Inhibitory effect of low molecular weight compound on cancer and fibrosis

Patent metadata

Field	Value
Publication number	US-2021386747-A1
Application number	US-202117459117-A
Country	US
Kind code	A1
Filing date	Aug 27, 2021
Priority date	Mar 28, 2014
Publication date	Dec 16, 2021
Grant date	—

Abstract

A novel therapeutic drug for malignant tumors, cancer stem cells, or fibrosis is obtained. A therapeutic drug for malignant tumors or cancer stem cells is used that includes at least one compound selected from the group consisting of compounds represented by formulas (1), (2), and (5), a salt thereof, or a solvate thereof. Alternatively, a therapeutic drug for fibrosis can be used that includes at least one compound selected from the group consisting of compounds represented by formulas (1), (2), and (5), a salt thereof, or a solvate thereof.

First claim

1 - 9 . (canceled)

10 . A method of treating a liver malignant tumor, comprising the step of administering to a subject at least one compound selected from the group consisting of compounds represented by formulas (1), a salt thereof, or a solvate thereof:

wherein
R 1 , R 2 , and R 4 are the same or different and each represent H, halogen, nitro, cyano, OH, optionally substituted C 1-6 alkyl, optionally substituted C 2-6 alkenyl, optionally substituted C 1-6 alkoxy, aryl, or heteroaryl;
R 3 represents H, optionally substituted C 1-6 alkyl, or optionally substituted C 2-6 alkenyl;
m represents an integer of any of 1 to 4;
n is an integer of any of 1 to 3; and
p represents an integer of any of 1 to 5.

11 . The method of treating a liver malignant tumor according to claim 10 , wherein the R 1 , R 2 , and R 4 are the same or different and each represent H, halogen, nitro, cyano, OH, C 1-6 alkyl, C 1-6 halogenoalkyl, C 1-6 hydroxyalkyl, C 1-6 alkylamino, C 1-6 alkoxy, C 1-6 halogenoalkoxy, C 1-6 hydroxyalkoxy, or C 1-6 alkoxyamino, or C 1-6 alkoxy-substituted C 1-6 alkoxy, C 1-6 alkoxyphenyl-substituted C 1-6 alkoxy, (trialkylsiloxy) C 1-6 alkyl, or (alkyl diphenyl siloxy) C 1-6 alkyl; and
the R 3 are H.

12 . The method of treating a liver malignant tumor according to claim 10 , wherein in the formula (1),
the R 1 , R 2 , and R 3 are each H, the R 4 is at position 4 and represents H, F, Cl, nitro, OH, CH 2 OH, methoxy, methoxymethoxy, tert-butyl dimethyl siloxymethyl, or 4-methoxybenzyloxy.

13 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents H.

14 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents F.

15 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents Cl.

16 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents nitro.

17 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents OH.

18 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents CH 2 OH.

19 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents methoxy.

20 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents methoxymethoxy.

21 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents tert-butyl dimethyl siloxymethyl.

22 . The method of treating liver malignant tumor according to claim 12 , wherein R 4 represents 4-methoxybenzyloxy.

Assignees

• Nat Univ Corp Tottori Univ
• Kanoncure Inc

Inventors

• Shiota Goshi
• Itaba Noriko
• Kanki Keita
• Seto Kenzo
• Shimizu Hiroki
• Kouno Yohei
• Kunita Shinya
• Adumi Zyunya
• Sakabe Tomohiko
• Abe Kenichiro
• Morimoto Minoru
• Oka Hiroyuki

Classifications

• A61K31/166

  having the carbon of a carboxamide group directly attached to the aromatic ring, e.g. procainamide, procarbazine, metoclopramide, labetalol · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K31/519 Primary

  ortho- or peri-condensed with heterocyclic rings · CPC title

• A61K31/09

  having two or more such linkages · CPC title