利索-全球专利检索

  1. Login
  2. Sign Up

Search Results

256 records (took 0.026 seconds)

    N,N-bis (quinolin-4-yl)-diamine derivatives, their preparation and their use as antimalarials
    77.
    发明授权
    N,N-bis (quinolin-4-yl)-diamine derivatives, their preparation and their use as antimalarials 失效
    N，N-双（喹啉-4-基） - 二胺衍生物，它们的制备及其作为抗疟药物的用途

    公开(公告)号：US5736557A

    公开(公告)日：1998-04-07

    申请号：US765751

    申请日：1996-12-16

    Applicant: Werner Hofheinz ,  Werner Leupin

    Inventor： Werner Hofheinz ,  Werner Leupin

    IPC: C07D215/42 ,  A61K31/47 ,  A61P33/02 ,  C07D215/44 ,  C07D215/46

    CPC classification number: C07D215/46 ,  C07D215/44

    Abstract: Disclosed are N,N'-bis(quinolin-4-yl)diamine derivatives of general formula I wherein R.sup.1 signifies halogen or trifluoromethyl, R.sup.2 signifies hydrogen or halogen, A signifies cyclohexane-1,3-diyl, 2-methyl-cyclohexane-1,3-diyl, cyclohexane-1,4-diyl, dicyclohexylmethane-4,4'-diyl, cyclopentane-1,3-diyl, phenylene-1,4, phenylene-1,3 and phenylene-1,2; n is 1 or 2; m is 1 or 2, as well as their pharmaceutically acceptable salts. These products are useful as agents for preventing malaria and for treating it, especially where the pathogens are resistant to chloroquine. ##STR1##

    Abstract translation: PCT No.PCT / EP95 / 02123 Sec。 371日期1996年12月16日第 102（e）日期1996年12月16日PCT提交1995年6月3日PCT公布。 公开号WO95 / 35287 日期1995年12月28日公开是通式I的N，N'-双（喹啉-4-基）二胺衍生物，其中R1表示卤素或三氟甲基，R2表示氢或卤素，A表示环己烷-1,3-二基，2 环己烷-1,3-二基，环己烷-1,4-二基，二环己基甲烷-4,4'-二基，环戊烷-1,3-二基，亚苯基-1,4-亚苯基-1,3-亚苯基 - 1,2; n为1或2; m为1或2，以及其药学上可接受的盐。 这些产品可用作预防疟疾和治疗疟疾的药剂，特别是在病原体耐氯喹的情况下。 我

    Amine derivatives
    79.
    发明授权
    Amine derivatives 失效
    胺衍生物

    公开(公告)号：US5654298A

    公开(公告)日：1997-08-05

    申请号：US685944

    申请日：1991-04-16

    Applicant: Stuart Dennett Mills ,  Rodney Brian Hargreaves ,  Bernard Joseph McLoughlin

    Inventor： Stuart Dennett Mills ,  Rodney Brian Hargreaves ,  Bernard Joseph McLoughlin

    IPC: A61K31/44 ,  A61K31/4409 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4425 ,  A61K31/4439 ,  A61P9/00 ,  A61P9/06 ,  C07D213/74 ,  C07D215/44 ,  C07D401/04 ,  C07D471/04 ,  A01N43/62 ,  A01N43/40 ,  C07D211/68 ,  C07D211/92

    CPC classification number: C07D213/74 ,  C07D215/44 ,  C07D401/04 ,  C07D471/04

    Abstract: This invention concerns novel aminopyridinium compounds of the formula I wherein R.sup.1, R.sup.2, R.sup.3, R.sup.5 and R.sup.6 are selected from the following combinations: ##STR1## (a) one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino, or is alkyl, alkenyl, alkoxyalkyl, alkoxy, alkylthio, phenyl, phenylalkyl, cycloalkyl or cycloalkylalkyl; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl or one of the above defined basic groups;R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl, cycloalkylalkyl; and R.sup.3 and R.sup.5 are independently hydrogen, alkyl or alkenyl;(b) R.sup.2 is a basic group as defined above, R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyridine ring, complete a benzene ring; has any of the meanings defined in(a) above; and R.sup.3 is hydrogen, alkyl or alkenyl; and(c) R2 has any of the meanings defined above and R.sup.6 is a group of the formula --NR.sup.7.A-- in which A together with R.sup.1 forms an ethylene, trimethylene or tetramethylene link and R.sup.7 is hydrogen or alkyl; andR.sup.3 and R.sup.5 have, independently, any of the meanings defined in (a) above; and wherein R.sup.4 is hydrogen, cycloalkylalkyl, alkyl, alkenyl, alkynyl or phenylalkyl; and Q is phenyl; or the group Q.N(R.sup.4)-- together constitutes an azaheterocyclic moietyo; Y is a physiologically acceptable anion; and any one or more of said phenyl or benzene moieties may optionally be unsubstituted or bear one or more selected substituents.The invention also includes certain closely related anhydro-base derivatives which, like the formula I compounds, possess beneficial effects on the cardiovascular system. Also included are pharmaceutical compositions and processes for the manufacture of the various novel compounds.

    Abstract translation: 本发明涉及式I的新型氨基吡啶鎓化合物，其中R 1，R 2，R 3，R 5和R 6选自以下组合：选自氨基，烷基氨基，至多8个碳原子的二烷基氨基，吡咯烷子基，哌啶子基和吗啉代，或烷基 ，烯基，烷氧基烷基，烷氧基，烷硫基，苯基，苯基烷基，环烷基或环烷基烷基; R2和R6中的另一个是氢，烷基或上述定义的基团之一; R1是烷基，烯基，环烷基，苯基，苯基烷基，环烷基烷基; 并且R 3和R 5独立地是氢，烷基或链烯基; （b）R2是如上定义的碱性基团，R5和R6一起形成亚烷基，或与吡啶环的上述碳原子一起形成苯环; 具有上述（a）中定义的任何含义; 并且R 3是氢，烷基或烯基; 和（c）R 2具有上述定义的任何含义，R 6是式-NR 7 A的基团，其中A与R 1一起形成乙烯，三亚甲基或四亚甲基，R 7为氢或烷基; 和R3和R5独立地具有上述（a）中定义的任何含义; 并且其中R4是氢，环烷基烷基，烷基，烯基，炔基或苯基烷基; Q为苯基; 或基团Q.N（R4） - 一起构成氮杂环基; Y是生理上可接受的阴离子; 并且所述苯基或苯部分中的任何一个或多个可以任选地是未取代的或承载一个或多个选定的取代基。 本发明还包括某些密切相关的脱氢基衍生物，其如式I化合物对心血管系统具有有益作用。 还包括用于制备各种新型化合物的药物组合物和方法。

Patent Agency Ranking