784-77-0Relevant academic research and scientific papers
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5
Nguyen, Duy,Lemos, Clara,Wortmann, Lars,Eis, Knut,Holton, Simon J.,Boemer, Ulf,Moosmayer, Dieter,Eberspaecher, Uwe,Weiske, Joerg,Lechner, Christian,Prechtl, Stefan,Suelzle, Detlev,Siegel, Franziska,Prinz, Florian,Lesche, Ralf,Nicke, Barbara,Nowak-Reppel, Katrin,Himmel, Herbert,Mumberg, Dominik,Von Nussbaum, Franz,Nising, Carl F.,Bauser, Marcus,Haegebarth, Andrea
supporting information, p. 928 - 940 (2019/01/30)
The availability of a chemical probe to study the role of a specific domain of a protein in a concentration- and time-dependent manner is of high value. Herein, we report the identification of a highly potent and selective ERK5 inhibitor BAY-885 by high-throughput screening and subsequent structure-based optimization. ERK5 is a key integrator of cellular signal transduction, and it has been shown to play a role in various cellular processes such as proliferation, differentiation, apoptosis, and cell survival. We could demonstrate that inhibition of ERK5 kinase and transcriptional activity with a small molecule did not translate into antiproliferative activity in different relevant cell models, which is in contrast to the results obtained by RNAi technology.
IDENTIFICATION AND USE OF ERK5 INHIBITORS
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Page/Page column 99-100, (2019/10/01)
The present invention covers heterocyclic compounds of general formula (I) in which T, U, Y, Z, R1 and R3 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer disorders, as a sole agent or in combination with other active ingredients.
Design and synthesis of a novel series of orally active, selective somatostatin receptor 2 agonists for the treatment of type 2 diabetes
Banno, Yoshihiro,Sasaki, Shigekazu,Kamata, Makoto,Kunitomo, Jun,Miyamoto, Yasufumi,Abe, Hidenori,Taya, Naohiro,Oi, Satoru,Watanabe, Masanori,Urushibara, Tomoko,Hazama, Masatoshi,Niwa, Shin-ichi,Miyamoto, Saku,Horinouchi, Akira,Kuroshima, Ken-ichi,Amano, Nobuyuki,Matsumoto, Shin-ichi,Matsunaga, Shinichiro
, p. 5995 - 6006 (2017/10/10)
The discovery of a novel series of β-methyltryptophan (β MeTrp) derivatives as selective and orally active non-peptide somatostatin receptor 2 (SSTR2) agonists for the treatment of Type 2 diabetes is described. In our previous research, Compound A, β-MeTr
TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 83; 84, (2016/10/31)
The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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Page/Page column 64; 65, (2015/12/08)
The present invention is directed to substituted five membered heteroaryl benzamide compounds compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Page/Page column 113, (2015/12/30)
The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
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Page/Page column 55, (2016/03/04)
The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula(I) which are tropomyosin-related kinase(Trk)family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF)receptor TrkA.
1-PHENYL-2-PYRIDINYL ALKYL ALCOHOL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS
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Paragraph 0651; 0652, (2014/06/23)
Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
BISAMLDE DERIVATIVES AND USE THEREOF AS FATTY ACID SYNTHASE INHIBITORS
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Page/Page column 147-148, (2008/12/05)
A compound of formula I, or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity and diabetes mellitus,
PIPERIDINE DERIVATIVES FOR THE TREATMENT OF OBESITY
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Page/Page column 212-213, (2008/12/06)
A compound of formula (I) or a pharmaceutically acceptable salt thereof, processes for preparing such compounds, their use as Fatty Acid Synthase inhibitors, methods for their therapeutic use, particularly in the treatment of obesity, diabetes mellitus, c
