 0, S, and NH, or is absent;m1 is an integer from 0 to 2;m2 is an integer from 0 to 2;W is chosen from 0 and S, or is absent;Y is chosen from CO(CH2)m3, (CH2)m3, and CONH(CH2)m3;m3 is an integer from 1 to 10; andall non-hydrogen atoms in the pyrrole ring can be substituted by N, S, or O provided the substitution maintain aromaticity. 2. The composition of claim 1, wherein the compound of Formula (II-A) is chosen from: or a pharmaceutically acceptable salt or derivative thereof, wherein:R6 is chosen from H, OH, CH2OH, and NH2;m is an integer from 3 to 10;n is an integer from 5 to 10;X is chosen from (CH2)m1V1(CH2)m2V2(CH2)m3;V1 and V2 are independently chosen from C, C(OH), O, S, and NH, or are absent;m1 is an integer from 0 to 4;m2 is an integer from 0 to 4; andm3 is an integer from 0 to 4. 3. The composition of claim 1, wherein the compound of Formula (II-A) is chosen from: or a pharmaceutically acceptable salt or derivative thereof. 4. A kit comprising a composition according to claim 1. 5. The kit of claim 4, wherein the composition is in the form of an injectable composition. 6. A pharmaceutical composition comprising a composition of claim 1 and a pharmaceutically acceptable carrier, excipient, or adjuvant. 7. The compound of claim 1, wherein the compound of Formula (IIA) is: or a pharmaceutically acceptable salt thereof. 8. The compound of claim 1, wherein: R1 is phenyl;R2 is N[(CH2)7NH2]2;R4 is phenyl;R5 is phenyl;R6 is CH2OH;X is (CH2)2;Y is (CH2)2;W is O; andU is (CH2)2,or a pharmaceutically acceptable salt thereof. 9. The compound of claim 8, wherein R3 is COOH. 10. The compound of claim 1, wherein: R1 is phenyl;R2 is N[(CH2)7NH2]2;R3 is COOH;R4 is phenyl;R5 is phenyl;R6 is CH2OH;X is (CH2)2;Y is (CH2)2;W is O; andU is (CH2)2,or a pharmaceutically acceptable salt thereof. 11. The kit of claim 4, wherein the compound of Formula (IIA) is: or a pharmaceutically acceptable salt thereof. 12. The kit of claim 4, wherein: R1 is phenyl;R2 is N[(CH2)7NH2]2;R4 is phenyl;R5 is phenyl;R6 is CH2OH;X is (CH2)2;Y is (CH2)2;W is O; andU is (CH2)2,or a pharmaceutically acceptable salt thereof. 13. The kit of claim 12, wherein R3 is COOH. 14. The kit of claim 4, wherein: R1 is phenyl;R2 is N[(CH2)7NH2]2;R3 is COOH;R4 is phenyl;R5 is phenyl;R6 is CH2OH;X is (CH2)2;Y is (CH2)2;W is O; andU is (CH2)2,or a pharmaceutically acceptable salt thereof. 15. The pharmaceutical composition of claim 6, wherein the compound of Formula (IIA) is: or a pharmaceutically acceptable salt thereof. 16. The pharmaceutical composition of claim 6, wherein: R1 is phenyl;R2 is N[(CH2)7NH2]2;R4 is phenyl;R5 is phenyl;R6 is CH2OH;X is (CH2)2;Y is (CH2)2;W is O; andU is (CH2)2,or a pharmaceutically acceptable salt thereof. 17. The pharmaceutical composition of claim 16, wherein R3 is COOH. 18. The pharmaceutical composition of claim 6, wherein: R1 is phenyl;R2 is N[(CH2)7NH2]2;R3 is COOH;R4 is phenyl;R5 is phenyl;R6 is CH2OH;X is (CH2)2;Y is (CH2)2;W is O; andU is (CH2)2,or a pharmaceutically acceptable salt thereof.
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