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Heparan sulfate glycomimetic compounds and their pharmaceutical and cosmeceutical uses

一种化合物、酰基的技术，应用在硫酸化树状化合物领域，能够解决合成过程长等问题

Active Publication Date: 2019-12-24
VICTORIA LINK LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method reduces the number of reaction steps compared with other methods for the synthesis of heparan sulfate oligosaccharides, the synthesis process is still very long.

Method used

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  • Heparan sulfate glycomimetic compounds and their pharmaceutical and cosmeceutical uses
  • Heparan sulfate glycomimetic compounds and their pharmaceutical and cosmeceutical uses
  • Heparan sulfate glycomimetic compounds and their pharmaceutical and cosmeceutical uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 6

[0245] Example 6 shows that at least one compound of the present invention, compound 17c, is effective in the treatment of myeloma in mice, which indicates that this compound and structurally related compounds have therapeutic potential for myeloma and other potential cancers in humans.

[0246] Without being bound by theory, applicants hypothesize that the compounds of the invention may achieve an "aggregation effect" by utilizing multiple copies of sulfated sugar fragments in each dendrimer structure. This aggregation effect is advantageous because the repeating individual subunit structures can enhance the normally weaker interactions of the individual subunit structures in sulfated carbohydrates.

[0247] Cosmeceutical use

[0248] In addition to the aforementioned therapeutic uses, the compounds of the present invention are also believed to have potential cosmeceutical uses.

[0249] A reduction in fibrillar type I collagen is a hallmark of age-related or "unhealthy" ski...

Embodiment 11

[0253] Example 11 shows that compounds 17c and 17d are also potent inhibitors of testicular hyaluronidase.

[0254] Formulation and Administration

[0255] The compounds of the present invention can be administered to patients by a variety of routes including orally, parenterally, by inhalation spray, topically, rectally, nasally, buccally or via implanted reservoirs. The compounds can also be administered by intracerebral, intracerebroventricular or intrathecal delivery. For parenteral administration, it can be intravenous, intraarterial, intramuscular or subcutaneous injection.

[0256] The dosage of a compound of the invention administered to a patient will vary widely depending on the condition of the patient and the nature and extent of the condition being treated. Usually, the dosage for an adult is about 0.01 μg / kg to about 1 g / kg, preferably about 0.01 mg / kg to about 100 mg / kg. The specific dosage required for any particular patient will depend on factors such as th...

Embodiment 1

[0305] Embodiment 1: the synthesis of tetrasuccinimide ester

[0306] The tetrasuccinimide ester was synthesized according to Scheme 7 below, which is described in WO 2014 / 084744.

[0307] Option 7

[0308]

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PUM

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Abstract

The invention relates to dendritic compounds, the use of these compounds as pharmaceuticals, pharmaceutical and cosmeceutical compositions containing the compounds, and methods of treating cancer, inflammation, diabetic nephropathy, neurodegenerative disorders, Niemann-Pick Type C disease, or dermatological conditions.

Description

[0001] field of invention [0002] The present invention generally relates to sulfated dendrimers mimicking heparan sulfate, the use of these compounds as pharmaceuticals and cosmetics, pharmaceutical or cosmeceutical compositions comprising the compounds, methods of preparing the compounds, and methods of treating various diseases or conditions. The invention relates in particular to the treatment or prevention of cancer, inflammation, diabetic nephropathy, neurodegenerative diseases, Niemann-Pick disease type C, and to some cosmeceutical and dermatological uses. Background technique [0003] Heparanase is an endo-β-D-glucuronidase that degrades the heparan sulfate glycosaminoglycan side chains of proteoglycans in the extracellular matrix and basement membrane. Heparanase regulates glycan aggregation, shedding, and mitogen binding. The enzymatic activity of heparanase is known to be important in promoting tumor angiogenesis, primary tumor growth, invasion and metastasis. He...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/04C07H15/08A61K31/7004A61K31/7016A61K31/7028A61P25/28A61P17/00A61P35/00
CPCC07H15/04C07H15/08A61P25/28A61P35/00A61P17/00A61K8/602A61K8/608A61Q19/08
Inventor 杰里米.E.特恩布尔A.芒卡西P.C.泰勒O.V.朱布科娃
Owner VICTORIA LINK LTD
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