公开(公告)号：US4874856A

公开(公告)日：1989-10-17

申请号：US86138

申请日：1987-08-17

申请人： Seiji Iimura ,  Yoshio Abe ,  Jun Okumura ,  Takayuki Naito ,  Hajime Kamachi

发明人： Seiji Iimura ,  Yoshio Abe ,  Jun Okumura ,  Takayuki Naito ,  Hajime Kamachi

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/34 ,  C07D501/46

CPC分类号： C07D501/22 ,  C07D501/24

摘要： This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, or lower acyl, R.sup.3 is hydrogen, or lower alkanoyloxy, andR.sup.4 is hydrogen, 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl, 1-(ethoxycarbonyloxy)ethyl,1-(pivaloyloxy)ethyl, 1-(cyclohexylacetoxy)ethyl, or 1-(cyclohexyloxycarbonyloxy) ethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art. The acids (R.sup.4 is hydrogen) are useful as intermediates for making the esters.

摘要翻译： 本发明提供了具有通式为：其中R2为氢或低级酰基，R3为氢或低级烷酰氧基，R4为氢的通式为“IMAGE”+ TR“IMA”的新型头孢菌酸及其酯，5-甲基-2-氧代 乙基，1-（环己基乙酰氧基）乙基或1-（环己基氧基羰基氧基）乙基）。 这些化合物，特别是酯可用作广谱抗生素，用于治疗和预防哺乳动物感染性疾病以及本领域已知的其它目的。 酸（R4是氢）可用作制备酯的中间体。

公开(公告)号：US4708955A

公开(公告)日：1987-11-24

申请号：US748359

申请日：1985-06-24

申请人： Seiji Iimura ,  Yoshio Abe ,  Jun Okumura ,  Takayuki Naito ,  Hajime Kamachi

发明人： Seiji Iimura ,  Yoshio Abe ,  Jun Okumura ,  Takayuki Naito ,  Hajime Kamachi

IPC分类号： C07D501/20 ,  A61K20060101 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07C20060101 ,  C07D20060101 ,  C07D277/28 ,  C07D277/40 ,  C07D277/42 ,  C07D417/12 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/22 ,  C07D501/24 ,  C07D501/26 ,  C07D501/34

CPC分类号： C07D501/22 ,  C07D501/24

摘要： This invention provides novel cephalosporanic acids and esters thereof having the general formula ##STR1## wherein R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cyclo(lower)alkyl or acyl, R.sup.3 is hydrogen, lower alkyl, lower alkoxy, lower alkanoyloxy, andR.sup.4 is hydrogen, pivaloyloxymethyl, acetoxymethyl, 1-acetoxyethyl, 5-methyl-2-oxo-1, 3-dioxolen-4-ylmethyl or 4-glycyloxybenzoyloxymethyl. These compounds, especially esters, are useful as broad spectrum antibiotics in the treatment and prevention of infectious diseases of mammals, and for other purposes known in the art.

摘要翻译： 本发明提供了具有通式“IMAGE”的新型头孢菌酸及其酯，其中R2为氢，低级烷基，低级烯基，低级炔基，环（低级）烷基或酰基，R3为氢，低级烷基，低级烷氧基，低级烷酰氧基 ，R4为氢，新戊酰氧基甲基，乙酰氧基甲基，1-乙酰氧基乙基，5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基甲基或4-甘氨酰氧基苯甲酰氧基甲基。 这些化合物，特别是酯可用作广谱抗生素，用于治疗和预防哺乳动物感染性疾病以及本领域已知的其它目的。

公开(公告)号：US4151352A

公开(公告)日：1979-04-24

申请号：US877132

申请日：1978-02-13

申请人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi ,  Seiji Iimura ,  Hideaki Hoshi ,  Masahisa Oka

发明人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi ,  Seiji Iimura ,  Hideaki Hoshi ,  Masahisa Oka

IPC分类号： C07D217/24 ,  C07D333/24 ,  C07D487/04 ,  C07D495/04 ,  C07D501/18 ,  C07D501/36

CPC分类号： C07D487/04 ,  C07D217/24 ,  C07D333/24 ,  C07D495/04

摘要： Certain 7-acylamido-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. A preferred embodiment was 7-[o-(methylaminomethyl)phenylacetamido]-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acid.

公开(公告)号：US4198506A

公开(公告)日：1980-04-15

申请号：US22408

申请日：1979-03-21

申请人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi ,  Seiji Iimura ,  Hideaki Hoshi ,  Masahisa Oka

发明人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi ,  Seiji Iimura ,  Hideaki Hoshi ,  Masahisa Oka

IPC分类号： C07D217/24 ,  C07D333/24 ,  C07D487/04 ,  C07D495/04

CPC分类号： C07D487/04 ,  C07D217/24 ,  C07D333/24 ,  C07D495/04

摘要： Certain 7-acylamido-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. A preferred embodiment was 7-[o-(methylaminomethyl)phenylacetamido]-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acid.

摘要翻译： 某些7-酰基酰氨基-3-（2-羧基烷基-2,3-二氢 - 三唑并[4,3-b]哒嗪-3-酮-6-基硫甲基）-3-头孢烯-4-羧酸及其盐 合成了4-羧基的易水解酯，发现其具有良好的水溶性。 优选的实施方案是7- [O-（甲基氨基甲基）苯基乙酰氨基] -3-（2-羧基烷基-2,3-二氢 - 三唑并[4,3-b]哒嗪-3-酮基）硫基甲基）-3 - 头孢-4-羧酸。

公开(公告)号：US4082912A

公开(公告)日：1978-04-04

申请号：US784885

申请日：1977-04-05

申请人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi ,  Seiji Iimura ,  Hideaki Hoshi ,  Masahisa Oka

发明人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi ,  Seiji Iimura ,  Hideaki Hoshi ,  Masahisa Oka

IPC分类号： C07D217/24 ,  C07D333/24 ,  C07D487/04 ,  C07D495/04 ,  C07D501/18 ,  C07D501/36 ,  C07D501/20 ,  A61K31/545

CPC分类号： C07D487/04 ,  C07D217/24 ,  C07D333/24 ,  C07D495/04

摘要： Certain 7-acylamido-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acids and their salts and easily hydrolyzed esters of the 4-carboxyl group were synthesized and found to be potent antibacterial agents which exhibited good aqueous solubility. A preferred embodiment was 7-[o-(methylaminomethyl)phenylacetamido]-3-(2-carboxyalkyl-2,3-dihydro-s-triazolo[4,3-b]pyridazin-3-on-6-ylthiomethyl)-3-cephem-4-carboxylic acid.

摘要翻译： 某些7-酰基酰氨基-3-（2-羧基烷基-2,3-二氢 - 三唑并[4,3-b]哒嗪-3-酮-6-基硫甲基）-3-头孢烯-4-羧酸及其盐 合成了4-羧基的易水解酯，发现其具有良好的水溶性。 优选的实施方案是7- [O-（甲基氨基甲基）苯基乙酰氨基] -3-（2-羧基烷基-2,3-二氢 - 三唑并[4,3-b]哒嗪-3-酮基）硫基甲基）-3 - 头孢-4-羧酸。

公开(公告)号：US5410029A

公开(公告)日：1995-04-25

申请号：US209687

申请日：1994-03-10

申请人： Shimpei Aburaki ,  Tetsuro Yamasaki ,  Toshikazu Oki ,  Seiji Iimura ,  Hajime Kamachi ,  Hideo Kamei ,  Takayuki Naito

发明人： Shimpei Aburaki ,  Tetsuro Yamasaki ,  Toshikazu Oki ,  Seiji Iimura ,  Hajime Kamachi ,  Hideo Kamei ,  Takayuki Naito

IPC分类号： C07H15/24 ,  A61K31/70 ,  A61K31/7028 ,  A61K31/7034 ,  A61K31/704 ,  A61P31/04 ,  C07C231/12 ,  C07C235/84 ,  C07H15/244 ,  C07H15/252

CPC分类号： C07H15/244 ,  C07C235/84 ,  C07C2103/90

摘要： The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.

摘要翻译： 本发明涉及普拉德霉素的中性糖衍生物，它们作为抗真菌剂的用途，其制备方法及其合成中间体。

公开(公告)号：US5227370A

公开(公告)日：1993-07-13

申请号：US802020

申请日：1991-12-03

申请人： Hajime Kamachi ,  Seiji Iimura ,  Satsuki Okuyama ,  Shimpei Aburaki ,  Takayuki Naito ,  Yasutsugu Ueda ,  Leonard B. Crast, Jr. ,  Amarendra B. Mikkilineni

发明人： Hajime Kamachi ,  Seiji Iimura ,  Satsuki Okuyama ,  Shimpei Aburaki ,  Takayuki Naito ,  Yasutsugu Ueda ,  Leonard B. Crast, Jr. ,  Amarendra B. Mikkilineni

IPC分类号： C07H15/244

CPC分类号： C07H15/244

摘要： The present invention provides pradimicin analogs which exhibit improved water solubility relative to parent compounds. These novel agents are useful in treatment of fungal infections.

摘要翻译： 本发明提供了相对于母体化合物表现出改善的水溶性的普拉迪霉素类似物。 这些新型药剂可用于治疗真菌感染。

公开(公告)号：US5126336A

公开(公告)日：1992-06-30

申请号：US572518

申请日：1990-08-23

申请人： Kiyoto Imae ,  Hajime Kamachi ,  Shinji Masuyoshi ,  Seiji Iimura ,  Takayuki Naito

发明人： Kiyoto Imae ,  Hajime Kamachi ,  Shinji Masuyoshi ,  Seiji Iimura ,  Takayuki Naito

IPC分类号： A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/00 ,  C07D501/24

CPC分类号： C07D501/00

摘要： This invention relates to novel cephalosporin derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, a straight, branched, or cyclic lower alkyl group having up to six carbon atoms or a radical of the formula ##STR2## in which R.sup.3 and R.sup.4 are each independently hydrogen, methyl or ethyl, or R.sup.3 and R.sup.4, taken together with the carbon atom to which they are attached, may be a cycloalkylidene ring containing from 3 to 5 carbon atoms;R.sup.2 is a radical selected from the group consisting of ##STR3## wherein R.sup.5 is hydrogen or acetyl; R.sup.6, R.sup.7 and R.sup.8 each are independently C.sub.1-5 alkyl; n is 1 or 2; and y is 1 to 5.In another aspect, this invention relates to compounds of formula I and their nontoxic pharmaeutically acceptable salts, physiologically hydrolyzable esters or solvates.Representative compounds of this invention were selected for testing and were shown to display potent antibacterial activity.

公开(公告)号：US5837828A

公开(公告)日：1998-11-17

申请号：US378201

申请日：1995-05-02

申请人： Shimpei Aburaki ,  Tetsuro Yamasaki ,  Toshikazu Oki ,  Seiji Iimura ,  Hajime Kamachi ,  Hideo Kamei ,  Takayuki Naito

发明人： Shimpei Aburaki ,  Tetsuro Yamasaki ,  Toshikazu Oki ,  Seiji Iimura ,  Hajime Kamachi ,  Hideo Kamei ,  Takayuki Naito

IPC分类号： C07H15/252 ,  C07H1/00 ,  C07H15/24

CPC分类号： C07H15/252

摘要： The present invention concerns neutral sugar derivatives of pradimicins, their use as antifungal agents, methods for their preparation, and intermediates for their synthesis.

公开(公告)号：US3985738A

公开(公告)日：1976-10-12

申请号：US473040

申请日：1974-05-24

申请人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi

发明人： Takayuki Naito ,  Jun Okumura ,  Hajime Kamachi

IPC分类号： C07D501/20 ,  C07D501/36

摘要： 7-(D-.alpha.-Hydroxy-2-arylacetamido)-3-(tetrazolo-[4,5-b]pyridazin-6-ylthiomethyl)-3-cephem-4-carboxylic acids and their nontoxic, pharmaceutically acceptable salts are valuable as antibacterial agents and are particularly valuable as therapeutic agents in poultry and animals, including man, in the treatment of infectious diseases caused by many Gram-positive and Gram-negative bacteria.

摘要翻译： 7-（D-α-羟基-2-芳基乙酰胺基）-3-（四唑并[4,5-b]哒嗪-6-基硫甲基）-3-头孢烯-4-羧酸及其无毒的药学上可接受的盐是有价值的 作为抗菌剂，并且作为包括人在内的家禽和动物的治疗剂在治疗由许多革兰氏阳性和革兰氏阴性菌引起的感染性疾病中是特别有价值的。