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US 12,673,952 B2Granted
Processes for preparing modulators of alpha-1 antitrypsin
AssigneeVertex Pharmaceuticals Incorporated
InventorsCavan McKeon Bligh, Robert Daniel Giacometti, Cristian Harrison, Stephen W. Laws, Adam Looker, Stefanie Roeper
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Abstract
This disclosure provides large-scale processes for preparing a modulator of alpha-1 antitrypsin (AAT) activity that may be useful for treating alpha-1 antitrypsin deficiency (AATD), such as 4-(5-(4-fluorophenyl)-6-(tetrahydro-2H-pyran-4-yl)-1,5-dihydropyrrolo[2,3-f]indazol-7-yl)benzoic acid (Compound 1), 3-[5-(4-fluorophenyl)-6-isopropyl-1H-pyrrolo[2,3-f]indazol-7-yl]propanoic acid (Compound 2), or a pharmaceutically acceptable salt of any of the foregoing.
Claims5
A process for preparing a solid form of Compound 1
- or a pharmaceutically acceptable salt thereof, comprising:
- (a) reacting
- or a pharmaceutically acceptable salt thereof with
- to form
- or a pharmaceutically acceptable salt thereof;
- and
- (b) de-esterifying C58B or a pharmaceutically acceptable salt thereof to yield the solid form of Compound 1 or a pharmaceutically acceptable salt thereof.
4 more elements
Dependencies are inferred from the claim text.