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公开(公告)号:US08614253B2
公开(公告)日:2013-12-24
申请号:US12941530
申请日:2010-11-08
申请人: John Bruce Patterson , David Gregory Lonergan , Gary A. Flynn , Qingping Zeng , Peter V. Pallai
发明人: John Bruce Patterson , David Gregory Lonergan , Gary A. Flynn , Qingping Zeng , Peter V. Pallai
IPC分类号: A61K31/11
CPC分类号: C07C65/21 , A61K31/11 , A61K31/135 , A61K31/166 , A61K31/192 , A61K31/357 , A61K31/381 , A61K31/505 , A61K31/5375 , A61K31/5377 , C07C47/55 , C07C47/565 , C07C47/575 , C07C65/11 , C07C65/26 , C07C65/30 , C07C205/44 , C07C205/61 , C07C223/02 , C07C233/65 , C07C235/42 , C07C235/84 , C07C251/24 , C07C317/24 , C07C321/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/48 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D217/16 , C07D231/12 , C07D235/08 , C07D239/26 , C07D239/54 , C07D241/18 , C07D249/18 , C07D261/08 , C07D277/34 , C07D295/125 , C07D295/15 , C07D295/192 , C07D307/80 , C07D317/54 , C07D319/08 , C07D319/18 , C07D321/10 , C07D333/22 , C07D333/58 , C07D401/12 , C07D403/12 , C07D417/10 , Y02A50/389 , Y02A50/393
摘要: Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译: 在体外直接抑制IRE-1α活性的化合物,其前药和药学上可接受的盐。 这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病,并可用作单一药剂或联合疗法。
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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:US07858666B2
公开(公告)日:2010-12-28
申请号:US12135571
申请日:2008-06-09
CPC分类号: C07C65/21 , A61K31/11 , A61K31/135 , A61K31/166 , A61K31/192 , A61K31/357 , A61K31/381 , A61K31/505 , A61K31/5375 , A61K31/5377 , C07C47/55 , C07C47/565 , C07C47/575 , C07C65/11 , C07C65/26 , C07C65/30 , C07C205/44 , C07C205/61 , C07C223/02 , C07C233/65 , C07C235/42 , C07C235/84 , C07C251/24 , C07C317/24 , C07C321/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/48 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D217/16 , C07D231/12 , C07D235/08 , C07D239/26 , C07D239/54 , C07D241/18 , C07D249/18 , C07D261/08 , C07D277/34 , C07D295/125 , C07D295/15 , C07D295/192 , C07D307/80 , C07D317/54 , C07D319/08 , C07D319/18 , C07D321/10 , C07D333/22 , C07D333/58 , C07D401/12 , C07D403/12 , C07D417/10 , Y02A50/389 , Y02A50/393
摘要: Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译: 在体外直接抑制IRE-1α活性的化合物,其前药和药学上可接受的盐。 这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病,并可用作单一药剂或联合疗法。
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公开(公告)号:US20110065162A1
公开(公告)日:2011-03-17
申请号:US12941530
申请日:2010-11-08
IPC分类号: C12N9/99
CPC分类号: C07C65/21 , A61K31/11 , A61K31/135 , A61K31/166 , A61K31/192 , A61K31/357 , A61K31/381 , A61K31/505 , A61K31/5375 , A61K31/5377 , C07C47/55 , C07C47/565 , C07C47/575 , C07C65/11 , C07C65/26 , C07C65/30 , C07C205/44 , C07C205/61 , C07C223/02 , C07C233/65 , C07C235/42 , C07C235/84 , C07C251/24 , C07C317/24 , C07C321/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/48 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D217/16 , C07D231/12 , C07D235/08 , C07D239/26 , C07D239/54 , C07D241/18 , C07D249/18 , C07D261/08 , C07D277/34 , C07D295/125 , C07D295/15 , C07D295/192 , C07D307/80 , C07D317/54 , C07D319/08 , C07D319/18 , C07D321/10 , C07D333/22 , C07D333/58 , C07D401/12 , C07D403/12 , C07D417/10 , Y02A50/389 , Y02A50/393
摘要: Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译: 在体外直接抑制IRE-1α活性的化合物,其前药和药学上可接受的盐。 这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病,并可用作单一药剂或联合疗法。
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公开(公告)号:US20090186893A1
公开(公告)日:2009-07-23
申请号:US12135571
申请日:2008-06-09
IPC分类号: A61K31/5355 , C07D265/30 , C07D413/04 , A61K31/535 , A61P35/00
CPC分类号: C07C65/21 , A61K31/11 , A61K31/135 , A61K31/166 , A61K31/192 , A61K31/357 , A61K31/381 , A61K31/505 , A61K31/5375 , A61K31/5377 , C07C47/55 , C07C47/565 , C07C47/575 , C07C65/11 , C07C65/26 , C07C65/30 , C07C205/44 , C07C205/61 , C07C223/02 , C07C233/65 , C07C235/42 , C07C235/84 , C07C251/24 , C07C317/24 , C07C321/04 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/48 , C07D213/64 , C07D213/69 , C07D213/74 , C07D215/14 , C07D217/16 , C07D231/12 , C07D235/08 , C07D239/26 , C07D239/54 , C07D241/18 , C07D249/18 , C07D261/08 , C07D277/34 , C07D295/125 , C07D295/15 , C07D295/192 , C07D307/80 , C07D317/54 , C07D319/08 , C07D319/18 , C07D321/10 , C07D333/22 , C07D333/58 , C07D401/12 , C07D403/12 , C07D417/10 , Y02A50/389 , Y02A50/393
摘要: Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
摘要翻译: 在体外直接抑制IRE-1α活性的化合物,其前药和药学上可接受的盐。 这样的化合物和前药可用于治疗与未折叠的蛋白质应答相关的疾病,并可用作单一药剂或联合疗法。
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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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