US 11,787,833 B2
Modified cyclic dinucleoside compounds as sting modulators
Leonid Beigelman, San Mateo, CA (US); Santhosh Kumar Thatikonda, Fremont, CA (US); and Antitsa Dimitrova Stoycheva, Half Moon Bay, CA (US)
Assigned to Aligos Therapeutics, Inc., South San Francisco, CA (US)
Filed by ALIGOS THERAPEUTICS, INC., South San Francisco, CA (US)
Filed on May 6, 2020, as Appl. No. 16/868,013.
Claims priority of provisional application 62/981,475, filed on Feb. 25, 2020.
Claims priority of provisional application 62/845,703, filed on May 9, 2019.
Prior Publication US 2020/0369711 A1, Nov. 26, 2020
Int. Cl. C07H 21/02 (2006.01); A61P 35/04 (2006.01); A61K 9/00 (2006.01)
CPC C07H 21/02 (2013.01) [A61P 35/04 (2018.01); A61K 9/0019 (2013.01)] 18 Claims
 
1. A compound selected from Formula (I), or a pharmaceutically acceptable salt thereof:

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wherein:
Ring A1A is

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Ring A2A is independently selected from the group consisting of

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B1A is an optionally substituted [5,6] bicyclic heteroaryl or an optionally substituted [5,6] bicyclic heterocyclyl, and wherein B1A is attached to the 1′-position of Ring A1A;
B2A is an optionally substituted [5,6] bicyclic heteroaryl or an optionally substituted [5,6] bicyclic heterocyclyl, and wherein B2A is attached to the 1′-position of Ring A2A;
X1A and X3A are independently OH, O−, SH, S−, O(unsubstituted C1-4 alkyl), S(unsubstituted C1-4 alkyl), O—CH2—O—C(═O)-(unsubstituted C1-4 alkyl), S—CH2—O—C(═O)-(unsubstituted C1-4 alkyl), O—CH2—O—C(═O)—O-(unsubstituted C1-4 alkyl), S—CH2—O—C(═O)—O-(unsubstituted C1-4 alkyl),

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or

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X2A and X4A are independently O or S;
R1A is hydrogen or halogen, and wherein R1A is attached to the 2′-position of Ring A1A;
R2A is selected from the group consisting of hydrogen, halogen, hydroxy, an unsubstituted C1-4 alkoxy and

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and wherein R2A is attached to the 2′-position of Ring A1A, and when R2A is

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then the * indicates an attachment point to the 4′-position of Ring A1A;
R3A is hydrogen or halogen, and wherein R3A is attached to the 3′-position of Ring A2A;
R4A is selected from the group consisting of hydrogen, halogen, hydroxy and an unsubstituted C1-4 alkoxy, and wherein R4A is attached to the 3′-position of Ring A2A;
R5A is hydrogen, and wherein R5A is attached to the 4′-position of Ring A2A; or
R4A and R5A are taken together to form

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wherein each * indicates a point of attachment to ring A2A.