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公开(公告)号:US5723467A
公开(公告)日:1998-03-03
申请号:US773737
申请日:1996-12-24
申请人: Jean Louis Mesens , Jozef Peeters
发明人: Jean Louis Mesens , Jozef Peeters
IPC分类号: A61K31/505 , A61K31/519 , A61P25/00 , A61P25/18 , C07C65/11 , C07D221/00 , C07D239/00 , C07D471/04
CPC分类号: C07C65/11 , C07D471/04
摘要: A method of treating psychotic disorders by administering an effective amount of a permeate acid addition salt of risperidone having the formula: ##STR1##
摘要翻译: 一种通过施用有效量的利培酮的渗透酸加成盐来治疗精神病性疾病的方法,其具有下式:(I)< IMAGE>
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公开(公告)号:US5998413A
公开(公告)日:1999-12-07
申请号:US676531
申请日:1996-07-09
申请人: Jan Heeres , Jean Louis Mesens , Jozef Peeters
发明人: Jan Heeres , Jean Louis Mesens , Jozef Peeters
IPC分类号: C07D405/14 , A61K31/496 , A61P31/10 , C07D521/00 , C08B37/16 , A61K31/495 , A61K31/50 , C07D403/14
CPC分类号: C07D249/08 , B82Y15/00 , C07D231/12 , C07D233/56
摘要: Anti-infective compositions for the treatment of a human in need of therapy for a systemic or topical fungal infection which comprise a pharmaceutically acceptable carrier and a therapeutically effective amount of (2R,4S) itraconazole or a pharmaceutically acceptable salt thereof, substantially free of its (2S,4R) stereoisomer.
摘要翻译: 用于治疗需要治疗全身或局部真菌感染的人的抗感染组合物,其包含药学上可接受的载体和治疗有效量的(2R,4S)伊曲康唑或其药学上可接受的盐,基本上不含 (2S,4R)立体异构体。
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公开(公告)号:US5674871A
公开(公告)日:1997-10-07
申请号:US586700
申请日:1996-01-26
IPC分类号: A61N1/30 , A61K9/00 , A61K9/70 , A61K31/35 , A61K31/352 , A61K31/353 , A61K31/505 , A61K31/506 , A61P25/04 , A61P25/06 , A61K31/40 , A61K31/415 , A61K31/445
CPC分类号: A61K9/0009 , A61K31/35 , A61K31/505
摘要: The present invention relates to the iontophoretic delivery to a patient, more in particular to a migraine patient, of a compound of formula (I) as shown hereinunder. The invention also relates to a device for the iontophoretic delivery of a compound of formula (I), as well as to a composition containing a compound of formula (I), which can be applied in a device for iontophoretic delivery. Said compounds are benzopyranalkylaminoalkyl substituted guanidines having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl, C.sub.3-6 alkenyl or C.sub.3-6 alkynyl; R.sup.3 is hydrogen or C.sub.1-6 alkyl; or R.sup.2 and R.sup.3 taken together form a bivalent radical of formula --(CH.sub.2).sub.m - wherein m is 4 or 5; or R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH-- or of formula --(CH.sub.2).sub.n -, wherein n is 2, 3 or 4; or R.sup.3 may represent a bond when R.sup.1 and R.sup.2 taken together form a bivalent radical of formula --CH.dbd.CH--CH.dbd.; R.sup.4 and R.sup.5 each independently are hydrogen or C.sub.1-6 alkyl; Alk.sup.1 is a bivalent C.sub.1-3 alkanediyl radical; Alk.sup.2 is a bivalent C.sub.2-15 alkanediyl radical; and R.sup.6 and R.sup.7 each independently are hydrogen, halo, C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, hydroxy, C.sub.1-6 alkyloxy or cyano.
摘要翻译: PCT No.PCT / EP94 / 02764 Sec。 371日期1996年1月26日 102(e)日期1996年1月26日PCT 1994年8月19日PCT PCT。 公开号WO95 / 05815 日期1995年3月2日本发明涉及如下所示的式(I)化合物对患者,特别是偏头痛患者的离子电渗疗法输送。 本发明还涉及用于离子电渗疗法递送式(I)化合物的装置,以及含有式(I)化合物的组合物,其可以应用于用于离子电渗疗法递送的装置中。 所述化合物是具有下式的苯并吡喃烷基氨基烷基取代的胍(I)其药学上可接受的酸加成盐及其立体化学异构形式,其中R 1是氢或C 1-6烷基; R2是氢,C1-6烷基,C3-6烯基或C3-6炔基; R3是氢或C1-6烷基; 或R 2和R 3一起形成式 - (CH 2)m-的二价基团,其中m为4或5; 或R 1和R 2一起形成式-CH = CH-或式 - (CH 2)n - 的二价基团,其中n为2,3或4; 或者当R 1和R 2一起形成式-CH = CH-CH =的二价基团时,R 3可以表示键; R 4和R 5各自独立地为氢或C 1-6烷基; Alk1是二价C 1-3烷二基; Alk2是二价C2-15烷二基; R 6和R 7各自独立地为氢,卤素,C 1-6烷基,C 3-6烯基,C 3-6炔基,羟基,C 1-6烷氧基或氰基。
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公开(公告)号:US06346518B1
公开(公告)日:2002-02-12
申请号:US08295885
申请日:1995-01-26
申请人: Jan Heeres , Jean Louis Mesens , Jozef Peeters
发明人: Jan Heeres , Jean Louis Mesens , Jozef Peeters
IPC分类号: A61K31495
CPC分类号: A61K31/496 , A61K31/724 , Y10S514/965
摘要: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.
摘要翻译: 本发明涉及伊曲康唑(X = Cl)和沙美康唑(X = F)的立体异构形式,其可以由下式表示:其药学上可接受的酸加成盐形式,制备所述立体异构形式的方法及其复合物 与环糊精衍生物,包含所述复合物的药物组合物和制备所述复合物和药物组合物的方法。
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公开(公告)号:US5707977A
公开(公告)日:1998-01-13
申请号:US666270
申请日:1996-06-20
申请人: Jan Heeres , Leo Jacobus Jozef Backx , Luc Alfons Leo Van der Eycken , Frank Christopher Odds , Jean Louis Mesens
发明人: Jan Heeres , Leo Jacobus Jozef Backx , Luc Alfons Leo Van der Eycken , Frank Christopher Odds , Jean Louis Mesens
IPC分类号: C07D405/14 , A01N43/653 , A01N57/16 , A61K31/34 , A61K31/36 , A61K31/41 , A61K31/415 , A61K31/495 , A61K31/535 , A61K31/675 , A61P31/04 , A61P31/10 , C07D403/12 , C07D407/14 , C07D413/14 , C07D521/00 , C07F9/6558
CPC分类号: C07D249/08 , C07D231/12 , C07D233/56 , C07F9/65586
摘要: A compound of formula (I), ##STR1## an acid or base addition salt thereof or a stereochemically isomeric form thereof, wherein A and B taken together form --N.dbd.CH--, --CH.dbd.N--, --CH.sub.2 --CH.sub.2, CH.dbd.CH--, --C(.dbd.O)--CH.sub.2 --, --CH.sub.2 --C(.dbd.O); D is a radical of formula ##STR2## L is a radical of formula ##STR3## Alk is a C.sub.1-4 alkanediyl radical; R.sup.1 is halo; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.4 is hydrogen, C.sub.1-6 alkyl, phenyl or halophenyl; R.sup.5 is hydrogen or C.sub.1-6 alkyl; R.sup.6 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxycarbonyl, or R.sup.5 and R.sup.6 taken together with the nitrogen atom to which they are attached form a heterocyclic ring. Active intermediates, compositions and methods of preparing compounds, compositions are described.
摘要翻译: PCT No.PCT / EP95 / 00174 Sec。 371日期:1996年6月20日 102(e)1996年6月20日PCT 1995年1月17日PCT PCT。 公开号WO95 / 19983 日期:1995年7月27日一种式(I)化合物,其中A和B一起形成-N = CH-,-CH = N-,-CH 2 -CH 2, CH = CH - , - C(= O)-CH 2 - , - CH 2 -C(= O); (D1)(D1)图像(D1)图像(D1)图像(L2)Alk是C1-4烷二基; R1是卤素; R2是氢或卤素; R3是氢,C1-6烷基,苯基或卤代苯基; R4是氢,C1-6烷基,苯基或卤代苯基; R5是氢或C1-6烷基; R6是氢,C1-6烷基,C1-6烷氧基羰基或R5和R6与它们所连接的氮原子一起形成杂环。 描述了制备化合物的活性中间体,组合物和方法,组合物。
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