2326-26-3Relevant articles and documents
ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF
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Paragraph 442; 611, (2021/10/30)
The invention provides anti-VISTA antibody drug conjugates which may be used for targeted delivery of anti-inflammatory agents such as steroids to immune cells, e.g., myeloid cells. The invention also provides methods of using anti-VISTA antibody drug conjugates in the treatment of inflammatory and/or autoimmune conditions and/or for alleviating the toxicity of anti-inflammatory agents such as steroids.
Novel Pyrrolidine Derivatives of Budesonide as Long Acting Inhaled Corticosteroids for the Treatment of Pulmonary Inflammatory Diseases
Ghidini, Eleonora,Marchini, Gessica,Capelli, Anna Maria,Carnini, Chiara,Cenacchi, Valentina,Fioni, Alessandro,Facchinetti, Fabrizio,Rancati, Fabio
supporting information, p. 4757 - 4773 (2018/05/23)
Inhaled corticosteroids (ICSs) represent the first line therapy for the treatment of asthma and are also extensively utilized in chronic obstructive pulmonary disease. Our goal was to develop a new ICS with a basic group, which can allow solid state feature modulation, achieving at the same time high local anti-inflammatory effect and low systemic exposure. Through a rational drug design approach, a new series of pyrrolidine derivatives of budesonide was identified. Within the series, several compounds showed nanomolar binding affinity (Ki) with GR that mostly correlated with the effect in inducing GR nuclear translocation in CHO cells and anti-inflammatory effects in macrophagic cell lines. Binding and functional cell-based assays allowed identifying compound 17 as a potent ICS agonist with a PK profile showing an adequate lung retention and low systemic exposure in vivo. Finally, compound 17 proved to be more potent than budesonide in a rat model of acute pulmonary inflammation.
PYRROLIDINE DERIVATIVES
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Paragraph 0084; 0085; 0086; 0087, (2013/03/26)
Novel anti-inflammatory and antiallergic compounds of the glucocorticosteroid series according to formulae (I) and (I′) are effective for the prevention and/or treatment of diseases in which the number, activity, and movement of inflammatory cells is implicated.