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Histone deacetylase inhibitors

An alkyl and alkenyl technology, applied in the field of compounds that inhibit histone deacetylase enzymes, can solve the problem of less specific isomer effect

Inactive Publication Date: 2019-12-13
BIOMARIN PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although studies have shown that treatment with non-specific HDAC inhibitors such as sodium butyrate can lead to long-term memory formation (Stefanko, D.P. et al., Proc Natl Acad Sci USA 1069447 (2009)), the Little is known about the role of isomers

Method used

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[0111] The synthesis of specific compounds was carried out as follows.

[0112] abbreviation

[0113]

[0114]

[0115] Synthetic scheme of compound 485 and compound 486:

[0116]

[0117] Step 1: Synthesis of tert-butyl 4-(4-(methoxycarbonyl)benzyl)-1,4-diazepane-1-carboxylate (3): To compound 1 (1.92g, 1.1eq .) and a stirred solution of compound 2 (2 g, 1 eq.) in ACN (20 mL) was added potassium carbonate (1.8 g, 1.5 eq.). The reaction mixture was stirred at room temperature for 16 h. The reaction was monitored for completion by TLC. The reaction mixture was diluted with water and extracted with ethyl acetate. The combined organic extracts were washed with water, brine, and washed with anhydrous Na2 SO 4 Drying, filtration and concentration under reduced pressure afforded the title compound 3 which was used in the next step without further purification.

[0118] Step 2: Synthesis of 4-((1,4-diazepan-1-yl)methyl)benzoic acid methyl ester hydrochloride (4): at 0°...

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Abstract

Provided herein are compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (e.g., HDAC1, HDAC2, and HDAC3).

Description

technical field [0001] The present invention provides compounds and methods for inhibiting histone deacetylase ("HDAC") enzymes (eg, HDAC1, HDAC2, and HDAC3). Background technique [0002] To date, 18 HDAC enzymes have been identified in humans and mounting evidence indicates that the 18 HDAC enzymes in humans are not functionally redundant. HDAC enzymes are divided into three main groups based on their homology to yeast proteins. Class I includes HDAC1, HDAC2, HDAC3 and HDAC8 and has homology to yeast RPD3. HDAC4, HDAC5, HDAC7 and HDAC9 belong to class IIa and have homology to yeast HDAC1. HDAC6 and HDAC10 contain two catalytic sites and are classified as class IIb, whereas HDAC11 has conserved residues in the catalytic center shared by both its class I and class II deacetylases and is placed in class IV. These HDAC enzymes contain zinc in their catalytic site and are activated by compounds similar to trichostatin A (TSA) and vorinostat (suberoylanilide hydroxamic acid (...

Claims

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Application Information

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IPC IPC(8): C07D223/04C07D241/04C07D243/08C07D487/10C07D205/04C07D498/10C07D211/12C07D211/14A61K31/553A61K31/4965A61K31/44A61K31/55A61K31/397A61K31/4427A61P25/00
CPCC07D223/04C07D241/04C07D243/08C07D487/10C07D205/04C07D498/10C07D211/12C07D211/14A61P21/00A61P25/00A61P25/02A61P25/14A61P25/28A61P29/00A61P3/00A61P31/00A61P43/00A61K31/55A61K31/397A61K31/407A61K31/438A61K31/44A61K31/4965A61K31/551A61K31/553C07D207/09C07D211/34C07D223/12C07D491/107
Inventor G·吕特克S·布哈格瓦特
Owner BIOMARIN PHARMA INC
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