Patent ID: 6699855
Filing Date: 2004-03-02
Classification: A61P,C07D,C07F

Abstract:
A compound of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein:A1 is â€”CH2â€”, â€”CH2CH2â€”, or â€”CH2CH2CH2â€”; A2 is â€”CR6&boxH;; A3 is selected from â€”R9, â€”A4â€”R9, â€”A4â€”A5â€”R9, and â€”A4â€”A5â€”A6â€”R9; W is selected from the group â€”B(OR26) (OR27) â€”C(&boxH;O)C(&boxH;O)â€”Q, â€”C(&boxH;O)C(&boxH;O)NHâ€”Q, â€”C(&boxH;O)C(&boxH;O)â€”Oâ€”Q, â€”C(&boxH;O)CF2C(&boxH;O)NHâ€”Q, â€”C(&boxH;O)CF3, â€”C(&boxH;O)CF2CF3, â€”C(&boxH;O)H, an amino acid residue, â€”A7â€”A8, and â€”A7â€”A8â€”A9; Q is selected from â€”(CR10R10c)tâ€”Q1, â€”(CR10R10c)tâ€”Q2, C1-C4 alkyl substituted with Q1, C2-C4 alkenyl substituted with Q1, C2-C4 alkynyl substituted with Q1, an amino acid residue, â€”A7â€”A8, and â€”A7â€”A8â€”A9; Q1 is selected from â€”CO2R11, â€”SO2R11, â€”SO3R11, â€”P(O)2R11, â€”P(O)3R11, aryl substituted with 0-4 Q1a, 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, said heterocyclic group substituted with 0-4 Q1a; Q1a is H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, â€”CO2R19, â€”C(&boxH;O)NR19R19, â€”NHC(&boxH;O)R19, â€”SO2R19, â€”SO2NR19R19, â€”NR19R19, â€”OR19, â€”SR19, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy alternatively, NR19R19 may form a 5-6 membered heterocyclic group consisting of carbon atoms, a nitrogen atom, and optionally a second heteroatom selected from the group: O, S, and N; Q2 is â€”Xâ€”NR12â€”Z, â€”NR12â€”Yâ€”Z, or â€”Xâ€”NR12â€”Yâ€”Z; X is selected from the group: â€”C(&boxH;O)â€”, â€”Sâ€”, â€”S(&boxH;O)â€”, â€”S(&boxH;O)2â€”, â€”P(O)â€”, â€”P(O)2â€”, and â€”P(O)3â€”; Y is selected from the group: â€”C(&boxH;O)â€”, â€”Sâ€”, â€”S(&boxH;O)â€”, â€”S(&boxH;O)2â€”, â€”P(O)â€”, â€”P(O)2â€”, and â€”P(O)3â€”; Z is C1-C4 haloalkyl, C1-C4 alkyl substituted with 0-3 Za, C2-C4 alkenyl substituted with 0-3 Za, C2-C4 alkynyl substituted with 0-3 Za, C3-C10 cycloalkyl substituted with 0-5 Zb, C3-C10 carbocycle substituted with 0-5 Zb, aryl substituted with 0-5 Zb, 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, said heterocyclic group substituted with 0-4 Zb; an amino acid residue, â€”A7â€”A8, or â€”A7â€”A8â€”A9; Za is H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, â€”CO2R20, â€”C(&boxH;O)NR20R20, â€”NHC(&boxH;O)R20, â€”NR20R20, â€”OR20, â€”SR20, â€”S(&boxH;O)R20, â€”SO2R20, â€”SO2NR20R20, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C3-C10 cycloalkyl substituted with 0-5 Zb, C3-C10 carbocycle substituted with 0-5 Zb, aryl substituted with 0-5 Zb, or 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, said heterocyclic group substituted with 0-4 Zb; Zb is H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, â€”CO2R20, â€”C(&boxH;O)NR20R20, â€”NHC(&boxH;O)R20, â€”NR20R20, â€”OR20, â€”SR20, â€”S(&boxH;O)R20, â€”SO2R20, â€”SO2NR20R20, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, C3-C10 cycloalkyl substituted with 0-5 Zc, C3-C10 carbocycle substituted with 0-5 Zc, aryl substituted with 0-5 Zc, or 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, said heterocyclic group substituted with 0-4 Zc; Zc is H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, â€”CO2R20, â€”C(&boxH;O)NR20R20, â€”NHC(&boxH;O)R20, â€”NR20R20, â€”OR20, â€”SR20, â€”S(&boxH;O)R20, â€”SO2R20, â€”SO2NR20R20, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy; alternatively, NR20R20 may form a 5-6 membered heterocyclic group consisting of carbon atoms, a nitrogen atom, and optionally a second heteroatom selected from the group: O, S, and N; OR26 and OR27 are independently selected from: a) â€”OH, b) â€”F, c) â€”NR28R29, d) C1-C8 alkoxy, or â€ƒwhen taken together, OR26 and OR27 form: e) a cyclic boron ester where said chain or ring contains from 2 to 20 carbon atoms, and, optionally, 1, 2, or 3 heteroatoms which can be N, S, or O, f) a cyclic boron amide where said chain or ring contains from 2 to 20 carbon atoms and, optionally, 1, 2, or 3 heteroatoms which can be N, S, or O, g) a cyclic boron amide-ester where said chain or ring contains from 2 to 20 carbon atoms and, optionally, 1, 2, or 3 heteroatoms which can be N, S, or O; R1 is selected from the group: H, F, C1-C6 alkyl substituted with 0-3 R1a, C2-C6 alkenyl substituted with 0-3 R1a, C2-C6 alkynyl substituted with 0-3 R1a, aryl substituted with 0-5 R1a, and C3-C6 cycloalkyl substituted with 0-3 R1a; R1a is selected at each occurrence from the group: Cl, F, Br, I, CF3, CHF2, OH, &boxH;O, SH, â€”CO2R1b, â€”SO2R1b, â€”SO3R1b, â€”P(O)2R1b, â€”P(O)3R1b, â€”C(&boxH;O)NHR1b, â€”NHC(&boxH;O)R1b, â€”SO2NHR1b, â€”OR1b, â€”SR1b, C1-C3 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, â€”Sâ€”(C1-C6 alkyl), aryl substituted with 0-5 R1c, â€”Oâ€”(CH2)q-aryl substituted with 0-5 R1c, â€”Sâ€”(CH2)q-aryl substituted with 0-5 R1c, 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and substituted with 0-3 R1c; R1b is H, C1-C4 alkyl substituted with 0-3 R1c, C2-C4 alkenyl substituted with 0-3 R1c, C2-C4 alkynyl substituted with 0-3 R1c, C3-C6 cycloalkyl substituted with 0-5 R1c, C3-C6 carbocycle substituted with 0-5 R1c, aryl substituted with 0-5 R1c, 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, said heterocyclic group substituted with 0-4 R1c; R1c is selected at each occurrence from the group: C1-C4 alkyl, Cl, F, Br, I, OH, C1-C4 alkoxy, â€”CN, â€”NO2, â€”OR1d, â€”C(&boxH;O)OR1d, â€”NR1dR1d, â€”CF3, â€”OCF3, and aryl substituted by 0-3 R1e; R1d is H, C1-C4 alkyl, phenyl or benzyl; R1e is selected at each occurrence from the methyl, ethyl, Cl, F, Br, I, OH, methoxy, ethoxy, â€”CN, â€”NO2, â€”C(&boxH;O)OR1d, NR1dR1d, CF3, and OCF3; R2 is H, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, or C3-C4 cycloalkyl; R3 is â€”R4, â€”NR4R5, â€”OR4, or â€”SR4; R4 is selected from the group: H, C1-C8 alkyl substituted with 0-3 R4a, C2-C8 alkenyl substituted with 0-3 R4a, C2-C8 alkynyl substituted with 0-3 R4a, C3-C10 cycloalkyl substituted with 0-4 R4b, aryl substituted with 0-5 R4b, 5-10 membered heterocyclic group consisting: of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R4b; R4a is, at each occurrence, independently selected from: H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, &boxH;O, OH, â€”CO2H, phenyl, â€”C(&boxH;NH)NH2, â€”NH2, â€”NH(CH3), â€”N(CH3)2, â€”CO2R11, â€”C(&boxH;O)NR11R11, â€”NHC(&boxH;O)R11, â€”NR11R11, â€”OR11a, â€”SR11a, â€”C(&boxH;O)R11a, â€”S(&boxH;O)R11a, â€”SO2R11, â€”SO2NR11R11, C1-C4 haloalkyl, C1-C4 haloalkoxy, C3-C10 cycloalkyl substituted with 0-4 R4b, aryl substituted with 0-5 R4b, and 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R4b; R4b is, at each occurrence, independently selected from: H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, &boxH;O, OH, â€”CO2H, phenyl, â€”C(&boxH;NH)NH2, â€”NH2, â€”NH(CH3), â€”N(CH3)2, â€”CO2R11, â€”C(&boxH;O)NR11R11, â€”NHC(&boxH;O)R11, â€”NR11R11, â€”OR11a, â€”SR11a, â€”C(&boxH;O)R11a, â€”S(&boxH;O)R11a, â€”SO2R11, â€”SO2NR11R11, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C6 alkyl substituted with 0-3 R4c, C2-C6 alkenyl substituted with 0-3 R4c, C2-C6 alkynyl substituted with 0-3 R4c, C3-C6 cycloalkyl substituted with 0-4 R4d, aryl substituted with 0-5 R4d, and 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R4d; R4c is, at each occurrence, independently selected from: H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, &boxH;O, OH, â€”CO2H, phenyl, â€”C(&boxH;NH)NH2, â€”NH2, â€”NH(CH3), â€”N(CH3)2, â€”CO2R11, â€”C(&boxH;O)NR11R11, â€”NHC(&boxH;O)R11, â€”NR11R11, â€”OR11a, â€”SR11a, â€”C(&boxH;O)R11a, â€”S(&boxH;O)R11a, â€”SO2R11, â€”SO2NR11R11, C1-C4 haloalkyl, C1-C4 haloalkoxy, C3-C6 cycloalkyl substituted with 0-4 R4d, aryl substituted with 0-5 R4d, 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R4d; R4d is, at each occurrence, independently selected from: H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, &boxH;O, OH, â€”CO2H, phenyl, â€”NH2, â€”NH(CH3), â€”N(CH3)2, â€”CO2R11, â€”C(&boxH;O)NR11R11, â€”NHC(&boxH;O)R11, â€”NR11R11, â€”OR11a, â€”SR11a, â€”C(&boxH;O)R11a, â€”S(&boxH;O)R11a, â€”SO2R11, â€”SO2NR11R11, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, and C1-C4 haloalkoxy; R5 is selected from the group: H, C1-C6 alkyl, phenyl, phenylmethyl-, phenylethyl-, C3-C6 cycloalkyl, C3-C6 cycloalkylmethyl-, and C3-C6 cycloalkylethyl-; R6 is selected from the group: H, F, Cl, Br, I, C1-C6 alkyl substituted with 0-3 R6a, C2-C6 alkenyl substituted with 0-3 R6a, C2-C6 alkynyl substituted with 0-3 R6a, C3-C6 cycloalkyl substituted with 0-4 R6b, aryl substituted with 0-5 R6b, 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R6b; R6a is selected from the group: H, F, Cl, Br, I, â€”CO2R11, â€”NR11R11, â€”OR11, â€”SR11, â€”C(&boxH;NH)NH2, C3-C6 cycloalkyl substituted with 0-4 R6b, aryl substituted with 0-5 R6b, 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R6b; R6b is selected from the group: H, F, Cl, Br, I, â€”CO2R11, â€”NR11R11, â€”OR11, â€”SR11, â€”C(&boxH;NH)NH2; C1-C6 alkyl substituted with 0-3 R6c, C2-C6 alkenyl substituted with 0-3 R6c, C2-C6 alkynyl substituted with 0-3 R6c, C3-C6 cycloalkyl substituted with 0-4 R6d, aryl substituted with 0-5 R6d, 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R6d; R6c is selected from the group: H, F, Cl, Br, I, â€”CO2R11, â€”NR11R11, â€”OR11, â€”SR11, â€”C(&boxH;NH)NH2, C3-C6 cycloalkyl substituted with 0-4 R6d, aryl substituted with 0-5 R6d, 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R6d; R6d is selected from the group: H, F, Cl, Br, I, â€”CO2R11, â€”NR11R11, â€”OR11, â€”SR11, â€”C(&boxH;NH)NH2; R8 is H, C1-C4 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, or C3-C4 cycloalkyl; R9 is selected from the group: â€”S(&boxH;O)R9a, â€”S(&boxH;O)2R9a, â€”C(&boxH;O)R9a, â€”C(&boxH;O)OR9a, â€”C(&boxH;O)NHR9a, C1-C3 alkyl-R9a, C2-C6 alkenyl-R9a, and C2-C6 alkynyl-R9a; R9a is selected from the group: H C1-C6 alkyl substituted with 0-3 R9b, C3-C6 cycloalkyl substituted with 0-3 R9c and aryl substituted with 0-3 R9c and 5-14 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-3 R9c; R9b is selected from the group: phenyl substituted with 0-3 R9c, naphthyl substituted with 0-3 R9c, benzyl substituted with 0-3 R9c, and 5-10 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N; and said heterocyclic group is substituted with 0-3 R9c; R9c is selected at each occurrence from the group: H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, &boxH;O, OH, â€”CO2H, phenyl, â€”NH2, â€”NH(CH3), â€”N(CH3)2, â€”CO2R11, â€”C(&boxH;O)NR11R11, â€”NHC(&boxH;O)R11, â€”NR11R11, â€”OR11a, â€”SR11a, â€”C(&boxH;O)R11a, â€”S(&boxH;O)R11a, â€”SO2R11, â€”SO2NR11R11, C1-C4 haloalkyl, C1-C4 haloalkoxy, C1-C4 alkyl substituted with 0-3 R9d, C1-C4 alkoxy substituted with 0-3 R9d, C3-C6 cycloalkyl substituted with 0-3 R9d, aryl substituted with 0-5 R9d, and 5-6 membered heterocyclic group consisting of carbon atoms and 1-4 heteroatoms selected from the group: O, S, and N, and said heterocyclic group is substituted with 0-4 R9d; R9d is selected at each occurrence from the group: H, F, Cl, Br, I, â€”NO2, â€”CN, â€”NCS, â€”CF3, â€”OCF3, â€”CH3, â€”OCH3, &boxH;O, OH, â€”CO2H, phenyl, â€”NH2, â€”NH(CH3), â€”N(CH3)2, â€”CO2R11, â€”C(&boxH;O)NR11R11, â€”NHC(&boxH;O)R11, â€”NR11R11, â€”OR11a, â€”SR11a, â€”C(&boxH;O)R11a, â€”S(&boxH;O)R11a, â€”SO2R11, â€”SO2NR11R11, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, and C1-C4 haloalkoxy; R10 is selected from the group: â€”CO2R11, â€”NR11R11, and C1-C6 alkyl substituted with 0-1 R10a; R10a is selected from the group: halo, â€”NO2, â€”CN, â€”CF3, â€”CO2R11, â€”NR11R11, â€”OR11, â€”SR11, â€”C(&boxH;NH)NH2, and aryl substituted with 0-1 R10b; R10b is selected from the group: â€”CO2H, â€”NH2, â€”OH, â€”SH, and â€”C(&boxH;NH)NH2; R10c is H or C1-C4 alkyl; alternatively, R10 and R10c can be combined to form a C3-C6 cycloalkyl group substituted with 0-1 R10a; R11 is, at each occurrence, independently H or C1-C4 alkyl; R11a is, at each occurrence, independently H, C1-C4 alkyl, aryl, or C1-C4 haloalkyl; R12 is H or C1-C4 alkyl; R13 is H or C1-C4 alkyl; R19 is C1-C4 alkyl, C1-C4 haloalkyl, aryl, aryl(C1-C4 alkyl), C3-C6 cycloalkyl, or C3-C6 cycloalkyl(C1-C4 alkyl); R20 is H, C1-C4 alkyl, C1-C4 haloalkyl, aryl, aryl(C1-C4 alkyl)-, C3-C6 cycloalkyl, or C3-C6 cycloalkyl(C1-C4 alkyl)-; R28 and R29, are independently selected from: H, C1-C4 alkyl, aryl(C1-C4 alkyl)-, and C3-C7 cycloalkyl; A4, A5, A6, A7, A8, and A9 are independently selected from an amino acid residue; an amino acid residue, at each occurence, independently comprises a natural amino acid, a modified amino acid or an unnatural amino acid wherein said natural, modified or unnatural amino acid is of either D or L configuration; t is 1, 2, 3, or 4; and q is 0, 1 or 2.