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    Serine protease inhibitors
    81.
    发明申请
    Serine protease inhibitors 失效
    丝氨酸蛋白酶抑制剂

    公开(公告)号：US20030055246A1

    公开(公告)日：2003-03-20

    申请号：US10030187

    申请日：2002-02-04

    Inventor： John Walter Liebeschuetz ,  Christopher William Murray ,  Stephen Clinton Young ,  Nicholas Paul Camp ,  Stuart Donald Jones ,  William Alexander Wylie ,  John Joseph Masters ,  Michael Robert Wiley ,  Scott Martin Sheehan ,  David Birenbaum Engel ,  Brian Morgan Watson ,  Peter Robert Guzzo ,  Michael John Mayer

    IPC: C07D201/00 ,  C07D213/00

    CPC classification number: C07D295/185 ,  C07D207/12 ,  C07D207/14 ,  C07D211/26 ,  C07D211/46 ,  C07D213/36 ,  C07D213/56 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D309/34 ,  C07D335/02 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14

    Abstract: The invention relates to serine protease inhibitor compounds of formula (I) where R1 is hydrogen, halo, cyano, nitro or hydroxyl, amino, alkoxy, alkyl, aminoalkyl, hydroxyalkyl, thiol, alkylthio, aminosulphonyl, alkoxyalkyl, alkoxycarbonyl, acyloxymethoxycarbonyl or alkylamino optionally substituted by hydroxy, alkylamino, alkoxy, oxo, aryl, cycloalkyl, amino, halo, cyano, nitro, thiol, alkylthio, alkylsulphonyl, alkylsulphenyl, alkylsulphonamido, alkylaminosulphonyl, haloalkoxy and haloalkyl; R2 is hydrogen, halo, methyl, amino, hydroxy, or oxo; and R is XnullXnullY(R7)nullLnullLp(D)n; wherein each X independently is a C, N, O or S atom or a CO, CR1, C(R1)2 or NR1 group, at least one X being C, CO, CR1 or a C(R1)2 group; Y (the null-atom) is a nitrogen atom or a CR1 group or Y and L taken together form a cyclic group; R7 is a lipophilic group selected from alkyl, alkenyl, mono- or bi-cycloalkyl, aryl, heteroaryl, mono- or bicycloalkylalkyl, mono- or bicycloalkylalkenyl, aralkyl, heteroaryl-alkyl, arylalkenyl, heteroarylalkenyl all optionally substituted by a group R1; L is an organic linker group containing 1 to 5 backbone atoms selected from C, N, O and S, or a branched alkyl or cyclic group; Lp is a lipophilic organic group selected from alkyl, heterocyclic, alkenyl, alkaryl, cycloalkyl, polycycloalkyl, cycloalkenyl, aryl, aralkyl or haloalkyl group or a combination of two or more such groups optionally substituted by one or more of oxa, thia, aza or R1 groups; D is a hydrogen bond donor group; and n is 0, 1 or 2 and salts thereof.

    Abstract translation: 本发明涉及式（I）的丝氨酸蛋白酶抑制剂化合物，其中R1是氢，卤素，氰基，硝基或羟基，氨基，烷氧基，烷基，氨基烷基，羟基烷基，硫醇，烷硫基，氨基磺酰基，烷氧基烷基，烷氧基羰基，酰氧基甲氧基羰基或烷基氨基 被羟基，烷基氨基，烷氧基，氧代，芳基，环烷基，氨基，卤素，氰基，硝基，硫醇，烷硫基，烷基磺酰基，烷基亚磺酰基，烷基磺酰氨基，烷基氨基磺酰基，卤代烷氧基和卤代烷基取代。 R2是氢，卤素，甲基，氨基，羟基或氧代; R为X-X-Y（R7）-L-Lp（D）n; 其中每个X独立地为C，N，O或S原子或CO，CR1，C（R1）2或NR1基团，至少一个X为C，CO，CR1或C（R1）2基团; Y（α原子）是氮原子或CR 1基，Y或L一起形成环状基团; R 7是选自烷基，烯基，单 - 或双 - 环烷基，芳基，杂芳基，单 - 或双环烷基烷基，单或双环烷基烯基，芳烷基，杂芳基 - 烷基，芳基烯基，杂芳基烯基的亲油基团，全部任选被基团R 1取代; L是含有1至5个选自C，N，O和S的骨架原子或支链烷基或环基的有机连接基团; Lp是选自烷基，杂环，烯基，烷芳基，环烷基，多环烷基，环烯基，芳基，芳烷基或卤代烷基中的亲脂性有机基团或两个或更多个这样的基团的组合，其任选被一个或多个氧杂，硫杂，氮杂或 R1组; D是氢键供体基团; 和n为0,1或2及其盐。

    Compositions containing reaction product of a cyclic compound containing both a nitrogen atom and a carbonyl group, an aldehyde or ketone, and an etheramine
    83.
    发明授权
    Compositions containing reaction product of a cyclic compound containing both a nitrogen atom and a carbonyl group, an aldehyde or ketone, and an etheramine 失效
    含有包含氮原子和羰基的环状化合物，醛或酮和醚胺的反应产物的组合物

    公开(公告)号：US5912189A

    公开(公告)日：1999-06-15

    申请号：US76344

    申请日：1998-05-12

    Applicant: Thomas J. Wolak ,  Richard M. Lange

    Inventor： Thomas J. Wolak ,  Richard M. Lange

    IPC: C08G65/333 ,  C10L1/14 ,  C10L1/18 ,  C10L1/22 ,  C10L1/232 ,  C10L1/238 ,  C10L1/2387 ,  C10L10/00 ,  C07D201/00 ,  C07D223/10

    CPC classification number: C10L1/232 ,  C08G65/33327 ,  C10L1/143 ,  C10L1/221 ,  C10L1/238 ,  C10L1/2387 ,  C10L10/04 ,  C10L10/06 ,  C10L1/1985 ,  C10L1/2383

    Abstract: The present invention is directed to a composition containing the reaction product of:(A) a cyclic compound containing a 5, 6, or 7-member ring, the ring containing at least one nitrogen and at least one carbonyl group, at least one carbonyl group being adjacent to at least one said nitrogen;(B) an aldehyde or ketone of 1 to about 15 carbon atoms, or a reactive equivalent thereof; and(C) an etheramine represented by the formulaR.sup.4 (O(CH.sub.2 CH(R)O).sub.n --R.sup.3 --NH.sub.2).sub.y(C-I)wherein in formula (C-I), each n independently is a number from 0 to about 50; each R independently is selected from the group consisting of hydrogen, hydrocarbyl groups of 1 to about 16 carbon atoms, and mixtures thereof; R.sup.3 is selected from the group consisting of hydrocarbylene groups of about 2 to about 18 carbon atoms and groups represented by the formula ##STR1## wherein R.sup.5 and each R.sup.6 are independently hydrocarbylene groups of about 2 to about 10 carbon atoms and p is a number from 1 to about 4; y is 1, 2 or 3; and R.sup.4 is a hydrocarbyl group having a valence of y and containing 1 to about 50 carbon atoms when y is 1, and 1 to about 18 carbon atoms when y is 2 or 3.These compositions are useful as fuel additives for reducing intake valve deposits and advantageously, they do not contribute to an increase in combustion chamber deposits in port fuel injected internal combustion engines. The invention also relates to concentrates and fuel compositions containing the foregoing fuel additive compositions and to a method for reducing intake valve deposits in an internal combustion engine.

    Abstract translation: 本发明涉及含有以下反应产物的组合物：（A）含有5,6或7元环的环状化合物，所述环含有至少一个氮和至少一个羰基，至少一个羰基 与至少一个所述氮相邻; （B）1至约15个碳原子的醛或酮或其活性当量; 和（C）由式R 4（O（CH 2 CH（R）O）n -R 3 -NH 2）y（C-I）表示的醚胺，其中在式（C-I）中，每个n独立地为0至约50的数; 每个R独立地选自氢，1至约16个碳原子的烃基及其混合物; R3选自由约2至约18个碳原子的亚烃基和由下式表示的基团：其中R 5和R 6各自独立地为约2至约10个碳原子的亚烃基，p为1至约 4; y为1,2或3; 且当y为1时，R 4为价数为y且含有1至约50个碳原子的烃基，当y为2或3时，R 4为含有1至约18个碳原子的烃基。这些组合物可用作减少进气阀沉积物的燃料添加剂 并且有利地，它们不会有助于燃料喷射的内燃机的燃料室沉积物的增加。 本发明还涉及含有上述燃料添加剂组合物的浓缩物和燃料组合物以及用于减少内燃机中的进气阀沉积物的方法。

    Process for preparing trialkylsilyldiazomethanes
    84.
    发明授权
    Process for preparing trialkylsilyldiazomethanes 失效
    三烷基甲硅烷基重氮甲烷的制备方法

    公开(公告)号：US4424158A

    公开(公告)日：1984-01-03

    申请号：US401268

    申请日：1982-07-23

    Applicant: Takayuki Shioiri ,  Toyohiko Aoyama ,  Shigehiro Mori

    Inventor： Takayuki Shioiri ,  Toyohiko Aoyama ,  Shigehiro Mori

    IPC: C07F7/10 ,  C07F7/08 ,  C07D201/00

    CPC classification number: C07F7/083

    Abstract: A process for preparing trialkylsilyldiazomethanes in which halomethyltrialkylsilane represented by the general formula R.sup.1 R.sup.2 R.sup.3 SiCH.sub.2 X (wherein R.sup.1, R.sup.2 and R.sup.3 denote an alkyl group of 1 to 4 carbon atoms, and X denotes a halogen group) is reacted with metallic magnesium to give a Grignard reagent, which is then reacted with diphenyl phosphoric acid azide.

    Abstract translation: 制备三烷基甲硅烷基重氮甲烷的方法，其中通式为R 1 R 2 R 3 SiCH 2 X（其中R 1，R 2和R 3表示1至4个碳原子的烷基，X表示卤素基团）表示的卤代甲基三烷基硅烷与金属镁反应，得到格氏试剂， 然后与二苯基磷酸叠氮化物反应。

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