Cilomilast - CAS 153259-65-5
Catalog number:
153259-65-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
PDE4
Description:
Selective phosphodiesterase 4 (PDE4) inhibitor. Antiasthmatic; used in treatment of chronic obstructive pulmonary disease.
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Purity:
0.98
Appearance:
White solid
Synonyms:
Cilomilast; Ariflo; SB-207499.
MSDS:
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1. Pd-mediated new synthesis of pyrroles: their evaluation as potential inhibitors of phosphodiesterase 4
G. Rajeshwar Reddy, T. Ram Reddy, Manojit Pal*. Chem. Commun., 2011, 47, 7779–7781
The phosphodiesterase 4 (PDE4) inhibitors are known to be beneficial for the potential treatment of asthma and chronic obstructive pulmonary disease (COPD). The existing therapies e.g. steroids, β2 agonists and antimuscarinics are effective but do not address the long-term decline of lung function, the hallmark of COPD. PDE4 inhibitors exert anti-inflammatory and bronchodilatory effects via elevation of the c-AMP level and therefore have potential to provide relief of symptoms, prevent complications and/or progression of these diseases. Indeed, the most advanced PDE4 inhibitors e.g. cilomilast and roflumilast have shown promising results in Phase III clinical trials. As part of our ongoing effort on the identification of novel inhibitors of PDE4 we report the evaluation of a series of pyrroles (C, Fig. 1) designed from the known inhibitors A11a and B. The synthesis and functionalization of C was carried out using a Pd-based new MCR in a single pot.
2. Facile assembly of two 6-membered fused N-heterocyclic rings: a rapid access to novel small molecules via Cu-mediated reaction
Raju Adepu, Rajnikanth Sunke, Chandana L. T. Meda, Manojit Pal*. Chem. Commun., 2013, 49, 190-192
Evaluation of phosphodiesterase 4 (PDE4) inhibition for the potential treatment of CNS related diseases in addition to COPD and asthma has underlined the importance of development of PDE4 inhibitors. Only one drug i.e. roflumilast (Daxas®,Nycomed)has been launched so far and side effects including nausea and emesis have delayed the market launch of cilomilast. Thus, discovery of novel PDE4 inhibitors having fewer side effects is desirable. In pursuance of our research on identification of fused N-heterocycle based PDE-4/TNF-a inhibitors we required new routes to access our target compound C that was derived from our earlier inhibitors A/B (Fig. 1). Accordingly, we have developed a new and versatile Cu-mediated domino reaction4 leading to one-pot synthesis of C (or 3 and 5, Scheme 1) under mild conditions without using any co-catalyst, ligand or additive. Herein we report our preliminary results.
3. Indion 860 catalyzed cascade reaction: a greener approach to functionalized cyclohexanones and their novel analogues
T. Bhaskar Kumar, G. Dhananjaya, Manojit Pal*. RSC Adv., 2013, 3, 2207–2210
In addition to their uses as precursors in natural product synthesis, cyclohexanone derivatives are also found to be an integral part of several biologically active compounds including herbicidal, antibacterial, antifungal and anticonvulsant agents. The cyclohexanone or cyclohexane framework has also been explored in the discovery and development of phosphodiesterase 4 (PDE4) inhibitors e.g. cilomilast. PDE4 inhibitors are known to be useful for the treatment of chronic obstructive pulmonary diseases (COPD) and asthma and have potential in the treatment of central nervous system (CNS) related diseases. Only one drug i.e. roflumilast (Daxas1, Nycomed) has been launched so far and side effects including nausea and emesis have delayed the market launch of cilomilast. Thus, the discovery of novel PDE4 inhibitors with fewer side effects is desirable. In pursuance of our research on the identification of PDE-4/TNF-a inhibitors based on a cyclohexane framework (A) we became interested in assessing a library of compounds B against PDE4 (Fig. 1).
4. Novel N-indolylmethyl substituted olanzapine derivatives: their design, synthesis and evaluation as PDE4B inhibitors
Dhilli Rao Gorja, Soumita Mukherjee, Kishore V. L. Parsa,* K. Mukkanti and Manojit Pal*. Org. Biomol. Chem., 2013, 11, 2075–2079
Chronic obstructive pulmonary disease (COPD), a major health problem, is projected to be the 3rd leading cause of death globally by 2020 according to the WHO. Asthma, on the other hand, affects ∼300 million people worldwide at present. The search for improved therapies therefore is necessary. Among the emerging agents to treat COPD or asthma, phos- phodiesterase 4 (PDE4) inhibitors have attracted particular attention. Additionally, evaluation of PDE4 inhibition for the potential treatment of a wider range of CNS related diseases including Parkinson’s disease, schizophrenia, and Alzheimer’s disease has underlined the importance of development of PDE4 inhibitors. The first-generation PDE4 inhibitor rolipram suffered from side effects including nausea and emesis. Similar side effects delayed the market launch of the second generation inhibitors cilomilast and roflumilast. Encouragingly, roflumilast (Daxas®, Nycomed) was launched in Europe for the treatment of chronic bronchitis in 2009 and in US (Daliresp, Forest Lab) for exacerbations during COPD in 2012.
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CAS 153259-65-5 Cilomilast

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