PMID

Data

Article Title

Organization

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

The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.

Smithkline Beecham Pharmaceuticals

New bronchodilators. 3. Imidazo[4,5-c][1,8]naphthyridin-4(5H)-ones.

Kyowa Hakko Kogyo

New 5H-pyridazino[4,5-b]indole derivatives. Synthesis and studies as inhibitors of blood platelet aggregation and inotropics.

Universidad De Navarra

Synthesis and cardiotonic activity of novel biimidazoles.

Merrell Dow Research Institute

Synthesis of a tritium-labeled indolidan analogue and its use as a radioligand for phosphodiesterase-inhibitor cardiotonic binding sites.

Eli Lilly

Inhibitors of cyclic AMP phosphodiesterase. 4. Synthesis and evaluation of potential prodrugs of lixazinone (N-cyclohexyl-N-methyl-4-[(1,2,3,5-tetrahydro-2- oxoimidazo[2,1-b]quinazolin-7-yl)-oxy]butyramide, RS-82856).

Syntex Research

Cardiotonic agents. 2. (Imidazolyl)aroylimidazolones, highly potent and selective positive inotropic agents.

TBA

2-(beta-Arylethylamino)- and 4-(beta-arylethylamino)quinazolines as phosphodiesterase inhibitors.

TBA

Orally active PDE4 inhibitors with therapeutic potential.

Minase Research Institute

New orally active PDE4 inhibitors with therapeutic potential.

Minase Research Institute

Highly potent PDE4 inhibitors with therapeutic potential.

Minase Research Institute

3D-QSAR studies on thieno[3,2-d]pyrimidines as phosphodiesterase IV inhibitors.

National Institute Of Pharmaceutical Education And Research (Niper)

Comparative molecular field analysis (CoMFA) of phthalazine derivatives as phosphodiesterase IV inhibitors.

National Institute Of Pharmaceutical Education And Research

Synthesis and biological activities of 1-pyridylisoquinoline and 1-pyridyldihydroisoquinoline derivatives as PDE4 inhibitors.

Tanabe Seiyaku

7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.

Celltech R&D

Synthesis and profile of SCH351591, a novel PDE4 inhibitor.

Schering-Plough

8-Methoxyquinolines as PDE4 inhibitors.

Schering-Plough

8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.

Celltech R&D

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

Zambon Group

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

Zambon Group

Synthesis and biological evaluation of 2,5-dihydropyrazol.

RhôNe-Poulenc Rorer

The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.

Zambon Group

7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.

Celltech-Chiroscience

Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.

Institut De Recherche Jouveinal-Parke Davis

Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds.

RhôNe-Poulenc Rorer

Quaternary substituted PDE IV inhibitors II: the synthesis and in vitro evaluation of a novel series of gamma-lactams.

Rh£Ne-Poulenc Rorer Central Research

Orally active indole N-oxide PDE4 inhibitors.

Rh£Ne-Poulenc Rorer Central Research

PDE4 inhibitors: new xanthine analogues.

Chiroscience

Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles.

Rh£Ne-Poulenc Rorer Central Research

Thalidomide analogs and PDE4 inhibition.

Celgene

2-Substituted-4-methoxybenzimidazole-based PDE4 inhibitors.

Rh£Ne-Poulenc Rorer

Synthesis and evaluation of a novel series of phosphodiesterase IV inhibitors. A potential treatment for asthma.

Chiroscience

The synthesis and biological evaluation of a novel series of indole PDE4 inhibitors I.

Rh£Ne-Poulenc Rorer Central Research

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

Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors.

Sanofi Research Center

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

Southern Medical University

Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.

Bristol-Myers Squibb R & D

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

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.

Merck Research Laboratories

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

Janssen Pharmaceutica

Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.

Merck Serono

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

The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.

Monash University (Parkville Campus)

Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.

Tanabe Seiyaku

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

Novel, potent, and selective phosphodiesterase-4 inhibitors as antiasthmatic agents: synthesis and biological activities of a series of 1-pyridylnaphthalene derivatives.

Tanabe Seiyaku

Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.

Smithkline Beecham Pharmaceuticals

1,7- and 2,7-naphthyridine derivatives as potent and highly specific PDE5 inhibitors.

Tanabe Seiyaku

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 Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAgg^III conditions

TBA

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

New substituted triaza-benzo[cd]azulen-9-ones as promising phosphodiesterase-4 inhibitors.

Pfizer

The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione analogues.

Glaxosmithkline

Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.

Bayer

Discovery of novel potent imidazo[1,2-b]pyridazine PDE10a inhibitors.

Janssen Research & Development

Solid-phase synthesis of an arylsulfone hydroxamate library.

Rhone-Poulenc Rorer

PDEStrIAn: A Phosphodiesterase Structure and Ligand Interaction Annotated Database As a Tool for Structure-Based Drug Design.

Vrije Universiteit Amsterdam

Synthesis and evaluation of clioquinol-rolipram/roflumilast hybrids as multitarget-directed ligands for the treatment of Alzheimer's disease.

Sun Yat-Sen University

Identification of

TBA

Lead Optimization of Phthalazinone Phosphodiesterase Inhibitors as Novel Antitrypanosomal Compounds.

University Of Antwerp

Discovery and Optimization of ?-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia.

Guangzhou University Of Chinese Medicine

Structure-Aided Identification and Optimization of Tetrahydro-isoquinolines as Novel PDE4 Inhibitors Leading to Discovery of an Effective Antipsoriasis Agent.

Shanghai Institute Of Materia Medica

Pharmacokinetics-Driven Optimization of 4(3 H)-Pyrimidinones as Phosphodiesterase Type 5 Inhibitors Leading to TPN171, a Clinical Candidate for the Treatment of Pulmonary Arterial Hypertension.

Chinese Academy Of Sciences

Design and Synthesis of Selective Phosphodiesterase 4D (PDE4D) Allosteric Inhibitors for the Treatment of Fragile X Syndrome and Other Brain Disorders.

Tetra Discovery Partners

InCl

University Of Hyderabad Campus

Dual functional cholinesterase and PDE4D inhibitors for the treatment of Alzheimer's disease: Design, synthesis and evaluation of tacrine-pyrazolo[3,4-b]pyridine hybrids.

Sun Yat-Sen University

Discovery of Potent, Selective, and Orally Bioavailable Inhibitors against Phosphodiesterase-9, a Novel Target for the Treatment of Vascular Dementia.

Sun Yat-Sen University

1-Arylnaphthalene lignan: a novel scaffold for type 5 phosphodiesterase inhibitor.

Tanabe Seiyaku

Discovery of a Brain-Penetrant ATP-Competitive Inhibitor of the Mechanistic Target of Rapamycin (mTOR) for CNS Disorders.

Novartis Institutes For Biomedical Research

Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.

Abbvie Deutschland

Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.

Changzhou University

Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.

Novartis Pharma

Aryl sulfonamides as selective PDE4 inhibitors.

Chiroscience

Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor.

Rti International

Validation of Phosphodiesterase-10 as a Novel Target for Pulmonary Arterial Hypertension via Highly Selective and Subnanomolar Inhibitors.

Sun Yat-Sen University

Design and Identification of a Novel, Functionally Subtype Selective GABA

Pfizer

Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).

Vrije Universiteit Amsterdam

Discovery of a pyrazolo[1,5-a]pyrimidine derivative (MT-3014) as a highly selective PDE10A inhibitor via core structure transformation from the stilbene moiety.

Mitsubishi Tanabe Pharma

Structure Overhaul Affords a Potent Purine PI3K? Inhibitor with Improved Tolerability.

TBA

Molecular Networking Reveals the Chemical Diversity of Selaginellin Derivatives, Natural Phosphodiesterase-4 Inhibitors from

Seoul National University

Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGF?R1 Inhibitor as an Immuno-oncology Agent.

Bristol-Myers Squibb Research & Development

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

Discovery of novel inhibitors of phosphodiesterase 4 with 1-phenyl-3,4-dihydroisoquinoline scaffold: Structure-based drug design and fragment identification.

South China Agricultural University

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

Bronchodilator activity of xanthine derivatives substituted with functional groups at the 1- or 7-position.

Hokuriku University

Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A).

Amgen

Identification of 2,3-disubstituted pyridines as potent, non-emetic PDE4 inhibitors.

Dainippon Sumitomo Pharma

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

Kyushu University

Novel class of benzoic acid ester derivatives as potent PDE4 inhibitors for inhaled administration in the treatment of respiratory diseases.

Chiesi Farmaceutici

Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.

Pfizer

1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.

Celgene

Functionalized pyrazoles and pyrazolo[3,4-d]pyridazinones: Synthesis and evaluation of their phosphodiesterase 4 inhibitory activity.

Universit£

Design of small-sized libraries by combinatorial assembly of linkers and functional groups to a given scaffold: application to the structure-based optimization of a phosphodiesterase 4 inhibitor.

Umr Cnrs 7081

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

Vrije Universiteit

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

Vrije Universiteit

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

Vrije Universiteit

Pyrazolopyrimidine-2,4-dione sulfonamides: novel and selective calcitonin inducers.

Wyeth Research

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

Vrije Universiteit

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

Vrije Universiteit

Novel and selective calcitonin-inducing agents.

Wyeth-Ayerst Research

Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase type 4 inhibitors.

Pfizer

1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.

Smithkline Beecham Pharmaceuticals

Synthesis of 7-benzylamino-6-chloro-2-piperazino-4-pyrrolidinopteridine and novel derivatives free of positional isomers. Potent inhibitors of cAMP-specific phosphodiesterase and of malignant tumor cell growth.

University Of Kaiserslautern

Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.

Sw 8 Rh£Ne-Poulenc Rorer Central Research

Design, synthesis, and biological activities of new thieno[3,2-d] pyrimidines as selective type 4 phosphodiesterase inhibitors.

RhôNe-Poulenc Rorer

7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.

Pfizer

Selective inhibitors of cyclic AMP-specific phosphodiesterase: heterocycle-condensed purines.

Hokuriku University

Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.

Dipartimento Di Scienze Farmaceutiche, Firenze, Italy.

Biarylcarboxylic acids and -amides: inhibition of phosphodiesterase type IV versus [3H]rolipram binding activity and their relationship to emetic behavior in the ferret.

Pfizer

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£

Inhibition of cyclic adenosine-3',5'-monophosphate phosphodiesterase from vascular smooth muscle by rolipram analogues.

Centre De Neurochimie Du Cnrs

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

Effects of alkyl substitutions of xanthine skeleton on bronchodilation.

Hokuriku University

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