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Acid-labile trigger units

A technology of heteroatoms and compounds, applied in the field of acid instability triggering subunits, can solve problems such as unsuitable cytotoxic drugs

Inactive Publication Date: 2012-11-28
KTB TUMORFORSCHUNGS GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, this technique is not applicable to most cytotoxic drugs that contain hydroxyl and / or amino moieties as the only reactive groups

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment

[0091] by Figure 4 The two steps shown carry out the synthesis of the model compounds.

[0092] General procedure for the preparation of 4-(benzylideneamino)benzyl alcohol

[0093] The corresponding benzaldehyde derivative (4.86 mmol) and 5 μL (90 μmol) of acetic acid were added to a stirred suspension of 200 mg (1.62 mmol) of 4-aminobenzyl alcohol in 20 mL of benzene. The mixture was heated to reflux for 17 hours and the water formed was removed using a Dean-Stark apparatus. After cooling to room temperature, the solvent was removed under reduced pressure and the product was crystallized from a mixture of n-hexane and ethyl acetate at -20°C.

[0094] 4-(Benzylideneamino)benzyl alcohol (1).

[0095] The pure product was obtained as a yellow solid in a yield of 252 mg (77%): 1 H-NMR (400.1MHz, DMSO-d 6 ): δ=4.52 (d, J=5.6Hz, 2H, C H 2 ), 5.21(t, J=5.6Hz, 1H, O H ), 7.24-7.26 (m, 2H, Ar- H ), 7.36-7.38 (m, 2H, Ar- H ), 7.53-7.54 (m, 3H, Ar- H ), 7.93-7.95 (m, 2H, A...

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Abstract

The present invention relates to a compound comprising an imine bond as an acid- labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.

Description

technical field [0001] The present invention relates to compounds comprising an imine bond as an acid-labile triggering subgroup, the use of the imine bond as an acid-labile triggering subgroup, a method for breaking an imine bond in said compound and a compound comprising said compound pharmaceutical composition. Background technique [0002] Most drugs currently used are small molecules, ie compounds with low molecular weight and exhibit high plasma clearance when systemically administered to patients. Furthermore, said low molecular weight compounds show a high tendency to penetrate body tissues by diffusion, resulting in a homogeneous biodistribution. These are the two main reasons why only a small amount of the drug reaches the site of action, and due to distribution throughout the healthy tissues of the body, the drug may cause unwanted side effects. These disadvantages are of particular concern for those drugs with high cytotoxic potential, such as cytotoxic agents,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D249/04C07D311/16C07D403/12C07D405/12C07D473/00C07D491/147C07H15/24A61K31/53A61K31/352A61P35/00A61K47/48
CPCC07H15/24C07D403/12A61K47/48061C07D491/22A61K47/48215C07D405/12C07D473/38A61K47/60A61K47/545A61P29/00A61P31/00A61P31/04A61P31/12A61P35/00A61P37/00A61P37/02
Inventor A·瓦尔内克I·穆勒
Owner KTB TUMORFORSCHUNGS GMBH
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