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1. 发明申请

US20050272950A1 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：US20050272950A1
公开(公告)日：2005-12-08
申请号：US10531382
申请日：2003-10-17
申请人： Takehiko Sawabe , Kazuhiro ihara , Kunio Atsumi , Keiichi Ajito
发明人： Takehiko Sawabe , Kazuhiro ihara , Kunio Atsumi , Keiichi Ajito
IPC分类号： C07C69/38 , C07C69/76 , C07C69/78 , C07C69/96 , C07D205/08 , C07D317/36 , C07C69/34 , C07C69/52
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。

2. 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。

3. 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

4. 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）]

5. 发明授权

US07662841B2 Imidazothiazole derivatives and process for producing the same 失效
标题翻译：咪唑并噻唑衍生物及其制备方法
公开(公告)号：US07662841B2
公开(公告)日：2010-02-16
申请号：US11795522
申请日：2006-01-19
申请人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
发明人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
IPC分类号： A61K31/429 , C07D235/02
CPC分类号： C07D513/04
摘要： The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.
摘要翻译：本发明涉及式（I）化合物及其制备方法。在式（I）中，X表示卤素原子，R1表示-COR2基团，其中R2表示基团OM或C1-12烷氧基，其中M表示氢原子，碱金属，碱土金属或季铵。使用该化合物作为合成中间体可以以低成本实现以高效安全的方式生产具有强效抗菌活性的碳青霉烯衍生物。

6. 发明申请

US20080114164A1 Imidazothiazole Derivatives and Process for Producing the Same 失效
标题翻译：咪唑噻唑衍生物及其制备方法
公开(公告)号：US20080114164A1
公开(公告)日：2008-05-15
申请号：US11795522
申请日：2006-01-19
申请人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
发明人： Eiki Shitara , Kunio Atsumi , Keiichi Ajito , Shinya Ikeda , Tadashi Katoh , Munenori Inoue , Mari Nakatani
IPC分类号： C07D513/02
CPC分类号： C07D513/04
摘要： The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and R1 represents group —COR2 wherein R2 represents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost.
摘要翻译：本发明涉及式（I）化合物及其制备方法。在式（I）中，X表示卤素原子，R 1表示基团-COR 2，其中R 2表示基团OM或C1- 12烷氧基，其中M表示氢原子，碱金属，碱土金属或季铵。使用该化合物作为合成中间体可以以低成本实现以高效安全的方式生产具有强效抗菌活性的碳青霉烯衍生物。

7. 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）。

8. 发明授权

US06420558B1 Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists 有权
标题翻译：氨基哌啶衍生物作为整联蛋白α2β拮抗剂
公开(公告)号：US06420558B1
公开(公告)日：2002-07-16
申请号：US09673017
申请日：2000-10-10
申请人： Minoru Ishikawa , Shoichi Murakami , Mikio Yamamoto , Dai Kubota , Mitsugu Hachisu , Kiyoaki Katano , Keiichi Ajito
发明人： Minoru Ishikawa , Shoichi Murakami , Mikio Yamamoto , Dai Kubota , Mitsugu Hachisu , Kiyoaki Katano , Keiichi Ajito
IPC分类号： C07D23902
CPC分类号： C07D235/14 , C07D401/12
摘要： An objective of the present invention is to provide compounds having integrin &agr;v&bgr;3 antagonistic activity, cell adhesion inhibitory activity, GP IIb/IIIa antagonistic activity, and/or human platelet aggregation inhibitory activity, and, therapeutic agents for treating cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases and the like 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 group containing two nitrogen atoms or the like; D represents >NH2, >CH2 or the like; X and Z represent CH or a nitrogen atom; R7 and R8 represent alkyl, halogen or the like; Q represents >C═O, >CH2 or the like; R9 represents H, alkyl, aralkyl or the like; R10 represents H, alkynyl or the like; R11 represents H, substituted amino or the like; R12 represents H or alkyl; m is 0 to 5; n is 0 to 4; p and q are each 1 to 3; and r is 0 or 1.
摘要翻译：本发明的目的是提供具有整合素α噬菌体拮抗活性，细胞粘附抑制活性，GP IIb / IIIa拮抗活性和/或人血小板聚集抑制活性的化合物，以及用于治疗心血管疾病，血管发生相关疾病脑血管疾病等，并用于抑制血小板聚集。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合物：其中A表示含有两个氮原子等的5-至7-元杂环基; D表示> NH 2，> CH 2等; X和Z表示CH或氮原子; R 7和R 8表示烷基，卤素等; Q表示> C = O，> CH2等; R 9表示H，烷基，芳烷基等; R 10表示H，炔基等; R11表示H，取代的氨基等; R 12表示H或烷基; m为0〜5; n为0〜4; p和q各自为1至3; r为0或1。

9. 发明授权

US08299035B2 10a-azalide compound having 4-membered ring structure 失效
标题翻译：具有4元环结构的10a-氮杂化合物
公开(公告)号：US08299035B2
公开(公告)日：2012-10-30
申请号：US12992335
申请日：2009-05-15
申请人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Satoshi Yoshida , Kou Kumura , Keiichi Ajito
发明人： Tomohiro Sugimoto , Kanako Yamamoto , Jun Kurosaka , Naoki Sasamoto , Masato Kashimura , Tomoaki Miura , Kenichi Kanemoto , Satoshi Yoshida , Kou Kumura , Keiichi Ajito
IPC分类号： A61K31/70 , C07H17/08
CPC分类号： C07H17/00
摘要： A 10a-azalide compound having a 4-membered ring structure crosslinked at the 10a- and 12-positions, which is represented by the formula (I), and is effective on even Haemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneunococci and streptococci).
摘要翻译：具有由式（I）表示的在10a-和12位交联的4元环结构的10a-氮杂化合物化合物，并且对偶联流感嗜血杆菌或抗红霉素抗性细菌（例如耐药性球芽孢杆菌和链球菌）。

10. 发明申请

US20050059669A1 M-substituted benzoic acid derivatives having integrin alpha v beta 3 antagonistic activity 审中-公开
标题翻译：具有整合素αvβ3拮抗活性的M取代苯甲酸衍生物
公开(公告)号：US20050059669A1
公开(公告)日：2005-03-17
申请号：US10944712
申请日：2004-09-21
申请人： Keiichi Ajito , Minoru Ishikawa , Dai Kubota , Shoichi Murakami , Mikio Yamamoto , Naokazu Yahata , Kazuyuki Fujishima , Makoto Oyama
发明人： Keiichi Ajito , Minoru Ishikawa , Dai Kubota , Shoichi Murakami , Mikio Yamamoto , Naokazu Yahata , Kazuyuki Fujishima , Makoto Oyama
IPC分类号： C07C229/54 , C07C229/60 , C07D239/14 , C07D239/42 , C07D401/12 , A61K31/496 , A61K31/454 , C07D43/02
CPC分类号： C04B35/632 , C07C229/54 , C07C229/60 , C07D239/14 , C07D239/42 , C07D401/12
摘要： An object of the present invention is to provide m-substituted benzoic acid derivatives having integrin αvβ3 antagonistic activity. The derivatives according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts or solvates thereof, which are useful for the treatment or prevention of cardiovascular diseases, angiogenesis-related diseases, cerebrovascular diseases, cancers and metastasis thereof, immunological diseases, osteopathy and other diseases: wherein A represents an optionally substituted heterocyclic group containing two nitrogen atoms, a bicylic group or the like; D represents a bond, >NR4, >CR5R6, O, S, or —NR4—CR5R6—; X represents CH or N; R7 and R8 represent hydroxyl, alkyl or the like; Q represents >C═O or the like; R9 represents hydrogen, alkyl or the like; J represents a bond or alkylene; R10 represents optionally substituted hydroxyl, amino or the like; R11 represents hydrogen, alkyl or the like; m is 0 to 5; n is 0 to 4; and p and q are each 0 to 3.
摘要翻译：本发明的目的是提供具有整合素α噬菌体拮抗活性的m取代苯甲酸衍生物。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，其可用于治疗或预防心血管疾病，血管生成相关疾病，脑血管疾病，癌症及其转移，免疫疾病，骨病和其他疾病：其中A表示任选取代的含有两个氮原子的杂环基团，二等基团等; D表示键，NR 4，CR 5 R 6，O，S或-NR 4 -CR 5 R 6 - 。 X表示CH或N; R 7和R 8代表羟基，烷基等; Q表示> C = O等; R 9表示氢，烷基等; J表示键或亚烷基; R 10表示任选取代的羟基，氨基等; R 11表示氢，烷基等; m为0〜5; n为0〜4; p和q各自为0〜3。

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