N-acyl-{4-[(4-aryl-phenyl)sulfonylmethyl]piperidine} compounds and their therapeutic use

A compound and solvate technology, applied in the field of therapeutic compounds, can solve problems affecting development, complexity of rodent toxicity assessment, etc.

Pending Publication Date: 2021-12-07
现代生物科学有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

This biarylsulfonamide metabolite can induce metabolism in rats, complicating the assessment of rodent toxicity and, in turn, potentially affecting the development of the compound for human use

Method used

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  • N-acyl-{4-[(4-aryl-phenyl)sulfonylmethyl]piperidine} compounds and their therapeutic use
  • N-acyl-{4-[(4-aryl-phenyl)sulfonylmethyl]piperidine} compounds and their therapeutic use
  • N-acyl-{4-[(4-aryl-phenyl)sulfonylmethyl]piperidine} compounds and their therapeutic use

Examples

Experimental program
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Embodiment approach

[0123] Some embodiments of the invention include the following:

[0124] (1) Compounds of the following formula:

[0125]

[0126] or a pharmaceutically acceptable salt or solvate thereof;

[0127] in:

[0128] -X= is independently -CH= or -N=;

[0129] "m" is independently 0, 1, 2 or 3;

[0130] each -R A independently -F, -Cl, -R AC ,-R AF or -CN;

[0131] -R AC Independently saturated linear or branched C 1-3 alkyl;

[0132] -R AF Independently saturated linear or branched C 1-3 Fluoroalkyl;

[0133] "n" is independently 0, 1 or 2;

[0134] each -R B independently -F, -Cl, -R BC ,-R BF or -CN;

[0135] -R BC Independently saturated linear or branched C 1-3 alkyl;

[0136] -R BF Independently saturated linear or branched C 1-3 Fluoroalkyl;

[0137] -R 1 independently -H or -R 1X ;

[0138] -R 1X Independently -F, -R 1C or -R 1F ;

[0139] -R 1C Independently saturated linear or branched C 1-3 alkyl;

[0140] -R 1F Independently saturated ...

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Abstract

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain N-acyl-{4-[(4-aryl- phenyl)sulfonylmethyl]piperidine} compounds of the following formula (collectively referred to herein as NASMP compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, e.g., multiple myeloma, diffuse large B-cell lymphoma, acute myeloid leukemia, eosinophilic leukemia, glioblastoma, melanoma, ovarian cancer, chemotherapy resistant cancer, radiation resistant cancer, inflammatory arthritis, rheumatoid arthritis, psoriatic arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus (SLE), lupus nephritis, asthma, chronic obstructive pulmonary disease (COPD), Hidradenitis suppurativa, autoimmune hepatitis, etc. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.

Description

[0001] related application [0002] This application relates to British (GB) patent application number 1905520.1 filed 18 April 2019, the contents of which are incorporated herein by reference in their entirety. technical field [0003] The present invention relates generally to the field of therapeutic compounds. More particularly, the present invention relates to certain N-acyl-{4-[(4-aryl-phenyl)sulfonylmethyl]piperidine} compounds (collectively referred to herein as NASMP compounds) which are useful, for example, in the treatment of Conditions (e.g., diseases) including, for example, multiple myeloma, diffuse large B-cell lymphoma, acute myelogenous leukemia, eosinophilic leukemia, glioblastoma, melanoma, ovarian cancer, chemotherapy-resistant cancer , radiation resistant cancer, inflammatory arthritis, rheumatoid arthritis, psoriatic arthritis, psoriasis, ulcerative colitis, Crohn's disease, systemic lupus erythematosus (SLE) , lupus nephritis, asthma, chronic obstructi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P35/00A61K31/445A61K31/4545A61P37/00C07D211/24C07D401/12
CPCC07D211/24C07D401/12A61P35/00A61P37/00A61K31/445A61P29/00A61P19/02C07D211/54
Inventor 利萨·帕特尔斯蒂芬·艾伦·史密斯斯蒂芬·保罗·科林伍德
Owner 现代生物科学有限公司
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