Patent ID: 6831075
Filing Date: 2004-12-14
Classification: A61P,C07D

Abstract:
A compound of Formula I: or a stereoisomer or pharmaceutically acceptable salt thereof, wherein: Het is a heterocycle selected from: R1 is selected from H, C1-10 alkyl substituted with 0-5 R6, C2-8 alkenyl substituted with 0-5 R6, C2-8 alkynyl substituted with 0-5 R6, NRaRa, C(&boxH;O)Rb, C(&boxH;O)NHRa, CO2Rc, and heterocycle substituted with 0-5 R6; with the provisos that when R1 and Het are both 2-pyridinyl, R2 and R3 are other than 4-diethylamino-2-phenyl or phenyl subsituted with methyl or diisopropylamino; and when R1 is 4-carboxy-phenethyl, Het and either R2 or R3 are other than both dimethylamino-thiophene; and when R1 and R2 are alkyl, Het is other than furanyl, thienyl or pyrrolyl; R2 and R3 are independently selected from H, C1-2 alkyl substituted with 1-5 R6, C3-10 alkyl substituted with 0-5 R6, C2-8 alkenyl substituted with 0-5 Ri, C2-6 alkynyl, Cl, Br, I, CN, (CH2)rNRaRa, (CH2)rORc, (CH2)rSRc, (CH2)rC(&boxH;O)Rb, (CH2)rCO2Rc, (CH2)rOC(&boxH;O)Rb, (CH2)rC(&boxH;O)NRaRa, (CH2)rNRaC(&boxH;O)Rb, (CH2)rNRaC(&boxH;O)ORb, (CH2)rOC(&boxH;O)NHRa, (CH2)rNRaS(&boxH;O)2Rb, (CH2)rS(&boxH;O)2NRaRa, (CH2)rS(O)pRb, (CH2)rcarbocycle substituted with 0-5 R4, and (CH2)rheterocycle substituted with 0-5 R4; alternatively, R2 and R3 join to form a heterocycle substituted with 0-4 R4, with the provisos that the heterocycle is other than 2-thiazolidinyl or 5-methyl-2-oxazolidinyl; and when Het is furanyl, R2 and R3 are not joined to form a heterocycle; with the provisos that R2 and R3 are other than both H or both SCH3; and when R2 is H, and R3 is phenyl, Het is other than 2-furanyl; and when R2 is H and R3 is (CH2)rNRaRa, r is other than 0; R4, at each occurrence, is independently selected from H, F, Cl, Br, I, CN, CF2CF3, CF3, NO2, CN, OH, NRaRa, ORc, C(&boxH;O)Rb, CO2Rc, OC(&boxH;O)Rb, NRaC(&boxH;O)Rb, C(&boxH;O)NRaRa, OC(&boxH;O)NRaRa, NRaC(&boxH;O)ORb, NRaS(&boxH;O)2Rb, S(&boxH;O)2NRaRa, NRaC(&boxH;S)Rb, C(&boxH;S)NRaRa, NRaC(&boxH;O)NRaRa, NRaC(&boxH;S)NRaRa, CH&boxH;NORc, CH&boxH;NRa, CH&boxH;NNRaRa, (CH2)rS(O)pRb, O(CH2)qNRaRa, O(CH2)qORc, (CH2)rORd, (CH2)rC(&boxH;O)Rdâ€², (CH2)rNHRd, (CH2)rS(O)pRdâ€², C1-10 alkyl subsituted with 0-5 R6, C2-8 alkenyl substituted with 0-5 R6, C2-8 alkynyl substituted with 0-5 R6; carbocycle substituted with 0-5 R6, and heterocycle substituted with 0-5 R6; R6, at each occurrence, is independently selected from C1-6 alkyl substituted with 0-5 Rh, C2-8 alkenyl, substituted with 0-5 Rh, C2-8 alkynyl substituted with 0-5 Rh, F, Cl, Br, I, CN, CF2CF3, CF3, NO2, CN, NRfRf, ORf, C(&boxH;O)Rf, CO2Rf, OC(&boxH;O)Rg, NRfC(&boxH;O)Rf, C(&boxH;O)NRfRf, OC(&boxH;O)NRfRf, NReC(&boxH;O)ORg, NReS(&boxH;O)2Rg, S(&boxH;O)2NRfRf, NRaC(&boxH;S)Rg, C(&boxH;S)NRfRf, NRfC(&boxH;O)NRfRf, NRfC(&boxH;S)NRfRf, CH&boxH;NORe, CH&boxH;NRe, CH&boxH;NNReRe, S(O)pRf, O(CH2)pNRfRf, O(CH2)pORf, ORd, NHRd, C(&boxH;O)Rdâ€², S(O)pRdâ€², carbocycle substituted with 0-5 Rh, heterocycle substituted with 0-5 Rh, P(&boxH;O)(ORc)2, and a C5-7 monosaccharide wherein each hydroxyl group of the monosaccharide is unsubstituted or replaced by a group selected from H, C1-4 alkyl, C1-4 alkoxy, and OC(&boxH;O)C1-4 alkyl; Ra, at each occurrence, is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, (CH2)rC3-6 cycloalkyl, and (CH2)rphenyl, wherein when Ra is other than H, Ra is substituted with 0-5 Rh; alternatively, two Ra may join to form a linker selected from (CH2)qO(CH2)q, (CH2)qS(CH2)q, and (CH2)m, wherein the linker is substituted with 0-5 Rh; Rb, at each occurrence, is independently selected from C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, (CH2)rphenyl, and (CH2)rheterocycle, wherein Rb is substituted with 0-5 Rh; Rc, at each occurrence, is independently selected from H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, and (CH2)rphenyl, wherein when Rc is other than H, Rc is substituted with 0-5 Rh; Rd, at each occurrence, is independently selected from the residue of an amino acid after the hydroxyl group of the carboxyl group is removed; Rdâ€², at each occurrence, is independently selected from the residue of an amino acid after the hydrogen of the amine is removed; Re, at each occurrence, is independently selected from H and C1-6 alkyl; Rf, at each occurrence, is selected from H, C1-6 alkyl substituted with 0-5 Rh, and (CH2)rphenyl substituted with 0-5 Rh; Rg, at each occurrence, is independently selected from C1-6 alkyl substituted with 0-5 Rh and (CH2)rphenyl substituted with 0-5 Rh; Rh, at each occurrence, is selected from F, Cl, Br, I, OH, NO2, CN, CF3, CF2CF3, C1-4 alkyl, C2-6 alkenyl, C2-6 alkynyl, alkoxy, C3-7 cycloalkyl, carboxyl, formyl, acetyl, propanoyl, butyryl, valeryl, pivaloyl, hexanoyl, acetamido, acetate, carbamyl, carboxy, NH2, monoalkylamino, dialkylamino, phenyl, benzyl, phenethyl, napthyl, heterocycle, and keto; Ri, at each occurrence, is selected from F, Cl, Br, I, OH, NO2, CN, CF3, CF2CF3, C1-4 alkyl, C2-6 alkenyl, C2-6 alkynyl, alkoxy, C3-7 cycloalkyl, carboxyl, formyl, acetyl, propanoyl, butyryl, valeryl, pivaloyl, hexanoyl, acetamido, carbamyl, NH2, monoalkylamino, dialkylamino, phenyl, benzyl, and phenethyl; m, at each occurrence, is independently selected from 2, 3, 4, and 5; n, at each occurrence, is selected from 0, 1, 2, 3, 4, and 5; p, at each occurrence, is independently selected from 0, 1, and 2; q, at each occurrence, is independently selected from 1, 2, 3, and 4; and r, at each occurrence, is independently selected from 0, 1, 2, 3 and 4.