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1. 发明授权

US4393058A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US4393058A
公开(公告)日：1983-07-12
申请号：US188417
申请日：1980-09-18
申请人： Osamu Makabe , Yasushi Murai , Tuneo Okonogi , Masahiro Onodera , Yoshiyuki Koyama , Takashi Yoshida
发明人： Osamu Makabe , Yasushi Murai , Tuneo Okonogi , Masahiro Onodera , Yoshiyuki Koyama , Takashi Yoshida
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07C45/71 , C07D213/80 , C07D213/82 , C07D213/85 , C07D501/36
CPC分类号： C07D213/80 , C07C45/71 , C07D213/82 , C07D213/85
摘要： Cephalosporin compounds, intermediate compounds therefor, and processes for preparation thereof are described; the compounds have the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 can each represent hydrogen, a hydroxyl group, a lower alkoxy group, or a substituted or unsubstituted phenylalkoxy group; R.sub.3 represents hydrogen or a lower alkyl group; R.sub.4 represents hydrogen or a hydroxyl group; and R.sub.5 represents ##STR2## wherein R.sub.6 is hydrogen, a lower alkyl group, an aminoalkyl group, an aminoaralkyl group, a --(CH.sub.2).sub.n --SO.sub.3 Na group, or a --(CH.sub.2).sub.n --COR.sub.9 group [wherein R.sub.9 is a hydroxyl group, an OM group (wherein M is an alkali metal), an alkoxy group, or an ##STR3## group, (wherein R.sub.10 and R.sub.11, which may be the same or different, can represent hydrogen or an alkyl group), and n is 0 or an integer of from 1 to 4]; R.sub.7 is hydrogen, a lower alkyl group, an amino group, or a substituted or unsubstituted aryl group; and R.sub.8 represents hydrogen or a lower alkyl group; or, a pharmaceutically acceptable salt thereof.
摘要翻译：描述头孢菌素化合物，其中间体化合物及其制备方法; 化合物具有式（I）其中R 1和R 2各自表示氢，羟基，低级烷氧基或取代或未取代的苯基烷氧基; R3表示氢或低级烷基; R4代表氢或羟基; 其中R6为氢，低级烷基，氨基烷基，氨基烷基， - （CH2）n-SO3Na基或 - （CH2）n-COR9基[ 其中R 9为羟基，OM基（其中M为碱金属），烷氧基或基团（其中R10和R11可以相同或不同，表示氢或烷基组），n为0或1〜4的整数]。 R7是氢，低级烷基，氨基或取代或未取代的芳基; R8代表氢或低级烷基; 或其药学上可接受的盐。

2. 发明授权

US4331597A Penicillin compounds 失效
标题翻译：青霉素化合物
公开(公告)号：US4331597A
公开(公告)日：1982-05-25
申请号：US193317
申请日：1980-10-02
申请人： Osamu Makabe , Yasushi Murai , Tuneo Okonogi , Masahiro Onodera , Takashi Yoshida , Shunzo Fukatsu
发明人： Osamu Makabe , Yasushi Murai , Tuneo Okonogi , Masahiro Onodera , Takashi Yoshida , Shunzo Fukatsu
IPC分类号： A61K31/43 , A61P31/04 , C07D499/00 , C07D499/64 , C07D499/68 , C07D499/70
CPC分类号： C07D499/00
摘要： Penicillin compounds and methods for the production thereof are described, said penicillin compounds being represented by the formula (I) ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 each represents hydrogen, a lower alkyl group, a halogen atom, a lower alkoxy group, a hydroxyl group, or a substituted or unsubstituted phenylalkoxy group except that R.sub.1, R.sub.2, and R.sub.3 cannot all represent hydrogen simultaneously; R.sub.4 represents hydrogen or a lower alkyl group; and R.sub.5 represents hydrogen or a hydroxyl group.
摘要翻译：描述了青霉素化合物及其制备方法，所述青霉素化合物由式（I）表示：其中R 1，R 2和R 3各自表示氢，低级烷基，卤原子，低级烷氧基，羟基或取代或未取代的苯基烷氧基，除了R1，R2和R3不能全部同时代表氢; R4代表氢或低级烷基; R5表示氢或羟基。

3. 发明授权

US06441162B2 Crystalline substance of cefditoren pivoxyl and the production of the same 有权
标题翻译：头孢托仑的新型结晶物质及其生产
公开(公告)号：US06441162B2
公开(公告)日：2002-08-27
申请号：US09854462
申请日：2001-05-15
申请人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
发明人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： A crystalline substance of Cefditoren pivoxyl is provided which has a high purity and enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving an amorphous form of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous form well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.
摘要翻译：提供了新戊酸头孢托仑的结晶物质，其具有高纯度和增强的储存热稳定性。这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，该方法包括将无定形形式的新戊酰氧基头孢托仑溶解在能够将所述无定形形式溶解在其中的无水第一有机溶剂中，以及将所得溶液的第一有机溶剂组分通过具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后浓缩至15℃以下。减压下等。由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

4. 发明授权

US4970305A Crystalline dihydrochloride of cephalosporin derivative and a method for preparation thereof 失效
标题翻译：头孢菌素衍生物的结晶二盐酸盐及其制备方法
公开(公告)号：US4970305A
公开(公告)日：1990-11-13
申请号：US413915
申请日：1989-09-28
申请人： Tsuneo Okonogi , Yasushi Murai , Masahiro Onodera , Toshio Nishizuka , Yasuhiko Abat , Seiji Shibahara , Shigeharu Inouye
发明人： Tsuneo Okonogi , Yasushi Murai , Masahiro Onodera , Toshio Nishizuka , Yasuhiko Abat , Seiji Shibahara , Shigeharu Inouye
IPC分类号： C07D501/00 , A61K31/545 , C07D501/36
CPC分类号： C07D501/36 , Y02P20/55
摘要： The crystalline dihydrochloride of a specific cephalosporin derivative is stable to heat and retains its antibacterial activity even after storage over long periods at high temperature. The crystalline dihydrochloride can be obtained by removing protective groups from the cephalosporin derivative wherein the amino group and carboxy groups are protected and then crystallizing the cephalosporin derivative from a hydrochloric acid aqueous solution. The crystalline dihydrochloride is useful for pharmaceutical preparations.

5. 发明授权

US06294669B1 Crystalline substance of cefditoren pivoxyl and the production of the same 有权
标题翻译：头孢托仑的新型结晶物质及其生产
公开(公告)号：US06294669B1
公开(公告)日：2001-09-25
申请号：US09269109
申请日：1999-03-19
申请人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
发明人： Kiyoshi Yasui , Masahiro Onodera , Masamichi Sukegawa , Tatsuo Watanabe , Yuichi Yamamoto , Yasushi Murai , Katsuharu Iinuma
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： As a novel substance is provided such a new, crystalline substance of Cefditoren povoxyl which has a high purity and an enhanced thermal stability on storage. This crystalline Cefditoren pivoxyl may be prepared by a process comprising a step of dissolving amorphous substance of Cefditoren pivoxyl in an anhydrous, first organic solvent capable of dissolving said amorphous substance well therein, and steps of replacing the first organic solvent component of the resulting solution by an anhydrous alkanol of 1 to 5 carbon atoms as a second organic solvent, in such a manner that the firstly prepared solution of Cefditoren pivoxyl in the first organic solvent is mixed with a volume of the alkanol and then is concentrated below 15° C. under reduced pressure, and so on. Thereby, the process proceeds so as to produce a solution containing 50 mg/ml to 250 mg/ml of Cefditoren pivoxyl dissolved in the alkanol alone. From the latter solution, crystals of Cefditoren pivoxyl are induced to deposit by addition of water at a temperature of 0-10° C. The resulting admixture of the concentrated solution of Cefditoren pivoxyl in alkanol with added water and the deposited Cefditoren pivoxyl is then agitated 10° C. or below, to effect a complete crystallization of Cefditoren pivoxyl.
摘要翻译：作为一种新物质，提供了这样一种具有高纯度和增加的储存热稳定性的新型头孢托仑聚氧乙烯醚的结晶物质。这种结晶的头孢托仑新戊基可以通过包括以下步骤的方法来制备，所述方法包括将能够将所述无定形物质溶解在其中的无水的第一有机溶剂中溶解新戊酰氧基甲基头孢托仑的无定形物质，以及将所得溶液的第一有机溶剂组分置换为将具有1至5个碳原子的无水链烷醇作为第二有机溶剂，使得将首先制备的在第一有机溶剂中的新戊酰氧基头孢托仑的溶液与一定体积的链烷醇混合，然后在15℃以下浓缩减压等。由此，进行处理，从而产生溶解在单独的链烷醇中的含有50mg / ml〜250mg / ml的新戊酰氧基甲基头孢地托仑的溶液。从后一种溶液中，通过在0-10℃的温度下，通过加入水诱导新戊酸头孢托仑的晶体沉淀。然后搅拌所得的新戊酰氧基甲基头孢地托仑在链烷醇中与加入的水的混合物和沉积的新戊糖酯 10℃或更低，以实现新戊酰氧基甲基头孢托仑的完全结晶。

6. 发明授权

US06486149B2 Composition comprising a crystallographically stable, amorphous cephalosporin and processes for the preparation thereof 有权
公开(公告)号：US06486149B2
公开(公告)日：2002-11-26
申请号：US09991694
申请日：2001-11-26
申请人： Masahiro Onodera , Masamichi Sukegawa , Kiyoshi Yasui , Tatsuo Watanabe , Toyomi Sato , Yasushi Murai , Katsuharu Iinuma
发明人： Masahiro Onodera , Masamichi Sukegawa , Kiyoshi Yasui , Tatsuo Watanabe , Toyomi Sato , Yasushi Murai , Katsuharu Iinuma
IPC分类号： A61K31545
CPC分类号： C07D501/00 , A61K9/146 , A61K31/545 , A61K31/546 , Y10S514/96
摘要： Processes are provided for the preparation of orally administrable, yellow and powdery compositions essentially consisting of particles composed of a homogeneous mixture of an amorphous Cefditoren pivoxil substance with a water soluble high-molecular additive. These compositions can be produced by dissolving crystalline Cefditoren pivoxil substance and the water-soluble high-molecular additive in an aqueous solution of an acid, then neutralizing the resultant solution, to co-precipitate the product, and drying the thus precipitated product, followed by recovering the product in the form of the above-mentioned particles.

7. 发明授权

US06342493B1 Crystallographically stable amorphous cephalosporin compositions and process for producing the same 有权
标题翻译：晶体学稳定的无定型头孢菌素组合物及其制备方法
公开(公告)号：US06342493B1
公开(公告)日：2002-01-29
申请号：US09582937
申请日：2000-07-07
申请人： Masahiro Onodera , Masamichi Sukegawa , Kiyoshi Yasui , Tatsuo Watanabe , Toyomi Sato , Yasushi Murai , Katsuharu Iinuma
发明人： Masahiro Onodera , Masamichi Sukegawa , Kiyoshi Yasui , Tatsuo Watanabe , Toyomi Sato , Yasushi Murai , Katsuharu Iinuma
IPC分类号： A61K31545
CPC分类号： C07D501/00 , A61K9/146 , A61K31/545 , A61K31/546 , Y10S514/96
摘要： Processes are provided for the preparation of orally administrable, yellow and powdery compositions essentially consisting of particles composed of a homogeneous mixture of an amorphous Cefditoren pivoxil substance with a water soluble high-molecular additive. These compositions can be produced by dissolving crystalline Cefditoren pivoxil substance and the water-soluble high-molecular additive in an aqueous solution of an acid, then neutralizing the resultant solution, to co-precipitate the product, and drying the thus precipitated product, followed by recovering the product in the form of the above-mentioned particles.
摘要翻译：提供了制备可口服的黄色和粉末状组合物的方法，其基本上由由无定形头孢托仑匹酯与水溶性高分子添加剂的均匀混合物组成的颗粒组成。这些组合物可以通过将结晶性匹戊头孢托仑物质和水溶性高分子添加剂溶解在酸的水溶液中，然后中和所得溶液，使产物共沉淀并干燥沉淀的产物，然后以上述颗粒的形式回收产物。

8. 发明授权

US4898858A Cephalosporin derivatives and antibiotics containing the same 失效
标题翻译：头孢菌素衍生物和含有相同的抗生素
公开(公告)号：US4898858A
公开(公告)日：1990-02-06
申请号：US928955
申请日：1986-11-10
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/36
CPC分类号： C07D501/00
摘要： New cephalosporin derivatives of a general formula (I) and non-toxic salts and non-toxic esters thereof are provided: ##STR1## (wherein R represents an acyclic or cyclic lower alkyl group having 1-6 carbon atoms, which may optionally be substituted by a halogen atom; the steric configuration as asterisked (*) includes an optical-active (R)-form or (S)-form or an optical-inactive (RS)-form; n is 0 or 1, n.sup.1 is 0 to 3, n.sup.2 is 0 to 3; and when n.sup.1 is 0, n.sup.2 is 3; when n.sup.1 is 1, n.sup.2 is 2; when n.sup.1 is 2, n.sup.2 is 1; when n.sup.1 is 3, n.sup.2 is 0).The new derivatives of the formula (I) and non-toxic salts and esters thereof have high bactericidal activity with broad antibacterial spectra, and these are useful as active ingredients in bactericides.
摘要翻译：提供了通式（I）的新型头孢菌素衍生物及其无毒盐和无毒酯：其中R表示具有1-6个碳原子的无环或环状低级烷基，其可以任选地被卤素原子取代;星号（*）的空间构型包括光学活性（R）形式或（S）形式或光学非活性（RS）形式; n是0或 1，n1为0〜3，n2为0〜3，n2为0时，n2为3，n1为1时n2为2，n1为2时，n2为1，n1为3时，n2为0 ）。式（I）的新衍生物及其无毒盐和酯具有广泛的抗菌谱具有高杀菌活性，可用作杀菌剂中的活性成分。

9. 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。

10. 发明授权

US4810702A Antibacterial agent for mammal use comprising cephalosporin derivatives as an effective ingredient 失效
标题翻译：哺乳动物用抗菌剂包括头孢菌素衍生物作为有效成分
公开(公告)号：US4810702A
公开(公告)日：1989-03-07
申请号：US131779
申请日：1987-12-11
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
IPC分类号： A61K31/435 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
CPC分类号： C07D501/36
摘要： Cephalosporin compounds having 2-(2-aminothiazol-4-yl)-2{(1S)-carboxyethoxyimino}acetyl group on the side chain at the 7-position thereof and 1-ethylpyridinium-4-ylthiomethyl group on the side chain at the 3-position thereof or non-toxic salts thereof are excellent antibacterial agents for mammals including human. The cephalosporin derivatives have low toxicity.

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