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公开(公告)号:US20080275033A1
公开(公告)日:2008-11-06
申请号:US12141747
申请日:2008-06-18
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
IPC分类号: A61K31/5415
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: A phenothiazinium compound of Formula (I) wherein: A and B each independently is in which R′ and R″ each independently is a linear, branched or cyclic hydrocarbon group, or R′ and R″ together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells.
摘要翻译: 式(I)的吩噻嗪鎓化合物其中:A和B各自独立地是其中R'和R“各自独立地是直链,支链或环状烃基,或者R'和R”与其中的N原子一起 它们连接形成任选取代的5-,6-或7-元环; 并且其中P SUP>是抗衡阴离子,P是1,2或3; 除了其中A和B均为-N(CH 3)2 - 或-N(CH 2 CH 2) 3 SUB>,用于需要去除,失活或杀死不想要的组织或细胞的治疗。
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公开(公告)号:US20080261960A1
公开(公告)日:2008-10-23
申请号:US12078805
申请日:2008-04-04
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R′ and R″ each independently is a linear, branched or cyclic hydrocarbon group, or R′ and R″ together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated.The compounds are biologically active photosensitisers which are strongly photocytotoxic and have application in the areas of photodynamic therapy (PDT), as well as for the diagnosis and detection of medical conditions and related uses in photochemical internalisation, in the production of cancer vaccines, in the treatment and prevention of microbial infections and in photodisinfection or photosterilisation.
摘要翻译: 本发明涉及式(I)的吩噻嗪鎓化合物:其中:A和B各自独立地是其中R'和R“各自独立地是直链,支链或环状烃基,或者R'和R”在一起 与它们所连接的N原子形成任选取代的5-,6-或7-元环; 并且其中X-P-P为抗衡阴离子,P为1,2或3; 除了其中A和B均为-N(CH 3)2 - 或-N(CH 2 CH 2) 3 SUB>,用于需要去除,失活或杀死不想要的组织或细胞的治疗。 本发明还涉及包含式I化合物的组合物,所选择的式I化合物,式I化合物用作药物和作为PDT剂或光诊断剂,在式I化合物之间形成的缀合物或复合物 和聚合物; 以及用于对液体进行灭菌的方法,其中流体在其被照射时通过共轭物或复合物。 这些化合物是具有强烈光细胞毒性并且在光动力疗法(PDT)领域中的应用的生物活性光敏剂,以及用于诊断和检测光化学内化中的医学病症和相关用途,在癌症疫苗的生产中 治疗和预防微生物感染和光消毒或光化学。
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公开(公告)号:US07915254B2
公开(公告)日:2011-03-29
申请号:US12078805
申请日:2008-04-04
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , David Ian Vernon
IPC分类号: A61K31/54
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a method of photodynamic therapy and to a method of inducing a photocytoxic effect which comprises applying to an area to be treated an effective amount of a compound of formula in which R1, R2, R3 and R4 each independently is an optionally -substituted linear, branched or cyclic hydrocarbon group, or R1 and R2 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7- membered ring or R3 and R4 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7- membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which —NR1R2 and —NR3R4 are the same and are selected from —N(CH3)2 or —N(CH2CH3)2; and exposing the area to light to activate the compound.
摘要翻译: 本发明涉及光动力学治疗的方法和诱导光毒性作用的方法,其包括向有待治疗的区域施用有效量的下式化合物,其中R 1,R 2,R 3和R 4各自独立地为任选的 取代的直链,支链或环状烃基,或者R 1和R 2与它们所连接的N原子一起形成任选取代的5-,6-或7-元环,或者R 3和R 4与它们 连接形成任选取代的5-,6-或7-元环; 而XP-是抗衡阴离子,P为1,2或3; 除了-NR 1 R 2和-NR 3 R 4相同并且选自-N(CH 3)2或-N(CH 2 CH 3)2的化合物之外) 并将该区域曝光以激活化合物。
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公开(公告)号:US20080268033A1
公开(公告)日:2008-10-30
申请号:US12171121
申请日:2008-07-10
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
IPC分类号: A61K9/127 , A61K31/5415
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R′ and R″ each independently is a linear, branched or cyclic hydrocarbon group, or R′ and R″ together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated.
摘要翻译: 本发明涉及式(I)的吩噻嗪鎓化合物:其中:A和B各自独立地是其中R'和R“各自独立地是直链,支链或环状烃基,或者R'和R”在一起 与它们所连接的N原子形成任选取代的5-,6-或7-元环; 并且其中P SUP>是抗衡阴离子,P是1,2或3; 除了其中A和B均为-N(CH 3)2 - 或-N(CH 2 CH 2) 3 SUB>,用于需要去除,失活或杀死不想要的组织或细胞的治疗。 本发明还涉及包含式I化合物的组合物,所选择的式I化合物,式I化合物用作药物和作为PDT剂或光诊断剂,在式I化合物之间形成的缀合物或复合物 和聚合物; 以及用于对液体进行灭菌的方法,其中流体在其被照射时通过共轭物或复合物。
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公开(公告)号:US20120302557A1
公开(公告)日:2012-11-29
申请号:US13453855
申请日:2012-04-23
申请人: Stanley Beames BROWN , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
发明人: Stanley Beames BROWN , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
IPC分类号: A61K31/5415 , A61P31/00
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a method of photodynamic therapy and to a method of inducing a photocytoxic effect which comprises applying to an area to be treated an effective amount of a compound of formula in which R1, R2, R3 and R4 each independently is an optionally-substituted linear, branched or cyclic hydrocarbon group, or R1 and R2 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring or R3 and R4 together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which —NR1R2 and —NR3R4 are the same and are selected from —N(CH3)2 or —N(CH2CH3)2; and exposing the area to light to activate the compound.
摘要翻译: 本发明涉及光动力学治疗的方法和诱导光毒性作用的方法,其包括向有待治疗的区域施用有效量的下式化合物,其中R 1,R 2,R 3和R 4各自独立地为任选的 取代的直链,支链或环状烃基,或R 1和R 2与它们所连接的N原子一起形成任选取代的5-,6-或7-元环,或者R 3和R 4与它们所在的N原子一起形成 连接形成任选取代的5-,6-或7-元环; 而XP-是抗衡阴离子,P为1,2或3; 除了-NR 1 R 2和-NR 3 R 4相同并且选自-N(CH 3)2或-N(CH 2 CH 3)2的化合物之外) 并将该区域曝光以激活化合物。
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公开(公告)号:US08188074B2
公开(公告)日:2012-05-29
申请号:US12149996
申请日:2008-05-12
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , David Ian Vernon
IPC分类号: A61K31/54
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a composition which includes a moiety of formula wherein R1, R2, R3 and R4 each represent n-pentyl, and to a method of sterilizing a su fluid using same.
摘要翻译: 本发明涉及一种组合物,其包含其中R 1,R 2,R 3和R 4各自表示正戊基的下式的部分,以及使用它们对su流体进行灭菌的方法。
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公开(公告)号:US07855197B2
公开(公告)日:2010-12-21
申请号:US12141747
申请日:2008-06-18
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , David Ian Vernon
IPC分类号: A61K31/54
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: A phenothiazinium compound of Formula (I) wherein: A and B each independently is in which R′ and R″ each independently is a linear, branched or cyclic hydrocarbon group, or R′ and R″ together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells.
摘要翻译: 式(I)的吩噻嗪鎓化合物其中:A和B各自独立地是其中R'和R“各自独立地是直链,支链或环状烃基,或者R'和R”与它们所在的N原子一起 连接形成任选取代的5-,6-或7-元环; 而XP-是抗衡阴离子,P为1,2或3; 除了其中A和B都是-N(CH 3)2或-N(CH 2 CH 3)2)的化合物,其用于需要去除,失活或杀死不想要的组织或细胞的处理中。
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公开(公告)号:US07732439B2
公开(公告)日:2010-06-08
申请号:US12171121
申请日:2008-07-10
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
IPC分类号: A61K31/54
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a pharmaceutical composition which contains a compound of formula in which R1, R2, R3 and R4 are each n-butyl, where XP− is a counteranion and P is 1, 2 or 3, together with a pharmaceutically acceptable carrier, excipient or adjuvant.
摘要翻译: 本发明涉及含有下式的化合物的药物组合物,其中R 1,R 2,R 3和R 4各自为正丁基,其中XP-为抗衡阴离子,P为1,2或3,以及药学上可接受的载体 ,赋形剂或佐剂。
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公开(公告)号:US20080312219A1
公开(公告)日:2008-12-18
申请号:US12149996
申请日:2008-05-12
申请人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
发明人: Stanley Beames Brown , Cassandra Claire O'Grady , John Griffiths , Kirste Joanne Mellish , Richard George Tunstall , David John Howard Roberts , David Ian Vernon
IPC分类号: A61K31/5415 , C07D279/18 , A61P35/00 , A61P31/04 , C07D413/12
CPC分类号: A61K49/003 , A61K8/4986 , A61K41/0057 , A61L2/0029 , A61L2/0082 , A61L2/08 , A61L2/232 , A61Q11/00 , C07D279/18
摘要: The present invention relates to a phenothiazinium compound of Formula (I): wherein: A and B each independently is in which R′ and R″ each independently is a linear, branched or cyclic hydrocarbon group, or R′ and R″ together with the N atom to which they are attached form an optionally substituted 5-, 6- or 7-membered ring; and where XP− is a counteranion and P is 1, 2 or 3; except for the compounds in which A and B are both either —N(CH3)2 or —N(CH2CH3)2 for use in a treatment that requires removal, deactivation or killing of unwanted tissues or cells. The invention also relates to compositions comprising the compounds of Formula I, to selected compounds of Formula I, use of the compounds of Formula I as medicaments and as a PDT agent or a photodiagnostic agent, a conjugate or composite formed between a compound of Formula I and a polymer; and to a method for sterilising fluids in which the fluid is passed over the conjugate or composite whilst it is illuminated.The compounds are biologically active photosensitisers which are strongly photocytotoxic and have application in the areas of photodynamic therapy (PDT), as well as for the diagnosis and detection of medical conditions and related uses in photochemical internalisation, in the production of cancer vaccines, in the treatment and prevention of microbial infections and in photodisinfection or photosterilisation.
摘要翻译: 本发明涉及式(I)的吩噻嗪鎓化合物:其中:A和B各自独立地是其中R'和R“各自独立地是直链,支链或环状烃基,或者R'和R”在一起 与它们所连接的N原子形成任选取代的5-,6-或7-元环; 而XP-是抗衡阴离子,P为1,2或3; 除了其中A和B都是-N(CH 3)2或-N(CH 2 CH 3)2)的化合物,其用于需要去除,失活或杀死不想要的组织或细胞的处理中。 本发明还涉及包含式I化合物的组合物,所选择的式I化合物,式I化合物用作药物和作为PDT剂或光诊断剂,在式I化合物之间形成的缀合物或复合物 和聚合物; 以及用于对液体进行灭菌的方法,其中流体在其被照射时通过共轭物或复合物。 这些化合物是具有强烈光细胞毒性并且在光动力疗法(PDT)领域中的应用的生物活性光敏剂,以及用于诊断和检测光化学内化中的医学病症和相关用途,在癌症疫苗的生产中 治疗和预防微生物感染和光消毒或光化学。
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