Wnt pathway modulators

Patent metadata

Field	Value
Publication number	US-2020270255-A1
Application number	US-201816646655-A
Country	US
Kind code	A1
Filing date	Sep 11, 2018
Priority date	Sep 14, 2017
Publication date	Aug 27, 2020
Grant date	—

Abstract

The application relates to a 2,6-dioxo-purine derivative, 2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-hydroxyphenyl)pyridazin-3-yl)acetamide, and the use of this compound in the modulation of the Wnt pathway, and treating a disease or condition associated with Wnt pathway activity, such as cancer, a fibrotic disease, a degenerative disease or a metabolic disease.

First claim

1 . A compound of the following formula:

or a pharmaceutically acceptable salt, solvate, or prodrug thereof.

2 . A compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof for use as a medicament.

3 . A method of modulating Wnt secretion and/or porcupine activity comprising exposing cells to a compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof.

4 . A method of treating a disease or condition associated with Wnt pathway activity comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof.

5 . The method of claim 4 , wherein the disease or condition is selected from the group consisting of cancer, or a fibrotic disease, or a degenerative disease, or a metabolic disease.

6 . The method of claim 5 , wherein the cancer is selected from cervical, colon, breast, bladder, head and neck, gastric, lung, ovarian, prostate, thyroid, non-small-cell lung, chronic lymphocytic leukemia, mesothelioma, melanoma, pancreatic adenocarcinoma, basal cell carcinoma, osteosarcoma, hepatocellular carcinoma, Wilm's tumor or medulloblastoma, wherein the fibrotic disease is selected from pulmonary fibrosis, liver fibrosis, skin fibrosis or renal fibrosis, and wherein the metabolic disease is diabetic retinopathy.

7 . The method of claim 4 wherein the disease or condition is a cancer characterized by high Wnt activity.

8 . A compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof for use in the treatment of a disease or condition associated with Wnt pathway activity.

9 . The compound according to claim 8 wherein the disease or condition is selected from the group consisting of cancer, or a fibrotic disease, or a degenerative disease, or a metabolic disease.

10 . The compound according to claim 9 , wherein the cancer is selected from cervical, colon, breast, bladder, head and neck, gastric, lung, ovarian, prostate, thyroid, non-small-cell lung, chronic lymphocytic leukemia, mesothelioma, melanoma, pancreatic adenocarcinoma, basal cell carcinoma, osteosarcoma, hepatocellular carcinoma, Wilm's tumor or medulloblastoma, wherein the fibrotic disease is selected from pulmonary fibrosis, liver fibrosis, skin fibrosis or renal fibrosis, and wherein the metabolic disease is diabetic retinopathy.

11 . The compound according to claim 8 , wherein the disease or condition is a cancer that is characterized by high Wnt activity.

12 . Use of a compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof in the manufacture of a medicament for the treatment of a disease or condition associated with Wnt pathway activity.

13 . The use of claim 12 wherein the disease or condition is selected from the group consisting of cancer, or a fibrotic disease, or a degenerative disease, or a metabolic disease.

14 . The use of claim 13 , wherein the cancer is selected from cervical, colon, breast, bladder, head and neck, gastric, lung, ovarian, prostate, thyroid, non-small-cell lung, chronic lymphocytic leukemia, mesothelioma, melanoma, pancreatic adenocarcinoma, basal cell carcinoma, osteosarcoma, hepatocellular carcinoma, Wilm's tumor or medulloblastoma, wherein the fibrotic disease is selected from pulmonary fibrosis, liver fibrosis, skin fibrosis or renal fibrosis, and wherein the metabolic disease is diabetic retinopathy.

15 . The use of claim 13 wherein the disease or condition is a cancer that is characterized by high Wnt activity.

16 . A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt, solvate or prodrug thereof.

17 . The pharmaceutical composition of claim 16 , wherein the pharmaceutical composition further comprises one or more pharmaceutically acceptable carriers, diluents or adjuvants.

Assignees

• Agency Science Tech & Res

Inventors

• Blanchard Stephanie Eliane

Classifications

• A61P35/00

  Antineoplastic agents · CPC title

• C07D473/08 Primary

  with methyl radicals in positions 1 and 3, e.g. theophylline · CPC title

• C07D487/04 Primary

  Ortho-condensed systems · CPC title

• A61K31/522

  having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title