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3D Carbon Based Tricyclic Spiropentane Building Blocks for Pharmaceutical Applications

Objective

Over the last decades there has been a growing demand to leave the flat land of drug design and to access the three-dimensional (3D) space by embedding 3D scaffolds into drug molecules. 3D building blocks such as cubanes, bicyclo[2.2.2]octanes or bicyclo[1.1.1]pentanes have been well explored, are commercially available and are commonly found in the patent literature of pharmaceuticals and agrochemicals. Substituting phenyl groups by 3D building blocks (bioisosters) can increase pharmacokinetics such as aqueous solubility or improves metabolic stability. SPIROPENT will establish novel building blocks based on the spiro[2.2]pentane core. Due to the intrinsic challenges associated with spiro[2.2]pentanes such as their complex stereochemistry, as well step-intense synthesis, such building blocks are so far not well explored, particularly as linker elements in pharmaceuticals. This proposal aims to embed the spiro[2.2]pentanes into an additional cycle yielding novel tricyclic, rigid, chiral and three-dimensional building blocks which will solve the typical problems associated with spiro[2.2]pentanes and represents a terra incognita for drug design. We will establish a new synthetic access based on single C-atom transfer which we have recently pioneered. SPIROPENT will explore and scale up the synthesis of the new tricyclic building blocks as well as incorporate them into biological targets with the overarching aim of commercialization.

Fields of science (EuroSciVoc)

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Programme(s)

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Topic(s)

Calls for proposals are divided into topics. A topic defines a specific subject or area for which applicants can submit proposals. The description of a topic comprises its specific scope and the expected impact of the funded project.

Funding Scheme

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HORIZON-ERC-POC - HORIZON ERC Proof of Concept Grants

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Call for proposal

Procedure for inviting applicants to submit project proposals, with the aim of receiving EU funding.

(opens in new window) ERC-2026-POC

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Host institution

TECHNISCHE UNIVERSITAT DORTMUND
Net EU contribution

Net EU financial contribution. The sum of money that the participant receives, deducted by the EU contribution to its linked third party. It considers the distribution of the EU financial contribution between direct beneficiaries of the project and other types of participants, like third-party participants.

€ 150 000,00
Address
AUGUST SCHMIDT STRASSE 4
44227 Dortmund
Germany

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Region
Nordrhein-Westfalen Arnsberg Dortmund, Kreisfreie Stadt
Activity type
Higher or Secondary Education Establishments
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Total cost

The total costs incurred by this organisation to participate in the project, including direct and indirect costs. This amount is a subset of the overall project budget.

No data

Beneficiaries (1)