Abstract: The invention provides methyl-substituted pyridine and pyridazine compounds, derivatives thereof, and methods of their use. The compounds are useful as pharmacological agents to treat a variety of conditions, including various pain states, itch, and cough.

Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “-----” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptable s

Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula I: wherein “ - - - ” is absent or is optionally a bond; q is 1 or 2; R1 is independently selected from hydrogen, —C1-C2 alkyl, halo, hydroxy, —C1-C2 haloalkyl, —C1-C3 alkoxy, cyano, —O—C3-C4 cycloalkyl, and —OC1-C2 haloalkyl; R2 is selected from the group consisting of hydrogen, —C1-C3 alkyl, hydroxy, —C1-C3 alkoxy, cyano, —C1-C2 haloalkyl, —OC1-C2 haloalkyl, and halo; R3 is selected from the group consisting of hydrogen, —C1-C4 alkyl, —C2-C4 haloalkyl, —C2-C4 alkylOH, —C3-C6 cycloalkyl, —CH2C3-C6 cycloalkyl, —C2-C4 alkyl-O—C1-C4 alkyl, —C(O)C1-C4 alkyl, —C(O)C1-C4 haloalkyl, —CH2-thiazole, phenyl, benzyl, tetrahydrothiopyranyl, and tetrahydropyranyl, wherein the cycloalkyl, tetrahydrothiopyranyl, tetrahydropyranyl and thiazolyl group is optionally substituted with one or two groups independently selected from the group consisting of halo, hydroxy, C1-C2 alkyl, and —C1-C2 haloalkyl; or a pharmaceutically acceptable

Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1 -4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an alkyl group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an alkyl group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.

Abstract: Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl-C.sub.1-4 alkoxy;R.sup.3 istetrazolyl, orand R.sup.4 and R.sup.5 are each hydrogen, hydroxy, acyloxy, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halo, optionally substituted phenyl, --SO.sub.3 H or --NR'R" where R' and R" are each hydrogen or C.sub.1-4 alkyl;provided that when R.sup.3 is --CR'R".CHR'"CO.sub.2 H or tetrazolyl, R.sup.1 and R.sup.2 are each hydroxyl, halo, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, acyloxy, --O-glucoside, optionally substituted phenyl or optionally substituted phenyl C.sub.1-4 alkoxy; andor a pharmaceutically acceptable salt or ester thereof.

Abstract: Methods of treating an immune disease, cell proliferation, restenosis and vascular smooth muscle cells using the pharmaceutical compounds of the formula ##STR1## in which R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl; and salts thereof.

Abstract: This invention provides a method of treating diabetic complications in mammals which comprises the administration of a compound of the Formula I: ##STR1## in which n, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are variables.