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1.发明授权Method of use of bicycloheptane substituted prostaglandin analogs as cardiovascular agents 失效使用双环庚烷取代的前列腺素类似物作为心血管药物的方法
公开(公告)号：US4542160A
公开(公告)日：1985-09-17
申请号：US635980
申请日：1984-07-30
IPC分类号： C07C405/00 , A61K31/19 , A61K31/21
CPC分类号： C07C405/00 , C07C405/0091 , Y10S514/826
摘要： Bicycloheptane substituted prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译： 提供具有结构式“IMAGE”并且包括其所有立体异构体的双环庚烷取代的前列腺素类似物。 该化合物是可用于例如治疗溶栓性疾病的心血管药。
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公开(公告)号：US4537981A
公开(公告)日：1985-08-27
申请号：US378547
申请日：1982-05-17
IPC分类号： C07C35/36 , C07D493/08 , C07F7/18 , C07F9/40
CPC分类号： C07D493/08 , C07C35/36 , C07F7/1856 , C07F9/4006 , C07F9/4018 , C07F9/4059
摘要： 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译： 提供7-氧杂双环庚烷和7-氧杂双环庚烯前列腺素类似物，具有结构式Ⅰ和其所有的立体异构体。 该化合物是可用于例如治疗溶栓性疾病的心血管药。
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3.发明授权6,6-Difluoro-5-hydroxy-4-(3-oxoalk-1-enyl)hexahydro cyclopenta[b] furan-2-ols 失效6,6-二氟-5-羟基-4-（3-氧代-1'-烯基）六氢环戊二烯并[b]呋喃-2-醇
公开(公告)号：US4362872A
公开(公告)日：1982-12-07
申请号：US305053
申请日：1981-09-24
IPC分类号： C07C29/03 , C07C29/128 , C07C29/48 , C07D307/935 , C07D307/937
CPC分类号： C07D307/935 , C07C29/03 , C07C29/1285 , C07C29/48 , C07D307/937 , C07B2200/07 , C07C2102/24
摘要： A method is provided for preparing intermediates for use in prostacyclin syntheses which method includes the steps of aceylating ketopinic acid or its acid halide to form the corresponding ketopinoyl diene ester intermediate, subjecting the diene ester to a Diels-Alder reaction by reacting same with cyclopentendione, subjecting the resulting chiral ester intermediate to a fluorination and reduction to form the corresponding chiral ester diol intermediate, subjecting the diol to solvolysis to form the chiral triol intermediate, hydroxylating the chiral triol to form a pentol intermediate, subjecting the pentol to a ring cleavage to form the difluoro dihydroxy prostacyclin intermediate: ##STR1## and subjecting same to a Wittig reaction to form the difluoro dihydroxy prostacyclin intermediate: ##STR2## All of the above-mentioned intermediates are novel compounds and thus are also provided.
摘要翻译： 提供了一种用于制备用于前列环素合成的中间体的方法，该方法包括以下步骤：将酮酸或其酰卤乙酰化形成相应的酮戊二烯二烯酯中间体，使二烯酯与环戊二酮反应进行狄尔斯 - 阿尔德反应， 使得到的手性酯中间体进行氟化和还原以形成相应的手性酯二醇中间体，使二醇溶剂分解形成手性三醇中间体，羟基化手性三醇以形成戊酸中间体，使戊醇进行环切割 形成二氟二羟基前列环素中间体：
并使其进行维蒂希反应以形成二氟二羟基前列环素中间体：所有上述中间体都是新化合物，因此也被提供。 -
公开(公告)号：US4424376A
公开(公告)日：1984-01-03
申请号：US422244
申请日：1982-09-23
IPC分类号： C07C29/03 , C07C29/128 , C07C29/48 , C07D307/935 , C07D307/937 , C07C35/32 , C07C69/757
CPC分类号： C07D307/935 , C07C29/03 , C07C29/1285 , C07C29/48 , C07D307/937 , C12C11/02 , C07C2101/06 , C07C2102/46
摘要： A method is provided for preparing intermediates for use in prostacyclin syntheses which method includes the steps of aceylating ketopinic acid or its acid halide to form the corresponding ketopinoyl diene ester intermediate, subjecting the diene ester to a Diels-Alder reaction by reacting same with cyclopentendione, subjecting the resulting chiral ester intermediate to a fluorination and reduction to form the corresponding chiral ester diol intermediate, subjecting the diol to solvolysis to form the chiral triol intermediate, hydroxylating the chiral triol to form a pentol intermediate, subjecting the pentol to a ring cleavage to form the difluoro dihydroxy prostacyclin intermediate ##STR1## and subjecting same to a Witting reaction to form the difluoro dihydroxy prostacyclin intermediate ##STR2## All of the above-mentioned intermediates are novel compounds and thus are also provided.
摘要翻译： 提供了一种用于制备用于前列环素合成的中间体的方法，该方法包括以下步骤：将酮酸或其酰卤乙酰化形成相应的酮戊二烯二烯酯中间体，使二烯酯与环戊二酮反应进行狄尔斯 - 阿尔德反应， 使得到的手性酯中间体进行氟化和还原以形成相应的手性酯二醇中间体，使二醇溶剂分解形成手性三醇中间体，羟基化手性三醇以形成戊酸中间体，使戊醇进行环切割 形成二氟二羟基前列环素中间体＆lt; IMAGE＆gt;并使其进行Witting反应以形成二氟二羟基前列环素中间体所有上述中间体都是新化合物，因此也被提供。
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公开(公告)号：US4360685A
公开(公告)日：1982-11-23
申请号：US305663
申请日：1981-09-25
IPC分类号： C07D493/22 , A61K31/34 , A61K31/35 , A61P7/02 , C07D493/08 , C07D493/18 , C07D311/78 , C07D307/93
CPC分类号： C07D493/08 , Y10S514/822
摘要： New dioxatricyclic prostacyclin analogs are provided which have the general formula ##STR1## wherein R is hydrogen or lower alkyl, Q is a single bond or --CH.sub.2 --, m is 1 to 9 and n is 3 or 4, and all stereoisomers thereof, and are useful as cardiovascular agents.
摘要翻译： 提供了具有通式为：其中R为氢或低级烷基，Q为单键或-CH 2 - ，m为1至9且n为3或4的通式的新的二氧杂三环环前列环素类似物，并且所有立体异构体 并且可用作心血管药剂。
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公开(公告)号：US4614825A
公开(公告)日：1986-09-30
申请号：US758908
申请日：1985-07-25
IPC分类号： C07C29/42 , C07C35/36 , C07D493/08 , C07F7/18 , C07F9/40 , A61K31/41 , A61K31/335 , C07D257/04 , C07D307/00
CPC分类号： C07D493/08 , C07C29/42 , C07C35/36 , C07F7/1804 , C07F9/4006 , C07F9/4018 , C07F9/4059
摘要： 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译： 提供7-氧杂双环庚烷和7-氧杂双环庚烯前列腺素类似物，具有结构式Ⅰ和其所有的立体异构体。 该化合物是可用于例如治疗溶栓性疾病的心血管药。
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7.发明授权Compositions of 7-oxabicycloheptane and 7-oxabicycloheptene compounds and a method for their use in inhibiting bronchoconstriction 失效7-氧杂双环庚烷和7-氧杂双环庚烯化合物的组合物及其用于抑制支气管收缩的方法
公开(公告)号：US4537904A
公开(公告)日：1985-08-27
申请号：US518227
申请日：1983-07-28
CPC分类号： C07D493/08 , C07C29/42 , C07C35/36 , C07F7/1804 , C07F9/4006 , C07F9/4018 , C07F9/4059
摘要： 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
摘要翻译： 提供7-氧杂双环庚烷和7-氧杂双环庚烯前列腺素类似物，其具有结构式Ⅰ和其所有的立体异构体。 该化合物是可用于例如治疗溶栓性疾病的心血管药。
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8.发明授权Method for preparing 10,10-difluoro prostacyclin intermediates and new compounds produced thereby 失效制备10,10-二氟前列环素中间体的方法和由此制备的新化合物
公开(公告)号：US4311644A
公开(公告)日：1982-01-19
申请号：US230133
申请日：1981-01-30
IPC分类号： C07C29/03 , C07C29/128 , C07C29/48 , C07D307/935 , C07D307/937
CPC分类号： C07D307/935 , C07C29/03 , C07C29/1285 , C07C29/48 , C07D307/937 , C07B2200/07 , C07C2102/24
摘要： A method is provided for preparing intermediates for use in 10,10-difluoro prostacyclin syntheses which method includes the steps of aceylating ketopinic acid or its acid halide to form the corresponding ketopinoyl diene ester intermediate, subjecting the diene ester to a Diels-Alder reaction by reacting same with cyclopentendione, subjecting the resulting chiral ester intermediate to a fluorination and reduction to form the corresponding chiral ester diol intermediate, subjecting the diol to solvolysis to form the chiral triol intermediate, hydroxylating the chiral triol to form a pentol intermediate, subjecting the pentol to a ring cleavage to form the difluoro dihydroxy prostacyclin intermediate ##STR1## and subjecting same to a Wittig reaction to form the difluoro dihydroxy prostacyclin intermediate ##STR2## All of the above-mentioned intermediates are novel compounds and thus are also provided.
摘要翻译： 提供了一种用于制备用于10,10-二氟前列环素合成的中间体的方法，该方法包括以下步骤：将酮苯甲酸或其酰基卤乙酰化形成相应的酮戊二烯二烯酯中间体，使二烯酯通过 与环戊二酮反应，使得到的手性酯中间体进行氟化和还原反应，形成相应的手性酯二醇中间体，使二醇溶剂分解形成手性三醇中间体，羟基化手性三醇以形成戊酸中间体， 以形成二氟二羟基前列环素中间体“IMAGE”，并使其进行维蒂希反应以形成二氟二羟基前列环素中间体所有上述中间体都是新化合物，因此也被提供。
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公开(公告)号：US4556675A
公开(公告)日：1985-12-03
申请号：US518245
申请日：1983-07-28
CPC分类号： C07D493/08 , C07C29/42 , C07C35/36 , C07F7/1804 , C07F9/4006 , C07F9/4018 , C07F9/4059
摘要： 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
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公开(公告)号：US4420626A
公开(公告)日：1983-12-13
申请号：US393207
申请日：1982-06-28
IPC分类号： C07D493/08 , C07D493/18 , C07D311/78 , C07D307/93
CPC分类号： C07D493/08
摘要： New dioxatricyclic prostacyclin analogs are provided which have the general formula ##STR1## wherein R is hydrogen or lower alkyl, Q is a single bond or --CH.sub.2 --, m is 1 to 9 and n is 3 or 4, and all stereoisomers thereof, and are useful as cardiovascular agents.
摘要翻译： 提供了具有通式为：其中R为氢或低级烷基，Q为单键或-CH 2 - ，m为1至9，n为3或4的通式的新的二氧杂环类环前列环素类似物，全部为 其立体异构体，并且可用作心血管剂。
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