Nitrosourea substituted phosphonates and pharmaceutical use
    1.
    发明授权
    Nitrosourea substituted phosphonates and pharmaceutical use 失效
    硝基脲取代膦酸盐和药物用途

    公开(公告)号:US4567169A

    公开(公告)日:1986-01-28

    申请号:US547881

    申请日:1983-11-02

    CPC分类号: C07F9/3808 C07F9/4006

    摘要: New nitrosourea compounds that can be used as medicaments and correspond to the general formula I ##STR1## in which R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, thienyl, or phenyl which may carry substituents,R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, or benzyl which may carry substituents, orR.sub.2 and R.sub.3 together represent --(CH.sub.2).sub.m --, m being 3 or 4.Pharmaceutical compositions; therapeutic administration especially for the treatment of tumours.

    摘要翻译: 可用作药物并且对应于通式I(I)的新的亚硝基脲化合物,其中R 1是氢,C 1 -C 6烷基或苯基,R 2是氢,C 1 -C 6烷基,噻吩基或苯基, 携带取代基,R 3是氢,可以带有取代基的C 1 -C 6烷基或苄基,或者R 2和R 3一起表示 - (CH 2)m - ,m为3或4。 特别是用于治疗肿瘤的治疗性给药。

    N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid useful for
treating neoplastic diseases
    2.
    发明授权
    N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid useful for treating neoplastic diseases 失效
    用于治疗肿瘤疾病的1-氨基甲基膦酸的N-(23-长春碱)基化合物

    公开(公告)号:US4946833A

    公开(公告)日:1990-08-07

    申请号:US276357

    申请日:1988-11-23

    CPC分类号: C07F9/6561

    摘要: The invention relates to N-(23-vinblastinoyl)compounds of 1-aminomethylphosphonic acid of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical containing from 1 to 6 carbon atoms, a linear or branched alkylene radical containing from 1 to 6 carbon atoms, an arylalkyl radical having 7 to 10 carbon atoms and capable of bearing a halogen atom as a substituent on the aromatic ring, a hydroxyl radical or an alkyl or alkoxy radical each containing from 1 to 5 carbon atoms, a 2-indolylmethyl radical, a 4-imidzolylmethyl radical or an alkoxycarbonylmethyl radical containing from 3 to 11 carbon atoms,R.sub.2 and R.sub.3, which may be identical or different, each denote a linear or branched alkyl radical containing from 1 to 4 carbon atoms,in the form of a mixture of diastereoisomers or of pure isomers, their N.sup.b' -oxides and their addition salts with a pharmaceutically acceptable inoranic or organic acid.These compounds are antitumor agents.

    摘要翻译: 本发明涉及通式I(I)的1-氨基甲基膦酸的N-(23-长春碱)基化合物,其中:R1表示氢原子,含有1至6个碳原子的直链或支链烷基, 含有1至6个碳原子的直链或支链亚烷基,具有7至10个碳原子且能够带有卤素原子作为芳族环上的取代基的芳基烷基,羟基或烷基或烷氧基,每个含有 1至5个碳原子,2-吲哚基甲基基团,4-亚氨基甲基基团或含有3至11个碳原子的烷氧羰基甲基基团,可以相同或不同,表示直链或支链烷基, 1至4个碳原子,以非对映异构体或纯异构体的混合物形式,其Nb'氧化物及其与药学上可接受的无机酸或有机酸的加成盐。 这些化合物是抗肿瘤剂。

    Oxaazaphosphorine compounds and pharmaceutical compositions
    3.
    发明授权
    Oxaazaphosphorine compounds and pharmaceutical compositions 失效
    奥氮平磷化合物和药物组合物

    公开(公告)号:US4605647A

    公开(公告)日:1986-08-12

    申请号:US752365

    申请日:1985-07-05

    CPC分类号: C07F9/65846

    摘要: New oxaazaphosphorine compounds corresponding to the formula: ##STR1## in which R is alkyl, cycloalkyl or alkoxy,phenyl, phenylalkyl, phenoxy or thiophenoxy in which the phenyl ring may be substituted by alkyl or alkoxy or by halogen.mono- or di-alkylamino optionally mono- or di-substituted by halogen, orpyrrolidinyl, piperidyl or morpholinyl or optionally substituted piperazinyl.These compounds may be used for antineoplastic therapy especially in the treatment of tumors.

    摘要翻译: 对应于下式的新的氮杂磷杂环丁烷化合物:其中R是烷基,环烷基或烷氧基,苯基,苯基烷基,苯氧基或硫代苯氧基,其中苯环可被烷基或烷氧基取代或被卤素取代。 任选被卤素或吡咯烷基,哌啶基或吗啉基或任选取代的哌嗪基单取代或二取代的单 - 或二 - 烷基氨基。 这些化合物可用于抗肿瘤治疗,特别是用于治疗肿瘤。

    Tripeptide compounds having a nitrogenous polycyclic structure
    4.
    发明授权
    Tripeptide compounds having a nitrogenous polycyclic structure 失效
    具有含氮多环结构的三肽化合物

    公开(公告)号:US5047400A

    公开(公告)日:1991-09-10

    申请号:US207710

    申请日:1988-06-16

    CPC分类号: C07K5/0815

    摘要: The invention relates to the compounds of general formula: ##STR1## in which: X denotes either an oxygen atom, or two hydrogen atoms;Y denotes either a hydrogen atom, or a hydroxyl group;or Y denotes an amino group on condition that X denotes two hydrogen atoms;R denotes a hydrogen atom, or a straight- or branched-chain alkyl group having 1 to 6 carbon atoms, optionally substituted with one or more hydroxy, amino, mercapto, methylthio or carboxy groups, or aryl groups such as phenyl, pyridyl or thienyl; ##STR2## denotes a polycyclic nitrogenous structure; their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.

    摘要翻译: 本发明涉及以下通式的化合物:其中:X表示氧原子或两个氢原子; Y表示氢原子或羟基; 或者Y表示氨基,条件是X表示两个氢原子; R表示氢原子或具有1至6个碳原子的直链或支链烷基,任选被一个或多个羟基,氨基,巯基,甲硫基或羧基取代,或芳基如苯基,吡啶基或噻吩基 ; “IMAGE”表示多环含氮结构; 它们的对映体,差向异构体和非对映异构体,以及它们与药学上可接受的酸或碱的加成盐。

    New heteroarotinoid compounds
    5.
    发明授权
    New heteroarotinoid compounds 失效
    新型类似物类化合物

    公开(公告)号:US4975455A

    公开(公告)日:1990-12-04

    申请号:US336224

    申请日:1989-04-11

    CPC分类号: C07D311/58

    摘要: Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.

    摘要翻译: 通式(I)的化合物:其中:R表示氢原子,卤素原子或羟基,低级烷基,低级烷氧基,羧基,(低级烷氧基)羰基,(低级芳基烷氧基)羰基,氨基羰基,( 低级单或二烷基)氨基羰基或(低级芳基烷基)氨基羰基,被杂环基取代的氨基羰基,或硫代(低级烷基)硫基,磺酰基或(低级烷基)磺酰基,R1,R2,R3 和可以相同或不同的R 4表示任选被一个或多个卤素原子取代的氢原子,卤素原子或低级烷基,低级链烯基,低级烷氧基或低级链烯氧基,它们的异构体,对映体,非对映异构体,以及 当R表示羧基时,其与药学上可接受的碱的加成盐,当R含有碱性基团时,其与药学上可接受的酸的加成盐。

    Peptide compounds having a nitrogenous polycyclic structure
    6.
    发明授权
    Peptide compounds having a nitrogenous polycyclic structure 失效
    具有含氮多环结构的肽化合物

    公开(公告)号:US4965250A

    公开(公告)日:1990-10-23

    申请号:US148027

    申请日:1988-01-25

    摘要: Tetrapeptide compounds of general formula: ##STR1## in which R denotes:a hydrogen atom,a straight- or branched-chain alkyl radical containing from 1 to 4 carbon atoms,an aryl radical such as phenyl or a heterocyclic aromatic radical such as thienyl, optionally substituted with a hydroxy, amino, mercapto, methylthio or lower alkyl group,a lower aralkyl radical such as benzyl,R' denotes a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms,X denotes an oxygen atom or an NH group,Y denotes an oxygen or sulfur atom when X denotes an NH group, or Y denotes an NH group when X denotes an oxygen atom,t denotes 0 or 1, ##STR2## denotes a nitrogen-containing polycyclic structure, their enantiomers, epimers and diastereoisomers, as well as their addition salts with a pharmaceutically acceptable acid or base.Medicinal products.

    摘要翻译: 具有以下通式的四肽化合物:其中R表示氢原子,含有1至4个碳原子的直链或支链烷基,芳基如苯基或杂环芳族基,如噻吩基 任选被羟基,氨基,巯基,甲硫基或低级烷基取代,低级芳烷基如苄基,R'表示氢原子或含有1至4个碳原子的直链或支链烷基,X 表示氧原子或NH基,当X表示NH基时,Y表示氧或硫原子,或当X表示氧原子时,Y表示NH基,t表示0或1,表示含氮 多环结构,它们的对映异构体,差向异构体和非对映异构体,以及它们与药学上可接受的酸或碱的加成盐。 药用产品。