Claims for Patent: 9,630,955

Summary for Patent: 9,630,955

Title:	Chemical compound useful as intermediate for preparing a catechol-O-methyltransferase inhibitor
Abstract:	There is disclosed a methylated intermediate which may be demethylated to provide an inhibitor of catechol-O-methyltransferase useful in the treatment of Parkinson's disease. Also disclosed are methods of making and using said intermediate.
Inventor(s):	Russo; Domenico (S. Mamede do Coronado, PT), Kiss; Laszlo Erno (S. Mamede do Coronado, PT), Wahnon; Jorge Bruno Reis (S. Mamede do Coronado, PT), Learmonth; David Alexander (Alfena, PT), Eszenyi; Tibor (Tiszalok, HU), Zimmermann; Axel (Kirkel-Altstadt, DE), Schlummer; Bjoern (Leverkusen, DE), Kreis; Michael (Leverkusen, DE), Reiter; Klaus (Linz, AT)
Assignee:
Application Number:	14/814,603
Patent Claims:	1. A crystalline compound of formula (II) ##STR00024## in microparticulate form having a particular size specification with D10 equivalent circle diameter not less than 4 .mu.m, a D50 equivalent circle diameter of 10-45 .mu.m and a D95 equivalent circle diameter of not more than 80 .mu.m. 2. A compound according to claim 1, wherein the microparticulate form is prepared by ball milling or by micronisation through spiral jet mills. 3. A compound according to claim 1, wherein the compound in the microparticulate form has a particle size specification with D10 equivalent circle diameter not less than 5 .mu.m. 4. A compound according to claim 1, wherein the compound in the microparticulate form has a particle size specification with D50 equivalent circle diameter being 15-30 .mu.m. 5. A compound according to claim 3, wherein the compound in the microparticulate form has a particle size specification with D50 equivalent circle diameter being 15-30 .mu.m. 6. A pharmaceutical composition in unit dosage form for oral administration comprises a compound of the formula (II) ##STR00025## in microparticulate form having a particular size specification with D10 equivalent circle diameter not less than 4 .mu.m, a D50 equivalent circle diameter of 10-45 .mu.m and a D95 equivalent circle diameter of not more than 80 .mu.m and a pharmaceutically acceptable carrier thereof. 7. A pharmaceutical composition according to claim 6, wherein the unit dosage form is a tablet or a capsule. 8. A method of treating Parkinson's disease in a patient suffering therefrom comprises administering to the patient an effective amount of a pharmaceutical composition according to claim 6. 9. A method according to claim 8, wherein the unit dosage form is a tablet or a capsule. 10. A compound according to claim 1, wherein the compound in the microparticulate form has a particle size specification with D10 equivalent circle diameter not less than 6.mu.m. 11. A compound according to claim 1, wherein the compound in the microparticulate form has a particle size specification with D50 equivalent circle diameter not less than 20-25 .mu.m. 12. A compound according to claim 3, wherein the compound in the microparticulate form has a particle size specification with D50 equivalent circle diameter not less than 20-25 .mu.m.