公开(公告)号：US5559225A

公开(公告)日：1996-09-24

申请号：US209484

申请日：1994-03-14

Applicant: Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

Inventor： Shigeto Negi ,  Motosuke Yamanaka ,  Kanemasa Katsu ,  Isao Sugiyama ,  Yuuki Komatu ,  Atsushi Kamata ,  Akihiko Tsuruoka ,  Yoshimasa Machida

IPC: A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D20060101 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06 ,  C07D501/18 ,  C07D501/26 ,  C07D501/28 ,  C07D501/34 ,  C07D501/36

CPC classification number: C07D501/00

Abstract: A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms, or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.4 denotes a carboxyl or protected carboxyl group; or a pharmaceutically acceptable salt thereof; and a process for the preparation thereof; as well as an antibacterial composition containing the above cephem compound.

Abstract translation: 由下式（1）表示的7-酰基-3-取代氨基甲酰氧基头孢烯化合物：其中A表示-CH =或-N =基团; R1表示羟基，低级烷氧基或被保护的羟基; R2和R3相同或不同，分别表示低级烷基，羟基取代的低级烷基，氨基甲酰取代的低级烷基或氰基取代的低级烷基，R2是氢原子，R3是低级烷氧基或烷基 任选地被一个或多个卤素原子取代，或者“IMAGE”是指含有一个氮原子或吗啉基的4-6元杂环基，所述杂环基或吗啉基任选被一个或多个低级烷基 ，羟基和/或羟基取代的低级烷基; R4表示羧基或被保护的羧基; 或其药学上可接受的盐; 及其制备方法; 以及含有上述头孢烯化合物的抗菌组合物。

公开(公告)号：US5527948A

公开(公告)日：1996-06-18

申请号：US402569

申请日：1995-03-13

Applicant: Makoto Okita ,  Hiroshi Shirota ,  Masayuki Tanaka ,  Toshihiko Kaneko ,  Katsuya Tagami ,  Shigeki Hibi ,  Yasushi Okamoto ,  Seiichiro Nomoto ,  Takeshi Suzuki ,  Kenichi Chiba ,  Masaki Goto ,  Ryoichi Hashida ,  Hideki Ono ,  Hideto Ohhara ,  Hideki Sakurai ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

Inventor： Makoto Okita ,  Hiroshi Shirota ,  Masayuki Tanaka ,  Toshihiko Kaneko ,  Katsuya Tagami ,  Shigeki Hibi ,  Yasushi Okamoto ,  Seiichiro Nomoto ,  Takeshi Suzuki ,  Kenichi Chiba ,  Masaki Goto ,  Ryoichi Hashida ,  Hideki Ono ,  Hideto Ohhara ,  Hideki Sakurai ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

IPC: C07C39/225 ,  C07C43/215 ,  C07C43/23 ,  C07C43/30 ,  C07C43/313 ,  C07C43/315 ,  C07C45/00 ,  C07C45/29 ,  C07C45/30 ,  C07C45/51 ,  C07C45/54 ,  C07C45/59 ,  C07C45/63 ,  C07C45/71 ,  C07C47/57 ,  C07C47/575 ,  C07C49/83 ,  C07C49/84 ,  C07C59/68 ,  C07C69/157 ,  C07F7/18 ,  C07C69/76 ,  C07C49/115

CPC classification number: C07F7/1852 ,  C07C39/225 ,  C07C43/215 ,  C07C43/23 ,  C07C43/30 ,  C07C43/313 ,  C07C43/315 ,  C07C45/00 ,  C07C45/298 ,  C07C45/30 ,  C07C45/305 ,  C07C45/513 ,  C07C45/54 ,  C07C45/59 ,  C07C45/63 ,  C07C45/71 ,  C07C47/57 ,  C07C47/575 ,  C07C49/83 ,  C07C49/84 ,  C07C59/68

Abstract: Naphthalene derivatives of the formula: ##STR1## wherein R.sup.1, represents a hydrogen atom, a lower alkyl group or an acyl group; R.sup.2 independently represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a cycloalkyl group, a cycloalkylalkyl group, a hydroxyl group, an aryl group which may be substituted, an arylalkyl group whose aryl group may be substituted, a heteroaryl group, or a heteroaryllakyl group; R.sup.3 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, an aryl group which may have a substituent, an arylalkyl group whose aryl group may be substituted, an arylalkenyl group whose aryl group may be substituted, a cycloalkyl group, an alkoxyalkyl group, a heteroaryl group, a heteroarylalkyl group, a carboxyl group, a carboxyalkyl group, an aminoalkyl group, or a cyano group; R.sup.6 is C.sub.1-6 alkyl; and m is 0 or an integer of from 1 to 2 useful in treating autoimmune diseases are disclosed.

Abstract translation: 下式的萘衍生物：其中R 1，表示氢原子，低级烷基或酰基; R2独立地表示氢原子，低级烷基，低级烷氧基，卤素原子，环烷基，环烷基烷基，羟基，可被取代的芳基，芳基可以被取代的芳基烷基 ，杂芳基或杂芳基烷基; R 3表示氢原子，低级烷基，低级烯基，可以具有取代基的芳基，可以被取代芳基的芳基烷基，可以被芳基取代的芳基烯基，环烷基， 烷氧基烷基，杂芳基，杂芳基烷基，羧基，羧基烷基，氨基烷基或氰基; R6是C1-6烷基; 并且公开了m为0或可用于治疗自身免疫性疾病的1〜2的整数。

公开(公告)号：US5482937A

公开(公告)日：1996-01-09

申请号：US318971

申请日：1994-10-06

Applicant: Kazuo Okano ,  Shuhei Miyazawa ,  Richard S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Shimomura ,  Osamu Asano ,  Hiroyuki Yoshimura ,  Mitsuaki Miyamoto ,  Yoshimori Sakuma ,  Kenzo Muramoto ,  Hiroshi Obaishi ,  Koukichi Harada ,  Hajime Tsunoda ,  Satoshi Katayama ,  Kouji Yamada ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

Inventor： Kazuo Okano ,  Shuhei Miyazawa ,  Richard S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Shimomura ,  Osamu Asano ,  Hiroyuki Yoshimura ,  Mitsuaki Miyamoto ,  Yoshimori Sakuma ,  Kenzo Muramoto ,  Hiroshi Obaishi ,  Koukichi Harada ,  Hajime Tsunoda ,  Satoshi Katayama ,  Kouji Yamada ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

IPC: C07D495/14 ,  C07D495/22 ,  C07F9/6561 ,  A61K31/55

CPC classification number: C07D495/14 ,  C07F9/6561

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are useful in the pharmaceutical field, especially in treating allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract translation: 以下给定式的三唑并-1,4-二氮杂化合物及其药理学上可接受的盐可用于制药领域，特别是用于治疗过敏性疾病。 其中R1和R2是氢或烷基，R3是氢或卤素，R4是氢或烷基，X是-OCO-，Y是环烷基，环烷基烷基，炔基等。

公开(公告)号：US5476864A

公开(公告)日：1995-12-19

申请号：US129302

申请日：1993-11-10

Applicant: Kazuo Okano ,  Osamu Asano ,  Naoyuki Shimomura ,  Tetsuya Kawahara ,  Shinya Abe ,  Shuhei Miyazawa ,  Mitsuaki Miyamoto ,  Hiroyuki Yoshimura ,  Koukichi Harada ,  Junsaku Nagaoka ,  Tsutomu Kawata ,  Tsutomu Yoshimura ,  Hiromasa Suzuki ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

Inventor： Kazuo Okano ,  Osamu Asano ,  Naoyuki Shimomura ,  Tetsuya Kawahara ,  Shinya Abe ,  Shuhei Miyazawa ,  Mitsuaki Miyamoto ,  Hiroyuki Yoshimura ,  Koukichi Harada ,  Junsaku Nagaoka ,  Tsutomu Kawata ,  Tsutomu Yoshimura ,  Hiromasa Suzuki ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

IPC: C07D213/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  A61K31/44 ,  C07D213/02

CPC classification number: C07D213/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12

Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##

公开(公告)号：US5468740A

公开(公告)日：1995-11-21

申请号：US386533

申请日：1995-02-10

Applicant: Kazuo Okano ,  Shuhei Miyazawa ,  Richard S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Shimomura ,  Osamu Asano ,  Hiroyuki Yoshimura ,  Mitsuaki Miyamoto ,  Yoshimori Sakuma ,  Kenzo Muramoto ,  Hiroshi Obaishi ,  Koukichi Harada ,  Hajime Tsunoda ,  Satoshi Katayama ,  Kouji Yamada ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

Inventor： Kazuo Okano ,  Shuhei Miyazawa ,  Richard S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Shimomura ,  Osamu Asano ,  Hiroyuki Yoshimura ,  Mitsuaki Miyamoto ,  Yoshimori Sakuma ,  Kenzo Muramoto ,  Hiroshi Obaishi ,  Koukichi Harada ,  Hajime Tsunoda ,  Satoshi Katayama ,  Kouji Yamada ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

IPC: C07D495/14 ,  C07D495/22 ,  C07F9/6561 ,  A61K31/675 ,  C07F9/00

CPC classification number: C07D495/14 ,  C07F9/6561

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract translation: 公开了以下给定式的三唑并-1,4-二氮杂化合物及其药理学上可接受的盐，尤其适用于过敏性疾病。 其中R 1和R 2是氢或烷基，R 3是氢或卤素，R 4是氢或烷基，X是-OCO - ， - NHCO-，-CO-或其它，Y是环烷基， 环烷基烷基，炔基等。

公开(公告)号：US5373000A

公开(公告)日：1994-12-13

申请号：US861717

申请日：1992-04-01

Applicant: Yoshimasa Machida ,  Takashi Kamiya ,  Shigeto Negi ,  Toshihiko Naito ,  Yuuki Komatu ,  Seiichiro Nomoto ,  Isao Sugiyama ,  Hiroshi Yamauchi

Inventor： Yoshimasa Machida ,  Takashi Kamiya ,  Shigeto Negi ,  Toshihiko Naito ,  Yuuki Komatu ,  Seiichiro Nomoto ,  Isao Sugiyama ,  Hiroshi Yamauchi

IPC: A61K31/545 ,  C07D501/24 ,  C07D501/34

CPC classification number: C07D501/24

Abstract: A cephalosporin derivative represented by the formula: ##STR1## wherein R.sub.1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R.sub.2 and R.sub.3 are the same or different lower alkyl group, R.sub.4 represents a substituted lower alkyl or amino group;a group which may be substituted and which is represented by the following formula: ##STR3## where R.sub.5 represents a lower alkyl group; or a group of the following formula: ##STR4## where R.sub.5 is as defined above, R.sub.6 represents a hydroxyl lower alkyl or carboxyl group, or its pharmacologically acceptable salt, and a process for preparing the same, as well as an antibacterial agent containing the same.

Abstract translation: 由下式表示的头孢菌素衍生物：其中R 1表示低级烷基，A选自：下式的基团：其中R 2和R 3是相同或不同的低级烷基，R 4表示 取代的低级烷基或氨基; 可以被取代并由下式表示的基团：其中R 5表示低级烷基; 或下式的基团：其中R 5如上定义，R 6表示羟基低级烷基或羧基或其药理学上可接受的盐，以及其制备方法，以及含有 相同。

公开(公告)号：US5304553A

公开(公告)日：1994-04-19

申请号：US68349

申请日：1993-05-28

Applicant: Kazuo Okano ,  Shuhei Miyazawa ,  Richar S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Shimomura ,  Osamu Asano ,  Hiroyuki Yoshimura ,  Mitsuaki Miyamoto ,  Yoshimori Sakuma ,  Kenzo Muramoto ,  Hiroshi Obaishi ,  Koukichi Harada ,  Hajime Tsunoda ,  Satoshi Katayama ,  Kouji Yamada ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

Inventor： Kazuo Okano ,  Shuhei Miyazawa ,  Richar S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Shimomura ,  Osamu Asano ,  Hiroyuki Yoshimura ,  Mitsuaki Miyamoto ,  Yoshimori Sakuma ,  Kenzo Muramoto ,  Hiroshi Obaishi ,  Koukichi Harada ,  Hajime Tsunoda ,  Satoshi Katayama ,  Kouji Yamada ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

IPC: C07D495/14 ,  C07D495/22 ,  C07F9/6561 ,  A61K31/55

CPC classification number: C07D495/14 ,  C07F9/6561

Abstract: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.

Abstract translation: 公开了以下给定式的三唑并-1,4-二氮杂化合物及其药理学上可接受的盐，其可用于药物领域，特别是过敏性疾病（*化学结构*），其中R 1和R 2为氢或 烷基，R 3是氢或卤素，R 4是氢或烷基，X是-OCO - ， - NHCO-，-CO-或其它，Y是环烷基，环烷基烷基，炔基或其它。

公开(公告)号：US5089491A

公开(公告)日：1992-02-18

申请号：US463518

申请日：1990-01-11

Applicant: Takashi Kamiya ,  Toshihiko Naito ,  Shigeto Negi ,  Yuuki Komatu ,  Yasunobu Kai ,  Takaharu Nakamura ,  Isao Sugiyama ,  Yoshimasa Machida ,  Seiichiro Nomoto ,  Kyosuke Kitoh ,  Kanemasa Katsu ,  Hiroshi Yamauchi

Inventor： Takashi Kamiya ,  Toshihiko Naito ,  Shigeto Negi ,  Yuuki Komatu ,  Yasunobu Kai ,  Takaharu Nakamura ,  Isao Sugiyama ,  Yoshimasa Machida ,  Seiichiro Nomoto ,  Kyosuke Kitoh ,  Kanemasa Katsu ,  Hiroshi Yamauchi

IPC: C07D501/46 ,  A61K31/545 ,  A61K31/546 ,  C07D20060101 ,  C07D285/08 ,  C07D501/00 ,  C07D501/04 ,  C07D501/24 ,  C07D501/56 ,  C07D519/00

CPC classification number: C07D501/24

Abstract: A 3-propenylcephem derivative of the following formula: ##STR1## wherein R.sub.1 represents a fluoro-substituted lower alkyl group or a cyano-substituted lower alkyl group, and A represents a cyclic or an acylic ammonio group, or a pharmaceutically acceptable salt thereof, exhibiting excellent anti-bacterial activities against both Gram-positive bacteria and Gram-negative bacteria; Process for the preparation thereof; Anti-bacterial composition; Intermediate for the 3-propenylcephem derivative; and Process for the preparation of the intermediate.

公开(公告)号：US5037827A

公开(公告)日：1991-08-06

申请号：US373350

申请日：1989-06-29

Applicant: Kazuo Okano ,  Osamu Asano ,  Naoyuki Shimomura ,  Tetsuya Kawahara ,  Shinya Abe ,  Shuhei Miyazawa ,  Mitsuaki Miyamoto ,  Hiroyuki Yoshimura ,  Koukichi Harada ,  Junsaku Nagaoka ,  Tsutomu Kawata ,  Tsutomu Yoshimura ,  Hiromasa Suzuki ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

Inventor： Kazuo Okano ,  Osamu Asano ,  Naoyuki Shimomura ,  Tetsuya Kawahara ,  Shinya Abe ,  Shuhei Miyazawa ,  Mitsuaki Miyamoto ,  Hiroyuki Yoshimura ,  Koukichi Harada ,  Junsaku Nagaoka ,  Tsutomu Kawata ,  Tsutomu Yoshimura ,  Hiromasa Suzuki ,  Shigeru Souda ,  Yoshimasa Machida ,  Kouichi Katayama ,  Isao Yamatsu

IPC: C07D211/46 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/495 ,  A61P7/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/02 ,  C07D213/20 ,  C07D213/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12

CPC classification number: C07D213/40 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  Y10S514/921

Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##

公开(公告)号：US5010188A

公开(公告)日：1991-04-23

申请号：US167152

申请日：1988-03-16

Applicant: Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

Inventor： Hiroshi Yamauchi ,  Isao Sugiyama ,  Isao Saito ,  Seiichiro Nomoto ,  Takashi Kamiya ,  Yoshimasa Machida ,  Shigeto Negi

IPC: C07D471/08 ,  C07D501/46

CPC classification number: C07D471/08

Abstract: Described herein is a cephem derivative represented by the general formula: ##STR1## wherein n stands for 1 or 2, Y stands for CH or nitrogen atom, R.sub.1 represents a lower hydrocarbon group or a carboxyl-substituted, a carbamoyl-substituted, or a cyclopropyl-substituted lower alkyl group, and R.sub.2 denotes hydroxyl group, a lower alkyl group, a hydroxy-substituted lower alkyl group, or carbamoyl group. The derivative is useful as an antibacterial composition. Also described herein are processes for the production of the derivative, antibacterial composition, intermediate of the derivative and process for the production thereof.