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1. 发明授权

US4225706A Polychalcogen ester of cephem compound, process for preparing the same and method for removing the protective group of the same 失效
标题翻译：头孢烯化合物的多元硫酸酯，其制备方法及其除去保护基的方法
公开(公告)号：US4225706A
公开(公告)日：1980-09-30
申请号：US898613
申请日：1978-04-21
申请人： Shigeo Seki , Ken Nishihata , Satoru Nakabayashi , Toshinori Saito , Hitoshi Ikeda , Nobuo Itoh , Shokichi Nakajima , Shunzo Fukatsu
发明人： Shigeo Seki , Ken Nishihata , Satoru Nakabayashi , Toshinori Saito , Hitoshi Ikeda , Nobuo Itoh , Shokichi Nakajima , Shunzo Fukatsu
IPC分类号： A61K20060101 , C07D501/04 , C07D501/20 , C07D501/22 , C07D501/26 , C07D501/34
CPC分类号： C07D501/20 , Y02P20/55
摘要： A novel ester of a cephem compound having a carboxyl group at the 4-position in the nucleus; a process for preparing the same by reacting a cephem carboxylic acid or its salt with a halogenide; and a method for removing the protective group for the carboxyl group in the nucleus of a cephem compound by contacting it with an alcohol, or with an organic solvent in the presence of a Lewis acid.
摘要翻译：一种在细胞核中4位具有羧基的头孢烯化合物的新型酯; 通过使头孢烯羧酸或其盐与卤化物反应来制备该方法; 以及通过使其与醇或与有机溶剂在路易斯酸的存在下接触来除去头孢烯化合物的核中的羧基的保护基的方法。

2. 发明授权

US4159372A Process for preparing cephalosporin esters in the presence of liquid sulfur dioxide 失效
标题翻译：在液体二氧化硫存在下制备头孢菌素酯的方法
公开(公告)号：US4159372A
公开(公告)日：1979-06-26
申请号：US883812
申请日：1978-03-06
申请人： Shigeo Seki , Satoru Nakabayashi , Ken Nishihata , Nobuo Itoh , Toshinori Saito , Masahiro Onodera , Shunzo Fukatsu
发明人： Shigeo Seki , Satoru Nakabayashi , Ken Nishihata , Nobuo Itoh , Toshinori Saito , Masahiro Onodera , Shunzo Fukatsu
IPC分类号： A61K31/545 , C07D501/04 , C07D501/20
CPC分类号： C07D501/20 , C07D501/04
摘要： A process for preparing a cephalosporin ester which comprises subjecting an organic halide or an alcohol to reaction with a cephalosporin acid, a cephalosporin acid halide or a salt thereof in the presence of liquid sulfur dioxide.
摘要翻译：一种制备头孢菌素酯的方法，其包括在液体二氧化硫存在下使有机卤化物或醇与头孢菌素酸，头孢菌素酰卤或其盐反应。

3. 发明授权

US4175185A Process for preparing cephalosporanic acid derivatives 失效
标题翻译：制备头孢菌酸衍生物的方法
公开(公告)号：US4175185A
公开(公告)日：1979-11-20
申请号：US892179
申请日：1978-03-31
申请人： Shigeo Seki , Satoru Nakabayashi , Toshinori Saito , Shunzo Fukatsu , Shokichi Nakajima , Toshiyasu Ishimaru
发明人： Shigeo Seki , Satoru Nakabayashi , Toshinori Saito , Shunzo Fukatsu , Shokichi Nakajima , Toshiyasu Ishimaru
IPC分类号： C07D501/20 , C07D501/26
CPC分类号： C07D501/26
摘要： A process for preparing a cephalosporanic acid derivative or a 7-acylaminocephalosporanic acid derivative which comprises subjecting an esterifying agent to reaction in liquid sulfur dioxide in the presence of a base with an N-protected-cephalosporin C to obtain a diester, subjecting the diester to reaction in an inert solvent with an iminohalide forming agent to produce an iminohalide, subjecting the iminohalide with a lower alcohol to produce an iminoether, subjecting the product produced, after subjecting the iminoether to reaction with a reactive derivative of an organic acid, to hydrolysis and further eliminating the ester group of the carboxylic acid.
摘要翻译：一种制备头孢菌酸衍生物或7-酰氨基头孢烷酸衍生物的方法，其包括在碱存在下，用N-保护型头孢菌素C使酯化剂在液态二氧化硫中进行反应，得到二酯，在惰性溶剂中与亚氨基卤化物形成剂反应以产生亚氨基卤化物，使亚氨基卤化物与低级醇反应生成亚氨基醚，使亚氨基醚与有机酸的反应性衍生物反应后生成的产物水解和进一步消除羧酸的酯基。

4. 发明授权

US4188480A Process for the production of a 9,3"-di-acyl derivative of a macrolide antibiotic 失效
标题翻译：用于生产大环内酯类抗生素的9,3“ - 二 - 酰基衍生物的方法
公开(公告)号：US4188480A
公开(公告)日：1980-02-12
申请号：US933188
申请日：1978-08-10
申请人： Takeshi Nakamura , Satoru Nakabayashi , Shunzo Fukatsu , Shigeo Seki
发明人： Takeshi Nakamura , Satoru Nakabayashi , Shunzo Fukatsu , Shigeo Seki
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C07H1/00
CPC分类号： C07H17/08
摘要： A 9,3"-di-acyl derivative of a macrolide antibiotic can be readily produced by reacting a macrolide antibiotic or an acyl derivative thereof with an organic acid halide, particularly an alkanoic acid halide, in a solvent and in the presence of a molecular sieve consisting of a synthetic zeolite and then de-acylating partially the resultant acylation products by a partial hydrolysis in an aqueous alcohol to give the 9,3"-di-acyl derivative of the macrolide antibiotic.
摘要翻译：通过使大环内酯类抗生素或其酰基衍生物与有机酰卤，特别是链烷酰卤反应，在溶剂中，并存在下可以容易地制备大环内酯类抗生素的9,3“ - 二 - 酰基衍生物分子筛由合成沸石组成，然后通过在含水醇中部分水解将所得酰化产物部分脱酰化，得到大环内酯类抗生素的9,3“ - 二 - 酰基衍生物。

5. 发明授权

US4791197A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4791197A
公开(公告)日：1988-12-13
申请号：US751208
申请日：1985-07-02
申请人： Kenji Sakagami , Kunio Atsumi , Ken Nishihata , Takashi Yoshida , Shunzo Fukatsu
发明人： Kenji Sakagami , Kunio Atsumi , Ken Nishihata , Takashi Yoshida , Shunzo Fukatsu
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D277/38 , C07D501/20 , C07D501/24 , C07D501/36 , C07D501/59 , C07D501/22
CPC分类号： C07D277/20 , Y02P20/55
摘要： A new cephalosporin compound is now provided, which is useful as antibacterial agent and is represented by the general formula (I) ##STR1## wherein R.sup.1 is an amino group or a protected amino group; R.sup.2 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group; R.sup.3 is a hydrogen atom, a halogen atom, a lower alkylthio group, a lower alkoxyl group, a vinyl group or a group of the formula: --CH.sub.2 Y where Y is a hydrogen atom, a halogen atom, an acyloxy group, an unsubstituted or substituted heterocyclic thio group or an unsubstituted or substituted pyridinio group, and a pharmaceutically acceptable salt or ester thereof.
摘要翻译：现提供一种新的头孢菌素化合物，其可用作抗菌剂并由通式（I）表示，其中R 1是氨基或被保护的氨基; R2是氢原子，成盐阳离子或羧基保护基; R3是氢原子，卤素原子，低级烷硫基，低级烷氧基，乙烯基或下式基团：-CH2Y其中Y是氢原子，卤素原子，酰氧基，未取代的或未取代的取代的杂环硫基或未取代或取代的吡啶并基及其药学上可接受的盐或酯。

6. 发明授权

US4839350A Cephalosporin compounds and the production thereof 失效
标题翻译：头孢菌素化合物及其生产
公开(公告)号：US4839350A
公开(公告)日：1989-06-13
申请号：US36124
申请日：1987-04-07
申请人： Kunio Atsumi , Kenji Sakagami , Yuichi Yamamoto , Takashi Yoshida , Ken Nishihata , Shinichi Kondo , Shunzo Fukatsu
发明人： Kunio Atsumi , Kenji Sakagami , Yuichi Yamamoto , Takashi Yoshida , Ken Nishihata , Shinichi Kondo , Shunzo Fukatsu
IPC分类号： C07D277/32 , C07D501/22 , C07D501/24
CPC分类号： C07D277/32 , Y02P20/55
摘要： A class of new caphalosporin compounds (syn-isomer) is now provided, which is useful as antibacterial agent and is represented by the general formula (I) ##STR1## wherein R.sup.1 is an amino group or a protected amino group; R.sup.2 is a lower alkyl group, a carboxymethyl group or a protected carboxymethyl group; R.sup.3 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group; A is an unsubstituted or substituted phenyl group, an unsubstituted or substituted furyl group, an unsubstituted or substituted thiazolyl group or an unsubstituted or substituted 3-lower-alkylthiazolio group, and a pharmaceutically acceptable salt or ester thereof.
摘要翻译：现在提供一类新的头孢菌素化合物（顺式异构体），其可用作抗菌剂并由通式（I）表示，其中R 1是氨基或被保护的氨基; R2是低级烷基，羧甲基或受保护的羧甲基; R3是氢原子，成盐阳离子或羧基保护基; A是未取代或取代的苯基，未取代或取代的呋喃基，未取代或取代的噻唑基或未取代或取代的3-低级烷基噻唑基及其药学上可接受的盐或酯。

7. 发明授权

US4785090A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4785090A
公开(公告)日：1988-11-15
申请号：US704077
申请日：1985-02-21
申请人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
发明人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
IPC分类号： C07D213/64 , C07D213/68 , C07D221/04 , C07D501/36 , C07D501/38 , A61K31/545
CPC分类号： C07D221/04 , C07D213/64 , C07D213/68
摘要： This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.
摘要翻译：这是一类具有下式的抗菌化合物：其中Y是直链或支链烷基或烯基链，3-6个碳原子的环烷基甲基，每个基团任选被卤素取代，或基团< 其中n为0或1-3的整数，A为基团-COR 3，其中R 3为羟基，其中R 4和R 5可以相同或不同，为氢或1-5碳的烷基原子，基团或含有氮和/或硫的5-或6-元杂环基，R 1和R 2可以相同或不同，为氢，1-5个碳原子的烷基或R1 并且R 2可以组合在一起形成3-5个碳原子的亚烷基，Z是下式的基团：其中m是0或3-5的整数，R6是氢或1-3个碳的烷基原子和R 7，当m是3-5的整数时，是1-5个碳原子的烷基，烯基，环丙基，基团 - （CH 2）pB，其中p是0或1-3的整数，B是氨基，烷基取代的氨基羟基，羧基，氨基甲酰基，三氟甲基，磺酸，磺酸酰胺，烷硫基或氰基，或当m为0时，其为1-5个碳原子的烷基，其可任选被卤素，链烯基，基团其中R8是氢，1-4个碳原子的烷基或苯基，或环丙基及其盐。

8. 发明授权

US4357465A 3',4'-Diedeoxykanamycin B derivatives 失效
标题翻译： 3'，4'-脱氧卡那霉素B衍生物
公开(公告)号：US4357465A
公开(公告)日：1982-11-02
申请号：US187014
申请日：1980-09-15
申请人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
发明人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
IPC分类号： C07H15/236 , A61K31/71 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.
摘要翻译：提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。

9. 发明授权

US4195170A 3',4'-Episulfido kanamycin B compounds 失效
标题翻译： 3'，4'-二硫代卡那霉素B化合物
公开(公告)号：US4195170A
公开(公告)日：1980-03-25
申请号：US880401
申请日：1978-02-23
申请人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
发明人： Hamao Umezawa , Sumio Umezawa , Shigeo Seki , Shunzo Fukatsu , Shuntaro Yasuda
IPC分类号： C07H15/236 , C07H15/22
CPC分类号： C07H15/234 , Y02P20/55
摘要： New routes are provided for the synthesis of 3',4'-dideoxykanamycin B which is effective in inhibiting kanamycin-resistant organisms from kanamycin B through new intermediate, of which a fundamental process comprises a new reaction of a 3',4'-epoxy derivative of amino- and hydroxyl-protected kanamycin B with a xanthate to form a corresponding 3',4'-dideoxy-3'-eno derivative followed by removal of the amino- and hydroxyl-protecting groups thereof and by hydrogenation of the resulting 3',4'-dideoxy-3'-eno-kanamycin B. A 3',4'-episulfide derivative corresponding to the 3',4'-epoxy derivative which is formed as second product in the reaction of 3',4'-epoxy derivative with xanthate is also used as intermediate for the preparation of 3',4'-dideoxykanamycin B.
摘要翻译：提供了用于合成3'，4'-双脱氧卡那霉素B的新途径，其通过新的中间体有效抑制卡那霉素B的卡那霉素抗性生物，其中基本方法包括3'，4'-环氧基氨基和羟基保护的卡那霉素B与黄原酸酯的衍生物形成相应的3'，4'-二脱氧-3'-烯衍生物，然后除去其氨基和羟基保护基团，并通过氢化得到的3 '，4'-二脱氧-3'-烯 - 卡那霉素B.对应于3'，4'-环氧衍生物的3'，4'-环硫化物衍生物，其在3'，4' 含有黄原酸酯的环氧衍生物也用作制备3'，4'-双脱氧卡那霉素B的中间体。

10. 发明授权

US4290972A Process for the production of 4-aminobutyric acid or its derivatives 失效
标题翻译：生产4-氨基丁酸或其衍生物的方法
公开(公告)号：US4290972A
公开(公告)日：1981-09-22
申请号：US92940
申请日：1979-11-09
申请人： Toshio Yoneta , Seiji Shibahara , Shigeo Seki , Shunzo Fukatsu
发明人： Toshio Yoneta , Seiji Shibahara , Shigeo Seki , Shunzo Fukatsu
IPC分类号： C07C227/04 , A61K31/19 , C07B31/00 , C07C20060101 , C07C67/00 , C07C227/00 , C07C227/06 , C07C227/26 , C07C229/04 , C07C229/06 , C07C229/22 , C07C229/26 , C07C99/10 , C07C121/42 , C07C121/453
CPC分类号： C07C255/00 , Y02P20/55
摘要： 4-Amino-2-hydroxybutyric acid or 2,4-diaminobutyric acid may be readily produced by a new process comprising reacting a propionic acid compound containing a .beta.-carboxamido substituent (-CONH.sub.2) on the carbon atom at the 3-position and optionally containing hydroxyl substituent and protected or unprotected amino substituent on the .alpha.-carbon atom thereof, with an alkanoic acid anhydride in liquid pyridine to convert the carboxamido group into a nitrile group, with occasional acylation of a .alpha.-hydroxyl group, occasionally removing the alkanoyl group from the .alpha.-acyloxyl group of the resulting nitrile intermediate, and then reducing the resultant nitrile compound with hydrogen to convert the nitrile group into an aminomethyl group, and further optionally removing the residual amino-protecting group from the resultant 4-aminobutyric acid compound.
摘要翻译： 4-氨基-2-羟基丁酸或2,4-二氨基丁酸可以通过一种新方法容易地产生，包括使含有β-羧酰胺基取代基（-CONH 2）的丙酸化合物在3-位上的碳原子上和任选地在其α-碳原子上含有羟基取代基和被保护或未被保护的氨基取代基，与链烷酸酐在液体吡啶中，将羧酰胺基转化为腈基，偶尔酰化α-羟基，偶尔除去烷酰基由得到的腈中间体的α-酰氧基，然后用氢还原得到的腈化合物，将腈基转化为氨基甲基，进一步任选地从所得的4-氨基丁酸化合物中除去残留的氨基保护基。

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