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    Process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes
    1.
    发明授权
    Process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes 失效
    制备10-甲基-2,9-二氧杂三环[4,3,1,03,7]癸烷的方法

    公开(公告)号：US4182889A

    公开(公告)日：1980-01-08

    申请号：US826636

    申请日：1977-08-22

    申请人： Akiji Asai ,  Ivan Ban ,  Samuel David ,  Peter W. Thies

    发明人： Akiji Asai ,  Ivan Ban ,  Samuel David ,  Peter W. Thies

    IPC分类号： A61K31/335 ,  C07D319/00 ,  C07D493/08

    CPC分类号： C07D493/08

    摘要： A process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives is disclosed, wherein a 10-methylen-3-iodomethyl compound of the formula ##STR1## is hydrogenated to obtain a mixture of the corresponding epimeric 10.beta.- and 10.alpha.-methyl-3-iodomethyl compounds, the pure 10.alpha.- and 10.beta.-methyl epimers are separated and recovered from this mixture and are reacted with a secondary amine. Optionally, the substituent in the 4-position of the resulting 10.alpha.- or 10.beta.-methyl-3-aminomethyl compounds are further changed.

    摘要翻译： 公开了制备10-甲基-2,9-二氧杂三环[4,3,1,03,7]癸烷衍生物的方法，其中将式“IMAGE”的10-亚甲基-3-碘甲基化合物氢化得到 相应的差向异构10β-和10α-甲基-3-碘甲基化合物的混合物，纯的10α-和10β-甲基差向异构体被从该混合物中分离回收并与仲胺反应。 任选地，所得10α-或10β-甲基-3-氨基甲基化合物的4-位上的取代基进一步改变。

    2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives and pharmaceutical compositions thereof
    2.
    发明授权
    2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives and pharmaceutical compositions thereof 失效
    2,9-二氧三环[4,3,1,03,7]癸烷衍生物及其药物组合物

    公开(公告)号：US4207331A

    公开(公告)日：1980-06-10

    申请号：US904742

    申请日：1978-05-11

    申请人： Peter W. Thies ,  Akiji Asai ,  Samuel David

    发明人： Peter W. Thies ,  Akiji Asai ,  Samuel David

    IPC分类号： C07D493/08 ,  C07D319/08 ,  A61K31/335

    CPC分类号： C07D493/08

    摘要： New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group one of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygen one of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.

    摘要翻译： 公开了新的2,9-二氧杂三环[4,3,1,03,7]癸烷衍生物，其被C3位上的氨基甲基取代，并且其表现出镇静剂，特别是睡眠改善性质， 图像（I）其中R1表示R2中的一个，R3是氢，另一个表示羟基酰氧基或氨基甲酰氧基或R2和R3共同表示氧，R4和R5之一是氢，另一个表示烷氧基或芳烷氧基y和y “各自表示氢或共同形成键及其药理学上可接受的盐，以及其药物制剂。

    N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine derivatives and medical compositions thereof
    3.
    发明授权
    N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine derivatives and medical compositions thereof 失效
    N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺衍生物及其医药组合物

    公开(公告)号：US4714709A

    公开(公告)日：1987-12-22

    申请号：US653707

    申请日：1984-09-24

    申请人： Peter W. Thies ,  Samuel David ,  Ulrich Kuehl ,  Gerd Buschmann ,  Peter Flecker

    发明人： Peter W. Thies ,  Samuel David ,  Ulrich Kuehl ,  Gerd Buschmann ,  Peter Flecker

    IPC分类号： A61K31/35 ,  A61K31/357 ,  A61P9/12 ,  C07D319/00 ,  C07D493/08 ,  A61K31/40 ,  C07D405/12

    CPC分类号： C07D493/08

    摘要： N-(2,10-dioxa-tricyclo-[5,3,1,0.sup.3,8 ]-undecane-5-yl)-tryptamine compounds corresponding to the formula ##STR1## with blood-pressure lowering effects, a method of producing such compounds and pharmaceutical compositions incorporating such compounds, wherein R.sub.1 is hydrogen, a benzyl or lower alkyl group; R.sub.2 is a lower alkyl or lower alkanoyl group; R.sub.3 is hydrogen or a lower alkyl group; R.sub.4 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; R.sub.5 is hydrogen, benzyloxy, hydroxy or a lower alkoxy group; and A and B either are both hydrogen or together represent a bond between their respective carbons.

    摘要翻译： 对应于具有降血压效果的式“IMAGE”I的N-（2,10-二氧杂 - 三环 - [5,3,1,03,8] - 十一烷-5-基） - 色胺化合物， 制备这样的化合物和掺入这种化合物的药物组合物，其中R 1是氢，苄基或低级烷基; R2是低级烷基或低级烷酰基; R3是氢或低级烷基; R4是氢，苄氧基，羟基或低级烷氧基; R5是氢，苄氧基，羟基或低级烷氧基; 并且A和B既可以是氢，也可以一起表示它们各自的碳之间的键。

    2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives, processes for their preparation and pharmaceutical compositions thereof
    4.
    发明授权
    2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives, processes for their preparation and pharmaceutical compositions thereof 失效
    2,9-二氧杂三环[8 4,3,1,0 {hu 3,7 {b {9癸烷衍生物，其制备方法及其药物组合物

    公开(公告)号：US4141988A

    公开(公告)日：1979-02-27

    申请号：US874626

    申请日：1978-02-02

    申请人： Peter W. Thies ,  Samuel David ,  Hartmut Hauth ,  Dietmar Roemer

    发明人： Peter W. Thies ,  Samuel David ,  Hartmut Hauth ,  Dietmar Roemer

    IPC分类号： A61K31/35 ,  A61P25/04 ,  C07D493/08 ,  A61K31/335 ,  C07D319/08

    CPC分类号： C07D493/08

    摘要： 4-amino-3-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ]decane derivatives are disclosed which exhibit analgesic properties, and which have the formula (I) ##STR1## wherein ONE OF R.sub.1 and R.sub.2 represents hydrogen and the other represents an amino group which is substituted by an arylalkyl group or an arylalkenyl group,One of R.sub.3 and R.sub.4 represents hydrogen and the other represents alkoxy, andY and y' each represent hydrogen or jointly form a bond, and pharmaceutically acceptable acid addition salts thereof, as well as pharmaceutical formulations thereof.

    摘要翻译： 公开了具有镇痛特性的4-氨基-3-甲基-2,9-二氧杂三环[4,3,1,03,7]癸烷衍生物，其具有式（I）其中一个 R1和R2表示氢，另一个表示被芳烷基或芳烯基取代的氨基，其中一个R 3和R 4表示氢，另一个表示烷氧基，Y和Y各自表示氢或稠合形式 ，以及药学上可接受的酸添加量，以及其药物配方。

    2,9-Dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds and process of making same
    5.
    发明授权
    2,9-Dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds and process of making same 失效
    2,9-二氧杂三环[4,3,1,03,7]癸烷化合物及其制备方法

    公开(公告)号：US4391819A

    公开(公告)日：1983-07-05

    申请号：US283104

    申请日：1981-07-13

    申请人： Peter W. Thies ,  Samuel David

    发明人： Peter W. Thies ,  Samuel David

    IPC分类号： C07D311/00 ,  C07D311/94 ,  C07D493/00 ,  C07D493/08 ,  A61K31/335 ,  C07D405/06

    CPC分类号： C07D493/08 ,  C07D311/94 ,  Y10S514/923

    摘要： Novel and highly effective sleep inducing 3.beta.-hydroxy methyl-4.alpha.-hydroxy-8.beta.-alkoxy-2,9-dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds of the following Formula: ##STR1## in which R.sub.1 indicates an alkoxy group and preferably a lower alkoxy group, such as the methoxy group, the ethoxy group, or the n-butoxy group, whileR.sub.2 indicates the 10-methylene group or the 10.beta.-methyl group, are produced from didrovaltratum, i.e., 1-isovaleroxy-4-isovaleroxy methyl-7-acetoxy-spiro-oxirano-1,9-dihydrocyclopenta(c)pyrane or from extracts of plants of the genus Valerianaceae which contain about 70% of didrovaltratum. The novel compounds have a surprisingly low toxicity.

    摘要翻译： 诱导3β-羟基甲基-4α-羟基-8β-烷氧基-2,9-二氧杂三环[4,3,1,03,7]癸烷化合物的新型和高效睡眠下列化学式： in R1表示烷氧基，优选为低级烷氧基，例如甲氧基，乙氧基或正丁氧基，R2表示10-亚甲基或10β-甲基，由didrovaltalatum ，即1-异戊氧基-4-异戊氧基甲基-7-乙酰氧基 - 螺 - 环氧基-1,9-二氢环戊（c）pyrane，或来自含有约70％didrovaltratum的缬草科植物的提取物。 新化合物具有惊人的低毒性。

    2,6-Dioxa-bicyclo-[2,2,2]-octane-7-yl-acetaldehydes
    8.
    发明授权
    2,6-Dioxa-bicyclo-[2,2,2]-octane-7-yl-acetaldehydes 失效
    2,6-二氧杂 - 双环 - [2,2,2] - 辛烷-7-基 - 乙醛

    公开(公告)号：US4526991A

    公开(公告)日：1985-07-02

    申请号：US653708

    申请日：1984-09-24

    申请人： Peter W. Thies ,  Samuel David

    发明人： Peter W. Thies ,  Samuel David

    IPC分类号： C07D319/00 ,  C07D493/08 ,  C07D319/14

    CPC分类号： C07D493/08

    摘要： 2,6-Dioxa-bicyclo-[2,2,2]-octane-7-yl-acetaldehydes of the general Formula I, ##STR1## wherein R.sub.1 is a benzyl or lower alkyl group, and A and B either are each hydrogen or together represent a single bond between their respective carbons, and a method for producing such compounds. The compounds are valuable intermediates in the synthesis of pharmacologically active substances having, for example, cardiovascular effects.

    摘要翻译： 2,6-二氧杂 - 双环 - [2,2,2] - 辛烷-7-基 - 乙醛，通式Ⅰ，其中R1是苄基或低级烷基，A和B分别为 氢或一起表示它们各自的碳之间的单键，以及这些化合物的制造方法。 这些化合物是合成具有例如心血管效应的药理活性物质的有价值的中间体。

    2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives, processes for their preparation and pharmaceutical compositions thereof
    9.
    发明授权
    2,9-Dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives, processes for their preparation and pharmaceutical compositions thereof 失效
    2,9-二氧杂三环[8 4,3,1,0 {hu 3,7 {b {9癸烷衍生物，其制备方法及其药物组合物

    公开(公告)号：US4158061A

    公开(公告)日：1979-06-12

    申请号：US897802

    申请日：1978-04-19

    申请人： Peter W. Thies ,  Samuel David

    发明人： Peter W. Thies ,  Samuel David

    IPC分类号： C07D493/08 ,  A61K31/335

    CPC分类号： C07D493/08

    摘要： 3-Azidomethyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which exhibit analgesic, as well as antipyretic and antiphlogistic properties, and which have the formula (I) ##STR1## wherein: R.sub.1 represents alkyloxy or aralkyloxy;One of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy, acyloxy or carbamyloxy, or R.sub.2 and R.sub.3 jointly represent oxygen; and,Y and y' each represent hydrogen or jointly form a bond,As well as pharmaceutical formulations thereof.By reducing the 3-azidomethyl compounds of formula (I), the corresponding 3-aminomethyl compounds are obtained which possess sedative properties and which are valuable intermediates for preparing 3-(mono- or dialkylaminomethyl)-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes which exhibit sedative and soporific activities.

    摘要翻译： 公开了具有镇痛作用的3-叠氮基甲基-2,9-二氧杂三环[4,3,1,03,7]癸烷衍生物，以及解热和消炎性质，其具有式（I） 其中：