Histone deacetylase inhibtors

A compound, cycloalkyl technology, applied in anti-inflammatory agents, drug combinations, organic chemistry, etc., can solve the problem of little understanding of the role of specific isoforms

Inactive Publication Date: 2018-04-17
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 nonspecific HDAC inhibitors, such as sodium butyrate, can induce long-term memory formation (Stefanko, D.P. et al., PNAS USA 1069447 (2009)), the role of specific isoforms is poorly understood few

Method used

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  • Histone deacetylase inhibtors
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[0140] General procedure for compounds 1-6: General procedure for Boc deprotection : To a stirred solution of tert-butoxycarbonyl (Boc)-protected compound (1 eq) in dioxane:methanol (4:1, 5 vol) was added 4N HCl in dioxane (3 vol) and heated at room temperature The reaction mixture was stirred under pressure. Reaction progress was monitored by TLC. After completion, the reaction mixture was evaporated to dryness (if the compound precipitated, it was then filtered and further purified). The crude product was purified by trituration with ether / pentane / MTBE or by preparative HPLC to afford the title compound.

[0141] General procedure for N-alkylation : Procedure A: To a stirred solution of the amine substrate (1 eq) and cesium carbonate / potassium carbonate (3 eq) in DMF (10 vol) was added the corresponding alkyl halide (1.1 eq). The reaction mixture was heated at 80 °C for 5h to 30h. Reaction progress was monitored by TLC. After completion, the reaction mixture was pour...

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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] Provided herein are compounds and methods for inhibiting histone deacetylases ("HDACs") (eg, HDAC1, HDAC2, and HDAC3). Background technique [0002] So far, 18 HDAC enzymes have been identified in humans and there is increasing evidence 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 is homologous to yeast RPD3. HDAC4, HDAC5, HDAC7 and HDAC9 belong to class IIa and are homologous to yeast HDAC1. HDAC6 and HDAC10 contain two catalytic sites and are classified into class IIb, whereas HDAC11 has conserved residues at its catalytic center shared by class I and class II deacetylases and is placed in class IV. These HDAC enzymes contain zinc at their catalytic site and are activated by compounds such as trichostatin A (TSA) and vorinostat [suberoylanilide hydroxamic acid (SAHA)] to suppress. Cla...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D223/08A61K31/397A61K31/40A61K31/44A61K31/4409A61K31/46A61K31/55C07D223/12C07D451/04C07D451/06C07D205/04C07D207/12C07D207/14C07D211/46C07D211/58
CPCC07D223/08C07D223/12C07D451/04C07D451/06C07D205/04C07D207/12C07D207/14C07D211/58C07D211/46C07D451/02A61P21/00A61P25/00A61P25/02A61P25/14A61P25/28A61P25/30A61P29/00A61P31/00A61P35/00A61P43/00A61K31/40A61K31/44A61K31/4409A61K31/46A61K31/55C07D211/54
Inventor S·布哈格瓦特G·吕特克A·布里奇斯
Owner BIOMARIN PHARMA INC
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