Pyrazolopyrimidines as therapeutic agents

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, hydrogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl or substituted or unsubstituted alkoxy;
• A is —(C1-C6)—, —O—;
• —S—;
• —S(O)p—;
• —N(R)—;
• —N(C(O)OR)—;
• —N(C(O)R)—;
• —N(SO2R)—;
• —CH2O—;
• —CH2S—;
• —CH2N(R)—;
• —CH(NR)—;
• —CH2N(C(O)R))—;
• —CH2N(C(O)OR)—;
• —CH2N(SO2R)—;
• —CH(NHR)—;
• —CH(NHC(O)R)—;
• —CH(NHSO2R)—;
• —CH(NHC(O)OR)—;
• —CH(OC(O)R)—;
• —CH(OC(O)NHR)—;
• —CH═CH—;
• —C(═NOR)—;
• —C(O)—;
• —CH(OR)—;
• —C(O)N(R)—;
• —N(R)C(O)—;
• —N(R)S(O)p—;
• —OC(O)N(R)—;
• —N(R)—C(O)—(CH2)n—N(R)—, —N(R)C(O)O—;
• —N(R)—(CH2)n+1—C(O)—, —S(O)pN(R)—;
• —O—(CR2)n+1—C(O)—, —O—(CR2)n+1—O—, —N(C(O)R)S(O)p—;
• —N(R)S(O)pN(R)—;
• —N(R)—C(O)—(CH2)n—O—, —C(O)N(R)C(O)—;
• —S(O)pN(R)C(O)—;
• —OS(O)pN(R)—;
• —N(R)S(O)pO—;
• —N(R)S(O)pC(O)—;
• —SOpN(C(O)R)—;
• —N(R)SOpN(R)—;
• —C(O)O—;
• —N(R)P(ORb)O—;
• —N(R)P(ORb)—;
• —N(R)P(O)(ORb)O—;
• —N(R)P(O)(ORb)—;
• —N(C(O)R)P(ORb)O—;
• —N(C(O)R)P(ORb)—;
• —N(C(O)R)P(O)(ORb)O—, or —N(C(O)R)P(ORb)—;
• where R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• Rb for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• or
• in a phosphorus containing group, the nitrogen atom, the phosphorus atom, R and Rb together form a five- or six-membered heterocyclic ring;
• or
• A is NRSO2 and R, Ra and the nitrogen atom together form a substituted or unsubstituted five or-six-membered heterocyclic ring fused to ring 1;
• or
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is a) hydrogen;
• b) substituted or unsubstituted trityl;
• c) substituted or unsubstituted cycloalkenyl;
• d) azaheteroaryl substituted with a substituted or unsubstituted alkyl;
• e) azacycloalkyl which is substituted with one or more substituents selected from substituted or unsubstituted —(C1-C6)-alkyl, substituted or unsubstituted —C1-C6-alkyl-OR, substituted or unsubstituted —C(O)—C1-C6-alkyl-N(R)2, substituted or unsubstituted —C1-C6-alkyl-N(R)2, substituted or unsubstituted —C1-C6-alkyl-cycloalkyl, substituted or unsubstituted tetrahydrothienyl, and substituted or unsubstituted tetrahydrothiopyranyl;
• or f) a group of the formula:
• wherein E1 is piperidinyl, piperazinyl, imidazolyl, morpholinyl, pyrrolidinyl, amino, amido, or tetrahydrothiazolyl, and wherein E is optionally substituted with one or more substituents selected from —C0-C6-alkyl-OR, —C1-C6-alkyl-C(O)OR, —C1-C6-alkyl-heteroaryl, —C1-C6-alkyl-heterocycloalkyl, and —C1-C6-alkyl-N(R)2;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6;
• provided that when Z110-A-Z111 taken together are a covalent bond, then Z100 is not alkyl;
• and
• provided that when Z110-A-Z111 taken together are a C1-C6 alkyl, then Z100 is not phenyl, pyrrolyl, imidazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl or thienyl.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• wherein Z100 is pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, H-pyridinone, 1,1-dioxybenzoisothiazolyl, benzoisoxazolyl, alkyl, imidazo[1,2-a]pyridinyl, pyrrolopyridinyl or
• wherein all of the foregoing Z100 groups are optionally substituted with R1;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, hydrogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl or substituted or unsubstituted alkoxy;
• A is —(C1-C6)—, —O—;
• —S—;
• —S(O)p—;
• —N(R)—;
• —N(C(O)OR)—;
• —N(C(O)R)—;
• —N(SO2R)—;
• —CH2O—;
• —CH2S—;
• —CH2N(R)—;
• —CH(NR)—;
• —CH2N(C(O)R))—;
• —CH2N(C(O)OR)—;
• —CH2N(SO2R)—;
• —CH(NHR)—;
• —CH(NHC(O)R)—;
• —CH(NHSO2R)—;
• —CH(NHC(O)OR)—;
• —CH(OC(O)R)—;
• —CH(OC(O)NHR)—;
• —CH═CH—;
• —C(═NOR)—;
• —C(O)—;
• —CH(OR)—;
• —C(O)N(R)—;
• —N(R)C(O)—;
• —N(R)S(O)p—;
• —OC(O)N(R)—;
• —N(R)—C(O)—(CH2)n—N(R)—, —N(R)C(O)O—;
• —N(R)—(CH2)n+1—C(O)—, —S(O)pN(R)—;
• —O—(CR2)n+1—C(O)—, —O—(CR2)n+1—O—, —N(C(O)R)S(O)p—;
• —N(R)S(O)pN(R)—;
• —N(R)—C(O)—(CH2)n—O—, —C(O)N(R)C(O)—;
• —S(O)pN(R)C(O)—;
• —OS(O)pN(R)—;
• —N(R)S(O)pO—;
• —N(R)S(O)pC(O)—;
• —SOpN(C(O)R)—;
• —N(R)SOpN(R)—;
• —C(O)O—;
• —N(R)P(ORb)O—;
• —N(R)P(ORb)—;
• —N(R)P(O)(ORb)O—;
• —N(R)P(O)(ORb)—;
• —N(C(O)R)P(ORb)O—;
• —N(C(O)R)P(ORb)—;
• —N(C(O)R)P(O)(ORb)O—, or —N(C(O)R)P(ORb)—;
• where R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• Rb for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• or
• in a phosphorus containing group, the nitrogen atom, the phosphorus atom, R and Rb together form a five- or six-membered heterocyclic ring;
• or
• A is NRSO2 and R, Ra and the nitrogen atom together form a substituted or unsubstituted five or-six-membered heterocyclic ring fused to ring 1;
• or
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is H or a group of the formula -Z101-Z102;
• Z101 is a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is hydrogen;
• a substituted or unsubstituted alkyl group;
• a substituted or unsubstituted cycloalkyl group;
• a substituted or unsubstituted cycloalkenyl, a substituted or unsubstituted, saturated or unsaturated heterocyclic group;
• or a substituted or unsubstituted, saturated or unsaturated heterobicyclic group;
• wherein said substituted alkyl, substituted cycloalkyl, substituted cycloalkenyl, substituted heterocyclic and substituted heterobicyclic group having one or more substituents each independently selected from the group consisting of hydroxyl, cyano, nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2, substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6)—C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted sulfonamido, substituted or unsubstituted ureido, substituted or unsubstituted carboxamido, substituted or unsubstituted amino, substituted or unsubstituted —N(R)—(C1-C6)—OR, oxo, and a saturated, unsaturated or aromatic, substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of N, O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• or
• R2 is a group of the formula -B-E, wherein B is a substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted azacycloalkyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkylsulfonyl, substituted or unsubstituted alkoxyalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aminoalkylcarbonyl, substituted or unsubstituted alkylene, substituted or unsubstituted aminoalkyl, substituted or unsubstituted alkylenecarbonyl or substituted or unsubstituted aminoalkylcarbonyl group;
• and E is substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, substituted or unsubstituted azacycloalkyl, a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted (C1-C6)-azacycloalkyl-, substituted or unsubstituted azacycloalkylcarbonyl, substituted or unsubstituted azacycloalkylsulfonyl, substituted or unsubstituted azacycloalkylalkyl, substituted or unsubstituted heteroaryl-N(R)—(C1-C6)—, substituted or unsubstituted aryl-N(R)—(C1-C6)—, substituted or unsubstituted alkyl-N(R)—(C1-C6)—, substituted or unsubstituted heteroaryl-(C1-C6)—N(R)—, substituted or unsubstituted aryl-(C1-C6)—N(R)—, substituted or unsubstituted alkyl-(C1-C6)—N(R)—, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroarylsulfonyl, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted azacycloalkylcarbonylamino, substituted or unsubstituted heteroarylcarbonylamino, substituted or unsubstituted arylcarbonylamino, substituted or unsubstituted alkylcarbonylamino or substituted or unsubstituted aryl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6;
• provided that when A is —N(R)—, Z110 and Z111 are each a covalent bond, and R2 is a 3,4-dihydroxytetrahydrofur-2-yl or a 3,4-diacyloxytetrahydrofur-2-yl, then Z100 is not alkyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl or pyrrolidinyl;
• provided that when Z110 and Z111 are each a covalent bond, and R2 is a 3,4-dihydroxytetrahydrofur-2-yl or a 3,4-diacyloxytetrahydrofur-2-yl, Z100 is a substituted or unsubstituted alkyl, then A is not alkyl, —O—, —C(O)—, —NHC(O)— or —C(O)O—;
• provided that when Z110-A-Z111 taken together are a covalent bond, then Z100 is not alkyl;
• provided that when Z110-A-Z111 taken together are a C1-C6 alkyl, then Z100 is not phenyl, pyrrolyl, imidazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl or thienyl;
• and
• provided that when R2 is a substituted or unsubstituted cyclopentyl, Z100 is an substituted or unsubstituted alkyl, Z110 and Z111 are each a covalent bond, then A is not —O—, —C(O)O—, or —N(R)—.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, and wherein at least one of Ra and R1 is not hydrogen;
• R3 for each occurrence is, independently, hydrogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl or substituted or unsubstituted alkoxy;
• A is —(C1-C6)—, —O—;
• —S—;
• —S(O)p—;
• —N(R)—;
• —N(C(O)OR)—;
• —N(C(O)R)—;
• —N(SO2R)—;
• —CH2O—;
• —CH2S—;
• —CH2N(R)—;
• —CH(NR)—;
• —CH2N(C(O)R))—;
• —CH2N(C(O)OR)—;
• —CH2N(SO2R)—;
• —CH(NHR)—;
• —CH(NHC(O)R)—;
• —CH(NHSO2R)—;
• —CH(NHC(O)OR)—;
• —CH(OC(O)R)—;
• —CH(OC(O)NHR)—;
• —CH═CH—;
• —C(═NOR)—;
• —C(O)—;
• —CH(OR)—;
• —C(O)N(R)—;
• —N(R)C(O)—;
• —N(R)S(O)p—;
• —OC(O)N(R)—;
• —N(R)—C(O)—(CH2)n—N(R)—, —N(R)C(O)O—;
• —N(R)—(CH2)n+1—C(O)—, —S(O)pN(R)—;
• —O—(CR2)n+1—C(O)—, —O—(CR2)n+1—O—, —N(C(O)R)S(O)p—;
• —N(R)S(O)pN(R)—;
• —N(R)—C(O)—(CH2)n—O—, —C(O)N(R)C(O)—;
• —S(O)pN(R)C(O)—;
• —OS(O)pN(R)—;
• —N(R)S(O)pO—;
• —N(R)S(O)pC(O)—;
• —SOpN(C(O)R)—;
• —N(R)SOpN(R)—;
• —C(O)O—;
• —N(R)P(ORb)O—;
• —N(R)P(ORb)—;
• —N(R)P(O)(ORb)O—;
• —N(R)P(O)(ORb)—;
• —N(C(O)R)P(ORb)O—;
• —N(C(O)R)P(ORb)—;
• —N(C(O)R)P(O)(ORb)O—, or —N(C(O)R)P(ORb)—;
• where R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• Rb for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• or
• in a phosphorus containing group, the nitrogen atom, the phosphorus atom, R and Rb together form a five- or six-membered heterocyclic ring;
• or
• A is NRSO2 and R, Ra and the nitrogen atom together form a substituted or unsubstituted five or-six-membered heterocyclic ring fused to ring 1;
• or
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is H or a group of the formula -Z101-Z102;
• Z101 is a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is hydrogen;
• a substituted or unsubstituted alkyl group;
• a substituted or unsubstituted cycloalkyl group;
• a substituted or unsubstituted cycloalkenyl, a substituted or unsubstituted, saturated or unsaturated heterocyclic group;
• or a substituted or unsubstituted, saturated or unsaturated heterobicyclic group;
• wherein said substituted alkyl, substituted cycloalkyl, substituted cycloalkenyl, substituted heterocyclic and substituted heterobicyclic group having one or more substituents each independently selected from the group consisting of hydroxyl, cyano, nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2,substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6)—C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted sulfonamido, substituted or unsubstituted ureido, substituted or unsubstituted carboxamido, substituted or unsubstituted amino, substituted or unsubstituted —N(R)—(C1-C6)—OR, oxo, and a saturated, unsaturated or aromatic, substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of N, O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• or
• R2 is a group of the formula -B-E, wherein B is a substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted azacycloalkyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkylsulfonyl, substituted or unsubstituted alkoxyalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aminoalkylcarbonyl, substituted or unsubstituted alkylene, substituted or unsubstituted aminoalkyl, substituted or unsubstituted alkylenecarbonyl or substituted or unsubstituted aminoalkylcarbonyl group;
• and E is substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, substituted or unsubstituted azacycloalkyl, a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted (C1-C6)-azacycloalkyl-, substituted or unsubstituted azacycloalkylcarbonyl, substituted or unsubstituted azacycloalkylsulfonyl, substituted or unsubstituted azacycloalkylalkyl, substituted or unsubstituted heteroaryl-N(R)—(C1-C6)—, substituted or unsubstituted aryl-N(R)—(C1-C6)—, substituted or unsubstituted alkyl-N(R)—(C1-C6)—, substituted or unsubstituted heteroaryl-(C1-C6)—N(R)—, substituted or unsubstituted aryl-(C1-C6)—N(R)—, substituted or unsubstituted alkyl-(C1-C6)—N(R)—, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroarylsulfonyl, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted azacycloalkylcarbonylamino, substituted or unsubstituted heteroarylcarbonylamino, substituted or unsubstituted arylcarbonylamino, substituted or unsubstituted alkylcarbonylamino or substituted or unsubstituted aryl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6;
• provided that when A is —N(R)—, Z110 and Z111 are each a covalent bond, and R2 is a 3,4-dihydroxytetrahydrofur-2-yl or a 3,4-diacyloxytetrahydrofur-2-yl, then Z100 is not alkyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl or pyrrolidinyl;
• provided that when Z110 and Z111 are each a covalent bond, and R2 is a 3,4-dihydroxytetrahydrofur-2-yl or a 3,4-diacyloxytetrahydrofur-2-yl, Z100 is a substituted or unsubstituted alkyl, then A is not alkyl, —O—, —C(O)—, —NHC(O)— or —C(O)O—;
• provided that when Z110-A-Z111 taken together are a covalent bond, then Z100 is not alkyl;
• provided that when Z110-A-Z111 taken together are a C1-C6 alkyl, then Z100 is not phenyl, pyrrolyl, imidazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl or thienyl;
• and
• provided that when R2 is a substituted or unsubstituted cyclopentyl, Z100 is an substituted or unsubstituted alkyl, Z110 and Z111 are each a covalent bond, then A is not —O—, —C(O)O—, or —N(R)—.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, hydrogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl or substituted or unsubstituted alkoxy;
• A is —(C1-C6)—;
• R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• R2 is H or a group of the formula -Z101-Z102;
• Z101 a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is hydrogen;
• a substituted or unsubstituted alkyl group;
• a substituted or unsubstituted cycloalkyl group;
• a substituted or unsubstituted cycloalkenyl, a substituted or unsubstituted, saturated or unsaturated heterocyclic group;
• or a substituted or unsubstituted, saturated or unsaturated heterobicyclic group;
• wherein said substituted alkyl, substituted cycloalkyl, substituted cycloalkenyl, substituted heterocyclic and substituted heterobicyclic group having one or more substituents each independently selected from the group consisting of hydroxyl, cyano, nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2,substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6)—C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted sulfonamido, substituted or unsubstituted ureido, substituted or unsubstituted carboxamido, substituted or unsubstituted amino, substituted or unsubstituted —N(R)—(C1-C6)—OR, oxo, and a saturated, unsaturated or aromatic, substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of N, O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• or
• R2 is a group of the formula -B-E, wherein B is a substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted azacycloalkyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkylsulfonyl, substituted or unsubstituted alkoxyalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aminoalkylcarbonyl, substituted or unsubstituted alkylene, substituted or unsubstituted aminoalkyl, substituted or unsubstituted alkylenecarbonyl or substituted or unsubstituted aminoalkylcarbonyl group;
• and E is substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, substituted or unsubstituted azacycloalkyl, a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted (C1-C6)-azacycloalkyl-, substituted or unsubstituted azacycloalkylcarbonyl, substituted or unsubstituted azacycloalkylsulfonyl, substituted or unsubstituted azacycloalkylalkyl, substituted or unsubstituted heteroaryl-N(R)—(C1-C6)—, substituted or unsubstituted aryl-N(R)—(C1-C6)—, substituted or unsubstituted alkyl-N(R)—(C1-C6)—, substituted or unsubstituted heteroaryl-(C1-C6)—N(R)—, substituted or unsubstituted aryl-(C1-C6)—N(R)—, substituted or unsubstituted alkyl-(C1-C6)—N(R)—, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroarylsulfonyl, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted azacycloalkylcarbonylamino, substituted or unsubstituted heteroarylcarbonylamino, substituted or unsubstituted arylcarbonylamino, substituted or unsubstituted alkylcarbonylamino or substituted or unsubstituted aryl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6;
• provided that when Z110-A-Z111 taken together are a C1-C6 alkyl, then Z100 is not phenyl, pyrrolyl, imidazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl or thienyl.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, hydrogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl or substituted or unsubstituted alkoxy;
• R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is H or a group of the formula -Z101-Z102;
• Z101 is a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is hydrogen;
• a substituted or unsubstituted alkyl group;
• a substituted or unsubstituted cycloalkyl group;
• a substituted or unsubstituted cycloalkenyl, a substituted or unsubstituted, saturated or unsaturated heterocyclic group;
• or a substituted or unsubstituted, saturated or unsaturated heterobicyclic group;
• wherein said substituted alkyl, substituted cycloalkyl, substituted cycloalkenyl, substituted heterocyclic and substituted heterobicyclic group having one or more substituents each independently selected from the group consisting of hydroxyl, cyano, nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2,substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6) —C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted sulfonamido, substituted or unsubstituted ureido, substituted or unsubstituted carboxamido, substituted or unsubstituted amino, substituted or unsubstituted —N(R)—(C1-C6)—OR, oxo, and a saturated, unsaturated or aromatic, substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of N, O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• or
• R2 is a group of the formula -B-E, wherein B is a substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted azacycloalkyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkylsulfonyl, substituted or unsubstituted alkoxyalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aminoalkylcarbonyl, substituted or unsubstituted alkylene, substituted or unsubstituted aminoalkyl, substituted or unsubstituted alkylenecarbonyl or substituted or unsubstituted aminoalkylcarbonyl group;
• and E is substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, substituted or unsubstituted azacycloalkyl, a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted (C1-C6)-azacycloalkyl-, substituted or unsubstituted azacycloalkylcarbonyl, substituted or unsubstituted azacycloalkylsulfonyl, substituted or unsubstituted azacycloalkylalkyl, substituted or unsubstituted heteroaryl-N(R)—(C1-C6)—, substituted or unsubstituted aryl-N(R)—(C1-C6)—, substituted or unsubstituted alkyl-N(R)—(C1-C6)—, substituted or unsubstituted heteroaryl-(C1-C6)—N(R)—, substituted or unsubstituted aryl-(C1-C6)—N(R)—, substituted or unsubstituted alkyl-(C1-C6)—N(R)—, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroarylsulfonyl, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted azacycloalkylcarbonylamino, substituted or unsubstituted heteroarylcarbonylamino, substituted or unsubstituted arylcarbonylamino, substituted or unsubstituted alkylcarbonylamino or substituted or unsubstituted aryl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl.
• A is —(C1-C6)—, —O—;
• —S—;
• —S(O)p—;
• —N(R)—;
• —N(C(O)OR)—;
• —N(C(O)R)—;
• —N(SO2R)—;
• —CH2O—;
• —CH2S—;
• —CH2N(R)—;
• —CH(NR)—;
• —CH2N(C(O)R))—;
• —CH2N(C(O)OR)—;
• —CH2N(SO2R)—;
• —CH(NHR)—;
• —CH(NHC(O)R)—;
• —CH(NHSO2R)—;
• —CH(NHC(O)OR)—;
• —CH(OC(O)R)—;
• —CH(OC(O)NHR)—;
• —CH═CH—;
• —C(═NOR)—;
• —C(O)—;
• —CH(OR)—;
• —C(O)N(R)—;
• —N(R)C(O)—;
• —N(R)S(O)p—;
• —OC(O)N(R)—;
• —N(R)—C(O)—(CH2)n—N(R)—, —N(R)C(O)O—;
• —N(R)—(CH2)n+1—C(O)—, —S(O)pN(R)—;
• —O—(CR2)n+1—C(O)—, —O—(CR2)n+1—O—, —N(C(O)R)S(O)p—;
• —N(R)S(O)pN(R)—;
• —N(R)—C(O)—(CH2)n—O—, —C(O)N(R)C(O)—;
• —S(O)pN(R)C(O)—;
• —OS(O)pN(R)—;
• —N(R)S(O)pO—;
• —N(R)S(O)pC(O)—;
• —SOpN(C(O)R)—;
• —N(R)SOpN(R)—;
• —C(O)O—;
• —N(R)P(ORb)O—;
• —N(R)P(ORb)—;
• —N(R)P(O)(ORb)O—;
• —N(R)P(O)(ORb)—;
• —N(C(O)R)P(ORb)O—;
• —N(C(O)R)P(ORb)—;
• —N(C(O)R)P(O)(ORb)O—, or —N(C(O)R)P(ORb)—;
• where R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• Rb for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• or
• in a phosphorus containing group, the nitrogen atom, the phosphorus atom, R and Rb together form a five- or six-membered heterocyclic ring;
• or
• A is NRSO2 and R, Ra and the nitrogen atom together form a substituted or unsubstituted five or-six-membered heterocyclic ring fused to ring 1;
• or
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is H or a group of the formula -Z101-Z102;
• Z101 is a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is hydrogen;
• a substituted or unsubstituted alkyl group;
• a substituted or unsubstituted cycloalkyl group;
• a substituted or unsubstituted cycloalkenyl, a substituted or unsubstituted, saturated or unsaturated heterocyclic group;
• or a substituted or unsubstituted, saturated or unsaturated heterobicyclic group;
• wherein said substituted alkyl, substituted cycloalkyl, substituted cycloalkenyl, substituted heterocyclic and substituted heterobicyclic group having one or more substituents each independently selected from the group consisting of hydroxyl, cyano, nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2,substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6) —C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted sulfonamido, substituted or unsubstituted ureido, substituted or unsubstituted carboxamido, substituted or unsubstituted amino, substituted or unsubstituted —N(R)—(C1-C6)—OR, oxo, and a saturated, unsaturated or aromatic, substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of N, O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• or
• R2 is a group of the formula -B-E, wherein B is a substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted azacycloalkyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkylsulfonyl, substituted or unsubstituted alkoxyalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aminoalkylcarbonyl, substituted or unsubstituted alkylene, substituted or unsubstituted aminoalkyl, substituted or unsubstituted alkylenecarbonyl or substituted or unsubstituted aminoalkylcarbonyl group;
• and E is substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl, substituted or unsubstituted azacycloalkyl, a substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted (C1-C6)-azacycloalkyl-, substituted or unsubstituted azacycloalkylcarbonyl, substituted or unsubstituted azacycloalkylsulfonyl, substituted or unsubstituted azacycloalkylalkyl, substituted or unsubstituted heteroaryl-N(R)—(C1-C6)—, substituted or unsubstituted aryl-N(R)—(C1-C6)—, substituted or unsubstituted alkyl-N(R)—(C1-C6)—, substituted or unsubstituted heteroaryl-(C1-C6)—N(R)—, substituted or unsubstituted aryl-(C1-C6)—N(R)—, substituted or unsubstituted alkyl-(C1-C6)—N(R)—, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylcarbonyl, substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroarylsulfonyl, substituted or unsubstituted alkylsulfonyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted azacycloalkylcarbonylamino, substituted or unsubstituted heteroarylcarbonylamino, substituted or unsubstituted arylcarbonylamino, substituted or unsubstituted alkylcarbonylamino or substituted or unsubstituted aryl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6;
• provided that when A is —N(R)—, Z110 and Z111 are each a covalent bond, and R2 is a 3,4-diacyloxytetrahydrofur-2-yl, then Z100 is not alkyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl or pyrrolidinyl;
• provided that when Z110 and Z111 are each a covalent bond, and R2 is a 3,4-diacyloxytetrahydrofur-2-yl, Z100 is a substituted or unsubstituted alkyl, then A is not alkyl, —O—, —C(O)—, —NHC(O)— or —C(O)O—;
• provided that when Z110-A-Z111 taken together are a covalent bond, then Z100 is not alkyl;
• and
• provided that when Z110-A-Z111 taken together are a C1-C6 alkyl, then Z100 is not phenyl, pyrrolyl, imidazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl or thienyl;
• and
• provided that when R2 is a substituted or unsubstituted cyclopentyl, Z100 is an substituted or unsubstituted alkyl, Z110 and Z111 are each a covalent bond, then A is not —O—, —C(O)O—, or —N(R)—.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heterparyl or a substituted or unsubstituted alkoxy;
• A is —(C1-C6)—, —O—;
• —S—;
• —S(O)p—;
• —N(R)—;
• —N(C(O)OR)—;
• —N(C(O)R)—;
• —N(SO2R)—;
• —CH2O—;
• —CH2S—;
• —CH2N(R)—;
• —CH(NR)—;
• —CH2N(C(O)R))—;
• —CH2N(C(O)OR)—;
• —CH2N(SO2R)—;
• —CH(NHR)—;
• —CH(NHC(O)R)—;
• —CH(NHSO2R)—;
• —CH(NHC(O)OR)—;
• —CH(OC(O)R)—;
• —CH(OC(O)NHR)—;
• —CH═CH—;
• —C(═NOR)—;
• —C(O)—;
• —CH(OR)—;
• —C(O)N(R)—;
• —N(R)C(O)—;
• —N(R)S(O)p—;
• —OC(O)N(R)—;
• —N(R)—C(O)—(CH2)n—N(R)—, —N(R)C(O)O—;
• —N(R)—(CH2)n+1—C(O)—, —S(O)pN(R)—;
• —O—(CR2)n+1—C(O)—, —O—(CR2)n+1—O—, —N(C(O)R)S(O)p—;
• —N(R)S(O)pN(R)—;
• —N(R)—C(O)—(CH2)n—O—, —C(O)N(R)C(O)—;
• —S(O)pN(R)C(O)—;
• —OS(O)pN(R)—;
• —N(R)S(O)pO—;
• —N(R)S(O)pC(O)—;
• —SOpN(C(O)R)—;
• —N(R)SOpN(R)—;
• —C(O)O—;
• —N(R)P(ORb)O—;
• —N(R)P(ORb)—;
• —N(R)P(O)(ORb)O—;
• —N(R)P(O)(ORb)—;
• —N(C(O)R)P(ORb)O—;
• —N(C(O)R)P(ORb)—;
• —N(C(O)R)P(O)(ORb)O—, or —N(C(O)R)P(ORb)—;
• where R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• Rb for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• or
• in a phosphorus containing group, the nitrogen atom, the phosphorus atom, R and Rb together form a five- or six-membered heterocyclic ring;
• or
• A is NRSO2 and R, Ra and the nitrogen atom together form a substituted or unsubstituted five or-six-membered heterocyclic ring fused to ring 1;
• or
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is a group of the formula -Z101-Z102;
• Z101 is a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is a substituted or unsubstituted cycloalkenyl, wherein said substituted cycloalkenyl has one or more substituents each independently selected from the group consisting of hydroxyl, cyano, nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2, substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6)—C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted sulfonamido, substituted or unsubstituted ureido, substituted or unsubstituted carboxamido, substituted or unsubstituted amino, substituted or unsubstituted —N(R)—(C1-C6)—OR, oxo, and a saturated, unsaturated or aromatic, substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of N, O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6.

A compound of Formula (I):

• racemic-diastereomeric mixtures, optical isomers, pharmaceutically-acceptable salts or prodrugs thereof wherein:
• G is
• where Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazolyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Z110 is a covalent bond, or an optionally substituted (C1-C6) which is optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Z111 is a covalent bond, an optionally substituted (C1-C6) or an optionally substituted —(CH2)n-cycloalkyl-(CH2)n—;
• where the optionally substituted groups are optionally substituted with one or more substituents selected from the group consisting of alkyl, CN, OH, halogen, NO2, COOH, substituted or unsubstituted amino and substituted or unsubstituted phenyl;
• Ra and R1 each represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino , substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• R3 for each occurrence is, independently, hydrogen, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted —C(O)-alkyl, a substituted or unsubstituted —C(O)-aryl, or a substituted or unsubstituted —C(O)-heteroaryl or substituted or unsubstituted alkoxy;
• A is —(C1-C6)—, —O—;
• —S—;
• —S(O)p—;
• —N(R)—;
• —N(C(O)OR)—;
• —N(C(O)R)—;
• —N(SO2R)—;
• —CH2O—;
• —CH2S—;
• —CH2N(R)—;
• —CH(NR)—;
• —CH2N(C(O)R))—;
• —CH2N(C(O)OR)—;
• —CH2N(SO2R)—;
• —CH(NHR)—;
• —CH(NHC(O)R)—;
• —CH(NHSO2R)—;
• —CH(NHC(O)OR)—;
• —CH(OC(O)R)—;
• —CH(OC(O)NHR)—;
• —CH═CH—;
• —C(═NOR)—;
• —C(O)—;
• —CH(OR)—;
• —C(O)N(R)—;
• —N(R)C(O)—;
• —N(R)S(O)p—;
• —OC(O)N(R)—;
• —N(R)—C(O)—(CH2)n—N(R)—, —N(R)C(O)O—;
• N(R)—(CH2)n+1—C(O)—, —S(O)pN(R)—;
• —O—(CR2)n+1—C(O)—, —O—(CR2)n+1—O—, —N(C(O)R)S(O)p;
• —N(R)S(O)pN(R)—;
• —N(R)—C(O)—(CH2)n—O—, —C(O)N(R)C(O)—;
• —S(O)pN(R)C(O)—;
• —OS(O)pN(R)—;
• —N(R)S(O)pO—;
• —N(R)S(O)pC(O)—;
• —SOpN(C(O)R)—;
• —N(R)SOpN(R)—;
• —C(O)O—;
• —N(R)P(ORb)O—;
• —N(R)P(ORb)—;
• —N(R)P(O)(ORb)O—;
• —N(R)P(O)(ORb)—;
• —N(C(O)R)P(ORb)O—;
• —N(C(O)R)P(ORb)—;
• —N(C(O)R)P(O)(ORb)O—, or —N(C(O)R)P(ORb)—;
• where R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• Rb for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted cycloalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• or
• in a phosphorus containing group, the nitrogen atom, the phosphorus atom, R and Rb together form a five- or six-membered heterocyclic ring;
• or
• A is NRSO2 and R, Ra and the nitrogen atom together form a substituted or unsubstituted five or-six-membered heterocyclic ring fused to ring 1;
• or
• Z110-A-Z111 taken together is a covalent bond;
• and
• R2 is a group of the formula -Z101-Z102;
• Z101 is a covalent bond, —(C1-C6)—, —(C1-C6)— —O—, —(C1-C6)— —C(O)—, —(C1-C6)— —C(O)O—, —(C1-C6)—C(O)—NH—, —(C1-C6)—C(O)—N((C1-C6))— or a substituted or unsubstituted phenyl group;
• Z102 is a substituted, saturated or unsaturated heterocyclic group;
• or a substituted, saturated or unsaturated heterobicyclic group;
• wherein said substituted heterocyclic and substituted heterobicyclic group have one or more substituents each independently selected from the group consisting of nitro, halo, substituted or unsubstituted (C1-C6), substituted or unsubstituted aryl, substituted or unsubstituted —C(O)-alkyl, substituted or unsubstituted —N(R)—(C1-C6)—OR, substituted or unsubstituted —N((C1-C6)—OR)2,substituted or unsubstituted —N(R)—(C1-C6)—C(O)2R, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—OR, substituted or unsubstituted —(C1-C6)—N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —(C1-C6)—C(O)N(R)—(C1-C6)—N(R)2, substituted or unsubstituted —N(R)—(C1-C6)—OR, and a substituted or unsubstituted heterocyclic group comprising one or more heteroatoms selected from the group consisting of O, and S;
• wherein the nitrogen atoms of said heterocyclic group or heterobicyclic group are independently optionally substituted by oxo, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted —C(O)N(R)2, substituted or unsubstituted —C(O)—(C1-C6)—N(R)2, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted arylalkyl group, or substituted or unsubstituted heteroarylalkyl;
• a is 1 and D1, G1, J1, L1 and M1 are each independently selected from the group consisting of CRa and N, provided that at least two of D1, G1, J1, L1 and M1 are CRa;
• or
• a is 0, and one of D1, G1, L1 and M1 is NRa, one of D1, G1, L1 and M1 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• and
• n for each occurrence is independently an integer from 0 to 6;
• provided that when A is —N(R)—, Z110 and Z111 are each a covalent bond, and R2 is a 3,4-diacyloxytetrahydrofur-2-yl, then Z100 is not alkyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl or pyrrolidinyl;
• provided that when Z110 and Z111 are each a covalent bond, and R2 is a 3,4-diacyloxytetrahydrofur-2-yl, Z100 is a substituted or unsubstituted alkyl, then A is not alkyl, —O—, —C(O)—, —NHC(O)— or —C(O)O—;
• provided that when Z110-A-Z111 taken together are a covalent bond, then Z100 is not alkyl;
• and
• provided that when Z110-A-Z111 taken together are a C1-C6 alkyl, then Z100 is not phenyl, pyrrolyl, imidazolyl, pyrazolyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, furyl or thienyl.

A method of preparing a 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl intermediate represented by the following structural formula:

• wherein:
• Z100 is
• or a group optionally substituted with R1 selected from the group consisting of alkyl, cycloalkyl, pyrrolidinyl, quinolinyl, quinoxalinyl, quinazolinyl, isoquinolinyl, phthalazinyl, imidazo[1,2-a]pyrimidinyl, 1H-imidazo[1,2-a]imidazolyl, imidazo[2,1-b][1,3]thiazolyl, naphthyl, tetrahydronaphthyl, benzothienyl, furanyl, thienyl, benzoxazolyl, benzoisoxazolyl, benzothiazoplyl,
• thiazolyl, benzofuranyl, 2,3-dihydrobenzofuranyl, indolyl, isoxazolyl, tetrahydropyranyl, tetrahydrofuranyl, piperidinyl, pyrazolyl, pyrrolyl, pyrrolopyridinyl, H-pyridinone, oxazolyl, isothiazolyl, oxadiazolyl, thiadiazolyl, indolinyl, indazolyl, imidazo[1,2-a]pyridinyl, benzoisothiazolyl, 1,1-dioxybenzoisothiazolyl, pyrido-oxazolyl, pyrido-thiazolyl, pyrimido-oxazolyl, pyrimido-thiazolyl and benzimidazolyl;
• Ra and R1 represent one or more substituents for each occurrence independently selected from the group consisting of hydrogen, halogen, —CN, —NO2, —C(O)OH, —C(O)H, —OH, —C(O)O-alkyl, —C(O)O-aryl, —C(O)O-heteroaryl, —C(O)-alkyl, —C(O)-aryl, —C(O)-heteroaryl, substituted or unsubstituted carboxamido, tetrazolyl, trifluoromethylcarbonylamino, trifluoromethylsulfonamido, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryloxy, substituted or unsubstituted heteroaryloxy, substituted or unsubstituted heteroarylalkoxy, substituted or unsubstituted arylalkoxy, substituted or unsubstituted alkyl-S(O)p—, substituted or unsubstituted alkyl-S—, substituted or unsubstituted aryl-S(O)p—, substituted or unsubstituted heteroaryl-S(O)p—, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted alkynyl, substituted or unsubstituted amino, substituted or unsubstituted aminoalkyl, substituted or unsubstituted amido groups, substituted or unsubstituted heteroarylthio, substituted or unsubstituted arylthio, -Z105-C(O)N(R)2, -Z105-N(R)—C(O)-Z200, -Z105-N(R)—S(O)2-Z200, -Z105-N(R)—C(O)—N(R)-Z200, Rc and CH2ORc;
• where Rc for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH2—NRdRe, —W—(CH2)t—NRdRe, —W—(CH2)t—O-alkyl, —W—(CH2)t—S-alkyl, or —W—(CH2)t—OH;
• Z105 for each occurrence is independently a covalent bond or (C1-C6);
• Z200 for each occurrence is independently a substituted or unsubstituted (C1-C6), substituted or unsubstituted phenyl or substituted or unsubstituted —(C1-C6)-phenyl;
• Rd and Re for each occurrence are independently H, alkyl, alkanoyl or SO2-alkyl;
• or Rd, Re and the nitrogen atom to which they are attached together form a five- or six-membered heterocyclic ring;
• t for each occurrence is independently an integer from 2 to 6;
• W for each occurrence is independently a direct bond or O, S, S(O), S(O)2, or NRf, wherein Rf for each occurrence is independently H or alkyl;
• or
• R1 is a substituted or unsubstituted carbocyclic or heterocyclic ring fused with ring 2;
• and
• R for each occurrence is independently H, substituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl or substituted or unsubstituted aryl;
• p is 1 or 2;
• and
• b is 1 and D2, G2, J2, L2 and M2 are each independently selected from the group consisting of CRa and N, provided that at least two of D2, G2, J2, L2 and M2 are CRa;
• or
• b is 0, and one of D2, G2, L2 and M2 is NRa, one of D2, G2, L2 and M2 is CRa and the remainder are independently selected from the group consisting of CRa and N, wherein Ra is as defined above;
• comprising the step of reacting in the presence of an aprotic base an acid chloride represented by the following structural formula:
• with a (4,4,5,5-tetramethyl-1,3,2-dioxaborolanyl)aniline represented by the following structural formula:
• to form said 4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl intermediate.