HIV-integrase inhibitors, pharmaceutical compositions, and methods for their use
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/437
A61K-031/4353
C07D-471/02
C07D-471/00
C07D-471/12
출원번호
US-0765227
(2004-01-26)
발명자
/ 주소
Kuki,Atsuo
Li,Xinqiang
Plewe,Michael Bruno
Wang,Hai
Zhang,Junhu
출원인 / 주소
Agouron Pharmaceuticals, Inc.
인용정보
피인용 횟수 :
6인용 특허 :
4
초록▼
Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and condi
Beta-carboline hydroxamic acid compounds represented by formula (I) are described. The beta-carboline hydroxamic acid compounds and compositions containing those compounds may be used to inhibit or modulate the activity of HIV integrase enzyme and to treat HIV integrase-mediated diseases and conditions.
대표청구항▼
We claim: 1. A compound of formula (I), wherein: R1, R2, R3, R4, R 5, and R6 are independently selected from hydrogen, halogen, C1-C6 alkyl, alkoxy C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl,--OR c,--NO2, and--N(Rc)2; each Rc is independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, and
We claim: 1. A compound of formula (I), wherein: R1, R2, R3, R4, R 5, and R6 are independently selected from hydrogen, halogen, C1-C6 alkyl, alkoxy C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl,--OR c,--NO2, and--N(Rc)2; each Rc is independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, and C 2-C6 alkynyl; R7 is C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl, all of which are optionally substituted by one or more substituents independently selected from halogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, aryl, cycloalkyl, heterocycloalkyl, and heteroaryl, wherein said aryl, cycloalkyl, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C 2-C6 alkenyl, and C2-C6 alkynyl; R8 and R9 are independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl, wherein said alkyl, alkenyl, and alkynyl are optionally substituted with one or more substituents independently selected from halogen, aryl, cycloalkyl, heterocycloalkyl, and heteroaryl group, wherein said aryl, cycloalkyl, and heterocycloalkyl are optionally substituted with one or more substituents independently selected from halogen, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl; and pharmaceutically acceptable salts and solvates thereof. 2. A compound according to claim 1, wherein: R1, R2, R3, R4, R5, and R6 are independently selected from hydrogen,--N(Rc)2, and--NO2. 3. A compound according to claim 1, wherein R7 is C1-C6 alkyl, optionally substituted with aryl, cycloalkyl, heterocycloalkyl, and heteroaryl, wherein said aryl, cycloalkyl, heterocycloalkyl, and heteroaryl are optionally substituted with at least one substituent selected from halogen, C1-C6 alkyl, C2-C6 alkenyl, and C2-C6 alkynyl. 4. A compound according to claim 1, wherein R8 and R9 are independently selected from hydrogen and C1-C 6 alkyl, wherein said alkyl group is optionally substituted with aryl, and wherein said aryl is optionally substituted with at least one substituent selected from halogen and C1-C6 alkyl. 5. A compound according to claim 1, wherein: R1, R2, R3, R4, R 5, R6 are independently selected from hydrogen,--NH 2; and--NO2; R7 is 4-fluorobenzyl, (5-chlorothien-2-yl)methyl, 3-chloro-2-fluorobenzyl, benzyl, 4-methylbenzyl, 2,4-difluorobenzyl, 3-chloro-2,6-difluorobenzyl, or 3-chlorobenzyl; and R8 and R9 are independently selected from hydrogen, methyl, and benzyl. 6. A compound according to claim 1, wherein: R1, R2, R3, R4, R5 and R6 are hydrogen; R7 is--CH2phenyl, wherein said phenyl is substituted with at least one substitutent chosen from fluorine and chlorine; R8 is hydrogen or--CH3; and R9 is hydrogen or--CH3. 7. A compound according to claim 1, wherein: R1, R2, R3, R5 and R6 are hydrogen; R4 is--NO2 or--NH2; R7 is--CH2phenyl, wherein said phenyl is substituted with at least one substitutent chosen from fluorine and chlorine; R8 is hydrogen or--CH3; and R9 is hydrogen or--CH3. 8. A compound according to claim 1, wherein: R1, R2, R3, R4, R5 and R6 are hydrogen; R7 is--CH2phenyl, wherein said phenyl is substituted with at least one substitutent chosen from fluorine and chlorine; and R8 and R9 are hydrogen. 9. A compound according to claim 1, wherein: R1, R2, R3, R4, R5 and R6 are hydrogen; R7 is--CH2phenyl, wherein said phenyl is substituted with at least one substitutent chosen from fluorine and chlorine; and R8 and R9 are--CH3. 10. A compound according to claim 1, wherein: R1, R2, R3, R4, R5 and R6 are hydrogen; R7 is--CH2phenyl, wherein said phenyl is substituted with at least one substitutent chosen from fluorine and chlorine; R8 is hydrogen; and R9 is--CH3. 11. A compound according to claim 1, wherein: R1, R2, R3, R4, R5 and R6 are hydrogen; R7 is--CH2phenyl, wherein said phenyl is substituted with at least one substitutent chosen from fluorine and chlorine; R8 is--CH3; and R9 is hydrogen. 12. A compound according to claim 1, selected from 9-(4-fluorobenzyl)-N-hydroxy-9H-β-carboline-3-carboxamide; 9-[(5-chlorothien-2-yl)methyl]-N-hydroxy-9H-β-carboline-3-carboxamide; 9-(3-chloro-2-fluorobenzyl)-N-hydroxy-9H-β-carboline-3-carboxamide; 9-Benzyl-N-hydroxy-9H-β-carboline-3-carboxamide; 9-(4-methylbenzyl)-N-Hydroxy-9H-β-carboline-3-carboxamide; 9-(2,4-difluorobenzyl)-N-hydroxy-9H-β-carboline-3-carboxamide; 9-(3-chloro-2,6-difluorobenzyl)-N-hydroxy-9H-β-carboline-3-carboxamide; 6-amino-9-(3-chlorobenzyl)-N-hydroxy-9H-β-carboline-3-carboxamide; 9-(3-chloro-2,6-difluorobenzyl)-N-methoxy-9H-β-carboline-3-carboxamide; N-(benzyloxy)-9-(3-chloro-2,6-difluorobenzyl)-9H-β-carboline-3-carboxamide; 9-(3-chloro-2,6-difluorobenzyl)-N-hydroxy-N-methyl-9H-β-carboline-3-carboxamide; N-benzyl-9-(3-chloro-2,6-difluorobenzyl)-N-hydroxy-9H-β-carboline-3-carboxamide; 9-(4-fluorobenzyl)-N-hydroxy-N-methyl-9Hβ-carboline-3-carboxamide; and pharmaceutically acceptable salts and solvates thereof. 13. A pharmaceutical composition, comprising a therapeutically effective amount of at least one compound according to claim 1 and a pharmaceutically acceptable carrier, diluent, or vehicle. 14. A pharmaceutical composition, comprising a therapeutically effective amount of at least one compound according to claim 12 and a pharmaceutically acceptable carrier, diluent, or vehicle.
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