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23 条记录 (耗时 0.021 秒)

    Process for producing brominated 1,3-dioxolen-2-ones
    2.
    发明授权
    Process for producing brominated 1,3-dioxolen-2-ones 失效
    生产溴化1,3-二氧戊环-2-酮的方法

    公开(公告)号：US4428806A

    公开(公告)日：1984-01-31

    申请号：US426158

    申请日：1982-09-28

    申请人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto ,  Isamu Utsumi

    发明人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto ,  Isamu Utsumi

    IPC分类号： A61K31/43 ,  A61P31/04 ,  A61P43/00 ,  C07D317/40 ,  C07D317/46 ,  C07D499/32 ,  B01J19/12

    CPC分类号： C07D317/46 ,  C07D317/40

    摘要： A process for producing a brominated 1,3-dioxolen-2-one of the following general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group, or an aryl group, and R.sub.2 represents a hydrogen atom, or R.sub.1 and R.sub.2 may be bonded together to form --(CH.sub.2).sub.n -- in which n represents an integer of 3 to 5, which comprises reacting a compound of the following formula (II) ##STR2## wherein R.sub.1 and R.sub.2 are as defined, with bromine under radical generating conditions.

    摘要翻译： 制备以下通式（I）的溴化1,3-二氧杂环戊烯-2-酮的方法其中R 1表示氢原子，甲基或芳基，R 2表示氢 原子或R 1和R 2可以键合在一起形成 - （CH 2）n - ，其中n表示3至5的整数，其包括使下式（II）的化合物其中R 1和 R 2如定义，溴在自由基产生条件下。

    Novel ampicillin esters and production thereof
    3.
    发明授权
    Novel ampicillin esters and production thereof 失效
    新型氨苄西林酯及其生产

    公开(公告)号：US4389408A

    公开(公告)日：1983-06-21

    申请号：US327735

    申请日：1981-12-04

    申请人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto ,  Isamu Utsumi

    发明人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto ,  Isamu Utsumi

    IPC分类号： C07D317/40 ,  C07D317/64 ,  C07D499/00 ,  C07D499/12 ,  C07D499/32 ,  C07D499/42 ,  C07D499/68 ,  A61K31/43

    CPC分类号： C07D317/40 ,  C07D317/64 ,  C07D499/00

    摘要： A novel Ampicillin ester of the general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, a methyl group or an aryl group, and R.sub.2 represents a hydrogen atom or may be taken together with R.sub.1 to form a divalent carbon chain residue, or its acid addition salt.The novel Ampicillin ester or its acid addition salt is prepared by (1) reacting a corresponding 6-N-acylamino penicillanic acid (II) or its salt with a compound of the formula ##STR2## wherein R.sub.1 and R.sub.2 are as defined above, and X is a halogen atom, or reacting a compound of the formula ##STR3## wherein R.sub.1 and R.sub.2 are as defined above, or its acid addition salt with a corresponding carboxylic acid (VI) or its reactive derivative, (2) thereafter, if required, when the resulting compound has the protected amino group or the group convertible to an amino group, deprotecting the protected amino group or converting said convertible group to an amino group, and (3) if further required, converting the product to an acid addition salt.The present invention provides also an antibacterial agent comprising the novel Ampicillin ester and a method for the treatment of infectious disease.

    摘要翻译： 一种通式为“IMAGE”的新型氨苄青霉素酯，其中R 1表示氢原子，甲基或芳基，R 2表示氢原子，或可与R 1一起形成二价碳链残基，或其酸 加盐。 通过（1）使相应的6-N-酰基氨基青霉烷酸（II）或其盐与式（III）的化合物反应，其中R 1和R 2如上所定义，制备新型氨苄青霉素酯或其酸加成盐 或者其中R1和R2如上所定义的式（VI）化合物或其酸加成盐与相应的羧酸（Ⅵ）或其反应性衍生物反应， 2）此后，如果需要，当所得化合物具有被保护的氨基或可转化为氨基的基团时，将保护的氨基脱保护或将所述可转换基团转化为氨基，和（3）如果需要，将 产物加酸加成盐。 本发明还提供了包含新型氨苄青霉素酯的抗菌剂和治疗感染性疾病的方法。

    Quinolinecarboxylic acid derivative, and antibacterial agent containing said compound as active ingredient
    4.
    发明授权
    Quinolinecarboxylic acid derivative, and antibacterial agent containing said compound as active ingredient 失效
    喹啉羧酸衍生物和含有所述化合物作为活性成分的抗菌剂

    公开(公告)号：US4455310A

    公开(公告)日：1984-06-19

    申请号：US382353

    申请日：1982-05-26

    申请人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto

    发明人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto

    IPC分类号： C07D405/12 ,  A61K31/495 ,  A61P31/04 ,  C07D317/40 ,  C07D403/14

    CPC分类号： C07D317/40

    摘要： A novel quinolinecarboxylic acid derivative of the formula ##STR1## or a pharmaceutically acceptable salt thereof. These compounds are useful as antibacterial agents, and are prepared by a process which comprises reacting a compound of the formula ##STR2## with a compound of the formula ##STR3##wherein X represents a halogen atom, and thereafter, as required, converting the resulting compound to a pharmaceutically acceptable salt thereof.

    摘要翻译： 式（I）的新型喹啉羧酸衍生物或其药学上可接受的盐。 这些化合物可用作抗菌剂，并且通过包括使下式化合物（II）与下式化合物（III）反应的方法制备，其中X表示卤素原子，其后， 根据需要将所得化合物转化为其药学上可接受的盐。

    Ester of 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanic acid, and its use as antibacterial agent
    5.
    发明授权
    Ester of 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanic acid, and its use as antibacterial agent 失效
    6 - [（六氢-1H-吖庚因-1-基）亚甲基氨基]青霉烷酸酯，其用作抗菌剂

    公开(公告)号：US4416891A

    公开(公告)日：1983-11-22

    申请号：US399132

    申请日：1982-07-16

    申请人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto

    发明人： Fumio Sakamoto ,  Shoji Ikeda ,  Goro Tsukamoto

    IPC分类号： A61K31/43 ,  A61P31/04 ,  C07D317/40 ,  C07D499/00 ,  C07D499/08 ,  C07D499/10 ,  C07D499/21 ,  C07D499/32 ,  A61K31/425

    CPC分类号： C07D499/00 ,  C07D317/40

    摘要： (5-Methyl-2-oxo-1,3-dioxolen-4-yl)methyl 6-[(hexahydro-1H-azepin-1-yl)methyleneamino]penicillanate of the following formula (I) ##STR1## or its pharmaceutically acceptable acid addition salt. The compound is useful as an antibacterial agent and may be prepared by reacting (5-methyl-2-oxo-1,3-dioxolen-4-yl)-methyl 6-aminopenicillanate of the following formula (II) ##STR2## or its acid addition salt with chloro-N,N-hexamethyleneformiminium chloride, and as required, converting the resulting compound to its pharmaceutically acceptable acid addition salt.

    摘要翻译： （I）的（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基6 - [（六氢-1H-吖庚因-1-基）亚甲基氨基]青霉烷酸 或其药学上可接受的酸加成盐。 该化合物可用作抗菌剂，并且可以通过使下式（II）的（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基） - 6-氨基青霉烷酸甲酯（II） ）或其与氯-N，N-六亚甲基酰亚胺氯化物的酸加成盐，并根据需要将所得化合物转化为其药学上可接受的酸加成盐。

    Ester of 1,1-dioxopenicillanic acid, and use thereof as .beta.-lactamase inhibitor
    6.
    发明授权
    Ester of 1,1-dioxopenicillanic acid, and use thereof as .beta.-lactamase inhibitor 失效
    1,1-二氧代青霉烷酸酯，其用作β-内酰胺酶抑制剂

    公开(公告)号：US4448769A

    公开(公告)日：1984-05-15

    申请号：US396471

    申请日：1982-07-08

    申请人： Shoji Ikeda ,  Fumio Sakamoto ,  Goro Tsukamoto ,  Shigeru Yamabe

    发明人： Shoji Ikeda ,  Fumio Sakamoto ,  Goro Tsukamoto ,  Shigeru Yamabe

    IPC分类号： C07D317/40 ,  C07D499/00 ,  C07D499/32 ,  A61K31/425

    CPC分类号： C07D317/40 ,  C07D499/00

    摘要： A 1,1-dioxopenicillanic acid ester represented by formula (I) ##STR1## wherein R represents a methyl or phenyl group. The ester of formula (I) may be prepared by reacting 1,1-dioxopenicillanic acid or its salt with a compound represented by formula (III) ##STR2## wherein R is as defined above, and X represents a halogen atom, or by oxidizing a compound of formula (V) ##STR3## wherein R is as defined above. The ester of the formula (I) is useful as a .beta.-lactamase inhibitor and may be used in association with a .beta.-lactam antibiotic.

    摘要翻译： 由式（I）表示的1,1-二氧代青霉烷酸酯其中R表示甲基或苯基。 式（I）的酯可以通过使1,1-二氧代青霉烷酸或其盐与式（III）表示的化合物反应制备，其中R如上定义，X​​表示卤素原子， 或通过氧化其中R如上定义的式（V）化合物（V）。 式（I）的酯可用作β-内酰胺酶抑制剂，并且可以与β-内酰胺抗生素结合使用。

    Novel ethyl benzylphosphinate derivatives, process for production thereof, and their use as calcium antagonist
    8.
    发明授权
    Novel ethyl benzylphosphinate derivatives, process for production thereof, and their use as calcium antagonist 失效
    新型乙基苄基次膦酸盐衍生物，其制备方法及其作为钙拮抗剂的用途

    公开(公告)号：US4607031A

    公开(公告)日：1986-08-19

    申请号：US737037

    申请日：1985-05-22

    申请人： Koichiro Yoshino ,  Tominori Morita ,  Masaru Moriyama ,  Keizo Ito ,  Goro Tsukamoto

    发明人： Koichiro Yoshino ,  Tominori Morita ,  Masaru Moriyama ,  Keizo Ito ,  Goro Tsukamoto

    IPC分类号： C07F9/6558 ,  A61K31/675 ,  C07F9/65

    CPC分类号： C07F9/65583

    摘要： An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4.The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.

    摘要翻译： 由通式（I）表示的乙基苄基次膦酸盐衍生物其中Y表示氢或氟原子，X表示亚甲基或氧原子，n为2,3或4.所述化合物可以 通过使下式（II）表示的化合物（其中Y如上定义）与由下式（III）表示的化合物（III）反应制备：其中X和n为 并且在惰性介质中M是碱金属原子。 这些化合物可用作钙拮抗剂。

    Novel 4,5-Bis (4-methoxyphenyl)-2-(pyrrol-2-yl) thiazoles and pharmaceutical composition containing the same
    10.
    发明授权
    Novel 4,5-Bis (4-methoxyphenyl)-2-(pyrrol-2-yl) thiazoles and pharmaceutical composition containing the same 失效
    新的4,5-双（4-甲氧基苯基）-2-（吡咯-2-基）噻唑和含有它们的药物组合物

    公开(公告)号：US4659726A

    公开(公告)日：1987-04-21

    申请号：US722322

    申请日：1985-04-12

    申请人： Koichiro Yoshino ,  Norihiko Seko ,  Koichi Yokota ,  Keizo Ito ,  Goro Tsukamoto

    发明人： Koichiro Yoshino ,  Norihiko Seko ,  Koichi Yokota ,  Keizo Ito ,  Goro Tsukamoto

    IPC分类号： C07D207/34 ,  C07D417/04 ,  A61K31/425 ,  C07D277/24 ,  C07D277/28

    CPC分类号： C07D417/04 ,  C07D207/34

    摘要： Novel 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)-thiazoles of the formula: ##STR1## wherein R.sup.1 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, 2,2,2-trifluoroethyl, a group of the formula: --CH.sub.2 COOR.sup.2 R.sup.2 is C.sub.1-8 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, or phenyl-C.sub.1-2 alkyl), or a group of the formula: --(CH.sub.2).sub.n --A--R.sup.3 (A is oxygen or sulfur, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and n is 1, 2 or 3), a process for the preparation of the compounds, and a pharmaceutical composition useful as a platelet aggregation inhibitor which comprises as an active ingredient the above 4,5-bis(4-methoxyphenyl)-2-(pyrrol-2-yl)thiazole compound in admixture with a conventional pharmaceutically acceptable carrier or diluent.

    摘要翻译： 具有下式的新的4,5-双（4-甲氧基苯基）-2-（吡咯-2-基） - 噻唑其中R 1是C 1-4烷基，C 2-4烯基，C 2-4炔基 ，2,2,2-三氟乙基，式-CH 2 COOR 2 R 2的基团是C 1-8烷基，C 2-4烯基，C 2-4炔基或苯基-C 1-2烷基）或下式的基团： - （CH 2）n A -R 3（A是氧或硫，R 3是C 1-4烷基或C 2-4链烯基，n是1,2或3），化合物的制备方法和有用的药物组合物 作为血小板聚集抑制剂，其与常规药学上可接受的载体或稀释剂混合包含作为活性成分的上述4,5-双（4-甲氧基苯基）-2-（吡咯-2-基）噻唑化合物。