公开(公告)号：US4736026A

公开(公告)日：1988-04-05

申请号：US879540

申请日：1986-06-24

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

CPC classification number: C07D277/587

Abstract: The invention relates to a process for producing a cephalosporin of the formula ##STR1## by reacting the compound ##STR2## with the compound ##STR3## in the presence of boron trifluoride or a complex thereof.

Abstract translation: 本发明涉及通过在三氟化硼或其复合物存在下使化合物＆lt; IMAGE＆gt;（顺式异构体）与化合物＆lt; IMAGE＆gt;反应来制备式“头孢菌素”（顺式异构体）的方法。

公开(公告)号：US4704459A

公开(公告)日：1987-11-03

申请号：US819821

申请日：1986-01-17

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

CPC classification number: C07D213/74 ,  C07D213/78 ,  C07D213/80 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/04 ,  C07D471/04 ,  Y02P20/55

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：US4673738A

公开(公告)日：1987-06-16

申请号：US654681

申请日：1984-09-26

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: This invention relates to novel 7-(substituted or unsubstituted amino)-3-substituted methyl-.DELTA..sup.3 -cephem-4-carboxylic acids in which a substituted or unsubstituted 1,2,4-triazolyl or 2-(1,2,3,4-tetrazolyl) group attaches to the exomethylene group at the 3-position of the cephem ring through a carbon-nitrogen bond. These cephalosporins are useful intermediates for producing various novel cephalosporins. Also, this invention concerns a process for producing a compound represented by the formula: ##STR1## which comprises reacting a compound represented by the formula: ##STR2## with an optionally substituted triazole or tetrazole in the presence of an acid or a complex of the acid in an organic solvent at 0.degree. to 80.degree. C.

Abstract translation: 本发明涉及新的7-（取代或未取代的氨基）-3-取代的甲基-D-三头孢烯-4-羧酸，其中取代或未取代的1,2,4-三唑基或2-（1,2,3 ，4-四唑基）基团通过碳 - 氮键连接在头孢烯环的3-位上的外亚甲基基团。 这些头孢菌素是生产各种新型头孢菌素的有用中间体。 此外，本发明涉及一种制备由下式表示的化合物的方法：该方法包括使下式表示的化合物与任选取代的三唑或四唑在酸或其复合物的存在下反应： 酸在有机溶剂中于0〜80℃

公开(公告)号：US4618606A

公开(公告)日：1986-10-21

申请号：US552468

申请日：1983-11-16

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 ,  A61K31/545

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

Abstract: The invention relates to antibiotic compounds 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## R.sup.3 represents a hydrogen atom or an alkoxy group; R.sup.4 represents a hydrogen atom or a halogen atom; R.sup.5 represents a hydrogen atom or a protected or unprotected amino group; A represents a group of the formula, --CH.sub.2 -- or a group of the formula, ##STR3## or a group of the formula, ##STR4## and the bond means that the compound may be a synisomer or an anti-isomer or a mixture thereof.

Abstract translation: 本发明涉及下式的抗生素化合物：其中R 1表示氢原子或羧基保护基; R 2表示下式的基团：R 3表示氢原子或烷氧基; R4表示氢原子或卤素原子; R5表示氢原子或被保护或未被保护的氨基; A代表下式的基团-CH 2 - 或下式的基团或下式的基团和键意指化合物可以是异构体或反式异构体或混合物 其中。

公开(公告)号：US4563534A

公开(公告)日：1986-01-07

申请号：US504317

申请日：1983-06-14

Applicant: Hiroshi Sadaki ,  Hiroyuki Imaizumi ,  Kenji Takeda ,  Takihiro Inaba ,  Ryuko Takeno ,  Seishi Morita ,  Tetsuya Kajita ,  Isamu Saikawa

Inventor： Hiroshi Sadaki ,  Hiroyuki Imaizumi ,  Kenji Takeda ,  Takihiro Inaba ,  Ryuko Takeno ,  Seishi Morita ,  Tetsuya Kajita ,  Isamu Saikawa

IPC: C07C20060101 ,  C07C45/63 ,  C07C45/79 ,  C07C45/82 ,  C07C49/16 ,  C07D277/28 ,  C07D277/38 ,  C07D277/40 ,  C07D277/42 ,  C07D277/44 ,  C07D277/46 ,  C07D277/48

CPC classification number: C07C45/63 ,  C07C45/79 ,  C07C45/82 ,  C07C49/16 ,  C07D277/40 ,  C07D277/48 ,  Y02P20/55

Abstract: This invention relates to a novel process for producing a 2-(2-aminothiazol-4-yl)glyoxylic acid derivative or a salt thereof which are useful in producing a cephalosporin antibiotic, and to intermediates for said derivative and salt and a process for producing the intermediates.

Abstract translation: 本发明涉及可用于制备头孢菌素抗生素的2-（2-氨基噻唑-4-基）乙醛酸衍生物或其盐的新方法，以及所述衍生物和盐的中间体及其制备方法 中间体。

公开(公告)号：US4477437A

公开(公告)日：1984-10-16

申请号：US347871

申请日：1982-02-11

Applicant: Kenzo Tamai ,  Isamu Saikawa ,  Takashi Yasuda ,  Shohachi Murakami ,  Toyoo Maeda ,  Hisatsugu Tsuda ,  Hiroshi Sakai ,  Masatoshi Sugita ,  Yoshiko Yamamoto ,  Hisashi Minami ,  Takako Hori

Inventor： Kenzo Tamai ,  Isamu Saikawa ,  Takashi Yasuda ,  Shohachi Murakami ,  Toyoo Maeda ,  Hisatsugu Tsuda ,  Hiroshi Sakai ,  Masatoshi Sugita ,  Yoshiko Yamamoto ,  Hisashi Minami ,  Takako Hori

IPC: C12P1/04 ,  A61K31/715 ,  C08B37/00

CPC classification number: C12R1/01 ,  C12P1/04

Abstract: Novel TF-2 substances having carcinostatic and immunostimulating activity, which are obtained from a culture or its supernatant fluid prepared by culturing bacteria belonging to Fusobacterium genus. Said substances are useful for the treatment of cancerous diseases of the mammals including human being. This disclosure concerns such substances and a process for preparing the same and a carcinostatic agent containing the same.

Abstract translation: 具有制癌和免疫刺激活性的新型TF-2物质，其通过培养属于Fusobacterium属的细菌制备的培养物或其上清液获得。 所述物质可用于治疗包括人在内的哺乳动物的癌性疾病。 本公开涉及这些物质及其制备方法和含有该物质的制癌剂。

公开(公告)号：US4444753A

公开(公告)日：1984-04-24

申请号：US431563

申请日：1982-09-30

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 ,  A61K35/56

CPC classification number: A61K35/64

Abstract: A composition comprising a component obtained by deproteinizing an extract from the poison pouch contents of bee has an immunostimulating activity, a carcinostatic activity, an effect of enhancing the antibacterial activity of an antibacterial substance and an effect of enhancing the carcinostatic activity of a carcinostatic substance. This invention is directed to a carcinostatic, immunostimulating and antibacterial agent comprising said composition.

Abstract translation: 包含通过从蜜毒毒囊含量中提取物脱蛋白获得的成分的组合物具有免疫刺激活性，制癌活性，增强抗菌物质的抗菌活性的作用和增强制癌物质的制癌活性的作用。 本发明涉及包含所述组合物的制癌，免疫刺激和抗菌剂。

公开(公告)号：US4379152A

公开(公告)日：1983-04-05

申请号：US39904

申请日：1979-05-17

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 ,  C07D501/22 ,  C07D501/26 ,  A61K31/545

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.

公开(公告)号：US4327097A

公开(公告)日：1982-04-27

申请号：US47818

申请日：1979-06-12

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 ,  C07D499/64 ,  A61K31/495 ,  C07D499/70

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 have been prepared. These compounds are valuable anti-bacterial compounds for use in mammals including man. A process for the preparation of the compounds has also been discovered.

Abstract translation: 已经制备了含有单 - 或二 - 氧代或硫代 - 哌嗪子基（硫代）羰基氨基的新型青霉素和头孢菌素及其无毒盐。 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。 还已经发现了制备化合物的方法。

公开(公告)号：US4317907A

公开(公告)日：1982-03-02

申请号：US874637

申请日：1978-02-02

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.

Abstract translation: 本公开涉及一种用于生产7-（取代的）氨基-3-取代的硫代甲基头孢霉酸的新方法，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。