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    Spiro and dispiro 1,2,4-trioxolane antimalarials
    4.
    发明授权
    Spiro and dispiro 1,2,4-trioxolane antimalarials 有权
    螺和脱甲基-1,2,4-三恶烷抗疟药

    公开(公告)号：US06486199B1

    公开(公告)日：2002-11-26

    申请号：US09886666

    申请日：2001-06-21

    申请人： Jonathan L. Vennerstrom ,  Yuxiang Dong ,  Jacques Chollet ,  Hugues Matile

    发明人： Jonathan L. Vennerstrom ,  Yuxiang Dong ,  Jacques Chollet ,  Hugues Matile

    IPC分类号： A61K31335

    CPC分类号： C07D405/12 ,  A61K31/335 ,  A61K31/357 ,  C07D323/02 ,  C07D405/14 ,  C07D491/10 ,  C07D493/10 ,  C07D495/10 ,  Y02A50/411 ,  Y02A50/423 ,  A61K2300/00

    摘要： A means and method for treating malaria using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl or spiropiperidyl ring on the other side of the trioxolane group, whereby the spirocyclohexyl ring is preferably functionalized or substituted at the 4-position or a spiropiperidyl ring that is functionalized or substituted at the nitrogen atom. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites.

    摘要翻译： 描述了使用螺或二脱氧-1,2,4-三恶烷处理疟疾的方法和方法。 优选的1,2,4-三氧杂环戊烷包括在三氧杂环戊烷基一侧的双金刚烷基，三氧杂环戊烷基的另一侧上的螺环己基或螺哌啶环，其中螺环己基环优选在4位官能化或取代 或在氮原子上被官能化或取代的螺哌啶基环。 与青蒿素半合成衍生物相比，本发明的化合物在结构上简单，易于合成，无毒，对抗疟疾寄生虫有效。

    Bisquinolines and processes for their production and use to treat malaria
    9.
    发明授权
    Bisquinolines and processes for their production and use to treat malaria 失效
    双喹啉及其生产和使用过程来治疗疟疾

    公开(公告)号：US5510356A

    公开(公告)日：1996-04-23

    申请号：US770638

    申请日：1991-10-03

    申请人： Jonathan L. Vennerstrom

    发明人： Jonathan L. Vennerstrom

    IPC分类号： C07D215/46 ,  A61K31/47 ,  C07D215/38

    CPC分类号： C07D215/46 ,  Y10S514/895

    摘要： The present invention relates to new bisquinolines useful in the treatment of malaria and to processes for the production thereof. The invention also relates to methods for the treatment of malaria and, in particular, to the treatment of chloroquine-resistant strains of malaria. The compounds of the invention have the following formula: ##STR1## wherein R is a bivalent radical derived from an acyclic or cyclic hydrocarbon by removal of one hydrogen atom from each of two different carbon atoms. R' is hydrogen or lower alkyl (generally containing between about 1 and about 4 carbon atoms). X is hydrogen (--H), fluoro (--F), chloro (--Cl), bromo (--Br), trifluoromethyl (--CF.sub.3), cyano (--CN), or methylsulfoxide (--SOCH.sub.3). In its acyclic form, R generally contains at least two, and no more than about 12, carbon atoms and, preferably, is an unsubstituted straight or branched alkane. In its cyclic form, R contains at least three and, generally, no more than about eight carbon atoms and, preferably, is an unsubstituted cycloalkane. In a preferred embodiment, this invention relates to N,N-bis(7-chloroquinolin-4-yl)alkane diamines which are active against chloroquine-resistant malaria.The bisquinolines of this invention are useful agents against chloroquine-resistant malaria. .+-.-Trans-N.sup.1,N.sup.2 -Bis(7-chloro-quinolin-4-yl)cyclohexane-1,2-diamine is highly preferred for treatment of chloroquine-resistant malaria. This compound is one of the most potent antimalarials discovered to date and is clearly unique in its in vivo activity -80% and 100% cure rates being achieved at doses of 160 and 320 mg/kg, respectively.

    摘要翻译： 本发明涉及可用于治疗疟疾的新型双喹啉及其生产方法。 本发明还涉及治疗疟疾的方法，特别是治疗氯喹抗性疟疾菌株。 本发明的化合物具有下式：其中R是通过从两个不同的碳原子中的每一个除去一个氢原子而衍生自无环或环状烃的二价基团。 R'是氢或低级烷基（通常含有约1至约4个碳原子）。 X是氢（-H），氟（-F），氯（-Cl），溴（-Br），三氟甲基（-CF 3），氰基（-CN）或甲基亚砜（-SOCH 3）。 在其无环形式中，R通常含有至少两个且不超过约12个碳原子，并且优选为未取代的直链或支链烷烃。 在其环状中，R含有至少三个，通常不超过约八个碳原子，优选为未取代的环烷烃。 在优选的实施方案中，本发明涉及对氯喹抗性疟疾具有活性的N，N-双（7-氯喹啉-4-基）烷烃二胺。 本发明的双喹啉是抗氯喹抗性疟疾的有用药剂。 + / - 反式-N1，N2-双（7-氯 - 喹啉-4-基）环己烷-1,2-二胺是治疗氯喹抗性疟疾的方法。 该化合物是迄今发现的最有效的抗疟药之一，其体内活性明显独特，分别在160和320mg / kg剂量下达到80％和100％的治愈率。