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1. 发明申请

WO1994008959A1 PROSTAGLANDINE DERIVATIVE 审中-公开
公开(公告)号：WO1994008959A1
公开(公告)日：1994-04-28
申请号：PCT/JP1993001493
申请日：1993-10-18
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/0016
摘要： A prostaglandine derivative represented by general formula (I), wherein R represents hydrogen or C1-C6 alkyl, and R represents cyclohexyl or cyclopentylmethyl. It has various physiological activities including the inhibition of platelet aggregation and the dilation of renal and coronary blood vessels, thus being useful for treating nephropathy and cardiovascular diseases.
摘要翻译：由通式（I）表示的前列腺素衍生物，其中R 1表示氢或C 1 -C 6烷基，R 2表示环己基或环戊基甲基。它具有各种生理活性，包括抑制血小板聚集和肾和冠状血管扩张，因此可用于治疗肾病和心血管疾病。

2. 发明申请

WO1994002457A1 PROSTAGLANDIN DERIVATIVE 审中-公开
公开(公告)号：WO1994002457A1
公开(公告)日：1994-02-03
申请号：PCT/JP1993000938
申请日：1993-07-08
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/0016 , C07C405/00
摘要： To provide a novel PG derivative with an excellent platelet aggregation inhibitor effect. A prostaglandin derivative represented by general formula (I) and a salt thereof.
摘要翻译：提供具有优异血小板聚集抑制作用的新型PG衍生物。由通式（I）表示的前列腺素衍生物及其盐。

3. 发明申请

WO1992018472A1 PROSTAGLANDIN E1 ANALOGUE 审中-公开
标题翻译： PROSTAGLANDIN E1模拟
公开(公告)号：WO1992018472A1
公开(公告)日：1992-10-29
申请号：PCT/JP1992000513
申请日：1992-04-21
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： Object: to provide a novel prostaglandin E1 which is excellent in drug efficacy while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE1 analogue represented by general formula (I) and its salt, wherein A represents vinylene or ethynylene; R represents hydrogen, C1 to C6 alkyl or aryl; and R represents C5 to C10 branched aliphatic hydrocarbyl.
摘要翻译：目的：提供一种与常规药物相比，药物功效优异，不良反应减少的新型前列腺素E1。结构：由通式（I）表示的PGE1类似物及其盐，其中A表示亚乙烯基或亚乙炔基; R 1表示氢，C 1至C 6烷基或芳基; 且R 2表示C5至C10支链脂族烃基。

4. 发明申请

WO1994008961A1 PROSTAGLANDIN E1 ANALOG 审中-公开
标题翻译： PROSTAGLANDIN E1模拟
公开(公告)号：WO1994008961A1
公开(公告)日：1994-04-28
申请号：PCT/JP1993001510
申请日：1993-10-20
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/0025 , C07C405/0033
摘要： A prostaglandin E1 analog represented by formula (I), wherein R represents hydrogen or C1-C6 alkyl; and X represents oxygen and R represents (a) or (b); or alternatively, X represents sulfur and R represents (c). This compound has a potent and persistent platelet aggregation inhibitor activity and is useful for treating various thrombotic diseases typified by peripheral circulatory disturbance.
摘要翻译：由式（I）表示的前列腺素E1类似物，其中R 1表示氢或C 1 -C 6烷基; X表示氧，R 2表示（a）或（b）。或者，X表示硫，R 2表示（c）。该化合物具有有效和持久的血小板聚集抑制剂活性，可用于治疗以周围循环障碍为代表的各种血栓性疾病。

5. 发明申请

WO1995018101A1 PROSTAGLANDIN DERIVATIVE, SALT THEREOF, AND USE THEREOF 审中-公开
标题翻译： PROSTAGLANDIN衍生物，其盐及其用途
公开(公告)号：WO1995018101A1
公开(公告)日：1995-07-06
申请号：PCT/JP1994002267
申请日：1994-12-27
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/0033
摘要： A prostaglandin derivative represented by general formula (I), a salt thereof, and a medicinal composition containing the same as the active ingredient for lowering the ocular tension. In said formula, R represents hydrogen, C1-C10 alkyl or C3-C10 cycloalkyl; R represents C3-C10 cycloalkyl optionally substituted by methyl, C1-C3 alkyl substituted by C3-C10 cycloalkyl, or C5-C10 branched alkyl or alkenyl; X represents alpha - or ss- chloro; and A represents ethylene, vinylene or ethynylene. This compound is useful as an ocular tension depressant which is free from side effects of, e.g., transient increased tension or is extremely reduced in these side effects.
摘要翻译：由通式（I）表示的前列腺素衍生物及其盐，以及含有与用于降低眼睛张力的活性成分相同的药物组合物。在所述式中，R 1表示氢，C 1 -C 10烷基或C 3 -C 10环烷基; R 2表示任选被甲基取代的C 3 -C 10环烷基，被C 3 -C 10环烷基取代的C 1 -C 3烷基或C 5 -C 10支链烷基或烯基; X表示α-或β-氯; A表示乙烯，亚乙烯基或亚乙炔基。该化合物可用作眼部张力抑制剂，其不含例如瞬时增加的张力或在这些副作用中极度降低的副作用。

6. 发明申请

WO1992018473A1 PROSTAGLANDIN E1 ANALOGUE 审中-公开
标题翻译： PROSTAGLANDIN E1模拟
公开(公告)号：WO1992018473A1
公开(公告)日：1992-10-29
申请号：PCT/JP1992000514
申请日：1992-04-21
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： Object: to provide a novel prostaglandin E1 which is excellent in drug efficacy and prolonged action while reduced in adverse reactions as compared with conventional ones. Constitution: a PGE1 analogue represented by general formula (I) and its salt, wherein R represents hydrogen, C1 to C6 alkyl or aryl; and R represents C3 to C6 alkyl or C3 to C6 alkenyl.
摘要翻译：目的：提供一种与常规的相比，药物功效优异且延长作用，同时减少不良反应的新型前列腺素E1。结构：由通式（I）表示的PGE1类似物及其盐，其中R 1表示氢，C 1至C 6烷基或芳基; 且R 2表示C 3至C 6烷基或C 3至C 6烯基。

7. 发明申请

WO1994027962A1 PROSTAGLANDIN E1 ANALOG 审中-公开
标题翻译： PROSTAGLANDIN E1模拟
公开(公告)号：WO1994027962A1
公开(公告)日：1994-12-08
申请号：PCT/JP1994000635
申请日：1994-04-18
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/00 , C07C405/0041
摘要： To provide a novel PGE1 analog having cytoprotective and gastric secretoinhibitory effects superior to those of the conventional PGE1 analogs and being excellent in the persistence of drug effect and reduced in side effects. A prostaglandin E1 analog represented by general formula (I) wherein R represents hydrogen, C1-C8 alkyl or C3-C8 cycloalkyl; and A represents oxygen or -NH-.
摘要翻译：提供具有优于常规PGE1类似物的细胞保护和胃分泌抑制作用的新型PGE1类似物，并且药物作用的持久性和副作用降低。由通式（I）表示的前列腺素E1类似物，其中R表示氢，C1-C8烷基或C3-C8环烷基; A表示氧或-NH-。

8. 发明申请

WO1995033845A1 PROCESS FOR PRODUCING OPTICALLY ACTIVE PROPARGYL ALCOHOL COMPOUND 审中-公开
标题翻译：用于生产光学活性丙醇醇化合物的方法
公开(公告)号：WO1995033845A1
公开(公告)日：1995-12-14
申请号：PCT/JP1995001064
申请日：1995-05-31
申请人： TAISHO PHARMACEUTICAL CO., LTD. , KAMEO, Kazuya , TANAMI, Tohru , TANAKA, Hideo , SHIMAZAKI, Yohichi , MUTOH, Masaru , TSUBOI, Mie , ONO, Naoya , HATAYAMA, Katsuo
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C12P41/00
CPC分类号： C12P41/004 , C12P7/62
摘要： A process for stereoselectively obtaining an optically active O-acylpropargyl alcohol compound represented by general formula (2) (wherein R and R represent each hydrogen or C1-C3 alkyl; R represents phenyl which may be substituted by C1-C5 alkyl, halogeno or trifluoromethyl at an arbitrary position of the ring, C1-C8 alkyl or C5-C8 cycloalkyl; R represents C1-C10 alkyl or phenyl which may be substituted by phenyl or halogeno at an arbitrary position of the ring; and the asterisk represents optical activity) by the reaction of an (RS)-propargyl alcohol compound represented by general formula (1) (wherein R , R and R are each as defined above) with an acylating agent R COOR (wherein R is as defined above; and R represents arbitrary alkyl or alkenyl) in the presence of an enzyme; and a process for obtaining an optically active propargyl alcohol compound either by hydrolyzing the above O-acyl compound or from the solution of the above acylation reaction.
摘要翻译：立体选择性地获得由通式（2）表示的光学活性O-酰基炔丙醇化合物的方法（其中R 1和R 2各自表示氢或C 1 -C 3烷基; R 3表示可被取代的苯基） C 1 -C 5烷基，C 1 -C 8烷基或C 5 -C 8环烷基上的C 1 -C 5烷基，卤代或三氟甲基; R 4表示任选位置可被苯基或卤素取代的C 1 -C 10烷基或苯基通过由通式（1）表示的（RS） - 炔丙醇化合物（其中R 1，R 2和R 3各自如上所定义）反应而得到的环，星号表示光学活性）上述）与酰化剂R 4 COOR（其中R 4如上所定义; R表示任意的烷基或链烯基）; 以及通过水解上述O-酰基化合物或从上述酰化反应的溶液获得光学活性炔丙醇化合物的方法。

9. 发明申请

WO1994008960A1 PROSTAGLANDIN E1 ANALOG 审中-公开
标题翻译： PROSTAGLANDIN E1模拟
公开(公告)号：WO1994008960A1
公开(公告)日：1994-04-28
申请号：PCT/JP1993001506
申请日：1993-10-20
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： C07C405/00
摘要： A prostaglandin E1 analog represented by formula (I), wherein A represents vinylene or ethinylene; and R represents hydrogen, C1-C8 alkyl or C3-C8 cycloalkyl. This compound has a selective, persistent and potent antiulcerative effect and hence is useful for treating peptic ulcer.
摘要翻译：由式（I）表示的前列腺素E1类似物，其中A表示亚乙烯基或亚乙烯基; 且R 1表示氢，C 1 -C 8烷基或C 3 -C 8环烷基。该化合物具有选择性，持久和有效的抗溃疡作用，因此可用于治疗消化性溃疡。

10. 发明申请

WO1993016041A1 PROCESS FOR PRODUCING PROSTAGLANDIN E 审中-公开
标题翻译：生产PROSTAGLANDIN的方法E
公开(公告)号：WO1993016041A1
公开(公告)日：1993-08-19
申请号：PCT/JP1993000115
申请日：1993-02-02
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SATO, Fumie , AMANO, Takehiro , KAMEO, Kazuya , TANAMI, Tohru , MUTOH, Masaru , ONO, Naoya , GOTO, Jun
发明人： TAISHO PHARMACEUTICAL CO., LTD.
IPC分类号： C07C405/00
CPC分类号： B01J31/2404 , B01J31/0237 , B01J31/0267 , B01J31/04 , B01J31/223 , B01J31/2282 , B01J31/2291 , B01J2531/824 , C07C405/00 , Y02P20/55
摘要： To produce a prostaglandin E in a short time and in a high yield while minimizing the formation of isomers. A process for producing a prostaglandin E represented by general formula (I) wherein A represents an arbitrary group not participating in the reaction; B represents vinylene or ethynylene; R and R may be the same or different from each other and each represents hydrogen or a protective group for a hydroxyl group; and R and R represent each an arbitrary group not participating in the reaction, which comprises reacting an allyl ester of a prostaglandin E represented by general formula (II) wherein R and R may be the same or different from each other and each represents hydrogen or lower alkyl; R represents hydrogen, lower alkyl, alkenyl or aryl; and R , R , R , R , A and B are each as defined above, with one or two compounds selected from the group consisting of bases and formic acid in the presence of a complex compound or a complex salt of 0-valent or divalent palladium atom.
摘要翻译：在短时间内以高产率产生前列腺素E，同时最小化异构体的形成。一种由通式（I）表示的前列腺素E的制备方法，其中A表示不参与反应的任意基团; B代表亚乙烯基或亚乙炔基; R 4和R 5可以彼此相同或不同，并且各自表示氢或羟基的保护基; R 6和R 7各自表示不参与反应的任意组，其包括使通式（II）表示的前列腺素E的烯丙酯与其中R 1和R 2可以是相同或不同，各自表示氢或低级烷基; R 3表示氢，低级烷基，烯基或芳基; 和R 4，R 5，R 6，R 7，A和B各自如上所定义，在一种有机溶剂存在下，使用一种或两种选自碱和甲酸的化合物络合物或0价或二价钯原子的络盐。

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