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US 6,747,034 B2Granted
CRF receptor antagonists and methods relating thereto
AssigneeNeurocrine Biosciences, Inc.
InventorsMustapha Haddach, Marion C. Lanier, Charles Q. Huang, James R. McCarthy
Life of this patent
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Abstract
CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke.
Claims31
A compound having the following structure:
- including stereoisomers and pharmaceutically acceptable salts thereof, wherein:
- R1 is —CH(R4)(R5);
- R2 is C1-6alkyl;
- R3 is hydrogen or C1-6alkyl;
- R4 is hydrogen, C1-6alkyl, mono- or di(C3-6cycloalkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxyC1-6alkyl, or C1-6alkyloxyC1-6alkyl, and
- R5 is C1-8alkyl, mono- or di(C3-6cycloalkyl)methyl, Ar1CH2, C3-6alkenyl, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, morpholinyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl, C1-6alkyl substituted with imidazolyl, —CH2Obenzyl, or a radical of the formula —(C1-6alkanediyl))—O—CO—Ar1,
- or R4 and R5 taken together with the carbon atom to which they are bonded form a C5-8cycloalkyl optionally substituted with one or more substituents independently selected from C1-6alkyl;
- Ar is phenyl substituted with 1, 2 or 3 substituents independently selected from halo, C1-6alkyl, trifluoromethyl, cyano, C1-6alkyloxy, benzyloxy, C1-6alkylthio, nitro, amino, and mono- or di(C1-6alkyl)amino;
- or an aromatic C3-12heterocycle optionally substituted with 1, 2 or 3 substituents independently selected from halo, C1-6alkyl, trifluoromethyl, hydroxy, cyano, C1-6alkyloxy, benzyloxy, C1-6alkylthio, nitro, amino, mono- or di(C1-6alkyl)amino, and piperidinyl;
- and
- Ar1is phenyl, pyridinyl, or phenyl substituted with 1, 2 or 3 substituents independently selected from halo, C1-6alkyl, C1-6alkyloxy, di(C1-6alkyl)aminoC1-6alkyl, trifluoromethyl and C1-6alkyl substituted with morpholinyl.
8 more elements
Dependencies are inferred from the claim text.