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25 条记录 (耗时 0.048 秒)

    16-membered macrolide derivatives and process for producing the same
    3.
    发明授权
    16-membered macrolide derivatives and process for producing the same 失效
    16元大环内酯衍生物及其制备方法

    公开(公告)号：US5407918A

    公开(公告)日：1995-04-18

    申请号：US143125

    申请日：1993-10-29

    申请人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

    发明人： Keiichi Ajito ,  Ken-ichi Kurihara ,  Akira Shimizu ,  Shuichi Gomi ,  Nobue Kikuchi ,  Minako Araake ,  Tsuneo Ishizuka ,  Aiko Miyata ,  Osamu Hara ,  Seiji Shibahara

    IPC分类号： C07H17/08 ,  C12P19/62 ,  A61K31/70 ,  C12P19/60

    CPC分类号： C07H17/08

    摘要： 16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 represents a straight-chain alkyl group having 1 to 3 carbon atoms; R.sup.2 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.3 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.4 represents a straight-chain alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted allyl group; and R.sup.5 represents a substituted or unsubstituted, straight-chain or branched alkyl, alkenyl or aralkyl group having 1 to 10 carbon atoms; and pharmaceutically acceptable salts thereof are disclosed. These compounds show excellent and long-acting antimicrobial activities. A novel process for producing these 16-membered macrolide derivatives is further disclosed.

    摘要翻译： 由式（I）表示的16元大环内酯衍生物：其中R 1表示氢原子或COR 6基团，其中R 6表示具有1至3个碳原子的直链烷基; R2表示氢原子或COR6基团，其中R6如上所定义; R3表示氢原子或COR6基团，其中R6如上所定义; R4表示碳原子数1〜4的直链烷基或取代或未取代的烯丙基; R 5表示具有1〜10个碳原子的取代或未取代的直链或支链烷基，烯基或芳烷基; 及其药学上可接受的盐。 这些化合物显示出优异的长效抗菌活性。 进一步公开了一种制备这些16元大环内酯衍生物的新方法。

    Novel 15-membered cyclic azalide, novel 16-membered cyclic diazalide derivative, and process for producing these
    5.
    发明申请
    Novel 15-membered cyclic azalide, novel 16-membered cyclic diazalide derivative, and process for producing these 审中-公开
    新的15元环氮杂环丁烷，新的16元环二氮杂衍生物及其制备方法

    公开(公告)号：US20050209446A1

    公开(公告)日：2005-09-22

    申请号：US10504327

    申请日：2003-02-25

    申请人： Tomoaki Miura ,  Ken-ichi Kurihara ,  Takuji Yoshida ,  Keiichi Ajito

    发明人： Tomoaki Miura ,  Ken-ichi Kurihara ,  Takuji Yoshida ,  Keiichi Ajito

    IPC分类号： A61P31/04 ,  C07H17/08 ,  A61K31/7052

    CPC分类号： C07H17/08

    摘要： A compound represented by the general formula (I) or a salt thereof which has excellent antibacterial activity (R1 represents hydrogen atom or an alkylcarbonyl group, R2 represents hydrogen atom, oxygen atom, hydroxyl group, or an alkylcarbonyloxy group, for example, when R2 is hydrogen atom, R3 represents group (a) (each of R5 and R6 represents hydrogen atom or an alkyl group), R4 represents hydrogen atom or group (c) (each of R8 and R9 represents hydrogen atom or an alkylcarbonyl group), and Me represents methyl group).

    摘要翻译： 由通式（I）表示的化合物或其盐具有优异的抗菌活性（R 1表示氢原子或烷基羰基，R 2表示氢原子， 氧原子，羟基或烷基羰基氧基，例如当R 2是氢原子时，R 3表示基团（a）（R 5 R 3和R 6代表氢原子或烷基），R 4表示氢原子或基团（c）（R 8各自独立地选自氢， 和R 9表示氢原子或烷基羰基，Me表示甲基）。

    3-modified leucomycin derivatives
    6.
    发明授权
    3-modified leucomycin derivatives 失效
    3修饰的leucomycin衍生物

    公开(公告)号：US06660718B1

    公开(公告)日：2003-12-09

    申请号：US09980113

    申请日：2001-11-30

    申请人： Ken-ichi Kurihara ,  Takeshi Furuuchi ,  Takuji Yoshida ,  Tomoaki Miura ,  Keiichi Ajito

    发明人： Ken-ichi Kurihara ,  Takeshi Furuuchi ,  Takuji Yoshida ,  Tomoaki Miura ,  Keiichi Ajito

    IPC分类号： C07H1708

    CPC分类号： C07H17/08

    摘要： A compound represented by the following general formula (I) or a salt thereof: wherein R&agr; represents a C1-C10 alkyl group, a C3-C10 alkenyl group, a C7-C15 aralkyl group, a quinolinylalkyl group, a quinolinylalkenyl group, a C2-C10 alkylcarbonyl group, a C7-C15 aralkylcarbonyl group, a C4-C7 cycloalkylcarbonyl group, benzoyl group, an imidazolylcarbonyl group and the like; R1 represents hydrogen atom, a C1-C10 alkyl group, or a C2-C10 alkylcarbonyl group; and R2 represents hydrogen atom, a C1-C10 alkyl group, or a C2-C10 alkylcarbonyl group, provided that the compound wherein R&agr; represents a C2-C10 alkylcarbonyl group and both of R1 and R2 represent a C1-C10 alkyl group is excluded.

    摘要翻译： 由以下通式（I）表示的化合物或其盐：其中R表示C1-C10烷基，C3-C10烯基，C7-C15芳烷基，喹啉基烷基，喹啉基烯基 C2-C10烷基羰基，C7-C15芳烷基羰基，C4-C7环烷基羰基，苯甲酰基，咪唑基羰基等; R 1表示氢原子，C 1 -C 10烷基或C 2 -C 10烷基羰基; 并且R 2表示氢原子，C 1 -C 10烷基或C 2 -C 10烷基羰基，条件是其中R 1表示C 2 -C 10烷基羰基并且R 1和R 2均为 2>表示不包括C1-C10烷基。

    Tetrahydronaphthofuranone derivatives and process for producing the same
    7.
    发明授权
    Tetrahydronaphthofuranone derivatives and process for producing the same 失效
    四氢萘并呋喃酮衍生物及其制备方法

    公开(公告)号：US06255339B1

    公开(公告)日：2001-07-03

    申请号：US09117070

    申请日：1998-07-21

    申请人： Kenichi Kurihara ,  Rie Shinei ,  Kiyoshi Tanabe ,  Yasuo Yamamoto ,  Keiichi Ajito ,  Kaori Miyajima ,  Yuji Tabata ,  Shohei Yasuda ,  Kuniaki Tatsuta ,  Tsuneo Okonogi

    发明人： Kenichi Kurihara ,  Rie Shinei ,  Kiyoshi Tanabe ,  Yasuo Yamamoto ,  Keiichi Ajito ,  Kaori Miyajima ,  Yuji Tabata ,  Shohei Yasuda ,  Kuniaki Tatsuta ,  Tsuneo Okonogi

    IPC分类号： A61K3134

    CPC分类号： C07D307/92 ,  C07D407/12 ,  C07D407/14 ,  C07D409/12 ,  C07D417/12

    摘要： Compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as abortifacients, oral contraceptive pills, carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for endometriosis, meningioma, and myeloma, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. wherein R1 and R2 represent a hydroxyl group, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, alkoxyalkyloxy, cycloalkyloxy containig one oxygen atom, aralkyloxy, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, cycloalkylcarbonyloxy, alkoxycarbonyloxy, aryloxy carbonyloxy, aralkylcarbonyloxy, aromatic acyloxy, heteroaromatic acyloxy, saturated heterocyclic carbonyloxy, alkylsulfonyloxy, aromatic sulfonyloxy, alkylcarbamoyloxy, aromatic carbamoyloxy, alkylcarbonylamino, or aromatic acylamino, provided that R1 may further represent a hydrogen atom, alkyl, alkenyl, or alkynyl; and R3, R4, and R5 each independently represent a hydrogen atom, alkyl or alkenyl.

    摘要翻译： 公开了由下式（I）表示的化合物及其药学上可接受的盐。 所述化合物具有孕酮受体结合抑制活性，因此可用作孕酮相关疾病的治疗和预防剂。 具体地说，它们可用作流产者，口服避孕药，乳腺癌和卵巢癌的制癌剂，子宫内膜异位症的治疗剂，脑膜瘤和骨髓瘤，以及骨质疏松症和更年期障碍的治疗和预防剂。其中R1和R2表示羟基， 烷氧基，链烯氧基，炔氧基，环烷氧基，烷氧基烷氧基，含有一个氧原子的环烷氧基，芳烷氧基，烷基羰基氧基，链烯基羰基氧基，炔基羰氧基，环烷基羰基氧基，烷氧基羰基氧基，芳氧基羰基氧基，芳烷基羰基氧基，芳香酰氧基，杂芳基酰氧基，饱和杂环羰氧基，烷基磺酰氧基，芳香磺酰氧基，烷基氨基甲酰氧基， 芳族氨基甲酰氧基，烷基羰基氨基或芳族酰氨基，条件是R 1可以进一步代表氢原子，烷基，烯基或炔基; 并且R 3，R 4和R 5各自独立地表示氢原子，烷基或链烯基。

    Malonic acid monoesters and process for producing the same
    9.
    发明授权
    Malonic acid monoesters and process for producing the same 失效
    丙二酸单酯及其制备方法

    公开(公告)号：US07553989B2

    公开(公告)日：2009-06-30

    申请号：US10531382

    申请日：2003-10-17

    申请人： Takehiko Sawabe ,  Kazuhiro Aihara ,  Kunio Atsumi ,  Keiichi Ajito

    发明人： Takehiko Sawabe ,  Kazuhiro Aihara ,  Kunio Atsumi ,  Keiichi Ajito

    IPC分类号： C07C69/34

    CPC分类号： C07D317/36 ,  C07C69/38 ,  C07C69/76 ,  C07C69/78 ,  C07C69/96

    摘要： The present invention relates to a compound represented by formula (1) or a salt thereof: wherein R represents a group that is easily removable upon hydrolysis in vivo. This compound is usable in the production of prodrug-type carbapenem antibacterial agents for oral administration. The use of this compound in the process of production of the antibacterial agents can realize enhanced production efficiency and reduced production cost.

    摘要翻译： 本发明涉及由式（1）表示的化合物或其盐：其中R表示在体内水解时容易除去的基团。 该化合物可用于生产用于口服给药的前药型碳青霉烯类抗生素。 在生产抗菌剂的过程中使用该化合物可以实现提高生产效率并降低生产成本。

    Azalide and azalactam derivatives and method for producing the same
    10.
    发明授权
    Azalide and azalactam derivatives and method for producing the same 失效
    氮杂吲哚衍生物及其制备方法

    公开(公告)号：US07365174B2

    公开(公告)日：2008-04-29

    申请号：US10569063

    申请日：2004-08-20

    申请人： Tomoaki Miura ,  Kenichi Kanemoto ,  Satomi Natsume ,  Naoto Ohkura ,  Yumiko Fujihira ,  Takashi Watanabe ,  Hideki Fushimi ,  Kunio Atsumi ,  Keiichi Ajito

    发明人： Tomoaki Miura ,  Kenichi Kanemoto ,  Satomi Natsume ,  Naoto Ohkura ,  Yumiko Fujihira ,  Takashi Watanabe ,  Hideki Fushimi ,  Kunio Atsumi ,  Keiichi Ajito

    IPC分类号： C07H17/08

    CPC分类号： A61K31/7052 ,  C07H15/04 ,  C07H17/00

    摘要： Compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof, effective in the prevention and/or treatment of infections with microbes: (1) (a) wherein R1 is hydrogen or straight-chain C1-6 alkylcarbonyl; R2 is hydrogen or C1-6 alkylcarbonyl; R3 is hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkenyl, C2-6 alkenylcarbonyl, C2-6 alkynyl, or an Ar—B— group (wherein Ar is aryl or a heterocyclic group; and B is C1-6 alkyl, C1-6 alkylcarbonyl, C2-6 alkenyl, C2-6 alkenylcarbonyl, or C2-6 alkynyl); R5, R6, R7 and R8 are each hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or an Ar—B′— group (wherein B′ is C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl); X is oxygen or —NR4— (wherein R4 is hydrogen, C1-6 alkyl or C1-6 alkyl which may be substituted with Ar); and R4′ is hydrogen or a group represented by the general formula (a) (wherein R3″ and R4″ are each hydrogen or straight-chain or branched C1-6 alkylcarbonyl)

    摘要翻译： 由通式（1）表示的化合物或其药学上可接受的盐在预防和/或治疗微生物感染方面有效：（1）（a）其中R 1是氢或直链 C 1-6烷基羰基; R 2是氢或C 1-6烷基羰基; R 3是氢，C 1-6烷基，C 1-6 - 烷基羰基，C 1-6 - 烯基 ，C 2-6链烯基羰基，C 2-6炔基或Ar-B基（其中Ar为芳基或杂环基; B为C