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1. 发明授权

US06218550B1 Intermediates useful for the manufacture of carbapenem and a stereoselective manufacturing method therefor 失效
标题翻译：可用于制造碳青霉烯类的中间体及其立体选择性制造方法
公开(公告)号：US06218550B1
公开(公告)日：2001-04-17
申请号：US09423825
申请日：1999-11-12
申请人： Takaaki Suzuki , Isao Sugiyama , Manabu Sasho , Nobuaki Sato , Atsushi Kamada , Kazuhide Ashizawa
发明人： Takaaki Suzuki , Isao Sugiyama , Manabu Sasho , Nobuaki Sato , Atsushi Kamada , Kazuhide Ashizawa
IPC分类号： C07D20748
CPC分类号： C07D477/20 , C07D207/12 , C07D263/22 , C07D413/06 , Y02P20/55
摘要： The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate. A method for manufacturing which comprises the step of reacting a compound of the formula (I): (wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II): (wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).
摘要翻译：本发明提供了制备（2S，4S）-2 - [[（R） - 羟基 - （3R） - 环胺-3-基]甲基]吡咯烷-4-硫醇或其盐的高效立体选择性方法，可用作制备碳青霉烯类的中间体，并且还提供中间体.1。一种制备方法，其包括使式（I）的化合物（其中，R 1为低级烷基磺酰基，任选取代的芳基磺酰基或烷基甲硅烷基; R2为氨基的保护基）与式（II）化合物反应:(其中，R3为取代或未取代的低级烷基或芳基; X为氧原子或硫原子 Y为叠氮基或硝基; m为2〜5的整数）。

2. 发明授权

US06372914B1 Intermediates useful for the manufacture of carbapenem and a stereoselective manufacturing method therefor 失效
标题翻译：可用于制造碳青霉烯类的中间体及其立体选择性制造方法
公开(公告)号：US06372914B1
公开(公告)日：2002-04-16
申请号：US09705183
申请日：2000-11-02
申请人： Takaaki Suzuki , Isao Sugiyama , Manabu Sasho , Nobuaki Sato , Atsushi Kamada , Kazuhide Ashizawa
发明人： Takaaki Suzuki , Isao Sugiyama , Manabu Sasho , Nobuaki Sato , Atsushi Kamada , Kazuhide Ashizawa
IPC分类号： C07D26318
CPC分类号： C07D477/20 , C07D207/12 , C07D263/22 , C07D413/06 , Y02P20/55
摘要： The present invention provides an efficient stereoselective method for manufacturing (2S,4S)-2-[[(R)-hydroxy-(3R)-cyclic amine-3-yl]methyl]pyrrolidine-4-thiol or a salt thereof which is useful as an intermediate for the manufacture of carbapenem and also provides the intermediate. A method for manufacturing which comprises the step of reacting a compound of the formula (I): (wherein, R1 is a lower alkylsulfonyl group, an optionally substituted arylsulfonyl group or an alkylsilyl group; and R2 is a protecting group for an amino group) with a compound of the formula (II): (wherein, R3 is a substituted or unsubstituted lower alkyl group or aryl group; X is an oxygen atom or a sulfur atom; Y is an azide group or a nitro group; and m is an integer of 2 to 5).
摘要翻译：本发明提供了制备（2S，4S）-2 - [[（R） - 羟基 - （3R） - 环胺-3-基]甲基]吡咯烷-4-硫醇或其盐的高效立体选择性方法，可用作制备碳青霉烯类的中间体，并且还提供中间体.1。一种制备方法，其包括使式（I）的化合物（其中，R 1为低级烷基磺酰基，任选取代的芳基磺酰基或烷基甲硅烷基; R2为氨基的保护基）与式（II）化合物反应:(其中，R3为取代或未取代的低级烷基或芳基; X为氧原子或硫原子 Y为叠氮基或硝基; m为2〜5的整数）。

3. 发明授权

US6037341A Carbapenem derivatives 失效
标题翻译：卡巴培南衍生物
公开(公告)号：US6037341A
公开(公告)日：2000-03-14
申请号：US765387
申请日：1996-12-18
申请人： Nobuaki Sato , Manabu Sasho , Atsushi Kamata , Takaaki Suzuki , Isao Sugiyama , Kanemasa Katsu , Takeshi Suzuki
发明人： Nobuaki Sato , Manabu Sasho , Atsushi Kamata , Takaaki Suzuki , Isao Sugiyama , Kanemasa Katsu , Takeshi Suzuki
IPC分类号： C07D477/00 , A61K31/397 , A61K31/40 , A61K31/445 , A61P31/04 , C07D477/20 , C07D7/18
CPC分类号： C07D477/20 , Y02P20/55
摘要： Compounds having potent antimicrobial effects over Gram-positive bacteria and Gram-negative bacteria, a high stability to .beta.-lactamases and DHP-I and a high safety for the human body and a process for producing the same. Carbapenem compounds represented by the following general formula (I) or salts thereof: ##STR1## wherein the ring A represents a 3- to 7-membered non-aromatic ring containing at least one nitrogen atom and optionally having a substituent other than R.sup.6 ; R.sup.1 represents hydrogen or methyl; R.sup.2 and R.sup.5 are the same or different and each represents hydrogen or a protecting group of the hydroxyl group; R.sup.3 represents hydrogen or a protecting group of the carboxyl group; R.sup.4 represents hydrogen, lower alkyl or a protecting group of the amino group; R.sup.6 represents: (1) hydrogen, (2) lower alkyl, optionally substituted by an optionally protected hydroxy, carbamoyl, formimidoyl, acetimidoyl or ##STR2## wherein R.sup.7 and R.sup.8 are the same or different and each represents hydrogen, lower alkyl, or a protecting group of the amino group), or (3) a protecting group of the amino group or a protecting group of the imino group; and m is 0 or 1. These compounds have antimicrobial effects and are useful as a drug.
摘要翻译： PCT No.PCT / JP95 / 01233 Sec。 371日期：1996年12月18日 102（e）日期1996年12月18日PCT提交1995年6月29日PCT公布。出版物WO96 / 01261 日期1996年1月18日具有对革兰氏阳性菌和革兰氏阴性菌具有强效抗菌作用的化合物，对β-内酰胺酶和DHP-1的高稳定性和对人体的高安全性及其制备方法。由以下通式（I）表示的碳青霉烯化合物或其盐：其中环A表示含有至少一个氮原子且任选具有除R6以外的取代基的3-至7-元非芳族环; R1代表氢或甲基; R2和R5相同或不同，各自表示氢或羟基的保护基; R3表示氢或羧基的保护基; R4表示氢，低级烷基或氨基的保护基; R 6表示：（1）氢，（2）任选被任选保护的羟基，氨基甲酰基，亚氨基，亚氨代乙酰基取代的低级烷基，或其中R 7和R 8相同或不同，各自表示氢，低级烷基或保护基氨基），或（3）氨基的保护基或亚氨基的保护基; 并且m为0或1.这些化合物具有抗微生物作用并且可用作药物。

4. 发明授权

US07803949B2 Process for preparation of water-soluble azole prodrugs 有权
标题翻译：制备水溶性唑前体药物的方法
公开(公告)号：US07803949B2
公开(公告)日：2010-09-28
申请号：US12097244
申请日：2006-12-20
申请人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
发明人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
IPC分类号： C07F9/06
CPC分类号： C07F9/65583
摘要： An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
摘要翻译：本发明的目的是提供一种适于工业化有效的脱保护反应而不使用有毒溶剂的方法，以及提供一种制备水溶性唑类药物的方法等。。本发明提供由式（I）表示的盐的制备方法。（其中X表示在苯基的第4位或第5位键合的氟原子），包括以下步骤：（a）进行式（II）表示的化合物的脱保护反应; （其中X表示在苯基的4位或5位键合的氟原子）在碳阳离子清除剂存在下进行。

5. 发明申请

US20090192316A1 PROCESS FOR PREPARATION OF WATER-SOLUBLE AZOLE PRODRUGS 有权
标题翻译：水溶性AZOLE PRODRUGS的制备方法
公开(公告)号：US20090192316A1
公开(公告)日：2009-07-30
申请号：US12097244
申请日：2006-12-20
申请人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
发明人： Manabu Sasho , Keizo Sato , Jun Niijima , Mamoru Miyazawa , Shigeto Negi , Atsushi Kamada
IPC分类号： C07F9/6539
CPC分类号： C07F9/65583
摘要： An object of the present invention is to provide a process, or the like, suitable for the industrialization of effective deprotection reaction without using a toxic solvent as well as to provide a process, or the like, for preparing a water-soluble azole prodrug effectively. The present invention provides a process for preparing a salt represented by Formula (I); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) comprising the steps of: (a) carrying out a deprotection reaction of a compound represented by Formula (II); (wherein X represents a fluorine atom bonded at position 4 or position 5 of a phenyl group) in the presence of a carbocation scavenger.
摘要翻译：本发明的目的是提供一种适于工业化有效的脱保护反应而不使用有毒溶剂的方法，以及提供一种制备水溶性唑类药物的方法等。。本发明提供由式（I）表示的盐的制备方法。（其中X表示在苯基的第4位或第5位键合的氟原子），包括以下步骤：（a）进行式（II）表示的化合物的脱保护反应; （其中X表示在苯基的4位或5位键合的氟原子）在碳阳离子清除剂存在下进行。

6. 发明授权

US5151417A 3-substituted vinyl cephalosporin derivatives 失效
标题翻译： 3-取代的乙烯基哌啶衍生物
公开(公告)号：US5151417A
公开(公告)日：1992-09-29
申请号：US550365
申请日：1990-07-10
申请人： Manabu Sasho , Hiroshi Yamauchi , Motosuke Yamanaka , Takaharu Nakamura , Kanemasa Katsu , Isao Sugiyama , Yuuki Komatu , Shigeto Negi
发明人： Manabu Sasho , Hiroshi Yamauchi , Motosuke Yamanaka , Takaharu Nakamura , Kanemasa Katsu , Isao Sugiyama , Yuuki Komatu , Shigeto Negi
IPC分类号： A61K31/545 , C07D20060101 , C07D501/00 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/56
CPC分类号： C07D501/00 , Y02P20/55
摘要： 3-Substituted vinyl cephalosporin derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a hydroxyl or lower alkoxyl group, X represents a nitrogen atom or a group represented by the formula --CH.dbd., R.sup.2 represents a carboxyl group or a carboxyl group protected with a protecting group, and R.sup.3 is as defined herein, and pharmaceutically acceptable salts thereof are potent antibacterial agents. Processes for their preparation, intermediates in such processes, and antibacterial compositions containing them as active ingredients are also described.

7. 发明授权

US5128465A Process for the preparation of cephem derivatives and intermediates therefor 失效
标题翻译：头孢衍生物及其中间体的制备方法
公开(公告)号：US5128465A
公开(公告)日：1992-07-07
申请号：US468319
申请日：1990-01-22
申请人： Takashi Kamiya , Toshihiko Naito , Yuuki Komatu , Yasunobu Kai , Takaharu Nakamura , Manabu Sasho , Shigeto Negi , Isao Sugiyama , Kanemasa Katsu , Hiroshi Yamauchi
发明人： Takashi Kamiya , Toshihiko Naito , Yuuki Komatu , Yasunobu Kai , Takaharu Nakamura , Manabu Sasho , Shigeto Negi , Isao Sugiyama , Kanemasa Katsu , Hiroshi Yamauchi
IPC分类号： C07D498/04 , C07C237/06 , C07D498/08 , C07D501/00 , C07D501/18 , C07D501/24 , C07D501/46 , C07D501/56 , C07D519/00
CPC分类号： C07D498/08 , C07C237/06 , C07D501/00 , Y02P20/55
摘要： A cephem derivative represented by the following formula: ##STR1## wherein R.sub.1 means a fluorine-substituted lower alkyl and A.sub.1 denotes a cyclic or acyclic ammonio group, or a non-toxic salt thereof, is prepared by reacting a compound represented by the following formula: ##STR2## wherein A.sub.1 has the same meaning as defined above, with another compound represented by the following formula: ##STR3## wherein R.sub.1 has the same meaning as defined above, and if necessary, removing the protecting groups.
摘要翻译：由下式表示的头孢烯衍生物：其中R1表示氟取代的低级烷基，A1表示环状或无环氨基，或其无毒盐，通过使下式表示的化合物其中A 1具有与上述定义相同的含义，另外由下式表示的化合物：其中R 1具有与上述相同的含义，如有必要，除去保护基。

8. 发明授权

US06642377B1 Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates 失效
标题翻译：碱性抗生素无机酸加成盐和草酸盐中间体的制备方法
公开(公告)号：US06642377B1
公开(公告)日：2003-11-04
申请号：US10030909
申请日：2002-01-14
申请人： Akio Kayano , Hiroyuki Chiba , Taiju Nakamura , Shin Sakurai , Hiroyuki Ishizuka , Hiroyuki Saito , Yuuki Komatsu , Manabu Sasho , Nobuaki Sato , Shigeto Negi
发明人： Akio Kayano , Hiroyuki Chiba , Taiju Nakamura , Shin Sakurai , Hiroyuki Ishizuka , Hiroyuki Saito , Yuuki Komatsu , Manabu Sasho , Nobuaki Sato , Shigeto Negi
IPC分类号： C07D47720
CPC分类号： C07D477/20 , C07D477/02 , C07D477/08 , Y02P20/55
摘要： A production process which comprises subjecting a basic antibiotic.oxalate (II) to salt-exchange with an alkali earth metal salt (III) of an inorganic acid: wherein the ring A means the basic antibiotic; R10 means a protected functional group used in organic synthesis; Ak—E means the alkali earth metal; and B means the inorganic acid, respectively.
摘要翻译：一种制备方法，其包括使碱性抗生素 - 草酸盐（II）与无机酸的碱土金属盐（III）进行盐交换：其中环A表示碱性抗生素; R 10表示有机合成中使用的被保护的官能团; Ak-E表示碱土金属; B分别表示无机酸。

9. 发明申请

US20080214564A1 MACROLIDE COMPOUND IN SOLID FORM, PROCESS FOR PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 失效
标题翻译：固体形式的MACROLIDE化合物，其制备方法和含有该化合物的药物组合物
公开(公告)号：US20080214564A1
公开(公告)日：2008-09-04
申请号：US12021184
申请日：2008-01-28
申请人： Hiroshi ISHIHARA , Manabu Sasho , Keizo Sato , Takashi Kamahara , Masashi Yoshida
发明人： Hiroshi ISHIHARA , Manabu Sasho , Keizo Sato , Takashi Kamahara , Masashi Yoshida
IPC分类号： A61K31/497 , C07D405/12
CPC分类号： C07D407/06
摘要： The present invention provides the compound of formula (I) in a solid form which, as a bulk medicament for pharmaceutical manufacture, is uniform, has a high purity, and is easy to work with. The invention further provides a process for preparing this compound, and pharmaceutical compositions containing the same. A solid form of (8E,12E,14E)-7-{(4-cycloheptylpiperazin-1-yl)carbonyl}oxy-3,6,16,21-tetrahydroxy-6,10,12,16,20-pentamethyl-18,19-epoxytricosa-8,12,14-trien-11-olide which has uniform specifications and is easy to work with was developed.
摘要翻译：本发明提供了固体形式的式（I）化合物，其作为药物制造的大量药物是均匀的，具有高纯度，并且易于加工。本发明还提供了制备该化合物的方法和含有该化合物的药物组合物。（8E，12E，14E）-7 - {（4-环庚基哌嗪-1-基）羰基}氧-3,6,16,21-四羟基-6,10,12,16,20-五甲基 - 开发了具有统一规格并且易于使用的18,19-环氧树脂-8,12,14-三烯-11-硼化物。

10. 发明授权

US07858809B2 Process for production of pyrazole-fused ring derivatives 失效
标题翻译：吡唑稠环衍生物的制备方法
公开(公告)号：US07858809B2
公开(公告)日：2010-12-28
申请号：US11578134
申请日：2005-04-08
申请人： Shigeto Negi , Toshikazu Shimizu , Hiroshi Kuroda , Naoyuki Shimomura , Manabu Sasho , Yorihisa Hoshino , Manabu Kuboto
发明人： Shigeto Negi , Toshikazu Shimizu , Hiroshi Kuroda , Naoyuki Shimomura , Manabu Sasho , Yorihisa Hoshino , Manabu Kuboto
IPC分类号： C07D231/54
CPC分类号： C07D471/04
摘要： Intermediates useful for the synthesis of pyrazole-fused ring derivatives, such as 7-phenylpyrazolo [1,5-a]pyridine derivatives, and method for producing the same. Method for producing compound represented by the general formula (II), wherein Z1 and Z2 each independently represents a methine group or a nitrogen atom; Rl represents an ethyl group or the like; R5 represents a hydrogen atom or the like; R2 and R3 each independently represents a C1-6 alkyl group or the like, salts thereof, or solvates of both, comprising the step of: reacting a compound represented by the general formula (I), wherein Z1, Z2, R5, R1, R2 and R3 each has the same definition as described above, with an organometallic reagent; and then reacting the resulting product with pentafluoroiodobenzene.
摘要翻译：用于合成吡唑稠合环衍生物如7-苯基吡唑并[1,5-a]吡啶衍生物的中间体及其制备方法。制备由通式（II）表示的化合物的方法，其中Z1和Z2各自独立地表示次甲基或氮原子; R1表示乙基等; R5表示氢原子等; R 2和R 3各自独立地表示C 1-6烷基等，其盐或两者的溶剂合物，包括以下步骤：使通式（I）表示的化合物与其反应，其中Z1，Z2，R5，R1， R2和R3各自具有与上述相同的定义，与有机金属试剂; 然后使所得产物与五氟碘苯反应。

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