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
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.
1 - 116 . (canceled)
117 . A pharmaceutical tablet comprising (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 (Compound 1) and a pharmaceutically acceptable excipient, prepared by a process comprising contacting a solid form of Compound 1 with the pharmaceutically acceptable excipient.
118 . The pharmaceutical tablet of claim 117 , wherein the pharmaceutically acceptable excipient is a filler.
119 . The pharmaceutical tablet of claim 118 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
120 . The pharmaceutical tablet of claim 119 , further comprising a release control polymer.
121 . The pharmaceutical tablet of claim 117 , wherein the solid form of Compound 1 comprises amorphous freebase Compound 1 having less than about 13% by weight water.
122 . The pharmaceutical tablet of claim 121 , wherein the pharmaceutically acceptable excipient is a filler.
123 . The pharmaceutical tablet of claim 122 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
124 . The pharmaceutical tablet of claim 123 , further comprising a release control polymer.
125 . The pharmaceutical tablet of claim 117 , wherein the solid form of Compound 1 comprises amorphous freebase Compound 1 having between about 0.8% and about 3.7% by weight water.
126 . The pharmaceutical tablet of claim 125 , wherein the pharmaceutically acceptable excipient is a filler.
127 . The pharmaceutical tablet of claim 126 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
128 . The pharmaceutical tablet of claim 127 , further comprising a release control polymer.
129 . The pharmaceutical tablet of claim 117 , wherein the solid form of Compound 1 comprises amorphous freebase Compound 1 having a glass transition temperature onset at about 119° C.
130 . The pharmaceutical tablet of claim 129 , wherein the pharmaceutically acceptable excipient is a filler.
131 . The pharmaceutical tablet of claim 130 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
132 . The pharmaceutical tablet of claim 131 , further comprising a release control polymer.
133 . The pharmaceutical tablet of claim 117 , wherein the solid form of Compound 1 comprises amorphous freebase Compound 1 having a glass transition temperature midpoint at about 122° C.
134 . The pharmaceutical tablet of claim 133 , wherein the pharmaceutically acceptable excipient is a filler.
135 . The pharmaceutical tablet of claim 134 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
136 . The pharmaceutical tablet of claim 135 , further comprising a release control polymer.
137 . The pharmaceutical tablet of claim 117 , wherein the solid form of Compound 1 comprises amorphous freebase Compound 1 having a glass transition temperature onset at about 119° C. and a glass transition temperature midpoint at about 122° C.
138 . The pharmaceutical tablet of claim 137 , wherein the pharmaceutically acceptable excipient is a filler.
139 . The pharmaceutical tablet of claim 138 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
140 . The pharmaceutical tablet of claim 139 , further comprising a release control polymer.
141 . The pharmaceutical tablet of claim 117 , wherein the solid form of Compound 1 comprises Freebase Hydrate Form C of Compound 1.
142 . The pharmaceutical tablet of claim 141 , wherein the pharmaceutically acceptable excipient is a filler.
143 . The pharmaceutical tablet of claim 142 , further comprising an acidic pH modifier that is an organic acid present in an amount from about 10 w/w % to about 35 w/w %.
144 . The pharmaceutical tablet of claim 143 , further comprising a release control polymer.