On March 24, 2016, Semeraro, Teresa; Tarsi, Luca; Micheli, Fabrizio; Luker, Tim; Cremonesi, Susanna published a patent.Category: esters-buliding-blocks The title of the patent was Preparation of 2-[bis(4-fluorophenyl)methyl]-2,7-diazaspiro[4.5]decan-10-one derivatives useful as inhibitors of human dopamine active transporter (DAT) protein. And the patent contained the following:
The invention relates to compounds of formula I, and in particular 2-[bis(4-fluorophenyl)methyl]-2,7-diazaspiro[4.5]decan-10-one derivatives and related compounds, method for their preparation and their use as inhibitors of human dopamine active transporter (DAT) protein for the treatment of sexual dysfunction, affective disorders, anxiety, depression, attention deficit hyperactivity disorder (ADHD), obesity, etc. Compounds of formula I, wherein Q is C=NOH, NH, Ncycloalkyl, etc.; X is CO, NH, Nalkyl, etc.; Y is O, SO0-2, Nalkyl, etc.; Z is O, S and CR11R12; A is (CHR5R6)0-2; B is (CR1R2)0-2; M is (R9R10)0-2; R1 and R2 are independently H, OH, F, alkyl, etc., or R1R2 together form =O; R3, R4, R7 and R8 are independently H, OH, alkoxy and alkyl, or R3 and R4, R7 and R8 may both be O, wherein said O atoms are linked by an alkylene group to form a straight chain or branched alkylenedioxy group; R5 and R6 are independently H and alkyl, or R5 and R6 from =O; R13 is substituted phenyl; R14 is (un)substituted phenyl; R9, R10, R11 and R12 are independently H and alkyl, are claimed. Example compound II was prepared by a multistep procedure (procedure given). All the invention compounds were evaluated for their affinity to the human transporters DAT, NET, SERT and hERG. From the assay, it was determined that example compound II exhibited pIC50 value of 6.89, 5.42, 4.65 and 5.7 towards human transporters DAT, NET, SERT and hERG resp. The experimental process involved the reaction of tert-Butyl 1-oxo-2,9-diazaspiro[5.5]undecane-9-carboxylate(cas: 1198284-94-4).Category: esters-buliding-blocks
The Article related to bisfluorophenylmethyldiazaspirodecanone preparation human dopamine active transporter inhibitor, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: esters-buliding-blocks
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