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1.发明公开7-HALO- AND 7$g(b),8$g(b)-METHANO-TAXOLS, ANTINEOPLASTIC USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 失效7-卤代-AND 7（BETA），8（BETA） - 亚甲基 - 紫杉醇，抗肿瘤用途和药物组合物含有它们。
公开(公告)号：EP0674630A1
公开(公告)日：1995-10-04
申请号：EP94903483.0
申请日：1993-12-13
申请人： THE UPJOHN COMPANY
发明人： HESTER, Jackson, B., Jr. , JOHNSON, Roy, A. , KELLY, Robert, C. , MIDY, Eldon, G. , SKULNICK, Harvey, I.
CPC分类号： C07D405/12 , C07D263/06 , C07D305/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07F7/1856
摘要： This invention provides 7-deoxy-taxol analogs of formula (I). The compounds of formula (I) (including formulae II and III) are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.
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公开(公告)号：EP0210228A1
公开(公告)日：1987-02-04
申请号：EP86900937.0
申请日：1986-01-23
申请人： THE UPJOHN COMPANY
CPC分类号： C07D239/42 , C07D239/47 , C07D403/04 , C07D403/12
摘要： L'invention décrit la synthèse et l'utilisation antinéoplastique de composés 4-aziridyl-5-substitué/non substitué 6-aryl-pyrimidine de formule (IA) ainsi que des N'- AD2-(1-aziridyl)éthyl BD-6-aryl-2,4-pyrimidinediamines de formule (IB) et des 4-chloro ou bromo-5-substitué/non substitué-6-aryl-pyrimidines.
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3.发明公开
公开(公告)号：EP0720607A1
公开(公告)日：1996-07-10
申请号：EP94926571.0
申请日：1994-09-07
申请人： THE UPJOHN COMPANY
发明人： CHRUSCIEL, Robert, A. , MAGGIORA, Linda, L. , THAISRIVONGS, Suvit , TUSTIN, James, M. , SMITH, Clark, W. , TOMMASI, Rubin, A. , ARISTOFF, Paul, A. , SKULNICK, Harvey, I. , HOWE, W., Jeffrey , BUNDY, Gordon, L.
CPC分类号： C07D405/06 , C07D307/60 , C07D307/94 , C07D405/12 , C07D417/12 , C07D473/00 , C07D491/10
摘要： The invention comprises novel substituted tetronic acid type compounds, 2,4-(3H,5H)-furandiones, that are useful for the inhibition of the HIV protease enzyme. The compounds may be useful for the treatment of a person with AIDS or AIDS related diseases. The compounds may be used in the attempt to retard the further replication of any retrovirus containing the aspartyl protease enzyme. Compounds are represented by formula (1), wherein 3 tautomers of the same structure are shown, R1, R2 and R3 are replaced with various substituents.
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公开(公告)号：EP0245357B1
公开(公告)日：1991-08-07
申请号：EP86906631.6
申请日：1986-10-16
申请人： THE UPJOHN COMPANY
IPC分类号： C07J5/00 , C07J13/00 , C07J31/00 , C07J33/00 , C07J41/00 , C07J43/00 , C07J51/00 , C07J71/00 , A61K31/57 , A61K31/58
CPC分类号： C07J5/0076 , C07J7/0055 , C07J51/00
摘要： Novel tetrahydro steroids which are useful in inhibiting angiogenesis and have the following structure: A compound of formula (I), wherein R15 is = O or -OH; wherein R23 with R10 forms a cyclic phosphate of formula (II) or wherein R23 is -OH, O-C(=O)-R11, -O-P(O)(OH)2, or -O-C(=O)-(CH2)tCOOH.
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5.发明公开$g(D)?6,7 -TAXOLS ANTINEOPLASTIC USE AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 失效DELTA 6，7-TAXOLEN，ANTINEOPLASTISCHE VERWENDUNG UND DIEE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSTELLUNGEN
公开(公告)号：EP0703909A1
公开(公告)日：1996-04-03
申请号：EP94920688.0
申请日：1994-06-03
申请人： THE UPJOHN COMPANY
CPC分类号： C07D263/04 , C07D263/06 , C07D305/14 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07F7/1856
摘要： This invention provides 7-deoxy-Δ6,7-taxol and 7-deoxy-Δ6,7-taxol analogs of formula (I). The compounds of formula (I) are useful for the same cancers for which taxol has been shown active, including human ovarian cancer, breast cancer, and malignant melanoma as well as lung cancer, gastric cancer, colon cancer, head and neck cancer, and leukemia.
摘要翻译： 本发明提供了式（I）的7-脱氧-ΔTA-δ-δ-羟考啉醇和7-脱氧-DΔTA-6,7-类似物。 式（I）化合物可用于已经显示紫杉醇具有活性的相同癌症，包括人卵巢癌，乳腺癌和恶性黑素瘤以及肺癌，胃癌，结肠癌，头颈癌和 白血病。
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公开(公告)号：EP0655066A1
公开(公告)日：1995-05-31
申请号：EP93918422.0
申请日：1993-07-30
申请人： THE UPJOHN COMPANY
CPC分类号： C07D498/22 , C07H9/06 , C07H19/23
摘要： This invention describes both known and novel compounds, some of which are protein kinase inhibitors, that may be combined with taxol type compounds. The combination of disclosed compounds plus taxol type compounds exhibits powerful synergistic effects and the combinations are useful in the treatment of cancer. The novel compounds and their synthesis are described. A compound of formula (I), above, is described wherein R1-R8 represent various substituents.
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公开(公告)号：EP0245357A1
公开(公告)日：1987-11-19
申请号：EP86906631.0
申请日：1986-10-16
申请人： THE UPJOHN COMPANY
IPC分类号： A61K31 , A61P7 , A61P9 , A61P13 , A61P15 , A61P35 , C07J1 , C07J5 , C07J7 , C07J13 , C07J17 , C07J31 , C07J33 , C07J41 , C07J43 , C07J51 , C07J71
CPC分类号： C07J5/0076 , C07J7/0055 , C07J51/00
摘要： Nouveaux stéroides tétrahydro utiles pour inhiber l'angiogenèse et ayant la structure de composé de formule (I) dans laquelle R15 représente =O ou -OH, et dans laquelle R23 forme avec R10 un phosphate cyclique de formule (II), ou dans laquelle R23 représente -OH, OC(=O)-R11, -OP(O)(OH)2, ou -OC(=O)-(CH2)tCOOH.
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