KR930003914A - 에이치아이브이(hiv) 및 관련 바이러스 억제를 위한 화합물 및 방법 - Google Patents
에이치아이브이(hiv) 및 관련 바이러스 억제를 위한 화합물 및 방법 Download PDFInfo
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- KR930003914A KR930003914A KR1019920013801A KR920013801A KR930003914A KR 930003914 A KR930003914 A KR 930003914A KR 1019920013801 A KR1019920013801 A KR 1019920013801A KR 920013801 A KR920013801 A KR 920013801A KR 930003914 A KR930003914 A KR 930003914A
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- substituted
- pyridyl
- thiourea
- ethyl
- alkyl
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- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract
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Claims (47)
- 하기 일반식(IB)의 화합물 또는 그의 염을 HIV와 접촉시키는 것을 포함하는 HIV 복제의 억제방법.상기식에서, n은 0 내지 4이고, Z는또는이며, Y는 0 또는 S이고, R11은 일반식R14는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화상태의 안정한 3내지 8원 유기 모노사이클릭 환이거나, 또는 S, 0및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 7 내지 10원 유기 비사이클릭 환이거나, 또는 일반식 (R10)y-X-[여기에서 y는 1또는 2이고, X는 N,S 또는 0이며, R10은 S,0 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포하 또는 불포화 상태의 안정한 3 내지 8원 유기 모노사이클릭환이건, 또는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화상태의 안정한 7 내지 10원 유기의 비사이클릭 환이거나, 또는 수소, C1-C6알킬, C2-C6알케닐 또는 C2-C6알키닐이다]의 그룹이거나, 또는 R14는 수소, 할로, 시아노, 카복시, 아미노, 티오, 히이드록시, C1-C4알콕시, C1-C6알킬, C2-C8알케닐, C2-C6알키닐 또는 C2-C8알켄옥시이고, R15및 R16은 각각 독립적으로 C3-C8사이클로알킬, 수소, C2-C6알킬, C2-C6알케일, 할로, 아미노, 니트로, 시아노, C1-C5알콕시, 하이드록시, 카복시, 하이드록시, 메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 카바모일 또는 할로-치환된 C1-C6알킬이며, R12는 수소, 하이드록시, C1-C6알킬, C1-C6알케닐, 아미노, 시아노, 니트로, C1-C5알콕시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 할로-치환된(C1-C6)알킬 또는 카바모일이고, R13은 S, O 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3내지 8원 유기 모노사이클릭 환이거나, 또는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 7내지 10원 유기 비사이클릭 환이거나, 또는 R11에 대해 정의한 바와 같다.
- 제1항에 있어서, R12, R15, R16이 수소이고 R13이 C1-C6알킬, 티아졸릴, 치환된 티아졸릴, 피라지닐, 치환된 피라지닐, 피리딜, 치환된 피리딜, 피리다지닐, 치환된 피리다지닐, 페닐 또는 치환된 페닐이며, R14가 페닐, 치환된 페닐, 피리딜, 치환된 피리딜 또는 사이클로헥세닐인 방법.
- 제2항에 있어서, R14가 페닐, 디플루오로페닐, 플루오로페닐, 사이클로 헥세닐, 피리딜 또는 p-하이드록시페닐인 방법.
- 제1항에 있어서, 적어도 하나의 다른 HIV억제제를 상기 HIV와 또한 접촉시킴을 추가로 포함하는 방법.
- 제4항에 있어서, 상기 억제제가, ddI, ddC 및 AZT중에서 선택되는 방법.
- 하기 일반식(IB)의 화합물 또는 그의 약제학적으로 허용되는 염과 적절한 담체를 포함하는 약제제제.상기식에서, n은 0 내지 4이고, Z는또는이며, Y는 0 또는 S이고, R11은 일반식R14는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화상태의 안정한 3내지 4원 유기 모노사이클릭 환이거나, 또는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 7 내지 10원 유기 비사이클릭 환이거나, 또는 일반식 (R10)y-X-[여기에서 y는 1또는 2이고, X는 N,S 또는 0이며, R10은 S,0 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포하 또는 불포화 상태의 안정한 3 내지 8원 유기 모노사이클릭환이건, 또는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화상태의 안정한 7내지 10원 유기의 비사이클릭 환이거나, 또는 수소, C1-C6알킬, C2-C6알케닐 또는 C2-C6알키닐이다]의 그룹이거나, 또는 R14는 수소, 할로, 시아노, 카복시, 아미노, 티오, 하이드록시, C1-C4알콕시, C1-C6알킬, C2-C8알케닐, C2-C6알키닐 또는 C2-C8알켄옥시이고, R15및 R16은 각각 독립적으로 C3-C8사이클로알킬, 수소, C1-C6알킬, C2-C6알케일, 할로, 아미노, 니트로, 시아노, C1-C5알콕시, 하이드록시, 카복시, 하이드록시, 메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 카바모일 또는 할로-치환된 C1-C6알킬이며, R12는 수소, 하이드록시, C1-C6알킬, C2-C6알케닐, 아미노, 시아노, 니트로, C1-C5알콕시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 트리할로(C1-C6)알킬 또는 카바모일이거나 할로-치환된 C1-C6알킬이고, R13은 S, 0 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3내지 8원 유기 모노사이클릭 환이거나, 또는 S, 0 및 N중에서 선택 된 헤테로원자 0 내지 5개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 7 내지 10원 유기 비사이클릭 환이거나, 또는 R11에 대해 정의한 바와 같으나 단, i)R11이 C1-C6알킬이고, R13이 C2-C8알케닐이며, Z가 >C=0이고, n이 0인 경우이거나, 또는 ii) R11이 C1-C6알킬 또는인 경우이거나, 또는 iii) R13이 C1-C6알킬 또는 페닐이고, Z가이며, n이 0인 경우에는 R12가 수소가 아니다.
- 제6항에 있어서, R12, R15및 R16이 수소이고 R13이 C1-C6알킬, 티아졸릴, 치환된 티아졸릴, 피라지닐, 치환된 피라지닐, 피리딜, 치환된 피리딜, 피리다지닐, 치환된 피리다지닐, 페닐 또는 치환된 페닐이며, R14가 페닐, 치환된 페닐, 피리딜, 치환된 피리딜 또는 사이클로헥세닐인 제제.
- 제7항에 있어서, R14가 페닐, 피리딜 또는 p-하이드록시페닐인 방법.
- 제6항에 있어서, 적어도 하나의 다른 치료제를 추가 함유하는 제제.
- 제9항에 있어서, 상기 치료제가, ddI, ddC 및 AZT중에서 선택되는 제제.
- 하기 일반식(IB)의 화합물 및 그의 염.상기식에서, n은 0 내지 4이고, Z는또는이며, Y는 0 또는 S이고, R11은 일반식R14는 사이클로(C3-C8)알킬, 사이클로(C3-C8)알케닐, 이소티아졸릴, 치환된 이소티아졸릴, 테트라졸릴, 치환된 테트라졸릴, 트리아졸릴, 치환된 트리아졸릴, 피리딜, 치환된 피리딜, 이미다졸릴, 치환된 이미다졸릴, 페닐, 치환된 페닐, 나프틸, 치환된 나프틸, 벤즈옥사졸릴, 치환된 벤즈옥사졸릴, 벤즈이미다졸릴, 치환된 벤즈이미다졸릴, 티아졸릴, 치환된 티아졸릴, 옥사졸릴, 치환된 옥사졸릴, 벤조티아졸릴, 치환된 벤조티아졸릴, 피라지닐, 치환된 피라지닐, 피리다지닐, 치환된 피리다지닐, 티아디아졸릴, 치환된 티아디아졸릴, 벤조트리아졸릴, 치환된 벤조트리아졸릴, 피롤릴, 치환된 피롤릴, 인돌릴, 치환된 인돌릴, 벤조티에닐, 치환된 벤조티에닐, 티에닐, 치환된 티에닐, 벤조푸릴, 치환된 벤조푸릴, 푸릴, 치환된 푸릴, 퀴놀리닐, 치환된 퀴놀리닐, 이소퀴놀리닐, 치환된 이소퀴놀리닐, 피라졸릴 또는 치환된 파라졸릴이거나, 또는 R14는 일반식 (R10)y-X-[여기에서, y는 1또는 2이고, X는 N, S 또는 0이며, R10은 사이클로(C3-C8)알킬, 사이클로(C3-C8)알케닐, 이소티아졸릴, 치환된 이소티아졸릴, 테트라졸릴, 치환된 테트라졸릴, 트리아졸릴, 치환된 트리아졸릴, 피리딜, 치환된 피리딜, 이미다졸릴, 치환된 이미다졸릴, 페닐, 치환된 페닐, 나프틸, 치환된 나프틸, 벤즈옥사졸릴, 치환된 벤즈옥사졸릴, 벤즈 이미다졸릴, 치환된 벤즈이미다졸릴, 티아졸릴, 치환된 티아졸릴, 옥사졸릴, 치환된 옥사졸릴, 벤조티아졸릴, 치환된 벤조티아졸릴, 피라지닐, 치환된 피라지닐, 피리다지닐, 치환된 피리다지닐, 티아디아졸릴, 치환된 티아디아졸릴, 벤조트리아졸릴, 치환된 벤조트리아졸릴, 피롤릴, 치환된 피롤릴, 인돌릴, 치환된 인돌릴, 벤조티에닐, 치환된 벤조티에닐, 티에닐, 치환된 티에닐, 벤조푸릴, 치환된 벤조푸릴, 푸릴, 치환된 푸릴, 퀴놀리닐, 치환된 퀴놀리닐, 이소퀴놀리닐, 치환된 이소퀴놀리닐, 피라졸릴 및 치환된 피라졸릴이다]의 그룹이거나, 또는 R14는 할로, 시아노, 카복시, 아미노, 티오, 하이드록시, C1-C4알콕시, C2-C8알카노일, C2-C8알키닐, 또는 C2-C8알켄옥시이고, R12는 수소, 하이드록시, C1-C6알킬, C2-C6알케일, 아미노, 시아노, 니트로, C1-C5알콕시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 할로-치환된 C1-C6알킬 또는 카바모일이며, R13은 사이클로(C3-C8)알킬, 사이클로(C3-C8)알케닐, 이소티아졸릴, 치환된 이소티아졸릴, 테트라졸릴, 치환된 테트라졸릴, 트리아졸릴, 치환된 트리아졸릴, 피리딜, 치환된 피리딜, 이미다졸릴, 치환된 이미다졸릴, 페닐, 피환된 페닐, 나프틸, 치환된 나프틸, 벤즈옥사졸릴, 치환된 벤즈옥사졸릴, 벤즈이미다졸릴, 치환된 벤즈이미다졸릴, 티아졸릴, 치환된 티아졸릴, 옥사졸릴, 치환된 옥사졸릴, 벤조티아졸릴, 치환된 벤조티아졸릴, 피라지닐, 치환된 피라지닐, 피리다지닐, 치환된 피리다지닐, 티아디아졸릴, 치환된 티아디아졸릴, 벤조트리아졸릴, 치환된 벤조트리아졸릴, 피롤릴, 치환된 피롤릴, 인돌릴, 치환된 인돌릴, 벤조티에닐, 치환된 벤조티에닐, 티에닐, 치환된 티에닐, 벤조푸릴, 치환된 벤조푸릴, 푸릴, 치환된 푸릴, 퀴놀리닐, 치환된 퀴놀리닐, 이소퀴놀리닐, 치환된 이소퀴놀리닐, 피라졸릴 또는 치환된 파라졸릴이거나, 또는 R13은 R11에서 정의한 바와 같고, R15및 R16은 각각 독립적으로 C3-C8사이클로알킬, 수소, C1-C6알킬, C2-C6알케닐, 할로, 아미노, 니트로, 시아노, C1-C5알콕시, 하이드록시, 카복시, 하이드록시 메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 카바모일, 또는 할로-치환된(C1-C6)알킬이지만, 단, R15및 R16이 둘다 수소이고, R14가 페닐이며, R13이 페닐이고, Z가이며, n이 0인 경우 R12는 수소가 아니다.
- 제11항에 있어서, 적어도 하나의 다른 치료제와 병용되는 화합물.
- 제12항에 있어서, 상기 치료제가 ddI, ddC 및 AZT중에서 선택되는 화합물.
- 하기 일반식의 화합물 및 그의 염.상기식에서 R11은 일반식 -CH2-R14의 그룹이고, R14는 페닐, p-하이드록시페닐, 디플루오로페닐, 플루오로페닐, 피리딜, 또는 사이클로헥세닐이며, R13은 메틸, 에틸, n-부틸, 페닐메틸, 티아졸릴, 벤조티아졸릴, 피리딜, 또는 티아디아졸이고, R14가 p-하이드록시페닐인 경우 R13은 페닐일수도 있다.
- 제14항에 있어서, 적어도 하나의 다른 치료제와 병용되는 화합물.
- 제15항에 있어서, 상기 치료제가 ddI, ddC 및 AZT중에서 선택되는 화합물.
- 하기 일반식(IA)의 화합물 또는 그의 염을 HIV와 접촉시키는 것을 포함하는, HIV복제의 억제 방법.상기식에서 R1은 S, 0및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3 내지 8원 유기 모노사이클릭 환이거나, 또는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 7 내지 10원 유기 비사이클릭 환이고, R2는 일반식의 그룹이며, R5는 R1에 대해 상기 정의한 바와 같거나, 또는 일반식 (R10)y-X[여기에서 y는 1 또는 2이고, X는 N,S 또는 0이며, R10은 은 R1에 대해 정의한 바와 같거나, 수소, C1-C6알킬, C2-C6알케닐, 또는 C2-C6알키닐이다]의 그룹이거나, 또는 R5는 수소, 할로, 시아노, 카복시, 아미노, 티오, 하이드록시, C1-C4알콕시, C1-C6알킬, C2-C8알케닐, C2-C6알키닐 또는 C2-C8알켄옥시이고, R6, R7, R8및 R9는 각각 독립적으로 C3-C8사이클로알킬, 수소, C1-C6알킬, C2-C6알케닐, C2-C6알키닐, 할로, 아미노, 니트로, 시아노, C1-C5알콕시, 하이드록시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 카바모일, 또는 할로-치환된 C1-C6알킬이거나, 이들중 2개의 그룹은 이들이 결합된 탄소와 함께 결합하여, S, O 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3 내지 7원 유기 모노사이클릭 환을 형성하거나, R6과 R8또는 R7과 R9가 이들이 결합된 탄소와 함께 결합하여 S, N 또는 0중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3 내지 7원 유기 모노사이클릭환을 형성하고, R3및 R4는 각각 독립적으로 수소, 하이드록시, C1-C6알킬, C2-C6알케닐, C2-C6알키닐, 아미노, 시아노, 니트로, C1-C5알콕시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 할로-치환된 (C1-C6)알킬 또는 카바모일이다.
- 제17항에 있어서, R3, R4, R6, R7, R8및 R9가 모두 수소인 방법.
- 제18항에 있어서, R5가 페닐, 치환된 페닐, 나프틸, 치환된 나프틸, 피리딜, 치환된 피리딜, 또는 사이클로헥세닐인 방법.
- 제18항에 있어서, R1이 티아졸릴, 치환된 티아졸릴, 벤조티아졸릴, 치환된 벤조티아졸릴, 피라지닐, 치환된 피라지닐, 피리딜, 치환된 피리딜, 피리다지닐, 치환된 피리다지닐, 티아디아졸릴 또는 치환된 티아디아졸릴인 방법.
- 제17항에 있어서, 상기 화합물이 N-[2-(2-피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아 및 그의 염산염인 방법.
- 제17항에 있어서, 적어도 하나의 다른 HIV 억제제를 상기 HIV와 또한 접촉시키는 것을 추가로 포함하는 방법.
- 제22항에 있어서, 상기 억제제가 ddI, ddC 및 AZT 중에서 선택되는 방법.
- 하기 일반식(IA)의 화합물 또는 그의 염.상기식에서 R1은 S, 0 및 N중에서 선택된 헤테로원자 0내지 4개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3 내지 8원 유기 모노사이클릭 환이거나, 또는 S, 0 및 N중에서 선택된 헤테로원자 0 내지 5개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 7 내지 10원 유기 비사이클릭 환이고, R2는 일반식의 그룹이며, R5는 R1에 대해 상기 정의한 바와 같거나, 또는 일반식 (R10)y-X[여기에서 y는 1 또는 2이고, X는 N,S 또는 0이며, R10은 은 R1에 대해 정의한 바와 같거나, 수소, C1-C6알킬, C2-C6알케닐, 또는 C2-C6알키닐이다]의 그룹이거나, 또는 R5는 수소, C1-C6할로, 시아노, 카복시, 아미노, 티오, 하이드록시, C1-C4알콕시, C2-C8알케닐, C2-C8알키닐 또는 C2-C8알켄옥시이고, R6및 R7는 각각 독립적으로 C3-C8사이클로알킬, 수소, C1-C6알킬, C2-C6알케닐, C1-C6알키닐, 할로, 아미노, 니트로, 시아노, C1-C3알콕시, 하이드록시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 카바모일, 또는 할로-치환된 C1-C6알킬이며, R8와 R9는 이들이 결합된 탄소와 함께 결합하여, S, 0 및 N중에서 선택된 헤테로원자 0 내지 4개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3 내지 7원 유기 모노사이클릭 환을 형성하거나, R6과 R8또는 R7과 R9가 이들이 결합된 탄소와 함께 결합하여 S, N 또는 0중에서 선택된 헤테로원자 0 내지 4개를 갖는 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3 내지 7원 유기 모노사이클릭 환을 형성하고, R3및 R4는 각각 독립적으로 수소, 하이드록시, C1-C6알킬, C2-C6알케닐, C2-C6알키닐, 아미노, 시아노, 니트로, C1-C5알콕시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 할로-치환된 (C1-C6)알킬 또는 카바모일이다.
- 제24항에 있어서, R1이 티아졸릴, 치환된 티아졸릴, 피리딜, 치환된 피리딜, 피리다지닐, 치환된 피리다지닐, 또는 치환된 파라지닐이고, R5가 피리딜, 치환된 피리딜, 페닐, 또는 치환된 페닐이며, R8및 R9가 이들이 결합된 탄소와 함께 결합하여 사이클로 프로필을 형성하는 화합물.
- 제24항에 있어서, N-(2-시스-페닐사이클로프로필)-N′-2-{티아졸릴}티오우레아인 화합물.
- 제24항에 있어서, N-(2-시스-페닐사이클로프로필)-N′-[2-(5-브로모)피리딜)티오우레아, N-(2-시스-페닐사이클로프로필)-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(시스-피리딜)사이클로프로필]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(시스-2-피리딜)사이클로프로필]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(시스-2-(6-플루오로)피리딜)사이클로프로필]-N′-[2-(5-클로로)피리딜]티오우레아, N- [2-(시스-2-(6-플루오로)피리딜)사이클로프로필]-N′-(2-(5-브로모)피리딜]티오우레아, N-[2-(시스-2-(6-메톡시)피리딜)사이클로프로필]-N′-[2-(5-클로로)피리딜]티오우레아, N- [2-(시스-2-(6-에톡시)피리딜)사이클로프로필]-N′-[2-(5-브로모)피리딜)티오우레아, N-[2-(시스-2-(6-에톡시)피리딜)사이클로프로필7]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(시스-2-(6-에톡시)피리딜)사이클로프로필]-N′-[2-(5-클로로)피리딜]티오우레아 및 이들의 염중에서 선택되는 화합물.
- 제24항에 있어서, 적어도 하나의 다른 치료제를 또한 포함하는 화합물.
- 제28항에 있어서, 상기 치료제가 ddI, ddC 및 AZT중에서 선택되는 화합물.
- 제24항의 화합물과 함께 그에 대한 담체, 부형제 또는 희석제 하나 이상을 포함하는 약학 제제.
- 제30항에 있어서, 적어도 하나의 다른 치료제를 포함하는 제제.
- 제31항에 있어서, 상기 치료제가 ddI, ddC 및 AZT인 제제.
- 하기 일반식(IA)의 화합물 또는 그의 염.상기식에서 R1은 사이클로(C3-C8)알킬, 사이클로(C3-C8)알케닐, 이소티아졸릴, 치환된 이소티아졸릴, 테트라졸릴, 치환된 테트라졸릴, 트리아졸릴, 치환된 트리아졸릴, 피리딜, 치환된 피리딜, 이미다졸릴, 치환된 이미다졸릴, 페닐, 피환된 페닐, 나프틸, 치환된 나프틸, 벤즈옥사졸릴, 치환된 벤즈옥사졸릴, 벤즈이미다졸릴, 치환된 벤즈이미다졸릴, 티아졸릴, 치환된 티아졸릴, 옥사졸릴, 치환된 옥사졸릴, 벤조티아졸릴, 치환된 벤조티아졸릴, 피라지닐, 치환된 피라지닐, 피리다지닐, 치환된 피리다지닐, 티아디아졸릴, 치환된 티아디아졸릴, 벤조트리아졸릴, 치환된 벤조트리아졸릴, 피롤릴, 치환된 피롤릴, 인돌릴, 치환된 인돌릴, 벤조티에닐, 치환된 벤조티에닐, 티에닐, 치환된 티에닐, 벤조푸릴, 치환된 벤조푸릴, 푸릴, 치환된 푸릴, 퀴놀리닐, 치환된 퀴놀리닐, 이소퀴놀리닐, 치환된 이소퀴놀리닐, 피라졸릴 또는 치환된 피라졸릴이고,R2는 일반식그룹이며, R5는 피리딜, 치환된 피리딜, 페닐, 치환된 페닐, 나프틸, 치환된 나프틸, 사이클로헥세닐, 벤질 또는 일반식 (R10)y-X-[여기에서 y는 1 또는 2이고, X는 N,S 또는 0이며, R10은 은 R1에 대해 정의한 바와 같거나, 수소, C1-C6알킬, C2-C6알케닐, 또는 C2-C6알키닐이다]의 그룹이거나, 또는 R5는 수소, 할로, 시아노, 카복시, 아미노, 티오, 하이드록시, C1-C4알콕시, C1-C6알킬, C2-C8알케닐, C2-C8알키닐 또는 C2-C8알켄옥시이고, R6, R7, R8및 R9는 각각 독립적으로 C3-C8사이클로알킬, 수소, C1-C6알킬, C2-C6알케닐, C21-C6알키닐, 할로, 아미노, 니트로, 시아노, C1-C3알콕시, 하이드록시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 카바모일, 또는 할로-치환된 C1-C6알킬이거나, R6와 R8또는 R7과 R9가 이들이 결합된 탄소와 함께 결합하여, S, N 및 0중에서 선택된 헤테로원자 0내지 4개를 갖는, 치환되거나 치환되지 않은 포화 또는 불포화 상태의 안정한 3내지 7원 유기 모노사이클릭 환을 형성하거나, R3및 R4는 각각 독립적으로 수소, 하이드록시, C1-C6알킬, C2-C6알케닐, C2-C6알키닐, 아미노, 시아노, 니트로, C1-C5알콕시, 카복시, 하이드록시메틸, 아미노메틸, 카복시메틸, C1-C4알킬티오, C1-C4알카노일옥시, 할로-치환된 (C1-C6)알킬 또는 카바모일이나, 단, R1이 피리딜이거나, 할로겐, 하이드록시, C1-C6알킬, 또는 C1-C6알콕시로 일치환된 피리딜이고, R3및 R4가 수소이며, R6, R7, R8및 R9가 수소인 경우에 R5는 비-치환된 페닐이 아니다.
- 제33항에 있어서, R3, R4, R5, R6, R7, R8및 R9가 모두 수소인 화합물.
- 제33항에 있어서, R5가 페닐, 치환된 페닐, 피리딜, 치환된 피리딜, 또는 사이클로헥세날인 화합물.
- 제33항에 있어서, R1이 피리딜, 피환된 피리딜, 티아졸릴, 치환된 티아졸릴, 벤조티아졸릴, 치환된 벤조티아졸릴, 티아디아졸릴, 치환된 티아디아졸릴, 피라지닐, 치환된 피라지닐, 피리다지닐 또는 치환된 피리다지닐인 화합물.
- 제33항에 있어서, R1이 피리딜, 플루오로피리딜, 클로로피리딜, 브로모피리딜, 시아노피리딜, 메틸피리틸, 에틸피리딜, 트리플루오로 메틸피리딜, 디메틸피리딜, 티아졸릴, 플루오로티아졸릴, 클로로티아졸릴, 브로모티아졸릴, 메틸티아졸릴, 에틸티아졸릴, (니트로페닐)티아졸릴, 트리플루오로 메틸티아졸릴, 디메틸티아졸릴, 시아노티아졸릴, 피리딜티아졸릴, 벤조티아졸릴, (플루오로벤조)티아졸릴, 플루오로피라지닐, 클로로피라지닐, 브로모피라지닐, 시아노피라지닐, 메틸피라지닐, 에틸 피라지닐, 트리플루오로메틸피라지닐, 디메틸피라지닐, 피리다지닐, 플루오로피리다지닐, 클로로피리다지닐, 브로모피리다지닐, 시아노피리다지닐, 메틸피라다지닐, 에틸피라다지닐, 트리플루오로메틸피리다지닐 또는 디메틸피라다지닐이며, R5가 피리딜, 치환된 피리딜, 사이클로헥세닐, 나프틸, 페닐, 또는 메톡시, 에톡시, 브로모, 메틸, 플루오로, 클로로, 아지도 또는 이들 2종 이상에 의해 1 내지 4치환된 페닐이고, R6및 R8이 각각 독립적으로 수소 또는 C1-C6알킬인 화합물 또는 그의염.
- 제33항에 있어서, N-(2-(2-메톡시페닐)에틸)-N′-[2-(4-시아노)티아졸릴]티오우레아, N-(2-(2-메톡시페닐)에틸)-N′-[2-(4-트리플루오로메틸)티아졸릴]티오우레아, N-(2-(2-메톡시페닐)에틸)-N′-[2-(4-에틸)티아졸릴]티오우레아, N-(2-(2-메톡시페닐)에틸)-N′-[2-(5-브로모)피리딜)티오우레아, N-(2-(2-메톡시페닐)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(3-메톡시페닐)에틸)-N′-[2-(4-시아노)티아졸릴]티오우레아, N-(2-(2-메톡시페닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(3-메톡시페닐)에틸)-N′-[2-(4-트리플루오로메틸)피리딜]티오우레아, N-(2-(3-메톡시페닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(3-메톡시페닐)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(2-에톡시페닐)에틸)-N′-[2-(5-브로모)피리딜)티오우레아, N-(2-(2-에톡시페닐)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[2-(4-시아노)티아졸릴)티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[2-(4-트리플루오로메틸)티아졸릴]티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[2-(4-에틸)티아졸릴)티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[2-(5-브로모)피라지닐]티오우레아, N-(2-(2,6-디플루오로페닐)에틸)-N′-[3-(6-클로로)피리다지닐)티오우레아, N-(2-(2-플루오로-6-메톡시페닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(2-플루오로-6-메록시페닐)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(2-클로로페닐)에틸)-N′-[2-(4-시아노)티아졸릴]티오우레아, N-(2-(2-클로로페닐)에틸)-N′-[2-(4-에틸)티아졸릴]티오우레아, N-(2-(2-클로로페닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(2-클로로페닐)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(3-클로로페닐)에틸)-N′-[2-(4-시아노)티아졸릴]티오우레아, N-(2-(3-클로로페닐)에틸)-N′-[2-(4-에틸)티아졸릴]티오우레아, N-(2-(3-클로로페닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(3-클로로페 닐)에틸)-N′-[2-(5-클로로)피리딜)티오우레아, N-(2-(1-사이클로헥세닐)에틸)-N′-(2-(4-시아노)티아졸릴]티오우레아, N-(2-(1-사이클로헥세닐)에틸)-N′-[2-(4-트리플루오로메틸)티아졸릴]티오우레아, N-(2-(1-사이클로헥세닐)에틸)-N′-[2-(4-에틸)티아졸릴]티오우레아, N-(2-(1-사이클로헥세닐)에틸)-N′-[2-(5-브로모)피리딜]티오우레아, N-(2-(1-사이클로헥세닐)에틸)-N′-[2-(5-클로로)티아졸릴)티오우레아, N-(2-(1-사이클로헥세닐)에틸)-N′-[3-(6-클로로)피리다지닐]티오우레아, N-(2-(2,5-디메톡시페닐)에틸)-N′-[2-(5-클로로)피라지닐)티오우레아, N-(2-(2,5-디메톡시페닐)에틸)-N′-[2-(5-브로모)피라지닐]티오우레아, N-(2-(2-피리딜)에틸)-N′-[2-(5-브로모)피리딜]티오우레아,N-(2-(2-피리딜)에틸)-N′-[2-(5-클로로)피리딜]티오우레아, N-(2-(2-피리딜)에틸)-N′-[2-(5-트리플루오로메틸)피리딜]티오우레아, N-(2-(2-피리딜)에틸)-N′-[2-(5-에틸)피리딜]티오우레아, N-(2-(2-피리딜)에틸)-N′-[2-(5-메틸)피리딜]티오우레아, N-[2-(2-(6-메톡시)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(6-메톡시)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(6-에톡시)피리딜)에틸]-N′-[2-(5-브로모)피리딜)티오우레아, N-[2-(2-(6-에톡시)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(6-플루오로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(6-플루오로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(3-플루오로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(3-플루오로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(6-클로로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(6-클로로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(6-클로로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(3-메톡시-6-플루오로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(3-메톡시-6-플루오로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(5-에톡시-6-플루오로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(5-에톡시-6-플루오로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(3-에톡시-6-플루오로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(3-에톡시-6-플루오로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(3,6-디플루오로)피리딜)에틸]-N′-[2-(5-브로모)피리딜]티오우레아, N-[2-(2-(3,6-디플루오로)피리딜)에틸]-N′-[2-(5-클로로)피리딜]티오우레아, N-[2-(2-(3,6-디플루오로-3-메톡시페닐)에틸]-N′-[2-(5-브로모)피리딜]티오우레아 및 이들의 염중에서 선택되는 화합물.
- 제33항에 있어서, 적어도 하나의 다른 치료제를 추가로 포함하는 화합물.
- 제39항에 있어서, 상기 치료제가 ddI, ddC 및 AZT중에서 선택되는 화합물
- 제33항의 화합물과 그에 대한 담체, 부형제 또는 희석제 하나 이상을 포함하는 약제 제제.
- 제41항에 있어서, 적어도 하나의 다른 치료제를 포함하는 제제.
- 제42항에 있어서, 상기 치료제가 ddI, ddC 및 AZT중에서 선택되는 제제.
- 하기 일반식 화합물 및 그의 염.상기식에서, R1은 피리딜, 플루오로피리딜, 클로로피리딜, 브로모피리딜, 시아노피리딜, 메틸피리딘, 에틸피리딘, 트리플루오로 메틸피리딜, 디메틸피리딜, 티아졸릴, 플루오로티아졸릴, 클로로아졸린, 브로모티아졸릴, 메틸티아졸릴, 에틸티아졸릴, (니트로페닐)티아졸릴, 트리플루오로 메틸티아졸릴, 디메틸티아졸릴, 시아노티아졸릴, 피리딜티아졸릴, 벤조티아졸릴, (플루오로벤조)티아졸릴, 플루오로피라지닐, 클로로피라지닐, 브로모피라지닐, 시아노피라지닐, 메틸피라지닐, 에틸 피라지닐, 트리플루오로메틸피라지닐, 디메틸피라지닐, 피리다지닐, 플루오로피리다지닐, 클로로피리다지닐, 브로모피리다지닐, 시아노피리다지닐, 메틸피라다지닐, 에틸피라다지닐, 트리플루오로메틸피리다지닐 또는 디메틸피라다지닐이고, R5는 피리딜, 치환된 피리딜, 사이클로헥세닐, 나프틸, 페닐이거나 메톡시, 에톡시, 브로모, 메틸, 플루오로, 클로로, 아지도 또는 이들 2종 이상에 의해 1 내지 4치환된 페닐이며, R6및 R8은 각각 독립적으로 수소 또는 C1-C6알킬이나, 단, R1이 피리딜이거나, 할로겐, 하이드록시, C1-C6알킬, 또는 C1-C6알콕시로 일치환된 피리딜이고, R3및 R4가 수소이며, R6및 R8이 수소인 경우, R8는 비치환된 페닐이 아니다.
- 제44항에 있어서, 적어도 하나의 다른 치료제와 병용되는 화합물.
- 제45항에 있어서, 상기 치료제가 ddI, ddC 또는 AZT중에서 선택되는 화합물.
- N-[2-(2-피리딜)에틸]-N′-[2-(5-브로모)피리딜)티오우레아 또는 그의 염산염.※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
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US5593993A (en) * | 1991-08-02 | 1997-01-14 | Medivir Ab | Method for inhibition of HIV related viruses |
EP0706514B1 (en) * | 1993-08-24 | 1998-11-18 | Medivir Ab | Compounds and methods for inhibition of hiv and related viruses |
CA2253502A1 (en) * | 1996-05-06 | 1997-11-13 | Stephen Warren Kaldor | Anti-viral compounds |
AU2752597A (en) * | 1996-05-06 | 1997-11-26 | Eli Lilly And Company | Anti-viral compounds |
AU2826597A (en) * | 1996-05-06 | 1997-11-26 | Eli Lilly And Company | Anti-viral compounds |
US6127422A (en) * | 1996-05-06 | 2000-10-03 | Eli Lilly And Company | Anti-viral method |
SI0806408T1 (en) * | 1996-05-06 | 2001-04-30 | Lilly Co Eli | Anti-viral compounds |
US6103923A (en) * | 1996-05-06 | 2000-08-15 | Eli Lilly And Company | Anti-viral compounds |
US6156924A (en) * | 1996-05-06 | 2000-12-05 | Eli Lilly And Company | Anti-viral compounds |
US6096917A (en) * | 1997-05-02 | 2000-08-01 | Eli Lilly And Company | Anti-viral compounds |
US5998411A (en) * | 1998-03-17 | 1999-12-07 | Hughes Institute | Heterocyclic nonnucleoside inhibitors of reverse transcriptase |
US6136335A (en) * | 1998-12-31 | 2000-10-24 | Hughes Institute | Phenethyl-5-bromopyridylthiourea (PBT) and dihydroalkoxybenzyloxopyrimidine (DABO) derivatives exhibiting spermicidal activity |
US7186736B1 (en) * | 1999-03-20 | 2007-03-06 | Parker Hughes Institute | NNI for treatment of multi-drug resistant HIV |
US6258831B1 (en) | 1999-03-31 | 2001-07-10 | The Procter & Gamble Company | Viral treatment |
US6245788B1 (en) * | 1999-03-31 | 2001-06-12 | The Procter & Gamble Company | Viral treatment |
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