Heterocyclic GLP-1 agonists
Inventors
Meng, Qinghua • Lei, Hui • Zhang, Haizhen • Lin, Xichen • Jennings, Andrew
Assignees
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Publication Number
US-11897851-B2
Publication Date
2024-02-13
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 a compound of Formula (I-A4-1), or a pharmaceutically acceptable salt thereof. The compounds are defined by a set of structural variables that constrain the chemical structure, including a single bond or a double bond, R0-1, X4, Ry, T2, Raa, Ring C, b, and each occurrence of Rb. The definition includes Ring C selected from phenyl or a 6-membered heteroaryl and a limited set of allowed substituents for the variable positions.
Within Formula (I-A4-1), R0-1 is selected from hydrogen and (C1-C3)alkyl, X4 is selected from N and CRy, and Ry is selected from hydrogen, —OH, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, CN, and halogen. T2 is defined as (C1-C3)alkyl substituted with a substituent selected from (C1-C3)alkoxy, S(O)2(C1-C3 alkyl), (C3-C6)cycloalkyl, 3- to 6-membered heterocycloalkyl, phenyl, and 5- to 6-membered heteroaryl, with optional halogen or (C1-C3)alkyl substitution on phenyl or 5- to 6-membered heteroaryl.
Raa is selected from hydrogen and (C1-C3)alkyl, b is 0, 1, or 2, and each occurrence of Rb is independently selected from (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, halogen, and CN. The disclosure also includes illustrated chemical structures and dependent claim refinements to selected illustrated compounds and pharmaceutical compositions with pharmaceutically acceptable excipients.
Claims Coverage
Independent claim clm-00001 covers a compound of Formula (I-A4-1) or a pharmaceutically acceptable salt thereof. It defines seven inventive feature groupings: the bond type, R0-1, X4 and Ry, the substituted alkyl group T2, Raa, Ring C, and the integer subscript b with independent Rb selection.
Compound of Formula (I-A4-1) and pharmaceutically acceptable salt
A compound of Formula (I-A4-1), or a pharmaceutically acceptable salt thereof.
Bond and R0-1 selection
A single bond or a double bond; R0-1 selected from hydrogen and (C1-C3)alkyl.
X4 and Ry substituent choices
X4 selected from N and CRy; Ry selected from hydrogen, —OH, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, CN, and halogen.
Substituted alkyl group T2
T2 is (C1-C3)alkyl substituted with a substituent selected from (C1-C3)alkoxy, S(O)2(C1-C3 alkyl), (C3-C6)cycloalkyl, 3- to 6-membered heterocycloalkyl, phenyl, and 5- to 6-membered heteroaryl, wherein phenyl or 5- to 6-membered heteroaryl are optionally substituted with halogen or (C1-C3)alkyl.
Raa and Ring C selection
Raa is selected from hydrogen and (C1-C3)alkyl; Ring C is selected from phenyl and 6-membered heteroaryl.
Counts b and independent Rb occurrence selection
b is 0, 1, or 2; and each occurrence of Rb is independently selected from (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)alkoxy, (C1-C6)haloalkoxy, halogen, and CN.
Claim clm-00001 defines a Formula (I-A4-1) compound family through tightly specified ring and substituent variables, including T2, Ring C, and b-controlled Rb substitution, and extends to pharmaceutically acceptable salts. Dependent claims refine scope to selected illustrated structures and pharmaceutical compositions with pharmaceutically acceptable excipients.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treatment of GLP-1-associated diseases, including type 2 diabetes mellitus (T2DM).
Combination therapy in anti-diabetic, anti-obesity, or GLP-1 treatment contexts.
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