Heterocyclic GLP-1 agonists
Inventors
Meng, Qinghua • XING, Weiqiang • Zhang, Haizhen • Lin, Xichen • Lei, Hui • Jennings, Andrew
Assignees
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Publication Number
US-12221442-B2
Publication Date
2025-02-11
Expiration Date
Abstract
This disclosure relates to GLP-1 agonists of Formula (I), including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.
Core Innovation
The invention relates to compounds of Formula I, or pharmaceutically acceptable salts or solvates thereof, wherein the compound includes a moiety represented by Formula (I-A). The Formula (I-A) moiety defines L3 as —O—, allows an optional single or double bond, and specifies atom-type positions including X1 as CH or N and other positions selected as C or N according to the stated formula. It also defines T1 as C(=O)OH and T2 as hydrogen or (C1-C6) alkyl optionally substituted with alkoxy, thioalkoxy, haloalkoxy, S(O)2(C1-C6 alkyl), cycloalkyl, heterocycloalkyl, phenyl, or heteroaryl groups.
Within the Formula I/I-A framework, W1 is CRY1 or N, and when W1 is CRY1, the RY1 and RY2 groups taken together form a (C1-C4)alkylene with one CH2 unit optionally replaced by O, S, NH, or N(C1-3 alkyl). The definition further provides selectable B1, B2, B3, and B4 positions as CR1 or N, with R1 selected from hydrogen, halogen, CN, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C3)alkyl(C3-C6)cycloalkyl, (C1-C3)alkyl(3- to 5-membered heterocycloalkyl), or —C(O)NR2R3, where R2 and R3 are independently hydrogen or (C1-C6)alkyl.
The compound family further defines linkage groups L4 and L5 from specified groups including —C(RcRc)—, —O—, —S—, —N(C1-3 alkyl)—, C(=O), and —S(O)1-2—, with conditional pairing constraints between L4 and L5. Ring C is selected from phenyl, 5- to 6-membered heteroaryl, (C3-C6)cycloalkyl, (C5-C10)bicycloalkyl, 5- to 10-membered bicycloheteroaryl, and 3- to 6-membered heterocycloalkyl, with additional Rb substituent options and b selected as an integer from 0-3. The document also provides specific illustrated and numbered compound embodiments within this Formula I scaffold.
Claims Coverage
The claim coverage centers on a compound of Formula I with a detailed Formula (I-A) moiety, together with dependent claims that narrow the scope to specific illustrated or numbered compounds and one claim for a pharmaceutical composition. Four core inventive feature groups are present in the independent claim framework.
Formula I compound with Formula I-A moiety
A compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, wherein the moiety is represented by the moiety of Formula (I-A), including L3 as —O—, an optional single or double bond, defined X positions, T1 as C(=O)OH, and T2 as hydrogen or (C1-C6) alkyl optionally substituted with defined substituent classes.
Conditional W1 alkylene formation and defined RY substituents
W1 is CRY1 or N, with RY1 and RY2 selected from defined groups and, when W1 is CRY1, RY1 and RY2 together forming a (C1-C4)alkylene with optional replacement of one CH2 unit by O, S, NH, or N(C1-3 alkyl).
Linkage groups L4 and L5 with pairing constraints
L4 and L5 are selected from specified linkage groups including —C(RcRc)—, —O—, —S—, —N(C1-3 alkyl)—, C(=O), and —S(O)1-2—, with conditional compatibility rules governing which combinations are permitted.
Ring C selection and substituent options
Ring C is selected from phenyl, heteroaryl, cycloalkyl, bicycloalkyl, bicycloheteroaryl, and heterocycloalkyl options, with Rb selected from alkyl, haloalkyl, alkoxy, haloalkoxy, halogen, cycloalkyl, and CN, and b selected from 0-3.
Selected from illustrated specific compounds
A compound according to the Formula I claim is selected from a group of illustrated specific compounds.
Selected from specific numbered chemical structures
A compound according to the Formula I claim is selected from the specific numbered chemical structures shown in the group.
Pharmaceutical composition including a pharmaceutically acceptable excipient
A pharmaceutical composition comprising a compound according to the Formula I claim, or a pharmaceutically acceptable salt or solvate thereof, together with a pharmaceutically acceptable excipient.
Claim coverage is anchored by the broad Formula I / Formula (I-A) chemical definition with detailed substituent, linkage, and ring selections. Dependent claims narrow this scope to specific illustrated or numbered compounds, and one claim covers a pharmaceutical composition including a pharmaceutically acceptable excipient.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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