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Stat3 inhibitors

A CF3, compound technology, applied in the field of pharmacy

Pending Publication Date: 2021-02-12
特维迪疗法公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

STAT3 in three cell lineages, myeloid cells, intestinal epithelial cells, and T cells, has been shown to contribute to colitis in mice and humans (Takeda K, Clausen BE, Kaisho T et al., "In macrophages and neutrophils "Enhanced Th1 activity and development of chronic enterocolitis in mice devoid of Stat3 in macrophages and neutrophils", IMMUNITY 1999,10:39-49; Atreya R, Mudter J, Finotto S, et al., "Blockade of interleukin 6 trans-signaling in chronic intestinal inflammation suppresses T cell resistance to apoptosis: in vivo evidence in Crohn's disease and experimental colitis" (Blockade of interleukin6trans signaling suppresses T-cell resistance against apoptosis in chronic intestinal inflammation: evidence incrohn disease and experimental colitis in vivo), NAT MED 2000, 6:583-8; SuzukiA, Hanada T, Mitsuyama K et al., "CIS3 / SOCS3 / SSI3 plays a negative regulatory role in STAT3 activation and intestinal inflammation" (CIS3 / SOCS3 / SSI3 plays a negative regulatory role in STAT3 activation and intestinal inflammation), J.EXP.MED.2001,193:471-81), but has the opposite Effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0356] Example 1. Synthesis of compounds of formula III and compounds of formula IIIx

[0357] Step 1: Formation of sulfonylamino-naphthol

[0358]

[0359] Step 1 is the reaction of 4-methoxybenzenesulfonyl chloride (1) and 4-amino-1-naphthol HCl (2) in the presence of sodium acetate to produce sulfonylamino-naphthol (3). To a 5 L round bottom flask with mechanical stirring was added 2 (139.19 g, 694 mmol) and water (2.0 L). To the stirred suspension was added sodium acetate (176.12 g, 2.13 mol) and 1 (177.52 g, 816 mmol) using a further water wheel (800 mL). The reaction was heated at 85°C by an electric mantel and the temperature was monitored using a calibrated thermocouple. The reaction was monitored by TLC and cooled after 2 h at set temperature. The purple precipitate formed during the reaction was filtered off, washed with water (1400 mL, in steps), and dried in a heated (55 °C) vacuum oven under a nitrogen purge for 18 h. The purple intermediate 3 (223.78 g, 95...

Embodiment 5

[0373] Example 5. STAT3 Inhibition ICs of Compounds of Formula IIIx and Compounds of Formula III 50

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Abstract

Compounds as STAT3 inhibitors are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing conditions such as cancer, chronic inflammation, and fibrosis using the same, are described.

Description

[0001] Cross References to Related Applications [0002] This application claims the benefit of and priority to U.S. Provisional Application No. 62 / 659,872, filed April 19, 2018, and U.S. Provisional Application No. 62 / 793,491, filed January 17, 2019, the contents of which are incorporated by reference in their entirety Incorporated into this article. [0003] incorporated by reference [0004] All patents, patent applications, and publications cited herein are hereby incorporated by reference in their entirety in order to more fully describe the state of the art as of now known to those skilled in the art in Japan on the inventions described herein. technical field [0005] The present invention relates generally to the field of pharmacy. More specifically, the invention relates to compounds and compositions useful as medicaments for the inhibition of STAT3. More specifically, the invention relates to compounds and their use in methods for the treatment of disorders such a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/18C07C311/21
CPCC07C311/29A61K31/18A61P11/00A61P25/00A61P31/12A61P35/02A61P37/08A61P43/00C07C2602/04C07C303/40
Inventor 索非亚·德亚加瓦尔·维德W·E·布塔W·R·小坎特雷尔大卫·约翰·泰迪
Owner 特维迪疗法公司