05-08-2021 дата публикации
Номер: US20210238195A1
Принадлежит:
Provided are novel crystalline forms of a spiro-compound which acts as a muscarinic acetylcholine receptor agonist. In particular, isolated crystalline polymorphs of (S)-2-ethyl-8-methyl-1-thia-4,8-diazaspiro[4.5]decane-3-one are described which have favorable properties in pharmaceutical manufacture. Also provided are methods to prepare said crystalline polymorphs, and to convert them into each other as well as methods for preparing medicaments containing the same which are suitable for use in the treatment of diseases and disorders that respond to modulation of the muscarinic acetylcholine receptor. 115-. (canceled)17. The method of claim 16 , wherein{'sub': 'α', '(a) the X-ray powder diffraction pattern contains at least two, three or all of the following 2-theta values as measured using CuK radiation: 8.8, 12.30, 17.30, 17.50, 17.80 and 23.0;'}{'sub': 'α', '(b) the X-ray powder diffraction pattern also contains at least one of the following 2-theta values as measured using CuK radiation: 12.3, 19.9, 21.6, 24.5, 26.3 and 31.6;'}(c) the X-ray powder diffraction pattern is substantially free of peaks having 2-theta values in the range of from 10.8-11.8;{'sub': 'α', '(d) the X-ray powder diffraction pattern contains at least one of the following 2-theta values as measured using CuK radiation: 12.2, 17.3, 19.9, 21.6, 24.5, 26.3 and 31.6, and wherein said X-ray powder diffraction is substantially free of peaks having 2-theta values in the range of from 10.8-11.8;'}{'sub': 'α', '(e) the X-ray powder diffraction pattern contains at least two, three, four, five or all of the following 2-theta values as measured using CuK radiation 12.2, 17.3, 17.5, 19.9, 21.6, 24.5, 26.3 and 31.2;'}{'sup': '13', '(f) the C solid-state NMR of the crystalline form contains resonances having at least two, three, four or all of the following chemical shift values as expressed in ppm relative to TMS: 67.56, 54.60, 41.49, 30.70 and 13.77;'}{'sup': '13', '(g) the C solid-state NMR of the ...
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