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153259-65-5,MFCD00924373
Catalog No.:AA00AOMN

153259-65-5 | Cilomilast

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1mg
≥98%
in stock  
$46.00   $32.00
- +
5mg
≥98%
in stock  
$188.00   $131.00
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10mg
≥98%
in stock  
$348.00   $243.00
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25mg
99%
in stock  
$490.00   $343.00
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100mg
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$1,947.00   $1,363.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00AOMN
Chemical Name:
Cilomilast
CAS Number:
153259-65-5
Molecular Formula:
C20H25NO4
Molecular Weight:
343.4168
MDL Number:
MFCD00924373
SMILES:
N#C[C@@]1(CC[C@H](CC1)C(=O)O)c1ccc(c(c1)OC1CCCC1)OC
Properties
Properties
 
Form:
Solid  
MP:
157˚C  
Storage:
-20 ℃;  

Computed Properties
 
Complexity:
511  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
25  
Hydrogen Bond Acceptor Count:
5  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
5  
XLogP3:
3.4  

Downstream Synthesis Route

[1]Christensen,SiegfriedB.;Guider,Aimee;Forster,CorneliaJ.;Gleason,JohnG.;Bender,PaulE.;Karpinski,JosephM.;DewolfJr.,WalterE.;Barnette,MaryS.;Underwood,DavidC.;Griswold,DonE.;Cieslinski,LenoraB.;Burman,Miriam;Bochnowicz,Steven;Osborn,RuthR.;Manning,CarolD.;Grous,Marilyn;Hillegas,LeonardM.;Bartus,JoanO'Leary;DominicRyan;Eggleston,DrakeS.;CurtisHaltiwanger;Torphy,TheodoreJ.[JournalofMedicinalChemistry,1998,vol.41,#6,p.821-835]

[1]Christensen,SiegfriedB.;Guider,Aimee;Forster,CorneliaJ.;Gleason,JohnG.;Bender,PaulE.;Karpinski,JosephM.;DewolfJr.,WalterE.;Barnette,MaryS.;Underwood,DavidC.;Griswold,DonE.;Cieslinski,LenoraB.;Burman,Miriam;Bochnowicz,Steven;Osborn,RuthR.;Manning,CarolD.;Grous,Marilyn;Hillegas,LeonardM.;Bartus,JoanO'Leary;DominicRyan;Eggleston,DrakeS.;CurtisHaltiwanger;Torphy,TheodoreJ.[JournalofMedicinalChemistry,1998,vol.41,#6,p.821-835]

[2]CurrentPatentAssignee:GLAXOSMITHKLINEPLC-US5552438,1996,A

[3]CurrentPatentAssignee:GLAXOSMITHKLINEPLC-US5602157,1997,A

[4]Amata,Emanuele;Bland,NicholasD.;Hoyt,CharlesT.;Settimo,Luca;Campbell,RobertK.;Pollastri,MichaelP.[BioorganicandMedicinalChemistryLetters,2014,vol.24,#17,p.4084-4089]

cis-(+/-)-6-3-(cyclopentyloxy)-4-methoxyphenyl-1-oxospiro2,5octane-2,6-dicarbonitrile 
  153259-65-5    153259-69-9 

[1]Badham,NeilF.;Mendelson,WilfordL.;Allen,Andrew;Diederich,AnnM.;Eggleston,DrakeS.;Filan,JohnJ.;Freyer,AlanJ.;KillmerJr.,LewisB.;Kowalski,ConradJ.;Liu,Li;Novack,VanceJ.;Vogt,FrederickG.;Webb,KevinS.;Yang,Jennifer[JournalofOrganicChemistry,2002,vol.67,#15,p.5440-5443]

[1]Badham,NeilF.;Mendelson,WilfordL.;Allen,Andrew;Diederich,AnnM.;Eggleston,DrakeS.;Filan,JohnJ.;Freyer,AlanJ.;KillmerJr.,LewisB.;Kowalski,ConradJ.;Liu,Li;Novack,VanceJ.;Vogt,FrederickG.;Webb,KevinS.;Yang,Jennifer[JournalofOrganicChemistry,2002,vol.67,#15,p.5440-5443]

[2]Christensen,SiegfriedB.;Guider,Aimee;Forster,CorneliaJ.;Gleason,JohnG.;Bender,PaulE.;Karpinski,JosephM.;DewolfJr.,WalterE.;Barnette,MaryS.;Underwood,DavidC.;Griswold,DonE.;Cieslinski,LenoraB.;Burman,Miriam;Bochnowicz,Steven;Osborn,RuthR.;Manning,CarolD.;Grous,Marilyn;Hillegas,LeonardM.;Bartus,JoanO'Leary;DominicRyan;Eggleston,DrakeS.;CurtisHaltiwanger;Torphy,TheodoreJ.[JournalofMedicinalChemistry,1998,vol.41,#6,p.821-835]

[1]Christensen,SiegfriedB.;Guider,Aimee;Forster,CorneliaJ.;Gleason,JohnG.;Bender,PaulE.;Karpinski,JosephM.;DewolfJr.,WalterE.;Barnette,MaryS.;Underwood,DavidC.;Griswold,DonE.;Cieslinski,LenoraB.;Burman,Miriam;Bochnowicz,Steven;Osborn,RuthR.;Manning,CarolD.;Grous,Marilyn;Hillegas,LeonardM.;Bartus,JoanO'Leary;DominicRyan;Eggleston,DrakeS.;CurtisHaltiwanger;Torphy,TheodoreJ.[JournalofMedicinalChemistry,1998,vol.41,#6,p.821-835]

Literature

Title: Cilomilast enhances osteoblast differentiation of mesenchymal stem cells and bone formation induced by bone morphogenetic protein 2.

Journal: Biochimie 20121101

Title: Design, synthesis, and pharmacological evaluation of N-acylhydrazones and novel conformationally constrained compounds as selective and potent orally active phosphodiesterase-4 inhibitors.

Journal: Journal of medicinal chemistry 20120913

Title: 3D QSAR pharmacophore, CoMFA and CoMSIA based design and docking studies on phenyl alkyl ketones as inhibitors of phosphodiesterase 4.

Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) 20120901

Title: PDE4 inhibition suppresses IL-17-associated immunity in dry eye disease.

Journal: Investigative ophthalmology & visual science 20120601

Title: Dual β2-adrenoceptor agonists-PDE4 inhibitors for the treatment of asthma and COPD.

Journal: Bioorganic & medicinal chemistry letters 20120215

Title: Anti-asthmatic effect of ASP3258, a novel phosphodiesterase 4 inhibitor.

Journal: International immunopharmacology 20120101

Title: Anti-neutrophilic inflammatory activity of ASP3258, a novel phosphodiesterase type 4 inhibitor.

Journal: International immunopharmacology 20120101

Title: Hesperetin, a Selective Phosphodiesterase 4 Inhibitor, Effectively Suppresses Ovalbumin-Induced Airway Hyperresponsiveness without Influencing Xylazine/Ketamine-Induced Anesthesia.

Journal: Evidence-based complementary and alternative medicine : eCAM 20120101

Title: PDE4-inhibitors: a novel, targeted therapy for obstructive airways disease.

Journal: Pulmonary pharmacology & therapeutics 20110801

Title: ASP3258, an orally active potent phosphodiesterase 4 inhibitor with low emetic activity.

Journal: International immunopharmacology 20110601

Title: Phosphodiesterase 4 inhibitors for chronic obstructive pulmonary disease.

Journal: The Cochrane database of systematic reviews 20110511

Title: GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization.

Journal: The Journal of pharmacology and experimental therapeutics 20110401

Title: In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor.

Journal: The Journal of pharmacology and experimental therapeutics 20110401

Title: S-Petasin, the Main Sesquiterpene of Petasites formosanus, Inhibits Phosphodiesterase Activity and Suppresses Ovalbumin-Induced Airway Hyperresponsiveness.

Journal: Evidence-based complementary and alternative medicine : eCAM 20110101

Title: Reduction of exacerbations by the PDE4 inhibitor roflumilast--the importance of defining different subsets of patients with COPD.

Journal: Respiratory research 20110101

Title: Inhibition of granulocyte migration by tiotropium bromide.

Journal: Respiratory research 20110101

Title: Cilomilast counteracts the effects of cigarette smoke in airway epithelial cells.

Journal: Cellular immunology 20110101

Title: Biochanin a, a phytoestrogenic isoflavone with selective inhibition of phosphodiesterase 4, suppresses ovalbumin-induced airway hyperresponsiveness.

Journal: Evidence-based complementary and alternative medicine : eCAM 20110101

Title: New therapeutic options in the management of COPD - focus on roflumilast.

Journal: International journal of chronic obstructive pulmonary disease 20110101

Title: β2-Agonist induced cAMP is decreased in asthmatic airway smooth muscle due to increased PDE4D.

Journal: PloS one 20110101

Title: Health status in the TORCH study of COPD: treatment efficacy and other determinants of change.

Journal: Respiratory research 20110101

Title: Update on pharmaceutical and minimally invasive management strategies for chronic obstructive pulmonary disease.

Journal: Pulmonary medicine 20110101

Title: Roflumilast attenuates allergen-induced inflammation in mild asthmatic subjects.

Journal: Respiratory research 20110101

Title: Hesperetin-7,3'-O-dimethylether selectively inhibits phosphodiesterase 4 and effectively suppresses ovalbumin-induced airway hyperresponsiveness with a high therapeutic ratio.

Journal: Journal of biomedical science 20110101

Title: Roflumilast, a Novel Phosphodiesterase 4 Inhibitor, for COPD Patients with a History of Exacerbations.

Journal: Clinical medicine insights. Circulatory, respiratory and pulmonary medicine 20110101

Title: Relationship between phosphodiesterase type 4 inhibition and anti-inflammatory activity of CI-1044 in rat airways.

Journal: Fundamental & clinical pharmacology 20100201

Title: Effects of phosphodiesterase 4 inhibition on bleomycin-induced pulmonary fibrosis in mice.

Journal: BMC pulmonary medicine 20100101

Title: Pharmacological studies of bronchial constriction inhibited by parasympatholytics and cilomilast using equine precision-cut lung slices.

Journal: Berliner und Munchener tierarztliche Wochenschrift 20100101

Title: Influencing the decline of lung function in COPD: use of pharmacotherapy.

Journal: International journal of chronic obstructive pulmonary disease 20100101

Title: Roflumilast: first phosphodiesterase 4 inhibitor approved for treatment of COPD.

Journal: Drug design, development and therapy 20100101

Title: Effects of the new benzimidazole derivative TAS-203, an orally active phosphodiesterase 4 inhibitor, on airway inflammation in rats and emetic responses in ferrets.

Journal: Arzneimittel-Forschung 20100101

Title: The identification of a novel phosphodiesterase 4 inhibitor, 1-ethyl-5-{5-[(4-methyl-1-piperazinyl)methyl]-1,3,4-oxadiazol-2-yl}-N-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-b]pyridin-4-amine (EPPA-1), with improved therapeutic index using pica feeding in rats as a measure of emetogenicity.

Journal: The Journal of pharmacology and experimental therapeutics 20090901

Title: Granulocyte-macrophage colony-stimulating factor expression in induced sputum and bronchial mucosa in asthma and COPD.

Journal: Thorax 20090801

Title: A phosphodiesterase inhibitor, cilomilast, enhances cAMP activity to restore conditioned odor preference memory after serotonergic depletion in the neonate rat.

Journal: Neurobiology of learning and memory 20090701

Title: Does PDE4 inhibition improve alveolarisation in hyperoxia-exposed immature rodents?

Journal: The European respiratory journal 20090501

Title: Inhibition of phosphodiesterase 4 enhances lung alveolarisation in neonatal mice exposed to hyperoxia.

Journal: The European respiratory journal 20090401

Title: Pharmacology of a novel, orally active PDE4 inhibitor.

Journal: Pharmacology 20090101

Title: A multi-target antisense approach against PDE4 and PDE7 reduces smoke-induced lung inflammation in mice.

Journal: Respiratory research 20090101

Title: Exacerbation rate, health status and mortality in COPD--a review of potential interventions.

Journal: International journal of chronic obstructive pulmonary disease 20090101

Title: Targeted treatment in COPD: a multi-system approach for a multi-system disease.

Journal: International journal of chronic obstructive pulmonary disease 20090101

Title: Chronic obstructive pulmonary disease: towards pharmacogenetics.

Journal: Genome medicine 20090101

Title: ABCD of the phosphodiesterase family: interaction and differential activity in COPD.

Journal: International journal of chronic obstructive pulmonary disease 20081201

Title: PDE4 inhibitors: current status.

Journal: British journal of pharmacology 20081001

Title: Can the anti-inflammatory potential of PDE4 inhibitors be realized: guarded optimism or wishful thinking?

Journal: British journal of pharmacology 20081001

Title: Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.

Journal: Journal of medicinal chemistry 20080925

Title: Curative effects of phosphodiesterase 4 inhibitors cilomilast, roflumilast, and rolipram in dermatitis mouse model.

Journal: Journal of dermatological science 20080901

Title: Airways inflammation and treatment during acute exacerbations of COPD.

Journal: International journal of chronic obstructive pulmonary disease 20080601

Title: Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.

Journal: European journal of medicinal chemistry 20080501

Title: PDE4 inhibitor, roflumilast protects cardiomyocytes against NO-induced apoptosis via activation of PKA and Epac dual pathways.

Journal: Cellular signalling 20080501

Title: Human PDE4A8, a novel brain-expressed PDE4 cAMP-specific phosphodiesterase that has undergone rapid evolutionary change.

Journal: The Biochemical journal 20080415

Title: Inhibition by salmeterol and cilomilast of fluticasone-enhanced IP-10 release in airway epithelial cells.

Journal: COPD 20080201

Title: Bronchiolar chemokine expression is different after single versus repeated cigarette smoke exposure.

Journal: Respiratory research 20080101

Title: New drugs targeting Th2 lymphocytes in asthma.

Journal: Journal of occupational medicine and toxicology (London, England) 20080101

Title: Effects of phosphodiesterase 4 inhibition on alveolarization and hyperoxia toxicity in newborn rats.

Journal: PloS one 20080101

Title: The efficacy and safety of cilomilast in COPD. Forward.

Journal: Drugs 20080101

Title: The efficacy and safety of cilomilast in COPD.

Journal: Drugs 20080101

Title: [Selective phosphodiesterase-4 (PDE-4) inhibitors in COPD].

Journal: Tuberkuloz ve toraks 20080101

Title: Pharmacological control of neutrophil-mediated inflammation: strategies targeting calcium handling by activated polymorphonuclear leukocytes.

Journal: Drug design, development and therapy 20080101

Title: Pulmonary epithelium, cigarette smoke, and chronic obstructive pulmonary disease.

Journal: International journal of chronic obstructive pulmonary disease 20071201

Title: Treating COPD with PDE 4 inhibitors.

Journal: International journal of chronic obstructive pulmonary disease 20071201

Title: Future therapeutic treatment of COPD: struggle between oxidants and cytokines.

Journal: International journal of chronic obstructive pulmonary disease 20070901

Title: Phosphodiesterase 4 inhibitors augment levels of glucocorticoid receptor in B cell chronic lymphocytic leukemia but not in normal circulating hematopoietic cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070815

Title: PDE4B5, a novel, super-short, brain-specific cAMP phosphodiesterase-4 variant whose isoform-specifying N-terminal region is identical to that of cAMP phosphodiesterase-4D6 (PDE4D6).

Journal: The Journal of pharmacology and experimental therapeutics 20070801

Title: L-454,560, a potent and selective PDE4 inhibitor with in vivo efficacy in animal models of asthma and cognition.

Journal: Biochemical pharmacology 20070615

Title: Differential effects of phosphodiesterase PDE-3/PDE-4-specific inhibitors on vasoconstriction and cAMP-dependent vasorelaxation following balloon angioplasty.

Journal: American journal of physiology. Heart and circulatory physiology 20070601

Title: PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast.

Journal: International journal of chronic obstructive pulmonary disease 20070601

Title: Therapeutic benefit of PDE4 inhibitors in inflammatory diseases.

Journal: Current opinion in investigational drugs (London, England : 2000) 20070501

Title: Effects of cyclosporin A and cilomilast on activated canine, murine and human keratinocytes.

Journal: Veterinary dermatology 20070401

Title: Highly selective phosphodiesterase 4 inhibitors for the treatment of allergic skin diseases and psoriasis.

Journal: Inflammation & allergy drug targets 20070301

Title: SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.

Journal: Journal of medicinal chemistry 20070125

Title: Selective inhibitors for phosphodiesterase 3 and 4 in antigen-induced increase of cough reflex sensitivity in guinea pigs.

Journal: Pulmonary pharmacology & therapeutics 20070101

Title: Evaluation of oral corticosteroids and phosphodiesterase-4 inhibitor on the acute inflammation induced by inhaled lipopolysaccharide in human.

Journal: Pulmonary pharmacology & therapeutics 20070101

Title: Phosphodiesterase-4 inhibitors as a novel approach for the treatment of respiratory disease: cilomilast.

Journal: Expert opinion on investigational drugs 20070101

Title: Cyclic AMP signalling pathways in the regulation of uterine relaxation.

Journal: BMC pregnancy and childbirth 20070101

Title: Maternal allergic contact dermatitis causes increased asthma risk in offspring.

Journal: Respiratory research 20070101

Title: Bronchial epithelial spheroids: an alternative culture model to investigate epithelium inflammation-mediated COPD.

Journal: Respiratory research 20070101

Title: Airways disease: phenotyping heterogeneity using measures of airway inflammation.

Journal: Allergy, asthma, and clinical immunology : official journal of the Canadian Society of Allergy and Clinical Immunology 20070101

Title: The phosphodiesterase type IV inhibitor cilomilast decreases pro-inflammatory cytokine production from primary bronchial epithelial cells in lung transplantation patients.

Journal: The Journal of heart and lung transplantation : the official publication of the International Society for Heart Transplantation 20061201

Title: Evaluation of PDE4 inhibition for COPD.

Journal: International journal of chronic obstructive pulmonary disease 20061201

Title: Pharmacological treatment of chronic obstructive pulmonary disease.

Journal: International journal of chronic obstructive pulmonary disease 20061201

Title: Phosphodiesterase 4 inhibition of beta2-integrin adhesion caused by leukotriene B4 and TNF-alpha in human neutrophils.

Journal: The European respiratory journal 20061101

Title: Phosphodiesterase 4 inhibitors modulate beta2-adrenoceptor agonist-induced human airway hyperresponsiveness.

Journal: Life sciences 20061012

Title: Effects of ciclamilast, a new PDE 4 PDE4 inhibitor, on airway hyperresponsiveness, PDE4D expression and airway inflammation in a murine model of asthma.

Journal: European journal of pharmacology 20061010

Title: Determination of drug binding to plasma proteins using competitive equilibrium binding to dextran-coated charcoal.

Journal: Journal of pharmacokinetics and pharmacodynamics 20061001

Title: Cilomilast: orally active selective phosphodiesterase-4 inhibitor for treatment of chronic obstructive pulmonary disease.

Journal: The Annals of pharmacotherapy 20061001

Title: Biological targets for therapeutic interventions in COPD: clinical potential.

Journal: International journal of chronic obstructive pulmonary disease 20060901

Title: An update and appraisal of the cilomilast Phase III clinical development programme for chronic obstructive pulmonary disease.

Journal: British journal of clinical pharmacology 20060801

Title: Involvement of MMP-12 and phosphodiesterase type 4 in cigarette smoke-induced inflammation in mice.

Journal: The European respiratory journal 20060601

Title: Preferential inhibition of human phosphodiesterase 4 by ibudilast.

Journal: Life sciences 20060501

Title: Roflumilast for the treatment of chronic obstructive pulmonary disease.

Journal: Current opinion in investigational drugs (London, England : 2000) 20060501

Title: [Pharmacological treatment of COPD and future of anti-inflammatory therapy].

Journal: Medizinische Klinik (Munich, Germany : 1983) 20060415

Title: Cilomilast.

Journal: Drugs of today (Barcelona, Spain : 1998) 20060401

Title: Effects of cilomilast, a selective phosphodiesterase 4 inhibitor, on esophageal motility and pH, and orocecal and colonic transit: two single-center, randomized, double-blind, placebo-controlled, two-part crossover studies in healthy volunteers.

Journal: Clinical therapeutics 20060401

Title: Phosphodiesterase inhibitors in airways disease.

Journal: European journal of pharmacology 20060308

Title: Eosinophilic airway inflammation in COPD.

Journal: International journal of chronic obstructive pulmonary disease 20060301

Title: Inhibition of airway hyperresponsiveness and pulmonary inflammation by roflumilast and other PDE4 inhibitors.

Journal: Pulmonary pharmacology & therapeutics 20060101

Title: Phosphodiesterase type 4 expression and anti-proliferative effects in human pulmonary artery smooth muscle cells.

Journal: Respiratory research 20060101

Title: COPD, inflammation and its modulation by phosphodiesterase 4 inhibitors: time to look beyond the FEV1.

Journal: Chest 20060101

Title: Cilomilast for COPD: results of a 6-month, placebo-controlled study of a potent, selective inhibitor of phosphodiesterase 4.

Journal: Chest 20060101

Title: Clinical pharmacology of Cilomilast.

Journal: Clinical pharmacokinetics 20060101

Title: The potential role of phosphodiesterase inhibitors in the management of asthma.

Journal: Treatments in respiratory medicine 20060101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20060101

Title: Phosphodiesterase 4 inhibitors for the treatment of asthma and COPD.

Journal: Current medicinal chemistry 20060101

Title: Cilomilast, tacrolimus and rapamycin modulate dendritic cell function in the elicitation phase of allergic contact dermatitis.

Journal: The British journal of dermatology 20050701

Title: Research on airway inflammation: present status in Mainland China.

Journal: Chinese medical journal 20050620

Title: Evidence for a role of phosphodiesterase 4 in lipopolysaccharide-stimulated prostaglandin E2 production and matrix metalloproteinase-9 activity in human amniochorionic membranes.

Journal: Journal of immunology (Baltimore, Md. : 1950) 20050615

Title: Identification and characterization of PDE4A11, a novel, widely expressed long isoform encoded by the human PDE4A cAMP phosphodiesterase gene.

Journal: Molecular pharmacology 20050601

Title: PDE4 inhibitors as new anti-inflammatory drugs: effects on cell trafficking and cell adhesion molecules expression.

Journal: Pharmacology & therapeutics 20050601

Title: Cilomilast GlaxoSmithKline.

Journal: Current opinion in investigational drugs (London, England : 2000) 20050501

Title: Cilomilast, an orally active phosphodiesterase 4 inhibitor for the treatment of COPD.

Journal: Expert review of clinical immunology 20050501

Title: CGH2466, a combined adenosine receptor antagonist, p38 mitogen-activated protein kinase and phosphodiesterase type 4 inhibitor with potent in vitro and in vivo anti-inflammatory activities.

Journal: British journal of pharmacology 20050401

Title: Selective phosphodiesterase-4 inhibitors in chronic obstructive lung disease.

Journal: Current opinion in pulmonary medicine 20050301

Title: Selective PDE4 inhibitors as potent anti-inflammatory drugs for the treatment of airway diseases.

Journal: Memorias do Instituto Oswaldo Cruz 20050301

Title: Phosphodiesterase 4 inhibition decreases MUC5AC expression induced by epidermal growth factor in human airway epithelial cells.

Journal: Thorax 20050201

Title: Phosphodiesterase 4-selective inhibition: novel therapy for the inflammation of COPD.

Journal: Pulmonary pharmacology & therapeutics 20050101

Title: The novel phosphodiesterase 4 inhibitor, CI-1044, inhibits LPS-induced TNF-alpha production in whole blood from COPD patients.

Journal: Pulmonary pharmacology & therapeutics 20050101

Title: Phosphodiesterase-4 inhibitors for asthma and chronic obstructive pulmonary disease.

Journal: Lancet (London, England) 20050101

Title: The effect of selective phosphodiesterase isoenzyme inhibition on neutrophil function in vitro.

Journal: Pulmonary pharmacology & therapeutics 20050101

Title: Potentiation and prolongation of long-term odor memory in neonate rats using a phosphodiesterase inhibitor.

Journal: Neuroscience 20050101

Title: Phosphodiesterase-4: selective and dual-specificity inhibitors for the therapy of chronic obstructive pulmonary disease.

Journal: Proceedings of the American Thoracic Society 20050101

Title: Roflumilast: the evidence for its clinical potential in the treatment of chronic obstructive pulmonary disease.

Journal: Core evidence 20050101

Title: Structural basis for the activity of drugs that inhibit phosphodiesterases.

Journal: Structure (London, England : 1993) 20041201

Title: Effects of phosphodiesterase 4 inhibitor on cough response in guinea pigs sensitized and challenged with ovalbumin.

Journal: Chinese medical journal 20041101

Title: TARC and RANTES, but not CTACK, are induced in two models of allergic contact dermatitis. Effects of cilomilast and diflorasone diacetate on T-cell-attracting chemokines.

Journal: The British journal of dermatology 20041001

Title: Role of PDE4 in superoxide anion generation through p44/42MAPK regulation: a cAMP and a PKA-independent mechanism.

Journal: British journal of pharmacology 20040901

Title: Lack of pharmacokinetic interactions between cilomilast and theophylline or smoking in healthy volunteers.

Journal: Journal of clinical pharmacology 20040901

Title: Highly potent PDE4 inhibitors with therapeutic potential.

Journal: Bioorganic & medicinal chemistry 20040901

Title: PDE4 inhibition: a novel approach for the treatment of inflammatory bowel disease.

Journal: Trends in pharmacological sciences 20040801

Title: Modulation of matrix metalloproteinase production from human lung fibroblasts by type 4 phosphodiesterase inhibitors.

Journal: Life sciences 20040702

Title: Cytokines modulate cilomilast response in lung fibroblasts.

Journal: Clinical immunology (Orlando, Fla.) 20040601

Title: PDE4 inhibitors in COPD--a more selective approach to treatment.

Journal: Respiratory medicine 20040601

Title: Orally active PDE4 inhibitors with therapeutic potential.

Journal: Bioorganic & medicinal chemistry letters 20040308

Title: Anti-inflammatory and utero-relaxant effects in human myometrium of new generation phosphodiesterase 4 inhibitors.

Journal: Biology of reproduction 20040201

Title: Anti-inflammatory potential of the selective phosphodiesterase 4 inhibitor N-(3,5-dichloro-pyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), in human cell preparations.

Journal: The Journal of pharmacology and experimental therapeutics 20040201

Title: Highly potent PDE4 inhibitors with therapeutic potential.

Journal: Bioorganic & medicinal chemistry letters 20040105

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20040101

Title: [Phosphosdiesterase 4 inhibitors in the treatment of pulmonary diseases].

Journal: Zhonghua jie he he hu xi za zhi = Zhonghua jiehe he huxi zazhi = Chinese journal of tuberculosis and respiratory diseases 20040101

Title: Effects of cilomilast on dendritic cell function in contact sensitivity and dendritic cell migration through skin.

Journal: European journal of pharmacology 20031128

Title: Antiinflammatory effects of the phosphodiesterase-4 inhibitor cilomilast (Ariflo) in chronic obstructive pulmonary disease.

Journal: American journal of respiratory and critical care medicine 20031015

Title: Phosphodiesterase 4 inhibitors: antiinflammatory therapy for chronic obstructive pulmonary disease at last?

Journal: American journal of respiratory and critical care medicine 20031015

Title: In vivo efficacy in airway disease models of N-(3,5-dichloropyrid-4-yl)-[1-(4-fluorobenzyl)-5-hydroxy-indole-3-yl]-glyoxylic acid amide (AWD 12-281), a selective phosphodiesterase 4 inhibitor for inhaled administration.

Journal: The Journal of pharmacology and experimental therapeutics 20031001

Title: AWD 12-281, a highly selective phosphodiesterase 4 inhibitor, is effective in the prevention and treatment of inflammatory reactions in a model of allergic dermatitis.

Journal: The Journal of pharmacy and pharmacology 20030801

Title: Effect of cilomilast (Ariflo) on TNF-alpha, IL-8, and GM-CSF release by airway cells of patients with COPD.

Journal: Thorax 20030701

Title: Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.

Journal: Journal of medicinal chemistry 20030508

Title: Inhibitor binding to type 4 phosphodiesterase (PDE4) assessed using [3H]piclamilast and [3H]rolipram.

Journal: The Journal of pharmacology and experimental therapeutics 20030501

Title: [Physiopathology of COPD: choosing the right therapeutic targets].

Journal: Revue de pneumologie clinique 20030401

Title: Does a single dose of the phosphodiesterase 4 inhibitor, cilomilast (15 mg), induce bronchodilation in patients with chronic obstructive pulmonary disease?

Journal: Pulmonary pharmacology & therapeutics 20030101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20030101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20030101

Title: Therapy for chronic obstructive pulmonary disease in the 21st century.

Journal: Drugs 20030101

Title: Phosphodiesterase-4 inhibitors in the treatment of inflammatory lung disease.

Journal: Drugs 20030101

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20021101

Title: Crystal structure of phosphodiesterase 4D and inhibitor complex(1).

Journal: FEBS letters 20021023

Title: Phosphodiesterase 4 inhibitor cilomilast inhibits fibroblast-mediated collagen gel degradation induced by tumor necrosis factor-alpha and neutrophil elastase.

Journal: American journal of respiratory cell and molecular biology 20021001

Title: Gateways to clinical trials.

Journal: Methods and findings in experimental and clinical pharmacology 20021001

Title: Benefit of phosphodiesterase 4 inhibitors as supplemental therapy after lung transplantation concerning their antiproliferative effects: an experimental study using a heterotopic rodent model.

Journal: Transplantation 20020815

Title: Pharmacology of N-(3,5-dichloro-1-oxido-4-pyridinyl)-8-methoxy-2-(trifluoromethyl)-5-quinoline carboxamide (SCH 351591), a novel, orally active phosphodiesterase 4 inhibitor.

Journal: The Journal of pharmacology and experimental therapeutics 20020701

Title: Effects of the phosphodiesterase 4 inhibitors SB 207499 and AWD 12-281 on the inflammatory reaction in a model of allergic dermatitis.

Journal: European journal of pharmacology 20020620

Title: Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.

Journal: Journal of medicinal chemistry 20020606

Title: Novel selective phosphodiesterase (PDE4) inhibitors. 4. Resolution, absolute configuration, and PDE4 inhibitory activity of cis-tetra- and cis-hexahydrophthalazinones.

Journal: Journal of medicinal chemistry 20020606

Title: Discovery of L-791,943: a potent, selective, non emetic and orally active phosphodiesterase-4 inhibitor.

Journal: Bioorganic & medicinal chemistry letters 20020603

Title: PDE4 inhibitors attenuate fibroblast chemotaxis and contraction of native collagen gels.

Journal: American journal of respiratory cell and molecular biology 20020601

Title: Phosphodiesterase 4 inhibitors for the treatment of COPD.

Journal: Chest 20020501

Title: Pharmacological profile of a novel phosphodiesterase 4 inhibitor, 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridin-6-yl)-benzoic acid (NVP-ABE171), a 1,7-naphthyridine derivative, with anti-inflammatory activities.

Journal: The Journal of pharmacology and experimental therapeutics 20020401

Title: Synthesis and biological evaluation of imidazol-2-one and 2-cyanoiminoimidazole derivatives: novel series of PDE4 inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20020225

Title: Development status of second generation PDE4 inhibitors for asthma and COPD: the story so far.

Journal: Monaldi archives for chest disease = Archivio Monaldi per le malattie del torace 20020201

Title: Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.

Journal: Bioorganic & medicinal chemistry letters 20020121

Title: Cyclic AMP-specific phosphodiesterase 4 inhibitors promote ABCA1 expression and cholesterol efflux.

Journal: Biochemical and biophysical research communications 20020118

Title: Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.

Journal: Bioorganic & medicinal chemistry letters 20020107

Title: Update on the therapeutic potential of PDE4 inhibitors.

Journal: Expert opinion on investigational drugs 20020101

Title: Cilomilast (Ariflo) does not potentiate the cardiovascular effects of inhaled salbutamol.

Journal: Pulmonary pharmacology & therapeutics 20020101

Title: Warfarin pharmacodynamics unaffected by cilomilast.

Journal: The Annals of pharmacotherapy 20011201

Title: Effects of inhibition of PDE4 and TNF-alpha on local and remote injuries following ischaemia and reperfusion injury.

Journal: British journal of pharmacology 20011101

Title: Cilomilast: a breath of relief?

Journal: Trends in molecular medicine 20011001

Title: An overview of the pharmacokinetics of cilomilast (Ariflo), a new, orally active phosphodiesterase 4 inhibitor, in healthy young and elderly volunteers.

Journal: Journal of clinical pharmacology 20010901

Title: Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.

Journal: Journal of medicinal chemistry 20010802

Title: Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.

Journal: Journal of medicinal chemistry 20010802

Title: The next generation of PDE4 inhibitors.

Journal: Current opinion in chemical biology 20010801

Title: Cilomilast, a selective phosphodiesterase-4 inhibitor for treatment of patients with chronic obstructive pulmonary disease: a randomised, dose-ranging study.

Journal: Lancet (London, England) 20010728

Title: Cilomilast: a second generation phosphodiesterase 4 inhibitor for asthma and chronic obstructive pulmonary disease.

Journal: Expert opinion on investigational drugs 20010701

Title: Bioavailability of the oral selective phosphodiesterase 4 inhibitor cilomilast.

Journal: Pharmacotherapy 20010601

Title: Cilomilast: pharmacokinetic and pharmacodynamic interactions with digoxin.

Journal: Clinical therapeutics 20010601

Title: Requirement of additional adenylate cyclase activation for the inhibition of human eosinophil degranulation by phosphodiesterase IV inhibitors.

Journal: European journal of pharmacology 20010406

Title: Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro.

Journal: The Journal of pharmacology and experimental therapeutics 20010401

Title: In vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor.

Journal: The Journal of pharmacology and experimental therapeutics 20010401

Title: Syntheses and evaluation of pyrido[2,3-dlpyrimidine-2,4-diones as PDE 4 inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20010312

Title: Phthalazine PDE4 inhibitors. Part 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.

Journal: Bioorganic & medicinal chemistry letters 20010108

Title: Comparison of PDE 4 inhibitors, rolipram and SB 207499 (ariflo), in a rat model of pulmonary neutrophilia.

Journal: Pulmonary pharmacology & therapeutics 20010101

Title: Ariflo (SB 207499), a second generation phosphodiesterase 4 inhibitor for the treatment of asthma and COPD: from concept to clinic.

Journal: Pulmonary pharmacology & therapeutics 19990101

Title: SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo.

Journal: The Journal of pharmacology and experimental therapeutics 19981101

Title: SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions.

Journal: The Journal of pharmacology and experimental therapeutics 19980101

Title: Griswold DE, et, al. SB 207499 (Ariflo), a second generation phosphodiesterase 4 inhibitor, reduces tumor necrosis factor alpha and interleukin-4 production in vivo. J Pharmacol Exp Ther. 1998 Nov;287(2):705-11.

Title: Hatzelmann A, et, al. Anti-inflammatory and immunomodulatory potential of the novel PDE4 inhibitor roflumilast in vitro. J Pharmacol Exp Ther. 2001 Apr;297(1):267-79.

Title: Barnette MS, et, al. SB 207499 (Ariflo), a potent and selective second-generation phosphodiesterase 4 inhibitor: in vitro anti-inflammatory actions. J Pharmacol Exp Ther. 1998 Jan;284(1):420-6.

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