77898-35-2Relevant academic research and scientific papers
9-AZABICYCLO [3 . 3 . 1] NONANE DERIVATIVES AS MONOAMINE REUPTAKE INHIBITORS
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Page/Page column 37, (2010/11/26)
The present invention relates to a 9-azabicyclo[3.3.1]nonane derivative of formula (I), wherein R1 is H or C1-5alkyl; X is O or NR2, wherein R2 is H, C1-5alkyl or C2-5acyl and Ar is C6-10aryl or a 5-10 membered heteroaryl ring system, both being optionally substituted with one to three of R3-R5 independently selected from halogen, C1-5alkyl, C1-5alkoxy, C3-6cycloalkyl, C2-5alkenyl, C2-5alkynyl, CN, NO2, hydroxy, phenyl, phenoxy and phenylC1-2alkoxy, wherein said C1-5alkyl and C1-5alkoxy are optionally substituted with one to three halogens and wherein said phenyl, phenoxy and phenylC1-2alkoxy are optionally substituted with one to three substituents independently selected from halogen and methyl or two of R3-R5 at adjacent positions together form a methylenedioxy or propylene unit, with the proviso that the compounds exo-9-methyl-3-phenoxy-9-azabicyclo[3.3.1]nonane and N-(9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1H indazole-5-amine are excluded, or a pharmaceutically acceptable salt or solvate thereof. The invention also relates to pharmaceutical compositions comprising said 9-azabicyclo[3.3.1]nonane derivatives and to their use in therapy.
SUBSTITUTED 4-ALKOXYOXAZOL DERIVATIVES AS PPAR AGONISTS
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Page/Page column 27, (2010/02/07)
The present invention relates to compounds of formula (I) wherein R1 to R8 and n are as defined in the description and claims, and pharmaceutically acceptable salts and esters thereof. The compounds are useful for the treatment of diseases such as diabetes.
Benzothienyloxy phenylpropanamines, novel dual inhibitors of serotonin and norepinephrine reuptake
Boot,Brace,Delatour,Dezutter,Fairhurst,Findlay,Gallagher,Hoes,Mahadevan,Mitchell,Rathmell,Richards,Simmonds,Wallace,Whatton
, p. 5395 - 5399 (2007/10/03)
A series of benzothienyloxy phenylpropylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake. A series of benzothienyloxy propylamines have been prepared and are demonstrated to be inhibitors of both serotonin and norepinephrine reuptake.
3-ARYLOXY/ THIO-2, 3-SUBSTITUTED PROPANAMINES AND THEIR USE IN INHIBITING SEROTONIN AND NOREPINEPHRINE REUPTAKE
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Page 54, (2010/02/07)
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, C1-C4 alkyl and C1-C4 alkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C1-C4 alkyl, and C2-C8 alkyl, C2-C8 alkenyl, C3-C8 cycloalkyl and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, -CF3, -CN and -CONH2; 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, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n- where n is 0, 1 or 2, nitro, acetyl, -CF3, -SCF3 and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1-C4 alkyl; Z is selected from OR3 or F, wherein R3 is selected from H, C1-C6 alkyl and phenyl C1-C6 alkyl; R1 and R2 are each independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereofwith the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is OR3 and X is optionally substituted phenyl then A is -S-.
Studies in sulfur heterocycles. Part 12. Use of 5,6-dihydrobenzo[b]-thiophen-7(4H)-one in the synthesis of condensed sulfur heterocycles
Samanta, Subhendu Sekhar,Ghosh, Sukhen Chandra,De, Asish
, p. 3673 - 3677 (2007/10/03)
Readily available 5,6-dihydrobenzo[b]thiophen-7(4H)-one has been used as a convenient intermediate for the synthesis of several condensed heterocyclic systems and substituted benzo[b]thiophenes.
Studies in sulfur heterocycles. Part 13. An expedient synthesis of 7-hydroxybenzo[b]thiophene and its 2- and 3-substituted derivatives
Samanta, Subhendu Sekhar,Ghosh, Sukhen Chandra,De, Asish
, p. 2683 - 2685 (2007/10/03)
Two expedient routes to 7-hydroxybenzo[b]thiophene and its 2- and 3-substituted derivatives from readily available starting materials are described which constitute a vast improvement over the known methods of synthesis.
7-Substituted Benzothiophenes and 1,2-Benzisothiazoles. Part 1. Hydroxy- or Methoxy-derivatives
Rahman, Loay K. A.,Scrowston, Richard M.
, p. 2973 - 2978 (2007/10/02)
Readily available 2-hydroxy-3-methoxybenzaldehyde (orthovanilin) is converted, via terminal rearrangement (Newman-Kwart) of the O-aryl-NN-dimethylthiocarbamate, into 2-mercapto-3-methoxybenzaldehyde (3).This thiol undergoes base-catalysed condensation wit
