PMID

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Article Title

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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

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 of a potent, selective, and orally active phosphodiesterase 10A inhibitor for the potential treatment of schizophrenia.

Janssen Pharmaceutica

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

Monash University (Parkville Campus)

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

Novel pyrazolopyrimidopyridazinones with potent and selective phosphodiesterase 5 (PDE5) inhibitory activity as potential agents for treatment of erectile dysfunction.

Università

Tuberculosis Drug Discovery: Challenges and New Horizons.

University College London

Therapeutic potential of phosphodiesterase inhibitors for cognitive amelioration in Alzheimer's disease.

Shaoxing University

Structural modification aimed for improving solubility of lead compounds in early phase drug discovery.

Indian Institute of Technology (B.H.U.)

Discovery of novel N-1 substituted pyrazolopyrimidinones as potent, selective PDE2 inhibitors.

Merck

Quinolines as extremely potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.

Bristol-Myers Squibb Pharmaceutical Research Institute

Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.

Pfizer

Novel PDE5 inhibitors derived from rutaecarpine for the treatment of Alzheimer's disease.

Changzhou University

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

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

Exploration of the 5-bromopyrimidin-4(3H)-ones as potent inhibitors of PDE5.

Chinese Academy of Sciences

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