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Dive into the research topics where Tor Svensson is active.

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Featured researches published by Tor Svensson.


MedChemComm | 2013

Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity

William Mccoull; Peter Barton; Anders Broo; Alastair J. H. Brown; David S. Clarke; Gareth Coope; Robert D. M. Davies; Alexander G. Dossetter; Elizabeth E. Kelly; Laurent Knerr; Philip A. MacFaul; Jane L. Holmes; Nathaniel G. Martin; Jane E. Moore; D. G. A. Morgan; Claire Newton; Krister Österlund; Graeme R. Robb; Eleanor Rosevere; Nidhal Selmi; Stephen Stokes; Tor Svensson; Victoria Ullah; Emma J. Williams

A pyrazolo-pyrimidinone based series of growth hormone secretagogue receptor type 1a (GHS-R1a) antagonists and inverse agonists were identified using a scaffold hop from known quinazolinone GHS-R1a modulators. Lipophilicity was reduced to decrease hERG activity while maintaining GHS-R1a affinity. SAR exploration of a piperidine substituent was used to identify small cyclic groups as a functional switch from partial agonists to neutral antagonists and inverse agonists. A tool compound was identified which had good overall properties and sufficient oral plasma and CNS exposure to demonstrate reduced food intake in mice through a mechanism involving GHS-R1a.


Bioorganic & Medicinal Chemistry | 2014

Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa).

Mikael Dan Brink; Anders Dahlén; Thomas Olsson; Magnus Polla; Tor Svensson

A series of 4,5,6,7-tetrahydro-1H-benzimidazole-5-carboxylic acid and 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-7-carboxylic acid derivatives designed as inhibitors of TAFIa has been prepared via a common hydrogenation-alkylation sequence starting from the appropriate benzimidazole and imidazopyridine system. We present a successful design strategy using a conformational restriction approach resulting in potent and selective inhibitors of TAFIa. The X-ray structure of compound 5 in complex with a H333Y/H335Q double mutant TAFI indicate that the conformational restriction is responsible for the observed potency increase.


Bioorganic & Medicinal Chemistry Letters | 2014

Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel

Roine I. Olsson; Ingemar Jacobson; Tommy Iliefski; Jonas Boström; Öjvind Davidsson; Ola Fjellström; Annika Björe; Christina Olsson; Johan Sundell; Ulrik Gran; Jonna Gyll; Jesper Malmberg; Olle Hidestål; Hans Emtenäs; Tor Svensson; Zhong-Qing Yuan; Gert Strandlund; Annika Åstrand; Emma Lindhardt; Gunilla Linhardt; Elin Forsström; Ågot Högberg; Frida Persson; Birgit Andersson; Anna Rönnborg; Boel Löfberg

A series of lactam sulfonamides has been discovered and optimized as inhibitors of the Kv1.5 potassium ion channel for treatment of atrial fibrillation. In vitro structure-activity relationships from lead structure C to optimized structure 3y are described. Compound 3y was evaluated in a rabbit PD-model and was found to selectively prolong the atrial effective refractory period at submicromolar concentrations.


Bioorganic & Medicinal Chemistry Letters | 2017

Discovery of triazole aminopyrazines as a highly potent and selective series of PI3Kδ inhibitors

Ina Terstiege; Matthew Perry; Jens Petersen; Christian Tyrchan; Tor Svensson; Helena Lindmark; Linda Öster

A novel class of potent PI3Kδ inhibitors with >1000-fold selectivity against other class I PI3K isoforms is described. Optimization of the substituents on a triazole aminopyrazine scaffold, emerging from an in-house PI3Kα program, turned moderately selective PI3Kδ compounds into highly potent and selective PI3Kδ inhibitors. These efforts resulted in a series of aminopyrazines with PI3Kδ IC50⩽1nM in the enzyme assay, some of the most selective PI3Kδ inhibitors published to date, with a cell potency in a JeKo-cell assay of 20-120nM.


Journal of Medicinal Chemistry | 2017

Design and Synthesis of Soluble and Cell-Permeable PI3Kδ Inhibitors for Long-Acting Inhaled Administration

Matthew Perry; Karin Björhall; Britta K. Bonn; Johan Carlsson; Yunhua Chen; Anders Eriksson; Linda Fredlund; Hai'e Hao; Neil S. Holden; Kostas Karabelas; Helena Lindmark; Feifei Liu; Nils Pemberton; Jens Petersen; Sandra Rodrigo Blomqvist; Reed W. Smith; Tor Svensson; Ina Terstiege; Christian Tyrchan; Wenzhen Yang; Shuchun Zhao; Linda Öster

PI3Kδ is a lipid kinase that is believed to be important in the migration and activation of cells of the immune system. Inhibition is hypothesized to provide a powerful yet selective immunomodulatory effect that may be beneficial for the treatment of conditions such as asthma or rheumatoid arthritis. In this work, we describe the identification of inhibitors based on a thiazolopyridone core structure and their subsequent optimization for inhalation. The initially identified compound (13) had good potency and isoform selectivity but was not suitable for inhalation. Addition of basic substituents to a region of the molecule pointing to solvent was tolerated (enzyme inhibition pIC50 > 9), and by careful manipulation of the pKa and lipophilicity, we were able to discover compounds (20b, 20f) with good lung retention and cell potency that could be taken forward to in vivo studies where significant target engagement could be demonstrated.


Bioorganic & Medicinal Chemistry Letters | 2006

A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Peter Bach; Karolina Nilsson; Andreas Wållberg; Udo Bauer; Lance G. Hammerland; Alecia Peterson; Tor Svensson; Krister Österlund; David Karis; Maria Boije; David Wensbo


Archive | 2006

GABA-B RECEPTOR MODULATORS

Udo Bauer; Wayne Brailsford; Linda Gustafsson; Tor Svensson


Bioorganic & Medicinal Chemistry Letters | 2006

Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Peter Bach; Karolina Nilsson; Tor Svensson; Udo Bauer; Lance G. Hammerland; Alecia Peterson; Andreas Wållberg; Krister Österlund; David Karis; Maria Boije; David Wensbo


Archive | 2006

Imidazole derivatives for the treatment of gastrointestinal disorders

Udo Bauer; Wayne Brailsford; Linda Gustafsson; Tor Svensson; Maria Saxin


Archive | 2006

Heterocyclic Gaba-b Modulators

Udo Bauer; Linda Gustafsson; Maria Saxin; Tor Svensson

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