Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Frank Himmelsbach"'
Autor:
Bradford S. Hamilton, Frank Himmelsbach, Barbara A. Kruk, Joan Guo, Gerard McGeehan, Peter Lindblom, Rong Guo, Colin M. Tice, Brian M. McKeever, Linghang Zhuang, David A. Claremon, Judith A. Johnson, Katerina Leftheris, Lamont Howard, Salvacion Cacatian, Heike Schauerte, Annette Schuler-Metz, Richard Gregg, Reshma Panemangalore, Deepak S. Lala, Paula Krosky, Zhenrong Xu, Yuri Bukhtiyarov, Suresh B. Singh, Yuanjie Ye, Yi Zhao, Wei Zhao, Shi Meng
Publikováno v:
Bioorganicmedicinal chemistry. 25(14)
A potent, in vivo efficacious 11β hydroxysteroid dehydrogenase type 1 (11β HSD1) inhibitor (11j) has been identified. Compound 11j inhibited 11β HSD1 activity in human adipocytes with an IC50 of 4.3nM and in primary human adipose tissue with an IC
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::307a3ef85dcc22b2889fcf6062c9a383
https://pubmed.ncbi.nlm.nih.gov/28528082
https://pubmed.ncbi.nlm.nih.gov/28528082
Autor:
Nitinchandra D. Patel, Xudong Wei, Nizar Haddad, Marisa C. Kozlowski, Jon C. Lorenz, Frank Himmelsbach, Nathan K. Yee, Zhulin Tan, Scot Campbell, Sergei Tcyrulnikov, Jun Wang, Chris H. Senanayake, Jean-Nicolas Desrosiers, Stefan Peters, Xingzhong Zeng, Maurice A. Marsini, Frederic G. Buono, Zhibin Li, Jolaine Savoie, Frank Roschangar, Bing-Shiou Yang, Keith R. Fandrick, Matthias Eckhardt, Heewon Lee, Wenjun Tang, Bo Qu, Jinhua J. Song, Shengli Ma, Osvaldo Gutierrez
Publikováno v:
Journal of the American Chemical Society. 138(47)
A concise asymmetric synthesis of an 11β-HSD-1 inhibitor has been achieved using inexpensive starting materials with excellent step-economy at low catalyst loadings. The catalytic enantioselective total synthesis of 1 was accomplished in 7 steps and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e285888aca8830b44533bbbd1d3dd5d9
https://pubmed.ncbi.nlm.nih.gov/27794616
https://pubmed.ncbi.nlm.nih.gov/27794616
Autor:
Achim Sauer, Michael Mark, D. E. Sharp, Peter Eickelmann, Leo Thomas, Frank Himmelsbach, Remko A. Bakker, Matthias Eckhardt, Rolf Grempler, Thomas Klein
Publikováno v:
Diabetes, Obesity and Metabolism. 14:83-90
Aims: Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor in clinical development for the treatment of type 2 diabetes mellitus. This study assessed pharmacological properties of empagliflozin in vitro and pharmacokinetic p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::98b7e4284afa95fd19fe39775539856c
https://doi.org/10.1111/j.1463-1326.2011.01517.x
https://doi.org/10.1111/j.1463-1326.2011.01517.x
Autor:
Frank Himmelsbach, Ralf Lotz, Moh Tadayyon, Elke Langkopf, Herbert Nar, Norbert Hauel, Leo Thomas, Matthias Eckhardt, Michael Mark, Brian Guth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3158-3162
Systematic variations of the xanthine scaffold in close analogs of development compound BI 1356 led to the class of 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones which provided, after substituent screening, a series of highly potent DPP-4 inhibitors.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::03b59de9fefdb0ce2e2888c2d4574bfc
https://doi.org/10.1016/j.bmcl.2008.04.075
https://doi.org/10.1016/j.bmcl.2008.04.075
Autor:
Shigeto Kubo, Anke Baum, Lauren Ambrogio, Wolfgang J. Rettig, Heidi Greulich, F. Solca, Geoffrey I. Shapiro, Frank Himmelsbach, Takeshi Shimamura, Masaya Takahashi, Robert F. Padera, Matthew Meyerson, Lucian R. Chirieac, Daizong Li, K-K Wong
Publikováno v:
Oncogene. 27:4702-4711
Genetic alterations in the kinase domain of the epidermal growth factor receptor (EGFR) in non-small cell lung cancer (NSCLC) patients are associated with sensitivity to treatment with small molecule tyrosine kinase inhibitors. Although first-generat
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aacb58a7f728b04ce1e8e2a39c122d8d
https://doi.org/10.1038/onc.2008.109
https://doi.org/10.1038/onc.2008.109
Publikováno v:
Tetrahedron Letters. 49:1931-1934
Two synthetic routes to the versatile 3,5-dihydro-imidazo[4,5-d]pyridazin-4-ones 2 and 5 have been developed that allow the production of multigram quantities without the need of any chromatographic purification. Broad and selective elaboration of th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e7335322c41a8553b0ba400157a62082
https://doi.org/10.1016/j.tetlet.2008.01.102
https://doi.org/10.1016/j.tetlet.2008.01.102
Autor:
Matthias Eckhardt, Michael Mark, Rolf Grempler, Leo Thomas, Frank Himmelsbach, Achim Sauer, Peter Eickelmann, Thomas Klein
Publikováno v:
Diabetes, Obesity and Metabolism. 14:94-96
Empagliflozin is a potent, selective sodium glucose co-transporter-2 inhibitor that is in development for the treatment of type 2 diabetes. This series of studies was conducted to assess the in vivo pharmacological effects of single or multiple doses
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f7eee104cb1214d888ce4cc32331df9
https://doi.org/10.1111/j.1463-1326.2011.01518.x
https://doi.org/10.1111/j.1463-1326.2011.01518.x
Autor:
Holger Lang, Margarete Gottlieb, Frank Himmelsbach, Wolfgang Pfleiderer, Ramamurthy Charubala, Michael Schwarz, Silke Farkas, Bernd S. Schulz
Publikováno v:
Helvetica Chimica Acta. 82:2172-2185
A series of new base-protected and 5′-O-(4-monomethoxytrityl)- or 5′-O-(4,4′-dimethoxytrityl)-substituted 3′-(2-cyanoethyl diisopropylphosphoramidites) and 3′-[2-(4-nitrophenyl)ethyl diisopropylphosphoramidites] 52 – 66 and 67 – 82, res
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8ecc112feb0b897ec5efee427dc33261
https://doi.org/10.1002/(sici)1522-2675(19991215)82:12<2172::aid-hlca2172>3.0.co
https://doi.org/10.1002/(sici)1522-2675(19991215)82:12<2172::aid-hlca2172>3.0.co
Autor:
Elke Dipl Biol Seewaldt-Becker, Hans Weisenberger, Thomas Muller, Brian Guth, Frank Himmelsbach
Publikováno v:
Journal of Cardiovascular Pharmacology. 30:261-272
The glycoprotein (GP) IIb/IIIa (the alphallb beta3 integrin) found on platelets binds fibrinogen or von Willebrand factor when the platelet is activated, thereby mediating the aggregation of platelets. Blockade of the GPIIb/IIIa should prevent platel
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92246be9594d7c95f780cd91c43d221f
https://doi.org/10.1097/00005344-199708000-00017
https://doi.org/10.1097/00005344-199708000-00017
Autor:
Göran Dahl, Oliver Kraemer, Christian Klein, Eric E. J. Haaksma, Guenther Adolf, Michael P. Sanderson, Frank Himmelsbach, Gerd Bader, Flavio Solca, Andreas Zoephel
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 343(2)
Deregulation of the ErbB (proto-oncogene B of the avian erythroblastosis virus AEV-H strain) receptor network is well recognized as an oncogenic driver in epithelial cancers. Several targeted drugs have been developed, including antibodies and small-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8557342474469bf973348cccde09b2e5
https://pubmed.ncbi.nlm.nih.gov/22888144
https://pubmed.ncbi.nlm.nih.gov/22888144