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22 条记录 (耗时 0.022 秒)

    Imidazole derivatives, production method thereof and use thereof
    3.
    发明授权
    Imidazole derivatives, production method thereof and use thereof 有权
    咪唑衍生物及其制备方法及用途

    公开(公告)号：US07141598B2

    公开(公告)日：2006-11-28

    申请号：US10416986

    申请日：2001-11-16

    申请人： Akihiro Tasaka ,  Takenori Hitaka ,  Nobuyuki Matsunaga ,  Masami Kusaka

    发明人： Akihiro Tasaka ,  Takenori Hitaka ,  Nobuyuki Matsunaga ,  Masami Kusaka

    IPC分类号： A61K31/4184 ,  C07D235/02

    CPC分类号： C07D233/64 ,  C07D471/04 ,  C07D487/04

    摘要： The present invention provides a compound having a steroid C17,20-lyase-inhibitory activity and useful for the therapy and prophylaxis of tumor such as prostatism, breast cancer and the like, and a method for efficiently separating an optically active compound of this compound from a mixture of optical isomers thereof, a compound of the formula: wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof, and a method for obtaining an optically active compound by optically resolving a mixture of optical isomers by the use of a resolving agent such as tartranilic acid and the like.

    摘要翻译： 本发明提供了具有类固醇C 17,20 - 酶抑制活性并可用于治疗和预防诸如前列腺症，乳腺癌等肿瘤的化合物和有效分离的方法 该化合物的旋光异构体的混合物的光学活性化合物，下式的化合物：其中每个符号如说明书中所定义，其盐或其前药，以及通过光学获得光学活性化合物的方法 通过使用诸如格列硝酸等拆分剂来拆分光学异构体的混合物。

    Pyrrolopyrimidine derivatives, their production and use
    4.
    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.

    Thienopyrimidine compounds and use thereof
    5.
    发明授权
    Thienopyrimidine compounds and use thereof 有权
    噻吩并嘧啶化合物及其用途

    公开(公告)号：US07300935B2

    公开(公告)日：2007-11-27

    申请号：US10544069

    申请日：2004-01-28

    申请人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

    发明人： Nobuo Cho ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

    IPC分类号： C07D495/04 ,  C07D237/04 ,  A61K31/519 ,  A61K31/501 ,  A61P5/04

    CPC分类号： C07D495/04 ,  A61K31/519

    摘要： The present invention provides a compound represented by the formula: wherein R1 is a C1-4alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C1-4alkyl and (4′) a C1-4alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C1-4alkoxy-C1-4alkyl, (3′) a mono-C1-4alkyl-carbamoyl-C1-4alkyl, (4′) a C1-4alkoxy and (5′) a mono-C1-4alkylcarbamoyl-C1-4alkoxy, or the like; R3 is a C1-4alkyl; R4 is a C1-4alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

    摘要翻译： 本发明提供由下式表示的化合物：其中R 1是C 1-4烷基; R 2是（1）可以具有选自（1'）卤素，（2'）羟基的取代基的5-至7-元含氮杂环基 ，（3'）C 1-4烷基和（4'）C 1-4烷氧基，（2）可具有选自以下的取代基的苯基： （1'）卤素，（2'），C 1-4烷氧基-C 1-4烷基，（3'）单-C 烷基 - 氨基甲酰基-C 1-4烷基，（4'）C 1-4烷氧基和（5'）单 -C 1-4烷基氨基甲酰基-C 1-4烷氧基等; R 3是C 1-4烷基; R 4是C 1-4烷氧基等; n为1〜4的整数， 或其盐作为具有促性腺激素释放激素拮抗活性的噻吩并嘧啶化合物。

    Heterocyclic compounds their production and use
    6.
    发明授权
    Heterocyclic compounds their production and use 失效
    杂环化合物的生产和使用

    公开(公告)号：US06716863B2

    公开(公告)日：2004-04-06

    申请号：US09889974

    申请日：2001-07-24

    申请人： Akihiro Tasaka ,  Takenori Hitaka ,  Etsuya Matsutani

    发明人： Akihiro Tasaka ,  Takenori Hitaka ,  Etsuya Matsutani

    IPC分类号： A61K31422

    CPC分类号： C07D413/12 ,  C07D263/32

    摘要： A compound represented by the formula: wherein m is 1 or 2, R1 is a halogen or an optionally halogenated C1-2 alkyl; one of R2 and R3 is a hydrogen atom and the other is a group represented by the formula: wherein n is 3 or 4; R4 is a C1-4 alkyl group substituted by 1 or 2 hydroxy groups, or a salt thereof shows tyrosine kinase-inhibiting activity.

    摘要翻译： 由下式表示的化合物：其中m为1或2，R 1为卤素或任选卤代的C 1-2烷基; R 2和R 3之一是氢原子，另一个是由下式表示的基团：其中n是3或4; R 4是被1或2个羟基取代的C 1-4烷基，或其盐表示酪氨酸激酶抑制活性。

    Production of pyrrolopyrimidines
    7.
    发明授权
    Production of pyrrolopyrimidines 失效
    吡咯并嘧啶的生产

    公开(公告)号：US5349064A

    公开(公告)日：1994-09-20

    申请号：US29310

    申请日：1993-03-08

    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 the pyrrole ring thus formed to a 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，将由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
    8.
    发明授权
    Pyrrolopyrimidine derivatives 失效
    吡咯烷酮衍生物

    公开(公告)号：US5106974A

    公开(公告)日：1992-04-21

    申请号：US578258

    申请日：1990-09-06

    申请人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    发明人： Hiroshi Akimoto ,  Takenori Hitaka ,  Tetsuo Miwa

    IPC分类号： C07D487/04

    CPC分类号： C07D487/04

    摘要： 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.

    Thienopyrimidines, process for preparing the same and use thereof
    10.
    发明授权
    Thienopyrimidines, process for preparing the same and use thereof 有权
    噻吩并嘧啶，其制备方法及其用途

    公开(公告)号：US07569570B2

    公开(公告)日：2009-08-04

    申请号：US10502903

    申请日：2003-01-29

    申请人： Shuichi Furuya ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

    发明人： Shuichi Furuya ,  Takashi Imada ,  Takenori Hitaka ,  Kazuhiro Miwa ,  Masami Kusaka ,  Nobuhiro Suzuki

    IPC分类号： A61K31/519 ,  C07D495/04

    CPC分类号： C07D495/04

    摘要： The present invention provides a thienopyrimidine compound, represented by the formula [wherein, R1 is C1-4 alkyl, R2 is (1) phenyl optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino, or (2) a heterocyclic group optionally having a substituent such as amino, mono C1-4 alkylamino and di C1-4 alkylamino and the like, R3 is a hydrogen atom or C1-4 alkyl, R4 is C1-4 alkyl optionally having a substituent such as C1-4 alkoxy-carbonyl, carboxyl, mono C1-4 alkylamino and N—C1-4 alkyl-N—C7-10 aralkylamino and the like] or a salt thereof, which has antagonistic action for gonadotropin-releasing hormone.

    摘要翻译： 本发明提供由式[其中，R 1为C 1-4烷基，R 2为（1）任选具有取代基的苯基，例如氨基，单C 1-4烷基氨基和二C 1-4烷基氨基的噻吩并嘧啶化合物或（ 2）任选具有取代基的杂环基，例如氨基，单C 1-4烷基氨基和二C 1-4烷基氨基等，R 3是氢原子或C 1-4烷基，R 4是任选具有取代基的C 1-4烷基 作为对促性腺激素释放激素具有拮抗作用的C 1-4烷氧基 - 羰基，羧基，单C 1-4烷基氨基和N-C 1-4烷基-N C 7-10芳烷基氨基等]或其盐。