- PROCESSES FOR THE PREPARATION OF ELUXADOLINE
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The present invention relates to processes for the preparation of eluxadoline. The present invention also provides a compound of Formula V, a process for its preparation, and its use for the preparation of eluxadoline.
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Page/Page column 29-30; 31; 32
(2018/04/20)
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- PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN THE SYNTHESIS OF ELUXADOLINE
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The invention relates to an improved process for preparing [(S)-1-(4-phenyl-1-H-imidazol-2- yl)-ethyl]-amine. The process involves formation of the novel intermediate crystalline compound[(S)-1-(4-phenyl-1-H-imidazol-2-yl)-ethyl]-carbamic acid tert-butyl ester oxalate.
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Page/Page column 9
(2017/05/28)
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- Identification of a dual δ or antagonist/μ or agonist as a potential therapeutic for diarrhea-predominant Irritable Bowel Syndrome (IBS-d)
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A small set of acyclic analogs 5 were prepared to explore their structure-activity relationships (SARs) relative to heterocyclic core, opioid receptor (OR) agonists 4. Compound 5l was found to have very favorable OR binding affinities at the δ and μ ORs (r Ki δ = 1.3 nM; r Ki μ = 0.9 nM; h Ki μ = 1.7 nM), with less affinity for the κ OR (gp Ki κ = 55 nM). The OR functional profile for 5l varied from the previously described dual δ/μ OR agonists 4, with 5l being a potent, mixed dual δ OR antagonist/μ OR agonist [δ IC50 = 89 nM (HVD); μ EC50 = 1 nM (GPI); κ EC50 = 1.6 μM (GPC)]. Compound 5l has progressed through a clinical Phase II Proof of Concept study on 800 patients suffering from diarrhea-predominant Irritable Bowel Syndrome (IBS-d). This Phase II study was recently completed successfully, with 5l demonstrating statistically significant efficacy over placebo.
- Breslin, Henry J.,Diamond, Craig J.,Kavash, Robert W.,Cai, Chaozhong,Dyatkin, Alexey B.,Miskowski, Tamara A.,Zhang, Sui-Po,Wade, Paul R.,Hornby, Pamela J.,He, Wei
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p. 4869 - 4872
(2012/08/13)
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- PROCESS FOR THE PREPARATION OF OPIOID MODULATORS
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The present invention is directed to novel processes for the preparation of opioid modulators (agonists and antagonists) and intermediates in their synthesis. The opioid modulators are useful for the treatment and prevention of as pain and gastrointestina
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Page/Page column 28-29
(2008/06/13)
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- NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS
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The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may
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Page/Page column 32
(2010/02/13)
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