wherein A₁ and A₂ groups are independently selected from hydrogen, halogen, CN, CF₃, CHF₂, an optionally substituted radical selected from C₁-C₆ alkyl, C₃-C₈ cycloalkyl, heteroalkyl, heterocycloalkyl, alkoxy, amino, carboxy, alkoxycarbonyl; A₃ is selected from hydrogen and halogen; Rⁱ is selected from the group of hydrogen, halogen, CN, CF₃, CHF₂, an optionally substituted radical selected from C₁-C₆ alkyl, C₃-C₈ cycloalkyl, heteroalkyl, heterocycloalkyl, carboxy; Rⁱⁱ is hydrogen or an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo C₁-C₆ alkyl, an optionally substituted halo C₃-C₈ cycloalkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted hereroaryl C₁-C₆ alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted hydroxy C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted alkoxycarbonyl C₁-C₆ alkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted hereroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted halo C₃-C₈ cycloalkyl; Ar¹ is selected from:

R¹ and R⁴ are independently hydrogen, halogen, CN, CF₃, CHF₂, NH₂, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, alkoxy, amino, an optionally substituted heterocycloalkyl, carboxy, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted amino heterocycloalkyl C₁-C₆ alkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl; R² is selected from hydrogen, halogen, CF₃, CHF₂, NH₂, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted alkoxy, amino, an optionally substituted heterocycloalkyl, carboxy, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted amino heterocycloalkyl C₁-C₆ alkyl, an optionally substituted C₃-C₈ carboxy cycloalkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl; R³ is selected from hydrogen, halogen, CF₃, CHF₂, NH₂, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted alkoxy, amino, an optionally substituted heterocycloalkyl, carboxy, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted amino heterocycloalkyl C₁-C₆ alkyl, an optionally substituted C₃-C₈ carboxy cycloalkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl; R⁵ is selected from hydrogen, halogen, CF₃, CHF₂, NH₂, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted alkoxy, amino, an optionally substituted heterocycloalkyl, carboxy, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted amino heterocycloalkyl C₁-C₆ alkyl, an optionally substituted C₃-C₈ carboxy cycloalkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl; wherein when one from R¹, R², R³ and R⁴ is not H, the other from this group are H or any of R¹, R², R³, R⁴ and R⁵ can be linked together to form an optionally substituted bicyclic heteroaryl; Ar¹ is also selected from an optionally substituted bicyclic heteroaryl, in particular from the group consisting of:

wherein R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹² and R¹³ are each independently selected from hydrogen, halogen, hydroxy, CN, CF₃, CHF₂, NH₂, alkoxy, amino, carboxy, aminocarbonyl, alkoxy carbonyl, or an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl, an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl, acylamino, ureido, sulfonyl, sulfonylamino; Ar² is selected from the following group:

 or from the following group:

 or from the following group:

wherein R¹⁵, R¹⁶ and R¹⁹ are independently selected from hydrogen, halogen, hydroxy, CN, CF₃, CHF₂, NH₂, alkoxy, amino, carboxy, aminocarbonyl, alkoxy carbonyl, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted alkenyl, alkynyl, an optionally substituted haloalkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl, an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl, acylamino, ureido and sulfonyl, or selected from the groups listed below:

Wherein y, w, z and t are independently an integer ranging from 1 to 3; h is an integer ranging from 0 to 3; n is an integer ranging from 0 to 4; G is selected from N—R²³, O, S and SO₂; J is selected from C(B)n and N—R²³; L is C—(B) n, N—R²³, O, S, SO₂; R²³ is selected from hydrogen, aminocarbonyl, alkoxy carbonyl, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl, an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl and aminosulfonyl; B is selected from hydrogen, halogen, hydroxy, CN, CF₃, CHF₂, NH₂, alkoxy, amino, carboxy, aminocarbonyl, alkoxy carbonyl, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl, an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl, acylamino, ureido, sulfonyl and sulfonylamino; R¹⁷ and R¹⁸ are independently selected from hydrogen, halogen, CN, CF₃, CHF₂, alkoxy, amino, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, acylamino, ureido, sulfonyl, aminosulfonyl and sulfonylamino; R²⁰ and R²² are independently selected from hydrogen, halogen, CN, CF₃, CHF₂, alkoxy, amino, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted haloalkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl and an optionally substituted amino C₃-C₈ cycloalkyl; R²¹ is selected from hydrogen, aminocarbonyl, alkoxy carbonyl, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl and an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl; R¹⁵ and R¹⁶ can be linked together to form an optionally substituted bicyclic heteroaryl of formula

 wherein X, Y and Z and each independently C(R²⁴R²⁵), CH₂C(R²⁴R²⁵), C(═O), O and N—R²⁶; or

R¹⁵ and R¹⁶ can be linked together to form an optionally substituted bicyclic heteroaryl of formula

 to form 3,4-dihydro-2H-pyrido [3,2-b][1,4]oxazine, wherein the nitrogen in the Z position is N—R²⁶; R²⁴ and R²⁵ are each independently selected from hydrogen, halogen, hydroxy, CN, CF₃, CHF₂, NH₂, alkoxy, amino, carboxy, aminocarbonyl, alkoxy carbonyl, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, an optionally substituted amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl, an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl, acylamino, ureido, sulfonyl and sulfonylamino; R²⁴ and R²⁵ can be linked together to form an optionally substituted C₃-C₈ cycloalkyl or an optionally substituted heterocycloalkyl; R²⁶ is selected from hydrogen, aminocarbonyl, alkoxy carbonyl, an optionally substituted C₁-C₆ alkyl, an optionally substituted C₃-C₈ cycloalkyl, an optionally substituted halo alkyl, an optionally substituted heteroalkyl, an optionally substituted heterocycloalkyl, an optionally substituted aryl, an optionally substituted heteroaryl, an optionally substituted C₃-C₈ cycloalkyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₁-C₆ alkyl, an optionally substituted aryl C₁-C₆ alkyl, an optionally substituted heteroaryl C₁-C₆ alkyl, an optionally substituted alkoxy C₁-C₆ alkyl, amino C₁-C₆ alkyl, an optionally substituted carboxy C₁-C₆ alkyl, an optionally substituted aminocarbonyl C₁-C₆ alkyl, an optionally substituted heterocycloalkyl C₃-C₈ cycloalkyl, an optionally substituted aryl C₃-C₈ cycloalkyl, an optionally substituted heteroaryl C₃-C₈ cycloalkyl, an optionally substituted alkoxy C₃-C₈ cycloalkyl, an optionally substituted amino C₃-C₈ cycloalkyl, an optionally substituted carboxy C₃-C₈ cycloalkyl and an optionally substituted aminocarbonyl C₃-C₈ cycloalkyl, aminosulfonyl; R¹⁵ and R¹⁹ can be linked together to form an optionally substituted bicyclic heteroaryl; R¹⁵ and R²¹ can be linked together to form an optionally substituted bicyclic heteroaryl; R¹⁷ and R²¹ can be linked together to form an optionally substituted bicyclic heteroaryl; R²⁰ and R²¹ can be linked together to form an optionally substituted bicyclic heteroaryl, wherein when A₃ is hydrogen at least one of A₁ and A₂ is not hydrogen, as well as a tautomer, a geometrical isomer, an optically active form, and a pharmaceutically acceptable salt thereof.