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16 条记录 (耗时 0.016 秒)

    Activated polyers and conjugates thereof
    1.
    发明授权
    Activated polyers and conjugates thereof 失效
    活性聚合物及其共轭物

    公开(公告)号：US5081295A

    公开(公告)日：1992-01-14

    申请号：US572727

    申请日：1990-08-24

    申请人： Dayton T. Reardan ,  Dane A. Goff

    发明人： Dayton T. Reardan ,  Dane A. Goff

    IPC分类号： C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/333 ,  C08G65/338 ,  C12N11/08

    CPC分类号： C08G65/33389 ,  C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/338 ,  C12N11/08

    摘要： Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.

    摘要翻译： 含有反应性羰基或易于转化成反应性羰基的基团的酶，蛋白质，药物和固体载体的大分子物质通过与下式化合物的反应来进行修饰：其中R1是H，C1-C20 烷基，苯基，（C 1 -C 10烷基）取代的苯基或苯基取代的C 1 -C 10烷基; R2是C2-C5亚烷基或（C1-C4烷氧基） - 取代C2-C5亚烷基; R 3是H或C 1 -C 4烷基; n至少为5; m为零或1。

    Activated polymers and conjugates thereof
    2.
    发明授权
    Activated polymers and conjugates thereof 失效
    活性聚合物及其共轭物

    公开(公告)号：US5103039A

    公开(公告)日：1992-04-07

    申请号：US717431

    申请日：1991-06-19

    申请人： Dayton T. Reardan ,  Dane A. Goff

    发明人： Dayton T. Reardan ,  Dane A. Goff

    IPC分类号： C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/333 ,  C08G65/338 ,  C12N11/08

    CPC分类号： C12N11/08 ,  C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/33389 ,  C08G65/338

    摘要： Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.

    摘要翻译： 含有反应性羰基或易于转化成反应性羰基的基团的酶，蛋白质，药物和固体载体的大分子物质通过与下式化合物的反应来进行修饰：其中R1是H，C1-C20 烷基，苯基，（C 1 -C 10烷基）取代的苯基或苯基取代的C 1 -C 10烷基; R2是C2-C5亚烷基或（C1-C4烷氧基） - 取代C2-C5亚烷基; R 3是H或C 1 -C 4烷基; n至少为5; m为零或1。

    Activated polymers and conjugates thereof
    3.
    发明授权
    Activated polymers and conjugates thereof 失效
    活性聚合物及其共轭物

    公开(公告)号：US5157099A

    公开(公告)日：1992-10-20

    申请号：US806690

    申请日：1991-12-12

    申请人： Dayton T. Reardan ,  Dane A. Goff

    发明人： Dayton T. Reardan ,  Dane A. Goff

    IPC分类号： C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/333 ,  C08G65/338 ,  C12N11/08

    CPC分类号： C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/33389 ,  C08G65/338 ,  C12N11/08

    摘要： Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl, groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.

    摘要翻译： 含有反应性羰基，容易转化成反应性羰基的基团或基团的酶，蛋白质，药物和固体支持物的大分子物质通过与式（III）化合物反应而被修饰，其中R1是H，C1- C20烷基，苯基，（C1-C10烷基）取代的苯基或苯基取代的C1-C10烷基; R2是C2-C5亚烷基或（C1-C4烷氧基） - 取代C2-C5亚烷基; R 3是H或C 1 -C 4烷基; n至少为5; m为零或1。

    Activated polymers and conjugates thereof
    4.
    发明授权
    Activated polymers and conjugates thereof 失效
    活性聚合物及其共轭物

    公开(公告)号：US5090914A

    公开(公告)日：1992-02-25

    申请号：US572726

    申请日：1990-08-24

    申请人： Dayton T. Reardan ,  Dane A. Goff

    发明人： Dayton T. Reardan ,  Dane A. Goff

    IPC分类号： C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/333 ,  C08G65/338 ,  C12N11/08

    CPC分类号： C07C271/28 ,  C07C229/60 ,  C07C237/32 ,  C08G65/322 ,  C08G65/33389 ,  C08G65/338 ,  C12N11/08

    摘要： Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.

    摘要翻译： 含有反应性羰基或易于转化成反应性羰基的基团的酶，蛋白质，药物和固体载体的大分子物质通过与下式化合物的反应来进行修饰：其中R1是H，C1-C20 烷基，苯基，（C 1 -C 10烷基）取代的苯基或苯基取代的C 1 -C 10烷基; R2是C2-C5亚烷基或（C1-C4烷氧基） - 取代C2-C5亚烷基; R 3是H或C 1 -C 4烷基; n至少为5; m为零或1。

    Linking agents and methods
    5.
    发明授权
    Linking agents and methods 失效
    链接代理和方法

    公开(公告)号：US5218112A

    公开(公告)日：1993-06-08

    申请号：US573615

    申请日：1990-08-27

    申请人： Dayton T. Reardan ,  Dane A. Goff

    发明人： Dayton T. Reardan ,  Dane A. Goff

    IPC分类号： C07C323/20 ,  C07C323/32 ,  C07C327/30 ,  C07D213/71 ,  G01N33/531

    CPC分类号： G01N33/531 ,  C07C323/20 ,  C07C323/32 ,  C07C327/30 ,  C07D213/71

    摘要： Compounds containing carbohydrate moieties or carboxyl groups are linked to either compounds containing thiol moieties or electron-deficient moieties by the use of linking agents of the formula ##STR1## in which R.sup.1 is NH.sub.2 -- or NH.sub.2 --NH--; R.sup.2 is --NH--C(O)--, --C(O)--NH--, or --C(O)--; R.sup.3 is C.sub.1 -C.sub.10 alkylene, C.sub.5 -C.sub.7 cyclic alkylene, arylene, phenyl-substituted C.sub.1 -C.sub.10 alkylene, benzyl-substituted C.sub.1 -C.sub.10 alkylene, or amino-substituted C.sub.1 -C.sub.10 alkylene; R.sup.4 is H, acetyl, ##STR2## where R.sup.5 is C.sub.1 -C.sub.5 alkyl; m is zero or 1; and n ia zero or 1.

    摘要翻译： 含有碳水化合物部分或羧基的化合物通过使用其中R1是NH2-或NH2-NH-的式“IMAGE”的连接剂与包含硫醇部分或电子缺乏部分的化合物连接; R2是-NH-C（O） - ， - C（O）-NH-或-C（O） - ; R3是C1-C10亚烷基，C5-C7环亚烷基，亚芳基，苯基取代的C1-C10亚烷基，苄基取代的C1-C10亚烷基或氨基取代的C1-C10亚烷基; R4是H，乙酰基，其中R 5是C 1 -C 5烷基; m为零或1; 和n ia为零或1。

    Activated polymers and conjugates thereof
    7.
    发明授权
    Activated polymers and conjugates thereof 失效
    活性聚合物及其共轭物

    公开(公告)号：US5221771A

    公开(公告)日：1993-06-22

    申请号：US914688

    申请日：1992-07-15

    申请人： Dayton T. Reardan ,  Dane A. Goff

    发明人： Dayton T. Reardan ,  Dane A. Goff

    IPC分类号： C07C229/60 ,  C07C237/32 ,  C07C271/28 ,  C08G65/322 ,  C08G65/333 ,  C08G65/338 ,  C12N11/08

    CPC分类号： C07C237/32 ,  C07C229/60 ,  C07C271/28 ,  C08G65/322 ,  C08G65/33389 ,  C08G65/338 ,  C12N11/08

    摘要： Macromolecular species such as enzymes, proteins, drugs, and solid supports which contain reactive carbonyl groups or groups which are readily converted to reactive carbonyl groups are modified by reaction with a compound of the formula ##STR1## in which R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, phenyl, (C.sub.1 -C.sub.10 alkyl)-substituted phenyl, or phenyl-substituted C.sub.1 -C.sub.10 alkyl; R.sup.2 is C.sub.2 -C.sub.5 alkylene or (C.sub.1 -C.sub.4 alkoxy)-substituted C.sub.2 -C.sub.5 alkylene; R.sup.3 is ##STR2## R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; n is at least 5; and m is zero or 1.

    摘要翻译： 含有反应性羰基或易于转化成反应性羰基的基团的酶，蛋白质，药物和固体载体的大分子物质通过与下式化合物的反应来进行修饰：其中R1是H，C1-C20 烷基，苯基，（C 1 -C 10烷基）取代的苯基或苯基取代的C 1 -C 10烷基; R2是C2-C5亚烷基或（C1-C4烷氧基） - 取代C2-C5亚烷基; R 3是H或C 1 -C 4烷基; n至少为5; m为零或1。

    Synthesis of N-substituted oligomers
    8.
    发明授权
    Synthesis of N-substituted oligomers 失效
    N-取代的低聚物的合成

    公开(公告)号：US5977301A

    公开(公告)日：1999-11-02

    申请号：US485106

    申请日：1995-06-07

    申请人： Ronald N. Zuckerman ,  Janice M. Kerr ,  Stephen B. H. Kent ,  Walter H. Moos ,  Reyna J. Simon ,  Dane A. Goff

    发明人： Ronald N. Zuckerman ,  Janice M. Kerr ,  Stephen B. H. Kent ,  Walter H. Moos ,  Reyna J. Simon ,  Dane A. Goff

    IPC分类号： A61K38/00 ,  C07B61/00 ,  C07K1/04 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  C08G69/10

    CPC分类号： C40B50/14 ,  C07K1/04 ,  C07K1/047 ,  C07K14/001 ,  C07K7/06 ,  C07K7/08 ,  C08G69/10 ,  A61K38/00 ,  B01J2219/00497 ,  B01J2219/00596 ,  B01J2219/0072 ,  C07B2200/11 ,  C40B40/10

    摘要： A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two "sub-monomers" directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by --NH.sub.2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a resin-bound .alpha.-haloacetamide) with a sufficient amount of a second sub-monomer comprising an --NH.sub.2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability.

    摘要翻译： 用于合成N-取代的低聚物（例如聚（N-取代的甘氨酸）（本文称为多聚NSG））的固相方法用于获得低聚物，例如聚NSG可具有的潜在治疗兴趣的聚NSG 各种各样的侧链取代基。 每个N-取代的甘氨酸单体直接在固体支持物上由两个“亚单体”组装。 单体添加的每个循环由两个步骤组成：（1）用包含能通过-NH 2的亲核置换的离去基团（如卤代乙酸）的酰化剂酰化与载体结合的仲胺，和（2）引入 通过亲核取代离去基团的侧链，例如卤素（作为树脂结合的α-卤代乙酰胺）与足够量的包含-NH 2基团的第二亚单体如伯胺，烷氧基胺，氨基脲 酰基酰肼，肼基甲酸酯等。 重复酰化和置换的两个步骤循环，得到所需的低聚物。 使用本发明方法的自动化合成技术有效合成各种各样的低聚NSG使得这些寡聚物成为用于不同肽模拟文库的产生和快速筛选的有吸引力的候选者。 本文公开的本发明的低聚物，例如N-取代的甘氨酸（即多聚NSG）提供了一类新型的肽样化合物，它们在自然界中没有发现，但是它们是合成可及的，并且已被证明具有显着的生物活性和蛋白水解稳定性 。

    Hindered linking agents and methods
    9.
    发明授权
    Hindered linking agents and methods 失效
    受阻连接剂和方法

    公开(公告)号：US5183904A

    公开(公告)日：1993-02-02

    申请号：US796048

    申请日：1991-11-20

    申请人： Stephen F. Carroll ,  Dane A. Goff

    发明人： Stephen F. Carroll ,  Dane A. Goff

    IPC分类号： A61K47/48 ,  C07D333/36 ,  C07D333/50 ,  C07D333/66 ,  C07D409/04

    CPC分类号： C07D333/50 ,  A61K47/48715 ,  C07D333/36 ,  C07D333/66 ,  C07D409/04

    摘要： Novel compounds and methods for the formation of disulfide linkages are presented. The novel compounds employed are substituted 2-iminothiolane hydrohalide linking agents of the following formula (I): ##STR1## wherein, X is halogen;R.sub.1 is COOR.sub.5 ; halogen; nitro; unsubstituted or halogenated C.sub.1-8 alkyl; unsubstituted or halogenated C.sub.1-8 alkoxy; unsubstituted or halogenated C.sub.2-8 alkenyl; unsubstituted or halogenated C.sub.2-8 alkynyl; unsubstituted C.sub.3-8 cycloalkyl; unsubstituted aryl; aryl substituted with 1 to 3 substituents selected from halogen, amino, unsubstituted or halogenated C.sub.1-8 alkyl, or unsubstituted or halogenated C.sub.1-8 alkoxy; unsubstituted heterocycle; or heterocycle substituted with 1 to 3 substituents selected from amino, halogen, unsubstituted or halogenated C.sub.1-8 alkyl, or unsubstituted or halogenated C.sub.1-8 alkoxy;each of R.sub.2, R.sub.3 and R.sub.4 is independently hydrogen or selected from the values of R.sub.1 ; orR.sub.1 and R.sub.2 together form a C.sub.2-5 alkylene bridge, unsubstituted or substituted with one to five C.sub.1-4 alkyl groups; orR.sub.1 or R.sub.2 together with R.sub.3 form a C.sub.1-5 alkylene bridge, unsubstituted or substituted with one to five C.sub.1-4 alkyl groups; andR.sub.5 is hydrogen or C.sub.1-8 alkyl.Also included in the invention are methods for covalently linking two species, which methods comprise reacting one or both of the two species with a crosslinking agent of the above formula (I) and mixing the two species together. The resulting conjugated species containing the linking group are also included in the invention.Further included in the invention is the use of a quenching agent which allows direct measurement of the reaction of 2-iminothiolanes with nucleophilic groups.

    摘要翻译： 提出了新的化合物和形成二硫键的方法。 所用的新化合物是下式（I）的取代的2-亚氨基硫烷氢卤化物连接剂：其中X是卤素; R1为COOR5; 卤素; 硝基 未取代或卤代C 1-8烷基; 未取代或卤代C 1-8烷氧基; 未取代或卤代C 2-8烯基; 未取代或卤代C 2-8炔基; 未取代的C 3-8环烷基; 未取代的芳基; 被1至3个选自卤素，氨基，未取代或卤代C 1-8烷基的取代基取代的芳基，或未取代或卤代C 1-8烷氧基; 未取代的杂环; 或被1至3个选自氨基，卤素，未取代或卤代C 1-8烷基，或未取代或卤代C 1-8烷氧基取代的杂环; R 2，R 3和R 4各自独立地为氢或选自R 1的值; 或R 1和R 2一起形成未被取代或被一至五个C 1-4烷基取代的C 2-5亚烷基桥; 或R 1或R 2与R 3一起形成未被取代或被一至五个C 1-4烷基取代的C 1-5亚烷基桥; 并且R 5是氢或C 1-8烷基。 本发明还包括共价连接两种物质的方法，该方法包括使两种物质中的一种或两种与上式（I）的交联剂反应并将两种物质混合在一起。 所得到的含有连接基团的共轭物质也包括在本发明中。 进一步包括在本发明中的是使用猝灭剂，其允许直接测量2-亚氨基硫醇与亲核基团的反应。