225517-15-7Relevant articles and documents
IMIDAZOPYRIDAZINES AS MODULATORS OF IL-17
-
Page/Page column 212-213, (2021/11/06)
The present application discloses compounds having the following formula: (I), or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
-
Paragraph 00384; 00387; 00388, (2017/09/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
NOVEL INHIBITORS
-
Page/Page column 70; 71; 102; 130; 131, (2014/09/29)
The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N- terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS
-
Page/Page column 23, (2009/04/25)
The present invention is directed to therapeutic compounds which have dual activity as agonists of GPR119 and inhibitors of DPP-IV and are useful for the treatment of metabolic disorders including type II diabetes.
INHIBITORS OF IAP
-
Page/Page column 106-107, (2008/12/08)
The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1 - M - U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3', R4, R4' and R5, are as described herein.
Suppression of racemization in the carbonylation of amino acid-derived aryl triflates
Grimm, Jonathan B.,Wilson, Kevin J.,Witter, David J.
, p. 4509 - 4513 (2008/02/03)
The carbonylation of enantiopure phenylglycine-derived aryl triflates was achieved to afford 4-carboxyphenylglycine analogs with high enantiomeric excesses (88 to >99% ee). Amide analogs of phenylglycine were well-tolerated in the hydroxy- and methoxycarbonylation processes, providing efficient access to benzoic acid and ester building blocks. The % ee of the product was dependent on the relative steric bulk of both the amino acid substrate and the requisite amine base, with iPr2NEt proving optimal in minimizing product racemization.
Chiral borromeates
Pentecost, Cari D.,Peters, Andrea J.,Chichak, Kelly S.,Cave, Gareth W. V.,Cantrill, Stuart J.,Stoddart, J. Fraser
, p. 4099 - 4104 (2007/10/03)
The fellowship of the rings: Circular dichroism measurements reveal that chirality is transferred from 12 stereogenic centers to 6 octahedral zinc(II) centers (see picture) in two enantiomeric pairs of chiral Borromeates, one of which has been found to be
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors
Parmee, Emma R.,He, Jiafang,Mastracchio, Anthony,Edmondson, Scott D.,Colwell, Larry,Eiermann, George,Feeney, William P.,Habulihaz, Bahanu,He, Huaibing,Kilburn, Ruth,Leiting, Barbara,Lyons, Kathryn,Marsilio, Frank,Patel, Reshma A.,Petrov, Aleksandr,Di Salvo, Jerry,Wu, Joseph K.,Thornberry, Nancy A.,Weber, Ann E.
, p. 43 - 46 (2007/10/03)
Substituted 4-amino cyclohexylglycine analogues were evaluated for DP-IV inhibitory properties. Bis-sulfonamide 15e was an extremely potent 2.6 nM inhibitor of the enzyme with excellent selectivity over all counterscreens. 2,4-Difluorobenzenesulfonamide 1
The anandamide membrane transporter. Structurea€"activity relationships of anandamide and oleoylethanolamine analogs with phenyl rings in the polar head group region
Di Marzo, Vincenzo,Ligresti, Alessia,Morera, Enrico,Nalli, Marianna,Ortar, Giorgio
, p. 5161 - 5169 (2007/10/03)
A new series of arachidonic and oleic acids derivatives, most of which with aromatic moieties in the head group region, has been synthesized and evaluated as inhibitors of anandamide uptake. A new series of anandamide and N-oleoylethanolamine analogs, most of which with aromatic moieties in the head group region, has been synthesized and evaluated as inhibitors of anandamide uptake. Some of them efficaciously inhibit the uptake process with Ki values in the low micromolar range (2.4-21.2 μM). Strict structural requisites are needed to observe a significant inhibition and in no case inhibition of fatty acid amidohydrolase overlaps with inhibition of anandamide uptake.
Ring-closing metathesis for the synthesis of side chain knotted pentapeptides inspired by vancomycin
Ten Brink, Hefziba T.,Rijkers, Dirk T.S.,Kemmink, Johan,Hilbers, Hans W.,Liskamp, Rob M.J.
, p. 2658 - 2663 (2007/10/03)
A versatile method for the synthesis of bicyclic side chain knotted peptides inspired by vancomycin is described. The synthetic approach is based on the incorporation of a central amino acid derivative 3 having two allylic groups - introduced by a Stille
