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    • 1. 发明授权
    • Pentacyclic compound
    • 五环化合物
    • US06545151B2
    • 2003-04-08
    • US09759378
    • 2001-01-16
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • C07D49308
    • C07D493/08C07D305/14
    • The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31 (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
    • 本发明涉及由式(1)表示的具有抗肿瘤活性的新型紫杉醇衍生物[式(I)中,R 1为苯基,R 2为烷基,烯基,炔基 ,环烷基或烷氧基,R3:氢原子,羟基,卤素原子,烷氧基,-O-R31基,酰氧基或-O-CO-R31基(其中R31 :烷基氨基,烯基,炔基,环烷基,芳基或杂环基),R4和R5:氢原子,烷基,烯基,炔基,芳基或 杂环基,Z 1:氢原子,羟基,卤原子或烷基,Z 2:氢原子,羟基,卤素原子或烷基,Z 3:烷基,烯基, 炔基,环烷基,芳基或杂环基]。
    • 2. 发明授权
    • Pentacyclic Compound
    • 五环化合物
    • US06646123B2
    • 2003-11-11
    • US10126653
    • 2002-04-22
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • C07D49308
    • C07D493/08C07D305/14
    • The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R311 an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
    • 本发明涉及由式(1)表示的具有抗肿瘤活性的新型紫杉醇衍生物[在式(I)中,R 1:苯基,R 2:烷基,烯基 基团,炔基,环烷基或烷氧基,R 3:氢原子,羟基,卤素原子,烷氧基,基团-OR 31,酰氧基或基团, O-CO-R 31(其中R 31:烷基氨基,烯基,炔基,环烷基,芳基或杂环基),R 4和R 5 >:氢原子,烷基,烯基,炔基,芳基或杂环基,Z 1:氢原子,羟基,卤素原子或烷基,Z 2 >:氢原子,羟基,卤素原子或烷基,Z 3:烷基,烯基,炔基,环烷基,芳基或杂环基]。
    • 3. 发明授权
    • Pentacyclic compound
    • 五环化合物
    • US06211363B1
    • 2001-04-03
    • US09513852
    • 2000-02-25
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • C07D49308
    • C07D493/08C07D305/14
    • The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1). [In the formula (I), R1: a phenyl group, R2: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R3: a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group —O—R31, an acyloxy group or a group —O—CO—R31, (in which R31: an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R4 and R5: a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z1: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z2: a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z3: an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
    • 本发明涉及由式(1)表示的具有抗肿瘤活性的新型紫杉醇衍生物[式(I)中,R 1为苯基,R 2为烷基,烯基,炔基 ,环烷基或烷氧基,R3:氢原子,羟基,卤素原子,烷氧基,-O-R31基,酰氧基或-O-CO-R31基(其中 R 31:烷基氨基,烯基,炔基,环烷基,芳基或杂环基),R 4和R 5:氢原子,烷基,烯基,炔基,芳基 或杂环基,Z1:氢原子,羟基,卤素原子或烷基,Z2:氢原子,羟基,卤素原子或烷基,Z3:烷基,烯基 ,炔基,环烷基,芳基或杂环基]。
    • 4. 发明授权
    • Pentacyclic compound
    • 五环化合物
    • US6075140A
    • 2000-06-13
    • US945276
    • 1998-02-05
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • Hirofumi TerasawaTsunehiko SogaTakashi Ishiyama
    • C07D305/14C07D493/08
    • C07D493/08C07D305/14
    • The present invention relates to a novel taxol derivative having an antitumor activity which is represented by formula (1). ##STR1## [In the formula (I), R.sup.1 : a phenyl group, R.sup.2 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group or an alkoxyl group, R.sup.3 : a hydrogen atom, a hydroxyl group, a halogen atom, an alkoxyl group, a group --O--R.sup.31, an acyloxy group or a group --O--CO--R.sup.31, (in which R.sup.31 : an alkylamino group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group), R.sup.4 and R.sup.5 : a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an aryl group or a heterocyclic group, Z.sup.1 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.2 : a hydrogen atom, a hydroxyl group, a halogen atom or an alkyl group, Z.sup.3 : an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, an aryl group or a heterocyclic group].
    • PCT No.PCT / JP96 / 01145 Sec。 371日期:1998年2月5日 102(e)1998年2月5日PCT 1996年4月25日PCT PCT。 出版物WO96 / 33998 日期:1996年10月31日本发明涉及由式(1)表示的具有抗肿瘤活性的新型紫杉醇衍生物。 [式(I)中,R 1为苯基,R 2为烷基,烯基,炔基,环烷基或烷氧基,R 3为氢原子,羟基,卤素原子, 烷氧基,基团-O-R31,酰氧基或基团-O-CO-R31(其中R31:烷基氨基,烯基,炔基,环烷基,芳基或 杂环基),R4和R5:氢原子,烷基,烯基,炔基,芳基或杂环基,Z1:氢原子,羟基,卤素原子或烷基, Z2:氢原子,羟基,卤原子或烷基,Z3:烷基,烯基,炔基,环烷基,芳基或杂环基)。
    • 6. 发明授权
    • Hexa-cyclic compound
    • 六环化合物
    • US06407115B1
    • 2002-06-18
    • US08451993
    • 1995-05-26
    • Hirofumi TerasawaAkio EjimaSatoru OhsukiKouichi Uoto
    • Hirofumi TerasawaAkio EjimaSatoru OhsukiKouichi Uoto
    • C07D49122
    • C07D491/22C07D495/22
    • Accordingly, an object of this invention is to provide a hexa-cyclic compound represented by the following general formula: wherein R1 and R2 individually represent a hydrogen atom, a hydroxyl group, a C1-6 alkyl group (“C1-6 alkyl group means an alkyl group having 1 to 6 carbon atoms. Hereinafter defined in the same manner.) The present inventors have conducted extensive studies for the purpose of obtaining camptothecin derivatives with more excellent activity and higher safety, as well as excellent characteristics required for a drug to be administered, and found that hexa-cyclic compounds obtained by the addition of a water-soluble ring to camptothecin had characteristics superior to camptothecin. This finding has led to the completion of this invention.
    • 因此,本发明的目的是提供由以下通式表示的六环化合物:其中R 1和R 2各自表示氢原子,羟基,C 1-6烷基(“C 1-6烷基” 具有1〜6个碳原子的烷基,以下相同的方式定义。)本发明人为了得到活性更高,安全性更好的喜树碱衍生物进行了广泛的研究, 并且发现通过向喜树碱中加入水溶性环获得的六环化合物具有优于喜树碱的特征,这一发现导致本发明的完成。