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31 条记录 (耗时 0.031 秒)

    Novel nitrosourea compounds and process for preparing the same
    21.
    发明授权
    Novel nitrosourea compounds and process for preparing the same 失效
    新型亚硝基脲类化合物及其制备方法

    公开(公告)号：US4241052A

    公开(公告)日：1980-12-23

    申请号：US38638

    申请日：1979-05-14

    申请人： Kenji Tsujihara ,  Masakatsu Ozeki ,  Yoshihisa Arai

    发明人： Kenji Tsujihara ,  Masakatsu Ozeki ,  Yoshihisa Arai

    IPC分类号： C07H13/12 ,  C07H17/00 ,  A61K31/70 ,  A61K31/73

    CPC分类号： C07H13/12 ,  C07H17/00

    摘要： A nitrosourea compound of the formula: ##STR1## wherein R.sup.1 is an alicyclic group having 3 to 6 carbon atoms, phenyl, phenyl substituted with one to substituents selected from halogen, lower alkyl, lower alkoxy, hydroxy and nitro, or a heteromonocyclic group selected from oxiranyl, tetrahydrofuryl, 1,3-dioxolanyl, 1,4-dioxanyl, morpholino, tetrahydro-S,S-dioxo-thienyl, furyl, thienyl and pyridyl; R.sup.2 is aldopentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl or O-aldo-hexopyranosyl-(1.fwdarw.4)-aldo-hexopyranosyl; and A is a single bond or straight or branched alkylene having one to 3 carbon atoms, is prepared by nitrosation of a compound of the formula: ##STR2## wherein R.sup.1, R.sup.2 and A are the same as above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent however, effectiveness in human beings has not yet been demonstrated.

    摘要翻译： 具有下式的亚硝基脲化合物：其中R 1是具有3至6个碳原子的脂环基，苯基，被一个选自卤素，低级烷基，低级烷氧基，羟基和硝基的取代基取代的苯基或被选择的杂单环基团 由环氧乙烷基，四氢呋喃基，1,3-二氧戊环基，1,4-二恶烷基，吗啉代，四氢S，S-二氧代噻吩基，呋喃基，噻吩基和吡啶基; R2是醛二糖呋喃糖基，醛 - 吡喃葡萄糖基，醛 - 六吡喃糖基或O-羟基 - 六吡喃糖基 - （1-> 4） - 六氢吡喃糖基; 并且A是单键或具有1至3个碳原子的直链或支链亚烷基，是通过亚化下式化合物制备的：其中R1，R2和A与上述相同。 所述的亚硝基脲化合物可用作抗肿瘤或抗白血病药物，但人类尚未证明其有效性。

    S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
    23.
    发明授权
    S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof 失效
    S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物及其制备方法

    公开(公告)号：US06716983B2

    公开(公告)日：2004-04-06

    申请号：US10337476

    申请日：2003-01-08

    申请人： Takayuki Kawaguchi ,  Sumihiro Nomura ,  Kenji Tsujihara

    发明人： Takayuki Kawaguchi ,  Sumihiro Nomura ,  Kenji Tsujihara

    IPC分类号： C07D49120

    CPC分类号： C07D491/14 ,  C07B2200/07 ,  C07D209/42 ,  C07D217/26

    摘要： A process for preparing S type 2-substituted hydroxy-2-indolidinylbutyric ester compound [II]: wherein Ro is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R” (in which the nitrogen atom is protected), R1 and R2 are lower alkyl groups, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.

    摘要翻译： 制备S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物[II]的方法：其中R 0是具有绝对构型“R”（其中氮原子被保护的）的含氮稠合杂环羧酸的残基 ），R1和R2是低级烷基，E是酯残基，其可用作制备具有抗肿瘤活性的喜树碱衍生物的中间体，其包括2-乙基化2-取代的羟基-2-吲哚哩啶基乙酸酯化合物[I]：其中 符号如上所述。

    Camptothecin derivatives
    26.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US5892043A

    公开(公告)日：1999-04-06

    申请号：US773182

    申请日：1996-12-27

    申请人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    发明人： Kenji Tsujihara ,  Takayuki Kawaguchi ,  Satoshi Okuno ,  Toshiro Yano

    IPC分类号： A61K47/48 ,  C08B37/00 ,  C08B37/02 ,  C07D471/00

    CPC分类号： C08B37/0018 ,  A61K47/4823 ,  A61K47/48338 ,  C08B37/0021

    摘要： A camptothecin derivative comprising a compound of the formula �I!: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are (A) adjacent two groups combine to form alkylene, or both are H, and one of the remaining three groups is --X.sub.n --Alk.sub.m --R.sup.6, and the other two are H, alkyl or halogen, or (B) adjacent two groups combine to form alkylene, and one of the carbon atoms of said alkylene group is substituted by --X.sub.n --Alk.sub.m --R.sup.6, and the remaining three groups are H, alkyl or a halogen, and one or two --CH.sub.2 -- of the alkylene in (A) or (B) may optionally be replaced by --O--, --S-- or --NH--, X is --O-- or --NH--, Alk is alkylene, R.sup.6 is --NH.sub.2, ##STR2## or --OH, m and n are both 0 or 1, or m is 1 and n is 0, which camptothecin compound is bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects and are useful as a medicament.

    摘要翻译： 包含式[I]化合物的喜树碱衍生物：其中R 1，R 2，R 3，R 4和R 5是（A）相邻的两个基团结合形成亚烷基，或两者都是H，并且其中之一 其余三个为-Xn-Alkm-R6，另外两个为H，烷基或卤素，或（B）相邻的两个基团结合形成亚烷基，所述亚烷基的一个碳原子被-Xn- Al-C-R6，其余三个基团是H，烷基或卤素，并且（A）或（B）中亚烷基的一个或两个-CH 2可以任选地被-O - ， - S-或-NH - ，X为-O-或-NH-，Alk为亚烷基，R6为-NH2，或IMA为-OH，m和n均为0或1，或m为1，n为0，喜树碱化合物为 通过氨基酸或肽或其药学上可接受的盐与具有羧基的多糖结合。 所述喜树碱衍生物显示出增强的抗肿瘤活性，但副作用很少，可用作药物。

    Novel nitrosourea compounds and process for preparing the same
    27.
    发明授权
    Novel nitrosourea compounds and process for preparing the same 失效
    新型亚硝基脲类化合物及其制备方法

    公开(公告)号：US4182757A

    公开(公告)日：1980-01-08

    申请号：US922811

    申请日：1978-07-10

    申请人： Kenji Tsujihara ,  Masakatsu Ozeki ,  Yoshihisa Arai

    发明人： Kenji Tsujihara ,  Masakatsu Ozeki ,  Yoshihisa Arai

    IPC分类号： A61K31/17 ,  A61P35/00 ,  C07C275/68 ,  C07H13/12 ,  A61K31/70 ,  C07H15/02

    CPC分类号： C07H13/12 ,  C07C275/68

    摘要： A nitrosourea compound of the formula: ##STR1## wherein R.sup.1 is alkyl of one to six carbon atoms, hydroxyalkyl of one to six carbon atoms, alkenyl of three to five carbon atoms or alkynyl of three to five carbon atoms, R.sup.2 is aldopentofuranosyl, aldo-pentopyranosyl, aldo-hexopyranosyl, O-aldo-hexopyranosyl-(1.fwdarw.4)-aldo-hexopyranosyl or a group of the formula: --CH.sub.2 (CHOH).sub.n CH.sub.2 OH, and wherein n is zero or an integer of one to four. A method of preparation is disclosed whereby said nitrosourea compound is prepared by the nitrosation of a compound of the formula: ##STR2## wherein R.sup.1 and R.sup.2 are the same as above. Said nitrosourea compound is useful as an anti-tumor or anti-leukemic agent.

    摘要翻译： 一种下式的亚硝基脲化合物：其中R1是1-6个碳原子的烷基，1-6个碳原子的羟基烷基，3-5个碳原子的链烯基或3-5个碳原子的炔基，R2是醛戊二醛，醛 - 吡喃葡萄糖基，醛 - 六吡喃糖基，O-羟基 - 六吡喃糖基 - （1-> 4） - 羟基 - 六吡喃糖基或式-CH 2（CHOH）n CH 2 OH的基团，其中n为0或1〜4的整数。 公开了一种制备方法，其中所述亚硝基脲化合物是通过亚化下式化合物制备的：其中R1和R2与上述相同。 所述的亚硝基脲化合物可用作抗肿瘤或抗白血病药。

    S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof
    28.
    发明授权
    S type 2-substituted hydroxy-2-indolidinylbutyric ester compounds and process for preparation thereof 失效
    S型2-取代羟基-2-吲哚哩啶基丁酸酯化合物及其制备方法

    公开(公告)号：US06277992B1

    公开(公告)日：2001-08-21

    申请号：US09570172

    申请日：2000-05-12

    申请人： Takayuki Kawaguchi ,  Sumihiro Nomura ,  Kenji Tsujihara

    发明人： Takayuki Kawaguchi ,  Sumihiro Nomura ,  Kenji Tsujihara

    IPC分类号： C07D47112

    CPC分类号： C07D491/14 ,  C07B2200/07 ,  C07D209/42 ,  C07D217/26

    摘要： A process for preparing S type 2-substituted hydroxy-2-indolidinyl-butyric ester compound [II]: wherein R0 is residue of nitrogen-containing fused heterocyclic carboxylic acid having absolute configuration of “R”(in which the nitrogen atom is protected), R1 and R2 are lower alkyl group, and E is ester residue, which is useful as an intermediate for preparing camptothecin derivatives having antitumor activities, which comprises 2-ethylating 2-substituted hydroxy-2-indolidinylacetic ester compound [I]: wherein the symbols are as defined above.

    摘要翻译： 一种制备S型2-取代羟基-2-吲哚哩啶基 - 丁酸酯化合物[II]的方法：其中R 0是具有绝对构型“R”（其中保护氮原子）的含氮稠合杂环羧酸的残基， R 1和R 2为低级烷基，E为酯残基，其可用作制备具有抗肿瘤活性的喜树碱衍生物的中间体，其包括2-乙基化2-取代的羟基-2-吲哚哩啶基乙酸酯化合物[I]：其中 符号如上所述。

    Baccatin derivatives and processes for preparing the same
    29.
    发明授权
    Baccatin derivatives and processes for preparing the same 失效
    浆果赤霉素衍生物及其制备方法

    公开(公告)号：US5589502A

    公开(公告)日：1996-12-31

    申请号：US558772

    申请日：1995-11-15

    申请人： Kenji Tsujihara ,  Tomiki Hashiyama ,  Motoaki Ohashi ,  Noriyuki Nakanishi

    发明人： Kenji Tsujihara ,  Tomiki Hashiyama ,  Motoaki Ohashi ,  Noriyuki Nakanishi

    IPC分类号： C07D263/04 ,  C07D263/06 ,  C07D305/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  A61K31/335

    CPC分类号： C07D263/04 ,  C07D263/06 ,  C07D305/14 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12

    摘要： 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.

    摘要翻译： 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。