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1. 发明授权

US09181224B2 Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus 有权
标题翻译：具有针对人类免疫缺陷病毒的抗体募集和进入抑制活性的双功能分子
公开(公告)号：US09181224B2
公开(公告)日：2015-11-10
申请号：US13501592
申请日：2010-10-12
申请人： David Spiegel , Christopher Parker
发明人： David Spiegel , Christopher Parker
IPC分类号： A61K38/08 , A61P31/18 , C07D403/12 , A61K31/4745 , A61K45/06 , A61K47/48 , B82Y5/00 , C07D405/04 , C07D405/14 , C07D471/04
CPC分类号： A61K39/385 , A61K9/0019 , A61K9/0053 , A61K31/4745 , A61K45/06 , A61K47/545 , A61K47/6897 , A61K2039/54 , A61K2039/57 , A61K2039/58 , A61K2039/6012 , A61K2039/627 , B82Y5/00 , C07D403/12 , C07D405/04 , C07D405/14 , C07D471/04 , A61K2300/00
摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H′ function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
摘要翻译：本发明涉及新的双功能化合物和用于治疗HIV感染的方法。通过抑制gp120-CD4相互作用，通过募集抗gP120表达细胞的抗DNP抗体，通过正交途径通常称为ARM-H'功能的双官能小分子，从而防止细胞感染和HIV传播。已经表明，ARM-H与gp120和gp-120表达细胞结合，与CD4竞争性，从而降低病毒感染性，如MT-2细胞测定所示，通过募集抗DNP抗体导致形成三元复合物的结合与其结合，存在于三元复合物中的抗体促进表达gp120的细胞的补体依赖性破坏。本文描述了化合物和方法。

2. 发明申请

US20130245040A1 BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS 有权
标题翻译：具有抗人体免疫反应和入侵抑制活性的人类免疫缺陷病毒的双功能分子
公开(公告)号：US20130245040A1
公开(公告)日：2013-09-19
申请号：US13988251
申请日：2011-11-17
申请人： David Spiegel , Christopher Parker
发明人： David Spiegel , Christopher Parker
IPC分类号： C07D405/14 , A61K45/06 , A61K31/496
CPC分类号： C07D405/14 , A61K9/0014 , A61K31/496 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
摘要翻译：本发明涉及新的双功能化合物和用于治疗HIV感染的方法。通常称为ARM-HI的双功能小分子通过正交途径，通过抑制gp120-CD4相互作用和通过向表达gp120的细胞募集抗DNP抗体，从而防止细胞感染和HIV扩散而起作用。已经表明，ARM-HI与gp120和gp-120表达细胞的结合与CD4竞争性，从而降低病毒感染性，如MT-2细胞测定所示，通过募集抗DNP抗体导致形成三元复合物的结合与其结合，存在于三元复合物中的抗体促进表达gp120的细胞的补体依赖性破坏。本文描述了化合物和方法。

3. 发明授权

US09562038B2 Bifunctional molecules with antibody-recruiting and entry inhibitory activity against the human immunodeficiency virus 有权
标题翻译：具有针对人类免疫缺陷病毒的抗体募集和进入抑制活性的双功能分子
公开(公告)号：US09562038B2
公开(公告)日：2017-02-07
申请号：US13988251
申请日：2011-11-17
申请人： David Spiegel , Christopher Parker
发明人： David Spiegel , Christopher Parker
IPC分类号： C07D405/14 , A61K31/496 , A61K45/06
CPC分类号： C07D405/14 , A61K9/0014 , A61K31/496 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
摘要翻译：本发明涉及新的双功能化合物和用于治疗HIV感染的方法。通常称为ARM-HI的双功能小分子通过正交途径，通过抑制gp120-CD4相互作用和通过向表达gp120的细胞募集抗DNP抗体，从而防止细胞感染和HIV扩散而起作用。已经表明，ARM-HI与gp120和gp-120表达细胞的结合与CD4竞争性，从而降低病毒感染性，如MT-2细胞测定所示，通过募集抗DNP抗体导致形成三元复合物的结合与其结合，存在于三元复合物中的抗体促进表达gp120的细胞的补体依赖性破坏。本文描述了化合物和方法。

4. 发明申请

US20120269766A1 BIFUNCTIONAL MOLECULES WITH ANTIBODY-RECRUITING AND ENTRY INHIBITORY ACTIVITY AGAINST THE HUMAN IMMUNODEFICIENCY VIRUS 有权
标题翻译：具有抗人体免疫反应和入侵抑制活性的人类免疫缺陷病毒的双功能分子
公开(公告)号：US20120269766A1
公开(公告)日：2012-10-25
申请号：US13501592
申请日：2010-10-12
申请人： David Spiegel , Christopher Parker
发明人： David Spiegel , Christopher Parker
IPC分类号： C07D471/04 , C07H15/26 , A61K31/496 , A61K31/706 , A61K38/21 , A61P31/18 , A61K38/08 , A61K38/19 , A61K38/20 , A61K39/395 , A61K31/568 , C07D405/14 , A61K39/42
CPC分类号： A61K39/385 , A61K9/0019 , A61K9/0053 , A61K31/4745 , A61K45/06 , A61K47/545 , A61K47/6897 , A61K2039/54 , A61K2039/57 , A61K2039/58 , A61K2039/6012 , A61K2039/627 , B82Y5/00 , C07D403/12 , C07D405/04 , C07D405/14 , C07D471/04 , A61K2300/00
摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-H′ function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-H's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.
摘要翻译：本发明涉及新的双功能化合物和用于治疗HIV感染的方法。通过抑制gp120-CD4相互作用，通过募集抗gP120表达细胞的抗DNP抗体，通过正交途径通常称为ARM-H'功能的双官能小分子，从而防止细胞感染和HIV传播。已经表明，ARM-H与gp120和gp-120表达细胞结合，与CD4竞争性，从而降低病毒感染性，如MT-2细胞测定所示，通过募集抗DNP抗体导致形成三元复合物的结合与其结合，存在于三元复合物中的抗体促进表达gp120的细胞的补体依赖性破坏。本文描述了化合物和方法。

5. 发明授权

US09622469B2 Crosslink breakers for preservation of biological substances 有权
公开(公告)号：US09622469B2
公开(公告)日：2017-04-18
申请号：US14505992
申请日：2014-10-03
申请人： David Spiegel , Jeanne Hendrickson
发明人： David Spiegel , Jeanne Hendrickson
IPC分类号： A01N1/02
CPC分类号： A01N1/0226
摘要： A preservative for body fluids, proteins, cells and tissues comprising an effective amount of an AGE crosslink breaker for preventing formation of advanced glycation end products. The AGE crosslink breaker comprises a compound of Structure (1): wherein V, W, X, Y and Z are any atom suitable for a heterocyclic carbene or carbene precursor framework, including B, C, O, N, S, Se, P, and As in any chemically-feasible oxidation state; wherein Q, R, M, T and U are any atom or substituent, including but not limited to, H, CLn, NLn, PLn, OLn, SLn, SeLn, LnCl, LnBr, LnI, wherein L is any atom, substituent or group, and n is any integer such that Q, R, M, T, and U can access all chemically-feasible oxidation states; and wherein G comprises any charged counter ion including, but not limited to those derived from C, O, N, B, Al, S, Se, Cl, Br, I in any chemically-feasible oxidation state.

6. 发明申请

US20150099260A1 Crosslink Breakers for Preservation of Biological Substances 审中-公开
标题翻译：用于保存生物物质的交联断路器
公开(公告)号：US20150099260A1
公开(公告)日：2015-04-09
申请号：US14505992
申请日：2014-10-03
申请人： David Spiegel , Jeanne Hendrickson
发明人： David Spiegel , Jeanne Hendrickson
IPC分类号： A01N1/02
CPC分类号： A01N1/0226
摘要： A preservative for body fluids, proteins, cells and tissues comprising an effective amount of an AGE crosslink breaker for preventing formation of advanced glycation end products. The AGE crosslink breaker comprises a compound of Structure (1): wherein V, W, X, Y and Z are any atom suitable for a heterocyclic carbene or carbene precursor framework, including B, C, O, N, S, Se, P, and As in any chemically-feasible oxidation state; wherein Q, R, M, T and U are any atom or substituent, including but not limited to, H, CLn, NLn, PLn, OLn, SLn, SeLn, LnCl, LnBr, LnI, wherein L is any atom, substituent or group, and n is any integer such that Q, R, M, T, and U can access all chemically-feasible oxidation states; and wherein G comprises any charged counter ion including, but not limited to those derived from C, O, N, B, Al, S, Se, Cl, Br, I in any chemically-feasible oxidation state.
摘要翻译：一种用于体液，蛋白质，细胞和组织的防腐剂，其包含有效量的用于防止晚期糖基化终产物形成的AGE交联断裂剂。 AGE交联剂包括结构（1）的化合物：其中V，W，X，Y和Z是适用于杂环卡宾或卡宾前体骨架的任何原子，包括B，C，O，N，S，Se，P ，和在任何化学上可行的氧化态; 其中Q，R，M，T和U是任何原子或取代基，包括但不限于H，Cln，NLn，PLn，OLn，SLn，SeLn，LnCl，LnBr，LnI，其中L是任何原子，组，n是任何整数，使得Q，R，M，T和U可以访问所有化学上可行的氧化态; 并且其中G包括任何带电荷的对离子，包括但不限于在任何化学上可行的氧化态中衍生自C，O，N，B，Al，S，Se，Cl，Br，I的那些。

7. 发明申请

US20120034295A1 CHIMERIC SMALL MOLECULES FOR THE RECRUITMENT OF ANTIBODIES TO CANCER CELLS 有权
标题翻译：用于诱导癌细胞的抗体的CHIMERIC小分子
公开(公告)号：US20120034295A1
公开(公告)日：2012-02-09
申请号：US13173480
申请日：2011-06-30
申请人： David Spiegel , Ryan Murelli , Andrew Zhang
发明人： David Spiegel , Ryan Murelli , Andrew Zhang
IPC分类号： A61K9/127
CPC分类号： C07K16/44 , A61K9/0019 , A61K31/4192 , A61K45/06 , A61K47/48023 , A61K47/48092 , A61K47/481 , A61K47/4833 , A61K47/48653 , A61K47/48723 , A61K47/54 , A61K47/549 , A61K47/55 , A61K47/646 , A61K47/68 , A61K47/6803 , A61K47/6869 , A61K47/6873 , A61K47/6891 , C07D249/04 , C07K16/3069 , C07K2317/31
摘要： The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
摘要翻译：本发明涉及用于向癌细胞，特别是前列腺癌细胞或转移前列腺癌细胞募集抗体的嵌合化合物。根据本发明的化合物包含通过接头和任选的连接体分子共价键合到细胞结合末端（CBT）的抗体结合末端（ABT）部分。

8. 发明授权

US08852630B2 Chimeric small molecules for the recruitment of antibodies to cancer cells 有权
公开(公告)号：US08852630B2
公开(公告)日：2014-10-07
申请号：US13173480
申请日：2011-06-30
申请人： David Spiegel , Ryan Murelli , Andrew Zhang
发明人： David Spiegel , Ryan Murelli , Andrew Zhang
IPC分类号： A61K9/127
CPC分类号： C07K16/44 , A61K9/0019 , A61K31/4192 , A61K45/06 , A61K47/48023 , A61K47/48092 , A61K47/481 , A61K47/4833 , A61K47/48653 , A61K47/48723 , A61K47/54 , A61K47/549 , A61K47/55 , A61K47/646 , A61K47/68 , A61K47/6803 , A61K47/6869 , A61K47/6873 , A61K47/6891 , C07D249/04 , C07K16/3069 , C07K2317/31
摘要： The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.

9. 发明授权

US08859509B2 Chimeric small molecules for the recruitment of antibodies to cancer cells 有权
标题翻译：用于募集癌细胞抗体的嵌合小分子
公开(公告)号：US08859509B2
公开(公告)日：2014-10-14
申请号：US12991926
申请日：2009-05-13
申请人： David Spiegel , Ryan Murelli , Andrew Zhang
发明人： David Spiegel , Ryan Murelli , Andrew Zhang
IPC分类号： A61K31/702 , A61K31/675 , A61K31/66 , A61K31/4192 , A61K31/195 , C07H99/00 , A61K47/48 , C07K16/44 , A61K39/00
CPC分类号： C07K16/44 , A61K47/54 , A61K47/549 , A61K47/55 , A61K47/555 , A61K47/646 , A61K2039/505
摘要： The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
摘要翻译：本发明涉及用于向癌细胞，特别是前列腺癌细胞或转移前列腺癌细胞募集抗体的嵌合化合物。根据本发明的化合物包含通过接头和任选的连接体分子共价键合到细胞结合末端（CBT）的抗体结合末端（ABT）部分。

10. 发明申请

US20110201563A1 CHIMERIC SMALL MOLECULES FOR THE RECRUITMENT OF ANTIBODIES TO CANCER CELLS 有权
标题翻译：用于诱导癌细胞的抗体的CHIMERIC小分子
公开(公告)号：US20110201563A1
公开(公告)日：2011-08-18
申请号：US12991926
申请日：2009-05-13
申请人： David Spiegel , Ryan Murelli , Andrew Zhang
发明人： David Spiegel , Ryan Murelli , Andrew Zhang
IPC分类号： A61K31/702 , A61K31/675 , A61K31/66 , A61K31/4192 , A61K31/195 , C07H99/00 , C07F9/28 , C07D249/04 , C07C321/00 , C07D403/14 , A61P35/02 , A61P35/00
CPC分类号： C07K16/44 , A61K47/54 , A61K47/549 , A61K47/55 , A61K47/555 , A61K47/646 , A61K2039/505
摘要： The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.
摘要翻译：本发明涉及用于向癌细胞，特别是前列腺癌细胞或转移前列腺癌细胞募集抗体的嵌合化合物。根据本发明的化合物包含通过接头和任选的连接体分子共价键合到细胞结合末端（CBT）的抗体结合末端（ABT）部分。

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