MK2 inhibitors and uses thereof
The present invention provides compounds, compositions thereof, and methods of using the MK2 inhibitors of the Formula:
1 . A compound of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
Ring A is a 5-6 membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, provided that when Ring A is a 6-membered heteroaryl ring the 1-3 heteroatoms are each nitrogen;
each R 1 and R 1′ is independently selected from -hydrogen and C 1-4 aliphatic substituted with 0-3 instances of R x , or:
R 1 and R 1′ may, together with the intervening atoms to which they are attached, form an optionally substituted 3- to 6-membered saturated, or partially unsaturated, heterocyclyl, carbocycle, or aryl ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
R x is —CN, —NO 2 , halogen, —OR, —SR, —N(R) 2 , —C(O)N(R) 2 , —C(O)OR, —C(O)R, —N(R)C(O)R, —SO 2 N(R) 2 , or —N(R)SO 2 ;
R 2 is —CN, C 2-6 aliphatic substituted with m instances of R y , wherein the C 2-6 aliphatic has at least one unit of unsaturation, or R 2 is selected from the group consisting of
each R y is independently selected from D, halogen, —CN, —CO 2 R, —N(R) 2 , and a 3- to 6-membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
each R 3 is —(CH 2 ) r -Cy, or R 3 is selected from the group consisting of
each R 4 is independently selected from hydrogen, C 1-6 aliphatic, and —Cy, wherein the C 1-6 aliphatic is optionally substituted with one or more substituents each independently selected from D, halogen and —OR;
each R 5 is independently selected from —OR and —Cy;
each Cy is independently a ring selected from a 3- to 9-membered saturated or partially unsaturated monocyclic carbocyclic ring, a 3- to 9-membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, phenyl, a 5- to 6-membered heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, a 7- to 12-membered saturated or partially unsaturated fused, spirofused, or bridged bicyclic carbocyclic ring, or a 7- to 12-membered saturated or partially unsaturated fused, spirofused, or bridged bicyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, wherein the ring is optionally substituted with one or more substituents each independently selected from D, halogen, oxo, R, and —(CH 2 ) q —OR;
each R is independently hydrogen or a C 1-6 aliphatic optionally substituted with one or more substituents each selected from D, halogen, —OH, and —O—(C 1-6 aliphatic), or:
two R groups on the same nitrogen are taken together with the nitrogen to form a 3-7 membered saturated or partially unsaturated heterocyclic ring having 1-3 heteroatoms selected from nitrogen, oxygen, or sulfur;
n is 0;
each of q, and r is independently 0-4; and
tis 1-4.
2 . The compound according to claim 1 , wherein Ring A is selected from:
3 . The compound according to claim 1 , wherein the compound is selected from any of formulae II, III, IV, or V:
or a pharmaceutically acceptable salt thereof.
4 . The compound according to claim 1 , wherein R 2 is halogen.
5 . The compound according to claim 1 , wherein R 2 is selected from:
6 . The compound according to claim 1 , wherein R 2 is selected from
7 . The compound according to claim 1 , wherein the compound is selected from formulae II-a, II-b, II-c, III-a, III-b, IV-a, IV-b, IV-c, V-a, V-b, or V-c:
or a pharmaceutically acceptable salt thereof.
8 . The compound according to claim 1 , wherein the compound is selected from formulae II-a-i, II-a-ii, II-b-i, II-b-ii, II-c-i, II-c-ii, III-a-i, III-b-i, IV-a-i, IV-a-ii, IV-b-i, IV-b-ii, IV-c-i, IV-c-ii, V-a-i, V-b-i, or V-c-i:
or a pharmaceutically acceptable salt thereof.
9 . The compound according to claim 1 , wherein R 3 is selected from —CH 3 , —CD 3 , —CF 2 H, —CF 3 , —CH 2 CH 3 ,
10 . The compound according to claim 1 , wherein R 3 is selected from —OCH 3 , —OCF 2 H, —OCF 3 , —O(CH 2 ) 2 CH 3 , —O(CH 2 ) 2 OCH 2 CH 3 , —CH 2 OH, —CH 2 OCH 3 , —CH 2 OCH 2 CH 3 ,
11 . The compound of claim 1 or a pharmaceutically acceptable salt thereof, selected from the group consisting of:
(R)-3-(2-ethynyl-5-fluoropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-1)
(R)-3-(5-fluoro-2-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-2)
(R)-3-(2-chloro-5-(ethoxymethyl) pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-3)
(R)-3-(2-chloro-5-(trifluoromethyl) pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-4)
(R)-3-(5-(ethoxymethyl)-2-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-5)
(R)-3-(2-chloro-5-methylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-6)
(R)-3-(6-chloro-2-(methoxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-7)
(R)-3-(2-chloropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (1-8)
(R)-2-chloro-4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)pyrimidine-5-carbonitrile (I-9)
(R)-3-(2-chloro-5-methoxypyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-10)
(R)-3-(6-chloropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-11)
(R)-3-(5-(ethoxymethyl)-2-ethynylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-12)
(R)-3-(2-(methoxymethyl)-6-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-13)
(R)-3-(6-chloro-2-((piperidin-4-yloxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-14)
(R)-3-(6-chloro-2-(((1-methylpiperidin-4-yl)oxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-15)
(R)-3-(2-chloro-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-16)
(R)-3-(6-chloro-2-(4-methylpiperazin-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-17)
(R)-10-methyl-3-(6-(4-methylpiperazin-1-yl)-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-18)
(R)-10-methyl-3-(2-(4-methylpiperazin-1-yl)-6-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-19)
(R)-3-(2-chloro-5-((oxetan-3-yloxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-20)
(R)-10-methyl-3-(5-((oxetan-3-yloxy)methyl)-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-21)
(R)-3-(2-(ethoxymethyl)-6-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-22)
(R)-3-(6-chloro-2-(((tetrahydro-2H-pyran-4-yl)oxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-23)
(R)-3-(2-chloro-5-(((tetrahydro-2H-pyran-4-yl)oxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-24)
(R)-10-methyl-3-(5-(((tetrahydro-2H-pyran-4-yl)oxy)methyl)-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-25)
(R)-10-methyl-3-(5-((1-methylcyclobutoxy)methyl)-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-26)
(R)-3-(2-chloro-5-((1-methylcyclobutoxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-27)
(R)-3-(2-chloro-5-(((3-methyloxetan-3-yl)oxy)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-28)
(R)-10-methyl-3-(5-(((3-methyloxetan-3-yl)oxy)methyl)-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-29)
(R)-3-(6-chloro-2-(ethoxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-30)
(R)-3-(5-fluoro-2-(1-fluorovinyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-31)
(R)-3-(5-methoxy-2-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-32)
(R)-10-methyl-3-(5-methyl-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-33)
(R)-10-methyl-3-(6-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-34)
(R,E)-3-(2-(ethoxymethyl)-6-(prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-35)
(R,Z)-3-(2-(ethoxymethyl)-6-(prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-36)
(R)-3-(2-(ethoxymethyl)-6-(prop-1-en-2-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-37)
(R)-3-(6-ethynylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-38)
(R)-3-(2-(ethoxymethyl)-6-ethynylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-39)
(R)-3-(2-ethynylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-40)
(R)-3-(2-ethynyl-5-methylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-41)
(R)-3-(2-ethynyl-5-methoxypyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-42)
(R)-3-(4-chloro-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-43)
(R)-3-(5-fluoro-2-(prop-1-yn-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-44)
(R,E)-3-(5-fluoro-2-(prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-45)
(R,Z)-3-(5-fluoro-2-(prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-46)
(R)-3-(5-fluoro-2-(prop-1-en-2-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-47)
(R,E)-3-(5-(ethoxymethyl)-2-(prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-48)
(R,Z)-3-(5-(ethoxymethyl)-2-(prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-49)
(R)-3-(5-(ethoxymethyl)-2-(prop-1-en-2-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-50)
(R)-3-(6-ethynylpyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-51)
(R)-3-(6-chloropyridin-2-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-52)
(R)-10-methyl-3-(2-(prop-1-yn-1-yl)pyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-53)
(R)-10-methyl-3-(6-vinylpyridin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-54)
(R)-10-methyl-3-(2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-55)
(R)-3-(6-ethynylpyridin-2-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-56)
(R)-3-(2-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-57)
(R)-3-(2,6-dichloropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-58)
(R)-3-(6-ethynyl-2-(4-methylpiperazin-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-59)
(R)-3-(2-ethynyl-6-(4-methylpiperazin-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-60)
(R)-3-(4-ethynyl-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-61)
(R)-10-methyl-3-(4-(4-methylpiperazin-1-yl)-6-vinylpyrimidin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-62)
(R)-3-(6-(3-amino-3-methylbut-1-yn-1-yl)-2-chloropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-63)
(R)-3-(2-(3-amino-3-methylbut-1-yn-1-yl)-6-chloropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-64)
(R)-3-(6-(3-amino-3-methylbut-1-yn-1-yl)-2-ethynylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-65)
(R)-3-(2-(3-amino-3-methylbut-1-yn-1-yl)-6-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-66)
(R)-3-(2-(3-amino-3-methylbut-1-yn-1-yl)-6-ethynylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-67)
(R)-3-(2,6-dichloropyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-68)
(R)-3-(2-chloro-5-fluoropyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-69)
(R)-3-(5-fluoro-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-70)
(R)-3-(2-ethynyl-5-fluoropyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-71)
(R)-3-(2-chloro-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-72)
(R)-3-(2-chloro-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-73)
(R)-3-(6-chloro-2-(hydroxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-74)
(R)-3-(2-chloro-5-(hydroxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-75)
(R)-3-(2-(hydroxymethyl)-6-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-76)
(R)-3-(5-(hydroxymethyl)-2-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-77)
(R)-3-(6-ethynyl-2-(hydroxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-78)
(R)-3-(2-ethynyl-5-(hydroxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-79)
(R)-3-(2,6-divinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-80)
(R)-3-(5-chloropyridin-3-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-81)
(R)-10-methyl-3-(5-vinylpyridin-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-82)
(R)-3-(5-ethynylpyridin-3-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-83)
(R)-3-(2-chloro-6-(hydroxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-84)
(R)-3-(6-(hydroxymethyl)-2-vinylpyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-85)
(R)-3-(2-ethynyl-6-(hydroxymethyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-86)
(R)-3-(2-chloro-6-((4-methylpiperazin-1-yl)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-87)
(R)-10-methyl-3-(6-((4-methylpiperazin-1-yl)methyl)-2-vinylpyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-88)
(R)-3-(2-ethynyl-6-((4-methylpiperazin-1-yl)methyl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-89)
(R)-3-(6-(1-fluorovinyl)pyridin-2-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-90)
(R)-3-(6-ethynyl-3-methoxypyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-91)
(R)-3-(5-(difluoromethyl)-2-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-92)
(R)-3-(2-chloro-5-(difluoromethyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-93)
(R)-3-(2-chloro-6-(4-methylpiperazin-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-94)
(R)-3-(2-ethynyl-6-(4-methylpiperazin-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-95)
(R)-10-methyl-3-(2-(4-methylpiperazin-1-yl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-96)
(R)-3-(2-chloro-6-(hydroxymethyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-97)
(R)-3-(2-ethynyl-6-(hydroxymethyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-98)
(R)-3-(2-(hydroxymethyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-99)
(R)-3-(6-chloro-1′-methyl-1′,2′,3′,6′-tetrahydro-[2,4′-bipyridin]-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-100)
(R)-10-methyl-3-(1′-methyl-6-vinyl-1′,2′,3′,6′-tetrahydro-[2,4′-bipyridin]-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-101)
(R)-3-(6-ethynyl-1′-methyl-1′,2′,3′,6′-tetrahydro-[2,4′-bipyridin]-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-102)
(R)-3-(2-chloro-6-(1-methylpiperidin-4-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-103)
(R)-3-(6-ethynyl-3-(methylamino)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-104)
(R)-3-(3-(dimethylamino)-6-ethynylpyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-105)
(R)-10-methyl-3-(2-(1-methylpiperidin-4-yl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-106)
(R)-3-(2-ethynyl-6-(1-methylpiperidin-4-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-107)
(R)-3-(2-(1-fluorovinyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-108)
(R)-10-methyl-3-(5-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-109)
(R)-10-methyl-3-(2-methyl-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-110)
(R)-3-(2-ethynyl-5-methylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-111)
(R)-3-(2-ethynyl-6-methylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-112)
(R,E)-10-methyl-3-(2-(prop-1-en-1-yl)pyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-113)
(R,E)-3-(2-(3-(dimethylamino)prop-1-en-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-114)
(R,E)-3-(6-(3-(dimethylamino)prop-1-en-1-yl)pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-115)
(R)-10-methyl-3-(2-(3-(pyrrolidin-1-yl)prop-1-en-2-yl)pyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-116)
(R)-3-(2-(3-(dimethylamino)prop-1-en-2-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-117)
(R)-10-methyl-3-(3-(2-(pyrrolidin-1-yl)ethoxy)-6-vinylpyridazin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-118)
(R)-3-(6-chloro-3-(2-(pyrrolidin-1-yl)ethoxy)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-119)
(R)-3-(6-ethynyl-3-(2-(pyrrolidin-1-yl)ethoxy)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-120)
(R)-3-(2-((4-methoxypiperidin-1-yl)methyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-121)
(R)-3-(2-ethynyl-6-((4-methoxypiperidin-1-yl)methyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-122)
(R)-3-(2-((4,4-difluoropiperidin-1-yl)methyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-123)
(R)-3-(2-((4,4-difluoropiperidin-1-yl)methyl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-124)
(R)-10-methyl-3-(2-((4-methylpiperazin-1-yl)methyl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-125)
(R)-3-(2-ethynyl-6-((4-methylpiperazin-1-yl)methyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-126)
(R)-3-(3-methoxy-6-vinylpyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-127)
(R)-10-methyl-3-(3-(methylamino)-6-vinylpyridazin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-128)
(R)-3-(3-(dimethylamino)-6-vinylpyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-129)
(R)-3-(5-(difluoromethyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-130)
(R)-10-methyl-3-(2-(3-morpholinoprop-1-en-2-yl)pyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-131)
(R)-3-(6-chloro-3-(2-morpholinoethoxy)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-132)
(R)-10-methyl-3-(3-(2-morpholinoethoxy)-6-vinylpyridazin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-133)
(R)-3-(6-ethynyl-3-(2-morpholinoethoxy)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-134)
(R)-3-(2-(3-amino-3-methylbut-1-yn-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-135)
(R)-10-methyl-3-(3-methyl-6-vinylpyridazin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-136)
methyl (R)-4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)-6-vinylpyridazine-3-carboxylate (I-137)
(R)-3-(3-methoxy-6-(3-morpholinoprop-1-en-2-yl)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-138)
(R)-10-methyl-3-(6-(3-morpholinoprop-1-en-2-yl)pyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-139)
(R)-10-methyl-3-(2-(morpholinomethyl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-140)
(R)-3-(2-((1,1-difluoro-6-azaspiro[2.5]octan-6-yl)methyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-141)
(R)-10-methyl-3-(5-(methyl-d3)-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-142)
(R)-3-(5-chloro-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-143)
(R)-3-(5-chloro-2-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-144)
(R,E)-3-(6-(3-(dimethylamino)prop-1-en-1-yl)-3-methoxypyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-145)
(R)-10-methyl-3-(1-methyl-4-vinyl-1H-pyrazol-5-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-146)
(R)-10-methyl-3-(3-vinyl-1H-pyrazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-147)
(R)-10-methyl-3-(4-vinyl-1H-pyrazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-148)
(R)-10-methyl-3-(4-vinylthiazol-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-149)
(R)-10-methyl-3-(2-vinyl-1H-imidazol-5-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-150)
(R)-3-(2-chloro-1H-imidazol-5-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-151)
(R)-3-(4-chloro-1H-pyrazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-152)
(R)-10-methyl-3-(5-(morpholinomethyl)-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-153)
(R)-3-(2-ethynyl-5-(morpholinomethyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-154)
(R)-3-(5-((4-methoxypiperidin-1-yl)methyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-155)
(R)-10-methyl-3-(2-morpholino-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-156)
(R)-3-(2-ethynyl-6-morpholinopyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-157)
(R)-3-(2-(4-methoxypiperidin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-158)
(R)-3-(2-ethynyl-6-(4-methoxypiperidin-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-159)
(R)-6-chloro-4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)nicotinonitrile (I-160)
(R)-4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)-6-vinylnicotinonitrile (I-161)
(R)-6-ethynyl-4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)nicotinonitrile (I-162)
(R)-10-methyl-3-(6-vinylpyrazin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-163)
(R)-10-methyl-3-(2-vinyl-1H-imidazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-164)
(R)-3-(3-chloro-1H-pyrazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-165)
(R)-10-methyl-3-(5-methyl-6-vinylpyrazin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-166)
(R)-10-methyl-3-(3-methyl-6-vinylpyrazin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-167)
(R)-3-(2-(4,4-difluoropiperidin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-168)
(R)-3-(2-ethynyl-6-(morpholinomethyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-169)
(R)-3-(6-ethynyl-3-methylpyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-170)
(R)-10-methyl-3-(2-(4-(methyl-d3)piperazin-1-yl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-171)
(R)-3-(2-ethynyl-6-(4-(methyl-d3)piperazin-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-172)
(R)-3-(2-(4-ethylpiperazin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-173)
(R)-3-(2-(4-ethylpiperazin-1-yl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-174)
(R)-10-methyl-3-(2-(piperazin-1-yl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-175)
(R)-3-(2-ethynyl-6-(piperazin-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-176)
(R)-10-methyl-3-(2-(piperidin-1-yl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-177)
(R)-3-(2-ethynyl-6-(piperidin-1-yl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-178)
(R)-3-(2-(azetidin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-179)
(R)-3-(2-(azetidin-1-yl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-180)
(R)-10-methyl-3-(3-methyl-6-vinylpyrazin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-181)
(R)-3-(2-(4,4-difluoropiperidin-1-yl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-182)
(R)-3-(2-(3,3-difluoroazetidin-1-yl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-183)
(R)-3-(2-(3,3-difluoroazetidin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-184)
(R)-3-(2-(((2S,6R)-2,6-dimethylmorpholino)methyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-185)
(R)-3-(2-(((2S,6R)-2,6-dimethylmorpholino)methyl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-186)
(R)-3-(2-(((2R,6R)-2,6-dimethylmorpholino)methyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-187)
(R)-3-(2-(((2R,6R)-2,6-dimethylmorpholino)methyl)-6-ethynylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-188)
(R)-10-methyl-3-(2-((4-(trifluoromethoxy)piperidin-1-yl)methyl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-189)
(R)-3-(2-ethynyl-6-((4-(trifluoromethoxy)piperidin-1-yl)methyl)pyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-190)
(R)-10-methyl-3-(6-methyl-2-vinyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-191)
(R)-3-(2-chloro-6-methyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-192)
(R)-3-(2-ethynyl-6-methyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-193)
(R)-3-(2,3-dimethyl-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-194)
(R)-3-(5-ethyl-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-195)
(R)-3-(5-cyclopropyl-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-196)
(R)-10-methyl-3-(3-methyl-2-(morpholinomethyl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-197)
(R)-3-(3-fluoro-2-(morpholinomethyl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-198)
(R,E)-10-methyl-3-(2-(3,3,3-trifluoroprop-1-en-1-yl)pyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-199)
(R,E)-3-(3-methoxy-6-(3,3,3-trifluoroprop-1-en-1-yl)pyridazin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-200)
(10R)-3-(2-(2,6-dimethylmorpholino)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-201)
(R)-10-methyl-3-(2-(4-(trifluoromethyl)piperidin-1-yl)-6-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-202)
(R)-10-methyl-3-(3-vinyl-4H-1,2,4-triazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-203)
(R)-3-(3-ethynyl-4H-1,2,4-triazol-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-204)
(R)-3-(2-chloro-1H-imidazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-205)
(R)-10-methyl-3-(4-methyl-2-vinyl-1H-imidazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-206)
(R)-10-methyl-3-(3-vinyl-1H-1,2,4-triazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-207)
(R)-10-methyl-3-(1-methyl-5-vinyl-1H-1,2,4-triazol-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-208)
(R)-10-methyl-3-(2-vinylthiazol-5-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-209)
(R)-3-(3-chloro-1H-1,2,4-triazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-210)
(R)-3-(5-((3,3-difluoroazetidin-1-yl)methyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-211)
(R)-10-methyl-3-(5-((4-(trifluoromethyl)piperidin-1-yl)methyl)-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-212)
(R)-3-(5-(((2S,6R)-2,6-dimethylmorpholino)methyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-213)
(R)-10-methyl-3-(5-vinyl-1H-1,2,4-triazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-214)
rac-(R)-8-(4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)-6-vinylpyridin-2-yl)-1-oxa-8-azaspiro[4.5]decan-2-one (I-215)
rac-(10R)-3-(2-(2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-216)
(R)-3-(3-fluoro-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-217)
(R)-3-(2-ethynyl-3-fluoropyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-218)
(R)-10-methyl-3-(3-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-219)
(R)-3-(2-ethynyl-3-methylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-220)
(R)-3-(2-chloro-3-fluoropyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-221)
(R)-3-(2-ethynyl-1H-imidazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-222)
(R)-10-methyl-3-(3-methyl-5-vinyl-4H-1,2,4-triazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-223)
(R)-10-methyl-3-(3-methyl-5-vinyl-1H-1,2,4-triazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-224)
(R)-10-methyl-3-(6-(3,3,3-trifluoroprop-1-en-2-yl)pyrazin-2-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-225)
(R)-10-methyl-3-(3-(trifluoromethyl)-5-vinyl-1H-1,2,4-triazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-226)
(R)-10-methyl-3-(5-methyl-3-vinylisoxazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-227)
(R)-10-methyl-3-(3-vinylisothiazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-228)
(R)-10-methyl-3-(5-vinylisothiazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-229)
(R)-10-methyl-3-(1-methyl-3-vinyl-1H-pyrazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-230)
(R)-3-(4,5-dimethyl-2-vinyl-1H-imidazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-231)
(R)-10-methyl-3-(2-methyl-5-vinyl-2H-1,2,3-triazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-232)
(R)-10-methyl-3-(1-methyl-4-vinyl-1H-1,2,3-triazol-5-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-233) ethyl (R)-5-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)-2-vinylthiazole-4-carboxylate (I-234)
(R)-10-methyl-3-(1-methyl-5-vinyl-1H-1,2,3-triazol-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-235)
(R)-10-methyl-3-(3-methyl-5-vinyl-1H-pyrazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-236)
(R)-3-(2-((2-methoxyethyl)(methyl)amino)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-237)
(R)-3-(2-(2-oxa-6-azaspiro[3.3]heptan-6-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-238)
(R)-3-(2-(4-fluoropiperidin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-239)
(R)-3-(2-(4-(methoxymethyl)piperidin-1-yl)-6-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-240)
(R)-10-methyl-3-(3-(trifluoromethyl)-5-vinyl-1H-pyrazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-241)
(R)-3-(2-bromo-4-(trifluoromethyl)-1H-imidazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-242)
(10R)-3-(5-(1-hydroxyethyl-2,2,2-d3)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-243)
di-tert-butyl (R)-10-methyl-3-(5-methyl-2-vinylpyridin-4-yl)-8-oxo-10,11-dihydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinoline-9,12-dicarboxylate (I-244)
(R)-10-methyl-3-(5-(trifluoromethoxy)-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-245)
(R)-1-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)-1H-imidazole-2-carbonitrile (I-246)
(R)-3-(5-(difluoromethoxy)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-247)
(R)-3-(5-cyclopropyl-3-vinyl-1H-1,2,4-triazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-248)
(R)-10-methyl-3-(5-(methyl-d3)-2-vinylpyridin-4-yl-3-d)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-249)
(R)-3-(2-bromo-4,5-dichloro-1H-imidazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-250)
(R)-3-(4,5-dichloro-2-vinyl-1H-imidazol-1-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-251)
(R)-3-(5-(hydroxymethyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-252)
(R)-3-(5-(methoxymethyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-253)
(S)-10-(fluoromethyl)-3-(5-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-254)
(S)-10-(fluoromethyl)-3-(2-vinyl-1H-imidazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-255)
(R)-3-(5-methoxy-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-256)
(R)-10-methyl-3-(5-(trifluoromethyl)-3-vinyl-1H-pyrazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-257)
(R)-3-(5-(2-hydroxypropan-2-yl-1,1,1,3,3,3-d6)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-258)
(10R)-3-(5-(1-hydroxyethyl-2,2,2-d3)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-259)
(10R)-3-(5-(1-hydroxyethyl-2,2,2-d3)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-260)
(R)-10-methyl-3-(5-methyl-3-vinyl-1H-1,2,4-triazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-261)
(R)-3-(5-(ethoxymethyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-262)
(R)-3-(5-((2-oxa-6-azaspiro[3.3]heptan-6-yl)methyl)-2-vinylpyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-263)
(R)-10-methyl-3-(5-vinylpyridazin-3-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-264)
(R,E)-10-methyl-3-(5-methyl-2-(prop-1-en-1-yl)pyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-265)
(R,E)-10-methyl-3-(2-(prop-i-en-1-yl)-1H-imidazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-266)
(R)-2-(5-methyl-4-(10-methyl-8-oxo-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-3-yl)pyridin-2-yl)acetonitrile (I-267)
1′-fluoro-2′-(2-((2-methoxyethyl)(methyl)amino)-6-vinylpyridin-4-yl)-1-methyl-6′,8′,9′,11′-tetrahydrospiro[azetidine-3,10′-pyrido[3′,4′:4,5]pyrrolo[2,3-f]isoquinolin]-7′(5′H)-one (I-268)
2′-(2-(2-oxa-7-azaspiro[4.4]nonan-7-yl)-6-vinylpyridin-4-yl)-1′-fluoro-1-methyl-6′,8′,9′,11′-tetrahydrospiro[azetidine-3,10′-pyrido[3′,4′:4,5]pyrrolo[2,3-f]isoquinolin]-7′(5′H)-one (I-269)
1′-fluoro-2′-(2-(4-(methoxymethyl)piperidin-1-yl)-6-vinylpyridin-4-yl)-1-methyl-6′,8′,9′,11′-tetrahydrospiro[azetidine-3,10′-pyrido[3′,4′:4,5]pyrrolo[2,3-f]isoquinolin]-7′(5′H)-one (I-270)
(R)-10-methyl-3-(2-vinyl-1H-benzo[d]imidazol-1-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-271)
(R)-3-(2-chloropyridin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-272)
(R)-3-(2-chloro-5-fluoropyrimidin-4-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-273)
(R)-3-(6-chloro-3-fluoro-5-(trifluoromethyl)pyridin-2-yl)-10-methyl-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one (I-274).
12 . A compound which is (R)-10-methyl-3-(5-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one.
13 . A compound which is (R)-10-methyl-3-(5-methyl-2-vinylpyridin-4-yl)-9,10,11,12-tetrahydro-8H-[1,4]diazepino[5′,6′:4,5]thieno[3,2-f]quinolin-8-one, or a pharmaceutically acceptable salt thereof.