Sant Feliu de Llobregat, Spain
Sant Feliu de Llobregat, Spain

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Esteve C.,Almirall Research Center | Gonzalez J.,Almirall Research Center | Gual S.,Almirall Research Center | Vidal L.,Almirall Research Center | And 8 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2015

Synthesis and SAR of a series of 7-azaindoles as Orai channel inhibitors showing good potency inhibiting IL-2 production in Jurkat cells is described. Compound 14d displaying best pharmacokinetic properties was further characterized in a model of allergen induced asthma showing inhibition in the number of eosinophils in BALF. High lipophilicity remains as one of the main challenges for this class of compounds. © 2015 Elsevier Ltd. All rights reserved.


Eastwood P.,Almirall Research Center | Gonzalez J.,Almirall Research Center | Gomez E.,Almirall Research Center | Caturla F.,Almirall Research Center | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38a inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation. © 2011 Elsevier Ltd. All rights reserved.


Eastwood P.,Almirall Research Center | Gonzalez J.,Almirall Research Center | Gomez E.,Almirall Research Center | Caturla F.,Almirall Research Center | And 3 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

Optimisation of a series of indolin-2-one p38α inhibitors was achieved via both blocking of a potential metabolic 'hot spot' and by increasing overall polarity of the lead series leading to non-cytotoxic compounds which showed improved oral bioavailabilities in the rat. © 2011 Elsevier Ltd. All rights reserved.


Forns P.,Almirall Barcelona Science Park Unit | Esteve C.,Almirall Research Center | Taboada L.,Almirall Research Center | Alonso J.A.,Almirall Research Center | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay. © 2012 Elsevier Ltd. All rights reserved.


Castillo M.,Almirall Barcelona Science Park Unit | Forns P.,Almirall Barcelona Science Park Unit | Erra M.,Almirall Research Center | Mir M.,Almirall Research Center | And 7 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2- pyridyl motif and represented by compound 13b IC50: 0.6 nM were identified. Substitution by a 2-pyrazinyl motif and SAR expansion in position 4 of the central core provided diverse potent non-cytotoxic Syk inhibitors showing nanomolar activity inhibiting human mast cell line LAD2 degranulation. © 2012 Elsevier Ltd. All rights reserved.


PubMed | Almirall Research Center
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2011

Optimisation of a series of indolin-2-one p38 inhibitors was achieved via both blocking of a potential metabolic hot spot and by increasing overall polarity of the lead series leading to non-cytotoxic compounds which showed improved oral bioavailabilities in the rat.


PubMed | Almirall Research Center
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2011

Crystallographic structural information was used in the design and synthesis of a number of bioisosteric derivatives to replace the amide moiety in a lead series of p38 inhibitors which showed general hydrolytic instability in human liver preparations. Triazole derivative 13 was found to have moderate bioavailability in the rat and demonstrated potent in-vivo activity in an acute model of inflammation.


PubMed | Almirall Research Center
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

Synthesis and SAR of a series of 7-azaindoles as Orai channel inhibitors showing good potency inhibiting IL-2 production in Jurkat cells is described. Compound 14d displaying best pharmacokinetic properties was further characterized in a model of allergen induced asthma showing inhibition in the number of eosinophils in BALF. High lipophilicity remains as one of the main challenges for this class of compounds.

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