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    • 1. 发明授权
    • Baccatin derivatives and processes for preparing the same
    • 浆果赤霉素衍生物及其制备方法
    • US5589502A
    • 1996-12-31
    • US558772
    • 1995-11-15
    • Kenji TsujiharaTomiki HashiyamaMotoaki OhashiNoriyuki Nakanishi
    • Kenji TsujiharaTomiki HashiyamaMotoaki OhashiNoriyuki Nakanishi
    • C07D263/04C07D263/06C07D305/14C07D405/12C07D407/12C07D409/12C07D413/12A61K31/335
    • C07D263/04C07D263/06C07D305/14C07D405/12C07D407/12C07D409/12C07D413/12
    • A compound represented by the formula [I]: ##STR1## wherein R.sup.3 represents a lower alkanoyl group; R.sup.4 represents a substituted or unsubstituted benzoyl group; ring A represents a substituted or unsubstituted cyclopropane ring; X represents a single bond or a group represented by --O--, --S-- or --NH--; R represents a substituted or unsubstituted lower alkyl group (wherein said lower alkyl group may have a cycloalkyl moiety), a substituted or unsubstituted aryl group or a substituted or unsubstituted aromatic heterocyclic group; E represents hydrogen atom or a group represented by --CO(CH.sub.2).sub.n ZY; Y represents a residue obtained from an amino acid or a dipeptide by removing hydroxyl group in one carboxyl group therefrom (wherein amino group existing in said residue may be protected, and carboxyl group existing in said residue may be esterified or amidated); Z represents a group represented by the formula of --O-- or --NH--; and n represents 1, 2, 3, 4, 5 or 6, or a pharmaceutically acceptable salt thereof. Said compounds have excellent antitumor activity so that they are useful in the prophylaxis or treatment of a wide range of tumors such as breast cancer, ovary cancer, lung cancer, malignant melanoma and the like.
    • 由式[I]表示的化合物:其中R 3表示低级烷酰基; R4表示取代或未取代的苯甲酰基; 环A表示取代或未取代的环丙烷环; X表示单键或由-O - , - S-或-NH-表示的基团; R表示取代或未取代的低级烷基(其中所述低级烷基可以具有环烷基部分),取代或未取代的芳基或取代或未取代的芳族杂环基; E表示氢原子或由-CO(CH 2)n ZY表示的基团; Y表示通过从其中除去一个羧基中的羟基从氨基酸或二肽获得的残基(其中存在于所述残基中的氨基可被保护,并且所述残基中存在的羧基可被酯化或酰胺化); Z表示由式-O-或-NH-表示的基团; 和n表示1,2,3,4,5或6或其药学上可接受的盐。 所述化合物具有优异的抗肿瘤活性,因此它们可用于预防或治疗广泛范围的肿瘤如乳腺癌,卵巢癌,肺癌,恶性黑素瘤等。
    • 3. 发明授权
    • Baccatin derivatives and processes for preparing the same
    • 浆果赤霉素衍生物及其制备方法
    • US5608073A
    • 1997-03-04
    • US673580
    • 1996-07-01
    • Kenji TsujiharaTomiki HashiyamaMotoaki OhashiNoriyuki Nakanishi
    • Kenji TsujiharaTomiki HashiyamaMotoaki OhashiNoriyuki Nakanishi
    • C07D263/04C07D263/06C07D305/14C07D405/12C07D407/12C07D409/12C07D413/12
    • C07D263/04C07D263/06C07D305/14C07D405/12C07D407/12C07D409/12C07D413/12
    • A compound represented by the formula [I]: ##STR1## wherein R.sup.3 represents a lower alkanoyl group; R.sup.4 represents a substituted or unsubstituted benzoyl group; ring A represents a substituted or unsubstituted cyclopropane ring; X represents a single bond or a group represented by --O--,--S-- or --NH--, R represents a substituted or unsubstituted lower alkyl group (wherein said lower alkyl group may have a cycloalkyl moiety), a substituted or unsubstituted aryl group or a substituted or unsubstituted aromatic heterocyclic group; E represents hydrogen atom or a group represented by --CO(CH.sub.2).sub.n ZY; Y represents a residue obtained from an amino acid or a dipeptide by removing hydroxyl group in one carboxyl group therefrom (wherein amino group existing in said residue may be protected, and carboxyl group existing in said residue may be esterified or amidated); Z represents a group represented by the formula of --O-- or --NH--; and n represents 1, 2, 3, 4, 5 or 6, or a pharmaceutically acceptable salt thereof. Said compounds have excellent antitumor activity so that they are useful in the prophylaxis or treatment of a wide range of tumors such as breast cancer, ovary cancer, lung cancer, malignant melanoma and the like.
    • 由式[I]表示的化合物:其中R 3表示低级烷酰基; R4表示取代或未取代的苯甲酰基; 环A表示取代或未取代的环丙烷环; X表示单键或由-O - , - S-或-NH-表示的基团,R表示取代或未取代的低级烷基(其中所述低级烷基可具有环烷基部分),取代或未取代的芳基 或取代或未取代的芳族杂环基; E表示氢原子或由-CO(CH 2)n ZY表示的基团; Y表示通过从其中除去一个羧基中的羟基从氨基酸或二肽获得的残基(其中存在于所述残基中的氨基可被保护,并且所述残基中存在的羧基可被酯化或酰胺化); Z表示由式-O-或-NH-表示的基团; 和n表示1,2,3,4,5或6或其药学上可接受的盐。 所述化合物具有优异的抗肿瘤活性,因此它们可用于预防或治疗广泛范围的肿瘤如乳腺癌,卵巢癌,肺癌,恶性黑素瘤等。
    • 4. 发明授权
    • Reagent preparation apparatus, reagent preparation system, and reagent preparation method
    • 试剂制备装置,试剂制备系统和试剂制备方法
    • US08862272B2
    • 2014-10-14
    • US13197371
    • 2011-08-03
    • Yutaka IkedaNoriyuki Nakanishi
    • Yutaka IkedaNoriyuki Nakanishi
    • G05B21/00G01N1/38G01N35/10
    • G01N1/38G01N35/1002
    • A reagent preparation apparatus for supplying a reagent, prepared by mixing a high concentration reagent and purified water supplied from a purified water production device, to a sample measurement device for measuring a sample using the prepared reagent, the reagent preparation apparatus comprising: a reagent preparation unit for preparing the reagent by mixing the high concentration reagent and the purified water supplied from the purified water production device; and a controller, communicably connected to the purified water production device, for controlling the purified water production device to continue producing the purified water until a predetermined time has elapsed from when the purified water production device starts the production of the purified water.Also, a reagent preparation system and a reagent preparation method.
    • 一种试剂调制装置,用于将通过将高浓度试剂和从净化水生成装置供给的净化水混合而制备的试剂供给到使用所制备的试剂测量样品的样品测量装置,所述试剂制备装置包括:试剂制备 通过混合高浓度试剂和从纯化水生产装置供给的净化水来制备试剂的单元; 以及与净化水生产装置可通信地连接的控制器,用于控制净化水生产装置继续生产净化水,直到净化水生产装置开始净化水的生产经过预定时间。 另外,也可以使用试剂调制系统和试剂调制方法。