Search Results - "Janus, Diana"
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Development of autotaxin inhibitors: A series of zinc binding triazoles
Published in Bioorganic & medicinal chemistry letters (15-07-2018)“…[Display omitted] •PF-8380 has been used as a template to design a new series of ATX inhibitors.•Reduction of crystallinity was key to improving solubility of…”
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Synthesis of the Marine Sponge Derived β2-Adrenoceptor Agonist S1319
Published in Organic letters (13-10-2005)“…The marine sponge derived β2-adrenoceptor agonist S1319 has been synthesized following a six-step linear sequence. Central to the approach employed is the…”
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The Identification of Indacaterol as an Ultralong-Acting Inhaled β2-Adrenoceptor Agonist
Published in Journal of medicinal chemistry (13-05-2010)“…Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of β2-adrenoceptor agonists have been prepared and evaluated…”
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The discovery of potent, orally bioavailable pyrimidine-5-carbonitrile-6-alkyl CXCR2 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-08-2014)“…A hit-to-lead optimisation programme was carried out on the Novartis archive screening hit, pyrimidine…”
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An investigation into the structure-activity relationships associated with the systematic modification of the β(2)-adrenoceptor agonist indacaterol
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…The synthesis of a series of indacaterol analogues in which each of the three structural regions of indacaterol are modified in a systematic manner is…”
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An investigation into the structure–activity relationships associated with the systematic modification of the β2-adrenoceptor agonist indacaterol
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…The synthesis of a series of indacaterol analogues in which each of the three structural regions of indacaterol are modified in a systematic manner is…”
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The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist
Published in Bioorganic & medicinal chemistry letters (01-09-2014)“…The optimisation of two series of 4-hydroxybenzothiazolone derived β2-adrenoceptor agonists, bearing α-substituted cyclopentyl and β-phenethyl…”
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Synthesis of the marine sponge derived beta2-adrenoceptor agonist S1319
Published in Organic letters (13-10-2005)“…[reaction: see text] The marine sponge derived beta2-adrenoceptor agonist S1319 has been synthesized following a six-step linear sequence. Central to the…”
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10
An investigation into the structure-activity relationships associated with the systematic modification of the [beta]2-adrenoceptor agonist indacaterol
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…The synthesis of a series of indacaterol analogues in which each of the three structural regions of indacaterol are modified in a systematic manner is…”
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11
Synthesis of the Marine Sponge Derived β 2 -Adrenoceptor Agonist S1319
Published in Organic letters (01-10-2005)Get full text
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Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the β 2-adrenoceptor activity
Published in Bioorganic & medicinal chemistry letters (20-09-2004)“…[Display omitted] The synthesis of a series of long-chain formoterol analogues in which the terminal ether residue of the β-phenethyl-amino-substituent has…”
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A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of β 2-adrenoceptor agonists as inhaled long-acting bronchodilators
Published in Bioorganic & medicinal chemistry letters (2010)“…The chiral synthesis of a 4-hydroxybenzothiazolone based series of β 2-adrenoceptor agonists is described. Using this methodology a library of N-substituted…”
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The Identification of Indacaterol as an Ultralong-Acting Inhaled β 2 -Adrenoceptor Agonist
Published in Journal of medicinal chemistry (13-05-2010)Get full text
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A physical properties based approach for the exploration of a 4-hydroxybenzothiazolone series of beta2-adrenoceptor agonists as inhaled long-acting bronchodilators
Published in Bioorganic & medicinal chemistry letters (01-09-2010)“…The chiral synthesis of a 4-hydroxybenzothiazolone based series of beta(2)-adrenoceptor agonists is described. Using this methodology a library of…”
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16
Long-chain formoterol analogues: an investigation into the effect of increasing amino-substituent chain length on the beta2-adrenoceptor activity
Published in Bioorganic & medicinal chemistry letters (20-09-2004)“…The synthesis of a series of long-chain formoterol analogues in which the terminal ether residue of the beta-phenethyl-amino-substituent has been extended…”
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The identification of indacaterol as an ultralong-acting inhaled beta2-adrenoceptor agonist
Published in Journal of medicinal chemistry (13-05-2010)“…Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of beta(2)-adrenoceptor agonists have been prepared and…”
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Design and Synthesis of Thrombin Inhibitors: Analogues of MD-805 with Reduced Stereogenicity and Improved Potency
Published in Journal of medicinal chemistry (04-11-1999)“…Mitsubishi's MD-805, a potent and selective inhibitor of thrombin which contains four stereogenic centers, has been the starting point for an optimization…”
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The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position
Published in Bioorganic & medicinal chemistry letters (17-07-2000)“…A series of monocyclic and bicyclic amino acids have been synthesised and incorporated into thrombin inhibitors based on CGH728, an analogue of the Mitsubishi…”
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