α-Haloketone derivatives of imidazolyl-substituted aromatic compounds and compounds prepared therefrom
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/44
C07D-401/00
출원번호
UP-0765397
(2007-06-19)
등록번호
US-7799808
(2010-10-11)
발명자
/ 주소
Cheng, Soan
Comer, Daniel D.
Mao, Long
Balow, Guity P.
Pleynet, David
출원인 / 주소
Neurogenetic Pharmaceuticals, Inc.
대리인 / 주소
Foley & Lardner LLP
인용정보
피인용 횟수 :
6인용 특허 :
52
초록
Novel compounds, compositions, and kits are provided. Methods of modulating Aβ levels, and methods of treating a disease associated with aberrant Aβ levels are also provided.
대표청구항▼
What is claimed is: 1. A compound having a structure corresponding to Formula (I): A-B-C(O)—CR2—X (I) wherein A is: wherein each E is independently CR1; and each R1 is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstitu
What is claimed is: 1. A compound having a structure corresponding to Formula (I): A-B-C(O)—CR2—X (I) wherein A is: wherein each E is independently CR1; and each R1 is independently hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylamido, substituted or unsubstituted alkylamino, substituted or unsubstituted amino, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted aryl; B is wherein each G is independently CR2 or N, provided that one or two G′ s are N; and wherein each R2 is independently selected from hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylamido, substituted or unsubstituted alkylamino, substituted or unsubstituted amino; each R is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted alkoxy, substituted or unsubstituted alkylamido, substituted or unsubstituted alkylamino, substituted or unsubstituted cycloalkyl, or substituted or unsubstituted aryl; and X is halogen. 2. A compound according to claim 1 having the structure: wherein one or two G′ s are N, and the remaining G′ s are CH. 3. A compound according to claim 1 having the structure: wherein: one or both G′ s are N and, when only one G is N, the other G is CH, and b is 0-2. 4. A compound according to claim 1 wherein A is unsubstituted imidazolyl. 5. A compound according to claim 1 wherein A is a substituted imidazolyl. 6. A compound according to claim 5 wherein A is a 4-substituted imidazolyl. 7. A compound according to claim 5 wherein said imidazolyl is alkyl substituted. 8. A compound according to claim 5 wherein said imidazolyl is C1-C5 alkyl substituted. 9. A compound according to claim 8 wherein said imidazolyl is methyl substituted. 10. A compound according to claim 8 wherein said imidazolyl is ethyl substituted. 11. A compound according to claim 5 wherein said imidazolyl is halogen substituted. 12. A compound according to claim 11 wherein said imidazolyl is chloro-substituted. 13. A compound according to claim 11 wherein said imidazolyl is bromo-substituted. 14. A compound according to claim 1 wherein B is unsubstituted 2-pyridinyl. 15. A compound according to claim 1 wherein at least one R2 is a halogen. 16. A compound according to claim 15 wherein said halogen is fluorine. 17. A compound according to claim 1 wherein at least one R2 is optionally substituted alkoxy. 18. A compound according to claim 1 wherein each R is hydrogen. 19. A compound according to claim 1 wherein X is chlorine. 20. A compound according to claim 1 wherein X is bromine. 21. A compound according to claim 1 wherein X is iodine. 22. A compound according to claim 1 having a structure selected from the group consisting of: 23. A method of making a compound according to claim 1, said method comprising: contacting an acetylpyridinyl-boronic acid with an optionally substituted imidazole in a suitable solvent under conditions suitable to form an imidazolyl pyridyl ketone, and thereafter contacting said imidazolyl pyridyl ketone with bromine under conditions suitable to form a compound of Formula (I). 24. A method of making a compound according to claim 1, said method comprising: contacting a chloropyridinyl-alkanone with an optionally substituted imidazole in a suitable solvent under conditions suitable to form an imidazolyl pyridyl ketone, and thereafter contacting said imidazolyl pyridyl ketone with bromine under conditions suitable to form a compound of Formula (I). 25. A method of making a compound according to claim 1, said method comprising: contacting a 3-fluoro, 4-chloropyridinyl-alkanone with an optionally substituted imidazole in a suitable solvent under conditions suitable to form an imidazolyl fluoro pyridyl ketone, and thereafter contacting said imidazolyl fluoropyridyl ketone with bromine under conditions suitable to form a compound of Formula (I). 26. A compound according to claim 1 wherein at least one R is hydrogen.
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