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Publication Number
US-11834462-B2
Publication Date
2023-12-05
Expiration Date
Abstract
Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
Core Innovation
The invention provides small-molecule, non-peptidyl somatostatin modulators, with particular emphasis on somatostatin receptor subtype 2 (SSTR2) and SSTR2a modulators. The disclosed concept is to modulate SSTR2 activity and to inhibit secretion of hormones including growth hormone (GH), insulin, glucagon, insulin-like growth factor 1 (IGF-1), and prolactin in a mammal.
The patent discloses compound structures defined by Formula (I), Formula (Ic), Formula (Ic-1), Formula (II), Formula (IIc), and Formula (III), including related variants and sub-variants, together with pharmaceutically acceptable salts, solvates, tautomers, enantiomers, and diastereomeric mixtures. Extensive variable definitions are provided for substituents and heteroaryl motifs, and representative example compounds are listed in Table 1 and Table 3 with specific R-group assignments and named compounds.
The disclosed chemical scope further includes stereoisomeric and enantiomeric forms, isotopic labeling such as 2H, 13C, 15N, 18F, 36Cl, and 123I, and prodrugs and active metabolites. The specification presents non-peptidyl somatostatin modulators rather than peptide analogs such as octreotide and pasireotide, and emphasizes that the disclosed small-molecule approach is intended to address resistance, desensitization, and internalization issues associated with SST2a.
Claims Coverage
The consolidated content supports two independent method claims. The inventive features center on administering a therapeutically effective amount of a structurally defined compound to suppress secretion of specified hormones or to modulate SSTR2 activity, with pharmaceutically acceptable salts and solvates included.
Suppressing secretion of specified hormones using a structure-defined non-peptidyl compound
A method of suppressing secretion of growth hormone (GH), insulin, glucagon, insulin-like growth factor 1 (IGF-1), prolactin, or combinations thereof in a mammal by administering a therapeutically effective amount of a compound having one of the following structures, or a pharmaceutically acceptable salt or solvate thereof.
Modulating SSTR2 activity using a structure-defined non-peptidyl compound
A method for modulating somatostatin receptor subtype 2 (SSTR2) activity in a mammal by administering a therapeutically effective amount of a compound having one of the following structures, or a pharmaceutically acceptable salt or solvate thereof.
Across the independent claims, the core coverage is method-based and is directed to administering a therapeutically effective amount of a compound with depicted structural embodiments to suppress specified hormone secretion or modulate SSTR2 activity in a mammal. The claimed scope explicitly includes pharmaceutically acceptable salts and solvates.
Stated Advantages
Reduced cost and frequency compared to peptide analogs such as octreotide and pasireotide.
Circumvention of resistance, desensitization, and internalization issues associated with SST2a.
Documented Applications
Treatment indications framed across endocrine, tumor, ophthalmic/retinopathy, pain/inflammation, neurodegenerative, and psychiatric conditions.
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