公开(公告)号：US3959256A

公开(公告)日：1976-05-25

申请号：US505310

申请日：1974-09-12

申请人： Shigeharu Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Taro Niida ,  Toyoaki Kawasaki ,  Takashi Tsuruoka

发明人： Shigeharu Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Taro Niida ,  Toyoaki Kawasaki ,  Takashi Tsuruoka

IPC分类号： C07H17/08

CPC分类号： C07H17/08

摘要： A 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is now synthetized, which is a new compound useful in that this new 9-O-alkanoyl-3"-O-alkanoyloxymethyl derivative of the SF-837 substance exhibits an antibacterial activity comparable to that of the parent SF-837 substance but is advantageously free from the unpleasant bitter taste inherent to the SF-837 substance and is hence adapted for oral administration. A process of producing the 9-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance is also provided, which comprises hydrolysing partially and selectively a 9,2'-di-O-alkanoyl-3"-O-alkanoyloxymethyl-SF-837 substance in an aqueous alkanol or aqueous acetone. The 9,2'-di-O-alkanoyl-3"-O-alkanopyloxymethyl-SF-837 substance may be prepared by reacting a 9,2'-di-alkanoyl- or O-mono-O-alkanoyl-3"-O-thiomethoxymethyl-SF-837 substance with an alkanoic anhydride which is exemplified by acetic anhydride or propionic anhydride in the specification.

摘要翻译： 现在合成了9-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质，这是一种新的化合物，有用的是这种新型的9-O-烷酰基-3'-O-烷酰氧基甲基衍生物 -837物质表现出与母体SF-837物质相当的抗菌活性，但有利地没有SF-837物质固有的不愉快的苦味，因此适于口服给药。 还提供了制备9-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质的方法，其包括部分和选择性地水解9,2'-二-O-烷酰基-3'-O - 烷酰氧基甲基-SF-837物质在链烷醇水溶液或丙酮水溶液中。 9,2'-二-O-烷酰基-3“-O-烷酰氧基甲基-SF-837物质可以通过使9,2'-二烷酰基或O-单-O-烷酰基-3' 具有链烷酸酐的“-O-硫代甲氧基甲基-SF-837”物质，其例示在说明书中的乙酸酐或丙酸酐。

公开(公告)号：US4017607A

公开(公告)日：1977-04-12

申请号：US597188

申请日：1975-07-18

申请人： Shigeharo Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Taro Niida ,  Toyoaki Kawasaki

发明人： Shigeharo Inouye ,  Shoji Omoto ,  Katsuyoshi Iwamatsu ,  Takashi Tsuruoka ,  Taro Niida ,  Toyoaki Kawasaki

IPC分类号： A61K31/70 ,  A61K31/7042 ,  A61K31/7048 ,  A61P31/04 ,  C07H17/08

CPC分类号： C07H17/08

摘要： As new compounds are provided 9,3",4"-trialkanoyl SF-837 M.sub.1 substances which have therapeutically useful antibacterial activity and do not show any objectionable long-lasting bitter taste upon its oral administration. These 9,3",4"-trialkanoyl SF-837 M.sub.1 substances may be prepared from SF-837 substance, 9,2',3"-tri-acetyl SF-837 M.sub.1 substance, 9,2'-di-acetyl SF-837 substance, 9-propionyl SF-837 substance or 9,2'-dipropionyl SF-837 substance by acylating the latter with an alkanoic acid anhydride at 50.degree.-120.degree. C to produce the corresponding 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and occasionally the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance, with involving the shift of the 4"-alkanoyl group to the 3"-hydroxyl group. Partial and selective hydrolysis of the 9,2',3",4"-tetra-alkanoyl SF-837 M.sub.1 substance and/or the 9,18,2',3",4"-penta-alkanoyl SF-837 M.sub.1 substance so produced gives the desired 9,3",4"-tri-alkanoyl SF-837 M.sub.1 substance.

摘要翻译： 当新化合物被提供具有治疗上有用的抗菌活性的9,3“，4” - 三烷酰基SF-837M1物质，并且在其口服给药时不显示任何令人不快的持久苦味。 这些9,3“，4” - 三烷酰基SF-837 M1物质可以由SF-837物质，9,2'，3“ - 三乙酰基SF-837M1物质，9,2'-二 - 乙酰基SF-837物质，9-丙酰基SF-837物质或9,2'-二丙酰基SF-837物质，通过用烷基酸酐在50°-120℃下酰化后者，产生相应的9,2' 3“，4” - 四烷酰基SF-837 M1物质，偶尔有9,18,2'，3“，4” - 五烷酰基SF-837 M1物质，涉及4 “ - 烷酰基与3” - 羟基。 9,2'，3“，4” - 四烷酰基SF-837 M1物质和/或9,18,2'，3“，”4“ - 五烷酰基SF- 837如此生产的M1物质得到所需的9,3“，”4“ - 三烷酰基SF-837 M1物质。

公开(公告)号：US4302580A

公开(公告)日：1981-11-24

申请号：US185594

申请日：1980-09-09

申请人： Katsuyoshi Iwamatsu ,  Jiro Itoh ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inouye

发明人： Katsuyoshi Iwamatsu ,  Jiro Itoh ,  Shoji Omoto ,  Takashi Tsuruoka ,  Shigeharu Inouye

IPC分类号： C07D501/04 ,  C07D501/36 ,  C07D501/57 ,  C12P35/08

CPC分类号： C12P35/08

摘要： A chemotherapeutic, antibacterial agent, 7.beta.-[(2D-2-amino-2-carboxy)ethylthioacetamido]-7.alpha.-methoxy-3-[(1-methyl-1H-tetrazole-5-yl)thiomethyl]-3-cephem-4-carboxylic acid is produced economically and efficiently starting from cephamycin A and/or B by a "new route" process comprising the consecutive steps of reaction of cephamycin with 5-mercapto-1-methyl-1H-tetrazole; protection of the terminal amino group thereof by acylation; protection of the two carboxyl groups thereof by esterification; replacement of the acyl group initially having attached to the 7-amino group by a halogenoacetyl group; deprotection of the blocked 4-carboxyl group; and condensation of D-cysteine with the halogenoacetyl group attaching to the 7-amino group.

摘要翻译： 7β-[（2D-2-氨基-2-羧基）乙硫基乙酰氨基]-7α-甲氧基-3 - [（1-甲基-1H-四唑-5-基）硫代甲基] -3- 头孢霉素-4-羧酸从头孢霉素A和/或B开始通过包含头孢霉素与5-巯基-1-甲基-1H-四唑的连续步骤的“新途径”方法经济有效地产生; 通过酰化保护其末端氨基; 通过酯化保护其两个羧基; 用卤代乙酰基取代最初连接在7-氨基上的酰基; 封闭的4-羧基脱保护; 和D-半胱氨酸与连接于7-氨基的卤代乙酰基缩合。

公开(公告)号：US4229448A

公开(公告)日：1980-10-21

申请号：US23504

申请日：1979-03-23

申请人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

发明人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

IPC分类号： C07D213/65 ,  C07D213/79 ,  C07D213/81 ,  A61K31/455

CPC分类号： C07D213/79 ,  C07D213/65 ,  C07D213/81

摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.

摘要翻译： 由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基： 其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基， 酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的 苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基 或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基， 制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。

公开(公告)号：US4103083A

公开(公告)日：1978-07-25

申请号：US751877

申请日：1976-12-17

申请人： Yasuaki Ogawa ,  Yasumitsu Kondo ,  Takashi Shomura ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Taro Niida

发明人： Yasuaki Ogawa ,  Yasumitsu Kondo ,  Takashi Shomura ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Taro Niida

IPC分类号： C07D501/20 ,  C07D501/57

CPC分类号： C07D501/57 ,  Y10S435/886

摘要： Novel antibiotics derivatives 7-(5-acylamido-5-carboxyvaleramido)-3-(.alpha.-methoxy-p-acyloxycinnamoyloxymethyl)-7-methoxy-3-cephem-4-carboxylic acids and the salts thereof which are useful as antibiotics and intermediates for the preparation of cephamycin derivatives, a process for preparing the same, and a process for recovering the cephamycin derivatives effectively and stably from the fermentation broth in the form of an N-acyl derivative.

摘要翻译： 新型抗生素衍生物7-（5-酰氨基-5-羧基戊酰氨基）-3-（α-甲氧基 - 对酰氧基肉桂酰氧基甲基）-7-甲氧基-3-头孢烯-4-羧酸及其盐，可用作抗生素和中间体 用于制备头孢霉素衍生物，其制备方法，以及以N-酰基衍生物的形式从发酵液中有效稳定地回收头孢霉素衍生物的方法。

公开(公告)号：US4258184A

公开(公告)日：1981-03-24

申请号：US020224

申请日：1979-03-13

申请人： Fumio Kai ,  Takashi Tsuruoka ,  Osamu Makabe ,  Shigeharu Inouye ,  Hitoshi Ikeda ,  Yuzo Kazuno ,  Shokichi Nakajima ,  Shigeo Seki ,  Taro Niida

发明人： Fumio Kai ,  Takashi Tsuruoka ,  Osamu Makabe ,  Shigeharu Inouye ,  Hitoshi Ikeda ,  Yuzo Kazuno ,  Shokichi Nakajima ,  Shigeo Seki ,  Taro Niida

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/36 ,  C07D501/56

CPC分类号： C07D501/36 ,  A61K31/545

摘要： Novel cephalosporin derivatives having formulae (V) and (III): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.8 and A are defined as in the specification.

摘要翻译： 具有式（V）和（III）的新型头孢菌素衍生物：其中R 1，R 2，R 3，R 4，R 8和A如说明书中所定义。

公开(公告)号：US4563472A

公开(公告)日：1986-01-07

申请号：US433011

申请日：1982-10-06

申请人： Shigeharu Inouye ,  Taro Niida ,  Keinosuke Miyauchi ,  Kuniomi Matsumoto ,  Eiichi Akita ,  Masao Koyama ,  Fumio Kai ,  Takashi Tsuruoka

发明人： Shigeharu Inouye ,  Taro Niida ,  Keinosuke Miyauchi ,  Kuniomi Matsumoto ,  Eiichi Akita ,  Masao Koyama ,  Fumio Kai ,  Takashi Tsuruoka

IPC分类号： A01N43/36 ,  A01N43/50 ,  A01N43/56 ,  A01N43/653 ,  A01N43/713 ,  C07D207/34 ,  C07D207/42 ,  C07D233/91 ,  C07D257/04 ,  C07D257/06 ,  C07D521/00 ,  A61K31/41

CPC分类号： C07D257/04 ,  A01N43/36 ,  A01N43/50 ,  A01N43/56 ,  A01N43/653 ,  A01N43/713 ,  C07D207/34 ,  C07D207/42 ,  C07D231/12 ,  C07D233/56 ,  C07D233/91 ,  C07D249/08 ,  C07D257/06

摘要： Triiodoallyl- or iodopropargyl-substituted heterocyclic aromatic compounds which can be prepared by reacting unsubstituted- or substituted nitrogen-containing heterocyclic compounds with corresponding iodine containing alcohol reactive derivatives in the presence of a base in an inert organic solvent. These new heterocyclic aromatic compounds have remarkable antibacterial and antifungal activities and are useful as antibacterial and antifungal agents in medicinal, agricultural and industrial fields.

摘要翻译： 三碘代烯丙基或碘炔丙基取代的杂环芳族化合物，其可以通过在碱存在下在惰性有机溶剂中使未取代或取代的含氮杂环化合物与相应的含碘醇反应性衍生物反应来制备。 这些新的杂环芳族化合物具有显着的抗菌和抗真菌活性，可用作药用，农业和工业领域的抗菌和抗真菌剂。

公开(公告)号：US4198416A

公开(公告)日：1980-04-15

申请号：US944683

申请日：1978-09-22

申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

IPC分类号： C07D213/65 ,  C07D213/79 ,  A61K31/44

CPC分类号： C07D213/79 ,  C07D213/65

摘要： 5-Alkoxy-picolinic esters represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and R.sub.1 represents an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms or an acetyl group; a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an alkoxyalkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an indanyl group; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic esters, and anti-hypertensive compositions containing the 5-alkoxy-picolinic esters.

摘要翻译： 由式（I）表示的5-烷氧基 - 吡啶甲酸酯：其中R表示具有1至6个碳原子的烷基，R 1表示未取代的苯基; 被一个或多个具有1至4个碳原子的烷基或乙酰基取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷氧基烷基; 茚满基; 或具有式“IMAGE”的酰氧基烷基，其中R 2表示氢原子或甲基，R 3表示具有1至5个碳原子的烷基（例如甲基，正丙基，异丁基，叔丁基等） ，基团），具有1至4个碳原子的烷氧基，苯基，被一个或多个具有1至4个碳原子的烷基取代的苯基，具有1至4个碳原子的烷氧基或卤素原子 （例如氯，溴，碘等原子）或其中烷基部分具有1〜3个碳原子的芳烷基，其可用作抗高血压剂，制备5-烷氧基 - 吡啶甲酸酯的方法和 含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物。

公开(公告)号：US4122171A

公开(公告)日：1978-10-24

申请号：US786468

申请日：1977-04-11

申请人： Tetsutaro Niizato ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Takemi Koeda ,  Taro Niida

发明人： Tetsutaro Niizato ,  Takashi Tsuruoka ,  Shigeharu Inouye ,  Takemi Koeda ,  Taro Niida

IPC分类号： C07D211/78 ,  A61K31/445 ,  A61K31/455 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/7036 ,  A61P13/02 ,  A61P15/00 ,  A61P31/04 ,  C07H15/22 ,  A61K31/71

CPC分类号： A61K31/70 ,  A61K31/445

摘要： D-glucaro-1,5-lactam and its pharmaceutically acceptable salts are useful as an agent of protecting against renal failure or damage induced by administration of aminoglycosidic antibiotics.

摘要翻译： D-葡聚糖-1,5-内酰胺及其药学上可接受的盐可用作防止肾衰竭或通过施用氨基糖苷类抗生素诱导的损伤的药剂。

公开(公告)号：US4647572A

公开(公告)日：1987-03-03

申请号：US545061

申请日：1983-10-25

申请人： Shigeharu Inouye ,  Masao Koyama ,  Keinosuke Miyauchi ,  Takashi Tsuruoka ,  Fumio Kai ,  Kuniomi Matsumoto ,  Taro Niida ,  Eiichi Akita

发明人： Shigeharu Inouye ,  Masao Koyama ,  Keinosuke Miyauchi ,  Takashi Tsuruoka ,  Fumio Kai ,  Kuniomi Matsumoto ,  Taro Niida ,  Eiichi Akita

IPC分类号： A01N43/713 ,  A61K31/41 ,  A61P17/00 ,  C07D257/04

CPC分类号： C07D257/04 ,  A01N43/713

摘要： Triiodoallyl- or iodopropargyl-substituted tetrazole compounds which are prepared by reacting substituted tetrazole compound with reactive derivatives of corresponding triiodoallyl alcohol or iodopropargyl alcohol or by iodinating propargyltetrazole compounds, as well as antibacterial and antifungal compositions for medicinal, agricultural and industrial fields which contain as active ingredient said tetrazole compounds.

摘要翻译： 通过使取代的四唑化合物与相应的三碘代烯丙醇或碘代炔丙醇的反应性衍生物或通过碘化炔丙基四唑化合物反应制备的三碘代烯丙基或碘炔丙基取代的四唑化合物，以及含有活性的药用，农业和工业领域的抗菌和抗真菌组合物 成分说四唑化合物。