Patent ID: 7608596
Filing Date: 2009-10-27
Classification: A61P,C07H

Abstract:
1. A 10-desmehtyl macrolide consisting of formula III: (1) R is methyl substituted with one or more substituents selected from the group consisting of (i) CN, (ii) F, (iii) CO (iv) OR (v) S(O) (vi) NR (vii) NR (viii) NR (a) hydrogen (b) C (c) C (d) C (e) aryl, and optionally substituted aryl (f) heteroaryl, and optionally substituted heteroaryl (g) heterocycloalkyl, and optionally substituted heterocycloalkyl (h) C (i) C (j) C (k) R (ix) aryl, and optionally substituted aryl, and (x) heteroaryl, and optionally substituted heteroaryl, (2) C (3) C (i) halogen, (ii) OR (iii) —CHO, (iv) oxo, (v) NR (vi) ═N—O—R (vii) —CN (viii) —S(O) (ix) aryl, and optionally substituted aryl (x) heteroaryl, and optionally substituted heteroaryl (xi) C (xii) heterocycloalkyl, and optionally substituted heterocycloalkyl (xiii) NR (xiv) NR (xv) ═N—NR (xvi) ═N—R (xvii) ═N—NR (xviii) ═N—NR (4) C (5) C (i) halogen, (ii) OR (iii) O—S(O) (iv) —CHO, (v) oxo, (vi) —CO (vii) —C(O)—R (viii) —CN (ix) aryl, and optionally substituted aryl (x) heteroaryl, and optionally substituted heteroaryl (xi) C (xii) C (xiii) NR (xiv) NR (xv) NR (xvi) ═N—O—R (xvii) ═N—NR (xviii) ═N—NR (xix) ═N—NR (xx) ═N—NR (6) C (7) C (i) trialkylsilyl (ii) halogen, (iii) —CN (iv) OR (v) —CHO, (vi) oxo, (vii) —CO (viii) —C(O)NR (ix) NR (x) O—S(O) (xi) C (xii) C (xiii) aryl, and optionally substituted aryl (xiv) heteroaryl, and optionally substituted heteroaryl (xv) NR (xvi) NR (xvii) ═N—O—R (xviii) ═N—NR (xix) ═N—NR (xx) ═N—NR (8) cyclic substituents selected from the group consisting of (i) aryl, and optionally substituted aryl (ii) heteroaryl, and optionally substituted heteroaryl (iii) heterocycloalkyl, and optionally substituted heterocycloalkyl, and (iv) C (9) C (i) —CHO (ii) —CN (iii) CO (iv) C(O)NR (v) C(S)NR (vi) C(NR (vii) CH═N—O—R (viii) CH═N—R (ix) CH═N—NR (x) CH═N—NR (xi) CH═N—NR R (1) H (2) methyl (3) methyl substituted with one or more substituents selected from the group consisting of (i) F (ii) —CN (iii) —CO (iv) —C(O)NR (v) aryl, and optionally substituted aryl, and (vi) heteroaryl, and optionally substituted heteroaryl (4) C (5) substituted C (i) halogen, (ii) OR (iii) C (iv) —CHO (v) oxo (vi) NR (vii) ═N—O—R (viii) —CN (ix) —S(O) (x) aryl, and optionally substituted aryl (xi) heteroaryl, and optionally substituted heteroaryl (xii) C (xiii) C (xiv) heterocycloalkyl (xv) NHC(O)R (xvi) NHC(O)NR (xvii) ═N—NR (xviii) ═N—R (xix) ═N—NHC(O)R (4) C (i) halogen, (ii) OR (iii) —CHO (iv) oxo (v) —S(O) (vi) —CN (vii) —CO (viii) NR (ix) ═N—O—R (x) —C(O)—R (xi) —C(O)NR (xii) aryl, and optionally substituted aryl (xiii) heteroaryl, and optionally substituted heteroaryl (xiv) C (xv) C (xvi) NHC(O)R (xvii) NHC(O)NR (xviii) ═N—NR (xix) ═N—R (xx) ═N—NHC(O)R (xxi) ═N—NHC(O)NR (5) C (6) C (i) halogen, (ii) OR (iii) —CHO (iv) oxo (v) —CO (vi) —C(O)NR (vii) —CN (viii) NR (ix) ═N—O—R (x) —S(O) (xi) aryl, and optionally substituted aryl (xii) heteroaryl, and optionally substituted heteroaryl (xiii) C (xiv) C (xv) NHC(O)R (xvi) NHC(O)NR (xvii) ═N—NR (xviii) ═N—R (xix) ═N—NHC(O)R (xx) ═N—NHC(O)NR R (1) hydrogen (2) OH (3) OR (4) OC(O)R (5) O(CO)OR and X and Y taken together are selected from the group consisting of (1) O (2) NOR (3) N—O C(R (4) NR (5) N—NR (1) —OR (2) —NR R wherein aryl groups have 5 to 10 ring atoms, and heteroaryl groups have 5 to 10 ring atoms including C and at least one of N, O or S.