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公开(公告)号:US4948899A
公开(公告)日:1990-08-14
申请号:US397850
申请日:1989-08-24
申请人: Toshihisa Ogawa , Tomomi Ota , Shuichi Sato , Takemi Sunaga , Yoshiaki Watanabe , Katsuo Hatayama
发明人: Toshihisa Ogawa , Tomomi Ota , Shuichi Sato , Takemi Sunaga , Yoshiaki Watanabe , Katsuo Hatayama
IPC分类号: C07D211/90 , A61K31/445 , A61K31/451 , A61P9/12
CPC分类号: C07D211/90
摘要: A 1,4-dihydropyridine derivative represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom, an alkoxy group having 1 to 4 carbon atoms, a mercapto group, an alkylcarbonylthio group in which the alkyl group has 1 to 4 carbon atoms or a benzoylthio group, R.sup.2 is a mercapto group, an alkylcarbonylthio group in which the alkyl group has 1 to 4 carbon atoms, a benzoylthio group or a 2-cyanoethylthio group, A and B are the same or different and are each an alkylene group having 1 to 4 carbon atoms, and X is a hydrogen atom, a halogen atom, a nitro group or a trifluoromethyl group is disclosed. These compounds increase the therapeutic effect of drug-resistant cancers.
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公开(公告)号:US4883876A
公开(公告)日:1989-11-28
申请号:US239687
申请日:1988-09-02
申请人: Shin-ichi Nakatsuka , Masatoshi Hayashi , Sadakazu Yokomori , Yoshimoto Nakashima , Katsuo Hatayama , Hiroaki Araki
发明人: Shin-ichi Nakatsuka , Masatoshi Hayashi , Sadakazu Yokomori , Yoshimoto Nakashima , Katsuo Hatayama , Hiroaki Araki
IPC分类号: C07D461/00
CPC分类号: C07D461/00
摘要: Vincaminic acid derivatives represented by the formula ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or an alkoxyalkyl group having 2 to 6 carbon atoms, R.sup.2 is a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a halogenated alkyl group having 1 to 5 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, an alkoxycarbonylallyl group having 3 to 8 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, a phenyl group, a phenyl group substituted by alkoxy groups each having 1 or 2 carbon atoms or a thienyl group, A is a hydroxy group, B is a hydrogen atom, or A and B together form a valence bond, and the acid addition salts thereof are disclosed. These compound are useful as thereapeutic effect on cerebovascular injuries.
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公开(公告)号:US4557871A
公开(公告)日:1985-12-10
申请号:US609858
申请日:1984-05-14
申请人: Katsuo Hatayama , Kensei Yoshikawa , Tatsuhiko Sano , Yutaka Ohuchi , Tomomi Ota , Kazuto Sekiuchi , Kaoru Sota
发明人: Katsuo Hatayama , Kensei Yoshikawa , Tatsuhiko Sano , Yutaka Ohuchi , Tomomi Ota , Kazuto Sekiuchi , Kaoru Sota
IPC分类号: A61K31/045 , A61K31/16 , A61K31/19 , A61K31/215 , A61P25/04 , A61P29/00 , C07C27/00 , C07C33/48 , C07C51/00 , C07C57/58 , C07C57/60 , C07C67/00 , C07C205/56 , C07C233/11 , C07C239/00 , C07C259/06 , C07D213/75 , C07D277/46 , C07D295/02 , C07D295/027 , C07D295/185 , C07F5/06 , C07C63/64
CPC分类号: C07D213/75 , C07C205/56 , C07C233/11 , C07C33/483 , C07C57/58 , C07C57/60 , C07C67/343 , C07C69/65 , C07D277/46 , C07D295/027 , C07D295/185
摘要: Novel styrene derivatives of the general formula ##STR1## wherein X is hydrogen or halogen, X.sup.1 is halogen, R is hydrogen or methyl, Y is hydroxymethyl, carboxyl, --COOR.sup.1 or --COR.sup.2 wherein R.sup.1 is prenyl, geranyl, farnesyl, cyclohexyl, phthalidyl, straight or branched chain alkyl having 1 to 6 carbon atoms, or said alkyl substituted with hydroxy, methoxy, pyridyl or alkanoyloxy having 2 to 16 carbon atoms, and R.sup.2 is amino, hydroxyamino mono-(or di-)alkylamino in which the alkyl moiety contains 1 or 2 carbon atoms, ethoxycarbonylmethylamino, carboxymethylamino, thiazolylamino, cyclohexylamino, pyridylamino, morpholino, N-methylpiperazino, phenylamino, phenylamino substituted with one or two of halogen, hydroxy, methyl, methoxy, trifluoromethyl or carboxyl at the phenyl ring, and the pharmaceutically acceptable salts thereof when Y is carboxyl are disclosed. These compounds exhibit high and long-lasting anti-inflammatory, analgesic and anti-pyretic activity.
摘要翻译: 通式为:其中X为氢或卤素,X1为卤素,R为氢或甲基,Y为羟基甲基,羧基,-COOR1或-COR2的新型苯乙烯衍生物,其中R1为异戊烯基,香叶基,法呢基,环己基, 或具有2至16个碳原子的羟基,甲氧基,吡啶基或烷酰氧基取代的所述烷基,R2是氨基,羟基氨基单(或二)烷基氨基,其中 烷基部分含有1或2个碳原子,乙氧基羰基甲基氨基,羧甲基氨基,噻唑基氨基,环己基氨基,吡啶基氨基,吗啉代,N-甲基哌嗪基,苯基氨基,苯基氨基,被苯基环上的一个或两个卤素,羟基,甲基,甲氧基,三氟甲基或羧基取代, 并且当Y是羧基时,其药学上可接受的盐被公开。 这些化合物表现出高且持久的抗炎,止痛和抗热解活性。
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公开(公告)号:US4472411A
公开(公告)日:1984-09-18
申请号:US486508
申请日:1983-04-19
申请人: Katsuo Hatayama , Aturo Nakazato , Toshihisa Ogawa , Shoichi Ito , Jiro Sawada
发明人: Katsuo Hatayama , Aturo Nakazato , Toshihisa Ogawa , Shoichi Ito , Jiro Sawada
IPC分类号: C07C69/72 , A61K31/455 , A61P9/00 , A61P9/02 , A61P9/08 , A61P9/10 , A61P9/12 , C07C203/04 , C07C229/30 , C07D211/90 , A61K31/44
CPC分类号: C07D211/90
摘要: The compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms or nitratoalkyl having 2 or 3 carbon atoms, and R' is nitratoalkyl having 2 or 3 carbon atoms, are disclosed. These compounds are useful as therapeutic agents for cardiovascular disorders such as coronary artery disease, cerebral artery disease, hypertension and the like.
摘要翻译: 公开了其中R为具有1至4个碳原子的烷基或具有2或3个碳原子的硝基烷基,R'为2或3个碳原子的硝基烷基的式“IMAGE”的化合物。 这些化合物可用作心血管疾病如冠状动脉疾病,脑动脉疾病,高血压等的治疗剂。
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公开(公告)号:US5753673A
公开(公告)日:1998-05-19
申请号:US578532
申请日:1996-01-18
IPC分类号: C07D215/54 , A61K31/47 , A61K31/535 , A61P1/00 , A61P43/00 , C07D401/06 , C07D451/04 , C07D451/06 , C07D451/12 , A61K31/46
CPC分类号: C07D451/04 , C07D451/12
摘要: Quinolinecarboxylic acid derivatives represented by the following formula: ##STR1## wherein C is hydroxymethyl, methoxy, ethoxy or morpholinyl, or pharmaceutically acceptable salts thereof exhibit a potent action for stimulating a serotonin 4 receptor. The compounds exhibit an action of enhancing the gastrointestinal motor function to improve the gastrointestinal conditions such as heartburn, anorexia, bowel pain, abdominal distension, etc., accompanied by chronic gastritis, diabetes mellitus or postoperative gastroparesis, and are thus effective for the treatment of gastro-esophagal reflux, intestinal pseudo-obstruction and constipation.
摘要翻译: PCT No.PCT / JP95 / 00954 Sec。 371日期:1996年1月18日 102(e)日期1996年1月18日PCT提交1995年5月18日PCT公布。 第WO95 / 31455号公报 日期:1月23日,下式表示的喹啉羧酸衍生物:其中C为羟甲基,甲氧基,乙氧基或吗啉基或其药学上可接受的盐,表现出刺激5-羟色胺4受体的有效作用。 化合物表现出增强胃肠运动功能的作用,以改善伴随慢性胃炎,糖尿病或术后胃轻瘫的胃肠道状况,例如胃灼热,厌食,肠痛,腹胀等,因此有效治疗 胃食管反流,肠道假梗阻和便秘。
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公开(公告)号:US5602239A
公开(公告)日:1997-02-11
申请号:US491860
申请日:1995-07-13
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: A novel macloride antibiotic having a potent antibacterial activity, represented by the formula: ##STR1## which is obtained by introducing a specific aryloxy or alkoxy group into the 3-position of a 5-O-desosaminylerythronolide derivative; or phamaceutically acceptable acid addition salts thereof.
摘要翻译: PCT No.PCT / JP94 / 00087 Sec。 371日期1995年7月13日 102(e)日期1995年7月13日PCT 1994年1月24日PCT公布。 公开号WO94 / 17088 日期1994年8月4日一种具有强效抗菌活性的新型macloride抗生素,由下式表示:通过将特定的芳氧基或烷氧基引入到5-O-去甲氨基戊三醇内酯衍生物的3-位而获得; 或其药学上可接受的酸加成盐。
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公开(公告)号:US5523399A
公开(公告)日:1996-06-04
申请号:US244981
申请日:1994-06-20
IPC分类号: C07H17/08
CPC分类号: C07H17/08
摘要: Provision of novel macrolide antibiotics having a strong antibacterial activity.Construction:Compounds represented by the formula: ##STR1## which are obtained by introducing a carbamoyl group into 5-O-desosaminyl-6-O-methylerythronolide derivatives at the 3-position; and pharmaceutically acceptable acid addition salts thereof.
摘要翻译: PCT No.PCT / JP92 / 01713 Sec。 371日期:1994年6月20日 102(e)日期1994年6月20日PCT提交1992年12月15日PCT公布。 出版物WO93 / 日期:1993年7月8日。具有强抗菌活性的新型大环内酯类抗生素的制备。 结构:通过在3-位上将氨基甲酰基引入5-O-脱氨基-6-O-甲基红霉内酯衍生物而获得的由下式表示的化合物:
及其药学上可接受的酸加成盐。 -
公开(公告)号:US5496829A
公开(公告)日:1996-03-05
申请号:US244330
申请日:1994-05-24
IPC分类号: A61K31/475 , A61K31/44
CPC分类号: A61K31/475
摘要: 2-nitroxyethyl (+)apovincaminate is used as an agent for relieving disturbance of consciousness and as a narcotic antagonist.
摘要翻译: PCT No.PCT / JP94 / 01601 Sec。 371日期:1994年5月24日 102(e)日期1994年5月24日PCT提交1992年12月8日PCT公布。 公开号WO93 / 11765 日期:1993年6月24日,2-氨基乙基(+)脱氨基甲酸酯被用作缓解意识紊乱和麻醉拮抗剂的药剂。
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公开(公告)号:US5089654A
公开(公告)日:1992-02-18
申请号:US562602
申请日:1990-08-03
IPC分类号: A61K31/19 , A61K31/12 , A61K31/215 , A61K31/22 , A61P1/04 , C07C45/51 , C07C45/74 , C07C49/82 , C07C49/84 , C07C59/00 , C07C59/90 , C07C69/712 , C07C69/738
CPC分类号: C07C69/712 , C07C45/513 , C07C45/74 , C07C49/84 , C07C59/90
摘要: Chalcone derivatives represented by the formula ##STR1## wherein R.sup.1 is a straight chain, branched chain or cyclic alkyl group having 4 to 15 carbon atoms or an alkenyl group having 3 to 15 carbon atoms, and occurs at the 2- or 4-position, R.sup.2 is a hydrogen atom, a straight or branched chain alkyl group having 1 to 3 carbon atoms, and X is a straight or branched chain alkylene group having 1 to 3 carbon atoms, are disclosed. These compounds have anti-ulcer effect, gastric mucosal protection effect and antisecretory effect.
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公开(公告)号:US4980474A
公开(公告)日:1990-12-25
申请号:US405972
申请日:1989-09-12
IPC分类号: A61K31/435 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/28 , C07D461/00
CPC分类号: C07D461/00
摘要: An apovincaminic acid derivative represented by the formula ##STR1## wherein n is an integer of from 2 to 11, and a pharmaceutically acceptable salt thereof are disclosed. These compounds are useful for therapy of cerebrovascular injuries, peripheral vessel injuries, angina pectoris, hypertension and senile dementia.
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