racemic-diastereomeric mixtures, optical isomers or pharmaceutically-acceptable salts thereof wherein:

where Z¹⁰⁰ is

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;

R_a 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, R_c and CH₂OR_c;

where R_c for each occurrence is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, —CH₂—NR_dR_e, —W—(CH₂)_t—NR_dR_e, —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;

R_d and R_e for each occurrence are independently H, alkyl, alkanoyl or SO₂-alkyl; or R_d, R_e 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 NR_f, wherein R_f 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)—; —SO_pN(C(O)R)—; —N(R)SO_pN(R)—; —C(O)O—; —N(R)P(OR_b)O—; —N(R)P(OR_b)—; —N(R)P(O)(OR_b)O—; —N(R)P(O)(OR_b)—; —N(C(O)R)P(OR_b)O—; —N(C(O)R)P(OR_b)—; —N(C(O)R)P(O)(OR_b)O—, or —N(C(O)R)P(OR_b)—;

R_b 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 R_b together form a five- or six-membered heterocyclic ring; or

A is NRSO₂ and R, R_a 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 CR_a and N, provided that at least two of D₁, G₁, J₁, L₁ and M₁ are CR_a; or

a is 0, and one of D₁, G₁, L₁ and M₁ is NR_a, one of D₁, G₁, L₁ and M₁ is CR_a and the remainder are independently selected from the group consisting of CR_a and N, wherein R_a is as defined above;

b is 1 and D₂, G₂, J₂, L₂ and M₂ are each independently selected from the group consisting of CR_a and N, provided that at least two of D₂, G₂, J₂, L₂ and M₂ are CR_a; or

b is 0, and one of D₂, G₂, L₂ and M₂ is NR_a, one of D₂, G₂, L₂ and M₂ is CR_a and the remainder are independently selected from the group consisting of CR_a and N, wherein R_a 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.