Naphthimidazolyl neuropeptide Y receptor antagonists
First Claim
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1. A method of treating a physiological disorder associated with an excess of neuropeptide Y, which method comprises administering to a mammal in need of said treatment an effective amount of a compound of the formula ##STR79## wherein:
- A is C1 -C6 alkylenyl;
B is --O--, --NH--, or --S--;
D is a bond or C1 -C6 alkylenyl;
R1 is C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, naphthyl, or naphthyloxy,any one of which phenyl, C3 -C8 cycloalkyl, phenoxy, naphthyl, or naphthyloxy moieties may be substituted with one or more moieties selected from the group consisting of halo, trifluoromethyl, C1 -C6 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, C1 -C6 alkylthio, C1 -C6 alkylamino, C2 -C7 alkanoyl, hydroxy, heterocyclic, unsaturated heterocyclic, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, benzyl, benzyloxy, and benzoyl;
R2 is C1 -C12 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)-,which C1 -C12 alkyl, C2 -C7 alkenyl, or C2 -C7 alkynyl may be substituted with halo or hydroxy, and any one of which heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)- groups may be substituted with one or more moieties selected from the group consisting of C1 -C6 alkyl, hydroxy, C1 -C6 alkoxy, phenyl, naphthyl, phenyl(C1 -C6 alkylenyl)-, naphthyl(C1 -C6 alkylenyl)-, halo, trifluoromethyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, heterocyclic, unsaturated heterocyclic, heterocyclic(C1 -C6 alkylenyl)-, unsaturated heterocyclic(C1 -C6 alkylenyl)-, heterocyclic(C1 -C6 alkoxy)-, unsaturated heterocyclic(C1 -C6 alkoxy)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, C2 -C7 alkanoyl, C2 -C7 alkanoyloxy, C1 -C6 alkylamino, C1 -C6 alkylthio, amino, nitro, and an amino-protecting group;
or a pharmaceutically acceptable salt or solvate thereof.
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Abstract
This invention provides a series of substituted 1H-naphth 2,3-d!imidazoles which are useful in treating a condition associated with an excess of neuropeptide Y. This invention also provides methods employing these substituted 1H-naphth 2,3-d!imidazoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these compounds.
13 Citations
30 Claims
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1. A method of treating a physiological disorder associated with an excess of neuropeptide Y, which method comprises administering to a mammal in need of said treatment an effective amount of a compound of the formula ##STR79## wherein:
- A is C1 -C6 alkylenyl;
B is --O--, --NH--, or --S--; D is a bond or C1 -C6 alkylenyl; R1 is C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, naphthyl, or naphthyloxy, any one of which phenyl, C3 -C8 cycloalkyl, phenoxy, naphthyl, or naphthyloxy moieties may be substituted with one or more moieties selected from the group consisting of halo, trifluoromethyl, C1 -C6 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, C1 -C6 alkylthio, C1 -C6 alkylamino, C2 -C7 alkanoyl, hydroxy, heterocyclic, unsaturated heterocyclic, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, benzyl, benzyloxy, and benzoyl; R2 is C1 -C12 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)-, which C1 -C12 alkyl, C2 -C7 alkenyl, or C2 -C7 alkynyl may be substituted with halo or hydroxy, and any one of which heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)- groups may be substituted with one or more moieties selected from the group consisting of C1 -C6 alkyl, hydroxy, C1 -C6 alkoxy, phenyl, naphthyl, phenyl(C1 -C6 alkylenyl)-, naphthyl(C1 -C6 alkylenyl)-, halo, trifluoromethyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, heterocyclic, unsaturated heterocyclic, heterocyclic(C1 -C6 alkylenyl)-, unsaturated heterocyclic(C1 -C6 alkylenyl)-, heterocyclic(C1 -C6 alkoxy)-, unsaturated heterocyclic(C1 -C6 alkoxy)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, C2 -C7 alkanoyl, C2 -C7 alkanoyloxy, C1 -C6 alkylamino, C1 -C6 alkylthio, amino, nitro, and an amino-protecting group; or a pharmaceutically acceptable salt or solvate thereof. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10)
- A is C1 -C6 alkylenyl;
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11. A compound of the formula ##STR80## wherein:
- A is C1 -C6 alkylenyl;
B is --O--, --NH--, or --S--; D is a bond or C1 -C6 alkylenyl; R1 is C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, naphthyl, or naphthyloxy, any one of which phenyl, C3 -C8 cycloalkyl, phenoxy, naphthyl, or naphthyloxy moieties may be substituted with one or more moieties selected from the group consisting of halo, trifluoromethyl, C1 -C6 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, C1 -C6 alkylthio, C1 -C6 alkylamino, C2 -C7 alkanoyl, hydroxy, heterocyclic, unsaturated heterocyclic, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, benzyl, benzyloxy, and benzoyl; R2 is C1 -C12 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)-, which C1 -C12 alkyl, C2 -C7 alkenyl, or C2 -C7 alkynyl may be substituted with halo or hydroxy, and any one of which heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)- groups may be substituted with one or more moieties selected from the group consisting of C1 -C6 alkyl, hydroxy, C1 -C6 alkoxy, phenyl, naphthyl, phenyl(C1 -C6 alkylenyl)-, naphthyl(C1 -C6 alkylenyl)-, halo, trifluoromethyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, heterocyclic, unsaturated heterocyclic, heterocyclic(C1 -C6 alkylenyl)-, unsaturated heterocyclic(C1 -C6 alkylenyl)-, heterocyclic(C1 -C6 alkoxy)-, unsaturated heterocyclic(C1 -C6 alkoxy)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, C2 -C7 alkanoyl, C2 -C7 alkanoyloxy, C1 -C6 alkylamino, C1 -C6 alkylthio, amino, nitro, and an amino-protecting group; or a salt or solvate thereof. - View Dependent Claims (12, 13, 14, 15, 16, 17, 18, 19, 20)
- A is C1 -C6 alkylenyl;
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21. A pharmaceutical formulation which comprised a compound of the formula ##STR81## wherein:
- A is C1 -C6 alkylenyl;
B is --O--, --NH--, or --S--; D is a bond or C1 -C6 alkylenyl; R1 is C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, naphthyl, or naphthyloxy, any one of which phenyl, C3 -C8 cycloalkyl, phenoxy, naphthyl, or naphthyloxy moieties may be substituted with one or more moieties selected from the group consisting of halo, trifluoromethyl, C1 -C6 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, C1 -C6 alkylthio, C1 -C6 alkylamino, C2 -C7 alkanoyl, hydroxy, heterocyclic, unsaturated heterocyclic, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, phenyl, phenoxy, benzyl, benzyloxy, and benzoyl; R2 is C1 -C12 alkyl, C2 -C7 alkenyl, C2 -C7 alkynyl, heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)-, which C1 -C12 alkyl, C2 -C7 alkenyl, or C2 -C7 alkynyl may be substituted with halo or hydroxy, and any one of which heterocyclic(C1 -C6 alkylenyl)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, unsaturated heterocyclic(C1 -C6 alkylenyl)-, phenyl, phenyl(C1 -C6 alkylenyl)-, naphthyl, naphthyl(C1 -C6 alkylenyl)-, phenoxy(C1 -C6 alkylenyl)-, naphthyloxy(C1 -C6 alkylenyl)-, or benzoyl(C1 -C6 alkylenyl)- groups may be substituted with one or more moieties selected from the group consisting of C1 -C6 alkyl, hydroxy, C1 -C6 alkoxy, phenyl, naphthyl, phenyl(C1 -C6 alkylenyl)-, naphthyl(C1 -C6 alkylenyl)-, halo, trifluoromethyl, C2 -C7 alkenyl, C2 -C7 alkynyl, C1 -C6 alkoxy, heterocyclic, unsaturated heterocyclic, heterocyclic(C1 -C6 alkylenyl)-, unsaturated heterocyclic(C1 -C6 alkylenyl)-, heterocyclic(C1 -C6 alkoxy)-, unsaturated heterocyclic(C1 -C6 alkoxy)-, C3 -C8 cycloalkyl, C3 -C8 cycloalkenyl, C2 -C7 alkanoyl, C2 -C7 alkanoyloxy, C1 -C6 alkylamino, C1 -C6 alkylthio, amino, nitro, and an amino-protecting group; or a pharmaceutically acceptable salt or solvate thereof, in combination with one or more pharmaceutically acceptable carriers, excipients, or diluents therefor. - View Dependent Claims (22, 23, 24, 25, 26, 27, 28, 29, 30)
- A is C1 -C6 alkylenyl;
Specification
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Current AssigneeEli Lilly and Company
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Original AssigneeEli Lilly and Company
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InventorsZarrinmayeh, Hamideh, Nunes, Anne Marie
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Primary Examiner(s)Jarvis, William R. A.
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Application NumberUS08/775,533Time in Patent Office544 DaysField of Search514/322, 514/232.8, 514/393, 514/394, 514/395, 548/302.1, 544/139, 546/199US Class Current514/232.8CPC Class CodesC07D 235/02 condensed with carbocyclic ...C07D 401/06 linked by a carbon chain co...C07D 401/12 linked by a chain containin...C07D 403/12 linked by a chain containin...C07D 405/06 linked by a carbon chain co...C07D 417/12 linked by a chain containin...C07D 417/14 containing three or more he...
