- SPIRO COMPOUND AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR
-
Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.
- -
-
-
- Cyclobutane-derived diamines: Synthesis and molecular structure
-
Cyclobutane diamines (i.e., cis- and trans-1,3-diaminocyclobutane, 6-amino-3-azaspiro[3.3]heptane, and 3,6-diaminospiro[3.3]heptane) are considered as promising sterically constrained diamine building blocks for drug discovery. An approach to the syntheses of their Boc-monoprotected derivatives has been developed aimed at the preparation of multigram amounts of the compounds. These novel synthetic schemes exploit classical malonate alkylation chemistry for the construction of cyclobutane rings. The conformational preferences of the cyclobutane diamine derivatives have been evaluated by X-ray diffraction and compared with the literature data on sterically constrained diamines, which are among the constituents of commercially available drugs.
- Radchenko, Dmytro S.,Pavlenko, Sergiy O.,Grygorenko, Oleksandr O.,Volochnyuk, Dmitriy M.,Shishkina, Svitlana V.,Shishkin, Oleg V.,Komarov, Igor V.
-
scheme or table
p. 5941 - 5952
(2010/11/04)
-
- Synthesis of conformationally restricted glutamic acid analogs based on the spiro[3.3]heptane scaffold
-
A library of isomeric glutamic acid analogs based on the spiro[3.3]heptane skeleton is designed. Two members of the library, (R)- and (S)-2-amino-spiro[3.3]heptane-2,6-dicarboxylic acid hydrochlorides, were synthesized. The stereochemistry of the synthesi
- Radchenko, Dmytro S.,Grygorenko, Oleksandr O.,Komarov, Igor V.
-
experimental part
p. 2924 - 2930
(2009/07/04)
-