摘要:
The present invention provides a novel class of compounds that have the activity of inhibiting HSP90 enzyme and are useful as anti-cancer agents or such, and compounds that are useful as synthetic intermediates thereof. Specifically, the present invention provides compounds represented by the following formula (1), and pharmaceutically acceptable salts thereof:
wherein X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , L 1 , L 2 , and L 3 are as defined in the specification.
摘要:
Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bicyclo-[2,2,3]-nonanes, having 2 or 3 ring hetero atoms selected from O, S and N substituted at the 1-position by a carbocyclic group other than an alkynylphenyl group, and substituted at the 4-position and optionally substituted at the 3 and/or 5 position, are valuable pesticides, particularly insecticides and acaracides. Various cyclisation processes are disclosed to form the various bicyclo ring systems.
摘要:
The present invention provides novel compounds of the formula (I): wherein R is a phenyl group, substituted by 1 to 5 fluorine atoms and optionally substituted at the para position by methyl or chloro or R is a group being a three of four membered ring, where R⁴ is oxygen or a group CR⁷R⁸ wherein groups R⁷, R⁸ are the same or different and each is hydrogen, fluoro, chloro or bromo or methyl or ethyl optionally substituted by 1 to 3 fluoro atoms, and when is a three-membered ring R⁵ is a group CR 7a R 8a wherein R 7a , R 8a are the same or different and each is hydrogen, fluoro, chloro or bromo or methyl or ethyl optionally substituted by 1 to 3 fluoro atoms, or when is a four membered ring R⁵ is a group CR 7a R 8a CR⁹R¹⁰ wherein R 7a , R 8a are as hereinbefore defined and R⁹ and R¹⁰ are the same or different and each is hydrogen, fluoro, chloro or bromo or methyl or ethyl optionally substituted by 1 to 3 fluoro atoms; R⁶ is hydrogen, fluoro, chloro or methyl; R¹ and R² may be the same or different, and each is hydrogen, halo, or a C₁₋₃ aliphatic group optionally substituted by halo, cyano, C₂₋₅ carbalkoxy, C₁₋₄ alkoxy, or a group S(O) m R¹¹ wherein m is 0, 1 or 2 and R¹¹ is C₁₋₄ alkyl; cyano, gem dimethyl, or C₂₋₅ carbalkoxy; R³ contains between 3 and 18 carbon atoms and is a group R¹² wherein R¹² is a C₁₋₁₃ non-aromatic hydrocarbyl group, optionally substituted by a C₂₋₄ carbalkoxy or cyano group and/or by one or two hydroxy groups and/or by one to five halo atoms which are the same or different and/or by one to three groups R¹³ which are the same or different and each contains one to four hetero atoms, which are the same or different and are chosen from oxygen, sulphur, nitrogen and silicon, 1 to 10 carbon atoms and optionally 1 to 6 fluoro or chloro atoms or R³ is a 6-membered aromatic ring substituted by cyano and/or by one to five halo atoms and/or by one to three C₁₋₄ haloalkyl groups and/or by a group -C≡CH, C≡C-halo or -C≡C-R¹² wherein R¹² is as hereinbefore defined or -C≡C-R¹⁴ wherein R¹⁴ is a group S(O) q R¹⁵ wherein R¹⁵ is methyl, ethyl or trifluoromethyl or R¹⁴ is SiR¹⁶R¹⁷R¹⁸ wherein R¹⁶ and R¹⁷ are the same or different and are each C₁₋₄ aliphatic groups and R¹⁸ is a C₁₋₄ aliphatic group or phenyl provided that R¹⁶, R¹⁷ and R¹⁸ do not contain more than 10 carbon atoms in total; and Y, Y¹ and Y² are the same or different and are each selected from oxygen and S(O) t where t is 0, 1 or 2, processes for their preparation, formulations containing them and their use in controlling pest infestation.
摘要翻译:本发明提供新的式(I)化合物:其中R为苯基,被1至5个氟原子取代,并且在对位被甲基或氯取代,或R为基团CHEM 其中R 4为氧或基团CR 7 R 8,其中基团R 7,R 8相同或不同,各自为氢,氟,氯或 溴或甲基或乙基,其任选被1至3个氟原子取代,当为三元环时,R 5为基团CR 7a R 8a,其中R 7a,R 8a, 各自为氢,氟,氯或溴或任选被1至3个氟原子取代的甲基或乙基,或当为四元环时R 5为基团CR 7a 其中R 7a,R 8a如上所定义,R 9和R 1相同或不同,各自为氢 氟,氯或溴或任选被1至3个氟原子取代的甲基或乙基; R 6是氢,氟,氯或甲基; R 1和R 2可以相同或不同,各自为氢,卤素或任选被卤素,氰基,C 2-5烷氧基,C 1-4烷氧基或基团取代的C 1-3脂族基团 S(O)m R 1,其中m为0,1或2,R 1为C 1-4烷基; 氰基,二甲基或C 2-5烷氧基; R 3含有3至18个碳原子,并且是基团R 1,其中R 1 2是C 1-13非芳族烃基,任选被C 2-4烷氧基取代或 氰基和/或一个或两个羟基和/或一至五个相同或不同的卤素原子和/或一至三个相同或不同的基团R 1,3各自包含 1至4个相同或不同的杂原子,选自氧,硫,氮和硅,1至10个碳原子和任选1至6个氟或氯原子或R 3为6元芳环 被氰基和/或一至五个卤素原子和/或一至三个C 1-4卤代烷基和/或被基团取代-C取代基C,C-C或卤代C 1 -C 2烷基 其中R 1'如上文所定义或-C元素CR 1其中R 1是S(O)q R 5基团,其中R 1是 > 5是甲基,乙基或三氟甲基,或者R 1是SiR 1 R 6 R 7 R 8其中R 1和R 2都是R <1> <7> R 1相同或不同,并且各自为C 1-4脂族基团,并且R 1'为C 1-4脂族基团或苯基,条件是R 1,R 2,R 1, 总共不含10个以上碳原子; Y,Y 1和Y 2相同或不同,各自选自氧和S(O)t,其中t为0,1或2,其制备方法,含有它们的制剂及其用途 防治虫害。
摘要:
The present invention provides a class of novel substituted bicyclooctanes which have pesticidal activity, particularly against arthropod pests. Pesticidal formulations containing the compounds of the formula (I), their use in the control of pests and methods for their preparation are also disclosed.
摘要:
Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bi- cyclo-[2,2,3]-nonanes having 2 or 3 ring hetero atoms selected from 0, S and N, substituted at the 1-position by a 4-alkynylphenyl group and at the 4-position and optionally at the 3 and/or 5-position are valuable pesticides, particularly insecticides and acaracides. The compounds may be prepared by reacting an alkyne with the corresponding 4- iodophenyl substituted compound or by debromination of the corresponding 4-dibrom- omethylphenyl substituted compound.
摘要:
The present invention relates to a process for producing predominantly pure cis nucleoside analogues using a novel bicyclic intermediate of formula (III), wherein X is S, or O; Y is S, CH2, O or CH(R); wherein R is azido or halogen; and Z is S or O.