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Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension.

Sun Yat-Sen University

Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.

Dart Neuroscience

Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.

Dart Neuroscience

Design, synthesis and biological evaluation of 2,4-disubstituted oxazole derivatives as potential PDE4 inhibitors.

South China Agricultural University

Development of highly potent phosphodiesterase 4 inhibitors with anti-neuroinflammation potential: Design, synthesis, and structure-activity relationship study of catecholamides bearing aromatic rings.

Southern Medical University

Design and synthesis of potent and selective pyridazin-4(1H)-one-based PDE10A inhibitors interacting with Tyr683 in the PDE10A selectivity pocket.

Takeda Pharmaceutical

Discovery and modelling studies of natural ingredients from Gaultheria yunnanensis (FRANCH.) against phosphodiesterase-4.

Sun Yat-Sen University

Development of thieno- and benzopyrimidinone inhibitors of the Hedgehog signaling pathway reveals PDE4-dependent and PDE4-independent mechanisms of action.

Vanderbilt University School of Medicine

Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

Mercachem

Catecholic amides as potential selective phosphodiesterase 4D inhibitors: Design, synthesis, pharmacological evaluation and structure-activity relationships.

Southern Medical University

Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD).

Novartis Institutes For Biomedical Research

Synthesis, biological activities and pharmacokinetic properties of new fluorinated derivatives of selective PDE4D inhibitors.

University of Genoa

Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors.

Janssen Pharmaceutica

Synthesis, biological evaluation, and molecular modeling of new 3-(cyclopentyloxy)-4-methoxybenzaldehyde O-(2-(2,6-dimethylmorpholino)-2-oxoethyl) Oxime (GEBR-7b) related phosphodiesterase 4D (PDE4D) inhibitors.

University of Genoa

Discovery of triazines as selective PDE4B versus PDE4D inhibitors.

Northern Illinois University

Discovery and early clinical development of 2-{6-[2-(3,5-dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a soft-drug inhibitor of phosphodiesterase 4 for topical treatment of atopic dermatitis.

Leo Pharma

Prostaglandin Derivatives: Nonaromatic Phosphodiesterase-4 Inhibitors from the Soft Coral Sarcophyton ehrenbergi.

Sun Yat-Sen University

Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.

TBA

Modulation of cAMP-specific PDE without emetogenic activity: new sulfide-like PDE7 inhibitors.

Centro De Investigaciones Biol�Gicas (Csic)

Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.

Janssen Pharmaceutica

Novel Roflumilast analogs as soft PDE4 inhibitors.

Amakem

Efficacious inhaled PDE4 inhibitors with low emetic potential and long duration of action for the treatment of COPD.

Astrazeneca

Prenylated coumarins: natural phosphodiesterase-4 inhibitors from Toddalia asiatica.

Sun Yat-Sen University

N-arylrolipram derivatives as potent and selective PDE4 inhibitors.

Novartis Horsham Research Center

Discovery of novel 1,4-dihydropyridine-based PDE4 inhibitors.

University of Hyderabad Campus

Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.

Amgen

Structure-based discovery of highly selective phosphodiesterase-9A inhibitors and implications for inhibitor design.

Sun Yat-Sen University

Catechol pyrazolinones as trypanocidals: fragment-based design, synthesis, and pharmacological evaluation of nanomolar inhibitors of trypanosomal phosphodiesterase B1.

Vu University Amsterdam

Imidazopyridazinones as novel PDE7 inhibitors: SAR and in vivo studies in Parkinson's disease model.

Glenmark Pharmaceuticals

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

Universidade Federal Do Rio De Janeiro

Solubility-driven optimization of phosphodiesterase-4 inhibitors leading to a clinical candidate.

Novartis Institutes For Biomedical Research

Effect of phosphodiesterase 7 (PDE7) inhibitors in experimental autoimmune encephalomyelitis mice. Discovery of a new chemically diverse family of compounds.

Instituto De Qu£Mica M£Dica (Csic)

Moracin M from Morus alba L. is a natural phosphodiesterase-4 inhibitor.

Sun Yat-Sen University

Discovery of oxazole-based PDE4 inhibitors with picomolar potency.

Merck Research Laboratories

In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.

King'S College London

Stereoselective inhibition of serotonin re-uptake and phosphodiesterase by dual inhibitors as potential agents for depression.

Human Biomolecular Research Institute

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

Matrix Laboratories

Potent and selective xanthine-based inhibitors of phosphodiesterase 5.

Novartis Institutes of Biomedical Research

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.

Pfizer

Discovery of a substituted 8-arylquinoline series of PDE4 inhibitors: structure-activity relationship, optimization, and identification of a highly potent, well tolerated, PDE4 inhibitor.

Merck Frosst Centre For Therapeutic Research

Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.

Novartis Pharma

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.

Novartis Pharma

Thiophene inhibitors of PDE4: crystal structures show a second binding mode at the catalytic domain of PDE4D2.

Monash University (Parkville Campus)

Synthesis and biological activity of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel and potent phosphodiesterase type 4 inhibitors.

RhôNe-Poulenc Rorer

Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment.

Merck Frosst Centre For Therapeutic Research

Discovery of selective PDE4B inhibitors.

Asahi Kasei Pharma

Triazoloquinazolines as a novel class of phosphodiesterase 10A (PDE10A) inhibitors.

H. Lundbeck

Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors.

Universit£

Synthesis and biological activity of pyrido[3',2':4,5]thieno[3,2-d]pyrimidines as phosphodiesterase type 4 inhibitors.

RhôNe-Poulenc Rorer

Spiroindolones, a potent compound class for the treatment of malaria.

Swiss Tropical and Public Health Institute

The discovery and synthesis of highly potent subtype selective phosphodiesterase 4D inhibitors.

Merck Frosst Centre For Therapeutic Research

Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors.

Pfizer

Surface plasmon resonance-based detection of ladder-shaped polyethers by inhibition detection method.

Osaka University

Design, synthesis, and evaluation of 2-aryl-7-(3',4'-dialkoxyphenyl)-pyrazolo[1,5-a]pyrimidines as novel PDE-4 inhibitors.

Korea Research Institute of Chemical Technology

Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).

Pfizer

Synthesis and biological evaluation of novel phthalazinone derivatives as topically active phosphodiesterase 4 inhibitors.

Kyoto 601-8550

Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.

Pfizer

New selective phosphodiesterase 4D inhibitors differently acting on long, short, and supershort isoforms.

University of Genoa

The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.

Pfizer

Design, synthesis, and structure-activity relationship, molecular modeling, and NMR studies of a series of phenyl alkyl ketones as highly potent and selective phosphodiesterase-4 inhibitors.

Georgia State University

Succinyl hydroxamates as potent and selective non-peptidic inhibitors of procollagen C-proteinase: design, synthesis, and evaluation as topically applied, dermal anti-scarring agents.

Pfizer

Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.

Merck Frosst Center For Therapeutic Research

A new chemical tool for exploring the physiological function of the PDE2 isozyme.

Pfizer

A new chemical tool for exploring the role of the PDE4D isozyme in leukocyte function.

Pfizer

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.

Pfizer

Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.

Pfizer

Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.

Pfizer

Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.

Novartis Pharma

Striking effect of hydroxamic acid substitution on the phosphodiesterase type 4 (PDE4) and TNF alpha inhibitory activity of two series of rolipram analogues: implications for a new active site model of PDE4.

Pfizer

Design, Synthesis, and Evaluation of Orally Available Clioquinol-Moracin M Hybrids as Multitarget-Directed Ligands for Cognitive Improvement in a Rat Model of Neurodegeneration in Alzheimer's Disease.

Sun Yat-Sen University

Identification of the 5,5-dioxo-7,8-dihydro-6H-thiopyrano[3,2-d]pyrimidine derivatives as highly selective PDE4B inhibitors.

Kyushu University

Lead-like Drugs: A Perspective.

Pfizer

Tetrahydroquinoline and tetrahydroisoquinoline derivatives as potential selective PDE4B inhibitors.

South China Agricultural University

Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors.

South China Agricultural University

Design, synthesis, and biological evaluation of novel catecholopyrimidine based PDE4 inhibitor for the treatment of atopic dermatitis.

Seoul National University

Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension.

Sun Yat-Sen University

Synthesis and molecular docking of new roflumilast analogues as preferential-selective potent PDE-4B inhibitors with improved pharmacokinetic profile.

Cairo University

Novel butanehydrazide derivatives of purine-2,6-dione as dual PDE4/7 inhibitors with potential anti-inflammatory activity: Design, synthesis and biological evaluation.

Jagiellonian University

Novel Phosphodiesterase Inhibitors for Cognitive Improvement in Alzheimer's Disease.

Sun Yat-Sen University

Structure-based design and structure-activity relationships of 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.

South China Agricultural University

Synthesis and biological evaluation of pyridazinone derivatives as potential anti-inflammatory agents.

Universit£

Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.

Sun Yat-Sen University

Selective Inhibitors of Phosphodiesterase 4B (PDE-4B) May Provide a Better Treatment for CNS, Metabolic, Autoimmune, and Inflammatory Diseases.

Therachem Research Medilab (India)

Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.

Novartis Institutes For Biomedical Research

Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1.

Pfizer

Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy.

Astrazeneca

Rational design of conformationally constrained oxazolidinone-fused 1,2,3,4-tetrahydroisoquinoline derivatives as potential PDE4 inhibitors.

South China Agricultural University

Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.

Takeda Pharmaceutical

Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.

Takeda Pharmaceutical

Discovery of N-{4-[5-(4-Fluorophenyl)-3-methyl-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-acetamide (CBS-3595), a Dual p38? MAPK/PDE-4 Inhibitor with Activity against TNF?-Related Diseases.

C-A-I-R Biosciences

Fragment-Based Drug Discovery of Phosphodiesterase Inhibitors.

Iota Pharmaceuticals

Nitrocinnamoyl and chlorocinnamoyl derivatives of dihydrocodeinone: in vivo and in vitro characterization of mu-selective agonist and antagonist activity.

University of Rochester

Cloning and expression of a human serotonin 5-HT4 receptor cDNA.

Janssen Research Foundation

5-Hydroxytryptamine receptors with a 5-HT6 receptor-like profile stimulating adenylyl cyclase activity in pig caudate membranes.

Sandoz Pharma

Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.

Seoul National University

A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.

Genentech

Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a

Upjohn