Piperazine-substituted [1,2,4]triazolo[1,5-C]quinazolin-5-amine compounds with A

1. A compound of Formula A, or a pharmaceutically acceptable salt thereof:

wherein:

“m” and “n” are independently an integer of from 1 to 3, with the proviso that no more than two R G2a substituents are located on adjacent ring carbon atoms;

R G2a is independently: (i) —OH; (ii) —CN; (iii) Halogen; (iv) —C 1-6 -linear alkyl, optionally substituted by one or more fluorine atoms; or (v) —C 1-6 -alkoxy, optionally substituted by a C 1-4 -alkoxy moiety;

R G4 and R G5 are:

(a) independently, for each occurrence, (i) —H; (ii) —F; or (iii) —C 1-6 -alkyl which is optionally substituted with one or more fluorine substituents; or

(b) R G4 and R G5 are taken together to form a carbonyl [—C(O)—] moiety, with the proviso that where “m”>1, R G4 and R G5 are not selected to form two adjacent carbonyl moieties; and

M G1 is a moiety of the formula:

wherein:

R a1 , R a2 , R a3 , R a4 , R a5 , and R a6 , are defined as follows:

(a) R a6 is: —H; or —CH 3 ; and R a1 ; R a2 ; R a3 ; R a4 ; and R a5 are independently:

(i) —H;

(ii) an aromatic moiety of from 6 to 10 carbon atoms; or

(iii) —C 1-5 linear, branched or cyclic alkyl which is optionally substituted with one or more of —F or —C 1-4 -alkyl substituent wherein one or more carbon atoms in said optional C 1-4 -alkyl substituent are optionally substituted with one or more —F atoms; or

(b) R a1 , R a2 , R a3 , and R a4 are independently: —H, —C 1-5 linear, —C 3-5 -branched or —C 3-5 -cyclic alkyl; and R a5 and R a6 together form a bridge of the formula: —(CH 2 ) q —, thereby providing a moiety of the structure:

 where “q” is 1 or 2;

(c) one pair of R a1 /R a2 or R a3 /R a4 together form an oxo-functional group and the other pair are hydrogen, providing a structure of Formula Ga 1 or Ga 2 :

(d) one pair of R a1 /R a2 or R a3 /R a4 are each —H and the other pair together comprise up to five carbon atoms which are cyclized to form a spirocyclo moiety of Formula Fb 3 or Formula Fb 4 :

wherein “p” is an integer from 1 to 3; or

(e) R a1 , R a2 , R a3 , R a4 , R a5 , and R a6 are selected to provide an ethylene-bridged moiety of the formula:

wherein: (i) R a6 together with one of R a3 or R a4 form an ethylene bridge and any of R a1 , R a2 , R a3 , R a4 , or R a5 , which are not part of said ethylene bridge are hydrogen; (ii) R a5 together with one of R a1 or R a2 form an ethylene bridge and any of R a1 , R a2 , R a3 , R a4 , or R a6 which are not part of said ethylene bridge are hydrogen; or (iii) R a6 together with one of R a3 or R a4 , and R a5 together with one of R a1 or R a2 each form ethylene bridge, and any of R a1 , R a2 , R a3 , or R a4 which are not selected to form an ethylene bridge are hydrogen; and

R b2 is:

(a) C 1-6 -linear, C 3-6 -branched, or C 3-6 -cyclic-alkyl, which alkyl moiety is optionally substituted with one or more substituents which are, independently: (i) halogen; (ii) C 1-6 -alkoxy; or (iii) C 1-6 -alkyl-SO 2 —;

(b) —C(O)—R c1 wherein, “R c1 ” is: (i) aryl; (ii) C 1-6 -alkoxy; or (iii) C 1-6 -linear, C 3-6 -branched, or C 3-6 -cyclic-alkyl;

(c) a mono- or polycyclic aryl moiety comprising from 5 to 10 carbon atoms which is optionally linked to a nitrogen of the piperazine moiety through a carbonyl carbon, thereby forming an amide linkage, and wherein the ring of said aryl moiety optionally comprises one or more substituents which are, independently:

(i) halogen;

(ii) C 1-6 -alkyl, optionally halogen substituted;

(iii) C 1-6 -alkoxy;

(iv) C 1-6 -alkoxy-C 1-6 -alkoxide;

(v) aryloxy of from 6 to 10 carbon atoms;

(vi) C 1-6 -heterocycloalkyl comprising from 1 to 3 heteroatoms which are, independently for each occurrence “N”, “S”, or “O”, wherein said heterocycl-ring may optionally include a carbonyl group (C═O);

(vii) (R d1 ) 2 N—, wherein “R d1 ” is independently —H or —C 1-6 -alkyl;

(viii) nitrile;

(ix) mono- or polycyclic heteroaryl of from 5 to 10 carbon atoms, comprising from 1 to 4 heteroatoms which are, independently for each occurrence, “N”, “O”, or “S”; or

(x) —C(O)—OH; or

(d) a mono- or polycyclic heteroaryl moiety comprising from 5 to 10 carbon atoms and from 1 to 4 heteroatoms which are independently for each occurrence, “N”, “O”, or “S”, which is optionally linked to a nitrogen of the piperazine moiety through a carbonyl carbon, thereby forming an amide linkage, and wherein, optionally one or more ring carbon atoms is substituted with a moiety which is, independently for each occurrence:

(i) —halogen;

(ii) —C 1-6 -alkyl-sulfonyl;

(iii) —C 1-6 -alkyl which is optionally substituted with one or more substituents that are, independently for each occurrence, halogen or C 1-6 -alkoxide;

(iv) —C 1-6 -alkoxide which is optionally substituted with one or more substituents that are, independently for each occurrence, halogen or —C 1-6 -alkyl;

(v) C 1-6 —C(O)—;

(vi) —CN; or

(vii) C 1-6 C(O)O—.

2. A compound of Formula A, or a pharmaceutically acceptable salt thereof, having the structure of Formula AI:

wherein:

“n”, M G1 , R G4 and R G5 are as defined for the compound of Formula A;

R G2 is independently:

(i) —OH;

(ii) —CN;

(iii) Halogen;

(iv) —C 1-3 -linear alkyl which is optionally substituted by one or more fluorine substituents; or

(v) —C 1-6 -alkoxy, which is optionally substituted by a C 1-4 -alkoxy moiety; and

R G3 is —H or —F.

3. A compound of claim 1 having the Formula CC1:

CC1, or a salt thereof,

wherein R c16 is:

4. The compound of claim 1 having the Formula CC2:

or a salt thereof,

wherein R d is:

5. The compound of claim 1 having the Formula CC3:

or a salt thereof,

wherein R a1 to R a4 and R b2 are each defined in Table CTI.

TABLE CTI

R a1 /R a2

R a3 /R a4

R b2

—CH 3 /—H

—H/—H

—H/—CH 3

—H/—H

—CH 3 /—H

—H/—H

—CH 3 /—H

—H/—H

—H/—H

—CH 3 /—H

6. A compound of claim 1 having the Formula CC4:

or a salt thereof,

wherein R e is:

7. A compound of claim 1 having the Formula CC5:

or a salt thereof,

where “R f ” is:

8. A compound of claim 1 having the Formula CC6:

or a salt thereof,

wherein R b2 is:

9. The compound of claim 1 having the Formula CC7:

or a salt thereof,

wherein R d is:

10. The following compounds, or a salt thereof:

11. A method of treating a central nervous system disease by administering a compound of claim 1 .

12. A pharmaceutical composition that comprises an inert carrier and a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

13. A compound of claim 1 , or a pharmaceutically acceptable salt thereof, for use in medicine.

14. A method of treating a central nervous system disorder in a mammalian patient in need thereof by administering a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

15. The method of claim 14 wherein said central nervous system disorder is a movement disorder associated with Parkinson's disease or the treatment thereof using dopaminergic therapy.