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公开(公告)号:US4937360A
公开(公告)日:1990-06-26
申请号:US373338
申请日:1989-06-28
申请人: Geng-tao Liu , Liang Huang , Er-chang Rao , Jin Zhou , Yan Li , Katsuo Hatayama , Tatsuhiko Sano , Kensei Yoshikawa , Shohei Higuchi , Iwao Arai
发明人: Geng-tao Liu , Liang Huang , Er-chang Rao , Jin Zhou , Yan Li , Katsuo Hatayama , Tatsuhiko Sano , Kensei Yoshikawa , Shohei Higuchi , Iwao Arai
IPC分类号: A61K31/357 , A61K31/36 , A61P1/16 , C07D317/58 , C07D317/68
CPC分类号: C07D317/58
摘要: N-substituted amide derivative represented by the formula ##STR1## wherein A is --CH(OH)-- or --C(.dbd.O)--, R.sup.1 is a hydrogen atom or anlkyl group having 1 to 3 carbon atoms, and R.sup.2 is an alkyl group having 1 to 6 carbon atoms, are disclosed. These compounds are useful for prevention and therapy for liver diseases.
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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:US5374764A
公开(公告)日:1994-12-20
申请号:US190123
申请日:1994-02-03
IPC分类号: C07C311/08 , C07C311/02
CPC分类号: C07C311/08 , C07C2101/14
摘要: 5-Aminosulfonanilide compounds represented by the formula: ##STR1## (wherein R is a hydrogen atom, a formyl group, an acetyl group, a propionyl group, an n-butyryl group, an n-valeryl group, an ethoxyoxalyl group, an n-propoxyoxalyl group, a methoxycarbonylacetyl group or a 3-ethoxycarbonylpropionyl group) have potent anti-inflammatory, antipyretic, analgesic and anti-allergic actions, and therefore they are useful as anti-inflammatory, antipyretic, analgesic and anti-allergic agents.
摘要翻译: PCT No.PCT / JP92 / 01013 Sec。 371日期:1994年2月3日 102(e)日期1994年2月3日PCT提交1992年8月7日PCT公布。 公开号WO93 / 03008 日期:1993年2月18日5-氨基磺酰苯胺化合物由下式表示:其中R为氢原子,甲酰基,乙酰基,丙酰基,正丁酰基,正戊酰基, 乙氧基草酰基,正丙氧基草酰基,甲氧基羰基乙酰基或3-乙氧基羰基丙酰基)具有有效的抗炎,解热,镇痛和抗过敏作用,因此它们可用作抗炎,解热,止痛和抗 - 过敏剂。
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公开(公告)号:US4885367A
公开(公告)日:1989-12-05
申请号:US271641
申请日:1988-11-16
申请人: Kensei Yoshikawa , Yutaka Ohuchi , Kazuto Sekiuchi , Shiuji Saito , Katsuo Hatayama , Kaoru Sota
发明人: Kensei Yoshikawa , Yutaka Ohuchi , Kazuto Sekiuchi , Shiuji Saito , Katsuo Hatayama , Kaoru Sota
IPC分类号: C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07D211/46 , C07D309/12 , C07D335/02
CPC分类号: C07D211/46 , C07C311/08 , C07C311/09 , C07C317/40 , C07C323/35 , C07D309/12 , C07D335/02 , C07C2101/08 , C07C2101/14 , C07C2101/18 , C07C2102/42
摘要: Sulfonanilide compounds represented by the formula ##STR1## wherein R.sup.1 is a lower alkyl group or a trifluoromethyl group, R.sup.2 is a cycloalkylidenemethyl group, a group of the formula --A--R.sup.3 (wherein A is an oxygen atom, a sulfur atom, a sulfynyl group or a sulfinyl group and R.sup.3 is a cycloalkyl group having 5-8 carbon atoms; a cycloalkyl group having 5-8 carbon atoms substituted by one or two of a lower alkyl group, an oxo group, a hydroxyl group or a methanesulfonyloxy group, a tetrahydropyranyl group; a tetrahydrothiopyranyl group; or a 1-methyl-piperidyl group) or a group of the formula --B--R.sup.4 (wherein B is a carbonyl group, a hydroxymethylene group or a methylene group, R.sup.4 is a cycloalkyl group having 5-8 carbon atoms) and the pharmaceutically acceptable salts thereof have anti-inflammatory activity.
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公开(公告)号:US5521311A
公开(公告)日:1996-05-28
申请号:US501029
申请日:1995-08-14
IPC分类号: C07C311/08 , C07D295/15 , C07D295/073
CPC分类号: C07D295/15 , C07C311/08 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14
摘要: The present compounds represented by the formula: ##STR1## (wherein R.sup.1 is a phenyl group, a halophenyl group or a cycloalkyl group having 3 to 8 carbon atoms, R.sup.2 is a hydrogen atom or an alkyl group having 1 to 5 carbon atoms, R.sup.3 is a hydrogen atom, an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 5 carbon atoms or a benzyl group, or R.sup.2 and R.sup.3 are bonded together to form a 5- to 7-membered heterocycle) and salts thereof have potent anti-inflammatory, antipyretic, analgesic and anti-allergic actions with less side effects such as gastrointestinal disorders and with such a high safety as to permit long-term administration.
摘要翻译: PCT No.PCT / JP94 / 00228 Sec。 371日期1995年8月14日 102(e)日期1995年8月14日PCT 1994年2月16日PCT PCT。 第WO94 / 19318号公报 日本公开日:1994年9月1日。由下式表示的本发明化合物:其中R1为苯基,卤代苯基或碳原子数为3〜8的环烷基,R2为氢原子或具有 1至5个碳原子,R 3是氢原子,具有1至7个碳原子的烷基,具有3至8个碳原子的环烷基,具有3至5个碳原子的烯基或苄基,或R 2和R 3 被结合在一起以形成5-至7-元杂环),其盐具有有效的抗炎,解热,镇痛和抗过敏作用,具有较少的副作用,例如胃肠道疾病,并具有如此高的安全性, 长期管理。
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公开(公告)号:US5449826A
公开(公告)日:1995-09-12
申请号:US351341
申请日:1994-12-09
IPC分类号: C07C311/08 , C07C211/45
CPC分类号: C07C311/08
摘要: To provide an excellent compound having anti-inflammatory, antipyretic, analgesic and antirheumatic actions.A 5-amino-2-phenoxysulfonanilide compound represented by the formula: ##STR1## and the salts thereof have potent anti-inflammatory, antipyretic, analgesic and antirheumatic actions, and therefore they are useful as anti-inflammatory, antipyretic, analgesic and antirheumatic agents.
摘要翻译: PCT No.PCT / JP93 / 00518 Sec。 371日期1994年12月9日第 102(e)日期1994年12月9日PCT 1993年4月21日PCT PCT。 公开号WO93 / 25520 日期为1993年12月23日。提供具有抗炎,解热,镇痛和抗风湿作用的优异化合物。 由下式表示的5-氨基-2-苯氧基亚磺酰苯胺化合物及其盐具有强力的抗炎,解热,止痛和抗风湿作用,因此它们可用作抗炎,解热,镇痛和抗风湿剂 。
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公开(公告)号:US5712263A
公开(公告)日:1998-01-27
申请号:US663929
申请日:1996-06-14
申请人: Chihiro Yokoo , Hisaya Wada , Hidemichi Mitome , Tatsuhiko Sano , Katsuo Hatayama , Yasuji Yamada
发明人: Chihiro Yokoo , Hisaya Wada , Hidemichi Mitome , Tatsuhiko Sano , Katsuo Hatayama , Yasuji Yamada
CPC分类号: C07J21/006 , C07J17/00 , C07J7/002 , C07J9/00
摘要: To provide novel steroid derivatives having an antitumor action which can be synthesized efficiently and stereoselectively by means of synthetic organic chemistry. A steroid derivative represented by the formula: ##STR1## wherein R is an alkyl group having 1 to 13 carbon atoms, A is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, X and Y together form an oxo group or an alkylenedioxy group having 2 or 3 carbon atoms, X is a hydroxyl group, an alkoxy group having 1 to 5 carbon atoms or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom or an alkoxy group having 1 to 5 carbon atoms, with the proviso that when X is a hydroxyl group or a group easily hydrolyzable to a hydroxyl group, Y is a hydrogen atom, and when X is an alkoxy group having 1 to 5 carbon atoms, Y is an alkoxy group having 1 to 5 carbon atoms, or a salt thereof.
摘要翻译: 提供具有抗肿瘤作用的新型类固醇衍生物,其可以通过合成有机化学有效地和立体选择性地合成。 由下式表示的类固醇衍生物:其中R是具有1至13个碳原子的烷基,A是羟基或易于水解成羟基的基团,X和Y一起形成氧代基 或具有2或3个碳原子的亚烷基二氧基,X是羟基,具有1至5个碳原子的烷氧基或易于水解成羟基的基团,Y是氢原子或具有1至5个碳原子的烷氧基 原子,条件是当X是羟基或易于水解成羟基的基团时,Y是氢原子,当X是具有1至5个碳原子的烷氧基时,Y是具有1至 5个碳原子,或其盐。
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公开(公告)号:US5347012A
公开(公告)日:1994-09-13
申请号:US952544
申请日:1992-12-11
IPC分类号: C07D335/08 , C07D409/06 , C07D521/00
CPC分类号: C07D249/08 , C07D231/12 , C07D233/56 , C07D335/08 , C07D409/06
摘要: A naphthothiopyranone derivative represented by the formula: ##STR1## (wherein R.sup.1 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms) and an acid addition salt thereof have more excellent antagonist effect at serotonin 3 receptors than the prior art compounds and the effects based thereon, e.g. anti-vomiting effect, gastrointestinal movement regulating effect and anti-anxiety effect.
摘要翻译: PCT No.PCT / JP91 / 00825 Sec。 371日期:1992年12月11日 102(e)日期1992年12月11日PCT提交1991年6月20日PCT公布。 公开号WO92 / 00294 日本1992年1月9日。由下式表示的萘并噻喃酮衍生物(其中R1为氢原子或碳原子数1〜4的烷基)及其酸加成盐在5-羟色胺3中具有更好的拮抗作用 受体比现有技术化合物和基于其的效果,例如 抗呕吐作用,消化道运动调节作用及抗焦虑作用。
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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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