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公开(公告)号:US4761409A
公开(公告)日:1988-08-02
申请号:US762560
申请日:1985-08-05
申请人: Hirotada Yamada , Naruhito Masai , Shinji Ueda , Takao Okuda , Masuhiro Kato , Masatomo Fukasawa , Masataka Fukumura
发明人: Hirotada Yamada , Naruhito Masai , Shinji Ueda , Takao Okuda , Masuhiro Kato , Masatomo Fukasawa , Masataka Fukumura
IPC分类号: A61K31/545 , C07D277/22 , C07D279/08 , C07D285/04 , C07D417/14 , C07D501/18 , C07D501/36
CPC分类号: C07D501/36
摘要: A cephem derivative represented by the general formula ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 represents carboxyl or esterified carboxyl, and n represents 0 or 1, or a pharmaceutically acceptable salt thereof; intermediates for the cephem derivative or salt thereof; processes for producing these compounds; and a pharmaceutical composition and method for preventing or treating bacterial infectious diseases, wherein the cephem derivative or the salt thereof is used.
摘要翻译: 由通式
表示的头孢烯衍生物,其中R1表示氢或甲基,R2表示羧基或酯化的羧基,n表示0或1,或其药学上可接受的盐; 头孢烯衍生物或其盐的中间体; 制备这些化合物的方法; 以及使用头孢衍生物或其盐的预防或治疗细菌感染性疾病的药物组合物和方法。 -
公开(公告)号:US4705784A
公开(公告)日:1987-11-10
申请号:US682283
申请日:1984-12-17
申请人: Hirotada Yamada , Naruhito Masai , Sinji Ueda , Takao Okuda , Masatomo Fukasawa , Masuhiro Kato , Masataka Fukumura
发明人: Hirotada Yamada , Naruhito Masai , Sinji Ueda , Takao Okuda , Masatomo Fukasawa , Masuhiro Kato , Masataka Fukumura
IPC分类号: A61K31/545 , A61K31/546 , A61P31/04 , C07D501/34
CPC分类号: A61K31/545
摘要: A cephem compound represent by the general formula ##STR1## wherein, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 and R.sup.3 are the same or different and each represents hydrogen or lower alkyl, R.sup.4 represents carboxyl or esterified carboxyl, and n represents 0 or 1, a salt of the cephem compound, and a process for producing the cephem compound or a salt thereof. Compounds of the above formula and salts thereof are valuable as antibacterial agents and are especially useful as oral drugs in the prevention or treatment of bacterial infectious diseases.
摘要翻译: 头孢烯化合物由通式
表示,其中R1表示氢或低级烷基,R2和R3相同或不同,各自表示氢或低级烷基,R4表示羧基或酯化羧基,n表示0或1, 头孢烯化合物的盐,以及头孢烯化合物或其盐的制备方法。 上述式的化合物及其盐作为抗菌剂是有价值的,并且特别可用作预防或治疗细菌感染性疾病的口服药物。 -
公开(公告)号:US06936713B2
公开(公告)日:2005-08-30
申请号:US10296234
申请日:2002-04-03
申请人: Naruhito Masai , Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa , István Barta , Takehiko Kawakami
发明人: Naruhito Masai , Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa , István Barta , Takehiko Kawakami
IPC分类号: C07D473/40
CPC分类号: C07D473/40 , Y02P20/55
摘要: A process for conveniently and efficiently preparing a 2,6-dihalogenopurine using an inexpensive starting material. A process for preparing a 2,6-dihalogenopurine, comprising treating a 2-amino-6-halogenopurine having a protective group at 7th position or 9th position with a diazotizating agent and a halogen source; and a process for preparing a 9-acyl-2-amino-6-halogenopurine, comprising treating a 2-amino-6-halogenopurine with an acylating agent in the presence of a base.
摘要翻译: 使用廉价起始原料方便有效地制备2,6-二卤代嘌呤的方法。 一种制备2,6-二卤代嘌呤的方法,包括用重氮化处理在第7位或第9位具有保护基的2-氨基-6-卤代嘌呤 代理和卤素源; 以及制备9-酰基-2-氨基-6-卤代嘌呤的方法,包括在碱的存在下用酰化剂处理2-氨基-6-卤代嘌呤。
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公开(公告)号:US20050090666A1
公开(公告)日:2005-04-28
申请号:US10991505
申请日:2004-11-19
申请人: Naruhito Masai , Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa , Istvan Barta , Takehiko Kawakami
发明人: Naruhito Masai , Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa , Istvan Barta , Takehiko Kawakami
IPC分类号: C07D473/40 , C07D473/00
CPC分类号: C07D473/40 , Y02P20/55
摘要: A process for conveniently and efficiently preparing a 2,6-halogenopurine using an inexpensive starting material. A process for preparing a 2,6-dihalogenopurine, comprising treating a 2-amino-6-halogenopurine having a protective group at 7th position or 9th position with a diazotizating agent and a halogen source; and a process for preparing a 9-acyl-2-amino-6-halogenopurine, comprising treating a 2-amino-6-halogenopurine with an acylating agent in the presence of a base.
摘要翻译: 使用廉价起始原料方便有效地制备2,6-卤代嘌呤的方法。 一种制备2,6-二卤代嘌呤的方法,包括用重氮化剂和卤素源处理在第7位或第9位具有保护基的2-氨基-6-卤代嘌呤; 以及制备9-酰基-2-氨基-6-卤代嘌呤的方法,包括在碱的存在下用酰化剂处理2-氨基-6-卤代嘌呤。
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公开(公告)号:US07321035B2
公开(公告)日:2008-01-22
申请号:US10991505
申请日:2004-11-19
申请人: Naruhito Masai , Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa , Istvan Barta , Takehiko Kawakami
发明人: Naruhito Masai , Taketo Hayashi , Hiroharu Kumazawa , Junichi Nishikawa , Istvan Barta , Takehiko Kawakami
IPC分类号: C07D473/40
CPC分类号: C07D473/40 , Y02P20/55
摘要: A process for conveniently and efficiently preparing a 2,6-dihalogenopurine using an inexpensive starting material. A process for preparing a 2,6-dihalogenopurine, comprising treating a 2-amino-6-halogenopurine having a protective group at 7th position or 9th position with a diazotizating agent and a halogen source; and a process for preparing a 9-acyl-2-amino-6-halogenopurine, comprising treating a 2-amino-6-halogenopurine with an acylating agent in the presence of a base.
摘要翻译: 使用廉价起始原料方便有效地制备2,6-二卤代嘌呤的方法。 一种制备2,6-二卤代嘌呤的方法,包括用重氮化处理在第7位或第9位具有保护基的2-氨基-6-卤代嘌呤 代理和卤素源; 以及制备9-酰基-2-氨基-6-卤代嘌呤的方法,包括在碱的存在下用酰化剂处理2-氨基-6-卤代嘌呤。
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6.
公开(公告)号:US5021435A
公开(公告)日:1991-06-04
申请号:US297313
申请日:1989-01-17
申请人: Naruhito Masai , Masao Enomoto , Atsuyuki Kojima , Hiroaki Masumori , Nobuyuki Hara , Youichi Hara , Shigeaki Morooka
发明人: Naruhito Masai , Masao Enomoto , Atsuyuki Kojima , Hiroaki Masumori , Nobuyuki Hara , Youichi Hara , Shigeaki Morooka
IPC分类号: A61K31/44 , A61P1/04 , C07D417/04
CPC分类号: C07D417/04
摘要: A 2-pyridyl-thiazolidin-4-one derivative represented by the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each a hydrogen atom, an C.sub.1 -C.sub.20 alkyl group, an C.sub.2 -C.sub.20 alkenyl group, an C.sub.2 -C.sub.20 alkynyl group, an aryl group, a C.sub.3 -C.sub.8 cycloalkyl group or an aralkyl group which may have a substituent, R.sub.3 is a hydrogen atom, an C.sub.1 -C.sub.20 alkyl group, an C.sub.2 -C.sub.20 alkenyl group, an C.sub.2 -C.sub.20 alkynyl group, a C.sub.3 -C.sub.8 cycloalkyl group or an aralkyl group which may have a substituent, P is a pyridyl group or its N-substituted pyridinium salt which may have a substituent, said substituent being selected from the group consisting of halogen atom, cyano group, hydroxy group, amino group, lower alkyl group, lower alkoxy group, lower alkylamino group, halogenated lower alkyl group, acyl group, acyloxy group, acylthio group, acylamino group, carboxyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkyl substituted carbamoyl group, heterocyclic group, and lower cycloalkyl group, and n represents an integer of 0, 1 or 2, or a pharmaceutically acceptable salts thereof and an anti-ulcer agent which contains, as an effective ingredient, said 2-pyridyl-thiazolidine-4-one derivative or a pharmaceutically acceptable salt thereof.
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