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1. 发明申请

WO1992016508A1 REISSERT COMPOUNDS AS ANTI-HIV AGENTS 审中-公开
标题翻译： REISSERT化合物作为抗HIV药物
公开(公告)号：WO1992016508A1
公开(公告)日：1992-10-01
申请号：PCT/US1992001746
申请日：1992-03-12
申请人： THE UPJOHN COMPANY , ARISTOFF, Paul, Adrian , BANNISTER, Brian , BILES, Carolyn , MARTIN, David, Glenn , ROMERO, Donna, Lee , SKULNICK, Harvey, Irving , SMITH, Herman, Walden , ALTHAUS, Irene, Wilson , REUSSER, Fritz
发明人： THE UPJOHN COMPANY
IPC分类号： C07D215/48
CPC分类号： C07D405/06 , C07D215/48 , C07D241/44
摘要： Disclosed are heterocyclic compounds of formula (I). The compounds of the invention are useful in the treatment of AIDS and AIDS related complex. The compounds of the invention are generally synthesized by following the reactions and conditions used to make Reissert compounds. Compounds included within the scope of formula (I) are 1,2-dihydroquinolines, 1,4-dihydroquinolines, 1,2,3,4-tetrahydroquinolines, 1,2-dihydroquinazolines, and the 1,2-dihydroquinoxalines. Representative compounds include 1-(4-bromobenzoyl)-2-cyano-1,2-dihydroquinoline, 1-(4-chlorobenzoyl)-2-cyano-5-fluoro-1,2-dihydroquinoline, 1-(4-chlorobenzoyl)-2-cyano-6-fluoro-1,4-dihydroquinoline, 1-(4-chlorobenzoyl)-2-cyano-1,2,3,4-tetrahydroquinoline, 1-(4-chlorobenzoyl)-2-carboximidamide-8-fluoro-1,2-dihydroquinoline, 1-(4-chlorobenzoyl)-2-cyano-1,4-dihydroquinoxaline, 1-E-(3-(4-chlorophenyl)-1-oxo-2-propenyl)-2-cyano-1,2-dihydroquinoline, and 1-E-(3-(4-chlorophenyl)-1-oxo-2-propenyl)-2-carboximidamide-1,2-dihydr oquinoline. Also included within the scope of the invention is a method of treating a human having AIDS or ARC with an effective amount of a compound of the invention.
摘要翻译：公开了式（I）的杂环化合物。本发明的化合物可用于治疗AIDS和AIDS相关复合物。本发明的化合物通常通过遵循用于制备Reissert化合物的反应和条件来合成。包括在式（I）范围内的化合物是1,2-二氢喹啉，1,4-二氢喹啉，1,2,3,4-四氢喹啉，1,2-二氢喹唑啉和1,2-二氢喹喔啉。代表性的化合物包括1-（4-溴苯甲酰基）-2-氰基-1,2-二氢喹啉，1-（4-氯苯甲酰基）-2-氰基-5-氟-1,2-二氢喹啉，1-（4-氯苯甲酰基） -2-氰基-6-氟-1,4-二氢喹啉，1-（4-氯苯甲酰基）-2-氰基-1,2,3,4-四氢喹啉，1-（4-氯苯甲酰基）-2-亚甲代酰胺-8 （4-氯苯甲酰基）-2-氰基-1,4-二氢喹喔啉，1-E-（3-（4-氯苯基）-1-氧代-2-丙烯基）-2 - 氰基-1,2-二氢喹啉和1-E-（3-（4-氯苯基）-1-氧代-2-丙烯基）-2-亚甲代酰胺-1,2-二氢喹啉。还包括在本发明的范围内的是用有效量的本发明化合物治疗患有AIDS或ARC的人的方法。

2. 发明申请

WO1993001181A1 SUBSTITUTED INDOLES AS ANTI-AIDS PHARMACEUTICALS 审中-公开
标题翻译：取而代之的是抗艾滋病药物
公开(公告)号：WO1993001181A1
公开(公告)日：1993-01-21
申请号：PCT/US1992005067
申请日：1992-06-23
申请人： THE UPJOHN COMPANY , ROMERO, Donna, Lee , THOMAS, Richard, Charles
发明人： THE UPJOHN COMPANY
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14
摘要： Substituted indoles of formula (I) are useful anti-AIDS pharmaceuticals.
摘要翻译：式（I）的取代的吲哚是有用的抗艾滋病药物。

3. 发明申请

WO1991009849A1 DIAROMATIC SUBSTITUTED ANTI-AIDS COMPOUNDS 审中-公开
标题翻译： DIALOMATIC替代抗艾滋病化合物
公开(公告)号：WO1991009849A1
公开(公告)日：1991-07-11
申请号：PCT/US1990007390
申请日：1990-12-24
申请人： THE UPJOHN COMPANY , ROMERO, Donna, Lee , MITCHELL, Mark, Allen , THOMAS, Richard, Charles , PALMER, John, Raymond , TARPLEY, William, Gary , ARISTOFF, Paul, Adrian , SMITH, Herman, W.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D213/74
CPC分类号： C07D213/74 , C07D209/42 , C07D295/192 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D471/04 , C07D491/04
摘要： The present invention includes diaromatic substituted heterocyclic compounds (III) which are useful in treating individuals infected with the HIV virus. The invention includes certain previously generically disclosed anti-AIDS piperazinyl compounds (IV) and a method of treating HIV infected individuals with the indoles of formula (V) and the anti-AIDS amines (X).
摘要翻译：本发明包括可用于治疗感染HIV病毒的个体的二芳基取代的杂环化合物（III）。本发明包括一些先前通用的抗艾滋病哌嗪基化合物（IV）和用式（V）的吲哚和抗艾滋病胺（X）治疗HIV感染个体的方法。

4. 发明申请

WO1994011361A1 PYRAN-2-ONES AND 5,6-DIHYDROPYRAN-2-ONES USEFUL FOR TREATING HIV AND OTHER RETROVIRUSES 审中-公开
标题翻译： PYRAN-2-ONES和5,6-DIHYDROPYRAN-2-ONES用于治疗艾滋病毒和其他肝炎病毒
公开(公告)号：WO1994011361A1
公开(公告)日：1994-05-26
申请号：PCT/US1993010645
申请日：1993-11-09
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit , YANG, Chih-Ping , STROHBACH, Joseph, Walter , TURNER, Steven, Ronald , ROMERO, Donna, Lee , SKALETZKI, Louis, L, , ARISTOFF, Paul, Adrian , GAMMILL, Ronald, B, , JOHNSON, Paul, D. , SKULNICK, Harvey, Irving , PIPER, Richard, C, , TOMMASI, Ruben, A. , ZHANG, Qingwei
发明人： THE UPJOHN COMPANY
IPC分类号： C07D309/38
CPC分类号： C07D405/06 , C07D309/32 , C07D309/38 , C07D311/96 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The present invention relates to compounds of formula (I) which are pyran-2-ones and 5,6-dihydropyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.
摘要翻译：本发明涉及可用于在感染该逆转录病毒的哺乳动物细胞中抑制逆转录病毒的吡喃-2-酮和5,6-二氢吡喃-2-酮的式（I）化合物。

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