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公开(公告)号:US4436939A
公开(公告)日:1984-03-13
申请号:US411481
申请日:1982-08-25
申请人: Takehiro Amano , Kensei Yoshikawa , Tatsuhiko Sano , Yutaka Ohuchi , Michihiro Ishiguro , Manzo Shiono , Yoshiji Fujita , Takashi Nishida
发明人: Takehiro Amano , Kensei Yoshikawa , Tatsuhiko Sano , Yutaka Ohuchi , Michihiro Ishiguro , Manzo Shiono , Yoshiji Fujita , Takashi Nishida
摘要: A process for producing 1-(p-prenylphenyl)ethanol, which comprises reacting p-chloroprenylbenzene with magnesium at a temperature between 100.degree. C. and 150.degree. C. to form a Grignard reagent, and then reacting it with acetaldehyde.
摘要翻译: 一种生产1-(对异戊基苯基)乙醇的方法,其包括在100℃至150℃的温度下使对氯丙烯基苯与镁反应,形成格氏试剂,然后与乙醛反应。
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公开(公告)号:US4433160A
公开(公告)日:1984-02-21
申请号:US411480
申请日:1982-08-25
申请人: Takehiro Amano , Kensei Yoshikawa , Tatsuhiko Sano , Yutaka Ohuchi , Michihiro Ishiguro , Manzo Shiono , Yoshiji Fujita , Takashi Nishida
发明人: Takehiro Amano , Kensei Yoshikawa , Tatsuhiko Sano , Yutaka Ohuchi , Michihiro Ishiguro , Manzo Shiono , Yoshiji Fujita , Takashi Nishida
IPC分类号: C07C69/003 , B01J27/128 , B01J31/18 , C07B61/00 , C07C57/30 , C07C57/42 , C07C67/30 , C07C69/612 , C07D207/20 , C07D263/56 , C07D263/57 , C07D333/24 , C07D471/04 , C07D491/04 , C07D491/052
CPC分类号: C07D263/57 , C07C57/30 , C07C57/42 , C07D207/20 , C07D333/24 , C07D471/04 , C07D491/04
摘要: A process for producing an .alpha.-arylalkanoic acid ester represented by the general formula ##STR1## wherein Ar represents an aryl group which may optionally be substituted, and R.sup.1 and R.sup.2, independently from each other, represent a lower alkyl group,which comprises reacting a Grignard reagent prepared from an aryl halide of the general formulaAr--X.sup.1 (II)wherein Ar is as defined above and X.sup.1 represents a halogen atom,and magnesium, with an .alpha.-haloalkanoic acid ester of the general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, and X.sup.2 represents a halogen atom,said reaction of the Grignard reagent with the .alpha.-haloalkanoic acid ester of general formula (III) being carried out in the presence of a nickel compound.
摘要翻译: 制备由通式(I)表示的α-芳基链烷酸酯的方法,其中Ar表示可任意取代的芳基,R 1和R 2彼此独立地表示低级烷基,其中 包括使由通式Ar-X1(II)的芳基卤制得的格利雅试剂与其中Ar定义如上并且X1表示卤素原子的镁反应,与通式为“IMAGE”的α-卤代链烷酸酯反应, (III)其中R1和R2如上定义,X2表示卤素原子,所述格利雅试剂与通式(III)的α-卤代烷酸酯的反应在镍化合物的存在下进行。
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公开(公告)号:US4420631A
公开(公告)日:1983-12-13
申请号:US379632
申请日:1982-05-19
申请人: Takehiro Amano , Toshihisa Ogawa , Kensei Yoshikawa , Yoshinori Shiobara , Tatsuhiko Sano , Yutaka Ohuchi , Tohru Tanami , Shoichi Ito , Jiro Sawada
发明人: Takehiro Amano , Toshihisa Ogawa , Kensei Yoshikawa , Yoshinori Shiobara , Tatsuhiko Sano , Yutaka Ohuchi , Tohru Tanami , Shoichi Ito , Jiro Sawada
IPC分类号: C07C69/618 , A61K31/215 , A61P29/00 , C07D307/12
CPC分类号: C07D307/12
摘要: A novel carboxylic acid ester having the following general formula ##STR1## wherein R is alkoxyalkyl having 2 to 6 carbon atoms, cycloalkyl having 5 or 6 carbon atoms, tetrahydrofurfuryl, or alkyl having 1 to 6 carbon atoms optionally substituted with 1 or 2 hydroxyl groups, is a useful anti-inflammatory and analgesic agent.
摘要翻译: 具有以下通式的新型羧酸酯:其中R为具有2至6个碳原子的烷氧基烷基,具有5或6个碳原子的环烷基,四氢糠基或具有1至6个碳原子的烷基,任选被1或2个羟基取代 ,是一种有用的消炎止痛剂。
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公开(公告)号:US4189607A
公开(公告)日:1980-02-19
申请号:US24110
申请日:1979-03-26
IPC分类号: A01N37/44 , C07C101/453 , A01N9/20
CPC分类号: A01N37/44
摘要: Anilinotropone derivatives represented by the following formula: ##STR1## wherein R is hydrogen or methyl and pharmaceutically acceptable salts thereof are disclosed. They exhibit anti-inflammatory and analgesic activity with low gastrointestinal action.
摘要翻译: 由下式表示的Anilinotropon衍生物:其中R是氢或甲基及其药学上可接受的盐。 它们具有抗消炎和镇痛作用,具有低胃肠作用。
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公开(公告)号:US5648526A
公开(公告)日:1997-07-15
申请号:US256924
申请日:1994-07-29
申请人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号: B01J31/22 , B01J31/24 , C07B61/00 , C07C405/00
CPC分类号: B01J31/2404 , B01J31/0237 , B01J31/0267 , B01J31/04 , B01J31/223 , B01J31/2282 , B01J31/2291 , C07C405/00 , B01J2531/824 , Y02P20/55
摘要: Object: To produce E-prostaglandins in a high yield and in a short time with suppressed formation of isomers.Structure: A process for preparing E-prostaglandins represented by the formula: ##STR1## (wherein A, R.sup.6 and R.sup.7 represent respectively an arbitrary group which does not participate in the reaction; B represents a vinylene or ethynylene group; and R.sup.4 and R.sup.5 may be the same or different from each other and each represents a hydrogen atom or a protective group of the hydroxyl group) which comprises reacting allyl esters of E-prostaglandins represented by the formula: ##STR2## (wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a lower alkyl group, an alkenyl group or an aryl group; and A, B, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as defined above) with at least one substance selected from the group consisting of bases and formic acid in the presence of a zero- or divalent palladium complex or a salt thereof.
摘要翻译: PCT No.PCT / JP93 / 00115 Sec。 371日期1994年7月29日第 102(e)日期1994年7月29日PCT提交1993年2月2日PCT公布。 公开号WO93 / 16041 日期1993年8月19日目的:以高产率和短时间产生E-前列腺素,抑制异构体的形成。 结构:由下式表示的E-前列腺素的制备方法:其中A,R6和R7分别表示不参与反应的任意基团; B表示亚乙烯基或亚乙炔基,R4和R5可以 彼此相同或不同,并且各自表示氢原子或羟基的保护基),其包括使由下式表示的E-前列腺素的烯丙基酯反应(其中R1和R2可以相同或相同) 彼此不同,各自表示氢原子或低级烷基; R 3表示氢原子,低级烷基,烯基或芳基; A,B,R 4,R 5,R 6和R 7如上所定义 上述)与至少一种选自碱或甲酸的物质在零或二价钯络合物或其盐的存在下反应。
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公开(公告)号:US5583158A
公开(公告)日:1996-12-10
申请号:US416871
申请日:1995-04-19
申请人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号: A61K31/557 , C07C405/00
CPC分类号: C07C405/0025 , C07C405/0033
摘要: A prostaglandin E.sub.1 analogue represented by formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; and X is an oxygen atom and R.sup.2 represents ##STR2## or X is a sulfur atom and R.sup.2 represents ##STR3## The compound has a strong and prolonged inhibitory action for platelet aggregation and is useful for treatment of various thrombotic diseases including peripheral circulatory disturbance.
摘要翻译: PCT No.PCT / JP93 / 01510 Sec。 371日期1995年04月19日 102(e)日期1995年4月19日PCT提交1993年10月20日PCT公布。 公开号WO94 / 08961 日本1994年4月28日由式
表示的前列腺素E1类似物,其中R1表示氢原子或C1-C6烷基; X是氧原子,R2表示 或 或X是硫原子,R2代表血小板聚集的作用,可用于治疗各种血栓形成疾病,包括外周循环障碍。 -
公开(公告)号:US4398026A
公开(公告)日:1983-08-09
申请号:US383526
申请日:1982-06-01
申请人: Seiichi Takano , Susumu Otomo , Takehiro Amano
发明人: Seiichi Takano , Susumu Otomo , Takehiro Amano
IPC分类号: A61K31/425 , A61K31/426 , A61P37/04 , C07D277/06 , C07D417/06
CPC分类号: C07D277/06
摘要: A novel thiazolidine derivative having the following general formula ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl having 1 to 3 carbon atoms, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring selected from the group consisting of morpholino, piperazino, piperidino and pyrrolidino, or said heterocyclic ring substituted with 1 or 2 methyl groups, and the pharmaceutically acceptable salts thereof are useful immunomodulators.
摘要翻译: 一种具有以下通式的新型噻唑烷衍生物,其中R 1和R 2各自为具有1至3个碳原子的低级烷基,或者R 1和R 2与它们所连接的氮原子一起形成选自以下的杂环: 吗啉代,哌嗪子基,哌啶子基和吡咯烷子基,或被1或2个甲基取代的所述杂环,其药学上可接受的盐是有用的免疫调节剂。
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公开(公告)号:US5599838A
公开(公告)日:1997-02-04
申请号:US606440
申请日:1996-02-23
申请人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号: C07C405/00 , A61K31/21
CPC分类号: C07C405/0033
摘要: A prostaglandin derivative represented by the formula: ##STR1## wherein X is halogen atom R.sup.1 is a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and R.sup.2 is a cycloalkyl group having 3 to 10 carbon atoms, a cycloalkylmethyl group having 4 to 10 carbon atoms or a cycloalkylethyl group having 5 to 12 carbon atoms, or a salt thereof, which has an excellent lowering action of intraocular pressure and improving actions of renal diseases, ischemic heart diseases and heart failure.
摘要翻译: 由下式表示的前列腺素衍生物:其中X为卤素原子,R1为氢原子或碳原子数为1〜6的烷基,R2为碳原子数3〜10的环烷基,环烷基甲基为4 至10个碳原子或具有5至12个碳原子的环烷基乙基或其盐,其具有优异的眼内降低作用和改善肾病,缺血性心脏病和心力衰竭的作用。
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公开(公告)号:US5449815A
公开(公告)日:1995-09-12
申请号:US137090
申请日:1993-10-19
申请人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
发明人: Fumie Sato , Takehiro Amano , Kazuya Kameo , Tohru Tanami , Masaru Mutoh , Naoya Ono , Jun Goto
IPC分类号: C07C405/00
CPC分类号: C07C405/00
摘要: Object: To provide novel prostaglandin E.sub.1 analogues which have more excellent pharmaceutical effects, longer duration of the effects and less side-effects than the prior art prostaglandin E.sub.1 's.Constitution: A PGE.sub.1 analogue represented by the formula: ##STR1## (wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or an allyl group, and R.sup.2 is an alkyl group having 3 to 6 carbon atoms, an alkenyl group having 3 to 6 carbon atoms), or a salt thereof.
摘要翻译: PCT No.PCT / JP92 / 00514 Sec。 371日期:1993年10月19日 102(e)日期1993年10月19日PCT 1992年4月21日PCT PCT。 WO92 / 18473 PCT出版物 日期:1992年10月29日。目的:提供与现有技术的前列腺素E1相比,具有更优异的药物作用,更长的作用时间和更少的副作用的新型前列腺素E1类似物。 结构:由下式表示的PGE1类似物:< IMAGE>(其中,R 1为氢原子,碳原子数为1〜6的烷基或烯丙基,R 2为碳原子数3〜6的烷基,烯基 具有3〜6个碳原子的基团)或其盐。
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公开(公告)号:US4686292A
公开(公告)日:1987-08-11
申请号:US838153
申请日:1986-03-10
申请人: Yoshihiro Migita , Tadashi Eguchi , Yukinari Kumazawa , Jozi Nakagami , Takehiro Amano , Kaoru Sota , Jinsaku Sakakibara
发明人: Yoshihiro Migita , Tadashi Eguchi , Yukinari Kumazawa , Jozi Nakagami , Takehiro Amano , Kaoru Sota , Jinsaku Sakakibara
IPC分类号: A61K31/495 , A61P35/00 , C07D241/38 , C07D241/46 , C07D401/06 , C07D403/06
CPC分类号: C07D241/38
摘要: Novel benzo[.alpha.]phenazine derivatives of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, methyl, hydroxyl or alkoxy, R.sup.2 is --COOR.sup.5 (wherein R.sup.5 is hydrogen, straight or branched chain alkyl, cycloalkyl having 3-6 carbon atoms, benzyl or phenyl) or ##STR2## wherein R.sup.6 and R.sup.7 are the same or different and are each hydrogen or lower alkyl, or R.sup.6 and R.sup.7 together with the nitrogen atom to which they are attached form pyrrolidine or piperidine), R.sup.3 and R.sup.4 are the same or different and are each hydrogen or lower alkyl, and n is an integer of 2 or 3, and the salts thereof are disclosed. These compounds have antitumor activity in mammals.
摘要翻译: 式(I)的新的苯并[b]吩嗪衍生物其中R 1是氢,卤素,甲基,羟基或烷氧基,R 2是-COOR 5(其中R 5是氢,直链或支链烷基,具有3-6 碳原子,苄基或苯基)或其中R6和R7相同或不同并且各自为氢或低级烷基,或R6和R7与它们所连接的氮原子一起形成吡咯烷或哌啶),R3和 R4相同或不同,各自为氢或低级烷基,n为2或3的整数,并且其盐被公开。 这些化合物在哺乳动物中具有抗肿瘤活性。
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