摘要:
The present invention relates to the scaled-up synthesis of biologically active compounds which display useful therapeutic activity in treating proliferative disorders. In particular the invention relates to process methods for the kilogram scale synthesis of a particular class of substituted benzofuran tubulin polymerisation inhibitors.
摘要:
A cannabinoid receptor modulator which contains a compound represented by the formula (I0): (I0) (wherein X represents oxygen, etc.; R represents optionally substituted acylamino; ring A represents a benzene ring optionally having a substituent besides R ; and ring B represents optionally substituted five-membered heterocycle), a salt of the compound, or a prodrug of either.
摘要翻译:含有由式(I0)表示的化合物:(I0)(其中X表示氧等)的大麻素受体调节剂; R 0表示任选取代的酰氨基;环A 0表示任选具有取代基的苯环 除了R 0之外,环B表示任选取代的五元杂环),化合物的盐或其前体药物。
摘要:
There is provided a compound of formula (I) wherein A is selected from -O- and -S-; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C 1 -C 4 alkyl and C 1 -C 4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C 1 -C 4 alkyl, and C 2 -C 8 alkyl, C 2 -C 8 alkenyl, C 3 -C 8 cycloalkyl and C 4 -C 8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl-S(O)n- where n is 0, 1 or 2, -CF 3 , -CN and -CONH 2 ; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF 3 , -SCF 3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C 1 -C 4 alkyl; Z is selected from OR 3 or F, wherein R 3 is selected from H, C 1 -C 6 alkyl and phenyl C 1 -C 6 alkyl; R 1 and R 2 are each independently H or C 1 -C 4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR 3 and X is optionally substituted phenyl then A is -S-.
摘要:
The invention relates to compounds of the general formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 8’ , R 9 , W, a, b and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.
摘要:
The invention relates to novel benzofuran derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as anti-infectives.
摘要:
A novel compound represented by general formula (I), having a potent TXA2 receptor antagonism and a PGI2 receptor agonism, and being useful in the treatment and prevention of diseases in which TXA2 participates. In said formula, the meaning of each symbol is as defined in the specification.
摘要:
Serine hydrolases are implicated in malconditions such as cancer, central nervous system disorders, cardiovascular disorders, obesity, and metabolic disorders. Many serine hydrolases expressed in proteomic libraries are of unknown function in vivo. Compounds identified through library versus library screening can be used for treatment of malconditions associated with the specific serine hydrolase KIAA1363 (also known as AADACL1). A library of inhibitors of KIAA1363 was prepared and candidate compounds were identified as a potent inhibitors having submicromolar IC 50 values. An exemplary compound of the invention was shown to be an effective inhibitor of prostate cancer pathogenesis. Other inhibitory compounds of the invention comprising fluorophore groups are shown to be effective in spatial and temporal localization of the serine hydrolase in cells and tissues.