Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Andreas Ritzen"'
Autor:
Mogens Trolle Larsen, Venkatarathnam Reddy Nasipireddy, Martin A. Carnerup, Paola Lovato, Jimmi Gerner Seitzberg, Andreas Ritzen, Burhardt Mia Norreskov, Thomas Vifian, Anders Jerre, Tue Heesgaard Jepsen, Jens Christian Højland Larsen, Rikke Sindet, Sanjay Rai, Bettina Borreschmidt Hansen, Christina Mølck
Publikováno v:
Journal of medicinal chemistry. 63(13)
Herein, we report the discovery of a series of JAK1-selective kinase inhibitors with high potency and excellent JAK family subtype selectivity. A fragment screening hit 1 with a pyrazolopyridone core and a JAK1 bias was selected as the starting point
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::886914e454d2cc366a197455d0cf4752
https://pubmed.ncbi.nlm.nih.gov/32462873
https://pubmed.ncbi.nlm.nih.gov/32462873
Autor:
Pia Cwarzko Rummel, Mette M. Rosenkilde, Sahar Mirsharghi, Trond Ulven, Stefanie Thiele, Andreas Ritzen, Trine P Petersen
Publikováno v:
Petersen, T P, Mirsharghi, S, Rummel, P C, Thiele, S, Rosenkilde, M M, Ritzén, A & Ulven, T 2013, ' Multistep continuous-flow synthesis in medicinal chemistry : discovery and preliminary structure-activity relationships of CCR8 ligands ', Chemistry: A European Journal, vol. 19, no. 28, pp. 9343-9350 . https://doi.org/10.1002/chem.201204350
A three-step continuous-flow synthesis system and its application to the assembly of a new series of chemo- kine receptor ligands directly from commercial building blocks is reported. No scavenger columns or solvent switches are necessary to recover
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54188f329a3f5c7cd3279844759e3b32
https://doi.org/10.1002/chem.201204350
https://doi.org/10.1002/chem.201204350
Autor:
Andreas Ritzen, Christoffer Bundgaard, Farah Mohamed M, Claus Tornby Christoffersen, John Paul Kilburn, Morten Langgård, Jacob Nielsen, Jan Kehler, Sebastian Leth Petersen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3738-3742
Novel triazoloquinazolines have been found as phosphodiesterase 10A (PDE10A) inhibitors. Structure–activity studies improved the initial micromolar potency which was found in the lead compound by a 100-fold identifying 5-(1H-benzoimidazol-2-ylmethy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e9436fcf472e4b5503c730939b373fc8
https://doi.org/10.1016/j.bmcl.2011.04.067
https://doi.org/10.1016/j.bmcl.2011.04.067
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3407-3410
A series of metabotropic glutamate 5 receptor (mGluR5) allosteric ligands with positive, negative or no modulatory efficacy is described. The ability of this series to yield both mGluR5 PAMs and NAMs with single-digit nanomolar potency is unusual, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8240f41d29dcca0e37700b370af03a93
https://doi.org/10.1016/j.bmcl.2011.03.103
https://doi.org/10.1016/j.bmcl.2011.03.103
Autor:
Andreas Ritzen, Christoffer Bundgaard, Robbin Brodbeck, Rikke Sindet, Nannette Svendsen, Morten Hentzer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3275-3278
This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC(50)=30 nM) in vitro, and reaches high brain levels in both rats and mice after oral administ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::203a7eedf537646a5221f2061fac8287
https://doi.org/10.1016/j.bmcl.2009.04.095
https://doi.org/10.1016/j.bmcl.2009.04.095
Publikováno v:
Expert Opinion on Therapeutic Patents. 17:147-158
The discovery of the enzyme phosphodiesterase 10A (PDE10A) was reported simultaneously in 1999 by three independent groups. PDE10A has been shown by localisation studies to have the most restricted distribution of all the 11 known PDE families, with
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4b9b581a4649f25a874c18d339f441af
https://doi.org/10.1517/13543776.17.2.147
https://doi.org/10.1517/13543776.17.2.147
Autor:
Karl-Heinz Altmann, Kyriacos C. Nicolaou, J. Fernando Díaz, Kenji Namoto, Paraskevi Giannakakou, José Manuel Andreu, Andreas Ritzen, Markus Wartmann, Rubén M. Buey, Aurora O'Brate
Publikováno v:
Tetrahedron. 58:6413-6432
In addition to the total synthesis of the thiomethyl thiazole side chain analogue of epothilone B ( 3 ), a series of related trans -12,13-cyclopropyl epothilone B analogues ( 6 , 8 , 10 , 12 – 14 ) was accomplished. While the synthesis of the epoth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::50ea3887f1ca3de5e8db9902a716b53e
https://doi.org/10.1016/s0040-4020(02)00655-5
https://doi.org/10.1016/s0040-4020(02)00655-5
Publikováno v:
Petersen, T P, Larsen, A F, Ritzén, A & Ulven, T 2013, ' Continuous Flow Nucleophilic Aromatic Substitution with Dimethylamine Generated in Situ by Decomposition of DMF ', Journal of Organic Chemistry, vol. 78, no. 8, pp. 4190-4195 . https://doi.org/10.1021/jo400390t
A safe, practical, and scalable continuous flow protocol for the in situ generation of dimethylamine from DMF followed by nucleophilic aromatic substitution of a broad range of aromatic and heteroaromatic halides is reported.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::159ce6bb716530ad9e694b7e4570d27a
https://pubmed.ncbi.nlm.nih.gov/23506299
https://pubmed.ncbi.nlm.nih.gov/23506299
Publikováno v:
ChemInform. 32
The epothilones have occupied center stage on the scenes of total synthesis, chemical biology and medicine for the last five years, no doubt because of their intriguing mode of action and unusually high potency against tumor cells, including multidru
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b7bce983cc9f44d0572de9288299e83a
https://doi.org/10.1002/chin.200144258
https://doi.org/10.1002/chin.200144258
Autor:
Kenji Namoto, J. Fernando Díaz, Andreas Ritzen, Aurora O'Brate, José Manuel Andreu, Rubén M. Buey, Kyriacos C. Nicolaou, Markus Wartmann, Karl-Heinz Altmann, Paraskevi Giannakakou
Publikováno v:
ChemInform. 33
In addition to the total synthesis of the thiomethyl thiazole side chain analogue of epothilone B ( 3 ), a series of related trans -12,13-cyclopropyl epothilone B analogues ( 6 , 8 , 10 , 12 – 14 ) was accomplished. While the synthesis of the epoth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f6e119cd73f775986295d71deeb2fcf0
https://doi.org/10.1002/chin.200250201
https://doi.org/10.1002/chin.200250201