US 12,337,002 B2
Enzymatic process for obtaining 17 alpha-monoesters of cortexolone and/or its 9,11-dehydroderivatives
Mauro Ajani, Lainate (IT); and Luigi Moro, Cairate (IT)
Assigned to CASSIOPEA S.P.A., Lainate (IT)
Filed by CASSIOPEA S.P.A., Lainate (IT)
Filed on Nov. 18, 2022, as Appl. No. 18/057,031.
Application 15/211,087 is a division of application No. 14/073,928, filed on Nov. 7, 2013, granted, now 9,433,628, issued on Sep. 6, 2016.
Application 14/073,928 is a division of application No. 12/671,932, granted, now 8,785,427, issued on Jul. 22, 2014, previously published as PCT/EP2008/059702, filed on Jul. 24, 2008.
Application 18/057,031 is a continuation of application No. 17/455,538, filed on Nov. 18, 2021, granted, now 11,938,141.
Application 17/455,538 is a continuation of application No. 16/686,738, filed on Nov. 18, 2019, granted, now 11,207,332, issued on Dec. 28, 2021.
Application 16/686,738 is a continuation of application No. 16/195,083, filed on Nov. 19, 2018, granted, now 10,716,796, issued on Jul. 21, 2020.
Application 16/195,083 is a continuation of application No. 15/211,087, filed on Jul. 15, 2016, granted, now 10,166,245, issued on Jan. 1, 2019.
Claims priority of application No. MI2007A001616 (IT), filed on Aug. 3, 2007.
Prior Publication US 2023/0104965 A1, Apr. 6, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/573 (2006.01); A61K 9/00 (2006.01); A61K 9/06 (2006.01); A61K 47/06 (2006.01); A61K 47/10 (2017.01); A61K 47/14 (2017.01); A61K 47/26 (2006.01); A61K 47/44 (2017.01); C07J 5/00 (2006.01); C07J 7/00 (2006.01); C12P 33/00 (2006.01)
CPC A61K 31/573 (2013.01) [A61K 9/0014 (2013.01); A61K 9/06 (2013.01); A61K 47/06 (2013.01); A61K 47/10 (2013.01); A61K 47/14 (2013.01); A61K 47/26 (2013.01); A61K 47/44 (2013.01); C07J 5/0053 (2013.01); C07J 7/008 (2013.01); C07B 2200/13 (2013.01); C12P 33/005 (2013.01)] 21 Claims
 
1. A pharmaceutical composition comprising cortexolone 17α-propionate in at least one of polymorphic forms I, III, or IV, propylene glycol, cetyl alcohol, glyceryl monostearate, liquid paraffin, tocopherol, polyoxyethylene (80) sorbitan monooleate, and water, wherein:
a) polymorphic form I is characterized by a DRX with at least peaks at about: 7.6, 8.4, 17.0, and 20.1 degrees 2theta;
b) polymorphic form III is characterized by a DRX with at least peaks at about: 6.2, 12.6, 22.4, and 23.7 degrees 2theta; and
c) polymorphic form IV is characterized by DRX with at least peaks at about: 4.8, 12.9, and 19.5 degrees 2theta.