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1. 发明申请

WO1991016324A1 NOVEL CC-1065 ANALOGS 审中-公开
公开(公告)号：WO1991016324A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002704
申请日：1991-04-24
申请人： THE UPJOHN COMPANY , ARISTOFF, Paul, Adrian , KELLY, Robert, Charles , MITCHELL, Mark, Allen
发明人： THE UPJOHN COMPANY
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K38/00 , A61K47/555 , A61K47/64 , A61K47/6809 , C07D487/10 , C07F9/6561 , C07K5/06026 , C07K5/06034 , C07K5/06043 , C07K5/06052 , C07K5/0802 , C07K17/06
摘要： This invention provides some new synthetically obtained compounds of formula (I and II), which are useful as chemical intermediates. Representative formula (I or II) compounds have also been shown to possess useful ranges of antitumor activity in standard laboratory animal tests. In addition, the compounds of formula (I or II) can be linked to monoclonal antibodies, either directly or via known linking group, as a means of selectively delivering the CC-1065 analogs (Compounds of Formula I and II) to those target cells expressing the target antigen and thus selectively eliminating those diseased cells from the animal or human. Further, the compounds of formula (I and II) can be linked to soluble human CD4 or a soluble human CD4 protein fragment capable of binding to the gp120 envelope protein of the human immuno-virus and thus eliminate virally infected cells.
摘要翻译：本发明提供一些合成获得的式（I和II）化合物，其可用作化学中间体。代表性的式（I或II）化合物也已被证明在标准实验动物试验中具有有效的抗肿瘤活性范围。此外，式（I或II）化合物可以直接或通过已知的连接基团与单克隆抗体连接，作为选择性递送CC-1065类似物（式I和II的化合物）到这些靶细胞的手段表达靶抗原，从而选择性地从动物或人中除去那些患病细胞。此外，式（I和II）化合物可以与可溶性人CD4或能够结合人免疫病毒的gp120包膜蛋白的可溶性人CD4蛋白片段连接，从而消除病毒感染的细胞。

2. 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。

3. 发明申请

WO1991019731A1 STEROIDS WHICH INHIBIT ANGIOGENESIS 审中-公开
标题翻译：抑制血管生成的STEROIDS
公开(公告)号：WO1991019731A1
公开(公告)日：1991-12-26
申请号：PCT/US1991003459
申请日：1991-05-23
申请人： THE UPJOHN COMPANY , WILKS, John, William , DEKONING, Thomas, Frank , ARISTOFF, Paul, Adrian
发明人： THE UPJOHN COMPANY
IPC分类号： C07J31/00
CPC分类号： C07J71/0015 , C07J3/005 , C07J5/0046 , C07J5/0053 , C07J5/0076 , C07J7/0085 , C07J9/00 , C07J31/006 , C07J51/00
摘要： Novel angiostatic DELTA -steroids (I), C21-oxygenated steroids (II) and other known steroidal compounds have been found to be useful in treating angiogenesis in mammals who have a need for the same. These steroids are useful in treating diseases of neovascularization such as cancer, diabetes and arthritis.
摘要翻译：已经发现新型血管狭窄DELTA <4,9（11）> - 类固醇（I），C21-氧化类固醇（II）和其它已知的甾体化合物可用于治疗需要相同的哺乳动物的血管生成。这些类固醇可用于治疗新生血管形成疾病如癌症，糖尿病和关节炎。

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。

5. 发明申请

WO1995030670A2 PYRANONE COMPOUNDS USEFUL TO TREAT RETROVIRAL INFECTIONS 审中-公开
标题翻译：吡咯烷酮化合物可用于治疗复发性感染
公开(公告)号：WO1995030670A2
公开(公告)日：1995-11-16
申请号：PCT/US1995005219
申请日：1995-05-04
申请人： THE UPJOHN COMPANY , ROMINES, Karen, Rene , BUNDY, Gordon, L. , SCHWARTZ, Theresa, M. , TOMMASI, Ruben, A. , STROHBACH, Joseph, Walter , TURNER, Steven, Ronald , THAISRIVONGS, Suvit , ARISTOFF, Paul, Adrian , JOHNSON, Paul, D. , SKULNICK, Harvey, Irving , SKALETZKI, Louis, L. , ANDERSON, David, John , MORRIS, Joel , GAMMILL, Ronald, B. , LUKE, George, P.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D309/32
CPC分类号： C07D405/12 , C07D309/32 , C07D309/38 , C07D311/02 , C07D311/74 , C07D405/14
摘要： The present invention relates to compounds of formulae (I) and (II) which are pyran-2-ones, 5,6-dihydro-pyran-2-ones, 4-hydroxy-benzopyran-2-ones, 4-hydroxy-cycloalkyl[b]pyran-2-ones, and derivatives thereof, useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus, wherein R10 and R20 taken together are formulae (III) and (IV).
摘要翻译：本发明涉及式（I）和（II）的化合物，其为吡喃-2-酮，5,6-二氢 - 吡喃-2-酮，4-羟基 - 苯并吡喃-2-酮，4-羟基 - 环烷基 [b]吡喃-2-酮及其衍生物，其用于抑制感染所述逆转录病毒的哺乳动物细胞中的逆转录病毒，其中R10和R20一起是式（III）和（IV）。

6. 发明申请

WO1994018188A1 4-HYDROXY-BENZOPYRAN-2-ONES AND 4-HYDROXY-CYCLOALKYL[B]PYRAN-2-ONES USEFUL TO TREAT RETROVIRAL INFECTIONS 审中-公开
标题翻译： 4-羟基苯并噻吩-2-酮和4-羟基环己基[B]吡喃-2-酮有助于治疗复发性感染
公开(公告)号：WO1994018188A1
公开(公告)日：1994-08-18
申请号：PCT/US1994000938
申请日：1994-02-03
申请人： THE UPJOHN COMPANY , ANDERSON, David, John , BANITT, Lee, S. , TOMICH, Paul, Kosta , BOHANON, Michael, John , TURNER, Steven, Ronald , STROHBACH, Joseph, Walter , THAISRIVONGS, Suvit , YANG, Chih-Ping , THOMAS, Richard, Charles , ROMINES, Karen, Rene , ARISTOFF, Paul, Adrian , SKULNICK, Harvey, Irving , JOHNSON, Paul, D. , GAMMILL, Ronald, B. , ZHANG, Qingwei , BUNDY, Gordon, L.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D311/46
CPC分类号： C07D405/04 , C07D311/56 , C07D311/74 , C07D311/94 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/12 , Y02P20/582
摘要： The present invention relates to compounds of formula (I) which are 4-hydroxy-benzopyran-2-ones and 4-hydroxy-cycloalkyl[b]pyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus. In formula (I) R10 and R20 taken together are formula (II) or formula (III).
摘要翻译：本发明涉及用于抑制感染该逆转录病毒的哺乳动物细胞中的逆转录病毒的4-羟基 - 苯并吡喃-2-酮和4-羟基 - 环烷基[b]吡喃-2-酮的式（I）化合物。在式（I）中，R 10和R 20一起是式（II）或式（III）。

7. 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。

8. 发明申请

WO1996018628A1 ALKYL SUBSTITUTED PIPERADINYL AND PIPERAZINYL ANTI-AIDS COMPOUNDS 审中-公开
标题翻译：烷基取代的哌嗪和哌嗪类抗艾滋病化合物
公开(公告)号：WO1996018628A1
公开(公告)日：1996-06-20
申请号：PCT/US1995014558
申请日：1995-11-28
申请人： THE UPJOHN COMPANY , ROMERO, Donna, L. , THOMAS, Richard, C. , MAY, Paul, D. , POEL, Toni-Jo
发明人： THE UPJOHN COMPANY
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14
摘要： Anti-AIDS compounds of formula (I), where the aromatic/heteroaromatic ring is bonded to a carbon atom of the R8 substituent are disclosed as well as specific Anti-AIDS pyridines (V).
摘要翻译：公开了芳族/杂芳环与R 8取代基的碳原子键合的式（I）的抗艾滋病化合物以及具体的抗艾滋病吡啶（V）。

9. 发明申请

WO1996018395A1 USE OF PRAMIPEXOLE AS A NEUROPROTECTIVE AGENT 审中-公开
标题翻译：使用作为神经保护剂的PRAMIPEXOLE
公开(公告)号：WO1996018395A1
公开(公告)日：1996-06-20
申请号：PCT/US1995015613
申请日：1995-12-12
申请人： THE UPJOHN COMPANY , BOEHRINGER INGELHEIM KG , HALL, Edward, Dallas , VON VOIGTLANDER, Philip, F. , ROHDE, Frank, A.
发明人： THE UPJOHN COMPANY , BOEHRINGER INGELHEIM KG
IPC分类号： A61K31/425
CPC分类号： A61K31/428 , Y10S514/879
摘要： The present invention provides the use of pramipexole as a neuroprotective agent.
摘要翻译：本发明提供了普拉克索作为神经保护剂的用途。

10. 发明申请

WO1996015258A1 A SCINTILLATION PROXIMITY ASSAY FOR N-ACETYLGALACTOSAMINYLTRANSFERASE ACTIVITY 审中-公开
标题翻译： N-乙酰胆碱酯酶基因活性的SCINTILLATION近似性测定
公开(公告)号：WO1996015258A1
公开(公告)日：1996-05-23
申请号：PCT/US1995013483
申请日：1995-11-08
申请人： THE UPJOHN COMPANY , ELHAMMER, Ake, P.
发明人： THE UPJOHN COMPANY
IPC分类号： C12Q01/48
CPC分类号： C07K7/06 , C12Q1/48
摘要： This invention comprises a scintillation proximity assay designed to assay for the presence of N-acetylgalactosaminyltransferase, also known as GalNAc-transferase. The assay is most conveniently carried out on 96-well microtiterplates. The assay is especially suitable for large volume screens for compounds affecting GalNAc-transferase activity.
摘要翻译：本发明包括设计用于测定N-乙酰半乳糖胺基转移酶（也称为GalNAc-转移酶）的存在的闪烁亲近测定。该测定最方便地在96孔微量滴定板上进行。该测定特别适用于影响GalNAc转移酶活性的化合物的大体积筛选。

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