C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/315.35
C07D 231/56 (2006.01)
Patent
CA 1128951
-1- Abstract of the Disclosure Described herein are novel amino-substituted- 4,5,6,7-tetrahydro-1H (or 2H)-indazoles of the formulae Image I II wherein one of R and R1 is H and the other is N(R2)2; where each R2 is individually allyl, methyl, ethyl or n-propyl; and pharmaceutically-acceptable acid addition salts thereof. These compounds are useful as prolactin inhibitors and in the treatment of Parkinson's Syndrome. They are prepared by reacting, by reductive alkylation with an aldehyde or by reacting with an alkyl halide or anhydride followed by reduction, an 5 (or 6)-amino-4,5,6,7-tetrahydro- 1H (or 2H)-indazole compound of the formulae Image IB IIB wherein one of R and R1 is H and the other is N(R2)2 where both R2,s are H. Also disclosed are intermediate tautomers of the general formula Image VIII VIIIa wherein R5 is (C1-C3) alkyl or benzyl, which are prepared by reacting a compound of the formula Image wherein R5 is defined as above, with hydrazine hydrate.
385098
Bach Nicholas J.
Kornfeld Edmund C.
Eli Lilly And Company
Gowling Lafleur Henderson Llp
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