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31 条记录 (耗时 0.034 秒)

    2,9-Dioxa tricyclo [4,3,1,0.sup.3,7 ] decane compounds and process of making same
    21.
    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。

    Method of treating or inhibiting obesity
    23.
    发明授权
    Method of treating or inhibiting obesity 有权
    治疗或抑制肥胖症的方法

    公开(公告)号：US07238470B2

    公开(公告)日：2007-07-03

    申请号：US10785042

    申请日：2004-02-25

    申请人： Johannes Hebebrand ,  Jochen Antel ,  Ulf Preuschoff ,  Samuel David ,  Holger Sann ,  Michael Weske

    发明人： Johannes Hebebrand ,  Jochen Antel ,  Ulf Preuschoff ,  Samuel David ,  Holger Sann ,  Michael Weske

    IPC分类号： C12Q1/00

    CPC分类号： A61K31/34 ,  C12Q1/527 ,  G01N33/6893 ,  G01N2800/044

    摘要： A method for the discovery of compounds suitable for the treatment and/or prophylaxis of obesity, in which the ability of the test compounds to inhibit de novo lipogenesis in mammals and/or man is determined. The use of compounds which are capable of inhibiting de novo lipogenesis in mammals, and which are substantially free of effects directed towards the CNS, for the preparation of pharmaceutical compositions for the treatment and/or prophylaxis of obesity, as well as for the treatment and/or inhibition of obesity, are also described.

    摘要翻译： 发现适用于治疗和/或预防肥胖症的化合物的方法，其中测定化合物在哺乳动物和/或人中抑制新生脂肪生成的能力。 使用能够在哺乳动物中抑制从头脂肪生成并且基本上没有针对CNS的作用的化合物用于制备用于治疗和/或预防肥胖症的药物组合物，以及用于治疗和/ /或抑制肥胖。

    2,6-Dioxa-bicyclo-[2,2,2]-octane-7-yl-acetaldehydes
    28.
    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。

    Process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decanes
    29.
    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, processes for their preparation and pharmaceutical compositions thereof
    30.
    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：