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    • 5. 发明申请
    • RUTHENIUM II COMPOUNDS
    • 二氢化钌
    • WO2007135410A1
    • 2007-11-29
    • PCT/GB2007/001874
    • 2007-05-21
    • THE UNIVERSITY COURT OF THE UNVERSITY OF EDINBURGHHABTEMARIAM, AbrahaBUGARCIC, TijanaSADLER, Peter John
    • HABTEMARIAM, AbrahaBUGARCIC, TijanaSADLER, Peter John
    • A61K31/00A61P35/00
    • C07F17/02
    • A ruthenium (II) compound of formula (I), or a solvate form thereof for use in a method of therapy, wherein: R 1 R 2 R 3 R 4 R 5 and R 6 are independently selected from H, C 1-7 alkyl, C 5-20 aryl, C 3-20 heterocyclyl, halo, ester, amido, acyl, sulfo, sulfonamido, ether, thioether, azo and amino, or R 1 and R 2 together with the ring to which they are attached form a saturated or unsaturated carbocyclic or heterocyclic group containing up to three 3- to 8- membered carbocyclic or heterocyclic rings, wherein each carbocyclic or heterocyclic ring may be fused to one or more other carbocyclic or heterocyclic rings; X is halo or a neutral or negatively charged O, N- or S- donor ligand; m is -1, 0, 1 or 2; q is 1, 2 or 3; R C1 and R C2 independently represent one or more optional substituents selected from hydroxy, C 1-7 alkoxy, C 5-20 aryloxy, C 1-7 alkyl, carboxy, C 1-7 alkyl ester and C 5-20 aryl ester; R N1 and R N2 are independently selected from hydroxy, C 1-7 alkoxy, C 5-20 aryloxy, C 1-7 alkyl, carboxy, C 1-7 alkyl ester and C 5-20 aryl ester; or R N1 and R N2 together with the pyridine rings to which they are bound form an tricyclic heteraromatic moiety, where the ring formed by R N1 and R N2 together may be optionally substituted by one or more substituents represented by R C3 selected from: hydroxy, C 1-7 alkoxy, C 5-20 aryloxy, C 1-7 alkyl, carboxy, C 1-7 alkyl ester and C 5-20 aryl ester.
    • 用于治疗方法的式(I)的钌(II)化合物或其溶剂化物形式,其中:R 1 R 2 R 3 R 4 R 5和R 6独立地选自H,C 1-7烷基 C 5-20芳基,C 3-20杂环基,卤素,酯,酰胺基,酰基,磺基,亚磺酰氨基,醚,硫醚,偶氮和氨基, 它们所连接的环与它们所连接的环一起形成含有至多三个3-至8-元碳环或杂环的饱和或不饱和碳环或杂环基, 其中每个碳环或杂环可以与一个或多个其它碳环或杂环稠合; X是卤素或中性或带负电荷的O,N-或S-供体配体; m为-1,0,1或2; q为1,2或3; R C1和R C2独立地表示一个或多个任选的选自羟基,C 1-7 - 烷氧基,C 5-20的取代基 芳氧基,C 1-7烷基,羧基,C 1-7 - 烷基酯和C 5-20-20芳基酯; R N1和R N2独立地选自羟基,C 1-7 - 烷氧基,C 5-20芳氧基 C 1-7烷基,羧基,C 1-7烷基酯和C 5-20-20芳基酯; 或R N1和R N2与它们所连接的吡啶环一起形成三环杂芳基部分,其中由R 1,R 2, 和R“N 2”可以任选被一个或多个选自以下的取代基取代:选自羟基,C 1-7 - 烷氧基,C 5-20芳氧基,C 1-7 - 烷基,羧基,C 1-7 - 烷基酯和C 5-20 - 芳基酯。
    • 9. 发明申请
    • PHOTOREACTIVE COMPOUNDS AND COMPOSITIONS
    • 光敏化合物和组合物
    • WO2003017993A1
    • 2003-03-06
    • PCT/GB2002/003939
    • 2002-08-27
    • THE UNIVERSITY COURT OF THE UNIVERSITY OF EDINBURGHSADLER, Peter, JohnMÜLLER, Philippe
    • SADLER, Peter, JohnMÜLLER, Philippe
    • A61K31/00
    • A61K33/24A61K31/28A61K31/555C07F15/0093
    • The present invention provides a compound of formula (I): Pt IV (N 3 ) 2 X 1 X 2 Y 1 Y 2 , wherein X 1 and X 2 are the same or different and each one is a group NR 1 R 2 R 3 wherein R 1 , R 2 and R 3 are the same or different and each can be any one of H and optionally substituted alkyl, aryl, aralkyl, acyl, cycloalkyl, heterocyclyl, alkenyl, aralkenyl, alkinyl, cycloalkenyl, or X 1 and X 2 together represent a group R 1 R 2 NR 4 NR 1 R 2 wherein R 1 and R 2 have the same meaning as before, and R 4 represents an optionally substituted divalent, saturated or unsaturated, alkyl chain, an optionally substituted divalent, saturated or unsaturated cycloalkyl or an optionally substituted divalent aryl, or R 4 or two or more of R 1 , R 2 , R 3 and R 4 and the respective N atom(s) to which they are linked, represent an optionally substituted heterocyclyl having at least one ring containing said N atom(s); and Y 1 and Y 2 are the same or different or when cis together represent a divalent moiety Y 3 , wherein at least one of Y 1 and Y 2 , or Y 3 , is a substantially labile ligand in the analogous Pt(II) complex without the azide groups, whilst being substantially resistant, in vivo , to hydrolysis and physiological reducing agents. One or more of R 1 , R 2 , R 3 and R 4 , may further represent a covalently bonded link to at least one further complex of formula (I) to form a dimer or oligomer, or to a targeting moiety having affinity for a predetermined tissue or cell type.
    • 本发明提供了式(I)化合物:其中X 1和X 2相同或不同,其中X 1和X 2都相同或不同, 不同,每个是NR 1 R 2 R 3基团,其中R 1,R 2和R 3相同或不同,并且各自可以是H中的任何一个和任选取代的 烷基,芳基,芳烷基,酰基,环烷基,杂环基,烯基,芳烯基,炔基,环烯基或X 1和X 2一起表示基团R 1,R 2 NR 4 NR 1 R 2其中R 1和R 2具有与之前相同的含义,并且R 4表示任选取代的二价,饱和或不饱和的烷基链,任选取代的二价饱和或不饱和环烷基或 或R 4或R 1,R 2,R 3和R 4中的两个或多个,以及与它们相连的各自的N原子代表一个 任选取代的具有至少一个含有所述N原子的环的杂环基; Y 1和Y 2相同或不同,或者当顺式一起代表二价基团Y 3时,其中Y 1和Y 2或Y 3中的至少一个是 在类似的Pt(II)络合物中没有叠氮基团的基本上不稳定的配体,同时在体内基本上对水解和生理还原剂具有抗性。 R 1,R 2,R 3和R 4中的一个或多个可以进一步代表与至少一个另外的式(I)的络合物的共价连接的连接基以形成二聚体或低聚物,或 涉及对预定组织或细胞类型具有亲和性的靶向部分。