Bis (benzylpyrrolidine) derivatives as dopamine agonists

C - Chemistry – Metallurgy – 07 – D

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167/233, 260/323

C07D 207/08 (2006.01) A61K 31/40 (2006.01) C07D 207/333 (2006.01)

Patent

CA 2019464

26690-FF ABSTRACT OF THE DISCLOSURE Dopamine agonist compounds useful in the treatment of hypertension and congestive heart failure in mammals are disclosed. The dopamine agonist compounds include racemic and non-racemic mixtures of chiral compounds as well as optically pure R,R; R,S and S,S stereoisomers which are all intended to be schematically described by the following general formula (I) (I) Image wherein: R1 is independently hydrogen, lower alkyl, -C(O)R3, or -C(O)NR3R4, wherein R3 and R4 are independently lower alkyl, optionally substituted phenyl or phenyl lower alkyl; R2 is hydrogen or lower alkyl; X is -(CH2)m- or -(CH2)nY(CH2)n-, where m is an integer from 1 to 10, n is an integer of 1 to 3, and Y is oxygen or sulfur; All of R1, and R2 are most preferably hydrogen, X is most preferably -(CH2)m- and the preferred optically pure R stereoisomer (most preferably R,R stereoisomer) of the dopamine agonist is preferably in the form of a pharmaceutically acceptable salt, preferably included in a dosage form with a suitable carrier. 1FF26690 26690-FF

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