- Design and synthesis of APTCs (aminopyrrolidinetricarboxylic acids): Identification of a new group III metabotropic glutamate receptor selective agonist
-
A new family of mGlu receptor orthosteric ligands called APTCs was designed and synthesized using a parallel chemistry approach. Amongst 65 molecules tested on mGlu4, mGlu6 and mGlu8 subtypes, (2S,4S)-4-amino-1-[(E)-3-carboxyacryloyl]pyrrolidine-2,4-dicar
- Schann, Stephan,Menet, Christel,Arvault, Paul,Mercier, Geraldine,Frauli, Melanie,Mayer, Stanislas,Hubert, Nadia,Triballeau, Nicolas,Bertrand, Hugues-Olivier,Acher, Francine,Neuville, Pascal
-
p. 4856 - 4860
(2007/10/03)
-
- TRANS PYRROLIDINYL DERIVATIVES AND THEIR PHARMACEUTICAL USE
-
The present invention relates to the use of trans pyrrolidinyl of the formula (I) or (II) in which: R1, R2or R3 are hydrogen or a carboxy or amino protecting group; R4 to R8 represent hydrogen or an a
- -
-
Page/Page column 41; 42-43
(2010/02/15)
-
- Pyrrolidinyl di-carboxylic acid derivatives as metabotropic glutamate receptor antagonists
-
The present invention provides pyrrolidinyl di-carboxylic acid derivatives that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders. This invention further provides novel pyrr
- -
-
-
- Synthesis of the four isomers of 4-aminopyrrolidine-2,4-dicarboxylate: Identification of a potent, highly selective, and systemically-active agonist for metabotropic glutamate receptors negatively coupled to adenylate cyclase
-
The four isomers of 4-aminopyrrolidine-2,4-dicarboxylate (APDC) were prepared and evaluated for their effects at glutamate receptors in vitro. (2R,4R)-APDC (2a), an aza analog of the nonselective mGluR agonist (1S,3R)- 1-aminocyclopentane-1,3-dicarboxylat
- Monn, James A.,Valli, Matthew J.,Johnson, Bryan G.,Salhoff, Craig R.,Wright, Rebecca A.,Howe, Trevor,Bond, Ann,Lodge, David,Spangle, Larry A.,Paschal, Jonathan W.,Campbell, Jack B.,Griffey, Kelly,Tizzano, Joseph P.,Schoepp, Darryle D.
-
p. 2990 - 3000
(2007/10/03)
-
- PYRROLIDINYL DI-CARBOXYLIC ACID DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS
-
The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
- -
-
-
- Asymmetric syntheses of all four isomers of 4-amino-4-carboxyproline: Novel conformationally restricted glutamic acid analogues
-
Asymmetric syntheses of all four isomers of 4-amino-4-carboxyprolines, i.e. (2S,4S)-3, (2S,4R)-4, and their corresponding enantiomers, as novel conformationally restricted analogues of glutamic acid, were performed from trans-4-hydroxy-L-proline as a homochiral starting material. The key step was the spirohydantoin ring formation by employing the Bucherer-Bergs reaction of 4-oxoproline derivatives. These structures were determined by NMR studies.
- Tanaka,Sawanishi
-
p. 1641 - 1656
(2007/10/02)
-