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    Process for preparing N-acyl amino acid salts
    35.
    发明授权
    Process for preparing N-acyl amino acid salts 有权
    制备N-酰基氨基酸盐的方法

    公开(公告)号：US09156777B2

    公开(公告)日：2015-10-13

    申请号：US14411971

    申请日：2013-06-27

    申请人： Stepan Company

    发明人： Bing Wang ,  Gregory P Dado

    IPC分类号： C07C233/91 ,  C07C231/02 ,  C07C231/10

    CPC分类号： C07C233/91 ,  C07C231/02 ,  C07C231/10 ,  C07C233/47

    摘要： Improved processes for making an N-acyl amino acid salt from a fatty alkyl ester or a polyol ester are disclosed. Each process uses a polyol selected from glycerin or propylene glycol in an amount effective to keep the reaction mixture fluid until conversion to the N-acyl amino acid salt reaches the desired level of completion. In one process, a fatty alkyl ester reacts with an amino acid salt in the presence of glycerin or propylene glycol to produce an N-acyl amino acid salt. In another process, a polyol ester reacts with the amino acid salt in the presence of added glycerin or propylene glycol to produce the N-acyl amino acid salt. We surprisingly found that an effective amount of glycerin or propylene glycol minimizes or eliminates reaction mixture solidification or foaming, reduces color, and minimizes the level of di- and tripeptide by-products. In a related process, water is added when conversion of the amino acid salt to the N-acyl amino acid salt is in the range of 50 to 90 mole %. Water addition improves processability, advances conversion without producing excessive soap, and helps to ensure that the N-acyl amino acid salt will have low color and a small proportion of by-products.

    摘要翻译： 公开了从脂肪烷基酯或多元醇酯制备N-酰基氨基酸盐的改进方法。 每个方法使用选自甘油或丙二醇的多元醇，其量可以有效地保持反应混合物流体，直到转化成N-酰基氨基酸盐达到所需的完成水平。 在一个过程中，脂肪烷基酯在甘油或丙二醇的存在下与氨基酸盐反应以产生N-酰基氨基酸盐。 在另一方法中，多元醇酯在加入的甘油或丙二醇的存在下与氨基酸盐反应以产生N-酰基氨基酸盐。 我们惊奇地发现，有效量的甘油或丙二醇使反应混合物固化或发泡最小化或消除，减少颜色，并使二肽和三肽副产物的水平最小化。 在相关方法中，当氨基酸盐转化为N-酰基氨基酸盐时，加入水是在50至90摩尔％的范围内。 添加水可改善加工性能，不会产生过量的肥皂进行转化，有助于确保N-酰基氨基酸盐具有低颜色和少量的副产物。

    Cell signaling inhibitors
    39.
    发明授权
    Cell signaling inhibitors 失效
    细胞信号传导抑制剂

    公开(公告)号：US5470878A

    公开(公告)日：1995-11-28

    申请号：US164081

    申请日：1993-12-08

    申请人： John Michnick ,  Gail E. Underiner ,  J. Peter Klein ,  Glenn C. Rice

    发明人： John Michnick ,  Gail E. Underiner ,  J. Peter Klein ,  Glenn C. Rice

    IPC分类号： A61K31/404 ,  A61K31/45 ,  A61K31/47 ,  A61K31/513 ,  A61K31/519 ,  A61K31/522 ,  C07C215/08 ,  C07C215/56 ,  C07C217/62 ,  C07C229/22 ,  C07C233/36 ,  C07C233/78 ,  C07C233/91 ,  C07D207/40 ,  C07D207/404 ,  C07D209/48 ,  C07D211/76 ,  C07D211/88 ,  C07D217/24 ,  C07D239/54 ,  C07D239/90 ,  C07D239/96 ,  C07D295/13 ,  C07D473/10 ,  A61K31/20 ,  C07C233/00

    CPC分类号： C07D207/404 ,  A61K31/404 ,  A61K31/45 ,  A61K31/47 ,  A61K31/513 ,  A61K31/519 ,  A61K31/522 ,  C07C215/08 ,  C07C215/56 ,  C07C217/62 ,  C07C229/22 ,  C07C233/36 ,  C07C233/78 ,  C07C233/91 ,  C07D209/48 ,  C07D211/76 ,  C07D211/88 ,  C07D217/24 ,  C07D239/54 ,  C07D239/90 ,  C07D239/96 ,  C07D295/13 ,  C07D473/10

    摘要： Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.3 is a hydrogen or C.sub.1-3. Or, therapeutic compounds may also have the formula: ##STR2## R.sub.4 is a hydrogen, a straight or branched chain alkane or alkene of up to eight carbon atoms in length, --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy, or a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms. r and s are independently integers from one to four, the sum (r+s) not being greater than five. t is an integer from one to fourteen and one or more carbon atoms of (CH.sub.2).sub.s or (CH.sub.2).sub.t may be substituted by a keto or hydroxy group.

    摘要翻译： 治疗化合物具有下式：（X）j-（非环核心部分），j为1至3的整数，核心部分为非环状，X为外消旋混合物，R或S对映异构体，溶剂合物，水合物 或其盐：C是手性碳原子，n是1-4的整数（优选1至3），（CH 2）n的一个或多个碳原子可被酮或羟基取代 组，m是从1到14的整数。 独立地，R 1和R 2可以是氢，长或多至十二个碳原子的直链或支链烷烃或烯烃，或 - （CH 2）w R 5，w为2至14的整数，R 5为单 - ，二 - 或三取代或未取代的芳基，R 5上的取代基是羟基，氯，氟，溴或C 1-6烷氧基。 或者共同地，R 1和R 2形成具有4至8个碳原子的取代或未取代的饱和或不饱和杂环基，N是杂原子。 R3是氢或C1-3。 或者，治疗性化合物也可以具有下式：R 4是氢，长或多至八个碳原子的直链或支链烷烃或烯烃， - （CH 2）w R 5，w是2至14的整数， R5是一个，二或三取代或未取代的芳基，R 5上的取代基是羟基，氯，氟，溴或C 1-6烷氧基，或取代或未取代的饱和或不饱和杂环基， 八个碳原子。 r和s独立为从1到4的整数，并且（r + s）不大于5。 t是1至14的整数，（CH 2）s或（CH 2）t的一个或多个碳原子可以被酮基或羟基取代。