| 主权项 |
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 RG2a substituents are located on adjacent ring carbon atoms; RG2a is independently: (i) —OH; (ii) —CN; (iii) Halogen; (iv) —C1-6-linear alkyl, optionally substituted by one or more fluorine atoms; or (v) —C1-6-alkoxy, optionally substituted by a C1-4-alkoxy moiety; RG4 and RG5 are:
(a) independently, for each occurrence, (i) —H; (ii) —F; or (iii) —C1-6-alkyl which is optionally substituted with one or more fluorine substituents; or(b) RG4 and RG5 are taken together to form a carbonyl [—C(O)—] moiety, with the proviso that where “m”>1, RG4 and RG5 are not selected to form two adjacent carbonyl moieties; and MG1 is a moiety of the formula: wherein: Ra1, Ra2, Ra3, Ra4, Ra5, and Ra6, are defined as follows:
(a) Ra6 is: —H; or —CH3; and Ra1; Ra2; Ra3; Ra4; and Ra5 are independently:
(i) —H;(ii) an aromatic moiety of from 6 to 10 carbon atoms; or(iii) —C1-5 linear, branched or cyclic alkyl which is optionally substituted with one or more of —F or —C1-4-alkyl substituent wherein one or more carbon atoms in said optional C1-4-alkyl substituent are optionally substituted with one or more —F atoms; or(b) Ra1, Ra2, Ra1, and Ra4 are independently: —H, —C1-5 linear, —C3-5-branched or —C3-5-cyclic alkyl; and Ra5 and Ra6 together form a bridge of the formula: —(CH2)q—, thereby providing a moiety of the structure: where “q” is 1 or 2;
(c) one pair of Ra1/Ra2 or Ra3/Ra4 together form an oxo-functional group and the other pair are hydrogen, providing a structure of Formula Ga1 or Ga2: (d) one pair of Ra1/Ra2 or Ra3/Ra4 are each —H and the other pair together comprise up to five carbon atoms which are cyclized to form a spirocyclo moiety of Formula Fb3 or Formula Fb4: wherein “p” is an integer from 1 to 3; or(e) Ra1, Ra2 Ra3, Ra4, Ra5, and Ra6 are selected to provide an ethylene-bridged moiety of the formula: wherein: (i) Ra6 together with one of Ra3 or Ra4 form an ethylene bridge and any of Ra1, Ra2 Ra3, Ra4, or Ra5, which are not part of said ethylene bridge are hydrogen; (ii) Ra5 together with one of Ra1 or Ra2 form an ethylene bridge and any of Ra1, Ra2 Ra3, Ra4, or Ra6 which are not part of said ethylene bridge are hydrogen; or (iii) Ra6 together with one of Ra3 or Ra4, and Ra5 together with one of Ra1 or Ra2 each form ethylene bridge, and any of Ra1, Ra2, Ra3, or Ra4 which are not selected to form an ethylene bridge are hydrogen; and Rb2 is:
(a) C1-6-linear, C3-6-branched, or C3-6-cyclic-alkyl, which alkyl moiety is optionally substituted with one or more substituents which are, independently: (i) halogen; (ii) C1-6-alkoxy; or (iii) C1-6-alkyl-SO2—;(b) —C(O)—Rc1 wherein, “Rc1” is: (i) aryl; (ii) C1-6-alkoxy; or (iii) C1-6-linear, C3-6-branched, or C3-6-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) C1-6-alkyl, optionally halogen substituted;(iii) C1-6-alkoxy;(iv) C1-6-alkoxy-C1-6-alkoxide;(v) aryloxy of from 6 to 10 carbon atoms;(vi) C1-6-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) (Rd1)2N—, wherein “Rd1” is independently —H or —C1-6-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) —C1-6-alkyl-sulfonyl;(iii) —C1-6-alkyl which is optionally substituted with one or more substituents that are, independently for each occurrence, halogen or C1-6-alkoxide;(iv) —C1-6-alkoxide which is optionally substituted with one or more substituents that are, independently for each occurrence, halogen or —C1-6-alkyl;(v) C1-6—C(O)—;(vi) —CN; or(vii) C1-6C(O)O—. |
