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    Penam derivatives
    1.
    发明授权
    Penam derivatives 失效
    Penam衍生物

    公开(公告)号：US4626384A

    公开(公告)日：1986-12-02

    申请号：US716948

    申请日：1985-03-28

    申请人： Motoaki Tanaka ,  Makoto Kajitani ,  Tomio Yamazaki

    发明人： Motoaki Tanaka ,  Makoto Kajitani ,  Tomio Yamazaki

    IPC分类号： C07D519/06 ,  A61K31/43 ,  A61P31/04 ,  C07D499/00 ,  C07D499/21 ,  C07D499/32 ,  C07D499/86 ,  C07D519/00

    CPC分类号： C07D499/00

    摘要： This invention provides a penam derivative represented by the formula ##STR1## wherein R is hydrogen or methyl and R.sub.1 is (hexahydro-1H-azepin-1-yl)methyleneamino, 2-phenylacetamido, 2-phenoxyacetamido, 2-amino-2-phenylacetamido, 2-amino-2-(p-hydroxyphenyl)acetamido or 2-(4-ethyl-2,3-dioxo-1-piperazine)carboxamido-2-phenylacetamido, and a salt thereof, and processes for preparing them.

    摘要翻译： 本发明提供由式（I）表示的对苯二甲酸衍生物，其中R是氢或甲基，R 1是（六氢-1H-吖庚因-1-基）亚甲基氨基，2-苯基乙酰氨基，2-苯氧基乙酰氨基， 2-氨基-2-（对羟基苯基）乙酰氨基或2-（4-乙基-2,3-二氧代-1-哌嗪）甲酰胺基-2-苯基乙酰氨基及其盐及其制备方法 。

    Penicillin derivatives
    2.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4668514A

    公开(公告)日：1987-05-26

    申请号：US658373

    申请日：1984-10-05

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Tomio Yamazaki ,  Naobumi Ishida ,  Makoto Kajitani

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Tomio Yamazaki ,  Naobumi Ishida ,  Makoto Kajitani

    IPC分类号： C07D499/86 ,  A61K31/43 ,  C07D499/00 ,  A61K31/425

    CPC分类号： C07D499/00 ,  A61K31/43 ,  Y02P20/55

    摘要： This invention provides a penicillin derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and represent hydrogen, C.sub.1-6 alkyl, C.sub.1-6 hydroxyalkyl, C.sub.3-9 acyloxyalkyl, C.sub.8-13 benzyloxyalkyl, C.sub.2-7 alkoxyalkyl, C.sub.2-7 alkoxycarbonyl, C.sub.3-8 alkenyloxycarbonyl, C.sub.3-8 alkynyloxycarbonyl, phenyl, amino, cyano, formyl, trifluoromethyl, C.sub.2-6 acyl, carbamoyl, C.sub.2-7 alkylcarbamoyl, benzyloxycarbonylamino, C.sub.2-7 alkoxycarbonylamino; and R.sub.3 is hydrogen, a group for forming a pharmaceutically acceptable salt, or a penicillin carboxyl protecting group, with the proviso that both of R.sub.1 and R.sub.2 are not hydrogen or C.sub.2-7 alkoxycarbonyl at the same time and that when one of R.sub.1 and R.sub.2 is hydrogen, the other is not C.sub.2-7 alkoxycarbonyl, or a pharmaceutically acceptable acid addition salt, process for preparing the derivative, and a pharmaceutical composition containing the derivative.

    摘要翻译： 本发明提供了一种下式的青霉素衍生物，其中R1和R2相同或不同，代表氢，C1-6烷基，C1-6羟烷基，C3-9酰氧基烷基，C8-13苄氧基烷基，C2-7烷氧基烷基， C 2-8烷氧基羰基，C 3-8烯氧基羰基，C 3-8炔氧基羰基，苯基，氨基，氰基，甲酰基，三氟甲基，C 2-6酰基，氨基甲酰基，C 2-7烷基氨基甲酰基，苄氧基羰基氨基，C 2-7烷氧基羰基氨基; 并且R 3是氢，用于形成药学上可接受的盐的基团或青霉素羧基保护基，条件是R 1和R 2同时不是氢或C 2-7烷氧基羰基，并且当R 1和R 2之一 是氢，另一个不是C 2-7烷氧基羰基，或其药学上可接受的酸加成盐，制备衍生物的方法和含有该衍生物的药物组合物。

    Penicillin derivatives
    3.
    发明授权
    Penicillin derivatives 失效
    青霉素衍生物

    公开(公告)号：US4562073A

    公开(公告)日：1985-12-31

    申请号：US519491

    申请日：1983-08-01

    申请人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Makoto Kajitani ,  Tomio Yamazaki ,  Naobumi Ishida

    发明人： Ronald G. Micetich ,  Shigeru Yamabe ,  Motoaki Tanaka ,  Makoto Kajitani ,  Tomio Yamazaki ,  Naobumi Ishida

    IPC分类号： C07D499/86 ,  C07D499/00 ,  C07F7/10 ,  A61K31/425

    CPC分类号： C07D499/00 ,  C07F7/10

    摘要： A penicillin derivative represented by the following formula ##STR1## wherein R.sub.1 is hydrogen or trialkylsilyl; R.sub.2 is hydrogen, trialkylsilyl or COOR.sub.2 ' wherein R.sub.2 ' is hydrogen, C.sub.1-18 alkyl, C.sub.2-7 alkoxymethyl, C.sub.3-8 alkylcarbonyloxymethyl, C.sub.4-9 alkylcarbonyloxyethyl, (C.sub.5-7 cycloalkyl)carbonyloxymethyl, C.sub.9-14 benzylcarbonyloxyalkyl, C.sub.3-8 alkoxycarbonylmethyl, C.sub.4-9 alkoxycarbonylethyl, phthalidyl, crotonolacton-4-yl, .gamma.-butyrolacton-4-yl, halogenated C.sub.1-6 alkyl substituted with 1 to 3 halogen atoms, C.sub.1-6 alkoxy- or nitro-substituted or unsubstituted benzyl, benzhydryl, tetrahydropyranyl, dimethylaminoethyl, dimethylchlorosilyl, trichlorosilyl, (5-substituted C.sub.1-6 alkyl or phenyl or unsubstituted-2-oxo-1,3-dioxoden-4-yl)methyl, C.sub.8-13 benzoyloxyalkyl or group for forming a pharmaceutically acceptable salt; and R.sub.3 has the same meaning as above R.sub.2 '.

    摘要翻译： 由下式（IMAGE）表示的青霉素衍生物，其中R1是氢或三烷基甲硅烷基; R2是氢，三烷基甲硅烷基或COOR2'，其中R2'是氢，C1-18烷基，C2-7烷氧基甲基，C3-8烷基羰氧基甲基，C4-9烷基羰氧基乙基，（C5-7环烷​​基）羰基氧基甲基，C9-14苄基羰氧基烷基，C3-8 烷氧基羰基甲基，C4-9烷氧基羰基乙基，苯酞基，巴豆酸内酯-4-基，γ-丁内酯-4-基，被1至3个卤素原子取代的卤代C 1-6烷基，C 1-6烷氧基或硝基取代或未取代的苄基，二苯甲基 ，四氢吡喃基，二甲基氨基乙基，二甲基氯甲硅烷基，三氯甲硅烷基，（5-取代的C 1-6烷基或苯基或未取代的-2-氧代-1,3-二氧杂环己烯-4-基）甲基，C8-13苯甲酰氧基烷基或用于形成药学上可接受的盐 ; 和R3具有与上述R2'相同的含义。

    Process for producing isoxazole derivatives
    4.
    发明授权
    Process for producing isoxazole derivatives 失效
    异恶唑衍生物的制备方法

    公开(公告)号：US5310926A

    公开(公告)日：1994-05-10

    申请号：US121557

    申请日：1993-09-16

    申请人： Yu-ichi Hagiwara ,  Motoaki Tanaka ,  Makoto Kajitani ,  Mitsugi Yasumoto

    发明人： Yu-ichi Hagiwara ,  Motoaki Tanaka ,  Makoto Kajitani ,  Mitsugi Yasumoto

    IPC分类号： C07D261/08

    CPC分类号： C07D261/08

    摘要： The present invention provides a process for producing isoxazole derivatives represented by the formula ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each a hydrogen atom or lower alkoxyl, and R.sup.3 is cyano or alkoxycarbonyl, the process being characterized by oxidizing an .alpha., .beta.-unsaturated ketoxime derivative represented by the formula ##STR2## wherein R.sup.1 , R.sup.2 and R.sup.3 are as defined above. The isoxazole derivatives (II) to be produced by the process of the present invention are useful as intermediates for preparing (3,4-diarylisoxazol-5-yl) acetic acid derivatives which are useful as anti-inflammatory agents, analgesics and antipyretics.

    摘要翻译： 本发明提供一种制备由式（II）表示的异恶唑衍生物的方法，其中R 1和R 2相同或不同，各自为氢原子或低级烷氧基，R 3为氰基或烷氧基羰基，该方法的特征在于 通过氧化由式（I）表示的α，β-不饱和酮肟衍生物，其中R 1，R 2和R 3如上所定义。 通过本发明的方法生产的异恶唑衍生物（II）可用作制备（3,4-二芳基异恶唑-5-基）乙酸衍生物的中间体，其可用作抗炎剂，止痛剂和解热药。

    .alpha., .beta.-unsaturated ketones and ketoxime derivatives
    5.
    发明授权
    .alpha., .beta.-unsaturated ketones and ketoxime derivatives 失效
    （ALPHA），（BETA） - 饱和的酮和酮替代衍生物

    公开(公告)号：US5142091A

    公开(公告)日：1992-08-25

    申请号：US690939

    申请日：1991-07-10

    申请人： Motoaki Tanaka ,  Yu-ichi Hagiwara ,  Makoto Kajitani ,  Mitsugi Yasumoto

    发明人： Motoaki Tanaka ,  Yu-ichi Hagiwara ,  Makoto Kajitani ,  Mitsugi Yasumoto

    IPC分类号： C07D261/08 ,  C07C69/738 ,  C07C251/48 ,  C07C255/37 ,  C07C255/40 ,  C07C255/62 ,  C07C255/64

    CPC分类号： C07C69/738 ,  C07C251/48 ,  C07C255/40 ,  C07C255/64

    摘要： The present invention provides an .alpha., .beta.-unsaturated ketone and ketoxime derivative represented by the formula ##STR1## wherein Y is oxygen atom or hydroxyimino group, Z is cyano or alkoxycarbonyl group, R.sup.1 and R.sup.2 are the same or different and are each hydrogen atom or lower alkoxyl group.The .alpha., .beta.-unsaturated ketones and ketoxime derivatives of the invention are useful as an intermediate for preparing a (3,4-diarylisoxazol-5-yl)acetic acid derivatives which is useful as an anti-inflammatory agent, analgesic and antipyretic.

    摘要翻译： PCT No.PCT / JP90 / 01512 Sec。 371日期：1991年7月10日 102（e）日期1991年7月10日PCT 1990年11月19日PCT PCT。 公开号WO91 / 07374 日本1991年5月30日。本发明提供由式（I）表示的+60，β-不饱和酮和酮肟衍生物，其中Y是氧原子或羟基亚氨基，Z是氰基或烷氧基羰基，R1和R2 相同或不同，为氢原子或低级烷氧基。 本发明的α，β-不饱和酮和酮肟衍生物可用作制备（3,4-二芳基异恶唑-5-基）乙酸衍生物的中间体，其可用作抗炎剂，镇痛和解热。

    Oxindole derivative
    7.
    发明授权
    Oxindole derivative 失效
    OXINDOLE DERIVATIVE

    公开(公告)号：US5206261A

    公开(公告)日：1993-04-27

    申请号：US663960

    申请日：1991-03-20

    申请人： Akihiro Kawaguchi ,  Atsushi Sato ,  Makoto Kajitani ,  Mitsugi Yasumoto ,  Junji Yamamoto

    发明人： Akihiro Kawaguchi ,  Atsushi Sato ,  Makoto Kajitani ,  Mitsugi Yasumoto ,  Junji Yamamoto

    IPC分类号： A61K31/40 ,  A61K31/44 ,  C07D209/34 ,  C07D401/06 ,  C07D405/06

    CPC分类号： C07D401/06 ,  C07D209/34 ,  C07D405/06

    摘要： The present invention provides an oxindole derivative which has the following formula and is useful as medicaments for treating senile dementia, i.e., as cerebral function improving agents and cerebral metabolism activators or anoxic brain damage protectives ##STR1## wherein R.sup.1 is hydrogen atom, halogen atom, lower alkyl group or lower alkoxyl group, R.sup.2 is hydrogen atom or lower alkyl group, R.sup.3 is --CH.sub.2 --R.sup.5 group (R.sup.5 being alkyl group which may form a ring; benzodioxanyl group; or phenyl group which may have plural substituents selected from among halogen atom, lower alkyl group, lower alkoxyl group, hydroxyl group, diethylamino group, trifluoromethyl group, nitrile group, nitro group and benzyloxy group), R.sup.2 and R.sup.3 may form together .dbd.CH--R.sup.5 (R.sup.5 being same as above), R.sup.4 is 1-propylbutyl group; pyridyl group; or phenyl group which may be substituted by lower alkoxyl group, halogen atom, diethylamino group, benzyloxy group, trifluoromethyl group, nitrile group, nitro group or lower alkyl group.