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    16-membered macrolide derivatives and process for producing the same
    2.
    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
    6.
    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
    7.
    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。

    &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity
    8.
    发明授权
    &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity 失效
    具有整合素α2β3拮抗活性的ω-氨基-α-羟基羧酸衍生物

    公开(公告)号：US06750219B1

    公开(公告)日：2004-06-15

    申请号：US10048914

    申请日：2002-02-05

    申请人： Keiichi Ajito ,  Naokazu Yahata ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Kazuyuki Fujishima ,  Shuichi Gomi ,  Shokichi Ouchi

    发明人： Keiichi Ajito ,  Naokazu Yahata ,  Minoru Ishikawa ,  Dai Kubota ,  Shoichi Murakami ,  Mikio Yamamoto ,  Kazuyuki Fujishima ,  Shuichi Gomi ,  Shokichi Ouchi

    IPC分类号： C07D40304

    CPC分类号： C07D239/42

    摘要： An objective of the present invention is to provide highly water-soluble compounds having integrin &agr;v&bgr;3 antagonistic activity. The compounds according to the present invention are compounds represented by formula (I) and pharmaceutically acceptable salts or solvates thereof: wherein A represents a two nitrogen atom-containing optionally substituted saturated or unsaturated five- to seven-membered heterocyclic group, which is optionally condensed with another carbocyclic ring or heterocyclic ring to form a bicyclic group, or —C(—NR1R2)(═NR3) wherein R1, R2, and R3 represent hydrogen, alkyl or the like; D represents a bond, >NR4, wherein R4 represents hydrogen or optionally substituted alkyl, —O—, or —S—; X and Z represent either CH or N; R7 and R8 represent C1-6 alkyl, halogen, oxygen or the like; Q represents >C═O, >CHR13 or >CHOR13 wherein R13 represents hydrogen or alkyl; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene having 1 to 3 carbon atoms; R10 and R11 represent hydrogen, alkyl or the like; m is an integer of 0 to 5; n is an integer of 0 to 4; and p and q are an integer of 1 to 3.

    摘要翻译： 本发明的目的是提供具有整合素α2拮抗活性的高水溶性化合物。 根据本发明的化合物是由式（I）表示的化合物及其药学上可接受的盐或溶剂化物：其中A表示两个含有氮原子的任选取代的饱和或不饱和的五至七元杂环基，其任选地稠合 与另一个碳环或杂环形成双环基团，或-C（-NR 1 R 2）（= NR 3）（其中R 1，R 2和R 3） 代表氢，烷基等; D表示键，NR 4，其中R 4表示氢或任选取代的烷基，-O-或-S-; X和Z表示CH或N; R 7和R 8表示C 1-6烷基，卤素，氧等; Q表示C = O，> CHR 13或CHOR 13，其中R 13表示氢或烷基; R 9表示氢，烷基等; J表示碳原子数1〜3的键或亚烷基。 R 10和R 11代表氢，烷基等; m为0〜5的整数。 n为0〜4的整数。 p和q为1〜3的整数。

    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists
    9.
    发明授权
    Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists 失效
    苯基哌嗪衍生物作为整合素α2β拮抗剂

    公开(公告)号：US06451800B1

    公开(公告)日：2002-09-17

    申请号：US09601176

    申请日：2000-07-28

    申请人： Keiichi Ajito ,  Shoichi Murakami ,  Minoru Ishikawa ,  Mikio Yamamoto ,  Dai Kubota ,  Shuichi Gomi ,  Mitsugu Hachisu ,  Kiyoaki Katano

    发明人： Keiichi Ajito ,  Shoichi Murakami ,  Minoru Ishikawa ,  Mikio Yamamoto ,  Dai Kubota ,  Shuichi Gomi ,  Mitsugu Hachisu ,  Kiyoaki Katano

    IPC分类号： A61K31497

    CPC分类号： C07D239/42 ,  C07D235/30 ,  C07D239/14

    摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and therapeutic agents for treating integrin &agr;v&bgr;3-mediated diseases and for inhibiting platelet aggregation. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein A represents a five- to seven-membered heterocyclic ring containing two nitrogen atoms or the like; X and Z represent CH or a nitrogen atom; R4 and R5 represent alkyl, halogen or the like; Q represents >C=O, >CH2 or the like; R6 represents H, alkyl, aralkyl or the like; R7 represents H, alkynyl or the like; R8 represents H, substituted amino or the like; R9 represents H or alkyl; m is 0 to 5; n is 0 to 4; p is 2 or 3; and q is 0 or 1.

    摘要翻译： 本发明的目的是提供具有整合素α2拮抗活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗整合素α1β介导的疾病和抑制血小板聚集的治疗剂。 根据本发明的衍生物是由式（I）表示的化合物或其药学上可接受的盐或溶剂化物：其中A表示含有两个氮原子等的5-至7-元杂环; X和Z表示CH或氮原子; R4和R5代表烷基，卤素等; Q表示> C = O，> CH2等; R6表示H，烷基，芳烷基等; R 7表示H，炔基等; R8表示H，取代的氨基等; R9代表H或烷基; m为0〜5; n为0〜4; p为2或3; q为0或1。

    Malonic acid monoesters and process for producing the same
    10.
    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。