Salt forms of bicyclic heterocyclic derivatives
View Patent ↗The present invention provides novel solid forms of pharmaceutically active agents and therapeutic uses thereof. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
1. A crystalline form of N-(5-(2-(2,2-dimethylpyrrolidin-1-yl)ethylcarbamoyl)-2-methylpyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carboxamide saccharinate.
2. The crystalline form according to claim 1 , characterized by a X-ray powder diffraction pattern comprising four or more 2Θ values chosen from 13.4±0.2°, 13.7±0.2°, 14.4±0.2°, 15.5±0.2°, 25.1±0.2° and 26.0±0.2° when measured at a temperature of about 25° C.
3. The crystalline form according to claim 1 , characterized by a X-ray powder diffraction pattern comprising five or more 2Θ values chosen from 6.7±0.2°, 8.4±0.2°, 12.3±0.2°, 13.4±0.2°, 13.7±0.2°, 14.4±0.2°, 15.5±0.2°, 21.2±0.2°, 21.7±0.2°, 25.1±0.2°, 25.6±0.2° and 26.0±0.2° when measured at a temperature of about 25° C.
4. A pharmaceutical composition comprising a crystalline form of N-(5-(2-(2,2-dimethylpyrrolidin-1-yl)ethylcarbamoyl)-2-methylpyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carboxamide saccharinate and one or more pharmaceutically acceptable carriers.
5. A pharmaceutical composition according to claim 4 , wherein the composition further comprises one or more additional therapeutically active agents.
6. A method of treating a respiratory disorder or disease mediated by the PDGF receptor in a subject in need thereof, comprising administering to the subject in need thereof a crystalline form of N-(5-(2-(2,2-dimethylpyrrolidin-1-yl)ethylcarbamoyl)-2-methylpyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carboxamide saccharinate, wherein the respiratory disorder or disease is chosen from asthma, allergic rhinitis, pulmonary arterial hypertension (PAH), and pulmonary fibrosis.
7. The method according to claim 6 wherein the respiratory disorder or disease is pulmonary arterial hypertension (PAH).
8. The method according to claim 6 wherein the respiratory disorder or disease is asthma.
9. The method according to claim 6 further comprising one or more additional therapeutically active agents.
10. The compound N-(5-(2-(2,2-dimethylpyrrolidin-1-yl)ethylcarbamoyl)-2-methylpyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carboxamide saccharinate.
11. A pharmaceutical composition comprising N-(5-(2-(2,2-dimethylpyrrolidin-1-yl)ethylcarbamoyl)-2-methylpyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carboxamide saccharinate and one or more pharmaceutically acceptable carriers.
12. A pharmaceutical composition according to claim 11 , wherein the composition further comprises one or more additional therapeutically active agents.
13. A method of treating a respiratory disorder or disease mediated by the PDGF receptor in a subject in need thereof, comprising administering N-(5-(2-(2,2-dimethylpyrrolidin-1-yl)ethylcarbamoyl)-2-methylpyridin-3-yl)-6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridine-3-carboxamide saccharinate to the subject in need thereof, wherein the respiratory disorder or disease is chosen from asthma, allergic rhinitis, pulmonary arterial hypertension (PAH), and pulmonary fibrosis.
14. The method according to claim 13 wherein the respiratory disorder or disease is pulmonary arterial hypertension (PAH).
15. The method according to claim 13 wherein the respiratory disorder or disease is asthma.
16. The method according to claim 13 further comprising one or more additional therapeutically active agents.
17. The pharmaceutical composition according to claim 4 wherein the crystalline form is characterized by a X-ray powder diffraction pattern comprising four or more 2Θ values chosen from 13.4±0.2°, 13.7±0.2°, 14.4±0.2°, 15.5±0.2°, 25.1±0.2° and 26.0±0.2°.