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1. 发明授权

US4101658A Antibacterial hydrazono cephalosporins 失效
标题翻译：抗菌亚肼基头孢菌素
公开(公告)号：US4101658A
公开(公告)日：1978-07-18
申请号：US583696
申请日：1975-06-04
申请人： Mitsuru Yoshioka , Yuji Sendo , Koji Ishikura , Masayuki Murakami , Sadao Miyazaki
发明人： Mitsuru Yoshioka , Yuji Sendo , Koji Ishikura , Masayuki Murakami , Sadao Miyazaki
IPC分类号： A61K31/545 , C07D501/20
CPC分类号： C07D501/20 , Y02P20/55
摘要： Antibacterial cephalosporins of the following formula: ##STR1## WHEREIN A and B each is a hydrogen or an amino protecting group; X is a hydroxy or a carboxy protecting group; Y is a hydrogen, halogen, alkyl, alkoxy, or an alkylthio; R is a hydrogen or an alkyl; Z is a group of the formula ##STR2## (in which R.sup.1 and R.sup.2 are the same or different and are a hydrogen, optionally substituted hydrocarbon group, organic acyl, or a group of the formula ##STR3## respectively, in which M and M' are the same or different and are an oxygen or sulfur; R.sup.3 is a hydrocarbon group; R.sup.1 and R.sup.2 can be combined together directly or through a hetero atom); m is 0 or 1; and the broken line shows the presence of a double bond at position 2 or 3, preparable from the compounds shown by the above formula in which Z is an oxygen by treatment with a compound shown by the formula H.sub.2 Z; and pharmaceuticals containing these compounds.
摘要翻译：抗细菌头孢菌素如下：其中A和B各自为氢或氨基保护基; X是羟基或羧基保护基; Y是氢，卤素，烷基，烷氧基或烷硫基; R是氢或烷基; Z是式（IMA）（其中R 1和R 2相同或不同，分别为氢，任选取代的烃基，有机酰基或式“IMAGE”的基团）的基团，其中M和M “相同或不同，为氧或硫; R3为烃基; R1和R2可以直接或通过杂原子组合在一起; m为0或1; 虚线表示在上述式表示的化合物2或3中存在双键，其中Z为氧，通过用式H2Z表示的化合物处理; 和含有这些化合物的药物。

2. 发明授权

US3997528A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US3997528A
公开(公告)日：1976-12-14
申请号：US517483
申请日：1974-10-22
申请人： Mitsuru Yoshioka , Masayuki Murakami , Yuji Sendo , Sadao Miyazaki , Koji Ishikura
发明人： Mitsuru Yoshioka , Masayuki Murakami , Yuji Sendo , Sadao Miyazaki , Koji Ishikura
IPC分类号： C07D501/18 , A61D7/00 , A61K31/43 , A61K31/545 , C07D501/04 , C07D501/06 , C07D501/16 , C07D501/20 , C07D501/24 , C07D501/38 , C07D501/40 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/60
CPC分类号： C07D501/38 , C07D501/24 , Y02P20/55
摘要： Antibacterial cephalosporin compounds of the following formula: ##STR1## wherein A and B each is a hydrogen, organic or inorganic acyl, or A and B combined together are a diacyl group derived from a polybasic acid; Y is a hydrogen or methoxy; R is a hydrogen or lower alkyl; R' is a hydrogen, alkali metal, organic base group or easily removable protecting group; m is 0 or 1; Z is an optionally substituted guanylhydrazono group, preparable from the corresponding oxo compound or its reactive derivative by reacting with a guanylhyrazine of the formula H.sub.2 Z or its reactive derivative, or by some other reactions.
摘要翻译：下式的抗菌头孢菌素化合物：其中A和B各自为氢，有机或无机酰基，或A和B组合在一起的是由多元酸衍生的二酰基; Y是氢或甲氧基; R是氢或低级烷基; R'是氢，碱金属，有机碱基或易脱除的保护基; m为0或1; Z是任选取代的脒基亚肼基，其可通过与式H2Z或其反应性衍生物的鸟苷酸反应或通过一些其它反应与相应的氧代化合物或其反应性衍生物制备。

3. 发明授权

US3987039A 3-Oxyiminomethyl-cephalosporins 失效
标题翻译： 3-氧代二甲基环己酮
公开(公告)号：US3987039A
公开(公告)日：1976-10-19
申请号：US446112
申请日：1974-02-26
申请人： Mitsuru Yoshioka , Masayuki Murakami , Yuji Sendo
发明人： Mitsuru Yoshioka , Masayuki Murakami , Yuji Sendo
IPC分类号： C07D501/18 , A61K20060101 , A61K31/545 , C07C20060101 , C07D20060101 , C07D205/00 , C07D279/00 , C07D501/04 , C07D501/16 , C07D501/24 , C07D501/42 , C07D501/46 , C07D501/57 , C07D501/60
CPC分类号： C07D501/24 , C07D501/18 , Y02P20/55
摘要： An antibacterial 7-protected amino-3-oxyiminomethyl-3-cephem-4-carboxylic acid is prepared by the reaction of a 7-protected amino-3-formyl-3-cephem-4-carboxylic acid or its reactive derivatives with a hydroxylamine compound or its reactive derivatives, the process being more suitable for large scale production when coupled with fermentative production of a 3-hydroxymethyl-3-cephem-4-carboxylic acid followed by its direct oxidation.

4. 发明授权

US4053469A Intermediates for the preparation of 7-acylamino-3-oxyiminomethyl-3-cephem-4-carboxylic acids 失效
标题翻译：制备7-亚氨基-3-氧代亚氨基-3-CEPHEM-4-羧酸的中间体
公开(公告)号：US4053469A
公开(公告)日：1977-10-11
申请号：US673882
申请日：1976-04-05
申请人： Mitsuru Yoshioka , Masayuki Murakami , Yuji Sendo
发明人： Mitsuru Yoshioka , Masayuki Murakami , Yuji Sendo
IPC分类号： C07D501/18
CPC分类号： C07D501/24 , C07D501/18
摘要： An antibacterial 7-protected amino-3-oxyiminomethyl-3-cephem-4-carboxylic acid is prepared by the reaction of a 7-protected amino-3-formyl-3-cephem-4-carboxylic acid or its reactive derivatives with a hydroxylamine compound or its reactive derivatives, the process being more suitable for large scale production when coupled with fermentative production of a 3-hydroxymethyl-3-cephem-4-carboxylic acid followed by its direct oxidation.

5. 发明授权

US4092474A Cephalosporins having a metaloxy group in 3-substituent 失效
标题翻译：在3-取代基中具有金属氧基的头孢菌素
公开(公告)号：US4092474A
公开(公告)日：1978-05-30
申请号：US637477
申请日：1975-12-03
申请人： Mitsuru Yoshioka , Yuji Sendo , Masayuki Murakami
发明人： Mitsuru Yoshioka , Yuji Sendo , Masayuki Murakami
IPC分类号： A61K31/545 , C07D501/04 , C07D501/14 , C07D501/16 , C07D501/18 , C07D501/24 , C07D501/26 , C07D501/28 , C07D501/34 , C07D501/60
CPC分类号： C07D501/04 , C07D501/14 , C07D501/18 , C07D501/24
摘要： Antibacterial cephalosporins of the formula ##STR1## wherein Acyl is an acyl group; R is a hydrogen or methoxy, R.sup.1 is a hydrocarbyl group containing 1 to 8 carbon atoms; R.sup.2 is a hydrogen, alkali metal, alkaline earth metal, halo-alkaline earth metal group or acyl group containing 1 to 12 carbon atoms; R.sup.3 is a hydrogen, pharmaceutically acceptable cation, or ester residue; or when R.sup.2 and R.sup.3 are both hydrogens, they can be combined to form a lactone ring; the broken line shows a double bond at position 2 or 3; and n is zero or one, and processes for preparing them by the reaction of the compound shown by above formula in which R.sup.1 and R.sup.2 combined to show a bond, with a Grignard type or organometallic reagent to introduce R.sup.1, followed by acylation, oxidation, reduction, double bond migration, or other reactions.
摘要翻译：其中酰基是酰基的式“IMAGE”的抗菌头孢菌素; R是氢或甲氧基，R 1是含有1至8个碳原子的烃基; R2是含有1〜12个碳原子的氢，碱金属，碱土金属，卤代 - 碱土金属或酰基; R3是氢，药学上可接受的阳离子或酯残基; 或当R 2和R 3均为氢时，它们可以组合形成内酯环; 虚线显示位置2或3的双键; 并且n为0或1，并且通过上式所示的化合物（其中R 1和R 2结合表示键）与格利雅类型或有机金属试剂反应以制备它们的方法以引入R1，然后酰化，氧化，还原，双键迁移或其他反应。

6. 发明授权

US4223132A Selective conversion of benzyl alcohol carboxylates to the free acid form 失效
标题翻译：将苄醇羧酸盐选择性转化为游离酸形式
公开(公告)号：US4223132A
公开(公告)日：1980-09-16
申请号：US818597
申请日：1977-07-25
申请人： Teruji Tsuji , Mitsuru Yoshioka , Takahiro Kataoka , Yuji Sendo , Shoichi Hirai , Takashi Maeda , Wataru Nagata
发明人： Teruji Tsuji , Mitsuru Yoshioka , Takahiro Kataoka , Yuji Sendo , Shoichi Hirai , Takashi Maeda , Wataru Nagata
IPC分类号： C07D487/04 , C07D499/04 , C07D501/04
CPC分类号： C07D501/04 , C07D487/04 , Y02P20/55
摘要： A process for preparing free carboxylic acids which comprises treating an optionally substituted benzyl ester with a Lewis acid, preferably in the presence of a cation acceptor, followed by hydrolysis, if required.
摘要翻译：制备游离羧酸的方法，其包括用路易斯酸处理任选取代的苄基酯，优选在阳离子受体存在下，然后如果需要水解。

7. 发明授权

US5360798A Aminooxypyrrolidinylthiocarbapenem compounds 失效
标题翻译：氨氧基吡咯烷基硫代碳青霉烯化合物
公开(公告)号：US5360798A
公开(公告)日：1994-11-01
申请号：US896669
申请日：1992-06-10
申请人： Yuji Sendo , Kii Makoto
发明人： Yuji Sendo , Kii Makoto
IPC分类号： A61K31/40 , A61K31/397 , A61K31/401 , A61K31/407 , A61P31/04 , C07D207/12 , C07D477/00 , C07D477/20 , C07D487/04 , A61F31/40
CPC分类号： C07D477/20 , C07D207/12 , Y02P20/55
摘要： An antibacterial aminooxypyrrolidinylthiocarbapenem I, its production from the corresponding carbapenem V and thiol VI, its pharmaceutical formulation, and its use or combating bacteria are presented. ##STR1## (wherein R is optionally substituted amino; R.sup.1 is hydrogen or 1C to 5C alkyl; R.sup.2 is hydrogen or a conventional hydroxy protective group; R.sup.3 is hydrogen or an imino protective group or imino substituent; R.sup.4 is 1C to 5C alkylene; and R.sup.5 is hydrogen or a conventional carboxy protective group; X is a leaving group; R.sup.6 is hydrogen or a thiol protective group; and wavy lines each shows a bond in R or S configuration).
摘要翻译：提出了抗生素氨基氧吡咯烷基硫代碳青霉烯I，其相应的碳青霉烯V和硫醇VI的生产，其药物制剂及其用途或对抗细菌。R是任选取代的氨基; R1是氢或1C至5C烷基; R2是氢或常规的羟基保护基; R3是氢或亚氨基保护基或亚氨基取代基; R4为1〜5个亚烷基; R5是氢或常规的羧基保护基; X是离职团体 R6是氢或硫醇保护基; 波浪线各呈现R或S构型的键）。

8. 发明授权

US5539102A Production method for sulfamide 失效
标题翻译：磺酰胺的生产方法
公开(公告)号：US5539102A
公开(公告)日：1996-07-23
申请号：US19105
申请日：1993-02-18
申请人： Yuji Sendo , Makoto Kii , Yasuhiro Nishitani , Tadashi Irie , Yutaka Nishino
发明人： Yuji Sendo , Makoto Kii , Yasuhiro Nishitani , Tadashi Irie , Yutaka Nishino
IPC分类号： B01J31/02 , C07B61/00 , C07C307/04 , C07D207/08 , C07D207/12 , C07D207/26 , C07D207/273 , C07D333/20 , C07D477/02 , C07D477/14 , C07D477/20 , C07D501/00 , C07D501/04 , C07D501/16 , C07D501/22 , C07D501/46 , C08L63/00 , C07D499/00
CPC分类号： C07D207/273 , C07C307/04 , C07D207/12 , C07D477/02 , C07D477/14 , C07D477/20 , C07D501/00 , C08L63/00 , Y02P20/55
摘要： The method for producing a sulfamide according to the present invention includes the step of reacting an alcohol and an oxycarbonylsulfamide compound in the presence of a trivalent phosphorus compound and an azodicarboxylic acid derivative. In one embodiment, the sulfamide is represented by Formula I, the alcohol is represented by Formula II, and the oxycarbonylsulfamide compound is represented by Formula III:R.sup.3 NHSO.sub.2 NR.sup.1 R.sup.2 (I)wherein R.sup.1 and R.sup.2 are independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, aryl, a heterocyclic group, and alkyl substituted with the heterocyclic group, respectively, said heterocyclic group being selected from the group consisting of pyranosyl, furanosyl, piperidinyl, pyrrolidinyl, an azetidinone ring, a cephem ring, a penem ring, and a carbapenem ring; R.sup.3 is selected from the group consisting of alkyl, alkenyl, alkynyl, aralkyl, a heterocyclic group, alkyl substituted with the heterocyclic group, and pyrrolidinylmethyl, said heterocyclic group being selected from the group consisting of pyranosyl, furanosyl, piperidinyl, pyrrolidinyl, an azetidinone ring, a cephem ring, a penem ring, and a carbapenem ring;R.sup.3 OH (II)wherein R.sup.3 is defined as above;R.sup.4 OOC--NHSO.sub.2 NR.sup.1 R.sup.2 (III)wherein R.sup.1 and R.sup.2 are defined as above; and R.sup.4 is a carboxy protecting group.
摘要翻译：根据本发明的磺酰胺的制备方法包括在三价磷化合物和偶氮二羧酸衍生物的存在下使醇和氧羰基磺酰胺化合物反应的步骤。在一个实施方案中，磺酰胺由式I表示，醇由式II表示，氧羰基磺酰胺化合物由式III表示：R3NHSO2NR1R2（I）其中R1和R2独立地选自氢，烷基，环烷基，烯基，炔基，芳烷基，芳基，杂环基和被杂环基取代的烷基，所述杂环基分别选自吡喃糖基，呋喃糖基，哌啶基，吡咯烷基，氮杂环丁酮环，头孢烯环，青铜戒指和碳青霉烯环; R 3选自烷基，烯基，炔基，芳烷基，杂环基，被杂环基取代的烷基和吡咯烷基甲基，所述杂环基选自吡喃糖基，呋喃糖基，哌啶基，吡咯烷基，氮杂环丁酮环，Cephem环，penem环和碳青霉烯环; R3OH（II）其中R3如上定义; R4OOC-NHSO2NR1R2（III）其中R1和R2如上定义; R4是羧基保护基。

9. 发明授权

US5523415A Intermediaties for aminooxypyrrolidinylthiocarbapenem compounds 失效
标题翻译：氨基氧吡咯烷基硫代碳青霉烯化合物的介质
公开(公告)号：US5523415A
公开(公告)日：1996-06-04
申请号：US273979
申请日：1994-07-12
申请人： Yuji Sendo , Makoto Kii
发明人： Yuji Sendo , Makoto Kii
IPC分类号： A61K31/40 , A61K31/397 , A61K31/401 , A61K31/407 , A61P31/04 , C07D207/12 , C07D477/00 , C07D477/20 , C07D207/00
CPC分类号： C07D477/20 , C07D207/12 , Y02P20/55
摘要： An antibacterial aminooxypyrrolidinylthiocarbapenem I, its production from the corresponding carbapenem V and thiol VI, its pharmaceutical formulation, and its use for combating bacteria are presented. ##STR1## (wherein R is optionally substituted amino; R.sup.1 is hydrogen or 1C to 5C alkyl; R.sup.2 is hydrogen or a conventional hydroxy protective group; R.sup.3 is hydrogen or an imino protective group or imino substituent; R.sup.4 is 1C to 5C alkylene; and R.sup.5 is hydrogen or a conventional carboxy protective group; X is a leaving group; R.sup.6 is hydrogen or a thiol protective group; and wavy lines each shows a bond in R or S configuration).
摘要翻译：提出了抗生素氨基氧吡咯烷基硫代碳青霉烯I，其相应的碳青霉烯类V和硫醇VI的生产，其药物制剂及其对抗细菌的用途。 VI（其中R为任选取代的氨基; R 1为氢或1C至5C烷基; R 2为氢或常规羟基保护基; R 3为氢或亚氨基保护基或亚氨基取代基 R 4为1〜5的亚烷基，R 5为氢或常规的羧基保护基; X为离去基团; R6为氢或硫醇保护基;波浪线各自表示R或S构型的键）。

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