Invention Grant
- Patent Title: CBP/catenin signaling pathway inhibitors and uses thereof
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Application No.: US17199304Application Date: 2021-03-11
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Publication No.: US11655253B2Publication Date: 2023-05-23
- Inventor: Fuqiang Ruan
- Applicant: 3+2 Pharma, LLC
- Applicant Address: US DE Lewes
- Assignee: 3+2 PHARMA, LLC
- Current Assignee: 3+2 PHARMA, LLC
- Current Assignee Address: US DE Lewes
- Agency: Aikin & Gallant, LLP
- Main IPC: C07D487/04
- IPC: C07D487/04 ; A61P17/08 ; A61P1/16 ; A61P11/00 ; A61K8/49 ; A61K9/00 ; A61K39/39 ; A61K45/06 ; A61Q19/08

Abstract:
Provided are compounds of formula (Ia), (Ib) and (IIa), and pharmaceutically acceptable salts thereof. Additionally provided are compositions and pharmaceutical compositions comprising the compounds, therapeutic methods using same for modulating (e.g., inhibiting) CREB binding protein (CBP)/β-catenin mediated signaling in treating a condition, disease or disorder (e.g., fibrosis, cancer, neurological conditions, metabolic disorders (e.g., diabetes, etc.), and skin conditions (dermatitis, psoriasis, scarring, alopecia, etc.) mediated by aberrant CBP/β-catenin signaling, and cosmetic methods for treating skin conditions (e.g., aging, etc.). Additionally, provided are methods for enhancing vaccine efficacy using the compounds and compositions. Further provided are methods for efficiently synthesizing a clinical grade drug, comprising use, in a penultimate, or last reaction step under GMP conditions, of an intermediate 2-propynyl-compound to form a clinical grade isoxazole derivative (e.g., via 3+2 cycloaddition).
Public/Granted literature
- US20210317123A1 CBP/CATENIN SIGNALING PATHWAY INHIBITORS AND USES THEREOF Public/Granted day:2021-10-14
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