COMPOUNDS, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THEM

Abstract

Claim 1: A compound characterized in that it is of formula (1), or a pharmaceutically acceptable salt thereof, wherein R¹ᵃ is selected from the group consisting of -H and -F; R¹ᵇ is selected from the group consisting of -H and -F, wherein R¹ᵃ and R¹ᵇ may not both be -F; R⁴ᵃ is selected from the group consisting of -H and -F; R⁴ᵇ is selected from the group consisting of -H and -F, wherein R⁴ᵃ and R⁴ᵇ may not both be -F; P¹ and P² each independently have an S or R stereochemical configuration; X¹ᵃ and X²ᵃ are the same or different and are independently selected from =O or =S; X¹ᵇ and X²ᵇ are the same or different and are independently selected from -OR⁵ and -SR⁵; where R⁵ is selected from the group consisting of -H, C₁₋₆ alkyl, -C(O)C₁₋₆ alkyl, and -OC(O)OC₁₋₆ alkyl;L¹ in formula (1) has four, five, or six carbons in length, and is of formula (2), wherein ⁻ ⁻ ⁻ ⁻ ⁻ indicates a single bond, a double bond, or a triple bond and wherein the occurrence of 0 or 1 of ⁻ ⁻ ⁻ ⁻ ⁻ in L¹ indicates a double bond or a triple bond, wherein the geometry around the double bond is cis or trans; wherein X¹⁰, X¹¹, X¹², X¹³, X¹⁴, and X¹⁵ are selected independently of a bond, -CH₂-, or -CH-, wherein the -CH₂- or -CH- is unsubstituted or substituted with (i) -OH, (ii) -F, (iii) -Cl, (iv) -NH₂, or (v) -D, and when X¹⁰ or X¹⁵ is a bond, that bond is not a double bond; and wherein any two members of the group including X¹⁰, X¹¹, X¹², X¹³, X¹⁴, and X¹⁵ can optionally form, with additional atoms, a C₃ cycloalkyl or a C₃ heterocycloalkyl, wherein said C₃ heterocycloalkyl includes an atom of N or O;wherein B¹ and B² are independently selected from the compounds of the group of formulas (3), wherein the bonds at points qyr in B¹ and B² are joined at points qyr in formula (1). Claim 19: A pharmaceutically acceptable salt of any one of claims 1 to 18, characterized in that the salt is a diammonium salt. Claim 20: A pharmaceutical composition characterized in that it comprises a compound according to any one of claims 1 to 18 or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient. Claim 30: A method for treating cancer in a patient having an AQ STING allele, characterized in that it comprises administering to said patient a compound, pharmaceutically acceptable salt, or pharmaceutical composition of any one of claims 1 to 20.

Claims

1. A compound of Formula (III): FOLLOWS FORMULA 1, or a pharmaceutically acceptable salt thereof, wherein R1a is selected from the group consisting of -H and -F; R1b is selected from the group consisting of -H and -F, wherein R1a and R1b may not both be -F; R4a is selected from the group consisting of -H and -F; R4b is selected from the group consisting of -H and -F, wherein R4a and R4b may not both be -F; P1 and P2 each independently have an S or R stereochemical configuration; X1a and X2a are the same or different and are independently selected from =O or =S; X1b and X2b are the same or different and are independently selected from -OR5 and -SR5; wherein R 5 is selected from the group consisting of -H, C1-6 alkyl, -C(O)C1-6 alkyl, and -COC(O)OC1-6 alkyl;L1 in formula (III) has four, five, or six carbons in length, and is, FOLLOWS FORMULA 2, wherein - - - - - indicates a single bond, a double bond, or a triple bond and wherein the occurrence of 0 or 1 of - - - - - in L1 indicates a double bond or a triple bond, wherein the geometry around the double bond is cis or trans; wherein X10, X11, X12, X13, X14, and X15 are selected independently of a bond, -CH2-, or -CH-, wherein the -CH2- or -CH- is unsubstituted or substituted with (i) -OH, (ii) -F, (iii) -Cl, (iv) -NH2, or (v) -D, and when X10 or X15 is a bond, that bond is not a double bond; and wherein any two adjacent members of the group including X10, X11, X12, X13, X14, and X15 can optionally form, with additional atoms, a C3 cycloalkyl or a C3 heterocycloalkyl, wherein said C3 heterocycloalkyl includes an atom of N or O;wherein B1 and B2 are independently selected from: FORMULAS 2, 3, 4 AND 5 FOLLOW, wherein the bonds at points qyr in B1 and B2 are joined at points qyr in Formula (III), the compound being characterized in that it is selected from the group consisting of: 22 FORMULAS FOLLOW, or a pharmaceutically acceptable salt thereof selected from the group consisting of a diammonium salt thereof and a triethylamine salt thereof. 16 Claims follow;