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1. 发明授权

US5008409A Process for preparing 1,4-bridged cyclohexane carboxylic acid derivatives 失效
标题翻译：制备1,4-桥环己烷羧酸衍生物的方法
公开(公告)号：US5008409A
公开(公告)日：1991-04-16
申请号：US447513
申请日：1989-12-07
申请人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Kyozo Kawata
发明人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Kyozo Kawata
IPC分类号： C07C303/40 , C07C311/20
CPC分类号： C07C303/40
摘要： A process for preparing a compound of Formula (I): ##STR1## wherein R is phenyl or phenyl substituted with hydroxy, lower alkoxy, halogen or lower alkyl; Y is unsubstituted or substituted methylene, ethylene, vinylene or oxygen; m is 0 or 1; n is 0, 1 or 2; and q is 1, 2, 3 or 4; with the limitation that when m is 0, n is not 0, and when m is 1, n is not 2, which process comprises:(a) reacting an aldehyde of Formula (II); ##STR2## wherein R, Y, m and n are as defined above, under reaction conditions for the Wittig Reaction with a ylide of Formula (III):(R.sup.1).sub.3 P.dbd.CH(CH.sub.2).sub.q COOM (III) wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl or aryl, M is an alkali metal and q is as defined above;(b) treating the reaction mixture of step (a) with an alkaline earth metal halide under alkaline conditions to form the alkaline earth metal salt of the carboxylic acid of Formula (I);(c) extracting the alkaline earth metal salt of the carboxylic acid of Formula (I) in an organic solvent; and(d) recovering the free carboxylic acid of Formula (I) from the organic solvent.

2. 发明授权

US4525355A 7-.beta.-Ureidoacetamido-oxacephalosporins 失效
标题翻译： 7-β-脲基乙酰氨基 - 氧杂七环素
公开(公告)号：US4525355A
公开(公告)日：1985-06-25
申请号：US566023
申请日：1983-12-27
申请人： Masayuki Narisada , Fumihiko Watanabe , Tetsuo Okada , Hiromu Matsumura
发明人： Masayuki Narisada , Fumihiko Watanabe , Tetsuo Okada , Hiromu Matsumura
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , Y02P20/55
摘要： A 7.beta.-ureidoacetamido-7.alpha.-methoxy-3-(1-carbamoylmethyl-1H-tetrazol-5-yl)thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid derivative represented by the following formula: ##STR1## wherein Ar is phenyl, hydroxyphenyl, or thienyl and R is hydrogen, a light metal, or a carboxy-protecting group.
摘要翻译：由以下所示的7β-脲基乙酰胺基-7α-甲氧基-3-（1-氨基甲酰基甲基-1H-四唑-5-基）硫代甲基-1-脱硫-1-氧代-3-头孢烯-4-羧酸衍生物式：其中Ar是苯基，羟基苯基或噻吩基，R是氢，轻金属或羧基保护基。

3. 发明授权

US4138486A Arylmalonamido-1-oxadethiacephalosporins 失效
标题翻译：芳基丙二酰胺-1-氧杂硫菌醚
公开(公告)号：US4138486A
公开(公告)日：1979-02-06
申请号：US780183
申请日：1977-03-22
申请人： Masayuki Narisada , Wataru Nagata
发明人： Masayuki Narisada , Wataru Nagata
IPC分类号： C07D505/00 , A61K31/535 , A61K31/5365 , A61P31/00 , A61P31/04 , C07D205/00 , C07D265/00 , C07D498/02 , C07D498/04 , C07D505/06 , C07D505/18 , C07D505/20 , A61K27/00 , A61K31/555 , A61K31/695
CPC分类号： C07D498/04 , A61K31/535 , C07D205/00 , C07D265/00 , C07D505/00
摘要： Antibacterial 1-oxadethiacephalosporins of the formula: ##STR1## [wherein Ar is ##STR2## (in which Acyl is organic or inorganic acyl); COB.sup.1 and COB.sup.2 each is carboxy or protected carboxy; Het is ##STR3## (in which COB.sup.3 is carboxy or protected carboxy); AND Y is hydrogen or methoxy;And when COB.sup.1, COB.sub.2, and/or COB.sup.3 is carboxy, pharmaceutically acceptable salts thereof are included,But with a proviso that when Y is methoxy, Het is ##STR4## a pharmaceutical or veterinary composition comprising the said 1-oxadethiacephalosporins and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering the said 1-oxadethiacephalosporin.
摘要翻译：下式的抗菌1-恶二硫醚孢子：其中Ar是有机或无机酰基;其中Ar是有机或无机酰基; COB1和COB2各自为羧基或保护的羧基; Het是（其中COB 3是羧基或被保护的羧基）; 且Y为氢或甲氧基; 当COB1，COB2和/或COB3为羧基时，包括其药学上可接受的盐，但是当Y为甲氧基时，Het为包含所述1-恶二硫醚类和药物载体的药物或兽用组合物，以及用于治疗或预防人或兽传染性疾病的方法，包括施用所述1-恶二硫醚类。

4. 发明授权

US4960909A 7-oxabicyclo[2.2.1] heptane sulfonamide derivatives 失效
标题翻译： 7-氧杂二环[2.2.1]庚烷磺酰胺衍生物
公开(公告)号：US4960909A
公开(公告)日：1990-10-02
申请号：US327772
申请日：1989-03-23
申请人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
发明人： Masayuki Narisada , Mitsuaki Ohtani , Fumihiko Watanabe , Sanji Hagishita , Kaoru Seno , Susumu Kamata , Nobuhiro Haga , Tatsuo Tsuri , Tadahiko Tsushima , Kenji Kawada
IPC分类号： C07D493/08 , A61K31/00 , A61K31/335 , A61K31/336 , A61K31/34 , A61K31/557 , A61P7/02 , A61P9/08 , A61P11/08 , C07C20060101 , C07C67/00 , C07C301/00 , C07C311/00 , C07C311/02 , C07C311/07 , C07C311/10 , C07C311/13 , C07C311/15 , C07C311/20 , C07C311/37 , C07C313/00 , C07C323/52 , C07D209/52 , C07D209/56 , C07D213/34 , C07D213/71 , C07D221/22 , C07D303/40 , C07D303/46 , C07D331/02 , C07D491/044 , C07D493/04 , C07D495/04
CPC分类号： C07D493/08 , C07D213/34 , Y02P20/55
摘要： Bicyclic sulfonamido derivatives represented by the formula: ##STR1## wherein R.sub.1 is a hydrogen or lower alkyl; R.sub.2 is an alkyl, substituted or unsubstituted aryl, aralkyl or hetelocycle; R.sub.3 is a hydrogen or methyl; X is an alkylene or alkenylene which may be substituted by a fluorine atom or atoms and may contain an oxygen, sulfur and/or phenylene in the chain; Y is straight or branched alkylene or alkenylene oxygen, or sulfur; m is 0 or 1; and n is 0, 1 or 2, or their salt, said derivatives being useful as antithrombotic, anti-vasoconstricting, and anti-bronchoconstricting drugs.

5. 发明授权

US4376770A Cephalosporin analogs for oral use 失效
标题翻译：头孢菌素类似物用于口服使用
公开(公告)号：US4376770A
公开(公告)日：1983-03-15
申请号：US285876
申请日：1981-07-23
申请人： Masayuki Narisada , Tetso Okada , Tadashi Yoshida , Shinzo Matsuura
发明人： Masayuki Narisada , Tetso Okada , Tadashi Yoshida , Shinzo Matsuura
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00
摘要： 7.beta.-(2-Cyano-aliphatic acylamino)-7.alpha.-methoxy-3-heterocyclic thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acids and salts or pharmacologically acceptable esters generically represented by the following formula are potent antibacterials and esters are prospective oral drugs: ##STR1## (wherein A is a lower alkyl, lower alkenyl or lower alkynyl group;B is a hydrogen atom, salt forming atom, salt forming group or physiologically hydrolyzable ester group; andHet is a heterocyclic group).
摘要翻译： 7β-（2-氰基 - 脂族酰氨基）-7α-甲氧基-3-杂环硫代甲基-1-脱氧-1-氧杂-3-头孢烯-4-羧酸和通常由下式表示的盐或药理学上可接受的酯（其中A为低级烷基，低级烯基或低级炔基; B为氢原子，成盐原子，成盐基团或生理水解性酯基; Het为杂环基）。

6. 发明授权

US4371532A Malonamidooxadethiacephem compounds 失效
标题翻译：马洛替胺恶唑硫醚化合物
公开(公告)号：US4371532A
公开(公告)日：1983-02-01
申请号：US227202
申请日：1981-01-22
申请人： Masayuki Narisada , Tetsuo Okada
发明人： Masayuki Narisada , Tetsuo Okada
IPC分类号： A61K31/535 , A61P31/04 , C07D505/00 , C07D413/14 , A61K31/425 , C07D498/04
CPC分类号： C07D505/00
摘要： An antibacterial compound represented by the following formula: ##STR1## (wherein R is a hydrogen atom or a lower alkyl, lower alkenyl, lower alkynyl or lower alkylthio-lower alkyl group;B.sup.1 and B.sup.2 each is a hydrogen atom or an ester or salt forming group or atom same or different for each; andHet is a monocyclic hetero-cyclic group)showing strong antipseudomonal activity, process for preparing the same, pharmaceutical preparation containing the same and method for combating bacterial infection by applying the same.
摘要翻译：由下式表示的抗菌化合物：其中R是氢原子或低级烷基，低级烯基，低级炔基或低级烷硫基 - 低级烷基; B1和B2各自是氢原子或酯或成盐基团或每个相同或不同的原子; Het是单环杂环基团），其显示出强的抗假单胞菌活性，其制备方法，含有该药物的药物制剂和通过应用它们来防治细菌感染的方法。

7. 发明授权

US4323567A Arylmalonamido-1-oxadethiacephalosporins 失效
标题翻译：芳基丙二酰胺-1-氧杂硫菌醚
公开(公告)号：US4323567A
公开(公告)日：1982-04-06
申请号：US156872
申请日：1980-06-05
申请人： Masayuki Narisada , Wataru Nagata
发明人： Masayuki Narisada , Wataru Nagata
IPC分类号： C07D505/00 , A61K31/535 , A61K31/5365 , A61P31/00 , A61P31/04 , C07D205/00 , C07D265/00 , C07D498/02 , C07D498/04 , C07D505/06 , C07D505/18 , C07D505/20 , C07D413/14 , A61K31/41 , C07D413/12
CPC分类号： C07D498/04 , A61K31/535 , C07D205/00 , C07D265/00 , C07D505/00
摘要： Antibacterial 1-oxadethiacephalosporins of the formula: ##STR1## wherein Ar is ##STR2## (in which Acyl is organic or inorganic acyl); COB.sup.1 and COB.sup.2 each is carboxy or protected carboxy;Het is ##STR3## (in which COB.sup.3 is carboxy or protected carboxy); and Y is hydrogen or methoxy;and when COB.sup.1 and COB.sup.2, and/or COB.sup.3 is carboxy, pharmaceutically acceptable salts thereof are included, but with a proviso that when Y is methoxy, Het is ##STR4## a pharmaceutical or veterinary composition comprising the said 1-oxadethiacephalosporins and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering the said 1-oxadethiacephalosporin.Also disclosed are epimers of the compounds of formula (I) wherein the asymmetric carbon of the malonic methine is in the D(R)- or L(S)- configuration. The individual epimers are separable by column chromatography and/or crystallization. The bactericidal activity of the D-epimers is greater than that of the L-epimers or the mixtures of the epimers.
摘要翻译：其中Ar是有机或无机酰基的酰基;其中Ar是有机或无机酰基;其中Ar是有机或无机酰基。 COB1和COB2各自为羧基或被保护的羧基; Het是（其中COB 3是羧基或被保护的羧基）; Y为氢或甲氧基; 并且当COB1和COB2和/或COB3为羧基时，包括其药学上可接受的盐，但条件是当Y为甲氧基时，Het为包含所述1-恶二硫醚类和药物载体的药物或兽用组合物，以及用于治疗或预防人或兽传染性疾病的方法，包括施用所述1-恶二硫醚类。还公开了式（I）化合物的差向异构体，其中丙二酸次甲基的不对称碳为D（R） - 或L（S） - 构型。单独的差向异构体可通过柱色谱和/或结晶分离。 D-差向异构体的杀菌活性大于L-差向异构体或差向异构体的混合物的杀菌活性。

8. 发明授权

US4211779A 7.alpha.-Methoxy substituted cephalosporins 失效
标题翻译： 7α-甲氧基取代头孢菌素
公开(公告)号：US4211779A
公开(公告)日：1980-07-08
申请号：US821314
申请日：1977-08-02
申请人： Masayuki Narisada , Teruji Tsuji , Hiromu Matsumura , Wataru Nagata
发明人： Masayuki Narisada , Teruji Tsuji , Hiromu Matsumura , Wataru Nagata
IPC分类号： A61K31/545 , C07D501/36
CPC分类号： C07D501/36
摘要： Antibacterial 7.alpha.-methoxy-3-cephem derivatives of the formula: ##STR1## [wherein R.sup.1 is hydrogen, or organic or inorganic acyl;R.sup.2 is alkyl; andCOR.sup.3 is carboxy or protected carboxy],methods of production, and pharmaceutical preparations thereof.
摘要翻译：下式的抗菌7α-甲氧基-3-头孢烯衍生物：其中R 1是氢或有机或无机酰基; R2是烷基; 和COR 3是羧基或受保护的羧基]，生产方法及其药物制剂。

9. 发明授权

US4183928A Haloarylmalonamidooxacephalosporins 失效
标题翻译：卤代芳基丙酰胺氧基头孢菌素
公开(公告)号：US4183928A
公开(公告)日：1980-01-15
申请号：US900235
申请日：1978-04-26
申请人： Yoshio Hamashima , Masayuki Narisada , Sadao Hayashi , Wataru Nagata
发明人： Yoshio Hamashima , Masayuki Narisada , Sadao Hayashi , Wataru Nagata
IPC分类号： C07D505/06 , A61K31/5365 , A61P31/00 , C07C59/56 , C07D505/00 , C07D505/20 , C07D413/02 , A61K31/395 , A61K31/535
CPC分类号： C07C59/56 , C07D505/00
摘要： Antibacterial haloarylmalonamido-1-dethia-1-oxacephalosporins of the following formula: ##STR1## wherein Ar is ##STR2## (in which Hal and Hal' each is halogen and RO is hydroxy or protected hydroxy);COA and COB each is carboxy or protected carboxy including a pharmaceutically acceptable salt group;and Het is 1-lower alkyl-5-tetrazolyl, 1,3,4-thiadiazol-2-yl or 5-lower alkyl-1,3,4-thiadiazol-2-yl,a pharmaceutical or veterinary composition comprising the said haloarylmalonamido-1-dethia-1-oxacephalosporin and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering an effective amount of the said antibacterial compound.
摘要翻译：其中Ar是卤素，Hal和Hal各自为卤素，RO为羟基或被保护的羟基）的抗菌卤代芳基丙二酰胺-1-脱氧-1-氧杂七环素：其中Ar为< ; COA和COB各自为羧基或受保护的羧基，包括药学上可接受的盐基; 和Het是1-低级烷基-5-四唑基，1,3,4-噻二唑-2-基或5-低级烷基-1,3,4-噻二唑-2-基，其包含所述卤代芳基丙二酰胺 -1-脱氢-1-氧杂环孢菌素和药物载体，以及治疗或预防人或兽传感疾病的方法，包括给予有效量的所述抗菌化合物。

10. 发明授权

US4139711A Dihydroethanoanthracene derivatives 失效
标题翻译：二氢山han蒽衍生物
公开(公告)号：US4139711A
公开(公告)日：1979-02-13
申请号：US767633
申请日：1977-02-10
申请人： Masayuki Narisada
发明人： Masayuki Narisada
IPC分类号： C07D233/06 , C07D263/12 , C07D265/08 , C07D277/10 , C07C93/20 , C07C93/00
CPC分类号： C07D277/10 , C07D233/06 , C07D263/12 , C07D265/08
摘要： Dihydroethanoanthracene derivatives of the formula: ##STR1## [wherein R represents a hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.1 represents a group ##STR2## (in which A represents a C.sub.2 -C.sub.4 alkylene optionally substituted by one or two C.sub.1 -C.sub.4 alkyls or by a phenyl; and Y represents an oxygen, sulfur, or imino) or group--COO--A--NH.sub.2(in which A is as defined above)] and their pharmaceutically acceptable acid addition salts, being useful as antidepressants or their synthetic intermediates.
摘要翻译：下式的二氢山
烷蒽衍生物：其中R表示氢或C 1 -C 4烷基; R1表示基团（其中A表示任选被一个或两个C 1 -C 4烷基或苯基取代的C 2 -C 4亚烷基; Y表示氧，硫或亚氨基）或-COO-A- NH2（其中A如上所定义）]及其药学上可接受的酸加成盐，可用作抗抑郁药或其合成中间体。

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