公开(公告)号：US3981865A

公开(公告)日：1976-09-21

申请号：US586015

申请日：1975-06-11

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

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

IPC: C07D499/00 ,  C07D499/44 ,  C07D499/48 ,  C07D499/64 ,  C07D499/68 ,  C07D499/66 ,  C07D499/70

CPC classification number: C07D499/00

Abstract: Novel bis-type penicillins containing a (thio)acylureido group in the molecule, which are valuable antibacterial compounds for use in mammals including a human being.This disclosure relates to such compounds and a process for the preparation thereof.

Abstract translation: 在分子中含有（硫代）酰基脲基的新型双型青霉素，其是用于哺乳动物（包括人）的有价值的抗菌化合物。

公开(公告)号：US5011973A

公开(公告)日：1991-04-30

申请号：US352610

申请日：1989-05-15

Applicant: Yasuyuki Suzuki ,  Noboru Takagawa ,  Mikio Kawabata ,  Mariko Hayashi ,  Akiko Takagi ,  Takako Wakamiya ,  Isamu Saikawa

Inventor： Yasuyuki Suzuki ,  Noboru Takagawa ,  Mikio Kawabata ,  Mariko Hayashi ,  Akiko Takagi ,  Takako Wakamiya ,  Isamu Saikawa

IPC: A61K31/14 ,  A61K31/185 ,  A61K31/225 ,  A61P1/00 ,  C07C20060101 ,  C07C67/00 ,  C07C69/66 ,  C07C213/02 ,  C07C217/08 ,  C07C219/06 ,  C07C301/00 ,  C07C303/22 ,  C07C303/32 ,  C07C309/35

CPC classification number: C07C213/10

Abstract: The process for producing bischoline-disulfonate derivatives of Formula (I) ##STR1## useful for enhancing the digestive function comprising reacting, in the presence of an organic solvent, a trimethylammonium salt derivative of Formula (II) ##STR2## wherein R.sup.1 and R.sup.2 are individually lower alkyl and X is a group removable by a disulfonic acid of Formula (III)R(SO.sub.3 H).sub.2 (III)wherein R is a naphthylene, or an organic base salt of said acid.

Abstract translation: 用于生产用于增强消化功能的式（I）的二萜类 - 二磺酸衍生物的方法，其包括在有机溶剂存在下使式（II）的三甲基铵盐衍生物（II） ）其中R 1和R 2各自为低级烷基，X为可由式（III）的二磺酸R（SO 3 H）2（III）除去的基团，其中R为亚萘基或所述酸的有机碱盐。

公开(公告)号：US4851535A

公开(公告)日：1989-07-25

申请号：US67264

申请日：1987-06-29

Applicant: Yozo Todo ,  Tetsuo Yamafuji ,  Katsuyuki Nagumo ,  Isao Kitayama ,  Hideyoshi Nagaki ,  Mikako Miyajima ,  Yoshinori Konishi ,  Hirokazu Narita ,  Shuntaro Takano ,  Isamu Saikawa

Inventor： Yozo Todo ,  Tetsuo Yamafuji ,  Katsuyuki Nagumo ,  Isao Kitayama ,  Hideyoshi Nagaki ,  Mikako Miyajima ,  Yoshinori Konishi ,  Hirokazu Narita ,  Shuntaro Takano ,  Isamu Saikawa

IPC: C07D213/74 ,  C07D213/78 ,  C07D213/80 ,  C07D401/04 ,  C07D471/04 ,  C07D521/00 ,  C07D213/30 ,  C07D213/32 ,  C07D401/12

CPC classification number: C07D213/74 ,  C07D213/78 ,  C07D213/80 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D471/04

Abstract: This invention relates to a process for industrially producing a 1-substituted aryl-1,4-dihydro-4-oxonaphthyridine derivative and a salt thereof which are useful as an antibacterial agent, and also to intermediates therefor and processes for producing the intermediates.

Abstract translation: 本发明涉及用作工业生产用作抗菌剂的1-取代芳基-1,4-二氢-4-氧代萘啶衍生物及其盐的方法，还涉及其中间体及其制备方法。

公开(公告)号：US4614819A

公开(公告)日：1986-09-30

申请号：US652012

申请日：1984-09-19

Applicant: Takashi Nagai ,  Hirokazu Ochiai ,  Takihiro Inaba ,  Isao Myokan ,  Hiroshi Sadaki ,  Isamu Saikawa

Inventor： Takashi Nagai ,  Hirokazu Ochiai ,  Takihiro Inaba ,  Isao Myokan ,  Hiroshi Sadaki ,  Isamu Saikawa

IPC: C07D501/46 ,  A61K31/545 ,  C07D277/20 ,  C07D501/04 ,  C07D501/06 ,  C07D501/20 ,  C07D501/24 ,  C07D501/59 ,  C07F9/6539 ,  C07D501/22 ,  C07D501/36

CPC classification number: C07D277/587 ,  C07C327/00 ,  C07F9/6539 ,  Y02P20/55

Abstract: This invention relates to a novel process for producing a useful cephalosporin which comprises reacting a thiolo ester compound with a 7-aminocephalosporin in the presence of boron trifluoride or a complex compound thereof. This process enables the cephalosporin to be produced with a high purity in a high yield.

Abstract translation: 本发明涉及一种生产有用的头孢菌素的新方法，其包括在三氟化硼或其络合物的存在下使硫代酯化合物与7-氨基头孢菌素反应。 该方法能够以高产率以高纯度生产头孢菌素。

公开(公告)号：US4489072A

公开(公告)日：1984-12-18

申请号：US304912

申请日：1981-09-23

Applicant: Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

Inventor： Hiroshi Sadaki ,  Hirokazu Narita ,  Hiroyuki Imaizumi ,  Yoshinori Konishi ,  Takihiro Inaba ,  Tatsuo Hirakawa ,  Hideo Taki ,  Masaru Tai ,  Yasuo Watanabe ,  Isamu Saikawa

IPC: C07D501/24 ,  A61K31/545 ,  C07D20060101 ,  C07D501/04 ,  C07D501/18 ,  C07D501/20 ,  C07D501/38 ,  C07D501/40 ,  C07D501/46 ,  C07D501/56 ,  C07D501/57

CPC classification number: C07D501/46 ,  A61K31/545 ,  C07D501/38 ,  C07D501/56 ,  C07D501/57

Abstract: Novel cephalosporins which has attached to the exomethylene group at the 3-position of the cephem ring a substituted or unsubstituted aryl, acylamino, aromatic heterocyclic, triazolyl or tetrazolyl group, said aromatic heterocyclic group being attached through a carbon-carbon bond and said triazolyl or tetrazolyl group being attached through a carbon-nitrogen bond, and has the following group attached to the amino group at the 7-position: ##STR1## wherein A represents a group of the formula, --CH.sub.2 -- or a group of the formula ##STR2## in which R.sup.5 represents a hydrogen atom or an alkyl group, and the bond represents syn or anti isomer or their mixture; R.sup.3 represents a hydrogen or halogen atom; and R.sup.4 represents a hydrogen atom or an amino group which may be protected or substituted. These cephalosporins have a broad antibacterial spectrum, are stable against .beta.-lactamase produced by bacteria, have a low toxicity, and are well absorbed when administered orally or parenterally.This invention relates to such novel cephalosporins, processes for producing said cephalosporins, intermediates for producing said cephalosporins, and a process for producing said intermediates.

Abstract translation: 在头孢烯环的3位连接到外亚甲基的新型头孢菌素是取代或未取代的芳基，酰氨基，芳族杂环，三唑基或四唑基，所述芳族杂环基通过碳 - 碳键连接，所述三唑基或 四唑基通过碳 - 氮键连接，并且具有与7-位上的氨基连接的下列基团：其中A表示下式的基团：-CH 2 - 或式 其中R 5表示氢原子或烷基，并且该键表示顺式或反式异构体或其混合物; R3表示氢或卤素原子; R4表示氢原子或可被保护或取代的氨基。 这些头孢菌素具有广泛的抗菌谱，对细菌产生的β-内酰胺酶是稳定的，具有低毒性，并且当口服或肠胃外给药时被良好吸收。 本发明涉及这种新型头孢菌素，生产所述头孢菌素的方法，用于生产所述头孢菌素的中间体，以及生产所述中间体的方法。

公开(公告)号：US4459407A

公开(公告)日：1984-07-10

申请号：US345055

申请日：1982-02-02

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: C07D241/08 ,  C07D403/10 ,  A61K31/495 ,  A61K31/505 ,  C07D403/12

CPC classification number: C07D241/08 ,  Y10S514/908

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

Abstract translation: 由下式表示的1-（4-氨基苄基）-2,3-二氧代哌嗪衍生物及其盐具有优异的制癌活性，但毒性低。 因此，所述化合物可用作药物，也可用作中间体。

公开(公告)号：US4436921A

公开(公告)日：1984-03-13

申请号：US169457

申请日：1980-07-16

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 ,  C07D401/00

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：US4312986A

公开(公告)日：1982-01-26

申请号：US54917

申请日：1979-07-05

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: A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/16 ,  C07D501/18 ,  C07D501/28 ,  C07D501/36 ,  C07D501/57 ,  C07D501/60

CPC classification number: C07D501/04 ,  C07D501/16 ,  C07D501/18

Abstract: This disclosure relates to a novel process for producing 7-(substituted)-amino-3-substituted thiomethyl-.DELTA..sup.3 -cephem-4-carboxylic acids which are intermediate products of cephalosporins being valuable antibacterial compounds for use in mammals including man.

Abstract translation: 本公开涉及一种用于生产7-（取代的） - 氨基-3-取代的硫代甲基-Detta 3-头孢烯-4-羧酸的新方法，其是头孢菌素的中间产物，其是用于包括人在内的哺乳动物的有价值的抗菌化合物。

公开(公告)号：US4304909A

公开(公告)日：1981-12-08

申请号：US69545

申请日：1979-08-24

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

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

IPC: A61K31/54 ,  A61K31/545 ,  C07C20060101 ,  C07D20060101 ,  C07D501/04 ,  C07D501/12 ,  C07D501/36 ,  C07D501/46

CPC classification number: C07D501/36

Abstract: The N,N-dimethylacetamide adduct of 7-[D(-)-.alpha.-(4-ethyl-2,3-dioxo-1-piperazinecarboxamido)-.alpha.-(4-hydroxyphenyl)acetamido]-3-[5-(1-methyl-1,2,3,4-tetrazolyl)thiomethyl]-.DELTA..sup.3 -cephem-4-carboxylic acid, a process for the production thereof, and a process for producing said acid and a pharmaceutically acceptable salt thereof through said adduct.

Abstract translation: 7- [D（ - ） - α-（4-乙基-2,3-二氧代-1-哌嗪甲酰氨基）-α-（4-羟基苯基）乙酰氨基] -3- [5-（ 1-甲基-1,2,3,4-四唑基）硫基] - 三唑-3-头孢烯-4-羧酸，其制备方法，以及通过所述方法制备所述酸及其药学上可接受的盐的方法 加合物

公开(公告)号：US4990508A

公开(公告)日：1991-02-05

申请号：US337656

申请日：1989-04-13

Applicant: Hirokazu Narita ,  Yozo Todo ,  Jun Nitta ,  Hiroyasu Takagi ,  Fumihiko Iino ,  Mikako Miyajima ,  Yoshikazu Fukuoka ,  Isamu Saikawa

Inventor： Hirokazu Narita ,  Yozo Todo ,  Jun Nitta ,  Hiroyasu Takagi ,  Fumihiko Iino ,  Mikako Miyajima ,  Yoshikazu Fukuoka ,  Isamu Saikawa

IPC: A61K31/535 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61K31/54 ,  A61P31/04 ,  C07D20060101 ,  C07D471/04 ,  C07D471/06 ,  C07D471/10 ,  C07D498/04 ,  C07D498/06 ,  C07D513/04 ,  C07D513/06

CPC classification number: C07D471/06 ,  C07D513/06 ,  Y02P20/55

Abstract: This invention relates to a novel pyridone carboxylic acid derivative having a substituted or unsubstituted cyclopropyl group at the 10-position of pyridobenzoxazine, pyridobenzothiazine or pyridoquinoxaline and a salt thereof, a process for the production thereof and an antibacterial agent comprising the same.

Abstract translation: 本发明涉及在吡啶并苯并恶嗪10位具有取代或未取代的环丙基基团的吡啶甲酸羧酸衍生物及其盐，其制备方法和含有它们的抗菌剂。