4068-68-2Relevant academic research and scientific papers
BENZO-FUSED HETEROCYCLIC DERIVATIVES USEFUL AS AGONISTS OF GPR120
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Paragraph 0871, (2014/09/30)
The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
BENZOFURAN COMPOUNDS
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Page/Page column 38, (2008/12/08)
A compound of formula (I), wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions comprising such compounds and the use of such compounds in
Substituted benzamides and radioligand analogs and methods of use
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, (2008/06/13)
This invention provides compounds of the formula I STR1 wherein, R1, R2, and R3 are independently ?a first halogen atom,! fluorine, chlorine, bromine, iodine, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, or alkynoxy, wherein R2 and R3 can also independently be H, wherein at least one of R1, R2, and R3 is ?a second halogen atom! fluorine, bromine, iodine or is substituted with ?a second halogen atom,! fluorine, bromine or iodine and R4 is H or lower alkyl. The invention also provides precursors of formula I, radioactive analogs of formula I, and methods of using the compounds for the identification of 5-HT-3 receptors and the detection and treatment of abnormal conditions associated therewith.
Labeling of (S)-des-4-amino-3-[125I]iodozacopride (DAIZAC), a high-affinity radioligand for the 5-HT-3 receptor
Mason,Hewlett,Ebert,Schmidt,De Paulis
, p. 955 - 961 (2007/10/03)
We have prepared (S)-5-chloro-3-[125I]iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl) -benzamide ([125I]DAIZAC, [125I]-3) as a radioligand for characterization of the 5-HT-3 receptor. Preparation of the 3-tri-n-butylstannyl precursor was accomplished from the corresponding unlabeled DAIZAC by reaction with bis(tributyltin). Treatment of the precursor with 5 mCi of Na125I and chloramine-T in dilute HCl gave 2.58 ± 0.22 mCi (52%) of [125I]DAIZAC with >98% radiochemical purity and 1500 Ci/mmol specific activity. Saturation analysis of the binding of [125I]DAIZAC to rat brain homogenates showed a single binding site with a receptor density B(max) of 0.66 ± 0.03 pmol/g and a receptor affinity K(D) of 0.15 ± 0.01 nM. Compared to [125I]iodozacopride, we find the 20-fold higher affinity and easy preparation of [125I]DAIZAC to be advantageous for in vitro identification of brain 5-HT-3 receptors.
Process for preparing dibenzofurans via catalytic heteroannulation
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, (2008/06/13)
The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxylic acid by a stereospecific catalytic heteroannulation synthesis free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydr
Process for preparing chiral dibenzofurans via intramolecular heck reaction
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, (2008/06/13)
The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxylic acid by an intramolecular Heck stereospecific synthesis substantially free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-t
