公开(公告)号：US4717767A

公开(公告)日：1988-01-05

申请号：US860317

申请日：1986-07-22

Applicant: Hiroshi Sadaki ,  Hiroyuki Imaizumi ,  Takashi Nagai ,  Kenji Takeda ,  Isao Myokan ,  Takihiro Inaba ,  Yasuo Watanabe ,  Yoshikazu Fukuoka ,  Shinzaburo Minami ,  Isamu Saikawa

Inventor： Hiroshi Sadaki ,  Hiroyuki Imaizumi ,  Takashi Nagai ,  Kenji Takeda ,  Isao Myokan ,  Takihiro Inaba ,  Yasuo Watanabe ,  Yoshikazu Fukuoka ,  Shinzaburo Minami ,  Isamu Saikawa

IPC: C07D241/18 ,  C07D405/04 ,  C07D501/18 ,  C07D501/46

CPC classification number: C07D405/04 ,  C07D241/18 ,  Y02P20/55

Abstract: This invention relates to a 7-amino-3-(pyrazinylmethyl)- or (pyridazinylmethyl)-cephalosporins of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents a group of the formula: ##STR2## in which R.sup.6 represents a hydrogen atom, a C.sub.1-5 alkyl group or a di-C.sub.1-5 alkylamino group; R.sup.13 represents a C.sub.1-5 alkyl group; and R.sup.28 represents an amino group.

Abstract translation: 本发明涉及下式的7-氨基-3-（吡嗪基甲基） - 或（哒嗪基甲基） - 头孢菌素，其中R 1表示氢原子或羧基保护基; R 2表示下式的基团：其中R 6表示氢原子，C 1-5烷基或二-C 1-5烷基氨基; R13表示C1-5烷基; R28表示氨基。

公开(公告)号：US4698352A

公开(公告)日：1987-10-06

申请号：US546165

申请日：1983-10-27

Applicant: Hirokazu Narita ,  Yoshinori Konishi ,  Jun Nitta ,  Shunjiro Misumi ,  Hideyoshi Nagaki ,  Isao Kitayama ,  Yoriko Nagai ,  Yasuo Watanabe ,  Nobuyuki Matsubara ,  Shinzaburo Minami ,  Isamu Saikawa

Inventor： Hirokazu Narita ,  Yoshinori Konishi ,  Jun Nitta ,  Shunjiro Misumi ,  Hideyoshi Nagaki ,  Isao Kitayama ,  Yoriko Nagai ,  Yasuo Watanabe ,  Nobuyuki Matsubara ,  Shinzaburo Minami ,  Isamu Saikawa

IPC: C07D213/63 ,  C07D209/20 ,  C07D211/90 ,  C07D213/55 ,  C07D213/80 ,  C07D215/14 ,  C07D215/38 ,  C07D215/40 ,  C07D249/08 ,  C07D307/81 ,  C07D317/66 ,  C07D333/24 ,  C07D333/28 ,  C07D333/60 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  C07D521/00 ,  A61K31/455 ,  C07D401/02 ,  C07D405/02

CPC classification number: C07D213/80 ,  C07D209/20 ,  C07D211/90 ,  C07D213/55 ,  C07D215/14 ,  C07D215/38 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D307/81 ,  C07D317/66 ,  C07D333/24 ,  C07D333/28 ,  C07D333/60 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D417/04 ,  Y02P20/55

Abstract: This invention relates to a novel 4-oxo-1,4-dihydronicotinic acid derivative ##STR1## or a salt thereof, wherein R.sup.1 is hydrogen or carboxyl-protecting group;R.sup.2 is substituted phenyl and naphthyl, or a substituted or unsubstituted heterocyclic group; andR.sup.3 is haloalkyl, aminoalkyl, or substituted or unsubstituted alkenyl, phenylalkenyl, naphthylalkenyl, phenylalkyl, naphthylalkyl, phenylalkynyl, naphthylalkynyl, heterocyclic alkyl, heterocyclic alkenyl, phenyl, naphthyl, cycloalkyl, cycloalkenyl, carboxylic acyl, iminoalkyl, heterocyclic or bridged hydrocarbon, which has a broad antibacterial spectrum and a low toxicity, and are useful for treatment of diseases of human beings and animals, to a process for producing the same and to an antibacterial agent containing the same.

Abstract translation: 本发明涉及一种新的4-氧代-1,4-二氢烟酸衍生物或其盐，其中R 1是氢或羧基保护基; R2是取代的苯基和萘基，或取代或未取代的杂环基团; 苯基，萘基烷基，苯基炔基，萘基炔基，杂环烷基，杂环烯基，苯基，萘基，环烷基，环烯基，羧酰基，亚氨基烷基，杂环或桥连烃，其中R 3为卤代烷基，氨基烷基或取代或未取代的链烯基 具有广泛的抗菌谱和低毒性，并且可用于治疗人和动物的疾病，其制备方法和含有它们的抗菌剂。

公开(公告)号：US4656287A

公开(公告)日：1987-04-07

申请号：US753942

申请日：1985-07-11

Applicant: Hiroyuki Imaizumi ,  Takihiro Inaba ,  Seishi Morita ,  Ryuko Takeno ,  Yoshiharu Murotani ,  Hirohiko Fukuda ,  Junichi Yoshida ,  Kiyoshi Tanaka ,  Shuntaro Takano ,  Isamu Saikawa

Inventor： Hiroyuki Imaizumi ,  Takihiro Inaba ,  Seishi Morita ,  Ryuko Takeno ,  Yoshiharu Murotani ,  Hirohiko Fukuda ,  Junichi Yoshida ,  Kiyoshi Tanaka ,  Shuntaro Takano ,  Isamu Saikawa

IPC: C07D501/48 ,  C07D277/20 ,  C07D277/40 ,  C07D501/06 ,  C07D501/46 ,  C07D501/56 ,  C07D277/38

CPC classification number: C07D277/587

Abstract: This invention relates to a novel aminothiazole intermediate for production of a cephalosporin of antibiotic activity.

Abstract translation: 本发明涉及用于产生抗生素活性的头孢菌素的新的氨基噻唑中间体。

公开(公告)号：US4477666A

公开(公告)日：1984-10-16

申请号：US348272

申请日：1982-02-12

Applicant: Takako Hori ,  Chosaku Yoshida ,  Yasuo Kiba ,  Ryuko Takeno ,  Joji Nakano ,  Jun Nitta ,  Sumiko Kishimoto ,  Shohachi Murakami ,  Hisatsugu Tsuda ,  Isamu Saikawa

Inventor： Takako Hori ,  Chosaku Yoshida ,  Yasuo Kiba ,  Ryuko Takeno ,  Joji Nakano ,  Jun Nitta ,  Sumiko Kishimoto ,  Shohachi Murakami ,  Hisatsugu Tsuda ,  Isamu Saikawa

IPC: A61K31/495 ,  A61P35/00 ,  C07D241/08 ,  C07D241/20 ,  C07D401/06 ,  C07D401/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D417/10 ,  C07D241/04

CPC classification number: C07D241/08

Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.

公开(公告)号：US4410522A

公开(公告)日：1983-10-18

申请号：US841608

申请日：1977-10-12

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Chosaku Yoshida ,  Okuta Takashima ,  Kaishu Momonoi ,  Seietsu Kuroda ,  Miwako Komatsu ,  Takashi Yasuda ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Chosaku Yoshida ,  Okuta Takashima ,  Kaishu Momonoi ,  Seietsu Kuroda ,  Miwako Komatsu ,  Takashi Yasuda ,  Yutaka Kodama

IPC: C07D241/08 ,  C07D499/00 ,  C07D501/20 ,  A61K31/545 ,  C07D501/56

CPC classification number: C07D241/08 ,  C07D499/00

Abstract: Novel penicillins and cephalosporins and non-toxic salts thereof, which contain a mono- or di-oxo- or thioxo-piperazino(thio)carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and a process for the preparation thereof.

Abstract translation: 新型青霉素和头孢菌素及其无毒盐，其在分子中含有一个或二个氧代或二硫代哌嗪子基（硫代）羰基氨基。 这些化合物是用于包括人在内的哺乳动物的有价值的抗菌化合物。 本公开涉及这些化合物及其制备方法。

公开(公告)号：US4385178A

公开(公告)日：1983-05-24

申请号：US331900

申请日：1981-12-17

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Kaishu Momonoi ,  Isamu Takakura ,  Seietsu Kuroda ,  Kiyoshi Tanaka ,  Kenshin Hayashi ,  Bunei Nagahashi ,  Chiaki Kutani

IPC: A61K20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/14 ,  C07D501/16 ,  C07D501/18 ,  C07D501/36 ,  C07D501/60

CPC classification number: C07D501/04

Abstract: This disclosure relates to a novel process for producing 7-(substituted)amino-3-substituted thiomethyl cephem carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

公开(公告)号：US4370316A

公开(公告)日：1983-01-25

申请号：US147530

申请日：1980-05-07

Applicant: Isamu Saikawa ,  Takashi Yasuda ,  Shohachi Murakami ,  Toyoo Maeda ,  Akira Yotsuji ,  Masahiro Takahata ,  Hisatsugu Tsuda ,  Hidetada Mikami ,  Hiroshi Sakai ,  Toshinori Ohashi

Inventor： Isamu Saikawa ,  Takashi Yasuda ,  Shohachi Murakami ,  Toyoo Maeda ,  Akira Yotsuji ,  Masahiro Takahata ,  Hisatsugu Tsuda ,  Hidetada Mikami ,  Hiroshi Sakai ,  Toshinori Ohashi

IPC: A61K35/64 ,  A61P31/04 ,  A61P35/00 ,  A61P37/04 ,  A61K35/58

CPC classification number: A61K35/64

Abstract: A method for treating a host mammal having a decreased immunity, comprising administering to said host mammal an immunostimulating effective amount of the deproteinized extract from the poison pouch contents of bee B-T, is disclosed.

Abstract translation: 一种用于治疗免疫力降低的宿主哺乳动物的方法，包括向所述宿主哺乳动物施用免疫刺激有效量的来自蜜蜂B-T的毒囊含量的去蛋白质提取物。

公开(公告)号：US4324783A

公开(公告)日：1982-04-13

申请号：US113065

申请日：1980-01-17

Applicant: Isamu Saikawa ,  Takashi Yasuda ,  Masaru Tai ,  Yutaka Takashita ,  Hiroshi Sakai ,  Michiko Mae ,  Masahiro Takahata ,  Susumu Mitsuhashi

Inventor： Isamu Saikawa ,  Takashi Yasuda ,  Masaru Tai ,  Yutaka Takashita ,  Hiroshi Sakai ,  Michiko Mae ,  Masahiro Takahata ,  Susumu Mitsuhashi

IPC: C07D499/68 ,  A61K31/43 ,  A61K31/545 ,  A61P31/04 ,  C07D499/64 ,  A61K35/00

CPC classification number: A61K31/43 ,  A61K31/545

Abstract: An antibacterial composition for medical use comprising 6-[D(-)-.alpha.-(4-ethyl-2,3-dioxo-1-piperazinylcarbonylamino)phenylacetamido]penicillanic acid or a pharmaceutically acceptable salt thereof and a .beta.-lactamase-inhibiting penicillin or cephalosporin. The composition exhibits synergistic effect which is much greater than the sum of antibacterial effects of each component used alone.

Abstract translation: 一种用于医疗用途的抗菌组合物，其包含6- [D（ - ） - α-（4-乙基-2,3-二氧代-1-哌嗪基羰基氨基）苯基乙酰胺基]青霉烷酸或其药学上可接受的盐和β-内酰胺酶抑制 青霉素或头孢菌素。 组合物显示出比单独使用的每种组分的抗菌作用的总和大得多的协同效应。

公开(公告)号：US4321265A

公开(公告)日：1982-03-23

申请号：US117784

申请日：1980-02-01

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masaru Tai ,  Yutaka Kodama

IPC: C07D295/20 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/57

CPC classification number: C07D295/20 ,  Y02P20/55

Abstract: A 7.alpha.-methoxycephalosporin represented by the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl-protecting group; R.sup.2 represents an organic group linked to the carbon atom through an oxygen or sulfur atom; R.sup.3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl or heterocyclic group, and a salt thereof. These compounds have a broad antibacterial spectrum, high resistance to .beta.-lactamase produced from bacteria, and an effective antibacterial activity against clinical isolates of bacteria.

Abstract translation: 由以下通式表示的7α-甲氧头孢菌素：其中R 1表示氢原子或羧基保护基; R2表示通过氧或硫原子与碳原子连接的有机基团; R3表示低级烷基; n为0,1或2; A表示氢原子或取代或未取代的烷基; B表示取代或未取代的烷基，环烷基，环烯基，环二烯基或杂环基，及其盐。 这些化合物具有广泛的抗菌谱，对细菌产生的β-内酰胺酶的高抗性，以及针对临床细菌分离株的有效抗菌活性。

公开(公告)号：US4200744A

公开(公告)日：1980-04-29

申请号：US845935

申请日：1977-10-27

Applicant: Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masuru Tai ,  Yutaka Kodama

Inventor： Isamu Saikawa ,  Shuntaro Takano ,  Hiroyuki Imaizumi ,  Isamu Takakura ,  Hirokazu Ochiai ,  Takashi Yasuda ,  Hideo Taki ,  Masuru Tai ,  Yutaka Kodama

IPC: C07D501/36 ,  C07D501/57

CPC classification number: C07D501/57

Abstract: Novel 7.alpha.-methoxy-cephalosporins and non-toxic salts thereof, which contain a di-oxo-piperazinyl-carbonylamino group in molecule. These compounds are valuable antibacterial compounds for use in mammals including man. This disclosure relates to such compounds and methods for producing the same.

Abstract translation: 新型7α-甲氧基头孢菌素及其无毒盐，其在分子中含有二 - 氧代 - 哌嗪基 - 羰基氨基。 这些化合物是用于包括人在内的哺乳动物的有价值的抗菌化合物。 本公开涉及这种化合物及其制备方法。