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    Composition containing polyamine transport inhibitor and use thereof
    3.
    发明申请
    Composition containing polyamine transport inhibitor and use thereof 有权
    含有多胺转运抑制剂的组合物及其用途

    公开(公告)号：US20050245615A1

    公开(公告)日：2005-11-03

    申请号：US11062481

    申请日：2005-02-23

    申请人： Mark Burns ,  Gerard Graminski ,  Nand Baindur ,  Reitha Weeks

    发明人： Mark Burns ,  Gerard Graminski ,  Nand Baindur ,  Reitha Weeks

    IPC分类号： C07C237/10 ,  C07C237/22 ,  C07C255/24 ,  C07C311/06 ,  C07C311/19 ,  C07C311/42 ,  C07D233/61 ,  C07D307/68 ,  C07D333/34 ,  A61K31/16

    CPC分类号： C07C237/10 ,  C07C237/22 ,  C07C255/24 ,  C07C311/06 ,  C07C311/19 ,  C07C311/42 ,  C07C2601/04 ,  C07C2601/14 ,  C07C2602/42 ,  C07C2603/74 ,  C07D307/68 ,  C07D333/34

    摘要： Proliferative cutaneous disease states or conditions are treated by administering a polyamine transport inhibitor R-X-L-polyamine wherein R is a straight or branched C10-50 saturated or unsaturated aliphatic, carboxyalkyl, carbalkoxyalkyl, or alkoxy; a C1-8 alicyclic; a single or multiring aryl substituted or unsubstituted aliphatic; and aliphatic-substituted or unsubstituted single or multiring aromatic; a single or multiring heterocyclic; a single or multiring heterocyclic aliphatic; an aryl sulfonyl; X is —CO—, —SO2—, or —CH2—; and L is a covalent bond or a naturally occurring amino acid, lysine, ornithine, 2,4-diaminobutyric acid, or pharmaceutically acceptable salts thereof or prodrug thereof, and a polyamine biosynthesis inhibitor.

    摘要翻译： 通过施用多胺转运抑制剂<？in-line-formula description =“In-Line Formulas”end =“lead”→> RXL-多胺<？in-line-formula description =“In”来治疗增生性皮肤疾病状态或病症 其中R是直链或支链的C10-50饱和或不饱和脂族，羧基烷基，烷氧基烷基或烷氧基; C1-8脂环族 单或多芳基取代或未取代的脂族基; 和脂族取代或未取代的单或多芳族芳族; 单一或多重杂环; 单一或多重杂环脂肪族; 芳基磺酰基; X是-CO - ， - SO 2 - 或-CH 2 - 。 L是共价键或天然存在的氨基酸，赖氨酸，鸟氨酸，2,4-二氨基丁酸或其药学上可接受的盐或其前药，以及多胺生物合成抑制剂。

    Selective thrombin inhibitors
    6.
    发明授权
    Selective thrombin inhibitors 失效
    选择性凝血酶抑制剂

    公开(公告)号：US5985899A

    公开(公告)日：1999-11-16

    申请号：US967661

    申请日：1997-11-10

    申请人： Yeong Soo Oh ,  Sang Soo Kim ,  Sang Yeul Hwang ,  Mi Kyung Yun ,  Seong Ryul Hwang ,  Seong Won Hong ,  Yong Hee Lee ,  Yi Na Jeong ,  Koo Lee ,  You Seung Shin

    发明人： Yeong Soo Oh ,  Sang Soo Kim ,  Sang Yeul Hwang ,  Mi Kyung Yun ,  Seong Ryul Hwang ,  Seong Won Hong ,  Yong Hee Lee ,  Yi Na Jeong ,  Koo Lee ,  You Seung Shin

    IPC分类号： C07C257/22 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07D211/60 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  A61K31/445 ,  C07D211/34

    CPC分类号： C07C257/22 ,  C07C311/19 ,  C07C311/29 ,  C07C311/42 ,  C07D211/60 ,  C07D295/185 ,  C07D295/205 ,  C07D295/26 ,  C07C2101/02 ,  C07C2101/10 ,  C07C2101/14

    摘要： The present invention relates to a novel selective thrombin inhibitor having the following formula (I), which is also effective by oral administration: ##STR1## in which R.sup.1 represents acetyl substituted with aryl or aryloxy, or represents sulfonyl substituted with substituted or unsubstituted aryl or N-containing heterocyclic group,X represents a group of formula ##STR2## R.sup.2 and R.sup.3 independently of one another represent hydrogen; cycloalkyl substituted or unsubstituted with carboxyl or alkoxycarbonyl; arylalkyloxy; hydroxy; or lower alkyl substituted or unsubstituted with carboxyl, alkoxycarbonyl or hydroxy, orR.sup.2 and R.sup.3 together with nitrogen atom to which they are attached can form a piperidine group substituted with carboxyl or alkoxycarbonyl,R.sup.4 represents hydrogen, lower alkyl or lower alkoxy,R.sup.5 represents alkanesulfonyl; alkoxycarbonyl; alkylcarbonyl; formyl; lower alkyl; aryl substituted or unsubstituted with alkoxy or haloalkyl; or hydroxy-substituted lower alkyl, andR.sup.6 and R.sup.7 independently of one another represent hydrogen, lower alkyl or amino,and to a process for preparation thereof and a pharmaceutical composition for thrombin inhibition which comprises the compound of formula (I) as an active ingredient.

    摘要翻译： 本发明涉及一种新型的具有下列通式（I）的选择性凝血酶抑制剂，其也可通过口服给药有效：其中R1表示被芳基或芳氧基取代的乙酰基，或表示被取代或未取代的芳基或含N 杂环基，X表示式R 2的基团，R 3彼此独立地表示氢; 被羧基或烷氧基羰基取代或未取代的环烷基; 芳基烷氧基; 羟基; 或与羧基，烷氧基羰基或羟基取代或未取代的低级烷基，或R 2和R 3与它们所连接的氮原子一起形成被羧基或烷氧基羰基取代的哌啶基，R 4表示氢，低级烷基或低级烷氧基，R 5表示烷磺酰基 ; 烷氧基羰基 烷基羰基; 甲酰基 低级烷基 被烷氧基或卤代烷基取代或未取代的芳基; 或羟基取代的低级烷基，R 6和R 7彼此独立地表示氢，低级烷基或氨基，以及其制备方法和用于凝血酶抑制的药物组合物，其包含式（I）化合物作为活性成分 。

    Catalytic asymmetric aminohydroxylation of olefins with sulfonamides
    7.
    发明授权
    Catalytic asymmetric aminohydroxylation of olefins with sulfonamides 失效
    用磺酰胺催化烯烃的不对称氨基羟基化

    公开(公告)号：US5859281A

    公开(公告)日：1999-01-12

    申请号：US651819

    申请日：1996-05-21

    申请人： K. Barry Sharpless ,  Guigen Li ,  Han-Ting Chang

    发明人： K. Barry Sharpless ,  Guigen Li ,  Han-Ting Chang

    IPC分类号： C07C213/00 ,  C07C303/40 ,  C07C311/04 ,  C07C311/06 ,  C07C311/07 ,  C07C311/17 ,  C07C311/19 ,  C07C311/20 ,  C07C311/29 ,  C07C311/42 ,  C07C303/00

    CPC分类号： C07C303/40 ,  C07C213/00 ,  C07B2200/07 ,  C07C2101/14

    摘要： .beta.-Hydroxyamines and .beta.-hydroxysulfonamides are synthesized from olefin substrates by means on a catalyzed asymmetric addition reaction. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. Sulfonamides are employed as an oxidant nitrogen source for the production of .beta.-hydroxysulfonamides. Excellent yields and enantiomeric efficiencies are achieved with co-solvents containing a 50/50 (v/v) mixtures of water and organic solvent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxysulfonamides.

    摘要翻译： 通过催化不对称加成反应由烯烃底物合成β-羟基胺和β-羟基磺酰胺。 加成反应由锇催化并被手性配体共催化。 除了与锇共助催化剂之外，手性配体还用于区域选择地和对映选择性地引导加成反应。 二价配体优于一价配体，因为它们具有增强的区域和对映选择性。 磺酰胺被用作生产β-羟基磺酰胺的氧化剂氮源。 使用含有水和有机溶剂的50/50（v / v）混合物的共溶剂可获得优异的收率和对映体效率。 通过脱保护相应的β-羟基磺酰胺得到β-羟基胺。

    Novel methine compounds, polymers containing them and formed articles therefrom
    10.
    发明授权
    Novel methine compounds, polymers containing them and formed articles therefrom 失效
    新型次甲基化合物，含有它们的聚合物和由其形成的制品

    公开(公告)号：US4958043A

    公开(公告)日：1990-09-18

    申请号：US182633

    申请日：1988-04-18

    申请人： Max A. Weaver ,  Wayne P. Pruett ,  Samuel D. Hilbert

    发明人： Max A. Weaver ,  Wayne P. Pruett ,  Samuel D. Hilbert

    IPC分类号： C07C229/44 ,  C07C255/34 ,  C07C311/35 ,  C07C311/42 ,  C07C317/44 ,  C07C323/60 ,  C08G63/685 ,  C08G64/04 ,  C08K5/00 ,  C08K5/315

    CPC分类号： C08K5/005 ,  C07C229/44 ,  C07C255/34 ,  C07C311/35 ,  C07C311/42 ,  C07C317/44 ,  C07C323/60 ,  C08G63/6858 ,  C08G64/045 ,  C08K5/315

    摘要： A composition useful for incorporation into polymer compositions employed for food packaging or the like comprising a bis- or tris-methine compound having the structural formula ##STR1## wherein A is selected from the radicals ##STR2## wherein R' and R" are each selected from chlorine, bromine, fluorine, alkyl, alkoxy, aryl, aryloxy and arylthio;each n is independently 0, 1, 2;R.sub.1 is selected from a large variety of radicals such as cycloalkyl, phenyl, and straight or branched alkyl which may be substituted;R.sub.2 is alkylene or the like;R.sub.3, R.sub.4, and R.sub.5 are each selected from hydrogen and alkyl; andP and Q and P.sup.1 and Q.sup.1 are selected from cyano, carbalkoxy, carbaryloxy, carbaralkyloxy, or the like.The invention compositions are especially useful in combination with molding or fiber-grade condensation polymer; most preferably such polymer having copolymerized therein a total of from 1.0 to about 100,000 ppm, of the reactant residue moieties of one or more of such bis- or tris-methine compounds.

    摘要翻译： 可用于掺入用于食品包装等的聚合物组合物中的组合物，其包含具有结构式为“IMAGE”的双或三 - 次甲基化合物，其中A选自基团 + TR＆lt; IMAGE＆gt;其中R'和R“各自选自氯，溴，氟，烷基，烷氧基，芳基，芳氧基和芳硫基; 每个n独立地为0,1,2; R1选自各种基团，例如环烷基，苯基，可被取代的直链或支链烷基; R2是亚烷基等; R3，R4和R5各自选自氢和烷基; 并且P和Q以及P1和Q1选自氰基，烷氧基，碳酰氧基，卡巴尔基氧基等。 本发明组合物特别适用于成型或纤维级缩聚物; 最优选地，其中共聚有总共为1.0至约100,000ppm的一种或多种这样的双 - 或三 - 次甲基化合物的反应物残余部分的这种聚合物。