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公开(公告)号：US20160347706A1
公开(公告)日：2016-12-01
申请号：US15232590
申请日：2016-08-09
发明人： John K. Lynch , Jeff Hutchison , Xiong Fu , Kevin Kunnen
IPC分类号： C07C227/16
CPC分类号： C07C227/16 , A61K31/365 , A61K47/64 , C07C227/02 , C07C227/18 , C07C229/08 , C07C269/04 , C07C269/06 , C07C271/22 , C07D307/93 , C07K5/06104 , C07K5/06113
摘要： Provided herein are methods of making the compound of Formula I: and certain intermediates involved in such process.
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公开(公告)号：US07767648B2
公开(公告)日：2010-08-03
申请号：US12323380
申请日：2008-11-25
IPC分类号： A61K38/07
CPC分类号： C07K5/06104 , A61K38/00 , A61K47/65 , C07K5/0819 , C07K5/1021 , C07K7/06 , G01N33/57434
摘要： The invention provides novel peptide prodrugs which contain cleavage sites specifically cleaved by prostate specific membrane antigen (PSMA). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. PSMA is secreted by prostatic glandular cells. Upon cleavage of the prodrug by PSMA, the therapeutic drugs are activated and exert their toxicity. Sesquiterpene-γ-lactones form part of the prodrugs, and are designed to be linked to carrier moieties such as the peptides of the invention. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由前列腺特异性膜抗原（PSMA）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 PSMA由前列腺细胞分泌。 通过PSMA裂解前药时，治疗药物被活化并发挥其毒性。 倍半萜-γ-内酯形成前药的一部分，并被设计为与载体部分如本发明的肽连接。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US07635682B2
公开(公告)日：2009-12-22
申请号：US11328491
申请日：2006-01-06
申请人： Samuel R. Denmeade , John T. Isaacs
发明人： Samuel R. Denmeade , John T. Isaacs
IPC分类号： A61K49/00
CPC分类号： A61K38/08 , A61K38/168 , A61K47/65 , C07K7/06
摘要： The instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1);Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the drug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions.
摘要翻译： 本发明提供包含前药的组合物，前药包含治疗活性药物; 和选自以下序列的肽：Ser-Ser-Lys-Tyr-Gln（SEQ ID NO：1）; Gly-Lys-Ser-Gln-Tyr-Gln（SEQ ID NO：2）; 和Gly-Ser-Ala-Lys-Tyr-Gln（SEQ ID NO：3），其中所述肽与治疗活性药物连接以抑制药物的治疗活性，并且其中治疗活性药物从肽切割 通过具有前列腺特异性抗原（PSA）的蛋白水解活性的酶进行蛋白水解。 本发明还提供制备和使用所要求保护的组合物的方法。
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公开(公告)号：US20090163426A1
公开(公告)日：2009-06-25
申请号：US12323380
申请日：2008-11-25
CPC分类号： C07K5/06104 , A61K38/00 , A61K47/65 , C07K5/0819 , C07K5/1021 , C07K7/06 , G01N33/57434
摘要： The invention provides novel peptide prodrugs which contain cleavage sites specifically cleaved by prostate specific membrane antigen (PSMA). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. PSMA is secreted by prostatic glandular cells. Upon cleavage of the prodrug by PSMA, the therapeutic drugs are activated and exert their toxicity. Sesquiterpene-γ-lactones form part of the prodrugs, and are designed to be linked to carrier moieties such as the peptides of the invention. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由前列腺特异性膜抗原（PSMA）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 PSMA由前列腺细胞分泌。 通过PSMA裂解前药时，治疗药物被活化并发挥其毒性。 倍半萜-γ-内酯形成前药的一部分，并被设计为与载体部分例如本发明的肽连接。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US08822406B2
公开(公告)日：2014-09-02
申请号：US13484795
申请日：2012-05-31
申请人： Samuel R. Denmeade , John T. Isaacs
发明人： Samuel R. Denmeade , John T. Isaacs
CPC分类号： A61K38/08 , A61K38/168 , A61K47/65 , C07K7/06
摘要： The instant invention provides compositions comprising a prodrug, the prodrug comprising a therapeutically active drug; and a peptide selected from the group consisting of the sequences: Ser-Ser-Lys-Tyr-Gln (SEQ ID NO:1); Gly-Lys-Ser-Gln-Tyr-Gln (SEQ ID NO:2); and Gly-Ser-Ala-Lys-Tyr-Gln (SEQ ID NO:3) wherein the peptide is linked to the therapeutically active drug to inhibit the therapeutic activity of the drug, and wherein the therapeutically active drug is cleaved from the peptide upon proteolysis by an enzyme having a proteolytic activity of prostate specific antigen (PSA). The invention further provides methods of making and using the claimed compositions.
摘要翻译： 本发明提供包含前药的组合物，前药包含治疗活性药物; 和选自以下序列的肽：Ser-Ser-Lys-Tyr-Gln（SEQ ID NO：1）; Gly-Lys-Ser-Gln-Tyr-Gln（SEQ ID NO：2）; 和Gly-Ser-Ala-Lys-Tyr-Gln（SEQ ID NO：3），其中所述肽与治疗活性药物连接以抑制药物的治疗活性，并且其中治疗活性药物从肽切割 通过具有前列腺特异性抗原（PSA）的蛋白水解活性的酶进行蛋白水解。 本发明还提供制备和使用所要求保护的组合物的方法。
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公开(公告)号：US08669231B2
公开(公告)日：2014-03-11
申请号：US12987409
申请日：2011-01-10
申请人： Samuel R. Denmeade , John Tod Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John Tod Isaacs , Hans Lilja
CPC分类号： C07K14/4748 , A61K38/00 , A61K47/62 , C07K7/06 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由人激肽释放酶2（hK2）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 当通过hK2裂解前体药物时，治疗药物被活化并发挥其毒性。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US07468354B2
公开(公告)日：2008-12-23
申请号：US10432849
申请日：2001-11-30
申请人： John T. Isaacs , Samuel R. Denmeade
发明人： John T. Isaacs , Samuel R. Denmeade
IPC分类号： A61K38/07
CPC分类号： C07K5/06104 , A61K38/00 , A61K47/65 , C07K5/0819 , C07K5/1021 , C07K7/06 , G01N33/57434
摘要： The invention provides novel peptide prodrugs which contain cleavage sites specifically cleaved by prostate specific membrane antigen (PSMA). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. PSMA is secreted by prostatic glandular cells. Upon cleavage of the prodrug by PSMA, the therapeutic drug are activated and exert their toxicity. Sesquiterpene-γ-lactones form part of the prodrugs, and are designed to be linked to carrier moieties such as the peptides of the invention. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由前列腺特异性膜抗原（PSMA）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 PSMA由前列腺细胞分泌。 在通过PSMA切割前药时，治疗药物被活化并发挥其毒性。 倍半萜-γ-内酯形成前药的一部分，并被设计为与载体部分例如本发明的肽连接。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US20160030589A1
公开(公告)日：2016-02-04
申请号：US14776730
申请日：2014-03-14
申请人： GENSPERA, INC.
发明人： John K Lynch , Jeff Hutchison , Xiong Fu , Kevin Kunnen
IPC分类号： A61K47/48 , C07C269/06 , C07C229/08 , C07C269/04 , A61K31/365 , C07C271/22 , C07C227/02 , C07K5/072 , C07D307/93
CPC分类号： C07C227/16 , A61K31/365 , A61K47/64 , C07C227/02 , C07C227/18 , C07C229/08 , C07C269/04 , C07C269/06 , C07C271/22 , C07D307/93 , C07K5/06104 , C07K5/06113
摘要： Provided is a method for making the compound of Formula 1: Various compounds utilized in that method are also provided, as are methods of making those compounds. Also provided is a compound having the formula XO—CO—(CH2)nNH2, where n is an integer greater than 2. A method of making that compound is additionally provided. Further provided is a method of making a prodrug of a bioactive compound.
摘要翻译： 提供制备式1化合物的方法：也提供了在该方法中使用的各种化合物，以及制备这些化合物的方法。 还提供了具有式XO-CO-（CH 2）n NH 2的化合物，其中n是大于2的整数。另外提供了制备该化合物的方法。 还提供了制备生物活性化合物的前体药物的方法。
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公开(公告)号：US07906477B2
公开(公告)日：2011-03-15
申请号：US10535351
申请日：2003-11-18
申请人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
CPC分类号： C07K14/4748 , A61K38/00 , A61K47/62 , C07K7/06 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由人激肽释放酶2（hK2）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 当通过hK2裂解前体药物时，治疗药物被活化并发挥其毒性。 治疗细胞增殖性疾病的方法也在本发明中。
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公开(公告)号：US20080247950A1
公开(公告)日：2008-10-09
申请号：US11725135
申请日：2007-03-15
申请人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
发明人： Samuel R. Denmeade , John T. Isaacs , Hans Lilja
IPC分类号： A61K49/00 , C07K7/06 , C07K7/08 , C07K5/00 , C07K9/00 , C07K16/00 , C07H21/00 , A61P35/00 , A61K47/42 , A61K31/343 , A61K31/7052 , A61K31/704 , C12Q1/02
CPC分类号： C12N9/6445 , A61K47/65 , C07K7/06 , C07K14/47
摘要： The invention provides novel peptide prodrugs that contain cleavage sites specifically cleaved by human kallikrein 2 (hK2). These prodrugs are useful for substantially inhibiting the non-specific toxicity of a variety of therapeutic drugs. Upon cleavage of the prodrug by hK2, the therapeutic drugs are activated and exert their toxicity. Methods for treating cell proliferative disorders are also featured in the invention.
摘要翻译： 本发明提供新的肽前体药物，其含有由人激肽释放酶2（hK2）特异性切割的切割位点。 这些前药可用于基本上抑制各种治疗药物的非特异性毒性。 当通过hK2裂解前体药物时，治疗药物被活化并发挥其毒性。 治疗细胞增殖性疾病的方法也在本发明中。
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