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1. 发明授权

US5219736A Process for producing 3-deacylated derivative of 16-membered macrolide antibiotic 失效
标题翻译：生产16-羟基磷灰石抗生素的3-脱乙酰衍生物的方法
公开(公告)号：US5219736A
公开(公告)日：1993-06-15
申请号：US925038
申请日：1992-08-05
申请人： Akira Shimizu , Shuichi Gomi , Keiichi Ajito , Takashi Yaguchi , Eriko Tanaka , Osamu Hara , Shinji Miyadoh
发明人： Akira Shimizu , Shuichi Gomi , Keiichi Ajito , Takashi Yaguchi , Eriko Tanaka , Osamu Hara , Shinji Miyadoh
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C12N1/14 , C12P19/62 , C12R1/645
CPC分类号： C07H17/08 , C12P19/62
摘要： A method of producing a 3-deacylated derivative of a 16-membered macrolide antibiotic using a microorganism belonging to the genus Phialophora or Preussia which comprises incubating said microorganism with a 16-membered macrolide antibiotic in a medium containing nutritional sources commonly used for incubating microorganisms, isolating a 3-deacylated derivative from the incubation medium, a microorganism to be used for the above method and a novel macrolide antibiotic.

2. 发明授权

US5407918A 16-membered macrolide derivatives and process for producing the same 失效
标题翻译： 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。

3. 发明授权

US5519122A 16-membered macrolide derivatives and process for producing the same 失效
公开(公告)号：US5519122A
公开(公告)日：1996-05-21
申请号：US359825
申请日：1994-12-20
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 , B01D53/047
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.

4. 发明授权

US5602106A 16-membered macrolide derivatives 失效
标题翻译： 16元大环内酯衍生物
公开(公告)号：US5602106A
公开(公告)日：1997-02-11
申请号：US271996
申请日：1994-07-08
申请人： Keiichi Ajito , Osamu Hara , Ken-ichi Kurihara , Nobue Kikuchi , Minako Araake , Akira Shimizu , Tsuneo Okonogi , Shigeharu Inouye , Seiji Shibahara
发明人： Keiichi Ajito , Osamu Hara , Ken-ichi Kurihara , Nobue Kikuchi , Minako Araake , Akira Shimizu , Tsuneo Okonogi , Shigeharu Inouye , Seiji Shibahara
IPC分类号： C07H17/08 , A61K31/70
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 substituent group which protects a hydroxyl group; R.sup.2 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.3 represents a hydrogen atom or a straight-chain aliphatic acyl group having 2 to 4 carbon atoms; and R.sup.4 represents a hydrogen atom or a straight-chain aliphatic or aromatic acyl group having 1 to 10 carbon atoms;or a pharmaceutically acceptable salt thereof are disclosed.A novel process for producing these 16-membered macrolide derivatives is also disclosed.
摘要翻译：由式（I）表示的16元大环内酯衍生物：其中R 1表示氢原子或保护羟基的取代基; R2表示氢原子或保护羟基的取代基; R3表示氢原子或碳原子数2〜4的直链脂肪族酰基， R 4表示氢原子或碳原子数1〜10的直链脂肪族或芳香族酰基，或其药学上可接受的盐。还公开了一种制备这些16元大环内酯衍生物的新方法。

5. 发明授权

US06750219B1 &OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity 失效
标题翻译：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。

6. 发明授权

US06451800B1 Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists 失效
标题翻译：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。

7. 发明授权

US07553989B2 Malonic acid monoesters and process for producing the same 失效
标题翻译：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。

8. 发明授权

US07365174B2 Azalide and azalactam derivatives and method for producing the same 失效
标题翻译：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

9. 发明申请

US20070042974A1 Nozel azalide and azalactam derivatives and method for producing the same 失效
标题翻译：诺贝尔氮杂和吖内酰胺衍生物及其制备方法
公开(公告)号：US20070042974A1
公开(公告)日：2007-02-22
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： A61K31/7052 , C07H17/08
CPC分类号： A61K31/7052 , C07H15/04 , C07H17/00
摘要： A compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, which is useful for a prophylactic and/or therapeutic treatment of a microbial infectious disease. [R1 is hydrogen atom, or a linear C1-6 alkylcarbonyl group; R2 is hydrogen atom, or a C1-6 alkylcarbonyl group; R3 is hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C1-6 alkenyl group, a C2-6 alkenylcarbonyl group, a C2-6 alkynyl group, or an Ar—B— group (Ar represents an aryl group, or a heterocyclic group, and B is a C1-6 alkyl group, a C1-6 alkylcarbonyl group, a C2-6 alkenyl group, a C2-6 alkenylcarbonyl group, or a C2-6 alkynyl group); R5, R6, R7, and R8 represent hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or an Ar—B′— group (B′ is a C1-6 alkyl group, a C2-6 alkenyl group, or a C2-6 alkynyl group); X is oxygen atom, or an —NR4— group (R4 is hydrogen atom, a C1-6 alkyl group, or a C1-6 alkyl group which may be substituted with an Ar group); and R4′ is hydrogen atom, or a group represented by the aforementioned formula (a) (R3″ and R4″ represent hydrogen atom, or a linear or branched C1-6 alkylcarbonyl group)]
摘要翻译：由以下通式（1）表示的化合物或其药学上可接受的盐，其可用于预防和/或治疗微生物感染性疾病。 R 1是氢原子或直链C 1-6烷基羰基; R 2是氢原子或C 1-6烷基羰基; R 3是氢原子，C 1-6烷基，C 1-6烷基羰基，C 1-6烯基，C 2-6烯基羰基，C 2-6炔基或 Ar-B-基（Ar表示芳基或杂环基，B为C1-6烷基，C1-6烷基羰基，C2-6烯基，C2-6链烯基羰基或 C 2-6炔基）; R 5，R 6，R 7和R 8表示氢原子，C 1-6烷基，C2-6烯基，C2-6炔基或Ar-B'-基（B'是C1-6烷基，C2-6链烯基或C2-6炔基）; X是氧原子或-NR 4 - 基团（R 4）是氢原子，C 1-6烷基或可以是C 1-6烷基的C 1-6烷基被Ar基团取代）; 和R 4'是氢原子，或由上述式（a）表示的基团（R 3'和R 4“ 代表氢原子，或直链或支链C 1-6烷基羰基）]

10. 发明申请

US20050209446A1 Novel 15-membered cyclic azalide, novel 16-membered cyclic diazalide derivative, and process for producing these 审中-公开
标题翻译：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）。

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