Harlow, United Kingdom
Harlow, United Kingdom

Time filter

Source Type

Namoto K.,Novartis | Sirockin F.,Novartis | Ostermann N.,Novartis | Gessier F.,Novartis | And 12 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

The successful launches of dipeptidyl peptidase IV (DPP IV) inhibitors as oral anti-diabetics warrant and spur the further quest for additional chemical entities in this promising class of therapeutics. Numerous pharmaceutical companies have pursued their proprietary candidates towards the clinic, resulting in a large body of published chemical structures associated with DPP IV. Herein, we report the discovery of a novel chemotype for DPP IV inhibition based on the C-(1-aryl-cyclohexyl)-methylamine scaffold and its optimization to compounds which selectively inhibit DPP IV at low-nM potency and exhibit an excellent oral pharmacokinetic profile in the rat. © 2014 Elsevier Ltd. All rights reserved. © 2014 Elsevier Ltd. All rights reserved.


Sutton J.M.,Argenta Discovery 2009 Ltd | Clark D.E.,Argenta Discovery 2009 Ltd | Dunsdon S.J.,Argenta Discovery 2009 Ltd | Fenton G.,Argenta Discovery 2009 Ltd | And 17 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

Novel deazaxanthine-based DPP-4 inhibitors have been identified that are potent (IC 50 <10 nM) and highly selective versus other dipeptidyl peptidases. Their synthesis and SAR are reported, along with initial efforts to improve the PK profile through decoration of the deazaxanthine core. Optimisation of compound 3a resulted in the identification of compound (S)-4i, which displayed an improved in vitro and ADME profile. Further enhancements to the PK profile were possible by changing from the deazahypoxanthine to the deazaxanthine template, culminating in compound 12g, which displayed good ex vivo DPP-4 inhibition and a superior PK profile in rat, suggestive of once daily dosing in man. © 2011 Elsevier Ltd. All rights reserved.


Trademark
Argenta Discovery 2009 Ltd | Date: 2013-06-03

Chemicals, chemical compounds and fragments used in the pharmaceutical and biotechnology industries as well as pharmaceutical, biotechnology, and academic scientific research; chemicals, chemical compounds and chemical fragments organized into libraries for use in the pharmaceutical and biotechnology industries as well as pharmaceutical, biotechnology, and academic scientific research; all the above expressly excluding any product related to the banking or financial sector.


PubMed | Argenta Discovery 2009 Ltd
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2012

Novel deazaxanthine-based DPP-4 inhibitors have been identified that are potent (IC(50) <10nM) and highly selective versus other dipeptidyl peptidases. Their synthesis and SAR are reported, along with initial efforts to improve the PK profile through decoration of the deazaxanthine core. Optimisation of compound 3a resulted in the identification of compound (S)-4i, which displayed an improved in vitro and ADME profile. Further enhancements to the PK profile were possible by changing from the deazahypoxanthine to the deazaxanthine template, culminating in compound 12g, which displayed good ex vivo DPP-4 inhibition and a superior PK profile in rat, suggestive of once daily dosing in man.


Trademark
Argenta Discovery 2009 Ltd | Date: 2012-12-11

Printed matter, namely, manuals and guides in the fields of chemistry, medicinal chemistry, biochemistry, chemical analysis, biotechnology, drug discovery and drug development; printed reports featuring dossiers in the fields of chemistry, medicinal chemistry, biochemistry, chemical analysis, biotechnology drug discovery and drug development. Providing medical and scientific research, and product design and development, all in the fields of pharmaceutical and healthcare products; reviewing standards and practices to assure compliance with laws and regulations in the fields of pharmaceutical and healthcare products; scientific research services, biological and chemical research and analysis services; drug discovery services, namely, pharmaceutical drug development services, medicinal and synthetic chemical research and development services; chemical compound and chemical compound library research and development services; pharmaceutical research and development, namely, provision of screening drug targets, automated screening of compounds, assay development and screening services for developing protocols and tests to qualitatively or quantitatively measure drug activity; research services in the fields of computation chemistry, informatics services including chemo- and bio-informatics and molecular informatics, and combinatorial chemistry; scientific analysis, namely, scientific data interpretation services.


Trademark
Argenta Discovery 2009 Ltd | Date: 2012-12-11

Printed matter, namely, manuals and guides in the fields of chemistry, medicinal chemistry, biochemistry, chemical analysis, biotechnology, drug discovery and drug development; printed reports featuring dossiers in the fields of chemistry, medicinal chemistry, biochemistry, chemical analysis, biotechnology drug discovery and drug development. Providing medical and scientific research, and product design and development, all in the fields of pharmaceutical and healthcare products; reviewing standards and practices to assure compliance with laws and regulations in the fields of pharmaceutical and healthcare products; scientific research services, biological and chemical research and analysis services; drug discovery services, namely, pharmaceutical drug development services, medicinal and synthetic chemical research and development services; chemical compound and chemical compound library research and development services; pharmaceutical research and development, namely, provision of screening drug targets, automated screening of compounds, assay development and screening services for developing protocols and tests to qualitatively or quantitatively measure drug activity; research services in the fields of computation chemistry, informatics services including chemo- and bio-informatics and molecular informatics, and combinatorial chemistry; scientific analysis, namely, scientific data interpretation services.

Loading Argenta Discovery 2009 Ltd collaborators
Loading Argenta Discovery 2009 Ltd collaborators