US 12,421,227 B2
Ribociclib salts and solid state forms thereof
Helena Ceric, Zagreb (HR); Elisa Vergani, Novara (IT); Paolo S. Tiseni, Bresso (IT); Hana Kantor, Ostrava (CZ); Piero Paravidino, Sedriano (IT); Nikolina Janton, Jakovlje (HR); Christian Galluzzo, Novara (IT); and Alexandr Jegorov, Dobra Voda (CZ)
Assigned to ASSIA CHEMICAL INDUSTRIES LTD., Tel Aviv (IL)
Filed by ASSIA CHEMICAL INDUSTRIES LTD., Tel Aviv (IL)
Filed on Oct. 25, 2021, as Appl. No. 17/509,140.
Application 17/509,140 is a continuation of application No. 16/641,390, granted, now 11,155,545, previously published as PCT/US2018/047434, filed on Aug. 22, 2018.
Claims priority of provisional application 62/593,319, filed on Dec. 1, 2017.
Claims priority of provisional application 62/577,446, filed on Oct. 26, 2017.
Claims priority of provisional application 62/555,170, filed on Sep. 7, 2017.
Claims priority of provisional application 62/550,208, filed on Aug. 25, 2017.
Prior Publication US 2022/0041598 A1, Feb. 10, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 471/04 (2006.01)
CPC C07D 471/04 (2013.01) [C07B 2200/13 (2013.01)] 12 Claims
 
1. A polymorphically pure crystalline form of Ribociclib succinate designated form B, defined by data selected from one or more of the following:
(i) an X-ray powder diffraction pattern having peaks at 6.5, 7.5, 10.2, 10.9 and 12.0 degrees two theta ±0.2 degrees two theta;
(ii) an X-ray powder diffraction pattern having peaks at 6.5, 7.5, 10.2, 10.9 and 12.0 degrees two theta ±0.2 degrees two theta and also having any one, two, three, four or five additional peaks selected from 14.6, 20.2, 20.7, 25.4 and 26.6 degrees two theta ±0.2 degrees two theta;
(iii) an X-ray powder diffraction pattern substantially as depicted in FIG. 2;
(iv) a solid state 13C NMR spectrum having peaks at 183.0, 165.5, 156.5, 138.3 and 103.1 ppm ±0.2 ppm;
(v) a solid state 13C NMR spectrum having the following chemical shift absolute differences between said characteristic peaks at 183.0, 165.5, 156.5, 138.3 and 103.1 ppm ±0.2 ppm and a reference peak at 122.3 ppm ±1 ppm of 60.7, 43.2, 34.1, 15.9 and (−19.2) ±0.1 ppm; or
(vi) a solid state 13C NMR spectrum substantially as depicted in FIG. 12 or substantially as depicted in FIG. 13;
(vii) an FT-IR spectrum having absorptions at 1605, 1525, 1399, 1261 and 786 cm−1 ±4 cm−1;
(viii) an FT-IR spectrum substantially as depicted in FIG. 8 or substantially as depicted in FIG. 9.