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1. 发明授权

US08506931B2 Perylenequinone derivatives and uses thereof 有权
标题翻译：苝醌衍生物及其用途
公开(公告)号：US08506931B2
公开(公告)日：2013-08-13
申请号：US11722423
申请日：2006-07-28
申请人： Sanjay K. Sharma , Thomas Woo , Selvaraj Naicker
发明人： Sanjay K. Sharma , Thomas Woo , Selvaraj Naicker
IPC分类号： A61K49/00
CPC分类号： C07C229/74 , A61K8/415 , A61K8/492 , A61K41/0033 , A61K41/0057 , A61K49/00 , A61K2800/434 , A61Q9/04 , C07C225/32 , C07C2603/54 , C07D209/94 , C07D241/38 , C07D241/52
摘要： The present invention relates to compounds which are perylenequinone derivatives, their stereoisomers and atropisomers. These compounds can be particularly useful as photosensitizers or sononsensitizers in photodynamic or sonodynamic therapy. The invention also relates to various methods for using these compounds in photodynamic and/or sonodynamic therapy. The compounds also are useful as therapeutic agents for treating various hyperproliferative disorders.
摘要翻译：本发明涉及苝醌衍生物，其立体异构体和阻转异构体的化合物。这些化合物在光动力学或儿子动力学治疗中可以特别用作光敏剂或超声敏剂。本发明还涉及在光动力学和/或超声动力学治疗中使用这些化合物的各种方法。所述化合物还可用作治疗各种过度增殖性疾病的治疗剂。

2. 发明申请

US20100047178A1 PERYLENEQUINONE DERIVATIVES AND USES THEREOF 有权
标题翻译：季戊四醇衍生物及其用途
公开(公告)号：US20100047178A1
公开(公告)日：2010-02-25
申请号：US11722423
申请日：2006-07-28
申请人： Sanjay K. Sharma , Thomas Woo , Selvaraj Naicker
发明人： Sanjay K. Sharma , Thomas Woo , Selvaraj Naicker
IPC分类号： A61K49/06 , C07D487/00 , A61K31/403 , C07C211/57 , A61K31/135 , C07D241/36 , A61K31/498 , A61K39/395 , A61K38/02 , A61K9/127 , A61K49/00 , A61P35/00 , G01N33/53
CPC分类号： C07C229/74 , A61K8/415 , A61K8/492 , A61K41/0033 , A61K41/0057 , A61K49/00 , A61K2800/434 , A61Q9/04 , C07C225/32 , C07C2603/54 , C07D209/94 , C07D241/38 , C07D241/52
摘要： The present invention relates to compounds which are perylenequinone derivatives, their stereoisomers and atropisomers. These compounds can be particularly useful as photosensitizers or sononsensitizers in photodynamic or sonodynamic therapy. The invention also relates to various methods for using these compounds in photodynamic and/or sonodynamic therapy. The compounds also are useful as therapeutic agents for treating various hyperproliferative disorders.
摘要翻译：本发明涉及苝醌衍生物，其立体异构体和阻转异构体的化合物。这些化合物在光动力学或儿子动力学治疗中可以特别用作光敏剂或超声敏剂。本发明还涉及在光动力学和/或超声动力学治疗中使用这些化合物的各种方法。所述化合物还可用作治疗各种过度增殖性疾病的治疗剂。

3. 发明授权

US07538189B2 Methods of making deuterated cyclosporin analogs 有权
标题翻译：制备氘代环孢菌素类似物的方法
公开(公告)号：US07538189B2
公开(公告)日：2009-05-26
申请号：US11245775
申请日：2005-10-06
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61K38/13
CPC分类号： C07K7/645 , A61K38/00 , C07B59/008 , C07K1/13 , C07K7/64 , Y10S530/806 , Y10S530/807
摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
摘要翻译：公开了与天然存在的和其他目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。

4. 发明授权

US07332472B2 Cyclosporine analogue mixtures and their use as immunomodulating agents 有权
标题翻译：环孢霉素类似物混合物及其作为免疫调节剂的用途
公开(公告)号：US07332472B2
公开(公告)日：2008-02-19
申请号：US11118830
申请日：2005-04-28
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61K38/13
CPC分类号： C07K7/645 , A61K9/0095 , A61K9/1075 , A61K9/4858 , A61K38/00 , A61K38/13 , B82Y5/00 , C07K7/64 , Y10S530/806
摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
摘要翻译：本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。本发明的实施方案涉及被称为ISA 247的环孢菌素A类似物及其衍生物的顺式和反式异构体。 ISA 247异构体的混合物显示了与天然存在的和目前已知的环孢菌素相比增强的效力和降低的毒性的组合。通过立体选择性途径合成烷基化，芳基化和氘代衍生物，其中反应的特定条件决定了立体选择性的程度。基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。

5. 发明申请

US20050192214A1 Cyclosporine analogue mixtures and their use as immunomodulating agents 有权
标题翻译：环孢霉素类似物混合物及其作为免疫调节剂的用途
公开(公告)号：US20050192214A1
公开(公告)日：2005-09-01
申请号：US11118830
申请日：2005-04-28
申请人： Selvaraj Naicker , Randall Yatscoff , Robert Foster
发明人： Selvaraj Naicker , Randall Yatscoff , Robert Foster
IPC分类号： A61K38/00 , A61K9/00 , A61K9/107 , A61K9/48 , A61K38/13 , A61P19/02 , A61P37/06 , C07K7/00 , C07K7/52 , C07K7/64
CPC分类号： C07K7/645 , A61K9/0095 , A61K9/1075 , A61K9/4858 , A61K38/00 , A61K38/13 , B82Y5/00 , C07K7/64 , Y10S530/806
摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of siereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
摘要翻译：本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。本发明的实施方案涉及被称为ISA 247的环孢菌素A类似物及其衍生物的顺式和反式异构体。 ISA 247异构体的混合物显示了与天然存在的和目前已知的环孢菌素相比增强的效力和降低的毒性的组合。通过立体选择性途径合成烷基化，芳基化和氘代衍生物，其中反应的特定条件决定了Silectoslectivity的程度。基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。

6. 发明申请

US20050176628A1 Deuterated cyclosporin analogs and their use as immunomodulating agents 有权
标题翻译：氘代环孢菌素类似物及其作为免疫调节剂的用途
公开(公告)号：US20050176628A1
公开(公告)日：2005-08-11
申请号：US11105897
申请日：2005-04-13
申请人： Selvaraj Naicker , Randall Yatscoff , Robert Foster
发明人： Selvaraj Naicker , Randall Yatscoff , Robert Foster
IPC分类号： A61K38/00 , C07B59/00 , C07K1/13 , C07K7/64 , A61K38/13
CPC分类号： C07K7/645 , A61K38/00 , C07B59/008 , C07K1/13 , C07K7/64 , Y10S530/806 , Y10S530/807
摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
摘要翻译：公开了与天然存在的和其他目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。

7. 发明授权

US06686454B1 Antibodies to specific regions of cyclosporine related compounds 失效
标题翻译：针对环孢菌素相关化合物的特定区域的抗体
公开(公告)号：US06686454B1
公开(公告)日：2004-02-03
申请号：US09390280
申请日：1999-09-03
申请人： Randall W. Yatscoff , Andrew J. Malcolm , S. Selvaraj Naicker
发明人： Randall W. Yatscoff , Andrew J. Malcolm , S. Selvaraj Naicker
IPC分类号： C07K1600
CPC分类号： C07K7/64 , A61K39/00 , C07K16/14 , G01N33/9493 , Y10S435/975
摘要： This invention relates to the production of polyclonal and monoclonal antibodies to specific regions of cyclosporine (CSA) and/or CSA metabolites/derivatives. The reactivity of these polyclonal and monoclonal antibodies make them particularly useful for immunoassays for therapeutic drug monitoring (TDM). These immunoassays or TDM kits may include polyclonal or monoclonal antibodies to specific sites of CSA and/or CSA metabolites. These kits may also include various combinations of polyclonal antibodies, polyclonal and monoclonal antibodies or a panel of monoclonal antibodies. Cyclosporine or CSA metabolite conjugate immunogens are prepared for the immunization of a host animal to produce antibodies directed against specific regions of the CSA or CSA metabolite molecule. By determining the specific binding region of a particular antibody, immunoassays which are capable of distinguishing between the parent molecule, active metabolites, inactive metabolites and other structurally similar immunosuppressant compounds are developed. The use of divinyl sulfone (DVS) as the linker arm molecule for forming cyclosporine and cyclosporine metabolite protein conjugate immunogens is described.
摘要翻译：本发明涉及针对环孢菌素（CSA）和/或CSA代谢物/衍生物的特定区域的多克隆和单克隆抗体的产生。这些多克隆抗体和单克隆抗体的反应性使其在治疗药物监测（TDM）的免疫测定中特别有用。这些免疫测定或TDM试剂盒可以包括针对CSA和/或CSA代谢物的特定位点的多克隆或单克隆抗体。这些试剂盒还可以包括多克隆抗体，多克隆和单克隆抗体或一组单克隆抗体的各种组合。制备环孢菌素或CSA代谢物缀合物免疫原用于免疫宿主动物以产生针对CSA或CSA代谢物分子的特定区域的抗体。通过确定特定抗体的特异性结合区域，开发了能够区分亲本分子，活性代谢物，无活性代谢物和其它结构相似的免疫抑制剂化合物的免疫测定。描述了使用二乙烯基砜（DVS）作为形成环孢菌素和环孢菌素代谢物蛋白质结合物免疫原的连接臂分子。

8. 发明授权

US07521421B2 Deuterated cyclosporine analogs and methods of making the same 有权
标题翻译：氘代环孢菌素类似物及其制备方法
公开(公告)号：US07521421B2
公开(公告)日：2009-04-21
申请号：US11280666
申请日：2005-11-15
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61K38/00
CPC分类号： C07K7/645 , A61K38/00 , C07B59/008 , C07K1/13 , C07K7/64 , Y10S530/806 , Y10S530/807
摘要： Cyclosporine derivatives are disclosed which possess enhanced efficacy and reduced toxicity over naturally occurring and other presently known cyclosporins and cyclosporine derivatives. The cyclosporine derivatives of the present invention are produced by chemical and isotopic substitution of the cyclosporine A (CsA) molecule by: (1) Chemical substitution and optionally deuterium substitution of amino acid 1; and (2) deuterium substitution at key sites of metabolism of the cyclosporine A molecule such as amino acids 1, 4, 9. Also disclosed are methods of producing the cyclosporine derivatives and method of producing immunosuppression with reduced toxicity with the disclosed cyclosporine derivatives.
摘要翻译：公开了与天然存在的和其他目前已知的环孢菌素和环孢菌素衍生物相比具有增强的功效和降低的毒性的环孢菌素衍生物。本发明的环孢菌素衍生物通过以下方式通过环孢菌素A（CsA）分子的化学和同位素取代产生：（1）氨基酸1的化学取代和任选的氘取代; 和（2）在环孢菌素A分子的代谢关键位置的氘代替，例如氨基酸1,4,9。还公开了产生环孢菌素衍生物的方法和与所公开的环孢菌素衍生物一起产生具有降低的毒性的免疫抑制的方法。

9. 发明授权

US06939878B2 Deuterated rapamycin compounds, method and uses thereof 失效
标题翻译：氘代雷帕霉素化合物，其方法和用途
公开(公告)号：US06939878B2
公开(公告)日：2005-09-06
申请号：US10754488
申请日：2004-01-09
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61L31/16 , C07D498/18 , A61P35/02 , A61P37/06
CPC分类号： C07D498/18 , A61L31/16 , A61L2300/416
摘要： The synthesis of deuterated analogues of rapamycin is disclosed together with a method for use for inducing immunosupression and in the treatment of transplantation rejection, graft vs host disease, autoimmune diseases, diseases of inflammation leukemia/lymphoma, solid tumors, fungal infections, hyperproliferative vascular disorders. Also described is a method for the synthesis of water soluble deuteratred rapamycin compounds and their use as described above.
摘要翻译：公开雷帕霉素的氘代类似物的合成以及用于诱导免疫抑制的方法和用于治疗移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症性白血病/淋巴瘤疾病，实体瘤，真菌感染，过度增殖性血管疾病。还描述了合成水溶性氘化雷帕霉素化合物的方法及其用途如上所述。

10. 发明授权

US06710053B2 Deuterated rapamycin compounds, method and uses thereof 失效
标题翻译：氘代雷帕霉素化合物，其方法和用途
公开(公告)号：US06710053B2
公开(公告)日：2004-03-23
申请号：US10300015
申请日：2002-11-20
申请人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
发明人： Selvaraj Naicker , Randall W. Yatscoff , Robert T. Foster
IPC分类号： A61K31445
CPC分类号： C07D498/18 , A61L31/16 , A61L2300/416
摘要： The synthesis of deuterated analogues of rapamycin is disclosed together with a method for use for inducing immunosupression and in the treatment of transplantation rejection, graft vs host disease, autoimmune diseases, diseases of inflammation leukemia/lymphoma, solid tumors, fungal infections, hyperproliferative vascular disorders. Also described is a method for the synthesis of water soluble deuteratred rapamycin compounds and their use as described above.
摘要翻译：公开雷帕霉素的氘代类似物的合成以及用于诱导免疫抑制的方法和用于治疗移植排斥反应，移植物抗宿主病，自身免疫性疾病，炎症性白血病/淋巴瘤疾病，实体瘤，真菌感染，过度增殖性血管疾病。还描述了合成水溶性氘化雷帕霉素化合物的方法及其用途如上所述。

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