公开(公告)号：US5142046A

公开(公告)日：1992-08-25

申请号：US754198

申请日：1991-08-28

申请人： Isao Hayakawa ,  Shohgo Atarashi ,  Masazumi Imamura ,  Shuichi Yokohama ,  Nobuyuki Higashihashi ,  Katsuichi Sakano ,  Masayuki Ohshima

发明人： Isao Hayakawa ,  Shohgo Atarashi ,  Masazumi Imamura ,  Shuichi Yokohama ,  Nobuyuki Higashihashi ,  Katsuichi Sakano ,  Masayuki Ohshima

IPC分类号： A61K31/50 ,  C07B57/00 ,  C07D265/36 ,  C07D413/06 ,  C07D498/06

CPC分类号： C07D413/06 ,  C07D265/36

摘要： An optically action pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active pyridobenzoxazine derivative are disclosed. The optically active pyridobenzoxazine derivative possesses increased antimicrobial activity and reduced toxicity. The intermediate is useful for preparing such optically active pyridobenzoxazine derivatives such as Ofloxacin and anolog compounds.

摘要翻译： 公开了光学活性吡啶并苯并恶嗪衍生物，其制备方法和可用于制备光学活性吡啶并苯并恶嗪衍生物的新型中间体。 光学活性的吡啶并苯并恶嗪衍生物具有增加的抗微生物活性和降低的毒性。 中间体可用于制备诸如氧氟沙星和anolog化合物之类的光学活性吡啶并苯并恶嗪衍生物。

公开(公告)号：US5098919A

公开(公告)日：1992-03-24

申请号：US552031

申请日：1990-07-13

申请人： Norio Suzuki ,  Atsushi Nakayama ,  Toru Hosokami ,  Masashi Hasegawa ,  Shuichi Yokohama

发明人： Norio Suzuki ,  Atsushi Nakayama ,  Toru Hosokami ,  Masashi Hasegawa ,  Shuichi Yokohama

IPC分类号： A61K31/425 ,  A61K31/429 ,  A61P1/16 ,  A61P7/00 ,  C07D207/24 ,  C07D207/36 ,  C07D513/04

CPC分类号： C07D513/04 ,  C07D207/24 ,  C07D207/36

摘要： A compound represented by the following formula (I): ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group or a cyclic alkyl group;R.sub.2 represents a hydroxyl group, an alkoxy group which may have one to three substituents in the alkyl group moiety, an arylthio group which may have one or more substituents in the aryl group moiety, an aryloxy group which may have one or more substituents in the aryl group moiety, an amino group, an alkylamino group or a cyclic amino group which may contain other hetero atoms as ring atoms selected from a nitrogen atom, an oxygen atom and a sulfur atom;R.sub.3 represents a hydrogen atom, an alkyl group, an aryl group which may have one or more substituents, or a hetero aryl group which may have one or more substituents; m represents 1 or 2 and represents a single bond or a double bond; salts thereof, and pharmaceutical preparations for preventing and treating hepatic diseases containing the compound of the formula (I) or salts thereof as an active ingredient are disclosed.

公开(公告)号：US4898943A

公开(公告)日：1990-02-06

申请号：US153677

申请日：1988-02-08

申请人： Sumiro Isoda ,  Shunzo Aibara ,  Tamotsu Miwa ,  Hiroyuki Fujiwara ,  Shuichi Yokohama ,  Hiroo Matsumoto

发明人： Sumiro Isoda ,  Shunzo Aibara ,  Tamotsu Miwa ,  Hiroyuki Fujiwara ,  Shuichi Yokohama ,  Hiroo Matsumoto

IPC分类号： C07D277/40 ,  C07D513/14

CPC分类号： C07D513/14

摘要： Novel tricyclic triazolopyrimidine compounds represented by formula (I) shown in the specification and physiologically acceptable salts thereof are disclosed. These compounds have an excellent anti-allergic activity and are useful for treatment and prophylaxis of allergic diseases.

公开(公告)号：US5053407A

公开(公告)日：1991-10-01

申请号：US876623

申请日：1986-06-20

申请人： Isao Hayakawa ,  Shohgo Atarashi ,  Masazumi Imamura ,  Shuichi Yokohama ,  Nobuyuki Higashihashi ,  Katsuichi Sakano ,  Masayuki Ohshima

发明人： Isao Hayakawa ,  Shohgo Atarashi ,  Masazumi Imamura ,  Shuichi Yokohama ,  Nobuyuki Higashihashi ,  Katsuichi Sakano ,  Masayuki Ohshima

IPC分类号： A61K31/50 ,  C07B57/00 ,  C07D265/36 ,  C07D413/06 ,  C07D498/06

CPC分类号： C07D413/06 ,  C07D265/36

摘要： An optically action pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active pyridobenzoxazine derivative are disclosed. The optically active pyridobenzoxazine derivative possesses increased antimicrobial activity and reduced toxicity. The intermediate is useful for preparing such optically active pyridobenzoxazine derivatives such as Ofloxacin and anolog compounds.

公开(公告)号：US4985557A

公开(公告)日：1991-01-15

申请号：US327653

申请日：1989-03-23

申请人： Isao Hayakawa ,  Shohgo Atarashi ,  Masazumi Imamura ,  Shuichi Yokohama ,  Nobuyuki Higashihashi ,  Katsuichi Sakano ,  Masayuki Ohshima

发明人： Isao Hayakawa ,  Shohgo Atarashi ,  Masazumi Imamura ,  Shuichi Yokohama ,  Nobuyuki Higashihashi ,  Katsuichi Sakano ,  Masayuki Ohshima

IPC分类号： A61K31/50 ,  C07B57/00 ,  C07D265/36 ,  C07D413/06 ,  C07D498/06

CPC分类号： C07D413/06 ,  C07D265/36

摘要： An optically action pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active pyridobenzoxazine derivative are disclosed. The optically active pyridobenzoxazine derivative possesses increased antimicrobial activity and reduced toxicity. The intermediate is useful for preparing such optically active pyridobenzoxazine derivatives such as Ofloxacin and anolog compounds.

摘要翻译： 公开了光学活性吡啶并苯并恶嗪衍生物，其制备方法和可用于制备光学活性吡啶并苯并恶嗪衍生物的新型中间体。 光学活性的吡啶并苯并恶嗪衍生物具有增加的抗微生物活性和降低的毒性。 中间体可用于制备诸如氧氟沙星和anolog化合物之类的光学活性吡啶并苯并恶嗪衍生物。

公开(公告)号：US4871852A

公开(公告)日：1989-10-03

申请号：US129424

申请日：1987-11-27

申请人： Isao Hayakawa ,  Shohgo Atarashi ,  Shuichi Yokohama ,  Masazumi Imamura

发明人： Isao Hayakawa ,  Shohgo Atarashi ,  Shuichi Yokohama ,  Masazumi Imamura

IPC分类号： C07C211/37 ,  A61K31/47 ,  A61K31/495 ,  A61P31/04 ,  C07C67/00 ,  C07C209/00 ,  C07C209/56 ,  C07C229/34 ,  C07C253/00 ,  C07C255/50 ,  C07D215/00 ,  C07D215/56 ,  C07D241/00 ,  C07D401/04 ,  C07D401/14

CPC分类号： C07D215/56 ,  C07D401/04

摘要： Novel 4-oxoguinoline-3-carboxylic acid derivatives having the formula ##STR1## wherein X.sup.1 represents a halogen or hydrogen atom, X.sup.2 represents a halogen or hydrogen atom, X.sup.3 represents a halogen atom, and R.sup.1, R.sup.2 and R.sup.3 each represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and physiologically acceptable salts thereof, are disclosed. These compounds have excellent antibacterial activity against gram-positive and gram-negative bacteria and beneficial pharmacokinetic properties.

摘要翻译： 具有式“IMAGE”的新型4-氧代庚烯啉-3-羧酸衍生物，其中X1表示卤素或氢原子，X2表示卤素或氢原子，X3表示卤素原子，R1，R2和R3各自表示氢原子 或具有1至6个碳原子的烷基，及其生理上可接受的盐。 这些化合物对革兰氏阳性和革兰氏阴性细菌具有优异的抗菌活性和有益的药代动力学性质。

公开(公告)号：US5919824A

公开(公告)日：1999-07-06

申请号：US894799

申请日：1997-09-12

申请人： Shuichi Yokohama ,  Keiichi Kawagoe ,  Yasuyuki Takeda ,  Yoshihiro Yokomizo ,  Aki Yokomizo

发明人： Shuichi Yokohama ,  Keiichi Kawagoe ,  Yasuyuki Takeda ,  Yoshihiro Yokomizo ,  Aki Yokomizo

IPC分类号： C07C275/16 ,  C07C275/28 ,  A61K37/44 ,  C07C59/235

CPC分类号： C07C275/28 ,  C07C275/16 ,  Y10S514/925 ,  Y10S514/927

摘要： Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.

摘要翻译： PCT No.PCT / JP96 / 00611 Sec。 371日期：1997年9月12日 102（e）1997年9月12日PCT PCT 1996年3月12日PCT公布。 公开号WO96 / 28416 日期：1996年9月19日由下式（1）表示的苯酚衍生物：其中X为O或S; A是亚烷基，R 1是苯基等，R 2和R 3是H或烷基; R4是取代的氨基甲酰基烷基等; R5是取代氨基等。 它们的盐和衍生物和盐的光学异构体。 还公开了胃泌素受体拮抗剂，胆囊收缩素受体拮抗剂和用于消化疾病的药物。 这些化合物对胃泌素受体或CCK-A受体具有强烈的结合抑制作用，并且对CCK-A受体或胃泌素受体组也具有较高的选择性，因此，该化合物也可用于预防和治疗胃肠疾病，包括消化性溃疡 作为中枢神经系统疾病。