On June 6, 2013, Steeneck, Christoph; Kinzel, Olaf; Gege, Christian; Kleymann, Gerald; Hoffmann, Thomas published a patent.HPLC of Formula: 93476-46-1 The title of the patent was Preparation of pyrrolocarboxamides as modulators of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases. And the patent contained the following:
The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administrating these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolocarboxamide compounds I [R1 = H, alkyl, cycloalkyl, etc.; R2 = H, alkyl, haloalkyl, hydroxyalkyl; or NR1R2 = (un)substituted 3-8 membered ring containing carbon atoms and optionally containing 1-2 heteroatoms selected from O, S and N; R3 = (un)substituted pyridinone, 6-10 membered mono- or bicyclic aryl, 5-10 membered mono- or bicyclic heteroaryl containing 1-4 heteroatoms selected from N, O or S, etc.; R4 = SO2(CR8R8)yR7, SO2NR12R7, (CR8R8)xR10 or cycloalkyl, which is spirocyclic fused with cycloalkyl; R5 = H, alkyl, haloalkyl, etc.; R6 = H, alkyl, haloalkyl, halo; R7 = (un)substituted cycloalkyl, heterocycloalkyl; R8 = H, F, alkyl, haloalkyl, OH; R10 = (un)substituted cycloalkyl; R12 = H, alkyl, haloalkyl; x = 1-2; y = 0-2; with the proviso] and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof. Over six hundred compounds I were prepared E.g., a multi-step synthesis of II, starting from 1-cyclohexylethanol, was described. Exemplified compounds I were tested in RORγ GaI4 reporter gene assay (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of Ethyl indolizine-1-carboxylate(cas: 93476-46-1).HPLC of Formula: 93476-46-1
The Article related to pyrrolocarboxamide preparation orphan nuclear receptor rar related gamma modulator, retinoid related orphan receptor gamma modulator pyrrolocarboxamide preparation antiinflammatory, autoimmune disease treatment pyrrolocarboxamide preparation ror gamma modulator and other aspects.HPLC of Formula: 93476-46-1
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