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Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.


Compounds of formula (I): wherein X, Y, A_(1), A_(2), R_(a), R_(b), R_(c), R_(d), R_(3), R_(4), T and R_(5 )are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.


Compounds of formula (I): wherein R_(a), R_(b), R_(c), R_(d), R_(1), R_(2), R_(3), R_(4), R_(5), X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.


Grant
Agency: European Commission | Branch: H2020 | Program: MSCA-ITN-ETN | Phase: MSCA-ITN-2015-ETN | Award Amount: 3.84M | Year: 2016

The promise of more efficient lead discovery is fuelling the enthusiasm for fragment-based lead discovery (FBLD). In this approach, highly sensitive biochemical and biophysical screening technologies are being used to detect the low affinity binding of low molecular weight compounds (the so-called fragments) to protein targets that are involved in pathophysiological processes. By investigating the molecular interactions between fragment hit(s) and the target protein, a detailed understanding of the binding event is obtained. This enables the rational and efficient optimisation of the hit fragment. The optimised compounds represent high quality leads for drug development. The necessary FBLD technologies and approaches have emerged mainly from small and specialised biotech companies. At present, FBLD is being adopted throughout pharmaceutical sciences, including by pharmaceutical companies, SMEs and academic research groups. So far, the necessary training that is needed to obtain an holistic view of the possibilities and opportunities that FBLD provides is missing, most likely because the highly multidisciplinary nature of the FBLD work is difficult to capture within one (academic) institute. Therefore, we have established FragNet as a dedicated FBLD training network. The consortium consists of the most prominent pharmaceutical companies, biotech companies and academic groups that have jointly shaped the FBLD research area. FragNet is committed to train 15 ESRs in all facets of FBLD using the combined technologies, skills and knowledge. This will include both research (e.g., technologies on the interface of chemistry and biology) and transferable skill sets (e.g., writing, media training, entrepreneurship and thorough understanding of scientific knowledge transfer). This will enable the ESRs to excel in todays drug discovery and chemical biology programmes that are performed in public and private organisations in the pharmaceutical sciences.


Patent
H. Lundebck A S and Vernalis | Date: 2016-10-07

The present invention is directed to arylpyrrolopyridine derivatives of Formula A: The compounds are considered useful for the treatment of diseases associated with LRRK2 such as Lewy body dementia, Parkinsons disease or cancer.


Patent
Vernalis | Date: 2015-03-09

Compounds of formula (I) are inhibitors of fatty acid amide hydrolase, (FAAH), and which are useful in the treatment of diseases or medical conditions which benefit from inhibition of FAAH activity, such as anxiety, depression pain, inflammation, and eating, sleep, neurodegenerative and movement disorders: Wherein Ar^(1 )is optionally substituted phenyl or optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms; Ar^(2 )is optionally substituted phenyl, optionally substituted monocyclic heteroaryl having 5 or 6 ring atoms or optionally substituted fused bicyclic heteroaryl having 5 or 6 ring atoms in each fused ring; and Ar^(3 )is a divalent radical selected from the group consisting of optionally substituted phenylene and optionally substituted monocyclic heteroarylene radicals having 5 or 6 ring atoms.


Patent
Lundbeck and Vernalis | Date: 2016-03-16

The present invention is directed to aminopyridine derived compounds of formula (A) The compounds are considered useful for the treatment of diseases associated with LRRK2 such a Lewy body dementia, Parkinsons disease or cancer.


Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are. disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning.


Compounds of formula (I):_(1), R_(2), R_(3), R_(4), R_(5), R_(6), R_(7), R_(12), X, A and n are as defined in the description.


Patent
Les Laboratoires Servier and Vernalis | Date: 2015-07-13

Compounds of formula (I): wherein A_(1), A_(2), R_(a), R_(b), R_(c), R_(d), R_(3), R_(4), R_(5 )and T are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.

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