-
公开(公告)号:US20070135346A1
公开(公告)日:2007-06-14
申请号:US11649822
申请日:2007-01-05
申请人: Robert Zhao , Ravi Chari
发明人: Robert Zhao , Ravi Chari
IPC分类号: A61K31/496 , A61K31/4545 , A61K38/16 , C07K14/00 , C07D403/14
CPC分类号: C07D307/85 , A61K31/407 , A61K31/4545 , A61K31/495 , A61K31/496 , A61K31/675 , A61K47/545 , A61K47/548 , A61K47/60 , C07D209/42 , C07D209/60 , C07D403/14 , C07D405/12 , C07F9/5728 , C07F9/65583 , Y02A50/423 , Y02A50/491 , Y02P20/55
摘要: Prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group such as a piperazino carbamate, a 4-piperidino-piperidino carbamate or a phosphate, in which the protecting group confers enhanced water solubility and stability upon the prodrug, and in which the prodrug also has a moiety, such as a disulfide, that can conjugate to a cell binding reagent such as an antibody. The therapeutic use of such prodrug conjugates is also described; such prodrugs of cytotoxic agents have therapeutic use because they can deliver cytotoxic prodrugs to a specific cell population for enzymatic conversion to cytoxic drugs in a targeted fashion.
摘要翻译: 具有可切割保护基的抗肿瘤抗生素CC-1065类似物的前药,例如哌嗪基氨基甲酸酯,4-哌啶子基 - 哌啶子基氨基甲酸酯或磷酸酯,其中保护基团赋予增强的水溶性和在前药上的稳定性, 其中前药还具有可与细胞结合试剂例如抗体缀合的部分,例如二硫化物。 还描述了这种前药缀合物的治疗用途; 这种细胞毒性药物的前药具有治疗用途,因为它们可以将细胞毒性前体药物递送至特定细胞群体,以靶向方式酶促转化为细胞毒性药物。
-
公开(公告)号:US08426402B2
公开(公告)日:2013-04-23
申请号:US12700131
申请日:2010-02-04
申请人: Wei Li , Nathan Fishkin , Robert Zhao , Michael Miller , Ravi Chari
发明人: Wei Li , Nathan Fishkin , Robert Zhao , Michael Miller , Ravi Chari
IPC分类号: C07D519/00 , A61K31/5517 , A61K31/55 , A61P35/00
CPC分类号: C07K16/2896 , A61K31/5517 , A61K38/07 , A61K45/06 , A61K47/60 , A61K47/6835 , A61K47/6849 , A61K47/6863 , A61P35/00 , C07D487/04 , C07D498/04 , C07D519/00 , C07K5/0202 , C07K5/1008 , C07K16/2803 , C07K16/46 , C07K19/00
摘要: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译: 本发明涉及具有抗增殖活性的新型苯并二氮杂衍生物,更具体地涉及式(I)和(II)的新型苯并二氮杂,其中二氮杂环(B)与杂环(CD)稠合,其中杂环是双环的 或其中二氮杂环(B)与杂环(C)稠合的式(III)化合物,其中杂环是单环的。 本发明提供这些化合物的细胞毒二聚体。 本发明还提供了单体和二聚体的共轭物。 本发明还提供了使用本发明的化合物或缀合物来抑制哺乳动物异常细胞生长或治疗增殖性病症的组合物和方法。 本发明还涉及将化合物或缀合物用于体外,原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。
-
公开(公告)号:US20100203007A1
公开(公告)日:2010-08-12
申请号:US12700131
申请日:2010-02-04
申请人: Wei Li , Nathan Fishkin , Robert Zhao , Michael Miller , Ravi Chari
发明人: Wei Li , Nathan Fishkin , Robert Zhao , Michael Miller , Ravi Chari
IPC分类号: A61K31/5517 , C07D487/04 , C07D498/04 , C07D513/04 , C07D471/04 , A61K31/5513 , C07K16/18 , A61K39/395 , C07K14/52 , A61K38/19 , A61K38/22 , A61K38/18 , C07K14/575 , C07K14/475 , C07K14/53 , A61P35/00 , A61P33/00 , A61P31/12 , A61P25/28 , A61P19/00
CPC分类号: C07K16/2896 , A61K31/5517 , A61K38/07 , A61K45/06 , A61K47/60 , A61K47/6835 , A61K47/6849 , A61K47/6863 , A61P35/00 , C07D487/04 , C07D498/04 , C07D519/00 , C07K5/0202 , C07K5/1008 , C07K16/2803 , C07K16/46 , C07K19/00
摘要: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译: 本发明涉及具有抗增殖活性的新型苯并二氮杂衍生物,更具体地涉及式(I)和(II)的新型苯并二氮杂,其中二氮杂环(B)与杂环(CD)稠合,其中杂环是双环的 或其中二氮杂环(B)与杂环(C)稠合的式(III)化合物,其中杂环是单环的。 本发明提供这些化合物的细胞毒二聚体。 本发明还提供了单体和二聚体的共轭物。 本发明还提供了使用本发明的化合物或缀合物来抑制哺乳动物异常细胞生长或治疗增殖性病症的组合物和方法。 本发明还涉及将化合物或缀合物用于体外,原位和体内诊断或治疗哺乳动物细胞或相关病理状况的方法。
-
公开(公告)号:US08012978B2
公开(公告)日:2011-09-06
申请号:US12204082
申请日:2008-09-04
申请人: Robert Zhao , Ravi V. J. Chari
发明人: Robert Zhao , Ravi V. J. Chari
IPC分类号: A61K31/497 , C07F9/02
CPC分类号: C07D401/14 , C07D209/60 , Y02P20/55
摘要: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.
摘要翻译: 本发明提供抗肿瘤抗生素CC-1065类似物的前药,其具有含可含有磺酸的苯基氨基甲酸酯的可切割保护基,其中保护基赋予前药上的水溶性增强,其中前药还具有 可以与细胞结合试剂如抗体结合的部分,例如硫化物或二硫化物,以及用于治疗用途的这种前药和缀合物,以及用于制备这些前药和缀合物的方法。
-
公开(公告)号:US20090028821A1
公开(公告)日:2009-01-29
申请号:US12204082
申请日:2008-09-04
申请人: Robert Zhao , Ravi V.J. Chari
发明人: Robert Zhao , Ravi V.J. Chari
IPC分类号: A61K38/21 , C07D403/12 , C07D401/14 , A61K31/404 , A61K31/4439 , A61P35/00 , C07K16/00 , C07K14/555 , A61K39/44
CPC分类号: C07D401/14 , C07D209/60 , Y02P20/55
摘要: The present invention provides prodrugs of analogs of the anti-tumor antibiotic CC-1065 having a cleavable protective group containing a sulfonic acid containing phenyl carbamate, in which the protecting group confers enhanced water solubility upon the prodrug, and in which the prodrug also has a moiety, such as a sulfide or a disulfide, that can conjugate to a cell binding reagent such as an antibody, and for the therapeutic use of such prodrug and conjugates, and for processes for preparing such prodrugs and conjugates.
摘要翻译: 本发明提供抗肿瘤抗生素CC-1065类似物的前药,其具有含可含有磺酸的苯基氨基甲酸酯的可切割保护基,其中保护基赋予前药上的水溶性增强,其中前药还具有 可以与细胞结合试剂如抗体结合的部分,例如硫化物或二硫化物,以及用于治疗用途的这种前药和缀合物,以及用于制备这些前药和缀合物的方法。
-
公开(公告)号:US20130175711A1
公开(公告)日:2013-07-11
申请号:US13608875
申请日:2012-09-10
申请人: Francis C. NUTTER , Zhijing Wang , Robert Zhao , Edison Lu , Yongming Sun , Sean Wang , Christopher S. Kanel
发明人: Francis C. NUTTER , Zhijing Wang , Robert Zhao , Edison Lu , Yongming Sun , Sean Wang , Christopher S. Kanel
CPC分类号: F24F13/00 , C02F1/32 , F24F6/02 , F24F6/043 , F24F13/20 , F24F2003/1667 , F24F2006/006 , F24F2006/008
摘要: A UV sterilization chamber is provided to a humidifier having a water reservoir, a humidifying element and a pathway for directing water provided by the water reservoir to the humidifying element of the humidifier. The pathway is provided in a humidifier base, over which a humidifier enclosure is removably placed. The UV sterilization chamber includes a serpentine portion of the pathway and a UV radiation source positioned for illuminating the portion of the pathway with UV light. Upwardly-directed projections in the base border a perimeter of the pathway; and a downwardly-directed projection of the UV radiation source extends between the upwardly-directed projections when the enclosure is mated with the base, thereby locating the UV radiation source over the portion of the pathway. A switch disables the UV radiation source when the enclosure is removed from the base.
摘要翻译: UV加压器设置在具有储水器,加湿元件和用于将由储水器提供的水引导到加湿器的加湿元件的通道的加湿器中。 该通道设置在加湿器基座中,加湿器外壳可移除地放置在该加湿器基座上。 UV消毒室包括路径的蛇形部分和定位成用UV光照射路径部分的UV辐射源。 在基部边界中的向上指向的突起在通路的周边; 并且当外壳与基座配合时,UV辐射源的向下指向的突出部在向上指向的突起之间延伸,从而将UV辐射源定位在路径的该部分上。 当外壳从基座上拆下时,开关会禁用紫外线辐射源。
-
公开(公告)号:US20120319311A1
公开(公告)日:2012-12-20
申请号:US13002598
申请日:2010-10-20
申请人: Francis C Nutter , Zhijing Wang , Robert Zhao , Edisen Lu , Yongming Sun , Sean Wang , Christopher S. Kanel
发明人: Francis C Nutter , Zhijing Wang , Robert Zhao , Edisen Lu , Yongming Sun , Sean Wang , Christopher S. Kanel
CPC分类号: F24F13/00 , C02F1/32 , F24F6/02 , F24F6/043 , F24F13/20 , F24F2003/1667 , F24F2006/006 , F24F2006/008
摘要: A UV sterilization chamber is provided to a humidifier having a water reservoir, a humidifying element and a pathway for directing water provided by the water reservoir to the humidifying element of the humidifier. The pathway is provided in a humidifier base, over which a humidifier enclosure is removably placed. The UV sterilization chamber includes a serpentine portion of the pathway and a UV radiation source positioned for illuminating the portion of the pathway with UV light. Upwardly-directed projections in the base border a perimeter of the pathway; and a downwardly-directed projection of the UV radiation source extends between the upwardly-directed projections when the enclosure is mated with the base, thereby locating the UV radiation source over the portion of the pathway. A switch disables the UV radiation source when the enclosure is removed from the base.
摘要翻译: UV加压器设置在具有储水器,加湿元件和用于将由储水器提供的水引导到加湿器的加湿元件的通道的加湿器中。 该通道设置在加湿器基座中,加湿器外壳可移除地放置在该加湿器基座上。 UV消毒室包括路径的蛇形部分和定位成用UV光照射路径部分的UV辐射源。 在基部边界中的向上指向的突起在通路的周边; 并且当外壳与基座配合时,UV辐射源的向下指向的突出部在向上指向的突起之间延伸,从而将UV辐射源定位在路径的该部分上。 当外壳从基座上拆下时,开关会禁用紫外线辐射源。
-
公开(公告)号:US08163736B2
公开(公告)日:2012-04-24
申请号:US12174195
申请日:2008-07-16
申请人: Laurence Gauzy , Herve Bouchard , Ravi V. J. Chari , Alain Commercon , Robert Zhao , Yonghong Deng , Wei Li
发明人: Laurence Gauzy , Herve Bouchard , Ravi V. J. Chari , Alain Commercon , Robert Zhao , Yonghong Deng , Wei Li
IPC分类号: C07D519/00 , C07D487/00 , A61K31/5517
CPC分类号: C07D487/04
摘要: The present invention is related to new tomaymycin derivatives, their process of preparation and their therapeutic uses.
摘要翻译: 本发明涉及新的茅屋霉素衍生物,其制备方法及其治疗用途。
-
-
-
-
-
-
-