公开(公告)号：US4219554A

公开(公告)日：1980-08-26

申请号：US915873

申请日：1978-06-15

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 ,  C07D501/20 ,  A61K31/43 ,  C07D499/68

CPC classification number: C07D499/00 ,  C07D241/08

Abstract: Novel penicillins 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 antibacterial 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：US4199566A

公开(公告)日：1980-04-22

申请号：US913105

申请日：1978-06-06

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-[-)-.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 - [ - ） - α-（4-乙基-2,3-二氧代-1-哌嗪基羰基氨基）苯乙酰胺基]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：US4744985A

公开(公告)日：1988-05-17

申请号：US180040

申请日：1980-08-21

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 ,  A61K35/74

CPC classification number: C12R1/01 ,  C12P1/04

Abstract: Novel 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 lower warm-blooded animals. 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较低温血动物的癌性疾病。 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：US4667040A

公开(公告)日：1987-05-19

申请号：US753068

申请日：1985-07-09

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：US4591558A

公开(公告)日：1986-05-27

申请号：US619895

申请日：1984-08-06

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 ,  C12P19/26 ,  C12P21/00 ,  C12N1/20 ,  A61K37/00

CPC classification number: C12R1/01 ,  C12P1/04 ,  Y10S435/822

Abstract: Novel TF-2 substances having antitumor 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 beings. This disclosure concerns such substances and a process for preparing the same and an antitumor agent containing the same.

Abstract translation: 具有抗肿瘤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抗肿瘤剂。

公开(公告)号：US4547462A

公开(公告)日：1985-10-15

申请号：US523438

申请日：1983-08-16

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: C12P1/02 ,  A61K35/74 ,  A61K38/00 ,  A61P35/00 ,  A61P37/04 ,  C07G11/00 ,  C07K14/005 ,  C07K14/195 ,  C07K14/41 ,  C12P1/04 ,  C12P21/00 ,  C12R1/01 ,  C12P19/00

CPC classification number: A61K35/74 ,  C12P1/04 ,  Y10S435/822

Abstract: This invention relates to a process for producing a TF-500 substance having carcinostatic and immunostimulating activities, which comprises subjecting organisms belonging to the Fusobacterium genus to extraction treatment with a dialkyl sulfoxide and obtaining said TF-500 substance from the resulting extract.

Abstract translation: 本发明涉及制备具有制癌和免疫刺激活性的TF-500物质的方法，该方法包括使属于所述Fusobacterium属的生物体用二烷基亚砜进行提取处理，并从所得提取物中获得所述TF-500物质。

公开(公告)号：US4460774A

公开(公告)日：1984-07-17

申请号：US348271

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 ,  C07D403/12

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.

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酸加成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：US4129730A

公开(公告)日：1978-12-12

申请号：US759134

申请日：1977-01-13

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: C07D501/06 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D501/04 ,  C07D501/20 ,  C07D501/22 ,  C07D501/24 ,  C07D501/34 ,  C07D501/36 ,  C07D501/57

CPC classification number: C07D501/57 ,  Y02P20/55

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

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。 本公开涉及这些化合物。

公开(公告)号：US4110327A

公开(公告)日：1978-08-29

申请号：US732860

申请日：1976-10-15

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: C07D499/00 ,  C07D499/64 ,  C07D501/20 ,  C07D241/08 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12

CPC classification number: 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：US5144027A

公开(公告)日：1992-09-01

申请号：US707221

申请日：1991-05-24

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.about.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.

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，并且键差D代表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。