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Compounds for use in treating kidney disorders

A technology for compounds and kidney diseases, applied in active ingredients of heterocyclic compounds, drug combinations, organic chemistry, etc., can solve problems such as unavailable, unmet needs for new drugs, unpredictable therapeutic responses, etc.

Pending Publication Date: 2021-03-09
F HOFFMANN LA ROCHE & CO AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, many of these treatments are based on case series, are not supported by randomized studies, are often associated with serious side effects, and are not designed for a specific pathogenic mechanism
Furthermore, the response to these treatments is unpredictable
Therefore, currently available drugs do not provide a safe and effective treatment
More specifically, there is a long-felt unmet need for novel agents for the prophylaxis or treatment of patients with glomerular disorders and more generally chronic kidney disease

Method used

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  • Compounds for use in treating kidney disorders
  • Compounds for use in treating kidney disorders
  • Compounds for use in treating kidney disorders

Examples

Experimental program
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Effect test

example

[0131] Preparation of ABCA1 inducer compounds

[0132] Compound list:

[0133]

[0134] The above compounds and their synthesis methods have been described in WO2014 / 180741.

[0135] G (5-(3,4-dichloro-phenyl)-N-((1R,2R)-2-hydroxy-cyclohexyl)-6-(2,2,2-trifluoro-ethoxy)-nicotine Amide) compound preparation

[0136] The compound consists of 5-bromo-6-chloro-3-pyridinecarboxylic acid, 2,2,2-trifluoroethanol, (1R,2R)-2-amino-cyclohexanol and 3,4-dichlorophenylboronic acid according to WO Prepared by the steps of Example 3 in 2011 / 029827. MS463.079, 465.077(M+H) + .

[0137] A 6-(3,4-Dichlorophenyl)-N-[(1R,2R)-2-hydroxycyclohexyl]-5-(2,2,2-trifluoroethoxy)pyridine-2-carboxamide Compound preparation

[0138] Compound A was prepared according to the steps described in WO 2014 / 180741, the steps are as follows:

[0139] a) 6-chloro-2-(3,4-dichlorophenyl)-3-fluoropyridine

[0140] In a 100 mL four-necked flask, 2,6-dichloro-3-fluoropyridine (765 mg, 4.61 mmol, Eq: 1.00, ...

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Abstract

The present disclosure relates to ABCA1 inducer compounds for use in treating kidney disorders, and in particular, chronic kidney diseases, glomerular diseases or proteinuric kidney diseases such as Alport syndrome, focal segmental glomerulosclerosis, and diabetic kidney disease.

Description

technical field [0001] The present disclosure relates to ABCA1 inducer compounds for use in the treatment of renal disorders, in particular for the treatment of chronic kidney disease, glomerular disease or proteinuric nephropathy such as Alport syndrome, focal segmental glomerulosclerosis and diabetic nephropathy. Background technique [0002] Chronic kidney disease (CKD), leading to end-stage renal disease (ESRD) requiring dialysis or kidney transplantation, is a growing epidemic affecting millions of patients worldwide (Bello AK et al., JAMA, 317:1864, 2017 ). Although diabetes remains the most common cause of ESRD worldwide, other causes such as hypertension, cystic kidney disease, and glomerulonephritis contribute to a significant portion of the ESRD prevalence (USRDS database). Many of these conditions may present with proteinuria ranging from mild proteinuria to severe nephrotic range proteinuria, with severe proteinuria being a major risk factor for progression to E...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/422A61K31/4245A61K31/44A61K31/506A61P13/12
CPCA61K31/422A61K31/4245A61K31/44A61K31/506A61K45/06A61P13/12A61K9/0053A61K31/455C07D213/81A61K31/4412C07D213/82C07D401/12
Inventor 阿尔西亚·弗农尼
Owner F HOFFMANN LA ROCHE & CO AG
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