(2R)-2-Phenylcarbonyloxypropyl(2S)-2-amino-3-(3, 4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.
대표청구항▼
What is claimed is: 1. A compound, crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate. 2. The compound of claim 1, having characteristic peaks (°2θ) at 5.0±0.2°, 8.5±0.2°, 13.6±0.2°, 15.0±0.2°, 17.0±0.2°, 17.7±0.2°, 20.4±0.2°, 21.1±0.2°, 25.0±0
What is claimed is: 1. A compound, crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate. 2. The compound of claim 1, having characteristic peaks (°2θ) at 5.0±0.2°, 8.5±0.2°, 13.6±0.2°, 15.0±0.2°, 17.0±0.2°, 17.7±0.2°, 20.4±0.2°, 21.1±0.2°, 25.0±0.2°, 25.8±0.2°, 28.2±0.2°, 30.1±0.2°, and 37.6±0.2° in an X-ray powder diffraction pattern measured using Cu Kα radiation. 3. The compound of claim 1, wherein the compound is characterized by a differential scanning calorimetry thermogram having an endothermic peak at about 164.5±2.5° C. 4. A pharmaceutical composition comprising a pharmaceutically acceptable vehicle and a therapeutically effective amount of the compound of claim 1. 5. The pharmaceutical composition of claim 4, and at least one other diastereomer of crystalline 2-phenylcarbonyloxypropyl-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate wherein the diastereomeric purity of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate is at least about 90%. 6. The pharmaceutical composition of claim 4, comprising an L-aromatic amino acid decarboxylase inhibitor. 7. The pharmaceutical composition of claim 4, comprising a catechol-O-methyltransferase inhibitor. 8. The pharmaceutical composition of claim 4, formulated for sustained release oral administration. 9. The compound of claim 1, having characteristic diffraction peaks(°2θ)at 4.7±0.2°, 5.0±0.2°, 8.5±0.2°, 9.6±0.2°, 13.6±0.2°, 15.0±0.2°, 17.0±0.2°, 17.4±0.2°, 17.7±0.2°, 19.1±0.2°, 19.5±0.2°, 20.0±0.2°, 20.4±0.2°, 21.1±0.2°, 22.3±0.2°, 22.9±0.2°, 23.1±0.2°, 23.3±0.2°, 24.3±0.2°, 25.0 ±0.2°, 25.3±0.2°, 25.7±0.2°, 25.8±0.2°, 26.9±0.2°, 27.3±0.2°, 28.2±0.2°, 30.1±0.2°, 30.5±0.2°, 32.0±0.2°, 33.8±0.2°, 34.3±0.2°, 37.6±0.2°, and 38.4±0.2° in an X-ray powder diffraction pattern measured using Cu Kα radiation. 10. The compound of claim 1 wherein the compound is characterized by a differential scanning calorimetry thermogram having an endothermic peak at 165.8±1.1° C. at a scan rate of 10° C./min or 15° C./min. 11. The compound of claim 1, wherein the compound exhibits a melting point from about 157° C. to about 162° C. 12. The compound of claim 1, wherein the compound exhibits a melting point from 160.5° C. to 161.3° C. 13. The pharmaceutical composition of claim 4, and at least one other diastereomer of crystalline 2-phenylcarbonyloxypropyl-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate wherein the diastereomeric purity of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate is at least about 95%. 14. The pharmaceutical composition of claim 4, and at least one other diastereomer of crystalline 2-phenylcarbonyloxypropyl-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate wherein the diastereomeric purity of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate is at least about 99%. 15. The pharmaceutical composition of claim 4, and at least one other diastereomer of crystalline 2-phenylcarbonyloxypropyl-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate wherein the compositional purity of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate is at least about 95%. 16. The pharmaceutical composition of claim 4, and at least one other diastereomer of crystalline 2-phenylcarbonyloxypropyl-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate wherein the compositional purity of crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate is at least about 97%. 17. The pharmaceutical composition of claim 4, comprising an L-aromatic amino acid decarboxylase inhibitor and a catechol-O-methyltransferase inhibitor.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (32)
Metcalf Brian W. (Strasbourg FRX) Jung Michel (Illkirch Graffenstaden FRX), a
상세보기
Xiang,Jia Ning; Gallop,Mark A.; Cundy,Kenneth C.; Li,Jianhua; Xu,Feng; Zhou,Cindy X.; Bhat,Laxminarayan, Carbidopa prodrugs and derivatives, and compositions and uses thereof.
Dempski Robert E. (Dresher PA) Scholtz Edward C. (King of Prussia PA) Nibbelink Donald W. (Lansdale PA) Reines Scott A. (New Hope PA), Controlled release combination of carbidopa/levodopa.
Budavari John (Watchung NJ) Czaja Robert F. (Scotch Plains NJ) Grabowski Edward J. J. (Westfield NJ) Shukis William F. (Edison NJ) Zambito Arthur J. (Clark NJ), Crystalline salts of L or (S)-3-(3,4-dihydroxyphenyl)-2-methylalanine esters and process.
Edgren David E. (El Granada CA) Bhatti Gurdish K. (Fremont CA) Carpenter Howard A. (Palo Alto CA), Dosage form for Parkinson\s disease, spasticity and muscle spasms.
Edgren David E. (El Granada) Carpenter Howard A. (Palo Alto) Bhatti Gurdish K. (Fremont) Ayer Atul D. (Palo Alto CA), Dosage form indicated for the management of abnormal posture, tremor and involuntary movement.
Grosswald Ralph R. (Fairfield IA) Anderson Jeffory B. (Springville UT) Andrew Clair S. (Provo UT), Method for the manufacture of pharmaceutical cellulose capsules.
Bckstrm Reijo J. (Helsinki FIX) Heinola Kalevi E. (JrvempFIX) Honkanen Erkki J. (Vantaa FIX) Kaakkola Seppo K. (Helsinki FIX) Kairisalo Pekka J. (Helsinki FIX) Linden Inge-Britt Y. (Helsinki FIX) Mnn, Pharmacologically active compounds, methods for the preparation thereof and compositions containing the same.
Mao, Chen; Pargaonkar, Nikhil; Maurer, Laura E.; Ma, Sarina Grace Harris, Pharmaceutical compositions and oral dosage forms of a levodopa prodrug and methods of use.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.