Processes for the preparation and purification of gpr119 agonist compounds and intermediates thereof
AssigneeMankind Pharma Ltd.
InventorsSazid ALI, Rakesh Ishwar PATIL, Santosh Kumar RAI, Anil KUMAR
Life of this patent
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Abstract
The present disclosure relates to improved processes for the preparation and purification of a compound of Formula (I) and pharmaceutically acceptable salts thereof, and its intermediates.
Claims15
A process for the preparation of a compound of Formula I or a pharmaceutically acceptable salt thereof
- the process comprising:
- (a) reacting a compound of Formula III-a or a salt thereof with a compound of Formula IV-a or a salt thereof to obtain a compound of Formula II-a or a salt thereof
- wherein X is a leaving group and n is 0, 1 or 2;
- (b) when n is 0 or 1, converting the compound of formula II-a to compound of Formula I-a or pharmaceutically acceptable salt thereof
- (c) separating the desired isomer of the compound of Formula I or a pharmaceutically acceptable salt thereof;
- and
- (d) optionally purifying the desired isomer of the compound of Formula I or a pharmaceutically acceptable salt thereof.
A process for the preparation of a compound of Formula I or a pharmaceutically acceptable salt thereof
- the process comprising:
- (a) reacting a compound of Formula III-1 or a salt thereof with a compound of Formula IV or a salt thereof to obtain a compound of Formula II or a salt thereof
- wherein X is a leaving group;
- (b) converting the compound of Formula II or a salt thereof to a compound of Formula I or pharmaceutically acceptable salt thereof;
- and
- (c) optionally purifying the compound of Formula I or a pharmaceutically acceptable salt thereof.
A process for the purification of a compound of Formula I or a pharmaceutically acceptable salt thereof
- the process comprising:
- (a) providing a solution, dispersion, or slurry of the compound of Formula I or a pharmaceutically acceptable salt thereof in one or more solvents;
- (b) heating the reaction mass of step (a);
- (c) cooling the reaction mass;
- (d) optionally adding one or more solvents;
- and
- (e) isolating the purified compound of Formula I or a pharmaceutically acceptable salt thereof.
The process according to claim 13, wherein the one or more solvents are selected from methanol, ethanol, acetonitrile, dimethyl sulfoxide, cyclohexane, dichloromethane, and any combination of any of the foregoing.
A compound of Formula I or a pharmaceutically acceptable salt thereof
- wherein the compound of Formula I or a pharmaceutically acceptable salt thereof has
- (i) a chemical purity of more than about 99%,
- (ii) an enantiomeric excess of more than about 99%, or
- (iii) both (i) and (ii).
A compound of Formula I or a pharmaceutically acceptable salt thereof
- wherein the compound of Formula I or a pharmaceutically acceptable salt thereof is substantially free of one or more compounds of the Formulas A, B, C, D, and E
A compound of Formula I or a pharmaceutically acceptable salt thereof
- wherein the compound of Formula I or a pharmaceutically acceptable salt thereof is characterized by a particle size distribution wherein
- (i) a d90 of less than about 60 μm,
- (ii) a d50 of less than about 20 μm,
- (iii) a d10 of less than about 10 μm, or
- (iv) any combination of any of (i), (ii) and (iii).
Dependencies are inferred from the claim text.