Phthalazine derivatives as inhibitors of PARP1, PARP2, and/or tubulin useful for the treatment of cancer

Inventors

Peto, Csaba J. • Jablons, David M. • TSANG, Tsze • Lemjabbar-Alaoui, Hassan

Assignees

Atlasmedx Inc • University of California San Diego UCSD

Abstract

This invention provides, among other things, compounds useful for treating diseases such as cancer, pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.

Core Innovation

The disclosure provides structure-defined compounds, including pharmaceutically acceptable salts and hydrochloric salt forms, built upon benzimidazole-based carbamate, urea, and phthalazinone derivatives. The compounds are specified through variable substituent definitions and embedded chemical structures, with recurring motifs including a benzimidazole core, a (4-oxo-3,4-dihydrophthalazin-1-yl)methyl group, and fluorinated aromatic variants.

The described structures include fused benzimidazole/imidazo[ ]pyridine systems, benzimidazole/phthalazinone scaffolds, and linked ring systems labeled T and U. The structural scope includes methyl, ethyl, and 2-methoxyethyl carbamate derivatives, together with fluorinated, chlorinated, methoxy, dimethoxy, trifluoromethyl, trifluoromethoxy, difluoromethoxy, hydroxyl, and methyl substituents, as well as heteroaromatic variants such as furan and imidazo[4,5-b]pyridine, imidazo[3,5-b]pyridine, imidazo[3,4-c]pyridine, and imidazo[4,5-c]pyridine.

The disclosure further defines substituent groups and variable attachment options that control the chemical structure, including Y groups described as C(O) or S(O)2 and Z linkers including —O—, —CH2—, —NH—, and —N(CH2)R7—. The compounds are further described as a family of structure-defined examples with carbamate, urea, and sulfonamide functionality, and the content focuses on the chemical structures, named examples, and associated structure images or molecule files for the listed compound series.

Claims Coverage

The independent claims provided cover four core categories: structure-defined compounds, hydrochloric salt forms of such compounds, and pharmaceutical formulations that include either the compound or the hydrochloric salt with a pharmaceutically acceptable excipient. Across the combined items, the claim coverage repeatedly centers on these four inventive feature types.

Across the independent claims, the coverage is organized around structure-defined compounds, their hydrochloric salt forms, and pharmaceutical formulations containing either the compound or the hydrochloric salt together with a pharmaceutically acceptable excipient.

Stated Advantages

Documented Applications