公开(公告)号：US4309354A

公开(公告)日：1982-01-05

申请号：US218403

申请日：1980-12-19

Applicant: Seiichiro Nomoto ,  Hironori Ikuta ,  Yoshimasa Machida ,  Shigeto Negi ,  Isao Sugiyama ,  Hiroshi Yamauchi ,  Kenro Nakatsuka ,  Isao Saito

Inventor： Seiichiro Nomoto ,  Hironori Ikuta ,  Yoshimasa Machida ,  Shigeto Negi ,  Isao Sugiyama ,  Hiroshi Yamauchi ,  Kenro Nakatsuka ,  Isao Saito

IPC: C07D501/34 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D311/22 ,  C07D501/24 ,  C07D501/36

CPC classification number: C07D311/22

Abstract: New chromone derivatives having the formula: ##STR1## wherein A represents a hydrogen atom, a halogen atom or a hydroxyl group, and R.sub.1 represents a lower alkyl or a chloro-substituted lower alkyl group. The derivatives are useful intermediates for synthesis of cephem derivatives as antibacterial drugs.

Abstract translation: 具有下式的新色酮衍生物：其中A表示氢原子，卤素原子或羟基，R 1表示低级烷基或氯取代的低级烷基。 该衍生物是合成头孢烯衍生物作为抗菌药物的有用中间体。

公开(公告)号：US4285940A

公开(公告)日：1981-08-25

申请号：US137754

申请日：1980-04-07

Applicant: Yoshimasa Machida ,  Isao Saito ,  Seiichiro Nomoto ,  Shigeto Negi ,  Hironori Ikuta ,  Kyosuke Kitoh

Inventor： Yoshimasa Machida ,  Isao Saito ,  Seiichiro Nomoto ,  Shigeto Negi ,  Hironori Ikuta ,  Kyosuke Kitoh

IPC: A61K31/43 ,  A61K31/545 ,  A61K31/546 ,  A61P31/04 ,  C07D311/22 ,  C07D501/34 ,  C07D501/26

CPC classification number: C07D311/22

Abstract: New cephalosporin derivatives having the general formula: ##STR1## wherein R.sub.1 and R.sub.2 each represents hydroxy or acyloxy and their salts, and processes for the production thereof. The cephalosporin derivatives of the present invention are useful as antibacterial drugs.

Abstract translation: 具有以下通式的新型头孢菌素衍生物：其中R1和R2各自表示羟基或酰氧基及其盐，以及其制备方法。 本发明的头孢菌素衍生物可用作抗菌药物。

公开(公告)号：US5849912A

公开(公告)日：1998-12-15

申请号：US855790

申请日：1997-05-12

Applicant: Kozo Akasaka ,  Masahiro Yonaga ,  Akiharu Kajiwara ,  Kunizo Higurashi ,  Kohshi Ueno ,  Satoshi Nagato ,  Makoto Komatsu ,  Noritaka Kitazawa ,  Masataka Ueno ,  Yoshiharu Yamanishi ,  Yoshimasa Machida ,  Yuki Komatsu ,  Naoyuki Shimomura ,  Norio Minami ,  Toshikazu Shimizu ,  Atsushi Nagaoka

Inventor： Kozo Akasaka ,  Masahiro Yonaga ,  Akiharu Kajiwara ,  Kunizo Higurashi ,  Kohshi Ueno ,  Satoshi Nagato ,  Makoto Komatsu ,  Noritaka Kitazawa ,  Masataka Ueno ,  Yoshiharu Yamanishi ,  Yoshimasa Machida ,  Yuki Komatsu ,  Naoyuki Shimomura ,  Norio Minami ,  Toshikazu Shimizu ,  Atsushi Nagaoka

IPC: C07D295/03 ,  A61K31/495 ,  A61P25/18 ,  C07D213/26 ,  C07D213/30 ,  C07D213/38 ,  C07D213/50 ,  C07D213/70 ,  C07D295/02 ,  C07D295/04 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/155 ,  C07D295/205 ,  C07D295/26 ,  C07D307/14 ,  C07D307/52 ,  C07D319/06 ,  C07D339/08 ,  C07F7/18 ,  C07D401/06

CPC classification number: C07D213/30 ,  C07D213/26 ,  C07D213/38 ,  C07D213/50 ,  C07D213/70 ,  C07D295/02 ,  C07D295/073 ,  C07D295/088 ,  C07D295/096 ,  C07D295/112 ,  C07D295/135 ,  C07D295/155 ,  C07D295/205 ,  C07D295/26 ,  C07D307/14 ,  C07D307/52 ,  C07D319/06 ,  C07D339/08 ,  C07F7/1856 ,  C07C2101/02

Abstract: A biphenyl derivative represented by the following formula (I) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are defined in the specification, is clinically useful for treating and ameliorating mental disorders such as cerebrovascular disorder, aggressive behavior due to senile dementia, mental excitation, poriomania, delirium, hallucination, hyperkinesia, schizophrenia, emotional disturbance, depression, neurosis, psychophysiologic disorder and anxiety neurosis. The compounds exhibit dopamine 2 receptor antagonism and/or serotonin 2 receptor antagonism.

Abstract translation: 由下式（I）表示的联苯衍生物或其药学上可接受的盐：其中R 1，R 2，R 3，R 4和R 5在本说明书中定义，其在临床上可用于治疗和改善精神障碍 脑血管障碍，老年性痴呆，精神激动，心脏虚弱，del妄，幻觉，运动过度，精神分裂症，情绪障碍，抑郁，神经症，心理生理障碍和焦虑神经症引起的侵略行为。 该化合物表现出多巴胺2受体拮抗作用和/或5-羟色胺2受体拮抗作用。

公开(公告)号：US5741902A

公开(公告)日：1998-04-21

申请号：US464341

申请日：1995-06-05

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 ,  C07D501/40

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, fluorine-substituted 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.

公开(公告)号：US5563265A

公开(公告)日：1996-10-08

申请号：US393074

申请日：1995-02-23

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 ,  C07D501/60

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, fluorine-substituted 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，氟取代的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：US5476863A

公开(公告)日：1995-12-19

申请号：US129301

申请日：1993-09-30

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 ,  A61K31/495 ,  C07D213/72

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##

Abstract translation: 具有下式（I）或（I'）的甘油衍生物及其药理学上可接受的盐可用于治疗血小板活化因子引起的疾病。 （I）（I）

公开(公告)号：US5409909A

公开(公告)日：1995-04-25

申请号：US214850

申请日：1994-03-18

Applicant: Kazuo Okano ,  Shuhei Miyazawa ,  Richard S. J. Clark ,  Shinya Abe ,  Tetsuya Kawahara ,  Naoyuki Kimomura ,  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 Kimomura ,  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 ,  A61K31/55

CPC classification number: C07D495/14

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 treat allergic diseases: ##STR1## in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 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，特别是治疗过敏性疾病：其中R 1和R 2为氢或烷基 ，R 3为氢或卤素，R 4为氢或烷基，X为-OCO - ， - NHCO - ， - CO-等，Y为环烷基，环烷基烷基，炔基等。

公开(公告)号：US5273985A

公开(公告)日：1993-12-28

申请号：US710089

申请日：1991-06-04

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 ,  C07D213/72

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##

Abstract translation: 具有下式（I）或（I'）的甘油衍生物及其药理学上可接受的盐可用于治疗血小板活化因子引起的疾病。 （I）（I）

公开(公告)号：US5134111A

公开(公告)日：1992-07-28

申请号：US451468

申请日：1989-12-15

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

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: A naphthalene derivative having the formula is new and useful for medicine. ##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 heteroarylalkyl group;R.sup.3 and R.sup.4 are the same or different and represent 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 carboxy group, a carboxyalkyl group, an aminoalkyl group, or a cyano group;R.sup.5 represents a group of the formula, --OR.sup.7, (wherein R.sup.7 represents a hydrogen atom or a lower alkyl group), or a group of the formula ##STR2## (wherein R.sup.8 and R.sup.9 are the same or different and represent a hydrogen atom or a lower alkyl group, or R.sup.8 and R.sup.9 can form, along with the nitrogen atom bonded with R.sup.8 and R.sup.9, a ring which may contain an oxygen atom);R.sup.6 independently represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, an amino group, an arylalkyl group, or an aryl group; andm is 0 or an integer of from 1 to 2, and n is 0 or an integer of from 1 to 4.]

公开(公告)号：US4468394A

公开(公告)日：1984-08-28

申请号：US363778

申请日：1982-03-31

Applicant: Yoshimasa Machida ,  Isao Saito ,  Isao Sugiyama ,  Shigeto Negi ,  Seiichiro Nomoto ,  Hironori Ikuta ,  Hiroshi Yamauchi ,  Kyosuke Kitoh

Inventor： Yoshimasa Machida ,  Isao Saito ,  Isao Sugiyama ,  Shigeto Negi ,  Seiichiro Nomoto ,  Hironori Ikuta ,  Hiroshi Yamauchi ,  Kyosuke Kitoh

IPC: C07D215/54 ,  C07D215/56 ,  C07D311/16 ,  C07D335/06 ,  C07D499/00 ,  C07D499/68 ,  C07D501/24 ,  A61K31/545 ,  C07D501/04 ,  C07D501/46 ,  C07D501/56

CPC classification number: C07D335/06 ,  C07D215/54 ,  C07D215/56 ,  C07D311/16 ,  C07D499/00

Abstract: A compound represented by the formula: ##STR1## wherein R.sub.1 is hydrogen or methoxy; R.sub.2 is hydrogen or hydroxy; R is ##STR2## wherein R.sub.3 and R.sub.4 are hydroxy or acyloxy, Y is oxygen, sulfur or >N-R.sub.5 wherein R.sub.5 is hydrogen or lower alkyl, and Z is sulfur or >N-R.sub.5 wherein R.sub.5 has the same meanings as defined above; and X is ##STR3## wherein R.sub.6 is acyloxy or nitrogen-containing heterocyclicthio which may have substituent(s), a pharmaceutically accpetable salt thereof, and a carboxylic ester thereof.This compound has improved antibacterial activity against Kleb. pneumoniae and Pseud. aeruginosa.

Abstract translation: 由下式表示的化合物：其中R1是氢或甲氧基; R2是氢或羟基; R为其中R3和R4为羟基或酰氧基，Y为氧，硫或> N-R5，其中R5为氢或低级烷基，Z为硫或> N-R5，其中R5具有与上述相同的含义 ; X为，其中R6为可具有取代基的酰氧基或含氮杂环硫基，其药学上可接受的盐及其羧酸酯。 该化合物对Kleb具有改善的抗菌活性。 肺炎和Pseud。 铜绿假单胞菌