US 11,717,522 B2
Solid pharmaceutical compositions comprising biopterin derivatives and uses of such compositions
Peter Scheurer, Randersacker (DE); Frank Tegtmeier, Bielefeld (DE); and Reinhard Schinzel, Gerbrunn (DE)
Assigned to VASOPHARM GMBH, Wuerzburg (DE)
Filed by VASOPHARM GMBH, Wuerzburg (DE)
Filed on Jan. 20, 2021, as Appl. No. 17/153,749.
Application 17/153,749 is a continuation of application No. 16/659,401, filed on Oct. 21, 2019, granted, now 10,925,877.
Application 16/659,401 is a continuation of application No. 16/003,374, filed on Jun. 8, 2018, granted, now 10,493,075, issued on Dec. 3, 2019.
Application 16/003,374 is a continuation of application No. 15/584,890, filed on May 2, 2017, granted, now 10,016,431, issued on Jul. 10, 2018.
Application 15/584,890 is a continuation of application No. 14/913,665, granted, now 9,895,372, issued on Feb. 20, 2018, previously published as PCT/EP2015/056824, filed on Mar. 30, 2015.
Claims priority of application No. 14162727 (EP), filed on Mar. 31, 2014.
Prior Publication US 2021/0137927 A1, May 13, 2021
Prior Publication US 2022/0031703 A9, Feb. 3, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/519 (2006.01); A61K 47/02 (2006.01); A61K 9/19 (2006.01); A61K 9/00 (2006.01); A61K 31/4985 (2006.01)
CPC A61K 31/519 (2013.01) [A61K 9/0019 (2013.01); A61K 9/19 (2013.01); A61K 31/4985 (2013.01); A61K 47/02 (2013.01)] 11 Claims
 
1. A method for preparing a lyophilized solid pharmaceutical composition comprising
a) a compound having the formula (I):

OG Complex Work Unit Chemistry
and/or a compound having the formula (II):

OG Complex Work Unit Chemistry
 and
b) two different sodium phosphate salts, wherein the two different sodium phosphate salts are NaH2PO4·2H2O and Na2HPO4·2H2O, and wherein the quantity of the NaH2PO4·2H2O and Na2HPO4·2H2O present in the composition is chosen such that the molar ratio of both NaH2PO4·2H2O and Na2HPO4·2H2O to compound (I) or compound (II) ranges from 0.02 to 0.5 and optionally NaCl;
the method comprising:
aa) dissolving the compound of the formula (III) and/or (II):

OG Complex Work Unit Chemistry
with a buffer,
wherein the buffer comprises the two different sodium phosphate salts, wherein the buffer is prepared by
separately dissolving in water NaH2PO4·2H2O and Na2HPO4·2H2O,
then adding the NaH2PO4·2H2O solution to the Na2HPO4·2H2O solution to obtain a sodium phosphate solution with a pH of 7.4, and
then adding the sodium phosphate solution to a 5N NaOH solution; and
bb) lyophilization of the solution obtained in aa).