206446-44-8Relevant articles and documents
NEW HETEROCYCLIC COMPOUNDS
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Page/Page column 67; 142, (2019/06/17)
The invention provides new heterocyclic compounds having the general formula (IA) wherein A, L, X, Y, m, n, R1 and R2 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.
An improved, gram-scale synthesis of protected 3-haloazetidines: Rapid diversified synthesis of azetidine-3-carboxylic acids
Ji, Youngran,Wojtas, Lukasz,Lopchuk, Justin M.
, p. 195 - 214 (2018/06/27)
Azetidines are increasingly important heterocycles found in a variety of natural products and pharmaceutical compounds. Protected 3-haloazetidines, widely used and versatile building blocks in medicinal chemistry, have been prepared in a one-pot, gram-scale strain-release reaction of 1-azabicyclo[1.1.0]butane from commercially available starting materials. These intermediates were subsequently used to prepare a series of high value azetidine-3-carboxylic acid derivatives including the first reported synthesis of 1-(tert-butoxy-carbonyl)-3-((trifluoromethyl)thio)azetidine-3-carboxylic acid. (Figure pressented)
Novel GlyT1 inhibitor chemotypes by scaffold hopping. Part 2: Development of a [3.3.0]-based series and other piperidine bioisosteres
Sheffler, Douglas J.,Nedelovych, Michael T.,Williams, Richard,Turner, Stephen C.,Duerk, Brittany B.,Robbins, Megan R.,Jadhav, Sataya B.,Niswender, Colleen M.,Jones, Carrie K.,Conn, P. Jeffrey,Daniels, R. Nathan,Lindsley, Craig W.
, p. 1062 - 1066 (2014/03/21)
This Letter describes the development and SAR of a novel series of GlyT1 inhibitors derived from a scaffold hopping approach, in lieu of an HTS campaign, which provided intellectual property position. Members within this new [3.3.0]-based series displayed excellent GlyT1 potency, selectivity, free fraction, and modest CNS penetration. Moreover, enantioselective GlyT1 inhibition was observed, within this novel series and a number of other piperidine bioisosteric cores.
PYRAZOLE CARBOXAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Page/Page column 65, (2014/03/21)
Provided herein are compounds of formula (AA): N N H HN O N N R R 6 A (R a ) p, (AA) stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, R a, p, R and R 6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.
SULFONYL-AZETIDIN-3-YL-METHYLAMINE AMIDE ANALOGS AS GLYT1 INHIBITORS, METHODS FOR MAKING SAME, AND USE OF SAME IN TREATING PSYCHIATRIC DISORDERS
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Page/Page column 53; 86, (2010/11/03)
In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GIyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GIyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Synthesis of C-substituted cyclic amines using azacycloalkyl organozinc reagents
Billotte
, p. 379 - 380 (2007/10/03)
Azetidine and piperidine derived organozinc species have been prepared from the corresponding azacycloalkyl iodides by direct Zn insertion. They have been shown to readily undergo Pd(0) mediated cross-coupling reactions and to transmetallate with CuCN.2LiCl.
