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DONEPEZIL: AD drug Molecule

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20 years' experience in driving medicinal chemistry

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Prestwick Chemical: Donepezil

Donepezil hydrochloride is the most prescribed drug for treatment of memory dysfunction. It is indicated for the symptomatic treatment of mild to moderate Alzheimer's disease. Marketed under the trade name Aricept by its developer Eisai and partner Pfizer, the molecule is a racemate mixture.


Prestwick Chemical: DONEPEZIL 3D
Prestwick Chemical

PRESTWICK CHEMICAL has 20 years' experience in driving medicinal chemistry, allowing us to provide to our customers high quality compounds. We offer tailor-made solutions from hit discovery to preclinical candidate selection.



Prestwick Chemical: DONEPEZIL crotonisation reaction
The original synthesis main step is a crotonisation reaction between 5,6-dimethoxy-1-indanone and 1-benzyl-4-formylpiperidine in the presence of a strong base, followed by reduction of the double bond.



T-Maze NEUROFT


Reversion of the cognitive deficit by donepezil in the mice as assessed by the T-maze continuous and spontaneous alternation task (graph by the courtesy of NEUROFIT, our in-vivo pharmacology partner).


Please contact us if you need more information or if you have any R&D project that you wish to happen.



Donepezil hydrochloride is part of the Prestwick Chemical Library®, a collection of 1280 off-patent approved drug molecules selected for their high chemical and pharmacological diversity.

F2L Library

Enhanced drug-likeness properties by combining fragments of approved drugs

High level of uniqueness

Prestwick Chemical: Core set of 480 fragments
F2L Library

Prestwick Chemical: Core set of 480 fragments
Prestwick Chemical
At Prestwick Chemical, we believe that upcoming and past successes are strongly correlated and share Sir James Black’s statement when he says that " the most fruitful basis for the discovery of a new drug is to start with an old drug ". It is in this way that our medicinal chemists designed in a two-step process the F2L Library, an innovative screening library arising from the combination of fragments of approved drugs.

To discover examples of fragment combination

To discover examples of fragment combination, click here

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Enhanced drug-likeness properties by combining fragments of approved drugs

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Good coverage of the lead-like space

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High level of uniqueness

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Valuable starting points for medchem optimization


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Drug-Fragment Library

To accelerate hit discovery and meet researchers' expectations, Prestwick Chemical is proud to offer a library of 480 small molecules (MW<300) pre-plated in deuterated DMSO solution at 100 mM.

Fragment-based drug discovery

Prestwick Chemical is proud to offer a library of 480 small molecules
Drug-Fragment Library

Prestwick Chemical is proud to offer a library of 480 small molecules
Prestwick Chemical is proud to offer a library of 480 small molecules
Fragment-based drug discovery (FBDD) has emerged as a highly successful way to identify quality leads and has yielded over 30 clinical drug candidates and 3 approved drugs.
NMR-based methods are ideally suited for fragment-based screening and allow detection of millimolar hits for challenging targets.

To accelerate hit discovery and meet researchers' expectations, Prestwick Chemical is proud to offer a library of 480 small molecules (MW<300) pre-plated in deuterated DMSO solution at 100 mM.



Fragment key features

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Fragments of approved drugs
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Suitable for target binding
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Appropriate for chemical expansion
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Synthetically accessible

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Prestwick Chemical is proud to offer a library of 480 small molecules


Other formats: DMSO solution (up to 100 mM) or undissolved (from 10 mg)
Cherry-picking available


MEDICINAL CHEMISTRY SERVICES

In a multidisciplinary environment, our medicinal chemistry experts help selecting the most promising scaffolds for progression into lead optimization in order to provide a suitable compound for pre-clinical phase.

HIT-TO-LEAD & LEAD OPTIMIZATION PROGRAMS

Prestwick Chemical
Medicinal Chemistry
Services

Prestwick Chemical
Tailored-made MedChem projects
Hit-to-lead programs: In a multidisciplinary environment, our medicinal chemistry experts help selecting the most promising scaffolds for progression into lead optimization.

Lead optimization programs: Starting from a validated lead, our medicinal chemists initiate the optimization process in order to provide a suitable compound for pre-clinical phase.


Prestwick Chemical

Customer oriented - FTE based packages

Services
Essential
Premium
Full
premium

Chemistry
+
+
+

MedChem Design
+
+

CADD
+
+

ADME-PK
+



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CASE STUDY
SUCCESS STORY


HIT DISCOVERY

This service solves the difficulty of finding a new starting point and allows customers to save time and money by avoiding medium or high-throughput screening (HTS).

PHARMACOPHORE MODELS AND VIRTUAL HIT LISTS

Prestwick Chemical
HIT DISCOVERY

Prestwick Chemical - Hit discovery
Prestwick Chemical - Hit discovery
Prestwick Chemical proposes in silico solutions to identify new hits for a biological target or a specific mechanism. Pharmacophore-based virtual screenings performed on millions of compounds allow rapid identification of virtual hits that can be confirmed experimentally on the biological target. This service solves the difficulty of finding a new starting point and allows customers to save time and money by avoiding medium or high-throughput screening (HTS).

Prestwick Chemical - Hit discovery



Prestwick Chemical DELIVERABLE:

project report, pharmacophore
models and virtual hit lists

Prestwick Chemical OVERALL DURATION:

8 weeks

Request a quote
SERVICE DESCRIPTION

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Literature/project search and analysis

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Pharmacophore model generation

Read more Virtual screening with several compound databases (10+ M cpds)

Read more Virtual hit analysis and selection for biochemical evaluation

PEPTIDIC MACROCYCLE LIBRARY

Prestwick and GENEPEP propose a library of high purity 400 short macrocyclic peptides designed with a mix of natural and non-natural amino acids and different types of cyclization (disulfide, lactam, triazole).

A COLLECTION OF 400 SHORT PEPTIDIC MACROCYCLES !

Prestwick Peptidic Macrocycle Library
Prestwick Peptidic
Macrocycle Library

Prestwick Peptidic Macrocycle Library
Prestwick Peptidic Macrocycle Library
PRESTWICK CHEMICAL / GENEPEP propose a library of 400 high purity short macrocyclic peptides designed with a mix of natural and non-natural amino acids and different types of cyclization (disulfide, lactam, triazole). This library is a great starting point to identify enzyme inhibitors, agonists or antagonists of GPCRs and protein-protein interaction disruptors (inhibitors).

Core set of 480 fragments



Prestwick Peptidic Macrocycle Library

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Short (5 amino acids), chemically synthesized macrocyclic peptides

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17 or 20-membered ring

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Different cyclization motifs (disulfide, lactam, triazole)

Read more Constrained, stabilized peptide sequences with exposed side chains

Read more Conveniently prepared for multiple screenings

Read more Lyophilized form (0.1µmol) or powder form (on request)

POST HTS SERVICES

After screening, the question to be addressed is: how to select the right hit to enter hit to lead phase? This post-screening phase is crucial and requires expert eyes to shorten time and cost. We offer to support you in this key stage through turnkey services.

YOU HAVE A HIT LIST ? WE CAN ASSIST YOU !

Prestwick Chemical: POST HTS SERVICES
POST HTS SERVICES

Prestwick Chemical: POST HTS SERVICES

Prestwick Chemical: POST HTS SERVICES
YOU HAVE A HIT LIST ?

WE CAN ASSIST YOU !
Prestwick Chemical: POST HTS SERVICES

After screening, the question to be addressed is: how to select the right hit to enter hit to lead phase? This post-screening phase is crucial and requires expert eyes to shorten time and cost. We offer to support you in this key stage through turnkey services.


HIT CONFIRMATION

Based on customer experimental data, our medicinal chemists perform:
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Analysis of customer screening hits
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Multiparameter selection of hit series of
interest
Read more Search and selection of structural analogues
Read more Purchase, QC for screening assay

Prestwick Chemical DELIVERABLE:

10-50 analogues

Prestwick Chemical OVERALL DURATION:

1-4 months

Request a quote




HIT / SERIES VALIDATION

Based on primary activity results and supplementary data, our medicinal chemists design and synthesize close/new analogues
Read more SAR-driven design with IP consideration and
chemical tractability
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Iterative cycles including design and synthesis
of analogues
Read more Early ADME characterization for selection
(optional)

Prestwick Chemical DELIVERABLE:

15-40 analogues

Prestwick Chemical OVERALL DURATION:

3-4 months

Request a quote



Prestwick Chemical: Events

GPCR Drug Library

Supporting and accelerating GPCR Drug Discovery, we are proud to launch the Prestwick GPCR Drug Library, a unique collection of 265 approved drugs targeting primarily G protein coupled receptors.

Ready for screening or customizable.

Prestwick Chemical: Core set of 480 fragments
GPCR Drug Library

Prestwick Chemical: Core set of 480 fragments
Prestwick Chemical
Recent breakthroughs and collaborative works have significantly contributed to GPCRs understanding and increased focus on this target. Supporting and accelerating GPCR Drug Discovery, we are proud to launch the Prestwick GPCR Drug Library, a unique collection of 265 approved drugs targeting primarily G protein coupled receptors.

Prestwick Chemical: Core set of 480 fragments
Read more Approved off-patent drugs

Read more Small molecules

Read more High chemical diversity

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High target diversity

Read more Applications:
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deorphanization
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repurposing
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assay validation

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Drug-Fragment Library

Prestwick Chemical medicinal chemists designed a unique collection of 1464 small molecules (MW<300) arising from the smart fragmentation of 1500 approved drugs (up to year 2016)

- High-quality hit by using drug fragments
- Rapid follow-up on primary hits
- 818 molecules (56%) are exclusive

Prestwick Chemical: Core set of 480 fragments
Drug-Fragment Library

Prestwick Chemical: Core set of 480 fragments
Prestwick Chemical
Prestwick Chemical medicinal chemists designed a unique collection of 1464 small molecules (MW<300) arising from the smart fragmentation of 1500 approved drugs
(up to year 2016)

Core set of 480 fragments


Read more

Order now

Prestwick Chemical: Core set of 480 fragments
High-quality hit by using drug fragments
Prestwick Chemical: Core set of 480 fragments
Rapid follow-up on primary hits
Prestwick Chemical: Core set of 480 fragments
818 molecules (56%) are exclusive



18+ YEARS OF SUCCESS STORIES

Prestwick Chemical is a contract research organization (CRO) supporting pharmaceutical and biotechnology companies, research institutes and academic groups. We provide libraries and services for the early stage of the drug discovery.


1 DRUG ON THE MARKET
in veterinary oncology; developed by Prestwick for a biotech client

10 MOLECULES IN CLINICAL PHASE
 in varied therapeutical domains

40+ SUCCESSFUL PROJECTS
14 000+ molecules synthesized and delvered


Full medicinal chemistry services from target analysis to pre- clinical candidate keeping customer satisfaction at the core of our concerns

Teams of experienced chemists with strong scientific background strive towards accelerating your drug discovery workflow. Objectives are usually reached in 12-18 months (from Hit to Candidate)

All projects are supported by specific skills in molecular modeling, distinctive know-how in organic and medicinal chemistry. ADME-Tox profile and PK issues are considered early in the project workflow


A Unique Service

From 2 FTEs with 1 senior PhD as dedicated project leader

IP: delivery of Freedom-to-Operate compounds

Iterative cycles adapting to customer's biological data

Biweekly reports followed by conference call

FTE based contracts : All included: QC, chemicals...


Three-level Package

Services
Essential
package
Premium
package
Full-
Premium
package

Synthetic Chemistry
Yes
Yes
Yes

Med Chem Design
Yes
Yes

CADD
Yes
Yes

ADME-PK
Yes






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45
PROJECTS

11 compounds
IN CLINICAL PHASE

1 COMPOUND
ON THE MARKET

625 Clients
FOR THE LIBRARIES

Free and rapid quotation (price, lead time) under request