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    1,2-Dithiolane derivatives
    5.
    发明授权
    1,2-Dithiolane derivatives 失效
    1,2-二硫戊环衍生物

    公开(公告)号：US6127394A

    公开(公告)日：2000-10-03

    申请号：US264370

    申请日：1999-03-08

    申请人： Harrihar A. Pershadsingh ,  Mitchell A. Avery

    发明人： Harrihar A. Pershadsingh ,  Mitchell A. Avery

    IPC分类号： C07C323/12 ,  C07C323/62 ,  C07D277/34 ,  C07D417/12 ,  A61K31/425

    CPC分类号： C07D417/12 ,  C07C323/12 ,  C07C323/62 ,  C07D277/34

    摘要： This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of certain cardiovascular certain diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (malignant) and non-malignant proliferative diseases, certain neuro-psychiatric disorders, certain viral diseases, and diseases associated with these viral infections as discussed herein.

    摘要翻译： 本发明提供了新的噻唑啉二酮衍生物和新的芳基乙酸衍生物。 这些化合物可用于治疗某些心血管疾病，某些内分泌疾病，某些炎性疾病，某些肿瘤（恶性）和非恶性增殖性疾病，某些神经精神障碍，某些病毒性疾病以及与这些病毒感染有关的疾病 如本文所讨论的。

    Process for preparing polyoxa tetracyclic compounds
    6.
    发明授权
    Process for preparing polyoxa tetracyclic compounds 失效
    制备多氧四环化合物的方法

    公开(公告)号：US4963683A

    公开(公告)日：1990-10-16

    申请号：US312376

    申请日：1989-02-15

    申请人： Mitchell A. Avery ,  Clive Jennings-White

    发明人： Mitchell A. Avery ,  Clive Jennings-White

    IPC分类号： C07D491/18 ,  C07D493/04 ,  C07D493/18 ,  C07D495/18

    CPC分类号： C07D493/04

    摘要： A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring matrial. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.

    摘要翻译： 一种合成多氧四环的方法，其涉及单环结构乙烯基硅烷的臭氧分解，从而直接形成所需的多环材料。 聚氧四环化合物具有下式：乙烯基硅烷具有以下结构：乙烯基硅烷是相应的初级臭氧化物和二氧杂环丁烷中间体的新化合物。 在优选的实施方案中，本发明提供抗疟青蒿素的全合成。

    Polyoxa tetracyclic compounds
    7.
    发明授权
    Polyoxa tetracyclic compounds 失效
    聚氧四环化合物

    公开(公告)号：US5225554A

    公开(公告)日：1993-07-06

    申请号：US554333

    申请日：1990-07-18

    申请人： Mitchell A. Avery ,  Clive Jennings-White

    发明人： Mitchell A. Avery ,  Clive Jennings-White

    IPC分类号： C07D491/18 ,  C07D493/04 ,  C07D493/18 ,  C07D495/18

    CPC分类号： C07D493/04

    摘要： A process for synthesizing polyoxa tetracyclics which involves the ozonolysis of a single-ring-structure vinyl silane with resulting direct formation of the desired multiple ring material. The polyoxa tetracyclic compounds have the formula ##STR1## The vinyl silanes have the structure ##STR2## The vinyl silanes are new chemical compounds as are corresponding primary ozonide and dioxetane intermediates. In a preferred embodiment, this invention provides a total synthesis of the antimalarial artemisinin.

    摘要翻译： 一种合成多氧四环的方法，其涉及单环结构乙烯基硅烷的臭氧分解，从而直接形成所需的多环材料。 聚氧四环化合物具有下式：乙烯基硅烷具有以下结构：乙烯基硅烷是相应的初级臭氧化物和二氧杂环丁烷中间体的新化合物。 在优选的实施方案中，本发明提供抗疟青蒿素的全合成。

    Process for preparing analogs of artemisinin
    9.
    发明授权
    Process for preparing analogs of artemisinin 失效
    制备青蒿素类似物的方法

    公开(公告)号：US5180840A

    公开(公告)日：1993-01-19

    申请号：US657095

    申请日：1991-02-19

    申请人： Mitchell A. Avery ,  Wesley K. M. Chong

    发明人： Mitchell A. Avery ,  Wesley K. M. Chong

    IPC分类号： C07D491/18 ,  C07D493/04 ,  C07D493/18 ,  C07D495/18

    CPC分类号： C07D493/04

    摘要： A process for synthesizing oxygen-containing polyoxatetracycle compounds and in particular analogs of the antimalarial agent known as qinghaosu or artemisinin is disclosed. The process employs as a reactant an olefinically unsaturated bicyclic bridging ketone having nonenolizable bridgehead moieties for both of its alpha positions. This ketone is converted to a vinylsilane that is subjected to ozonolytic cleavage of its olefinic bond to yield a member of a family of unique carboxyl/carbonyl-substituted vinylsilanes which may in turn optionally be subjected to a wide range of reactions prior to a final ozonolysis/acidification step which closes the oxygen-containing ring structure. The various intermediates are claimed as aspects of this invention as are novel tetracycles and their use as antimalarials.

    摘要翻译： 公开了一种合成含氧多氧四环化合物，特别是称为青蒿素或青蒿素的抗疟剂类似物的方法。 该方法采用作为反应物的烯属不饱和双环桥连酮，其具有两个α位置的不可烯化桥头馏分。 将该酮转化为乙烯基硅烷，其进行其烯属键的臭氧分解裂解，得到独特的羧基/羰基取代的乙烯基硅烷族的成员，其可任选在最终臭氧分解之前进行宽范围的反应 关闭含氧环结构的酸化步骤。 作为本发明的方面，各种中间体被称为新四环和它们作为抗疟药的用途。

    Antimalarial analogs of artemisinin
    10.
    发明授权
    Antimalarial analogs of artemisinin 失效
    青蒿素的抗疟药类似物

    公开(公告)号：US5019590A

    公开(公告)日：1991-05-28

    申请号：US414730

    申请日：1989-09-27

    申请人： Mitchell A. Avery ,  Wesley K. M. Chong

    发明人： Mitchell A. Avery ,  Wesley K. M. Chong

    IPC分类号： C07D491/18 ,  C07D493/04 ,  C07D493/18 ,  C07D495/18

    CPC分类号： C07D493/04

    摘要： A process for synthesizing oxygen-containing polyoxatetracycle compounds and in particular analogs of the antimalarial agent known as qinghaosu or artemisinin is disclosed. The process employs as a reactant an olefinically unsaturated bicyclic bridging ketone having nonenolizable bridgehead moieties for both of its alpha positions. This ketone is converted to a vinylsilane that is subjected to ozonolytic cleavage of its olefinic bond to yield a member of a family of unique carboxyl/carbonyl-substituted vinylsilanes which may in turn optionally be subjected to a wide range of reactions prior to a final ozonolysis/acidification step which closes the oxygen-containing ring structure. The various intermediates are claimed as aspects of this invention as are novel tetracycles and their use as antimalarials.

    摘要翻译： 公开了一种合成含氧多氧四环化合物，特别是称为青蒿素或青蒿素的抗疟剂类似物的方法。 该方法采用作为反应物的烯属不饱和双环桥连酮，其具有两个α位置的不可烯化桥头馏分。 将该酮转化为乙烯基硅烷，其进行其烯属键的臭氧分解裂解，得到独特的羧基/羰基取代的乙烯基硅烷族的成员，其可任选在最终臭氧分解之前进行宽范围的反应 关闭含氧环结构的酸化步骤。 作为本发明的方面，各种中间体被称为新四环和它们作为抗疟药的用途。