ERGOLINE DERIVATIVES AS DOPAMINE RECEPTOR MODULATORS

摘要

The invention provides compounds of formula (I) wherein R1-R4 have any of the values defined in the specification, and salts thereof. The compounds are useful as dopamine receptor modulators for the treatment of diseases where modulation of dopamine receptors is implicated (e.g. sexual dysfunction, prolactinoma, Parkinson's disease, and Cushings disease).;

主权项

1. A compound of formula I:wherein:
R1 is —C(═O)NRaRb, —C(═O)ORc, (C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkanoyloxy, wherein any (C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkanoyloxy can optionally be substituted with one or more halo, hydroxy, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, (C1-C6)alkanoyloxy, or NRdRe; R2 is H or (C1-C6)alkyl; R3 is methyl; R4 is H, halo, —C(═O)NRhRk, —C(═O)ORc, (C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkanoyloxy, wherein any (C1-C6)alkyl, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, or (C1-C6)alkanoyloxy can optionally be substituted with one or more halo, hydroxy, (C1-C6)alkoxy, (C1-C6)alkanoyl, (C1-C6)alkoxycarbonyl, (C1-C6)alkanoyloxy, or NRmRn; Ra and Rb are each independently H, (C1-C6)alkyl, —C(═O)NRfRg, or (C1-C6)alkanoyl, wherein any (C1-C6)alkyl or (C1-C6)alkanoyl can optionally be substituted with one or more NRfRg; or Ra and Rb together with the nitrogen to which they are attached form a heterocyclic ring; Rc is H, (C1-C6)alkyl, or aryl; Rd and Re are each independently H or (C1-C6)alkyl; or Rd and Re together with the nitrogen to which they are attached form a heterocyclic ring; Rf and Rg are each independently H or (C1-C6)alkyl; or Rf and Rg together with the nitrogen to which they are attached form a heterocyclic ring; Rh and Rk are each independently H, (C1-C6)alkyl or (C1-C6)alkanoyl, wherein any (C1-C6)alkyl or (C1-C6)alkanoyl can optionally be substituted with one or more NRfRg; or Rh and Rk together with the nitrogen to which they are attached form a heterocyclic ring; and Rm and Rn are each independently H or (C1-C6)alkyl; or Rm and Rn together with the nitrogen to which they are attached form a heterocyclic ring; or a salt thereof.