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公开(公告)号:US5677343A
公开(公告)日:1997-10-14
申请号:US467725
申请日:1995-06-06
申请人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
发明人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
IPC分类号: A61K31/795 , A61P31/12 , A61P31/18 , A61K31/185 , C07C309/32 , C07C309/35
CPC分类号: A61K31/795
摘要: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalene-sulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.
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公开(公告)号:US5614559A
公开(公告)日:1997-03-25
申请号:US245619
申请日:1994-05-19
申请人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
发明人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
IPC分类号: A61K31/795 , A61P31/12 , A61P31/18 , A61K31/185 , C07C309/32 , C07C309/35
CPC分类号: A61K31/795
摘要: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalene-sulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.
摘要翻译: 本发明涉及如下发现:如在CD4 / gp120结合测定中所证明的,醛和芳族磺酸的缩合聚合物及其部分如甲醛萘磺酸缩合聚合物可以消除结合CD4的HIV gp120。 除了gp120结合抑制之外,已经显示这些化合物抑制HIV诱导的合胞体形成和CD +细胞的感染性。 这种化合物的使用已被证明是非细胞毒性的,并且对抗原诱导的T淋巴细胞增殖是不抑制的。 基于这些发现,这些化合物可用作治疗获得性免疫缺陷综合征(AIDS)以及艾滋病相关综合征(ARC),AIDS相关性痴呆和无症状性艾滋病毒感染的治疗剂。 该化合物也可用于治疗血液制剂。
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公开(公告)号:US06365625B1
公开(公告)日:2002-04-02
申请号:US09398571
申请日:1999-09-17
申请人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
发明人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
IPC分类号: A61K31185
CPC分类号: A61K31/795
摘要: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.
摘要翻译: 本发明涉及如下发现:如在CD4 / gp120结合测定中所证明的,醛和芳族磺酸的缩合聚合物及其部分如甲醛萘磺酸缩聚物可以消除结合CD4的HIV gp120。 除了gp120结合抑制之外,已经显示这些化合物抑制HIV诱导的合胞体形成和CD +细胞的感染性。 这种化合物的使用已被证明是非细胞毒性的,并且对抗原诱导的T淋巴细胞增殖是不抑制的。 基于这些发现,这些化合物可用作治疗获得性免疫缺陷综合征(AIDS)以及艾滋病相关综合征(ARC),AIDS相关性痴呆和无症状性艾滋病毒感染的治疗剂。 该化合物也可用于治疗血液制剂。
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公开(公告)号:US6075050A
公开(公告)日:2000-06-13
申请号:US467728
申请日:1995-06-06
申请人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
发明人: Shyam K. Singh , Raymond J. Patch , Peter V. Pallai , Edith A. Neidhardt , Gerard P. Palace , Kevin J. Willis , Theresa M. Sampo , Kevin W. McDonald , Zhan Shi
IPC分类号: A61K31/795 , A61P31/12 , A61P31/18 , A61K31/185 , C07C309/32 , C07C309/35
CPC分类号: A61K31/795
摘要: This invention pertains to the discovery that condensation polymers of an aldehyde and aromatic sulfonic acids and fractions thereof, such as formaldehyde naphthalenesulfonic acid condensation polymers, can abrogate HIV gp120 binding to CD4, as demonstrated in CD4/gp120 binding assays. In addition to gp120 binding inhibition, the compounds have been shown to inhibit HIV-induced syncytia formation and infectivity of CD+ cells. The use of this compound has been shown to be non-cytotoxic and non-inhibitory to antigen induced T lymphocyte proliferation. Based on these findings, these compounds can be used as a therapeutic agent for the treatment of acquired immunodeficiency syndrome (AIDS), as well as AIDS-related complex (ARC), AIDS-related dementia and non-symptomatic HIV infection. The compounds can also be used to treat blood preparations.
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公开(公告)号:US5739169A
公开(公告)日:1998-04-14
申请号:US656468
申请日:1996-05-31
IPC分类号: C07C229/58 , C07C233/43 , C07D257/04 , A61K31/135 , A01N33/02 , C07C229/00
CPC分类号: C07D257/04 , C07C229/58 , C07C233/43
摘要: Novel compounds ##STR1## wherein R.sup.1 to R.sup.13 are independently selected from C.sub.2 -C.sub.4 linear and branched alkyls, H, NH.sub.2, CH.sub.3, OR.sup.14, fluorine, chlorine, iodine, NO.sub.2, CF.sub.3, NHCOCH.sub.3, NHCOOtBu, NHR.sup.15, NR.sup.16 R.sup.17 and phenyl, for use as immunosuppressive agents to prevent or significantly reduce graft rejection in organ and bone marrow transplantation are described. The novel compounds can also be used as an immunosuppressant drug for T-lymphocyte mediated autoimmune diseases, such as diabetes, and may be useful in alleviating psoriasis and contact dermatitis. Additionally, the novel compounds can be used for antiproliferation and gene therapy.
摘要翻译: 其中R 1至R 13独立地选自C 2 -C 4直链和支链烷基,H,NH 2,CH 3,OR 14,氟,氯,碘,NO 2,CF 3,NHCOCH 3,NHCOOtBu,NHR 15,NR 16 R 17和苯基, 用作免疫抑制剂以预防或显着降低器官和骨髓移植中的移植物排斥。 新型化合物也可用作T淋巴细胞介导的自身免疫性疾病如糖尿病的免疫抑制药物,可用于缓解牛皮癣和接触性皮炎。 另外,新型化合物可用于抗增殖和基因治疗。
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