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    • 1. 发明申请
    • Arene Ruthenium (ll) Compounds And Their Use In Cancer Therapy
    • 芳钌(II)化合物及其在癌症治疗中的应用
    • US20080096846A1
    • 2008-04-24
    • US11660627
    • 2005-08-19
    • Abraha HabtemariamPeter Sadler
    • Abraha HabtemariamPeter Sadler
    • A61K31/28A61K31/555A61K31/655A61P35/00C07C245/00C07F15/00
    • C07C211/65C07F17/02
    • A ruthenium (II) compound of formula (I): or a solvate on prodrug thereof, wherein: R1, R1, R3, R4, R5 and R6 are independently selected from H, C1-7 alkyl, C5-20 aryl, C3-20 heterocyclyl, halo, ester, amido, acyl, sulfo, sulfonamido, ether, thioether, azo, amino, or R1 and R2 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 a neutral or negatively charged N- or S-donor ligand; Y is a counterion; in is 0 or 1; q is 1, 2 or 3; C″ is C1-12 alkylene bound to two A groups; p is 0 or 1 and r is 1 when p is 0 and r is 2 when p is 1; and A and B are each independently O-donor, N-donor or S-donor ligands, and may be connected to one another. The compounds are used in cancer therapy.
    • 式(I)的钌(II)化合物或其前药上的溶剂化物,其中:R 1,R 1,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,氨基或R 1和R 2与它们所连接的环连同形成饱和或不饱和的含有至多三个3-8元碳环或杂环的碳环或杂环基团,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是中性或带负电荷的N-或S-供体配体; Y是反抗; in是0或1; q为1,2或3; C“是与两个A基团结合的C 1-12亚烷基; p为0或1,当p为0时r为1,p为1时r为2; A和B各自独立地为O-供体,N-供体或S-供体配体,并且可以彼此连接。 这些化合物用于癌症治疗。
    • 4. 发明申请
    • PHOTOREACTIVE COMPOUNDS AND COMPOSITIONS
    • US20070142466A1
    • 2007-06-21
    • US11674183
    • 2007-02-13
    • Peter SadlerPhilippe Muller
    • Peter SadlerPhilippe Muller
    • A61K31/282C07F15/00
    • A61K33/24A61K31/28A61K31/555C07F15/0093
    • The present invention provides a compound of formula (I): PtIV(N3)2X1X2Y1Y2, wherein X1 and X2 are the same or different and each one is a group NR1R2R3 wherein R1, R2 and R3 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 X1 and X2 together represent a group R1R2NR4NR1R2 wherein R1 and R2 have the same meaning as before, and R4 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 R4 or two or more of R1, R2, R3 and R4 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 Y1 and Y2 are the same or different or when cis together represent a divalent moiety Y3, wherein at least one of Y1 and Y2, or Y3, 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 R1, R2, R3 and R4, 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.
    • 6. 发明申请
    • Half-sandwich ruthenium (II) compounds comprising nitrogen containing ligands for treatment of cancer
    • 包含用于治疗癌症的含氮配体的半夹心钌(II)化合物
    • US20050239765A1
    • 2005-10-27
    • US11165372
    • 2005-06-23
    • Robert MorrisPeter SadlerHaimei ChenDuncan Jodrell
    • Robert MorrisPeter SadlerHaimei ChenDuncan Jodrell
    • C07D213/81A61K31/132A61K31/216A61K31/275A61K31/455A61K31/555A61K33/24A61P35/00C07F15/00C07F17/02
    • A61K31/555A61K33/24C07F15/0046C07F17/02
    • Compounds which may be used in the treatment and/or prevention of cancer have the formula (I) wherein: R1, R2, R3, R4, R5 and R6 independently represents H, alkyl, —CO2R′, aryl or akylaryl, which latter two groups are optionally substituted on the aromatic ring; R′ represent alkyl, aryl or alkaryl; X is halo, H2O, (R′)(R″)SO, R′CO2— or (R′)(R″)C═O, where R″ represents alkyl, aryl or alkaryl; Y is a counterion; m is 0 or 1; q is 1, 2 or 3; C′ is C1 to C12 alkylene, optionally substituted in or on the alkylene chain, bound to two A groups; p is 0 or 1 and r is 1 when p is 0 and r is 2 when p is 1, and A and B are: each independently N-donor nitrile ligands; or B is halo and A is an N-donor pyridine ligand, optionally substituted at one or more of the carbon atoms of the pyridine ring; or p is 0, A is NR7R8 and B is NR9R10, wherein R7, R8, R9 and R10 independently represent H or alkyl, and A and B are linked by an alkylene chain, optionally substituted in or on the alkylene chain, or p is 1, A is NR7 and B is NR9R10, wehrein R7, R9 and R10 are as previously defined, and A and B are linked by an alkylene chain, optionally substituted.
    • 可用于治疗和/或预防癌症的化合物具有式(I),其中:R 1,R 2,R 3, >,R 4,R 5和R 6独立地表示H,烷基,-CO 2 R', 芳基或烷基芳基,后两个基团任选在芳环上取代; R'代表烷基,芳基或烷芳基; X是卤素,H 2 O,(R')(R“)SO,R'CO 2 - 或(R')(R”')CO, 其中R“表示烷基,芳基或烷芳基; Y是反抗; m为0或1; q为1,2或3; C'是C 1至C 12亚烷基,任选在亚烷基链中或在亚烷基链上取代,与两个A基团结合; p为0或1,当p为0时r为1,p为1时r为2,A和B各自为N-供体腈配体; 或B是卤素,并且A是任选在吡啶环的一个或多个碳原子处被取代的N-供体吡啶配体; 或p为0,A为NR 7 R 8,B为NR 9 R 10,其中R' R 8,R 9,R 9和R 10独立地表示H或烷基,并且A和B通过 任选在亚烷基链中或亚烷基链上取代的亚烷基链,或p是1,A是NR 7,B是NR 9 R 10, ,wehrein R 7,R 9和R 10如前所定义,A和B通过任选取代的亚烷基链连接。