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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。
    • 5. 发明申请
    • RUTHENIUM (II) COMPOUNDS
    • (II)化合物
    • US20090186864A1
    • 2009-07-23
    • US12301373
    • 2007-05-21
    • Abraha HabtemariamTijana BugarcicPeter John Sadler
    • Abraha HabtemariamTijana BugarcicPeter John Sadler
    • A61K31/555C07F15/00A61P35/00
    • C07F17/02
    • A ruthenium (II) compound of formula (I): or a solvate form thereof for use in a method of therapy, wherein: R1, R2, 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 and 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 halo or a neutral or negatively charged O, N— or S— donor ligand; Y is a counterion; m is −1, 0, 1 or 2; q is 1, 2 or 3; RC1 and RC2 independently represent one or more optional substituents selected from hydroxy, C1-7 alkoxy, C5-20 aryloxy, C1-7 alkyl, carboxy, C1-7 alkyl ester and C5-20 aryl ester; RN1 and RN2 are independently selected from hydroxy, C1-7 alkoxy, C5-20 aryloxy, C1-7 alkyl, carboxy, C1-7 alkyl ester and C5-20 aryl ester; or RN1 and RN2 together with the pyridine rings to which they are bound form an tricyclic heteraromatic moiety, where the ring formed by RN1 and RN2 together may be optionally substituted by one or more substituents represented by RC3 selected from: hydroxy, C1-7 alkoxy, C5-20 aryloxy, C1-7 alkyl, carboxy, C1-7 alkyl ester and C5-20 aryl ester.
    • 用于治疗方法的式(I)的钌(II)化合物或其溶剂合物形式,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,C3-20杂环基,卤素,酯,酰氨基,酰基,磺基,亚磺酰氨基,醚,硫醚,偶氮和氨基,或R1和R2与它们所连接的环一起形成饱和或不饱和的碳环或杂环 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;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; Y是反抗; m为-1,0,1或2; q为1,2或3; RC1和RC2独立地表示选自羟基,C1-7烷氧基,C5-20芳氧基,C1-7烷基,羧基,C1-7烷基酯和C5-20芳基酯中的一个或多个任选的取代基; RN1和RN2独立地选自羟基,C1-7烷氧基,C5-20芳氧基,C1-7烷基,羧基,C1-7烷基酯和C5-20芳基酯; 或RN1和RN2与它们所连接的吡啶环一起形成三环杂芳基部分,其中由RN1和RN2一起形成的环可以任选地被一个或多个选自以下的RC 3所代表的取代基取代:选自:羟基,C 1-7烷氧基 ,C5-20芳氧基,C1-7烷基,羧基,C1-7烷基酯和C5-20芳基酯。