633328-40-2Relevant academic research and scientific papers
THERAPEUTIC INHIBITORY COMPOUNDS
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Paragraph 00196, (2019/01/08)
Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds which are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
THERAPEUTIC INHIBITORY COMPOUNDS
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Paragraph 00225, (2017/07/04)
Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds which are complement factor D inhibitors. Such compounds are useful for treating complement related disorders including, but are not limited to, autoimmune, inflammatory, and neurodegenerative diseases.
ALKYNYL ALCOHOLS AND METHODS OF USE
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Page/Page column 362; 363, (2015/03/13)
The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over- activation of NF-kB signaling is observed.
Optimisation of ITK inhibitors through successive iterative design cycles
Herdemann, Matthias,Weber, Alexander,Jonveaux, Jér?me,Schwoebel, Frank,Stoeck, Michael,Heit, Isabelle
scheme or table, p. 1852 - 1856 (2011/05/05)
Based on a hit cluster of compounds inhibiting interleukin-2 inducible T-cell kinase (ITK) in the submicromolar range a series of ITK inhibitor libraries were synthesized. Through iterative design cycles including kinase crystal structure information, indolylindazole libraries were identified which showed low nanomolar activity in enzymatic and cellular assays. The potential of these novel lead series was confirmed through in vivo tests in an anti-CD3-IL2 mouse model. The intravenous administration of highly potent ITK inhibitor 11o resulted in dose-dependent, efficient suppression of IL-2.
Identification of potent ITK inhibitors through focused compound library design including structural information
Herdemann, Matthias,Heit, Isabelle,Bosch, Frank-Uwe,Quintini, Gianluca,Scheipers, Claudia,Weber, Alexander
scheme or table, p. 6998 - 7003 (2010/12/25)
A series of novel compound libraries inhibiting interleukin-2 inducible T cell kinase (ITK) were designed, synthesized and evaluated. In the first design cycle two library scaffolds were identified showing low micromolar inhibition of ITK. Further iterative design cycles including crystal structure information of ITK and structurally related kinases led to the identification of indolylindazole and indolylpyrazolopyridine compounds with low nanomolar ITK inhibition.
