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    Immunomodulation with novel pharmaceutical compositions
    1.
    发明授权
    Immunomodulation with novel pharmaceutical compositions 失效
    用新型药物组合物进行免疫调节

    公开(公告)号：US06919483B2

    公开(公告)日：2005-07-19

    申请号：US10443743

    申请日：2003-05-23

    申请人： Mark R. Burns ,  Maralee McVean ,  Kevin J. Kennedy ,  Arthur Yeung ,  Bruce H. Devens

    发明人： Mark R. Burns ,  Maralee McVean ,  Kevin J. Kennedy ,  Arthur Yeung ,  Bruce H. Devens

    IPC分类号： A61K31/13 ,  A61K31/137 ,  A61K31/40 ,  A61K31/445 ,  C07C211/13 ,  C07C211/16 ,  C07C211/30 ,  C07C211/57

    CPC分类号： C07C211/30 ,  C07D215/12 ,  C07D217/14 ,  C07D307/52 ,  C07D333/20

    摘要： The synthesis and use of a novel class of tumor necrosis factor (TNFα) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNFα and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNFα and/or one or more other involved cytokines, alone or in combination with other agents. Examples of compounds of the present invention are those having the structures as shown below: wherein, a, b and c may be the same or different and are integers from 0 to 12, X equals NH or CHNH2, R1 and R2 can be the same or different and equal to a hydrogen or a straight or branched C1 to C20 saturated or unsaturated aliphatic; aliphatic amine; an alicyclic; single or multi-ring aromatic; a single or multi-ring aromatic heterocycle; a single or multi-ring saturated heterocycle and the halogenated forms thereof; and wherein, a, b and c may be the same or different and are integers from 0 to 12; R1, R2, R3, and R4 can be the same or different and equal to a hydrogen or a straight or branched C1 to C20 saturated or unsaturated aliphatic; aliphatic amine; an alicyclic; single or multi-ring aromatic; a single or multi-ring aromatic heterocycle; a single or multi-ring saturated heterocycle and the halogenated forms thereof.

    摘要翻译： 提供新型肿瘤坏死因子（TNFalpha）抑制剂和免疫调节剂的合成和使用。 这些化合物具有药理学应用以及与TNFα和其他涉及细胞因子相关的测定中的应用。 作为药物，这些化合物用于单独或与其它药剂组合治疗与TNFα和/或一种或多种其它涉及的细胞因子的不期望的存在或活性有关的炎性，感染性，自身免疫性或其它增殖性疾病和病症。 本发明化合物的实例是具有以下结构的那些：其中a，b和c可以相同或不同，为0-12的整数，X等于NH或CHNH 2 R 1和R 2可以相同或不同，并且等于氢或直链或支链C 1至C 1 - 20个饱和或不饱和脂肪族; 脂肪胺; 脂环族 单环或多环芳香族; 单环或多环芳族杂环; 单环或多环饱和杂环及其卤化形式; 并且其中a，b和c可以相同或不同，为0至12的整数; R 1，R 2，R 3和R 4可以相同或不同，并且等于 氢或直链或支链C 1至C 20饱和或不饱和脂族基; 脂肪胺; 脂环族 单环或多环芳香族; 单环或多环芳族杂环; 单环或多环饱和杂环及其卤化形式。

    Immunomodulation with novel pharmaceutical compositions
    2.
    发明授权
    Immunomodulation with novel pharmaceutical compositions 失效
    用新型药物组合物进行免疫调节

    公开(公告)号：US07388112B2

    公开(公告)日：2008-06-17

    申请号：US11171228

    申请日：2005-07-01

    申请人： Mark R. Burns ,  Maralee McVean ,  Kevin Kennedy ,  Arthur Yeung ,  Bruce H. Devens

    发明人： Mark R. Burns ,  Maralee McVean ,  Kevin Kennedy ,  Arthur Yeung ,  Bruce H. Devens

    IPC分类号： C07C211/13 ,  A61K31/13 ,  A61K31/40 ,  A61K31/445

    CPC分类号： C07C211/30 ,  C07D215/12 ,  C07D217/14 ,  C07D307/52 ,  C07D333/20

    摘要： The synthesis and use of a novel class of tumor necrosis factor (TNFα) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CHNH2, R1 and R2 each is a hydrogen or a C1 to C20 aliphatic; aliphatic amine; an alicyclic; aromatic; heterocycle; and halogenated forms thereof; and wherein, a, b and c are integers from 0 to 12; R1, R2, R3, and R4 each is a hydrogen or a C1 to C20; aliphatic amine; an alicyclic; aromatic; a heterocycle; and halogenated forms thereof.

    摘要翻译： 提供新型肿瘤坏死因子（TNFalpha）抑制剂和免疫调节剂的合成和使用。 实例是具有以下结构的那些：其中a，b和c是0至12的整数，X等于NH或CHNH 2，R 1和R 2， / SUB>各自为氢或C 1至C 20脂族基; 脂肪胺; 脂环族 芳香; 杂环 及其卤化形式; 并且其中a，b和c为0-12的整数; R 1，R 2，R 3和R 4各自为氢或C 1 -C 4烷基， 1至C 20; 脂肪胺; 脂环族 芳香; 杂环 及其卤化形式。

    Composition containing polyamine transport inhibitor and use thereof
    7.
    发明授权
    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：US07432302B2

    公开(公告)日：2008-10-07

    申请号：US11062481

    申请日：2005-02-23

    申请人： Mark R. Burns ,  Gerard F. Graminski ,  Nand Baindur ,  Reitha S. Weeks

    发明人： Mark R. Burns ,  Gerard F. Graminski ,  Nand Baindur ,  Reitha S. Weeks

    IPC分类号： A61K31/65

    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。