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1.发明授权Medical devices incorporating deuterated rapamycin for controlled delivery thereof 失效结合氘化雷帕霉素的医疗装置用于其控制递送公开(公告)号：US06884429B2
公开(公告)日：2005-04-26
申请号：US10301504
申请日：2002-11-20
IPC分类号： A61L29/16 , A61L31/16 , C07D498/18 , A61M25/00 , A61F2/00
CPC分类号： C07D498/18 , A61L29/16 , A61L31/16 , A61L2300/416 , A61L2300/602
摘要： Deuterated rapamycin can be controllably introduced target locations within the patient's body by using an implantable medical device having a structure incorporated with a therapeutic agent comprising a deuterated rapamycin. Representative deuterated rapamycins include epi-7-deuteromthyl rapamycin, 7,43-d6 rapamycin, 7-deuteromethyl rapamycin and 31,42-d2-rapamycin and isomers thereof, and mixtures thereof. The deuterated rapamycin can also be glycosylated.
摘要翻译： 氘化雷帕霉素可以通过使用具有结合有包含氘化雷帕霉素的治疗剂的结构的可植入医疗装置来可控地引入患者体内的靶位置。 代表性的氘代雷帕霉素包括表7-降血磷酸雷帕霉素，7,43-d6N雷帕霉素，7-氘代甲基雷帕霉素和31,42-d2-雷帕霉素及其异构体， 及其混合物。 氘代雷帕霉素也可以糖基化。
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2.发明授权公开(公告)号：US07358229B2
公开(公告)日：2008-04-15
申请号：US11105897
申请日：2005-04-13
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。
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公开(公告)号：US07521421B2
公开(公告)日：2009-04-21
申请号：US11280666
申请日：2005-11-15
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。
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公开(公告)号：US06939878B2
公开(公告)日：2005-09-06
申请号：US10754488
申请日：2004-01-09
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。
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公开(公告)号：US06710053B2
公开(公告)日：2004-03-23
申请号：US10300015
申请日：2002-11-20
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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公开(公告)号：US06225323B1
公开(公告)日：2001-05-01
申请号：US09125173
申请日：1998-08-11
IPC分类号： A61K31437
CPC分类号： C07D213/86 , C07C233/65 , C07C233/78 , C07D213/87 , C07D277/46 , C07D285/135 , C07D311/16
摘要： A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
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公开(公告)号：US07538189B2
公开(公告)日：2009-05-26
申请号：US11245775
申请日：2005-10-06
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。
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8.发明授权公开(公告)号：US07332472B2
公开(公告)日：2008-02-19
申请号：US11118830
申请日：2005-04-28
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％。
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9.发明申请Cyclosporine Analogue Mixtures and their Use as Immunomodulating Agents 审中-公开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：US20080171850A1
公开(公告)日：2008-07-17
申请号：US11969174
申请日：2008-01-03
IPC分类号： 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 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％。
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公开(公告)号：US06780995B2
公开(公告)日：2004-08-24
申请号：US10303048
申请日：2002-11-25
IPC分类号： C07D47104
CPC分类号： C07D213/86 , A61K31/166 , A61K31/426 , A61K31/4409 , A61K31/4745 , C07C233/65 , C07C233/78 , C07C237/30 , C07D213/87 , C07D277/46 , C07D285/135 , C07D311/16
摘要： A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.
摘要翻译： 一系列活化的碘代苯甲酰胺衍生物被描述为抗肿瘤和抗病毒药物化合物。 化合物通常具有螯合基团，硫醇捕获基团和活化基团。 预防癌细胞和病毒复制的推定机制是通过抑制转录因子与锌指结合结构域的结合。 该化合物在低浓度下有效抑制各种人和动物肿瘤和白血病细胞系的生长。
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