IP Library Patent Application 17618345
Patent Application
App. No. 17/618,345

COMPOUNDS AND COMPOSITIONS FOR TREATING CONDITIONS ASSOCIATED WITH STING ACTIVITY

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Patent No.
US None
App. No.
17/618,345
Abstract

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that inhibit (e.g., antagonize) Stimulator of Interferon Genes (STING). Said chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) STING activation (e.g., STING signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., (cancer) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

Claims (176)

1 . A compound of Formula I:

or a pharmaceutically acceptable salt thereof or a tautomer thereof,

wherein:

each of Y 1 , Y 2 , Y 3 , Y 4 , and Y 5 is independently selected from the group consisting of N and CR 1 ;

W-A is defined according to (A) or (B) below:

(A)

W is selected from the group consisting of:

(k) *C(═O)NR N , *C(═S)NR N , *C(═NR N )NR N (e.g., *C(═NCN)NR N ), *C(═CNO 2 )NR N

(l) *S(O) 1-2 NR N ;

(o) *Q 1 -Q 2 ;

wherein the asterisk denotes point of attachment to NR 6 ;

Q 1 is selected from the group consisting of:

(e) phenylene optionally substituted with from 1-2 independently selected R q1 ; and

(f) heteroarylene including from 5-6 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heteroarylene ring is optionally substituted with from 1-4 independently selected R q1 ;

Q 2 is selected from the group consisting of: a bond, NR N , —S(O) 0-2 —, —O—, and —C(═O)—;

A is:

(i) —Y A1 -Y A2 , wherein:

Y A1 is a bond; or

Y A1 is C 1-6 alkylene, which is optionally substituted with from 1-6 substituents each independently selected from the group consisting of:

R a ;

C 6-10 aryl optionally substituted with 1-4 independently selected C 1-4 alkyl; and

heteroaryl including from 5-10 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heteroaryl ring is optionally substituted with from 1-4 independently selected C 1-4 alkyl; or

Y A1 is —Y A3 -Y A4 —Y A5 which is connected to W via Y A3 wherein:

Y A3 is a C 1-3 alkylene optionally substituted with from 1-2 independently selected R a ;

Y A4 is —O—, —NH—, or —S—; and

Y A5 is a bond or C 1-3 alkylene which is optionally substituted with from 1-2 independently selected R a ; and

Y A2 is:

(a) C 3-20 cycloalkyl, which is optionally substituted with from 1-4 R b ,

(b) C 6-20 aryl, which is optionally substituted with from 1-4 R c ;

(c) heteroaryl including from 5-20 ring atoms, wherein from 1-3 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heteroaryl ring is optionally substituted with from 1-4 independently selected R c ; or

(d) heterocyclyl including from 3-16 ring atoms, wherein from 1-3 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heterocyclyl ring is optionally substituted with from 1-4 independently selected R b ,

OR

(ii) —Z 1 -Z 2 -Z 3 , wherein:

Z 1 is C 1-3 alkylene, which is optionally substituted with from 1-4 R a ;

Z 2 is —N(H)—, —N(R d )—, —O—, or —S—; and

Z 3 is C 2-7 alkyl, which is optionally substituted with from 1-4 R a ;

OR

(iii) C 1-20 alkyl, which is optionally substituted with from 1-6 independently selected R a ,

OR

(B)

W is selected from the group consisting of:

(a) C 8-20 bicyclic or polycyclic arylene, which is optionally substituted with from 1-4 R c ; and

(b) bicyclic or polycyclic heteroarylene including from 8-20 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heteroaryl ring is optionally substituted with from 1-4 independently selected R c ;

A is as defined for A or A is H;

each occurrence of R 1 is independently selected from the group consisting of

H;

halo;

cyano;

C 1-6 alkyl optionally substituted with 1-2 R a ;

C 2-6 alkenyl;

C 2-6 alkynyl;

C 1-4 haloalkyl;

C 1-4 alkoxy;

C 1-4 haloalkoxy;

—S(O) 1-2 (C 1-4 alkyl),

—S(O)(═NH)(C 1-4 alkyl),

SF 5

—NR e R f ,

—OH,

oxo,

—S(O) 1-2 (NR′R″),

—C 1-4 thioalkoxy,

—NO 2 ,

—C(═O)(C 1-4 alkyl),

—C(═O)O(C 1-4 alkyl),

—C(═O)OH,

—C(═O)N(R′)(R″), and

—L 3 -L 4 -L 5 -R i ;

or a pair of R 1 on adjacent atoms, taken together with the atoms connecting them, form a ring (e.g., aromatic or non-aromatic ring) including from 4-15 ring atoms, wherein from 0-3 ring atoms are heteroatoms each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 ; and wherein the ring is optionally substituted with from 1-4 independently selected R 2 ;

each R 2 is independently selected from the group consisting of:

halo;

cyano;

C 1-6 alkyl optionally substituted with 1-2 R a ;

C 2-6 alkenyl;

C 2-6 alkynyl;

C 1-4 haloalkyl;

C 1-4 alkoxy;

C 1-4 haloalkoxy;

—S(O) 1-2 (C 1-4 alkyl) optionally substituted with from 1-3 independently selected R a ,

—S(O)(═NH)(C 1-4 alkyl) optionally substituted with from 1-3 independently selected R a ,

SF 5 ,

—NR e R f ,

—OH,

oxo,

—S(O) 1-2 (NR′R″),

—C 1-4 thioalkoxy,

—NO 2 ,

—C(═O)(C 1-4 alkyl) optionally substituted with from 1-3 independently selected R a ,

—C(═O)O(C 1-4 alkyl) optionally substituted with from 1-3 independently selected R a ,

—C(═O)OH,

—C(═O)N(R′)(R″); and

—L 3 -L 4 -L 5 -R i ;

R 6 is selected from H; C 1-6 alkyl; —OH; C 1-4 alkoxy; C(═O)H; C(═O)(C 1-4 alkyl); CN; C 6-10 aryl optionally substituted with from 1-4 independently selected C 1-4 alkyl; and heteroaryl including from 5-10 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 and wherein the heteroaryl ring is optionally substituted with from 1-4 independently selected C 1-4 alkyl;

each occurrence of R q1 is independently selected from the group consisting of:

(a) halo; (b) cyano; (c) C 1-10 alkyl which is optionally substituted with from 1-6 independently selected R a ; (d) C 2-6 alkenyl; (e) C 2-6 alkynyl; (f) C 3-6 cycloalkyl; (g) C 1-4 alkoxy; (h) C 1-4 haloalkoxy; (i) —S(O) 1-2 (C 1-4 alkyl); (j) —NR e R f ; (k) —OH; (l) —S(O) 1-2 (NR′R″); (m) —C 1-4 thioalkoxy; (n) —NO 2 ; (o) —C(═O)(C 1-4 alkyl); (p) —C(═O)O(C 1-4 alkyl); (q) —C(═O)OH; (r) —C(═O)N(R′)(R″); and (s) oxo;

each occurrence of R a is independently selected from the group consisting of: —OH; —F; —Cl ; —Br; —NR e R f ; C 1-4 alkoxy; C 1-4 haloalkoxy; —C(═O)O(C 1-4 alkyl); —C(═O)(C 1-4 alkyl); —C(═O)OH; —CON(R′)(R″); —OCON(R′)(R″); —S(O) 1-2 (NR′R″); —S(O) 1-2 (C 1-4 alkyl); cyano, and C 3-6 cycloalkyl optionally substituted with from 1-4 independently selected C 1-4 alkyl;

each occurrence of R b is independently selected from the group consisting of: C 1-10 alkyl optionally substituted with from 1-6 independently selected R a ; C 1-4 haloalkyl; —OH; oxo; —F; —Cl ; —Br; —NR e R f ; C 1-4 alkoxy; C 1-4 haloalkoxy; —C(═O)(C 1-10 alkyl); —C(═O)O(C 1-4 alkyl); —C(═O)OH; —C(═O)N(R′)(R″); —S(O) 1-2 (NR′R″); —S(O) 1-2 (C 1-4 alkyl); cyano; and -L 1 -L 2 -R h ;

each occurrence of R c is independently selected from the group consisting of:

(a) halo; (b) cyano; (c) C 1-10 alkyl which is optionally substituted with from 1-6 independently selected R a ; (d) C 2-6 alkenyl; (e) C 2-6 alkynyl; (g) C 1-4 alkoxy; (h) C 1-4 haloalkoxy; (i) —S(O) 1-2 (C 1-4 alkyl) or —S(O) 1-2 (C 1-4 haloalkyl); (j) —NR e R f ; (k) —OH; (l) —S(O) 1-2 (NR′R″); (m) —C 1-4 thioalkoxy or —C 1-4 thiohaloalkoxy; (n) —NO 2 ; (o) —C(═O)(C 1-10 alkyl); (p) —C(═O)O(C 1-4 alkyl); (q) —C(═O)OH; (r) —C(═O)N(R′)(R″); (s) -L 1 -L 2 -R h ; (t) —SF 5 ; and (u) azido;

each occurrence of R d is selected from the group consisting of: C 1-6 alkyl; C 3-6 cycloalkyl; —C(O)(C 1-4 alkyl); —C(O)O(C 1-4 alkyl); —CON(R′)(R″); —S(O) 1-2 (NR′R″); —S(O) 1-2 (C 1-4 alkyl); —OH; C 1-4 alkoxy; and CN;

each occurrence of R e and R f is independently selected from the group consisting of: H; C 1-6 alkyl, wherein the C 1-6 alkyl is independently selected with from 1-4 substituents each independently selected from halo, CN, C 1-4 alkoxy, C 1-4 haloalkoxy, NR′R″, and —OH; C 1-6 haloalkyl; C 3-6 cycloalkyl; —C(O)(C 1-4 alkyl); —C(O)O(C 1-4 alkyl); —CON(R′)(R″); —S(O) 1-2 (NR′R″); —S(O) 1-2 (C 1-4 alkyl); —S(O)(═NR′)(C 1-4 alkyl); —OH; and C 1-4 alkoxy; or

R e and R f together with the nitrogen atom to which each is attached forms a ring including from 3-8 ring atoms, wherein the ring includes: (a) from 1-7 ring carbon atoms, each of which is substituted with from 1-2 substituents independently selected from H and C 1-3 alkyl; and (b) from 0-3 ring heteroatoms (in addition to the nitrogen atom attached to R e and R f ), which are each independently selected from the group consisting of N(R d ), NH, O, and S;

—L 1 is a bond or C 1-3 alkylene optionally substituted with oxo;

—L 2 is —O—, —N(H)—, —S(O) 0-2 —, or a bond;

R h is selected from:

C 3-8 cycloalkyl optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy (in certain embodiments, it is provided that when R h is C 3-6 cycloalkyl optionally substituted with from 1-4 independently selected C 1-4 alkyl, -L 1 is a bond, or -L 2 is —O—, —N(H)—, or —S—);

heterocyclyl, wherein the heterocyclyl includes from 3-16 ring atoms, wherein from 1-3 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , wherein the heterocyclyl is optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy;

heteroaryl including from 5-10 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 and wherein the heteroaryl ring is optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy; and

C 6-10 aryl, which is optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy;

—L 1 is a bond or C 1-3 alkylene optionally substituted with oxo;

—L 4 is a bond; —O—; —N(R N )—; —S(O) 0-2 —; C(═O); —NR N S(O) 0-2 —; —S(O) 0-2 NR N —; —NR N S(O) 1-2 NR N —; —S(═O)(═NR N ); —NR N S(═O)(═NR N ); —S(═O)(═NR N )NR N ; NR N S(═O)(═NR N )NR N ;

—NR N C(O)—; —NR N C(O)NR N —; C 3-6 cycloalkylene; or heterocyclylene including from 3-8 ring atoms wherein from 1-3 ring atoms are heteroatoms each independently selected from the group consisting of N, NH, N(R d ), O, and S(O) 0-2 ;

—L 5 is a bond or C 1-4 alkylene;

R i is selected from:

C 3-8 cycloalkyl optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy (in certain embodiments, it is provided that when R 1 is C 3-6 cycloalkyl optionally substituted with from 1-4 substituents independently selected C 1-4 alkyl, -L 1 is a bond, or -L 2 is —O—, —N(H)—, or —S—);

heterocyclyl, wherein the heterocyclyl includes from 3-16 ring atoms, wherein from 1-3 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , wherein the heterocyclyl is optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy;

heteroaryl including from 5-10 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 and wherein the heteroaryl ring is optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy; and

C 6-10 aryl, which is optionally substituted with from 1-4 substituents independently selected from the group consisting of halo; C 1-4 alkyl optionally substituted with from 1-2 independently selected R a ; C 1-4 haloalkyl; cyano; C 1-4 alkoxy; and C 1-4 haloalkoxy;

each occurrence of R N is independently H or R d ; and

each occurrence of R′ and R″ is independently selected from the group consisting of: H, C 1-4 alkyl, and C 6-10 aryl optionally substituted with from 1-2 substituents selected from halo, C 1-4 alkyl, and C 1-4 haloalkyl; or R′ and R″ together with the nitrogen atom to which each is attached forms a ring including from 3-8 ring atoms, wherein the ring includes: (a) from 1-7 ring carbon atoms, each of which is substituted with from 1-2 substituents independently selected from the group consisting of H and C 1-3 alkyl; and (b) from 0-3 ring heteroatoms (in addition to the nitrogen atom attached to R′ and R″), which are each independently selected from the group consisting of N(H), N(C 1-6 alkyl), O, and S;

provided that when the compound has Formula (I-a1) wherein R 2′ is H or R 2 , W-A is defined according to (A), and W is *C(O)NR N (e.g., *C(O)NH), then 1, 2, 3, 4, or 5 of the following provisions apply:

(i) when each of Y 1 and Y 2 is CH; Y 3 is CR 1 ; R 1 is CO 2 Me, CO 2 Et, CN, or Cl ; and

R 2 is absent (i.e., C2 and C3 are substituted with H), OR when each of Y 1 and Y 2 is N; and

Y 3 is OH or oxo, then A cannot be optionally substituted C 1-6 alkyl, such as methyl or butyl, 1,1,3,3-tetramethylbutyl, or optionally substituted C 3 or C 6 cycloalkyl (such as C 1-6 alkyl or C 3 or C 6 cycloalkyl optionally substituted with CO 2 H, isocyanate, or substituted amino);

(ii) when each of Y 1 and Y 2 is N; and Y 3 is CR 1 ; then

R 1 cannot be furyl, when W-A is benzyl; and

R 1 cannot be substituted N-linked aniline or chloro when either R 2′ is methyl or when W-A is phenyl substituted with from 1-2 substituents independently selected from —Cl , —F, —Br, and CF 3 ;

(iii) when each of Y 1 , Y 2 , and; Y 3 is CH; R 2′ is H, R 2 is present and attached at the C3-position of the indole ring; and A is phenyl, tolyl, optionally substituted quinazolinyl, optionally substituted pyrazolyl, optionally substituted indolyl, optionally substituted naphthyl, or optionally substituted moropholinyl-phenyl, then R 2 cannot be oxazolyl, pyridyl, C-linked-2-pyridylethyl, phenyl, cyano, or C(O)NH 2 ;

(iv) when each of Y 1 and Y 3 is CH; Y 2 is CH or CMe; R 2′ is H; and R 2 is absent, then:

R h cannot be a fused tricyclic ring;

Y A2 cannot be optionally substituted cyclohexyl, cyclohexenyl, imidazo[1,2-a][1,4]benzodiazepin-4-yl, indenyl, naphthyl, or tetrahydronaphthyl;

Y A1 cannot be alkylene substituted with phenyl;

when Y A1 is alkylene, Y A2 cannot be phenyl or the following substituted phenyl rings: 4-Br, 2,4-(Cl) 2 , 3-propenyl, 2,3-(OMe) 2 , and 4-CF 3 ; and

when Y A1 is absent, Y A2 cannot be phenyl or the following substituted phenyl rings: 3-NO 2 , 4-Br, 2,4-(Cl) 2 , 2,3-(OMe) 2 , 4-CF 3 , 4-CO 2 Et, 3-CF 3 -4-Cl, 2-Cl-4 CF 3 , 2-OEt, 2-OMe-4-NO 2 , 3,4-(OMe) 2 , 2,4-(Me) 2 , 3,4-(Cl ) 2 , 2,4-(F) 2 , 2-Et, 2-F, 2-Me, 2-Br, 2-Cl-4-Br, 2-CF 3 , 2,4-(OMe) 2 , 2,3-(Me) 2 , 3,5-(Cl ) 2 , 3-CF 3 -4-F, 4-iso-propyl, 4-OMe, 4-Cl, 3-F-4-Me, 3-CF 3 , 2,5-(OMe) 2 , 2-Me-3-Cl, 2,3-(Me) 2 , 2,3-(Cl ) 2 , 4-Bu, 3-OMe, 3-Cl, 4-Me-2-Cl, 3-SMe, 2-CO 2 Me, 4-Me-3-Cl, 3,4-(Me) 2 , 4-sec-butyl, 2-OMe, 2-Cl, 2,4-(OMe) 2 -5-Cl, 4-OEt, 4-acetyl, 2-OMe-5-Me, 2-Me-5-Cl, 3,5-(Me) 2 , 3,5-(Cl ) 2 , 4-NO 2 , 4-Br, 4-F, 4-Me, 4-Et, 3-F, 3-Me, 3-acetyl, or 2-Me-5-Cl ; and

(v) the compound is other than:

2 . The compound of claim 1 , wherein a pair of R 1 on adjacent atoms, taken together with the atoms connecting them, form an aromatic ring including 5 ring atoms, wherein from 1-2 (such as 1 or 2) ring atoms are heteroatoms each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 ; and wherein the ring is optionally substituted with from 1-4 independently selected R 2 .

3 . The compound of claims 1 or 2 , wherein a pair of R 1 on adjacent atoms, taken together with the atoms connecting them, form:

wherein each R 2′ is independently H or R 2 , such as

such as

4 . The compound of any one of claims 1 - 3 , wherein the compound has the following formula:

such as,

wherein R 2′ is H or R 2 , such as R 2′ is H.

5 . The compound of any one of claims 1 - 4 , wherein the compound has formula

wherein R 2′ is H or R 2 , such as

(e.g., R 1 is other than H) Formula (I-a1-b),

(e.g., R 1 is other than H) Formula (I-a1-e).

6 . The compound of any one of claims 1 - 5 , wherein each occurrence of R 1 that is not taken together with the atom to which it is attached in ring formation is independently selected from the group consisting of: H; halo; cyano; C 1-6 alkyl optionally substituted with 1-2 R a ; C 2-6 alkenyl; C 2-6 alkynyl; C 1-4 haloalkyl; C 1-4 alkoxy; C 1-4 haloalkoxy; —S(O) 1-2 (C 1-4 alkyl); —NR e R f ; —OH; oxo; —S(O) 1-2 (NR′R″); —C(═O)(C 1-4 alkyl); —C(═O)O(C 1-4 alkyl); —C(═O)OH; —C(═O)N(R′)(R″); and -L 3 -L 4 -R i , such as R 1 is halo; cyano; C 1-6 alkyl optionally substituted with 1-2 R a ; C 1-4 haloalkyl; C 1-4 alkoxy; or C 1-4 haloalkoxy, such as R 1 is halo.

7 . The compound of any one of claims 1 - 6 , wherein W-A as defined according to (A).

8 . The compound of claim 7 , wherein W is *C(═O)NR N , such as *C(═O)NH.

9 . The compound of any one of claims 1 - 6 , wherein W-A is as defined according to (B).

10 . The compound of any one of claims 1 - 6 and 9 , wherein W is bicyclic heteroarylene including from 8-10 ring atoms, wherein from 1-4 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heteroaryl ring is optionally substituted with from 1-4 independently selected R c ; and A is H,

such as W is selected from the group consisting of quinolinylene, isoquinolinylene, and quinazolinylene, each of which is optionally substituted with from 1-2 independently selected R c , such as W is

11 . The compound of any one of claims 1 - 9 , wherein A is —Y A1 -Y A2 .

12 . The compound of any one of claims 1 - 9 or 11 , wherein Y A2 is C 6-10 aryl, which is optionally substituted with from 1-3 R c .

13 . The compound of claim 1 , wherein the compound has one of the following formulae:

wherein:

n1 is 0, 1, or 2 (such as 0 or 1); each of R cA and R cB is an independently selected R c ;

W is *C(═O)NR N , such as *C(═O)NH; and

the

moiety is

wherein R 2′ is H or R 2 .

14 . The compound of claim 13 , wherein the

moiety is

(a1-b), such as (a1-b) wherein R 1 is other than H (e.g., R 1 is halo or cyano).

15 . The compound of claim 1 , wherein W is heteroarylene including from 9-10 ring atoms, wherein from 1-2 ring atoms are heteroatoms, each independently selected from the group consisting of N, N(H), N(R d ), O, and S(O) 0-2 , and wherein the heteroaryl ring is optionally substituted with from 1-2 independently selected R c , such as

W is selected from the group consisting of quinolinylene and quinazolinylene, each of which is optionally substituted with from 1-2 independently selected R c , such as:

W is

the

moiety is

and

A is H, optionally wherein R 6 is H.

16 . The compound of claim 1 , wherein the compound is selected from the group consisting of the compounds delineated in Table C1 or a pharmaceutically acceptable salt thereof.

17 . A pharmaceutical composition comprising a compound of any one of claims 1 - 16 , or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients.

18 . A method for inhibiting STING activity, the method comprising contacting STING with a compound as claimed in any one of claims 1 - 16 , or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as claimed in claim 17 .

19 . A method of inducing an immune response in a subject in need thereof, the method comprising administering to the subject an effective amount of a compound as claimed in any one of claims 1 - 16 , or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as claimed in claim 17 .

20 . A method of treatment of disease, disorder, or condition associated with STING, such as a disease, disorder, or condition, in which increased STING signaling, such as excessive STING signaling, contributes to the pathology and/or symptoms and/or progression of the disease, such as cancer, comprising administering to a subject in need of such treatment an effective amount of a compound as claimed in any one of claims 1 - 16 , or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition as claimed in claim 17 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 16, 2024
From: IFM DUE, INC.
To: NOVARTIS PHARMA AG
Reel/Frame 069303/0483 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 21, 2021
From: KATZ, JASON; VENKATRAMAN, SHANKAR; ROUSH, WILLIAM R.
To: IFM MANAGEMENT, INC.
Reel/Frame 058447/0390 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 21, 2021
From: IFM MANAGEMENT, INC.
To: IFM DUE, INC.
Reel/Frame 058447/0463 →