IP Library › Patent Application 18530071
Patent Application
App. No. 18/530,071

PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF

Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US None
App. No.
18/530,071
Abstract

The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process.

Claims (61)

1 - 116 . (canceled)

117 . An extended release tablet for oral administration, comprising:

(a) about 15 mg, about 30 mg or about 45 mg of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;

(b) microcrystalline cellulose;

(c) mannitol;

(d) hydroxypropyl methylcellulose;

(e) an organic acid selected from the group consisting of citric acid, succinic acid, fumaric acid, and tartaric acid;

(f) colloidal silica; and

(g) magnesium stearate.

118 . The extended release tablet of claim 117 , wherein the organic acid is citric acid.

119 . The extended release tablet of claim 117 , wherein the organic acid is succinic acid.

120 . The extended release tablet of claim 117 , wherein the organic acid is fumaric acid.

121 . The extended release tablet of claim 117 , wherein the organic acid is tartaric acid.

122 . An extended release tablet for oral administration, comprising:

(a) about 15 mg, about 30 mg or about 45 mg of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;

(b) microcrystalline cellulose;

(c) about 21 w/w % mannitol;

(d) about 20 w/w % hydroxypropyl methylcellulose;

(e) about 20 w/w % of an organic acid selected from the group consisting of citric acid, succinic acid, fumaric acid, and tartaric acid;

(f) about 0.5 w/w % colloidal silica; and

(g) about 1.5 w/w % magnesium stearate.

123 . The extended release tablet of claim 122 , wherein the organic acid is citric acid.

124 . The extended release tablet of claim 122 , wherein the organic acid is succinic acid.

125 . The extended release tablet of claim 122 , wherein the organic acid is fumaric acid.

126 . The extended release tablet of claim 122 , wherein the organic acid is tartaric acid.

127 . An extended release tablet for oral administration, comprising:

(a) about 15 mg or about 30 mg of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;

(b) about 30.6 w/w % to about 33.8 w/w % microcrystalline cellulose;

(c) about 21 w/w % mannitol;

(d) about 20 w/w % hydroxypropyl methylcellulose;

(e) about 20 w/w % of an organic acid selected from the group consisting of citric acid, succinic acid, fumaric acid, and tartaric acid;

(f) about 0.5 w/w % colloidal silica; and

(g) about 1.5 w/w % magnesium stearate.

128 . The extended release tablet of claim 127 , comprising:

(a) about 15 mg (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;

(b) about 33.8 w/w % microcrystalline cellulose;

(c) about 21 w/w % mannitol;

(d) about 20 w/w % hydroxypropyl methylcellulose;

(e) about 20 w/w % of an organic acid selected from the group consisting of citric acid, succinic acid, fumaric acid, and tartaric acid;

(f) about 0.5 w/w % colloidal silica; and

(g) about 1.5 w/w % magnesium stearate.

129 . The extended release tablet of claim 127 , comprising:

(a) about 30 mg (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide;

(b) about 30.6 w/w % microcrystalline cellulose;

(c) about 21 w/w % mannitol;

(d) about 20 w/w % hydroxypropyl methylcellulose;

(e) about 20 w/w % of an organic acid selected from the group consisting of citric acid, succinic acid, fumaric acid, and tartaric acid;

(f) about 0.5 w/w % colloidal silica; and

(g) about 1.5 w/w % magnesium stearate.

130 . The extended release tablet of claim 127 , wherein the organic acid is citric acid.

131 . The extended release tablet of claim 127 , wherein the organic acid is succinic acid.

132 . The extended release tablet of claim 127 , wherein the organic acid is fumaric acid.

133 . The extended release tablet of claim 127 , wherein the organic acid is tartaric acid.

134 . The extended release tablet of claim 128 , wherein the organic acid is citric acid.

135 . The extended release tablet of claim 128 , wherein the organic acid is succinic acid.

136 . The extended release tablet of claim 128 , wherein the organic acid is fumaric acid.

137 . The extended release tablet of claim 128 , wherein the organic acid is tartaric acid.

138 . The extended release tablet of claim 129 , wherein the organic acid is citric acid.

139 . The extended release tablet of claim 129 , wherein the organic acid is succinic acid.

140 . The extended release tablet of claim 129 , wherein the organic acid is fumaric acid.

141 . The extended release tablet of claim 129 , wherein the organic acid is tartaric acid.