PMID

Data

Article Title

Organization

Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.

Pfizer

Design and discovery of 6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one (PF-04447943), a selective brain penetrant PDE9A inhibitor for the treatment of cognitive disorders.

Pfizer

Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.

Pfizer

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

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

Identification of a brain penetrant PDE9A inhibitor utilizing prospective design and chemical enablement as a rapid lead optimization strategy.

Pfizer

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

Pfizer

Discovery of novel PDE4 inhibitors targeting the M-pocket from natural mangostanin with improved safety for the treatment of Inflammatory Bowel Diseases.

Guangzhou University of Chinese Medicine

Identification of Novel Quinolin-2(1

Sun Yat-Sen University

Advances in Cyclic Nucleotide Phosphodiesterase-Targeted PET Imaging and Drug Discovery.

Massachusetts General Hospital

The long and winding road of designing phosphodiesterase inhibitors for the treatment of heart failure.

Rural Federal University of Rio De Janeiro

Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects.

Sun Yat-Sen University

Discovery of Potent Phosphodiesterase-9 Inhibitors for the Treatment of Hepatic Fibrosis.

Sun Yat-Sen University

Mangostanin Derivatives as Novel and Orally Active Phosphodiesterase 4 Inhibitors for the Treatment of Idiopathic Pulmonary Fibrosis with Improved Safety.

Hainan University

Design, synthesis and biological evaluation of novel benzoxaborole derivatives as potent PDE4 inhibitors for topical treatment of atopic dermatitis.

China Pharmaceutical University

Discovery of Novel Selective and Orally Bioavailable Phosphodiesterase-1 Inhibitors for the Efficient Treatment of Idiopathic Pulmonary Fibrosis.

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

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

Sun Yat-Sen University

Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.

Smithkline Beecham Pharmaceuticals

Synthesis and characterization of novel classes of PDE10A inhibitors - 1H-1,3-benzodiazoles and imidazo[1,2-a]pyrimidines.

Celon Pharma

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

Pfizer

Spirocyclic compounds

C4 Therapeutics

Compositions and methods for treating CNS disorders

Sage Therapeutics

Substituted piperidine compounds and their use

Eisai R&D Management

Substituted macrocyclic indole derivatives

Bayer Aktiengesellschaft

Piperazine derivatives as MAGL inhibitors

Hoffmann-La Roche

Substituted pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines as tyrosine kinase inhibitors

Shenzhen Targetrx

Substituted pyridines as TYK2 inhibitors

Esker Therapeutics

Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit MNK1 and MNK2

Effector Therapeutics

Piperidines as menin inhibitors

The Regents of The University of Michigan

Inhibitors of cyclin-dependent kinases

Kinnate Biopharma

Substituted benzofuran, benzothiophene and indole Mcl-1 inhibitors

Vanderbilt University

Inhibitors of TRPC6

Boehringer Ingelheim International

HIV protease inhibitors

Gilead Sciences

Pyrrolopyrimidine comprising cyclopentyl substituent

Centaurus Biopharma

Tricyclic compounds as inhibitors of mutant IDH enzymes

Merck Sharp & Dohme

Oxime-based compound, pharmaceutical composition containing the same and method for preparing the same

Chang Gung University

Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.

Paris-Sud University

Structure-based discovery and in-parallel optimization of novel competitive inhibitors of thymidylate synthase.

Northwestern University