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    • 17. 发明授权
    • Novel product and process
    • 新产品和工艺
    • US4703099A
    • 1987-10-27
    • US909543
    • 1986-09-22
    • Dale F. Regelman
    • Dale F. Regelman
    • C07D295/02C08G18/02C08G18/16C08G18/79C08G18/08
    • C07D295/02C07C255/00C07C265/00C07C265/12C08G18/022C08G18/168C08G18/791C08G2105/02Y10S521/902
    • Disclosed are novel compositions capable of catalytically trimerizing organic isocyanates said compositions comprising solutions of the reaction products obtained by reacting in an inert solvent in substantially equimolar proportions electron-rich ketene-aminals with electron-poor olefins having the respective formulae (I) and (II) ##STR1## The variously substituted electron-rich ketene-aminals (I), as the name implies, have high electron density associated with the double bond because of the two tertiary amine groups while the electron-poor olefins (II) have the opposite situation due to the presence of electron withdrawing substituents R.sub.9 and R.sub.10.Also disclosed is an improved process for trimerizing organic isocyanates using the above catalyst compositions including the preparation of polyisocyanurate polymers and isocyanurate-modified polyisocyanates.
    • 公开了能够催化三聚有机异氰酸酯的新型组合物,所述组合物包含通过在惰性溶剂中基本上等摩尔比例的富含电子的乙烯酮 - 胺与具有各自式(I)和(II)的电子不足烯烃反应而获得的反应产物的溶液 (I)如下所述,不同取代的富电子酮乙烯酮(I)由于两个叔胺基团而具有与双键相关的高电子密度,而电子 由于吸电子取代基R9和R10的存在,α-烯烃(II)具有相反的情况。 还公开了使用上述催化剂组合物三聚有机异氰酸酯的改进方法,包括制备聚异氰脲酸酯聚合物和异氰脲酸酯改性的多异氰酸酯。
    • 19. 发明授权
    • Analgesic basic naphthalene derivatives
    • 镇痛碱性萘衍生物
    • US4062955A
    • 1977-12-13
    • US625863
    • 1975-10-28
    • Derek BurnRichard J. Coles
    • Derek BurnRichard J. Coles
    • C07D295/12A61K31/13A61K31/135A61K31/165A61K31/215C07C17/12C07C17/14C07C63/72C07C65/24C07C67/00C07C209/00C07C209/08C07C209/16C07C209/50C07C209/62C07C211/30C07C211/44C07C213/00C07C215/14C07C215/74C07C217/08C07C217/78C07C219/04C07C219/34C07D211/14C07D211/70C07D265/30C07D295/02C07D295/073C07D295/096C07D295/135
    • C07D295/02A61K31/165C07C17/12C07C17/14C07C63/72C07C65/24C07D211/14C07D211/70C07D265/30C07D295/073C07D295/096C07D295/135
    • Compounds of the general formula: ##STR1## wherein the groups CHR.sup.1 NR.sup.2 R.sup.3 and CHR.sup.4 NR.sup.5 R.sup.6 may be the same or different and where the group CHR.sup.4 NR.sup.5 R.sup.6 is in either the 1 or the 3 position and R.sup.1 and R.sup.4 independently represent a hydrogen atom or an aryl group;R.sup.2, r.sup.3, r.sup.5 and R.sup.6 which may be the same or different are each a hydrogen atom or an alkyl group or an aryl group both of which may in turn be substituted by one or more hydroxy, alkoxy, acyloxy, dialkylamino or aryl groups or the groups --NR.sup.2 R.sup.3 and/or NR.sup.5 R.sup.6 represent a heterocyclic ring containing one or more hetero atoms and which ring may optionally be substituted by an alkyl, aryl or aralkyl group and in which either aromatic ring of the naphthalene nucleus may be further substituted; with the proviso that when R.sup.1, R.sup.4, R.sup.2 and R.sup.5 are hydrogen, then R.sup.3 and R.sup.6 cannot both be benzyl, when the second substituent is in the 1 position; and when R.sup.1 and R.sup.4 are hydrogen, then R.sup.2, R.sup.3, R.sup.5 and R.sup.6 cannot all be methyl when the second substituent is in the 1 position; and when R.sup.1 and R.sup.4 are hydrogen, then R.sup.2 and R.sup.3 and R.sup.5 and R.sup.6 together with the nitrogen atom cannot both be piperidino when the second substituent is in the 3 position and the naphthalene nucleus is further substituted by hydroxy in the 1 and 4 positions; and pharmaceutically acceptable salts of such compounds; and hydrates of such compounds and such salts. The compounds have activity on the central nervous system in particular as analgesics.
    • 通式:其中CHR1NR2R3和CHR4NR5R6基团可以相同或不同,并且其中CHR4NR5R6基团在1或3位且R1和R4独立地表示氢原子或芳基的化合物 组; R 2,R 3,R 5和R 6可以相同或不同,分别为氢原子或烷基或芳基,二者可以依次被一个或多个羟基,烷氧基,酰氧基,二烷基氨基或芳基取代,或 基团-NR2R3和/或NR5R6表示含有一个或多个杂原子的杂环,并且该环可以任选地被烷基,芳基或芳烷基取代,并且其中萘核的任一个芳环可以进一步被取代; 条件是当R 1,R 4,R 2和R 5是氢时,则当第二取代基在1位时,R 3和R 6不能都是苄基; 当R 1和R 4为氢时,当第二取代基在1位时,R 2,R 3,R 5和R 6不能全部为甲基; 当R1和R4为氢时,当第二个取代基位于3位,R2和R3与R5和R6与氮原子一起不能同时为哌啶子基,而萘环在1和4位进一步被羟基取代; 和这些化合物的药学上可接受的盐; 和这些化合物的水合物和这些盐。 该化合物对中枢神经系统具有活性,特别是作为镇痛药。