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15 条记录 (耗时 0.024 秒)

    Carbapenem compound, their production and use
    1.
    发明授权
    Carbapenem compound, their production and use 失效
    碳青霉烯化合物，其生产和使用

    公开(公告)号：US06174877B1

    公开(公告)日：2001-01-16

    申请号：US09101470

    申请日：1998-07-10

    申请人： Yukio Ishibashi ,  Shinichi Imamura ,  Tetsuo Miwa

    发明人： Yukio Ishibashi ,  Shinichi Imamura ,  Tetsuo Miwa

    IPC分类号： A61K3140

    CPC分类号： C07D477/20

    摘要： A cephem compound of the formula: wherein R1 stands for an optionally substituted lower alkyl group, R2 stands for H or a lower alkyl group, R3 stands for H, an optionally substituted hydrocarbon group, cyano group, a lower alkyloxy group or a lower alkylthio group, and the ring A stands for an optionally substituted non-quaternarized nitrogen-containing heterocyclic ring, provided that, when A is unsubstituted 2-pyridyl group, R3 stands for a group other than hydrogen, or their esters or salts, has excellent antibacterial activities, oral absorbability and stability, and is useful as an antibacterial agent.

    摘要翻译： 下式的头孢烯化合物：其中R1代表任意取代的低级烷基，R2代表H或低级烷基，R3代表H，任意取代的烃基，氰基，低级烷氧基或低级烷硫基 并且环A代表任选取代的非季铵化含氮杂环，条件是当A是未取代的2-吡啶基时，R 3代表氢以外的基团或其酯或盐，具有优异的抗菌性 活性，口服吸收性和稳定性，可用作抗菌剂。

    Production of pyrrolopyrimidines and intermediates therefor
    2.
    发明授权
    Production of pyrrolopyrimidines and intermediates therefor 失效
    吡咯并嘧啶及其中间体的生产

    公开(公告)号：US5496946A

    公开(公告)日：1996-03-05

    申请号：US257512

    申请日：1994-06-09

    申请人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    发明人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    IPC分类号： A61K31/505 ,  A61P35/00 ,  C07D239/48 ,  C07D239/49 ,  C07D239/50 ,  C07D487/04

    CPC分类号： C07D239/48 ,  C07D239/50 ,  C07D487/04

    摘要： There is provided an improved process for producing novel compounds represented by the general formula: ##STR1## wherein the ring A/ represents a pyrrole ring which may be hydrogenated; X represents an amino, hydroxyl or mercapto group; R.sup.1, R.sup.2 and R.sup.3 each, being the same as or different from the other, represents hydrogen or an alkyl, alkenyl or alkynyl group which may be substituted; R.sup.4 represents OR.sup.5 wherein R.sup.5 represents hydrogen or a hydrocarbon group which may be substituted or NHCH(COOR.sup.6)CH.sub.2 CH.sub.2 COOR.sup.7 wherein R.sup.6 and R.sup.7 each represents hydrogen or a hydrocarbon group which may be substituted; and n represents an integer of 1 to 4, or a salt thereof from compounds represented by the general formula: ##STR2## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n are the same as defined above; Y.sup.1 and Y.sup.2 each represents oxygen or sulfur atom; R.sup.8 and R.sup.9 each, being the same as or different from the other, represents a hydrocarbon group which may be substituted, or salts thereof by an intramolecular ring closure reaction to form a pyrrolopyrimidine ring and, if necessary, reducing pyrrole ring thus formed to pyrroline ring. The compounds are useful as antitumor agents.

    摘要翻译： 提供了用于制备由以下通式表示的新化合物的改进方法：其中环+ E，crc / A /代表可被氢化的吡咯环; X表示氨基，羟基或巯基; R 1，R 2和R 3各自彼此相同或不同，表示氢或可被取代的烷基，烯基或炔基; R4表示OR5，其中R5表示氢或可被取代的烃基或NHCH（COOR6）CH2CH2COOR7，其中R6和R7各自表示氢或可被取代的烃基; 其中X，R1，R2，R3，R4和n与上述定义相同; n表示1〜4的整数，或其盐由通式： Y1和Y2各自表示氧或硫原子; R 8和R 9各自相同或不同，表示可以被取代的烃基，或其盐通过分子内闭环反应形成吡咯并嘧啶环，如果需要，将如此形成的吡咯环还原成吡咯啉 环。 该化合物可用作抗肿瘤剂。

    Pyrrolopyrimidine derivatives, their production
    3.
    发明授权
    Pyrrolopyrimidine derivatives, their production 失效
    吡咯并嘧啶衍生物，其生产

    公开(公告)号：US5539113A

    公开(公告)日：1996-07-23

    申请号：US161533

    申请日：1993-12-06

    申请人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    发明人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    IPC分类号： C07D487/04 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： A process of making a compound of the formula ##STR1## wherein the ring A is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, --COOR.sup.1 and --COOR.sup.2 are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof have excellent antitumor effects, and can be used as antitumor agents in mammals.

    摘要翻译： 制备式“IMAGE”化合物的方法，其中环+ E，crc A + EE为吡咯或吡咯啉环，X为氨基或羟基，Y为氢原子，氨基或 羟基，R为氢原子，氟原子，烷基，烯基或炔基，-COOR1和-COOR2独立地为可被酯化的n为2-4的整数，R为 可以在每个n个重复单元中不同，并且其盐具有优异的抗肿瘤效果，并且可以用作哺乳动物中的抗肿瘤剂。

    Pyrrolopyrimidine derivatives, their production and use
    5.
    发明授权
    Pyrrolopyrimidine derivatives, their production and use 失效
    吡咯并嘧啶衍生物，其生产和使用

    公开(公告)号：US4997838A

    公开(公告)日：1991-03-05

    申请号：US326901

    申请日：1989-03-21

    申请人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    发明人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： A compound of the formula ##STR1## wherein the ring .circle.A is a pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, --COOR.sup.1 and --COOR.sup.2 are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof have excellent antitumor effects, and can be used as antitumor agents in mammals.

    Pyrrolopyrimidine derivatives, their production and use
    7.
    发明授权
    Pyrrolopyrimidine derivatives, their production and use 失效
    吡咯并嘧啶衍生物，其生产和使用

    公开(公告)号：US5296600A

    公开(公告)日：1994-03-22

    申请号：US824106

    申请日：1992-01-22

    申请人： Akimoto Hiroshi ,  Takenori Hitaka ,  Tetsuo Miwa

    发明人： Akimoto Hiroshi ,  Takenori Hitaka ,  Tetsuo Miwa

    IPC分类号： C07D487/04 ,  C07D471/04

    CPC分类号： C07D487/04

    摘要： A compound of the formula ##STR1## wherein the ring A pyrrole or pyrroline ring, X is an amino group or a hydroxyl group, Y is a hydrogen atom, an amino group or a hydroxyl group, R is a hydrogen atom, a fluorine atom, an alkyl group, an alkenyl group or an alkynyl group, --COOR.sup.1 and --COOR.sup.2 are independently carboxyl groups which may be esterified and n is an integer of 2 to 4, and R may be different in each of the n repeating units, and salts thereof have excellent antitumor effects, and can be used as antitumor agents in mammals.

    摘要翻译： 式中，环+ E，crc / A /吡咯或吡咯啉环，X为氨基或羟基，Y为氢原子，氨基或羟基的化合物 基团，R为氢原子，氟原子，烷基，烯基或炔基，-COOR1和-COOR2独立地为可被酯化的羧基，n为2〜4的整数，R可以 在每个n个重复单元中是不同的，并且其盐具有优异的抗肿瘤效果，并且可以用作哺乳动物中的抗肿瘤剂。

    Pyrido[2,3-d]pyrimidine compounds useful as intermediates
    8.
    发明授权
    Pyrido[2,3-d]pyrimidine compounds useful as intermediates 失效
    吡啶并[2,3-d]嘧啶化合物可用作中间体

    公开(公告)号：US5223620A

    公开(公告)日：1993-06-29

    申请号：US830884

    申请日：1992-02-04

    申请人： Hiroaki Nomura ,  Hiroshi Akimoto ,  Tetsuo Miwa

    发明人： Hiroaki Nomura ,  Hiroshi Akimoto ,  Tetsuo Miwa

    IPC分类号： C07D239/95 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D239/95

    摘要： New fused pyrimidines of the general formula (I): ##STR1## wherein the ring A is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, fluorine or a lower alkyl group, and --COOR.sup.5 and --COOR.sup.6 are independently a carboxyl group which may be esterified, and salts thereof have excellent anti-tumor effects, and they can be produced by the following reaction scheme: ##STR2## in which A is, X, R.sup.1 to R.sup.4, --COOR.sup.5 have the above meanings.

    摘要翻译： 通式（I）的新的稠合嘧啶：其中环+ E，crc / A /是可被氢化的吡啶环或可被氢化的苯环，X是氨基或 羟基，R1，R2，R3和R4独立地是氢，氟或低级烷基，-COOR5和-COOR6独立地是可被酯化的羧基，其盐具有优异的抗肿瘤效果，并且它们 可以通过以下反应方案制备：其中+ E，crc / A / is，X，R 1至R 4，-COOR 5具有上述含义的 + TR 。

    Fused pyrimidines, their production and use
    9.
    发明授权
    Fused pyrimidines, their production and use 失效
    融合嘧啶，其生产和使用

    公开(公告)号：US4946846A

    公开(公告)日：1990-08-07

    申请号：US329374

    申请日：1989-03-27

    申请人： Hiroaki Nomura ,  Hiroshi Akimoto ,  Tetsuo Miwa

    发明人： Hiroaki Nomura ,  Hiroshi Akimoto ,  Tetsuo Miwa

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P35/00 ,  C07D239/95 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D239/95

    摘要： New fused pyrimidines of the general formula (I): ##STR1## wherein the ring .circle. A is a pyridine ring which may be hydrogenated or a benzene ring which may be hydrogenated, X is an amino group or a hydroxyl group, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently hydrogen, fluorine or a lower alkyl group, and --COOR.sup.5 and --COOR.sup.6 are independently a carboxyl group which may be esterified, and salts thereof have excellent anti-tumor effects, and they can be produced by the following reaction scheme: ##STR2## in which .circle. A is, X, R.sup.1 to R.sup.4, --COOR.sup.5 have the above meanings.