JP-2022514127-A5 -

Dates

Publication Date

20221212

Application Date

20191204

Description

[Invention 1001]Equation (I):A compound having,During the ceremony, X is selected from the group consisting of H, NR 4X , R 5X , and C1 -C6 alkyl groups which may be substituted with 1-3 Ra ; Y ( i ) CO₂R₆Y ; (ii) C(O)NR 4Y R 5Y ; (iii) A heteroaryl comprising 5 to 6 ring atoms, wherein 1 to 4 ring atoms are heteroatoms independently selected from the group consisting of N, N(H), N(Rd ) , O, and S, and one or more of the heteroaryl ring carbon atoms may be substituted by 1 to 2 independently selected Rc ; and (iv) A heterocycloalkenyl comprising 5 to 6 ring atoms, wherein 1 to 4 ring atoms are heteroatoms independently selected from the group consisting of N, N(H), N(Rd ) , O, and S, and one or more of the heterocycloalkenyl ring carbon atoms may be substituted with 1 to 2 independently selected Rb atoms . Selected from the group consisting of; Z (i) H, (ii) C1-6 alkyl, (iii) NR 4Z R 5Z , (iv) OR 6Z , (v)OC(O)R 7Z , (vi) OP(O) OR 8Z OR 9Z , and (vii) A heterocycline comprising 4 to 10 ring atoms, wherein 1 to 3 ring atoms are heteroatoms independently selected from the group consisting of N, N(H), N(Rd ) , and O, and one or more of the heterocycline ring carbon atoms may be substituted with 1 to 4 independently selected Rh atoms . Selected from the group consisting of; Each Z x is H; or each Z x , together with the carbon it is bonded to, forms C=O; Each of R1 , R2 , and R3 is independently selected from R6A , C(O)R7A , and P(O ) OR8AOR9A ; Each of R 4X and R 5X is independently selected from the group consisting of H, C1-6 alkyl; C3-6 cycloalkyl; -C(O)(C1-4 alkyl ); -C(O)O( C1-4 alkyl); -CON(R')(R'') ; -S(O) 1-2 (NR'R''); -S(O) 1-2 ( C1-4 alkyl); -OH; and C1-4 alkoxy; R 4Y and R 5Y are, (i) H; (ii) C1-12 alkyl groups which may be substituted with 1-6 R a groups ; (iii) A heteroaryl comprising 5 to 10 ring atoms, wherein 1 to 4 ring atoms are heteroatoms independently selected from the group consisting of N, N(H), N(Rd ) , O, and S, and one or more of the heteroaryl ring carbon atoms may be substituted with 1 to 4 independently selected Rh ; ( iv ) - ( W1 -W2 ) n -W3 , • W1 is a C1-3 alkylene which may be independently substituted by 1-4 Ra in each occurrence ; • W 2 is independently -N(H)-, -N(Rd)-, -O-, or -S- in each occurrence ; • W3 is a C1-7 alkyl which may be substituted with H or 1-4 Ra ; and n is between 2 and 4. The relevant - ( W1 -W2 ) n -W3 Whether they are independently selected from the group consisting of; or (v) R 4Y and R 5Y , together with the nitrogen atoms to which they are each bonded, form a ring containing 3 to 8 ring atoms, where the ring contains (a) 1 to 7 ring carbon atoms, each substituted by 1 to 2 substituents independently selected from H and C 1 to 3 alkyl groups; and (b) 0 to 3 ring heteroatoms independently selected from the group consisting of N(H), N(R d ), O, and S ( in addition to the nitrogen atoms bonded to R 4Y and R 5Y ); R 4Z and R 5Z , respectively, (i) H; (ii) C1-10 alkyl groups which may be substituted by 1-6 independently selected R a groups ; (iii) C3-6 cycloalkyl ; (iv)-C(O)(C1-4 alkyl ); (v)-C(O)O(C1-4 alkyl ); (vi)-CON(R')(R''); (vii)-S(O) 1~2 (NR'R''); (viii)-S(O) 1-2 (C 1-4 alkyl); (ix)-OH; (x) C 1-4 alkoxys; and (xi) - ( Q1 - Q2 ) q - Q3 , • In each occurrence, Q1 is independently a C1-3 alkylene which may be substituted by 1-4 R a ; Q2 in each occurrence is independently -N(H)-, -N(Rd ) -, -O-, or -S-; Q3 is a C1-7 alkyl which may be substituted with H or 1-4 Ra ; and q is between 2 and 4. ( Q1 -Q2 ) q -Q3​​ Selected independently from the group consisting of; In each appearance, R 6A is, (i) H; and (ii) C1-10 alkyl groups which may be substituted by 1-6 independently selected R a groups Selected independently from the group consisting of; R 6Z​ (i) H; (ii) C1-10 alkyl groups which may be substituted by 1-6 independently selected R a groups ; (iii) C6-10 aryls may be substituted by 1-2 independently selected Rh - ( C0-2 alkylene) - (C6-10 aryl ); (iv) a heteroaryl -(C0-2alkylene)-(heteroaryl) comprising 5-10 ring atoms, where 1-4 ring atoms are heteroatoms independently selected from the group consisting of N, N(H), N(C1-3 alkyl ), O, and S, and one or more of the heteroaryl ring carbon atoms may be substituted with 1-4 independently selected Rh ; (v)-( C1-2 alkylene)-C(=O)NH-(C1-3 alkylene ) -R6Z' ; and (vi) - (T 1 - T 2 ) t - T 3 , • In each occurrence, T1 is independently a C1-3 alkylene which may be substituted by 1-4 Ra ; - In each occurrence, T 2 is independently -N(H)-, -N(Rd ) -, -O-, or -S-; • T3 is a C1-7 alkyl which may be substituted with H or 1-4 Ra ; and t is between 2 and 4. The - ( T1 -T2 ) t -T3 Selected independently from the group consisting of; R 6Z ' A heterocycline comprising C(=O)OH, N( C1-4 alkyl) 2 , NH2 , NH( C1-4 alkyl), and 3 to 10 ring atoms, wherein 1 to 3 ring atoms are heteroatoms independently selected from the group consisting of N, N(H), N( Rd ), and O, and one or more of the heterocycline ring carbon atoms may be sub