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96 条记录 (耗时 0.034 秒)

    Polymeric thiol-linked prodrugs employing benzyl elimination systems
    81.
    发明授权
    Polymeric thiol-linked prodrugs employing benzyl elimination systems 失效
    使用苄基消除系统的聚合硫醇连接的前药

    公开(公告)号：US07262164B2

    公开(公告)日：2007-08-28

    申请号：US10290694

    申请日：2002-11-08

    申请人： Yun H. Choe ,  Richard B. Greenwald

    发明人： Yun H. Choe ,  Richard B. Greenwald

    IPC分类号： A61K38/16

    CPC分类号： A61K47/60

    摘要： Thiol-linked polymeric prodrugs, methods of making and using the same are disclosed. The use of a sulfhydryl bond in combination with a benzyl elimination system results in the formation of prodrugs which can take advantage of plasma enzymes in vivo for regeneration of the parent molecule. A preferred prodrug in accordance with the invention is: where S-MP is 6-mercaptopurine.

    摘要翻译： 公开了硫醇连接的聚合物前药，其制备和使用方法。 使用巯基键与苄基消除系统结合导致前体药物的形成，其可以在体内利用血浆酶来再生母体分子。 根据本发明优选的前药是：其中S-MP是6-巯基嘌呤。

    Prodrugs of anticancer agents employing substituted aromatic acids
    82.
    发明授权
    Prodrugs of anticancer agents employing substituted aromatic acids 失效
    使用取代芳香酸的抗癌药物的前药

    公开(公告)号：US06936597B2

    公开(公告)日：2005-08-30

    申请号：US10103323

    申请日：2002-03-21

    申请人： Richard B. Greenwald ,  Yun H. Choe

    发明人： Richard B. Greenwald ,  Yun H. Choe

    IPC分类号： A61K31/74 ,  A61K31/77 ,  A61K47/48 ,  A61P1/04 ,  A61P5/38 ,  A61P9/00 ,  A61P9/08 ,  A61P15/18 ,  A61P19/06 ,  A61P25/00 ,  A61P25/02 ,  A61P25/22 ,  A61P29/00 ,  A61P31/10 ,  A61P35/00 ,  A61P43/00 ,  C07C235/16 ,  C08G65/329 ,  A61K31/70 ,  A61K31/7068 ,  C07C63/00 ,  C07H19/06

    CPC分类号： C07C235/16 ,  A61K31/74 ,  A61K47/60

    摘要： Polymeric prodrugs of the formula: wherein B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.

    摘要翻译： 下式的聚合物前体药物：其中B选自OH，离去基团，含胺部分的残基和含羟基部分的残基; Y 1选自O，S和NR 5; M是NR 3，O或S; Ar是当式I中包含时形成多取代的芳族或杂芳族烃或多取代杂环基的部分; （m）为零或正整数; R 1-3和R 5各自独立地选自氢，C 1-6烷基，C 3-8环烷基， 12个支链烷基，C 3〜8个环烷基，C 1-6 - 取代的烷基，C 3-8 - 取代的环烷基，芳基 取代的芳基，芳烷基，C 1-6 - 杂烷基，取代的C 1-6 - 杂烷基，C 1-6烷氧基，苯氧基和C 1-6烷基， 杂烷基; R 4是聚合物残基; 以及制造和使用该方法的方法。

    .alpha.-interferon-polymer-conjugates having enhanced biological activity and methods of preparing the same
    84.
    发明授权
    .alpha.-interferon-polymer-conjugates having enhanced biological activity and methods of preparing the same 失效
    具有增强的生物活性的α-干扰素 - 聚合物缀合物及其制备方法

    公开(公告)号：US5981709A

    公开(公告)日：1999-11-09

    申请号：US994623

    申请日：1997-12-19

    申请人： Richard B. Greenwald ,  Carl W. Gilbert

    发明人： Richard B. Greenwald ,  Carl W. Gilbert

    IPC分类号： A61K38/21 ,  A61K47/48 ,  C07K1/107 ,  C07K14/56 ,  C07K1/113

    CPC分类号： A61K47/48215 ,  A61K38/212 ,  C07K1/1077 ,  C07K14/56

    摘要： A process for preparing .alpha.-interferon-polymer conjugates having high levels of retained interferon activity and relatively long circulating lives in vivo is disclosed. The process includes forming substantially non-antigenic .alpha.-interferon-polymer conjugates, combining the .alpha.-interferon-polymer conjugates with a sufficient amount of an acid to reduce the pH of the conjugates to a level which is sufficient to cleave the polymer linkages in an active site area of the interferon and thereafter adjusting the .alpha.-interferon-polymer conjugates to a physiologically-acceptable pH. Methods of treating interferon-susceptible conditions with the compositions of the present invention are also disclosed.

    摘要翻译： 公开了一种制备具有高水平的保留干扰素活性和相对长的循环寿命的α-干扰素 - 聚合物缀合物的方法。 该方法包括形成基本上非抗原性的α-干扰素 - 聚合物缀合物，将α-干扰素 - 聚合物缀合物与足够量的酸组合以将缀合物的pH降低至足以在 干扰素的活性位点面积，然后将α-干扰素 - 聚合物缀合物调节至生理学上可接受的pH。 还公开了用本发明组合物治疗干扰素敏感病症的方法。

    Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents
    85.
    发明授权
    Trialkyl-lock-facilitated polymeric prodrugs of amino-containing bioactive agents 失效
    含氨基的生物活性剂的三烷基锁定促进的聚合物前药

    公开(公告)号：US5965119A

    公开(公告)日：1999-10-12

    申请号：US676

    申请日：1997-12-30

    申请人： Richard B. Greenwald ,  Yun H. Choe

    发明人： Richard B. Greenwald ,  Yun H. Choe

    IPC分类号： A61K31/135 ,  A61K31/136 ,  A61K31/65 ,  A61K31/704 ,  A61K31/7068 ,  A61K38/00 ,  A61K45/00 ,  A61K47/48 ,  A61P43/00 ,  C07C237/22 ,  C07C271/16 ,  C07C271/22 ,  C08G65/329 ,  A61K31/765

    CPC分类号： A61K47/48215 ,  C07C237/22 ,  C07C271/16 ,  C07C271/22 ,  C07B2200/11

    摘要： The present invention is directed to double prodrugs containing polymeric-based transport forms. These polymeric prodrugs are preferably of the formula: ##STR1## wherein: B is a leaving group or a residue of an amine-containing target moiety;G is ##STR2## or CH.sub.2 ; Y.sub.1-2 are independently O or S;M is X or Q; where X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2);R.sub.1, R.sub.4, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and R.sub.13 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls, substituted C.sub.1-6 heteroalkyls;R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.1-6 alkoxy, phenoxy, C.sub.1-8 heteroalkyls, C.sub.1-8 heteroalkoxy, substituted C.sub.1-6 alkyls, C.sub.3-8 cycloalkyls, C.sub.3-8 substituted cycloalkyls, aralkyls, aryls, substituted aryls, such as aryls substituted with halo-, nitro- and cyano-; carboxy-, C.sub.1-6 carboxyalkyls and C.sub.1-6 alkyl carbonyls;(m) is zero or one;(n) is zero or a positive integer;(p) is zero, one or two; andR.sub.11 is a substantially non-antigenic polymer.The first prodrug is generated when the polymeric portion of the double prodrug is cleaved and the parent molecule is generated rapidly thereafter in vivo, as a result of a trialkyl lock type lactonization-type reaction.

    摘要翻译： 本发明涉及含有基于聚合物的输送形式的双重前药。 这些聚合前药优选具有下式：其中：B是离去基团或含胺目标部分的残基; G是或CH2; Y1-2独立地为O或S; M为X或Q; 其中X是吸电子基团，Q是含有从C（= Y2）定位3至6个原子的自由电子对的部分; R 1，R 4，R 7，R 8，R 9，R 10和R 13独立地选自氢，C 1-6烷基，C 3-12支链烷基，C 3-8环烷基，C 1-6取代的烷基，C 3-8取代的环烷基 芳基，取代的芳基，芳烷基，C 1-6杂烷基，取代的C 1-6杂烷基; R 2，R 3，R 5和R 6独立地选自氢，C 1-6烷基，C 1-6烷氧基，苯氧基，C 1-8杂烷基，C 1-8杂烷氧基，取代的C 1-6烷基，C 3-8环烷基， C 3-8取代的环烷基，芳烷基，芳基，取代的芳基，例如被卤素，硝基和氰基取代的芳基; 羧基，C 1-6羧基烷基和C 1-6烷基羰基; （m）为零或一; （n）为零或正整数; （p）为零，一或二; R11是基本上非抗原性的聚合物。 当双前体药物的聚合物部分被切割并且其后在体内快速产生母体分子时，由于三烷基锁定型内酯化反应的结果，产生第一种前体药物。

    2'-and/or 7-substituted taxanes
    86.
    发明授权
    2'-and/or 7-substituted taxanes 失效
    2'-和/或7-取代的紫杉烷类

    公开(公告)号：US5622986A

    公开(公告)日：1997-04-22

    申请号：US351462

    申请日：1994-12-12

    申请人： Richard B. Greenwald ,  Durgadas Bolikal

    发明人： Richard B. Greenwald ,  Durgadas Bolikal

    IPC分类号： A61K31/335 ,  C07D305/14

    CPC分类号： C07D305/14 ,  A61K31/335

    摘要： 2'- and/or 7'- substituted taxoid derivatives having improved water-solubility and/or enhanced therapeutic activity and methods of making the same are disclosed.

    摘要翻译： PCT No.PCT / US94 / 12133 Sec。 371日期1994年12月12日第 102（e）日期1994年12月12日PCT 1994年10月19日PCT PCT。 出版物WO95 / 11020 日期：1992年4月27日公开了具有改善的水溶性和/或增强的治疗活性的'和/或7'-取代的紫杉烷衍生物及其制备方法。

    Aryl imidate activated polyalkylene oxides
    87.
    发明授权
    Aryl imidate activated polyalkylene oxides 失效
    芳基酰亚胺酯活化聚环氧烷

    公开(公告)号：US5298643A

    公开(公告)日：1994-03-29

    申请号：US995585

    申请日：1992-12-22

    申请人： Richard B. Greenwald

    发明人： Richard B. Greenwald

    IPC分类号： C07C257/08 ,  C08G65/329 ,  C08G65/332 ,  C08G65/333 ,  C07C249/00

    CPC分类号： C07C257/08 ,  C08G65/329 ,  C08G65/3326 ,  C08G65/33365

    摘要： Water-soluble aryl imidate activated polyalkylene oxides having improved hydrolytic stability and conjugates of the aryl imidate activated polyalkylene oxides with biologically active nucleophiles are disclosed. Methods of preparing the activated polyalkylene oxides and conjugates thereof are also disclosed.

    摘要翻译： 公开了具有改进的水解稳定性的水溶性芳基亚胺化物活化聚亚烷基氧化物和芳基亚胺酯活化的聚环氧烷与生物活性亲核试剂的缀合物。 还公开了制备活性聚环氧烷及其共轭物的方法。

    Photographic compositions with silver halide solvents containing thioether groups
    89.
    发明授权
    Photographic compositions with silver halide solvents containing thioether groups 失效
    具有含硫醚基团的卤化银溶剂的摄影组合物

    公开(公告)号：US4211562A

    公开(公告)日：1980-07-08

    申请号：US930995

    申请日：1978-08-04

    申请人： Richard B. Greenwald

    发明人： Richard B. Greenwald

    IPC分类号： G03C5/38 ,  G03C8/36

    CPC分类号： G03C8/365 ,  G03C5/38

    摘要： Difunctional compounds wherein one of said functions is a hard or soft atom that ionizes to the corresponding anion in alkaline solution to combine with silver cation and the other of said functions is a non-ionizable soft base that additionally combines with said silver cation are employed as silver halide complexing agents in photography. In a preferred embodiment, the difunctional compounds possess (a) an O, N or C atom that ionizes to the corresponding O.sup..crclbar., N.sup..crclbar. or C.sup..crclbar. anion in basic solution and (b) an --S-- containing moiety excluding --SH and moieties that form --S.sup..crclbar. in basic solution wherein the --S-- of said moiety is positioned alpha, beta, gamma, delta, epsilon or zeta to said anion.

    摘要翻译： 其中所述功能之一是在碱性溶液中与相应阴离子电离以与银阳离子结合并且所述功能中的另一个是与所述银阳离子另外组合的不可离子化软碱的硬键或软原子用作 卤化银络合剂在摄影中。 在优选的实施方案中，双官能化合物具有（a）在碱性溶液中电离至相应的O（ - ），N（ - ）或C（ - ）阴离子的O，N或C原子，（b）-S- 含有-SH的部分和在碱性溶液中形成-S（ - ）的部分，其中所述部分的-S-位于所述阴离子的α，β，γ，δ，ε或zeta。

    Thioether substituted silver halide solvents
    90.
    发明授权
    Thioether substituted silver halide solvents 失效
    硫醚取代的卤化银溶剂

    公开(公告)号：US4150228A

    公开(公告)日：1979-04-17

    申请号：US811712

    申请日：1977-06-30

    申请人： Richard B. Greenwald

    发明人： Richard B. Greenwald

    IPC分类号： G03C8/36 ,  C07D239/24

    CPC分类号： G03C8/365

    摘要： The present invention is concerned with novel compounds useful as photographic silver halide complexing agents and with their photographic use. The subject compounds are represented by the formulas ##STR1## wherein one of R.sup.1 and R.sup.2 is --CH.sub.2).sub.x SR.sup.3 and the other of said R.sup.1 and R.sup.2 is --CH.sub.2).sub.y SR.sup.3 wherein R.sup.3 is alkyl, x is a whole number 0 or 1 and y is a whole number from 0 to 5.

    摘要翻译： 本发明涉及可用作照相卤化银络合剂和其照相用途的新型化合物。 主题化合物由下式表示：其中R1和R2之一为-CH2）xSR3，而所述R1和R2中的另一个为-CH2）ySR3，其中R3为烷基，x为0或1的整数，y为 是从0到5的整数。