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    Medicinal use of n-phenyl-2-cyano-3-hydroxycrotonamide derivatives
    3.
    发明授权
    Medicinal use of n-phenyl-2-cyano-3-hydroxycrotonamide derivatives 失效
    N-苯基-2-氰基-3-羟基巴豆酰胺衍生物的药用

    公开(公告)号：US5773470A

    公开(公告)日：1998-06-30

    申请号：US902626

    申请日：1997-07-29

    Applicant: Rudolf Schleyerbach ,  Robert Ryder Bartlett ,  Elizabeth Anne Kuo ,  Edward James Little

    Inventor： Rudolf Schleyerbach ,  Robert Ryder Bartlett ,  Elizabeth Anne Kuo ,  Edward James Little

    IPC: C07C255/30 ,  A61K31/16 ,  A61K31/275 ,  A61K31/277 ,  A61P29/00 ,  A61P37/00 ,  A61P37/06 ,  C07C253/00 ,  C07C255/20 ,  C07C255/21 ,  C07C255/23 ,  C07C255/27 ,  C07C323/36

    CPC classification number: A61K31/277 ,  A61K31/275 ,  C07C255/23

    Abstract: N-Phenyl-2-cyano-3-hydroxycrotonamide derivatives and their use as pharmaceuticals having an immunomodulatory property. The use of N-phenyl-2-cyano-3-hydroxycrotonamide derivatives of the formula I ##STR1## in which R.sup.1 is a hydrogen atom or (C.sub.1 -C.sub.4)-alkyl, R.sup.2 is CN, CX.sub.3, WCX.sub.3, W(CH.sub.2).sub.n CX.sub.3, NO.sub.2, (CH.sub.2).sub.n CX.sub.3, or halogen, in which X is halogen, W is an oxygen or sulfur atom and n is an integer from 1 to 3, R.sup.3 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, CN or --CO--R.sup.4, in which R.sup.4 is (C.sub.1 -C.sub.4)-alkyl or (C.sub.3 -C.sub.6)-cycloalkyl, and/or their physiologically tolerable salts, for the treatment of rheumatic diseases, autoimmune diseases, and of rejection reactions of the organ recipient to the transplanted organ, is described.

    Abstract translation: N-苯基-2-氰基-3-羟基巴豆酰胺衍生物及其作为具有免疫调节性的药物的用途。 使用式I C 1 -C 4） - 烷基，R 2的N-苯基-2-氰基-3-羟基巴豆酰胺衍生物是CN，CX3，WCX3，W（CH2）nCX3，NO2，（CH2）nCX3或卤素， 其中X是卤素，W是氧或硫原子，n是1-3的整数，R3是（C1-C4） - 烷基，（C3-C6） - 环烷基，CN或-CO-R4，其中 R4是用于治疗风湿性疾病，自身免疫疾病和器官受体对移植器官的排斥反应的（C 1 -C 4） - 烷基或（C 3 -C 6） - 环烷基和/或其生理上可耐受的盐，是 描述。

    Optically active compounds having plural chiral centers and production thereof
    4.
    发明授权
    Optically active compounds having plural chiral centers and production thereof 失效
    具有多个手性中心的光学活性化合物及其制备

    公开(公告)号：US5574182A

    公开(公告)日：1996-11-12

    申请号：US380519

    申请日：1995-01-30

    Applicant: Kazutoshi Miyazawa ,  Naoyuki Yoshida

    Inventor： Kazutoshi Miyazawa ,  Naoyuki Yoshida

    IPC: C07B53/00 ,  C07C67/03 ,  C07C67/475 ,  C07C67/48 ,  C07C69/675 ,  C07C69/732 ,  C07C253/30 ,  C07C255/20 ,  C07C255/23 ,  C07D213/55 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D319/06 ,  C07D405/06 ,  C07D407/06 ,  C12P7/62 ,  C12P41/00 ,  C07C69/66

    CPC classification number: C12P41/004 ,  C07D319/06 ,  C12P7/62 ,  Y10S435/822 ,  Y10S435/911

    Abstract: An ester is caused to act on a 2-substituted-3-hydroxycarboxylic acid ester as a racemate in the presence of hydrolase under substantially anhydrous conditions to effect a transesterification resulting in the resolution.The compound thus resolved is converted to an optically active 2,6-cis-2,5,6-substituted-1,3-dioxan-4-one and the resulting compound is recrystallized to give optically active 5,6-anti-2,5,6-substituted-1,3-dioxan-4-one and 5,6-syn-2,5,6-substituted-1,3-dioxan-4-one. Thus an optically active compound having plural chiral centers.Further, an optically active 2,5,6-substituted-1,3-dioxan-4-one obtained by transesterification and recrystallization is reacted with an alcohol to produce an optically active 2-substituted-3-hydroxycarboxylic acid ester.

    Abstract translation: 在基本上无水条件下，在水解酶的存在下，使酯作为外消旋物作用于2-取代-3-羟基羧酸酯上，进行酯交换反应，得到分辨率。 将如此分离的化合物转化为光学活性的2,6-顺式-2,5,6-取代-1,3-二恶烷-4-酮，将所得化合物重结晶，得到光学活性的5,6抗-2 ，5,6-取代-1,3-二恶烷-4-酮和5,6-syn-2,5,6-取代-1,3-二恶烷-4-酮。 因此，具有多个手性中心的光学活性化合物。 此外，通过酯交换和重结晶获得的光学活性的2,5,6-取代-1,3-二恶烷-4-酮与醇反应，得到光学活性的2-取代-3-羟基羧酸酯。

    DENDRIMERS WITH INTERIOR AND EXTERIOR FUNCTIONALITIES COMPRISING OF AZIDE OR ALKYNE GROUPS FOR POST-FUNCTIONALIZATION BY HUISGEN CLICK CYCLOADDITION
    6.
    发明申请
    DENDRIMERS WITH INTERIOR AND EXTERIOR FUNCTIONALITIES COMPRISING OF AZIDE OR ALKYNE GROUPS FOR POST-FUNCTIONALIZATION BY HUISGEN CLICK CYCLOADDITION 审中-公开
    具有包含AZID或ALKYNE组的内部和外部功能的吸收器，用于通过智慧点击循环进行后功能化

    公开(公告)号：US20140024815A1

    公开(公告)日：2014-01-23

    申请号：US14036520

    申请日：2013-09-25

    Applicant: POLYMER FACTORY SWEDEN AB

    Inventor： Anders HULT ,  Michael MALKOCH ,  Per ANTONI

    IPC: C07D407/14 ,  C07C245/04 ,  C07D405/14 ,  C07D405/12 ,  C07C229/30 ,  C07C255/20

    CPC classification number: C07D407/14 ,  C07C229/30 ,  C07C245/04 ,  C07C255/20 ,  C07D405/12 ,  C07D405/14 ,  C08G63/20 ,  C08G83/003

    Abstract: A dendritic structure includes a core and repeating units, wherein the repeating units comprise units of the type ABxCy, wherein x is 2, 3, or 4, wherein y is 1, 2, or 3, wherein C is selected from the group consisting of azides and alkynes, and wherein every repeating unit is bound to at least one other unit with at least one bond selected from the group consisting of the group consisting of an ester, an amide, a thioether, an ether, a urethane, an amine, and an imine. Advantages include that a “one-pot” growth of the dendritic structure is possible. It is possible to have more functional groups in a dendritic structure. It is possible to add different functional groups simultaneously both to an inner layer and to an outer layer in a dendritic structure.

    Abstract translation: 树枝状结构包括核和重复单元，其中重复单元包括ABxCy型单元，其中x为2,3或4，其中y为1,2或3，其中C选自由以下组成的组： 叠氮化物和炔烃，并且其中每个重复单元与至少一个其它单元结合，其中至少一个键选自由酯，酰胺，硫醚，醚，氨基甲酸酯，胺， 和亚胺。 优点包括树枝状结构的“一锅”生长是可能的。 可能在树枝状结构中具有更多的官能团。 可以同时向树状结构的内层和外层添加不同的官能团。

    N-substituted p-menthane carboxamides
    7.
    发明申请
    N-substituted p-menthane carboxamides 有权
    N-取代的对薄荷烷甲酰胺

    公开(公告)号：US20060276667A1

    公开(公告)日：2006-12-07

    申请号：US11437294

    申请日：2006-05-19

    Applicant: Christophe Galopin ,  Pablo Krawec ,  Jay Slack ,  Lori Tigani

    Inventor： Christophe Galopin ,  Pablo Krawec ,  Jay Slack ,  Lori Tigani

    IPC: C07C255/20 ,  C07C235/32

    CPC classification number: C07C255/60 ,  A61K8/42 ,  A61K2800/244 ,  A61Q11/00 ,  A61Q19/00 ,  C07C233/60 ,  C07C233/61 ,  C07C255/42 ,  C07C255/44 ,  C07C311/46 ,  C07C2601/14

    Abstract: Cooling compounds are provided having the formula: wherein, m is 0 or 1, Y and Z are selected independently from the group consisting of H, OH, C1-C4 straight or branched alkyl, and a C1-C4 straight or branched alkoxy, X is (CH2)n—R, where n is 0 or 1 and R is a group with non-bonding electrons, with the provisos that: (a) when Y and Z are H, X is not F, OH, MeO or NO2 in the 4-position and is not OH in the 2 or 6-position (b) when Y or Z is H then X, Y and Z are such that (i) the groups in the 3- and 4-positions are not both OMe, (ii) the groups in the 4- and 5-positions are not both OMe, (iii) the groups in 3- and 5-positions are not OMe if the group in the 4-position is OH, and (iv) the groups in the 3- and 5-positions are not OH if the group in the 4-position is methyl.

    Abstract translation: 提供具有下式的冷却化合物：其中m为0或1，Y和Z独立地选自H，OH，C 1 -C 4直链或支链烷基和C 1 -C 4直链或支链烷氧基，X 其中n为0或1，R为具有非键合电子的基团，前提条件是：（a）当Y（Y）为（CH 2） 并且Z是H，X不是4位的F，OH，MeO或NO 2 2，并且在Y或Z是H时不在2或6位（b）中的OH，则X ，Y和Z为（i）3-和4-位的基团不同时为OMe，（ii）4-和5-位的基团不同时为OMe，（iii）3 - 和5-位不是OMe，如果4位的基团是OH，和（iv）如果4位的基团是甲基，那么3-和5-位的基团不是OH。

    N-phenyl-2-cyano-3-hydroxy-propenamides
    9.
    发明授权
    N-phenyl-2-cyano-3-hydroxy-propenamides 失效
    N-苯基-2-氰基-3-羟基 - 丙烯酰胺

    公开(公告)号：US5416112A

    公开(公告)日：1995-05-16

    申请号：US254162

    申请日：1994-06-06

    Applicant: Elizabeth A. Kuo

    Inventor： Elizabeth A. Kuo

    IPC: A61K31/275 ,  A61P29/00 ,  C07C253/30 ,  C07C255/20 ,  C07C255/30 ,  C07C255/54 ,  C07C255/58 ,  C07C255/60 ,  C07C311/19 ,  C07C311/46 ,  C07C255/23

    CPC classification number: C07C255/20 ,  C07C2101/02

    Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms and alkenyl and alkynyl of 2 to 6 carbon atoms, R.sub.2 is hydrogen or alkyl of 1 to 3 carbon atoms, Y is selected from the group consisting of ##STR2## Z.sub.1 and Z.sub.2 are individually selected from the group consisting of hydrogen, halogen, --NO.sub.2, --CN and alkyl of 1 to 3 carbon atoms, R.sub.3 is hydrogen or alkyl of 1 to 3 carbon atoms, m is an integer from 0 to 6, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are individually selected from the group consisting of hydrogen, halogen, --CN, --NO.sub.2, alkyl, alkylthio and alkoxy of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, --COR.sub.10, --(CH.sub.2).sub.n --CX.sub.3, --O--(CH.sub.2).sub.n CX.sub.3 and --S--(CH.sub.2).sub.n --CX.sub.3, R.sub.10 is selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and cycloalkyl of 3 to 6 carbon atoms, n is an integer from 0 to 3, X is halogen or R.sub.6 and R.sub.7 together form --O--CH.sub.2 --O-- and their non-toxic, pharmaceutically acceptable salts with a base having anti-inflammatory and immunomodulatory activity.

    Abstract translation: 选自下式的化合物的化合物其中R 1选自1至6个碳原子的烷基，3至6个碳原子的环烷基和2至6个碳原子的链烯基和炔基 原子，R 2为氢或1〜3个碳原子的烷基，Y选自NR 3，SO 2 NR 3，NR 3 SO 2，CHOH，Z 1，Z 2分别选自 氢，卤素，-NO 2，-CN和1至3个碳原子的烷基，R 3是氢或1至3个碳原子的烷基，m是0至6的整数，R4，R5，R6，R7和R8分别是 选自氢，卤素，-CN，-NO 2，烷基，烷硫基和1至6个碳原子的烷氧基，3至6个碳原子的环烷基，-COR 10， - （CH 2）n -C CX 3，-O- （CH2）nCX3和-S-（CH2）n-CX3，R10选自氢，1至6个碳原子的烷基和3至6个碳原子的环烷基，n为0至3的整数， X是hal ogen或R6和R7一起与具有抗炎和免疫调节活性的碱形成-O-CH2-O-及其无毒的药学上可接受的盐。

    Optically active compounding having plural chiral centers and production thereof
    10.
    发明授权
    Optically active compounding having plural chiral centers and production thereof 失效
    具有多个手性中心的光学活性配混及其制造

    公开(公告)号：US5411877A

    公开(公告)日：1995-05-02

    申请号：US257666

    申请日：1994-06-08

    Applicant: Kazutoshi Miyazawa ,  Naoyuki Yoshida

    Inventor： Kazutoshi Miyazawa ,  Naoyuki Yoshida

    IPC: C07B53/00 ,  C07C67/03 ,  C07C67/475 ,  C07C67/48 ,  C07C69/675 ,  C07C69/732 ,  C07C253/30 ,  C07C255/20 ,  C07C255/23 ,  C07D213/55 ,  C07D237/08 ,  C07D239/26 ,  C07D241/12 ,  C07D319/06 ,  C07D405/06 ,  C07D407/06 ,  C12P7/62 ,  C12P41/00 ,  C12P17/06

    CPC classification number: C12P41/004 ,  C07D319/06 ,  C12P7/62 ,  Y10S435/822 ,  Y10S435/911

    Abstract: An ester is caused to act on a 2-substituted-3-hydroxycarboxylic acid ester as a racemate in the presence of hydrolase under substantially anhydrous conditions to effect a transesterification resulting in the resolution.The compound thus resolved is converted to an optically active 2,6-cis-2,5,6-substituted-1,3-dioxan-4-one and the resulting compound is recrystallized to give optically active 5,6-anti-2,5,6-substituted-1,3-dioxan-4-one and 5,6-syn-2,5,6-substituted-1,3-dioxan-4-one. Thus an optically active compound having plural chiral centers.Further, an optically active 2,5,6-substituted-1,3-dioxan-4-one obtained by transesterification and recrystallization is reacted with an alcohol to produce an optically active 2-substituted-3-hydroxycarboxylic acid ester.

    Abstract translation: 在基本上无水条件下，在水解酶的存在下，使酯作为外消旋物作用于2-取代-3-羟基羧酸酯上，进行酯交换反应，得到分辨率。 将如此分离的化合物转化为光学活性的2,6-顺式-2,5,6-取代-1,3-二恶烷-4-酮，将所得化合物重结晶，得到光学活性的5,6抗-2 ，5,6-取代-1,3-二恶烷-4-酮和5,6-syn-2,5,6-取代-1,3-二恶烷-4-酮。 因此，具有多个手性中心的光学活性化合物。 此外，通过酯交换和重结晶获得的光学活性的2,5,6-取代-1,3-二恶烷-4-酮与醇反应，得到光学活性的2-取代-3-羟基羧酸酯。

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