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US 9,670,199 B2Granted
Ergoline derivatives as dopamine receptor modulators
AssigneeRegents of the University of Minnesota
InventorsPeter Dosa, Suck Won Kim, Michael Walters
Life of this patent
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Abstract
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).
Claims10
A compound of formula I:
- wherein:
- R1 is —C(═O)NRaRb;
- R2 is (C1-C6)alkyl;
- R3 is methyl;
- R4 is H, halo, —C(═O)NRhRk, —C(═O)OK, (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 is —C(═O)NRfRg;
- Rb is (C1-C6)alkyl that is substituted with one or more NRfRg;
- Rc is H, (C1-C6)alkyl, or aryl;
- 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.
13 more elements
A compound of formula I:
- wherein R1 is:
- R2 is (C1-C6)alkyl;
- R3 is methyl;
- R4 is H, —C(═O)NRhRk, —C(═O)ORc, (C1-C6)alkyl, (C1-C6)alkanol, (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;
- Rc is H, (C1-C6)alkyl, or aryl;
- 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.
8 more elements
A compound of formula I:
- wherein R1 is:
- 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;
- Rc is H, (C1-C6)alkyl, or aryl;
- 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.
8 more elements
A compound which is:
- or a salt thereof.
Dependencies are inferred from the claim text.