Oxazolidinone antibacterial agents having a thiocarbonyl functionality

A compound of the formula I

• 199
• or pharmaceutical acceptable salts thereof wherein:
• G is
• 200
• R1 is
• a) HF
• b) NH2,
• c) NH—C1-4 alkyl,
• d) C1-4 alkly,
• e) —OC1-4 alkyl,
• f) —S1-4 alkyl,
• g) C1-4 alkyl substituted with 1-4 F, 1-2Cl, CNor —COOC1-4 alkyl
• h) C3-6 cyrcloalkyl,
• i) N(C1-4) alkyl)2or
• j) N(CH2)2-5;
• A is
• 201
• d) a 5-membered heteroaromatic moiety having one to three atoms selected from the group consisting of S, N, and O, wherein the 5-membered heteroaromatic moiety is bonded via a carbon atom,
• wherein the 5-membered heteroaromatic moiety can additionally have a fused-on benzene or naphthyl ring,
• wherein the heteroaromatic moiety is optionally substituted with one to three R48,
• e) a 6-membered heteroaromatic moiety having at least one nitrogen atom,
• wherein the heteroaromatic moiety is bonded via a carbon atom, wherein the 6-membered heteroaromatic moiety can additionally have a fused-on benzene or naphthyl ring,
• wherein the heteroaromatic moiety is optionally substituted with one to three R55,
• f) a β-carbolin-3-yl, or indolizinyl bonded via the 6-membered ring, optionally substituted with one to three R55,
• 202
• wherein R2 is
• a) H,
• b) F,
• c) Cl,
• d) Br,
• e) C1-3 alkyl,
• f) NO2, or
• g) R2 and R3 taken together are —O—(CH2)h—O—;
• R3 is
• a) —S(═O)i R4,
• b) —S(═O)2—N═S(O)jR3R6,
• c) —SC(═O)R7,
• d) —C(═O)R8,
• e) —C(═O)R9,
• f) —C(═O)NR10R11,
• g) —C(═NR12)R8,
• h) —C(R8)(R11)—OR13,
• i) —C(R9)(R11)—OR13,
• j) —C(R8)(R11)—OC(═O)R13,
• k) —C(R9)(R11)—OC(═O)R13,
• l) —NR10R11,
• m) —N(R10)—S(═)iR7,
• n) —N(R10)—S(═O)iR7,
• o) —C(OR14)(OR15)R8,
• p) —C(R8)R16)—NR10R11, or
• q) C1-8 alkyl substituted with one or more ═O other than at alpha position, —S(═O)iR17, —NR10R11, C2-5 alkenyl, or C4 alkynyl;
• R4 is
• a) C1-4 alkyl optionally substituted with one or more halos, OH, CN, NR10R11, or —CO2R13,
• b) C2-4 alkenyl,
• c) —NR16R18,
• d) —N3,
• e) —NHC(═O)R7,
• f) —NR20C(═O)R7,
• g) —N(R19)2,
• h) —NR16R19, or
• i) —NR19R20,
• R5 and R6 at each occrrence are the same or different and are
• a) C1-8 alkyl, or
• b) R5 and R6 taken together are —(CH2)k-;
• R7 is C1-4 alkyl optionally substituted with one or more halos;
• R8 is
• a) H, or
• b) C1-8 alkyl optionally substituted with one or more halos, or C3-8 cycloalkyl;
• R9 is C1-4 alkyl substituted with one or more
• a) —S(═O)R17,
• b) —OR13,
• c) —OC(═O)R13,
• d) —NR10R11, or
• e) C1-5 alkenyl optionally substituted with CHO;
• R10 and R11 at each occurrence are the same or different and are
• a) H,
• b) C1-4 alkyl, or
• c) C3-8 cycloalyl;
• R12 is
• a) —NR10R11,
• b) —OR10;
• or
• c) —NHC(═O)R10;
• R13 is
• a) H, or
• b) C1-4 alkyl;
• R14 and R15 at each occurrence are the same or different and are
• a) C1-4 alkyl, or
• b) R14 and R15 taken together are —(CH)1-;
• R15 is
• a) H,
• b) C1-4 alkyl, or
• c) C3-8 cycloalkyl;
• R17 is
• a) C1-4 alkyl, or
• b) C3-8 cycloalkyl;
• R18 is
• a) H,
• b) C1-4 alkyl,
• c) C2-4 alkenyl,
• d) C3-4 cycloalkyl,
• e) —OR13 or
• f) —NR21R22;
• R19 is
• a) Cl,
• b) Br, or
• c) I;
• R20 is a physiologically acceptable cation;
• R21 and R22 at each occurrence are the same or different and are
• a) H,
• b) C1-4 alkyl, or
• c) —NR21R22 taken together are —(CH2)m-;
• wherein R23 and R24 at each occurrence are the same or different and are
• a) H,
• b) F,
• c) Cl,
• d) C1-2 alkyl,
• e) CN
• g) C1-2 alkoxy,
• h) nitro, or
• i) amino;
• Q is
• 203
• m) a diazinyl group optionally substituted with X and Y,
• n) a triazinyl group optionally substituted with X and Y,
• o) a quinolinyl group optionally substituted with X and Y,
• p) a quinoxalinyl group optionally substituted with X and Y,
• q) a naphthyridinyl group optionally substituted with X and Y,
• 204
• Q and R24 taken together are
• 205
• wherein Z1 is
• a) CH2-,
• b) —CH(R104)—CH2-,
• c) —C(O)—, or
• d) —CH2CH2CH2-;
• wherein Z2 is
• a) —O2S
• b) —O—
• c) —N(R107)-,
• d) —OS—, or
• e) —S—;
• wherein Z3 is
• a) —O2S—,
• b) —O—,
• c) —OS—, or
• d) —S—;
• wherein A2 is
• a) H—, or
• b) CH3;
• wherein A2 is
• a) H—,
• b) HO—,
• c) CH3-,
• d) CH3O—,
• e) R102O—CH2—C(O)—NH—
• f) R103O—C(O)—NH—,
• g) (C1-C2)alkyl—O—C(O)—,
• h) HO—CH2—,
• i) CH3O—NH—,
• j) (C1-C3)alkyl—O2C—
• k) CH3—C(O)—,
• l) CH3—C(O)—CH2—,
• 206
• A1 and A2 taken together are:
• 207
• wherein R102 is
• a) H—, or
• b) CH3—;
• c) phenyl—CH2—, or
• d) CH3C(O)—;
• wherein R103 is
• a) (C1-C3)alkyl—, or
• b) phenyl—;
• wherein R104 is
• a) H—, or
• b) HO—;
• wherein R105 is
• a) H—,
• b) (C1C3)alkyl—,
• c) CH2═CH—CH2—, or
• d) CH3—O—(CH2)2—;
• wherein R106 is
• a) CH3—C(O)—,
• b) H—C(O)—,
• c) Cl2CH—C(O)—,
• d) HOCH2—C(O)—,
• e) CH3SO2—,
• 208
• g) F2CHC(O)—,
• 209
• i) H3C—C(O)—O—CH2(O)—,
• j) H—C(O)—O—CH2—C(O)—,
• 210
• l) HC═C—CH2O—CH2—C(O)—, or
• m) phenyl—CH2—O—CH2—C(O)—;
• wherein R107 is
• a) R102O—C(R110)(R111)—C(O)—,
• b) R103O—C(O)—,
• c) R106—C(O)—,
• 211
• f) H3C—C(O)—(CH2)2C(O)—,
• g) R109—SO2—,
• 212
• i) HO—CH2—C(O)—,
• j) R116—(CH2)2—,
• k) R113—C(O)—O—CH2—C(O)—,
• l) (CH3)2N—CH2—C(O)—NH—,
• m) NC—CH2—,
• n) F2—CH—CH2—, or
• wherein R108 is
• a) H—,
• b) (C1-C4)alkyl,
• c) aryl—CH2)p,
• e) ClH2C—,
• f) FH2C—,
• g) F2HC—,
• h) (C3-C6)cycloalky, or
• i) CNCN2—,
• wherein R109 is
• a) (C3-C4)alkyl;
• b) —CH2Cl
• c) —CH2CH═CH2,
• d) aryl, or
• e) —CH2CN;
• wherein R110 and R111 are independently
• a) H—,
• b) CH3—;
• or
• wherein R112 is
• a) H—,
• b) CH3O—CH2O—CH2—, or
• c) HOCH2—;
• wherein R113 is
• a) CH3—,
• b) HOCH2—,
• c) (CH3)2N—phenyl, or
• d) (CH3)2N—CH2—;
• wherein R114 is
• a) HO—,
• b) CH3O—,
• c) H2N—,
• d) CH3O—C(O)—O—,
• e) CH3—C(O)—O—CH2—C(O)—O—,
• f) phenyl—CH2—O—CH2—C(O)—O—,
• g) HO—CH2)2—O—,
• h) CH3O—CH2—O—(CH2)2—O—, or
• i) CH3O—CH2—O—;wherein R113 is
• a) CH3—,
• b) HOCH2—,
• c) (CH3)2N—phenyl, or
• d) (CH3)2N—CH2—;
• wherein R115 is
• a) H—, or
• b) Cl—;
• wherein R116 is
• a) HO—
• b) CH3O—, or
• c) F;
• wherein R150 and R151 are each H or alkylC1-4 or R150 and R151 taken together with the nitrogen atom to which each is attached form a monocyclic heterocclic ring having from 3 to 6 carbon atoms;
• B is an unsaturated 4-atom linker having one nitrogen and three carbons;
• M is
• a) H,
• b) C1-8 alkyl,
• c) C3-8 cycloalkyl,
• d) —(CH2)mOR13, or
• e) —(CH2)h—NR21R22;
• Z is
• a) O,
• b) S, or
• c) NM;
• W is
• a) CH,
• b) N, or
• c) S or O when Z is NM;
• Y is
• a) H,
• b) F,
• c) Cl,
• d) Br,
• e) C1-3 alkyl, or
• f) NO2;
• X is
• a) H,
• b) —CN,
• c) OR27,
• d) halo,
• e) NO2,
• f) tetrazoyl,
• g) —SH,
• h) —S(═O)iR4,
• i) —S(═O)2—N═S(O)jR6Rt,
• j) —SC(═O)R7,
• k) —C(═O)R25,
• l) —C(═O)NR27R28,
• m) —C(═NR29)R25,
• n) —C(R25)(R28)—OR13,
• o) —C(R25)(R28)—OC(═O)R13,
• p) —C(R28)(OR13)—(CH2)h—NR27R28,
• q) —NR27R28,
• r) —N(R27)C(═O)R7,
• s) —N(R27)—S(═O)iR7,
• t) —C(OR14)(OR15)R28,
• u) —C(R25)(R16)—NR27R26, or
• v) C1-8 alkyl substituted with one or more halos, OH, ═O other than at alpha position, —S(═O)iR17, —NR27,R28, C2-5 alkenyl, C2-5 alkynyl, or C3-8 cycloalkyl;
• R4, R5, R6, R7, R13, R14, R15, R16, and R17 are the same as defined above;
• R25 is
• a) H,
• b) C1-8 alkyl optionally substituted with one or more halos, C3-8 cycloalkyl, C1-4 alkyl substituted with one or more of —S(═O)iR17, —OR13, or OC(═O)R13, NR27R28, or
• c) C2-5 alkenyl optionally substituted with CHO, or CO2R13;
• R26 is
• a) R28, or
• b) NR27N28;
• R27 and R28 at each occurrence are the same or different and are
• a) H,
• b) C1-8 alkyl,
• c) C3-8 cycloalkyl,
• d) —(CH2)mOR13,
• e) —(CH2)h—NR21R22, or
• f) R27 and R28 taken together are —(CH2)2O(CH2)2—, —(CH2)hCH(COR7), or —(CH2)2N(CH2)2(R7);
• R29 is
• a) —NR27R28,
• b) —OR27, or
• c) —NHC(═O)R28;
• wherein R30 is
• a) H,
• b) C1-8 alkyl optionally substituted with one or more halos, or
• c) C1-8 alkyl optionally substituted with one or more OH, or C1-6 alkoxy,
• wherein E is
• a) NR39,
• b) —S(═O)i, or
• c) O;
• R38 is
• a) H,
• b) C1-6 alkyl,
• c) —(CH2)q—aryl, or
• d) halo;
• R39 is
• a) H,
• b) C1-6 alkyl optionally substituted with one or more OH, halo, or —CN,
• c) —(CH2)q—aryl,
• d) —CO2R40,
• e) —COR41,
• f) —C(═O)—(CH2)q—C(═O)R40,
• g) —S(═O)2—C1-6 alkyl,
• h) —S(═O)2—CH2)q—aryl, or
• i) —(C═O)j—Het;
• R40 is
• a) H,
• b) C1-6, alkyl optionally substituted with one or more OH, halo, or —CN,
• c) —(CH2)q—aryl, or
• d) —(CH2)q—OR42;
• R41 is
• a) C1-6 alkyl optionally substituted with one or more OH, halo, or -—CN,
• b) —CH2)q—aryl, or
• c) —(CH2)q—OR42;
• R42 is
• a) H,
• b) C1-6 alky,
• c) —(CH2)q—aryl, or
• d) —C(═O)—C1-6 alkyl;
• aryl is
• a) phenyl,
• b) pyridyl, or
• c) napthyl;
• a to c optionally substituted with one or more halo, —CN, OH, SH, C1-6 alkyl, C1-6 alkoxy, or C1-6 alkylthio;
• wherein R43 is
• a) H,
• b) C1-2 alkyl,
• c) F, or
• d) OH;
• R14 is
• a) H,
• b) CF3,
• c) C1-3 alkyl optionally substituted with one or more halo,
• d) phenyl optionally substituted with one or more halo,
• e) R44 and R45 taken together are a 5-, 6-, or 7-membered ring of the formula,
• or
• 213
• f) R44 and R45 taken together are —(CH2)k—, when R46 is an electron-withdrawing group;
• R45 and R46 at each occrrence are the same or different and are
• a) an electron-withdrawing group,
• b) H,
• c) CF3,
• d) C1-3 alkl optionally substituted with one halo,
• e) phenyl, provided at least one of R45 or R46 is an electron-withdrawing group, or
• f) R45 and R46 taken together are a 5-, 6-, 7-membered ring of the formula
• 214
• U is
• a) CH2,
• b) O,
• c) S, or
• d) NR47;
• R47 is
• a) H, or
• b) C1-5 alkyl;
• wherein R48 is
• a) carboxyl,
• b) halo,
• c) —CN,
• d) mercapto,
• e) formyl,
• f) CF3,
• g) —NO2,
• h) C1-6 alkoxy,
• i) C1-6 alkoxycarbonyl,
• j) C1-6 alkythio,
• k) C1-6 acyl,
• l) —NR49R50,
• m) C1-6 alkyl optionally substituted with OH, C1-5 alkoxy, C1-5 acyl, or —NR49R50,
• n) C2-8 alkenylphenyl optionally substituted with one or two R51,
• o) phenyl optionally substituted with one or two R51,
• p) a 5-, or 6-membered (un)saturated heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, optionally substituted with one or two R51, or
• 215
• R49 and R50 at each occurrence are the same or different and are
• a) H,
• b) C1-4 akyl,
• c) C5-6 cycloalkyl, or
• d) R49 and R50 taken together with the nitrogen atom is a 5-, 6- membered saturated heterocyclic moiety which optionally has a further hetero atom selected from the group consisting of S, N, and O, and can in turn be optionally substituted with, including on the further nitrogen atom, C1-3 alkyl, or C1-3 acyl;
• R51
• a) carboxyl,
• b) halo,
• c) —CN,
• d) mercapto,
• e) formyl,
• f) CF3,
• g) —NO2,
• h) C1-6 alkoxy,
• i) C1-6 alkoxycarbonyl,
• j) C1-6 alkythio,
• k) C1-6 acyl,
• l) C1-6 alkyl optionally substituted with OH, C1-5 alkoxy, C1-5 acyl, or —NR49R50,
• m) phenyl,
• n) —C(═O)NR52R53,
• o) —NR49R50,
• p) —N(R52)(—SO2R54),
• q) —SO2—NR52R53, or
• r) —S(═O)iR54;
• R52 and R53 at each occurrence are the same or different and are
• a) H,
• b) C1-6 alkyl, or
• c) phenyl;
• R54 is
• a) C1-4 alkyl, or
• b) phenyl optionally substituted with C1-4 alkyl;
• wherein R55 is
• a) carboxyl,
• b) halo,
• c) —CN,
• d) mercapto,
• e) formyl,
• f) CF3,
• g) —NO2,
• h) C1-6 alkoxy,
• i) C1-6 alkoxycarbonyl,
• j) C1-6 alkythio
• k) C1-6 acyl,
• l) —NR56R57,
• m) C1-4 alkyl optionally substituted with OH, C1-5 alkoxy, C1-5 acyl, or —NR56R57,
• n) C2-8 alkenylphenyl optionally substituted with one or two R58,
• o) phenyl optionally substituted with one or two R58,
• p) a 5- or 6-membered (un)saturated heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, optionally substituted with one or two R58, or
• 216
• R56 and R57 at each occurrence are the same or different and are
• a) H,
• b) formyl,
• c) C1-4 alkyl,
• d) C1-4 acyl,
• e) phenyl,
• f) C3-6 cycloalkyl, or
• g) R56 and R57 taken together with the nitrogen atom is a 5-, 6- membered saturated heterocyclic moiety which optionally has a further hetero atom selected from the group consisting of S, N, and O, and can in turn be optionally substituted with, including on the further nitrogen atom, phenyl, pyrimidyl, C1-3 alkyl, or C1-3 acyl;
• R58 is
• a) carboxyl,
• b) halo,
• c) —CN,
• d) mercapto,
• e) formyl,
• f) CF3,
• g) —NO2,
• h) C1-6 alkoxy,
• i) C1-6 alkoxycarbonyl,
• j) C1-6 alkythio,
• k) C1-6 acyl,
• l) phenyl,
• m) C1-5 alkyl optionally substituted with OH, azido, C1-5 alkoxy, C1-5 acyl, —NR65R66, —SR67, —O—SO2R65, or
• 217
• n) —C(═O)NR59R60,
• o) —NR56R57,
• p) —N(R59)(—SO2R54),
• q) —SO2—NR50R60,
• r) —S(═O)iR60,
• s) —CH═N—R61, or
• t) —CH(OH)—SO3R64;
• R54 is the same as defined above;
• R59 and R60 at each occurrence are the same or different and are
• a) H,
• b) C1-6 alkyl,
• c) phenyl, or
• d) tolyl;
• R61 is
• a) OH,
• b) benzyloxy,
• c) —NH—C(═O)—NH2,
• d) —NH—C(═S)—NH2, or
• e) —NH—C(═NH)—NR62R63;
• R62 and R63 at each occurrence are the same or different and are
• a) H, or
• b) C1-4 alkyl optionally substituted with phenyl or pyridyl;
• R64
• a) H, or
• b) a sodium ion;
• R65 and R66 at each occurrence are the same or different and are
• a) H,
• b) formyl,
• c) C1-4, alkyl,
• d) C1-4 acyl,
• e) phenyl,
• f) C3-6 cycloalkyl,
• g) R65 and R66 taken together are a 5-, 6-membered saturated heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, optionally substituted with, including on the nitrogen atom, phenyl, pyrimidyl, C1-3 alkyl, or C1-3 acyl,
• h) —P(O)(OR70)(OR71), or
• i) —SO2—R72;
• R67 is
• 218
• R68 is C1-3 alkyl;
• R69 is
• a) C1-6 alkoxycarbonyl, or
• b) carboxyl;
• R70 and R71 at each occurrence are the same or different and are
• a) H, or
• b) C1-3 alkyl;
• R72 is
• a) methyl,
• b) phenyl, or
• c) tolyl;
• wherein K is
• a) O, or
• b) S;
• R73,R74, R76, R76, and R77 at each occurrence are the same-or different and are
• a) H,
• b) carboxyl,
• c) halo,
• d) —CN,
• e) mercapto,
• f) formyl,
• g) CF3,
• h) —NO2,
• i) C1-6 alkoxy,
• j) C1-6 alkoxycarbonyl,
• k) C1-6 alkythio,
• l) C1-6 acyl,
• m) —NR78R79,
• n) C1-6 alkyl optionally substituted with OH, C1-5 alkoxy, C1-5 acyl, —NR78R79, —N(phenyl)(CH2—CH2—OH), —O—CH(CH3)(OCH2CH3), or —O—phenyl-[para-NHC(═O)CH3],
• o) C2-8 alkenylphenyl optionally substituted with R51,
• p) phenyl optionally substituted with R51, or
• q) a 5-, or 6-membered (un)saturated heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, optionally substituted with R51;
• R51 is the same as defined above;
• R78 and R79 at each occurrence are the same or different and are
• a) H,
• b) C1-4 alkyl,
• c) phenyl, or
• d) R78 and R79 taken together with the nitrogen atom is a 5-, 6-membered saturated heterocyclic moiety which optionally has a further hetero atom selected from the group consisig of S, N, and O, and can in turn be optionally substituted with, including on the further nitrogen atom, C1-3 alkyl, or C1-3 acyl;
• wherein T is
• a) O,
• b) S, or
• c) SO2;
• R75, R76, and R77 are the same as defined above;
• R80 is
• a) H,
• b) formyl,
• c) carboxyl,
• d) C1-6 alkoxycarbonyl,
• e) C1-8 alkyl,
• f) C2-8 alkenyl, wherein the substituents (e) and (f) can be optionally substituted with OH, halo, C1-6 alkoxy, C1-6 acyl, C1-6 alkylthio or C1-6 alkoxycarbonyl, or phenyl optionally substituted with halo,
• g) an aromatic moiety having 6 to 10 carbon atoms optionally substituted with carboxyl, halo, —CN, formyl, CF3, —NO2, C1-6 alkyl, C1-6 alkoxy, C1-6 acyl, C1-6 alkylthio, or C1-6 alkoxycarbonyl;
• h) —NR81R82,
• i) —OR90,
• j) —S(═O)i—R91,
• k) —SO2—N(R92)(R93), or
• l) a radical of the following formulas:
• R81 and R82 at each occurrence are the same or different and are
• a) H.
• b) C3-6 cycloalkyl,
• c) phenyl,
• d) C1-6 acyl,
• e) C1-8 alkyl optionally substituted with OH, C1-6 alkoxy which can be substituted with OH, a 5-, or 6-membered aromatic heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, phenyl optionally substituted with OH, CF3, halo, —NO2,
• C1-4 alkoxy, —NR83R84, or
• 219
• a) O,
• b) CH2, or
• c) NR87;
• R83 and R84 at each occurrence are the same or different and are
• a) H, or
• b) C1-4 alkyl;
• R85 is
• a) OH,
• b) C1-4 alkoxy, or
• c) —NR88R89;
• R86 is
• a) H, or
• b) C1-7 alkyl optionally substituted with indolyl OH, mercaptyl, imidazoly, methylthio, amino, phenyl optionally substituted with OH, —C(═O)—NH2, —CO2H, or —C(═NH)—NH2;
• R87 is
• a) H,
• b) phenyl, or
• c) C1-6 alkl optionally substituted by OH;
• R88 and R89 at each occurrence are the same or different and are
• a) H,
• b) C1-5 alkyl
• c) C3-6 cyloalky, or
• d) phenyl;
• R90 is
• a) C1-8 alkyl optionally substituted with C1-6 alkoxy or C1-6 hydroxy, C3-6 cycloalkyl, a 6-membered aromatic optionally benzo-&sed heterocyclic moiety having one to three nitrogen atoms, which can in turn be substituted with one. or two —NO2, CF3, halo, —CN, OH, C1-5 alkyl, C1-5 alkoxy, or C1-5 acyl;
• 220
• c) phenyl, or
• d) pyridyl;
• R91 is
• a) C1-16 alkyl,
• b) C2-16 alkenyl, wherein the substituents (a) and (b) can be optionally substituted with C1-6 alkoxycarbonyl, or a 5-, 6-, 7-membered aromatic heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O,
• c) an aromatic moiety having 6 to 10 carbon atoms, or
• d) a 5-, 6-, 7-membered aromatic heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, wherein the substituents (c) and (d) can be optionally substituted with carboxyl, halo, —CN, formyl, CF3, —NO2, C1-6 alkyl, C1-6 alkoxy, C1-6 acyl, C1-6 alkylthio, or C1-6 alkoxycarbonyl;
• R92 and R93 at each occurrence are the same or different and are
• a) H,
• b) phenyl,
• c) C1-6 alkyl, or
• d) benzyl;
• R94 and R95 at each occurrence are the same or different and are
• a) H,
• b) OH,
• c) C1-6 alkyl optionally substituted with —NR83R84, or
• d) R94 and R95 taken together are ═O;
• R96 is
• a) an aromatic moiety having 6 to 10 carbon atoms,
• b) a 5-, or 6-membered aromatic optionally benzo-fused heterocyclic moiety having one to three atoms selected from the group consisting of S, N, and O, wherein the substituents (a) and (b) which can in turn be substituted with one or three —NO2, CF3, halo, —CN, OH, phenyl, C1-5 alky, C1-5 alkoxy, or C1-5 acyl,
• c) morpholinyl,
• d) OH,
• e) C1-6 alkoxy,
• f) —NR83R84,
• g) —C(═O)—R97, or
• 221
• R97,
• a) morpholinyl,
• b) OH, or
• c) C1-6 alkoxy;
• h is 1, 2, or 3;
• i is0, 1,or2;
• j is 0 or 1;
• k is 3, 4, or 5;
• l is 2 or 3;
• m is 4 or 5;
• n is 0, 1, 2, 3, 4,or 5;
• p is 0, 1, 2, 3, 4, or 5;
• with the proviso that n and p together are 1, 2, 3, 4, or 5;
• q is 1, 2, 3, or 4;
• r is 2, 3, or 4;
• t is 0, 1, 2, 3, 4, 5, or 6;
• u is l or 2;
• w is 0, 1, 2, or 3.