IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
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| 국제특허분류(IPC7판) |
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| 출원번호 |
US-0323755
(1994-10-14)
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발명자
/ 주소 |
- Hudkins Robert L. (Chester Springs PA) Knight
- Jr. Ernest (Wilmington DE)
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| 출원인 / 주소 |
- Cephalon, Inc. (West Chester PA 02)
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| 인용정보 |
피인용 횟수 :
49 인용 특허 :
0 |
초록
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Disclosed herein are compounds referred to as “fused pyrrolocarbazoles”which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: [Figure] Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as wel
Disclosed herein are compounds referred to as “fused pyrrolocarbazoles”which possess a variety of functional activities. The disclosed compounds are represented by the following general formula: [Figure] Methodologies for the synthetic production of fused pyrrolocarbazoles are also disclosed, as well as exemplary uses of the compounds.
대표청구항
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A fused pyrrolocarbazole represented by the following general formula: [Figure] wherein: a) R1 is selected from the group consisting of H, alkyl of 1-4 carbons aryl, arylalkyl, heteroaryl, heteroarylalkyl, COR9, where R9 is selected from the group consisting of alkyl of 1-4 carbons, and aryl; －OR10,
A fused pyrrolocarbazole represented by the following general formula: [Figure] wherein: a) R1 is selected from the group consisting of H, alkyl of 1-4 carbons aryl, arylalkyl, heteroaryl, heteroarylalkyl, COR9, where R9 is selected from the group consisting of alkyl of 1-4 carbons, and aryl; －OR10, where R10 is selected from the group consisting of H and alkyl of 1-4 carbons; －CONH2, －NR7R8, －(CH2)nNR7R8, where n is an integer selected from the group consisting of 1, 2, 3, and 4; and －O(CH2)nNR7R8 wherein either 1) R7 and R8 independently are selected from the group consisting of H and alkyl of 1-4 carbons; or 2) R7 and R8 are combined together to form a linking group of the general formula －(CH2)2－X1－(CH2)2－, where X1 is selected from the group consisting of O, S and CH2; c) R2is selected from the group consisting of H, －SO2R9, －CO2R9, COR9, alkyl of 1-8 carbons, alkenyl of 1-8 carbons, alkynyl of 1-8 carbons, and a monosaccharide of 5-7 carbons wherein each hydroxyl group of said monosaccharide is independently selected from the group consisting of unsubstituted hydroxyl group and a replacement moiety replacing said hydroxyl group, said replacement moiety selected from the group consisting of H, alkyl of 1-4 carbons, alkylcarbonyloxy of 2-5 carbons and alkoxy of 1-4 carbons; wherein either 1 ) each alkyl of 1-8 carbons, alkenyl of 1-8 carbons, or alkynyl of 1-8 carbons is unsubstituted; or 2) each alkyl of 1-8 carbons, alkenyl of 1-8 carbons, or alkynyl of 1-8 carbons is independently substituted with a moiety selected from the group consisting of 1-3 aryl of 6-10 carbons, heteroaryl, F, Cl, Br, I, －CN, －NO2, OH, －OR9, －O(CH2)nNR7R8, －OCOR9, －OCONHR9, O-tetrahydropyranyl, NH2, －NR7R8, －NR10COR9, －NR10CO2R9, －NR10CONR7R8, －NHC(〓NH)NH2, －NR10SO2R9, －S(O)yR11, where R11 is selected from the group consisting of H, alkyl of 1-4 carbons, aryl of 6-10 carbons, and heteroaryl, wherein y is an integer selected from the group consisting of 1 and 2; －SR11 , －CO2R9, －CONR7R8, －CHO, COR9, －CH2OR7, －CH〓NNR11R12, －CH〓NOR11, －CH〓NR9, －CH〓NNHC(N〓NH)NH2, －SO2NR12R13 and －PO(OR11)2; and wherein either i) R12 and R13 are each independently selected from the group consisting of H, alkyl of 1-4 carbons, aryl of 6-10 carbons, and heteroaryl; or ii) R12 and R13 are combined together to form a linking group of the general formula －(CH2)2－X1－(CH2)2; d) R3, R4, R5 and R6, are each independently selected from the group consisting of H, aryl, heteroaryl; F, Cl, Br, I, －CN, CF3, －NO2, OH, －OR9, －O(CH2)nNR7R8, －OCOR9, －OCONHR9, NH2, －CH2OH, －NR7R8, －NR10COR9, －NR10CONR7R8, －SR11, －S(O)yR11 wherein y is an integer selected from the group consisting of 1 and 2; －CO2R9, －COR9, －CONR7R8, －CHO, －CH〓NOR11, －CH〓NR9, －CH〓NNR11R12, －(CH2)nSR9, wherein n is an integer selected from the group consisting of 1, 2, 3 and 4 －(CH2)nS(O)yR9, －CH2SR14 where R14 is alkyl of 1-4 carbons; －CH2S(O)yR14, －(CH2)nNR7R8, alkyl of 1-8 carbons; preferably alkyl of 1-4 carbons; alkenyl of 1-8 carbons, preferably alkenyl of 1-4 carbons; alkynyl of 1-8 carbons, preferably alkynyl of 1-4 carbons; wherein either 1) each alkyl of 1-8 carbons, alkenyl of 1-8 carbons, or alkynyl of 1-8 carbons is unsubstituted; or 2) each alkyl of 1-8 carbons, alkenyl of 1-8 carbons, or alkynyl of 1-8 carbons is independently substituted with a moiety selected from the group consisting of 1-3 aryl of 6-10 carbons, heteroaryl, F, Cl, Br, I, －CN, －NO2, OH, －OR9, －O(CH2)nNR7R8, －OCOR9, －OCONHR9, O-tetrahydropyranyl, NH2, －NR7R8, －NR10COR9, －NR10CO2R9, －NR10CONR7R8, －NHC(〓NH)NH2, －NR10SO2R9, －S(O)yR11, wherein R11 is selected from the group consisting of H, alkyl of 1-4 carbons, aryl of 6-10 carbons, and heteroaryl, wherein y is an integer selected from the group consisting of 1 and 2; －SR11 , －CO2R9, －CONR7R8, － CHO, COR9, －CH2OR7, －CH〓NNR11R12, －CH〓NOR11, －CH〓NR9, －CH〓NNHC(N〓NH)NH2, －SO2NR12R13 and －PO(OR11)2; and wherein either i) R12 and R13 are each independently selected from the group consisting of H, alkyl of 1-4 carbons, aryl of 6-10 carbons, and heteroaryl; or ii) R12 and R13 are combined together to form a linking group of the general formula －(CH2)2－X1－(CH2)2; d) X is selected from the group consisting of 1 ) an unsubstituted alkylene of 1-3 carbons; or 2) an alkylene of 1-3 carbons substituted by R2, OR10, －SR10, R14, where R14 is an alkyl of 1-4 carbons; phenyl, naphthyl, arylalkyl of 7-14 carbons; or [Figure] [Figure] －CH2Z－, －ZCH2－, －CH2ZCH2－, where Z is selected from the group consisting of [Figure] e) A1 and A2 are selected from the group consisting of H,H, H, －OR11, H, －SR11, H1－N(R11)2; and a group wherein A1 and A2 together form a moiety selected from the group consisting of: 〓O, 〓S; and 〓NR11; and g) B1 and B2 are selected from the group consisting of H,H, H, －OR11, H, －SR11, H1－N(R11)2; and a group wherein B1 and B2 together form a moiety selected from the group consisting of: 〓O, 〓S; and 〓NR11 with the proviso that at least one of the pairs A1, A2 or B1, B2 is 〓O.
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