Bial-portela Ca & S.a.

Other

Bial-Portela & Cª, S.a.

Tibor Eszenyi

David Alexander Learmonth

Jorge Bruno Reis Wahnon

Domenico Russo

Laszlo Erno Kiss

Michael Kreis

Klaus Reiter

Axel Zimmermann

Bjoern Schlummer

Jorge Bruno Wahnon

Keith Lorimer

William Maton

Kevin Wayne Meyer

Álmosné Kovách

Axel Zimmerman

Klaus Rieter

The present invention concerns a process for preparing a compound having the Formula A; or a pharmaceutically acceptable salt or derivative thereof, or for preparing a substituted urea compound of Formula IIa, or a pharmaceutically acceptable salt or ester thereof, the process comprising the reaction of an imidazolyl intermediate of Formula IIa' with a carbamoyl halide of the formula: R1R2NC(&#x2550;O)Hal, wherein Hal represents Cl, F, I or Br, wherein the intermediate of Formula IIa&#x2032; is prepared by oxidation of the derivative of R5 and R6, R6-C(&#x2550;O)CHR5 to form a glyoxal intermediate R6-C(&#x2550;O)(C&#x2550;O)R5, which is subjected to treatment with ammonium hydroxide and an aldehyde R8CHO to provide the intermediate of Formula IIa&#x2032; and wherein the compound substituents are as defined herein. 

Processes for the synthesis of substituted urea compounds

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.

Chemical compound useful as intermediate for preparing a catechol-O-methyltransferase inhibitor

Intermediate for preparing a catechol-O-methyltransferase inhibitor

This invention relates to novel polymorphs of (HO)NO(CH)&#x2014;(CNO)&#x2014;(CN)(CH)ClO, to processes for their preparation, and to pharmaceutical compositions containing said novel polymorphs as active pharmaceutical ingredient.

Crystal forms of 5-[3-(2,5-dichloro-4, 6-dimethyl-1-oxy-pyridine-3-yl)[1,2,4] oxadiazol-5-yl]-3-nitrobenzene-1,2-diol

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Tiszalök, Hungary

Tibor Eszenyi