PMID
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Article Title
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Discovery of Potent and Selective Inhibitors of Phosphodiesterase 1 for the Treatment of Cognitive Impairment Associated with Neurodegenerative and Neuropsychiatric Diseases.

Intra-Cellular Therapies
Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders.

Intra-Cellular Therapies
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.

Incyte
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis.

Bristol-Myers Squibb
Novel ligands lacking a positive charge for the delta- and mu-opioid receptors.

Clinical Research Institute of Montr£Al
An orally bioavailable pyrrolinone inhibitor of HIV-1 protease: computational analysis and X-ray crystal structure of the enzyme complex.

University of Pennsylvania
Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.

University of Pennsylvania
Discovery of novel alpha7 nicotinic receptor antagonists.

Intra-Cellular Therapies
Compelling P1 substituent affect on metalloprotease binding profile enables the design of a novel cyclohexyl core scaffold with excellent MMP selectivity and HER-2 sheddase inhibition.

Incyte
Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations.

Incyte
Design and identification of selective HER-2 sheddase inhibitors via P1' manipulation and unconventional P2' perturbations to induce a molecular metamorphosis.

Incyte
Discovery of (4-Pyrazolyl)-2-aminopyrimidines as Potent and Selective Inhibitors of Cyclin-Dependent Kinase 2.

Incyte
Discovery of ITI-333, a Novel Orally Bioavailable Molecule Targeting Multiple Receptors for the Treatment of Pain and Other Disorders.

Intra-Cellular Therapies, Inc.
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.

Incyte
Discovery of Orally Bioavailable FGFR2/FGFR3 Dual Inhibitors via Structure-Guided Scaffold Repurposing Approach.

Incyte
Potent and Selective Biaryl Amide Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).

Incyte Research Institute
Discovery of Pyrazolopyridine Derivatives as HPK1 Inhibitors.

Incyte Research Institute
Inhibition of ALK2 with bicyclic pyridyllactams.

Incyte
Discovery of 5,7-Dihydro-6

Incyte
Discovery of 1'-(1-phenylcyclopropane-carbonyl)-3H-spiro[isobenzofuran-1,3'-pyrrolidin]-3-one as a novel steroid mimetic scaffold for the potent and tissue-specific inhibition of 11β-HSD1 using a scaffold-hopping approach.

Incyte Research Institute
Development of an Orally Active Small-Molecule Inhibitor of Receptor Activator of Nuclear Factor-κB Ligand.

Shanghai Institute of Traumatology and Orthopaedics
Discovery of Novel Pyrazolopyrimidines as Potent, Selective, and Orally Bioavailable Inhibitors of ALK2.

Incyte
Discovery of a novel 2-spiroproline steroid mimetic scaffold for the potent inhibition of 11β-HSD1.

Incyte Research Institute
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3.

Prelude Therapeutics
Discovery of Pemigatinib: A Potent and Selective Fibroblast Growth Factor Receptor (FGFR) Inhibitor.

Incyte
Potent and selective aggrecanase inhibitors containing cyclic P1 substituents.

Bristol-Myers Squibb Pharmaceutical Research Institute
Discovery of First-In-Class Potent and Selective Tropomyosin Receptor Kinase Degraders.

Cullgen (Shanghai)
Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

Bristol-Myers Squibb Pharma
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.

Procter & Gamble Pharmaceuticals
Design and synthesis of a series of (2R)-N(4)-hydroxy-2-(3-hydroxybenzyl)-N(1)- [(1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl]butanediamide derivatives as potent, selective, and orally bioavailable aggrecanase inhibitors.

Dupont Pharmaceuticals
Unravel a neuroactive sHA sulfation pattern with neurogenesis activity by a library of defined oligosaccharides.

Peking University
INCB050465 (Parsaclisib), a Novel Next-Generation Inhibitor of Phosphoinositide 3-Kinase Delta (PI3Kδ).

Incyte
Modulation of receptor and receptor subtype affinities using diastereomeric and enantiomeric monosaccharide scaffolds as a means to structural and biological diversity. A new route to ether synthesis.

University of Pennsylvania
3-CYCLOAMINO-INDOLE COMPOUNDS AS SEROTONERGIC AGENTS USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Mindset Pharma
Thiazolopyridyl Amide Derivatives as DNA Polymerase Theta Inhibitors

Beigene
Compounds for modulating S1P1 activity and methods of using the same

Trevena
Discovery of OICR12694: A Novel, Potent, Selective, and Orally Bioavailable BCL6 BTB Inhibitor.

Ontario Institute for Cancer Research
4-ALKOXYPYRROLO[2,1-F][1,2,4]TRIAZINES AND PREPARATION AND USES THEREOF

Biosplice Therapeutics
IRE1α inhibitors and uses thereof

University of California
INHALED FORMULATIONS OF PGDH INHIBITORS AND METHODS OF USE THEREOF

Epirium Bio
Carboxylic acid, acyl sulfonamide and acyl sulfamide-derivatized bicyclic aza-heteroaromatics as selective Mcl-1 inhibitors and as dual Mcl-1/Bcl-2 inhibitors

University of Maryland, Baltimore
Substituted pyrido[2,1-a]isoquinolines as VMAT2 inhibitors

Neurocrine Biosciences
5-substituted difluoropiperidine compounds with blood-brain barrier penetrable capability

Wayshine Biopharm Holding
Compounds and compositions as protein kinase inhibitors

Array Biopharma
4-substitued cytisine analogues

University of Bristol
Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

Astrazeneca
Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists

Hoffmann-La Roche
Substituted 4-phenylpiperidines, their preparation and use

Columbia University
MTORC1 modulators and uses thereof

Aeovian Pharmaceuticals
Psilocin derivatives as serotonergic psychedelic agents for the treatment of CNS disorders

Mindset Pharma
Benzamide compounds

Recurium Ip Holdings
Methods of treatment using 4-(3-cyanophenyl)-6-pyridinylpyrimidine mGlu5 modulators

Heptares Therapeutics
Amino acid compounds and methods of use

Pliant Therapeutics
Indole compounds and analogues thereof

Biocryst Pharmaceuticals
Amide compounds as kinase inhibitors, compositions and methods of treatment

Translational Drug Development
Dihydropyrrolopyridine inhibitors of ROR-gamma

Vitae Pharmaceuticals
Use of known compounds as D-amino acid oxidase inhibitors

National Taiwan University
Indole and azaindole inhibitors of pad enzymes

Bristol-Myers Squibb
Compounds for treatment of PD-L1 diseases

Chemocentryx
Combination of pure 5-HT6 receptor antagonists with acetylcholinesterase inhibitors

Suven Life Sciences
Substituted pyrazolo[1,5-a]pyrimidines as tropomyosin receptor kinase inhibitors

Shenzhen Targetrx
Substituted 1,2,3,4-tetrahydroquinolines as inhibitors of repair enzyme 8-oxoguanine deoxyribonucleic acid glycosylase activity

The Leland Stanford Junior University
Bromodomain inhibitor compound and use thereof

Shanghai Institute of Material Medica, Chinese Academy of Sciences
Immunomodulator compounds

Chemocentryx
Aryl and heteroaryl substituted indole compounds

Bristol-Myers Squibb
Substituted piperidines as kinase inhibitors

Daewoong Pharmaceutical
Biochemical binding of RET9 and VEGFR2 inhibitors

Kala Pharmaceuticals
1,4-substituted isoquinoline inhibitors of KEAP1/NRF2 protein-protein interaction

University of Illinois
Pyrazolopyridines and triazolopyridines as A2A / A2B inhibitors

Incyte
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof

Beijing Tide Pharmaceutical
Heteroaryl plasma kallikrein inhibitors

Takeda Pharmaceutical
Imidopiperidine compounds as inhibitors of human polynucleotide kinase phosphatase

University of Alberta
EIF4E-inhibiting compounds and methods

Effector Therapeutics
Triple combination of pure 5-HT6 receptor antagonists, acetylcholinesterase inhibitors and NMDA receptor antagonist

Suven Life Sciences
Inhibitors of plasma kallikrein

Kalvista Pharmaceuticals
Protein kinase B inhibitors

Astrazeneca
Substituted heterocyclic sulfonamide compounds useful as TRPA1 modulators

Genentech
Cyclin dependent kinase inhibitors

Pfizer
Compositions and methods for treating parasitic diseases

University of California
4-pyrazin-2-ylmethyl-morpholine derivatives and the use thereof as medicament

Boehringer Ingelheim International
Substituted imidazoles as apoptosis signal regulating kinase 1 inhibitors

Jiangsu Hansoh Pharmaceutical Group
C7 substituted oxysterols and methods of use thereof

Sage Therapeutics
Methods for treating GI tract disorders

Neurogastrx
Autotaxin inhibitors

University of Tennessee Research Foundation
4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament

Boehringer Ingelheim International
Pyrazolyl substituted carbonic acid derivatives as modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto

Arena Pharmaceuticals
Ectonucleotidase inhibitors and methods of use thereof

Calithera Biosciences
Aminopyrimidinecarboxamides as CXCR2 modulators

Syntrix Biosystems
7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant IDH1 and IDH2 inhibitors

Eli Lilly
Compounds as autotaxin inhibitors and pharmaceutical compositions comprising the same

Legochem Biosciences
Quinoline and isoquinoline derivatives for treating pain and pain related conditions

Esteve Pharmaceuticals
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-p53 inhibitors

Boehringer Ingelheim International
LRRK2 inhibitors and methods of making and using the same

Dana-Farber Cancer Institute
PD-1/PD-L1 inhibitors

Gilead Sciences
Alpha-D-galactoside inhibitors of galectins

Galecto Biotech
Imidazopyrazine inhibitors of Bruton's tyrosine kinase

Acerta Pharma
Chromane, isochromane and dihydroisobenzofuran derivatives as mGluR2-negative allosteric modulators, compositions, and their use

Merck Sharp & Dohme
Use of agonists of formyl peptide receptor 2 for treating dermatological diseases

Allergan
Bicyclic-fused heteroaryl or aryl compounds

Pfizer
Hormone receptor modulators for treating metabolic conditions and disorders

Ardelyx
Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors

Pfizer
Dopamine D2 receptor ligands

The Broad Institute
Amido spirocyclic amide and sulfonamide derivatives

Forma Tm
2-aminoquinazoline derivatives as P70S6 kinase inhibitors

Sentinel Oncology
Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one compounds and derivatives as MDM2-P53 inhibitors

Boehringer Ingelheim International
Cyclopropylamines as LSD1 inhibitors

Incyte
MALT1 inhibitors and uses thereof

Cornell University
Somatostatin modulators and uses thereof

Crinetics Pharmaceuticals
Cyanopyrrolidines as dub inhibitors for the treatment of cancer

Mission Therapeutics
Bicyclic heterocycles as FGFR4 inhibitors

Incyte
Compounds, compositions and methods

Denali Therapeutics
Tricyclic heterocycles as BET protein inhibitors

Incyte
2,4-disubstituted pyrimidines useful as kinase inhibitors

Celgene Car
Acyl sulfonamide NaV1.7 inhibitors

Bristol-Myers Squibb
1 H-pyrazolo[4,3-B]pyridines as PDE1 inhibitors

H. Lundbeck
WDR5 inhibitors and modulators

Vanderbilt University
Non-aromatic difluoro analogues of resorcylic acid lactones

University of North Carolina At Greensboro
Thienopyrimidine compounds

Hoffmann-La Roche
Enhancer of zeste homolog 2 inhibitors

Glaxosmithkline
Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof

Euroscreen
Inhibitors of Bruton's tyrosine kinase

Hoffmann-La Roche
Substituted azoles, antiviral active component, pharmaceutical composition, method for preparation and use thereof

TBA
Sulfonamide derivatives with therapeutic indications

Pharmos
Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use

Merck Sharp & Dohme
Alpha-(3,5-dimethoxybenzylidene)-alpha′-hydrocarbyl methylene cyclic ketone and preparation method thereof

Pharmaxyn Laboratories
Substituted hetero-azepinones

F. Hoffmann-La Roche
Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics

Galderma Research & Devlopment
Cyanomethylpyrazole carboxamides as janus kinase inhibitors

Merck Sharp & Dohme
Pyrrolo[2,3-B]pyrazines as SYK inhibitors

Hoffmann-La Roche
Delineation of the Pasteurellaceae-specific GbpA-family of glutathione-binding proteins.

Ghent University
A L-lysine transporter of high stereoselectivity of the amino acid-polyamine-organocation (APC) superfamily: production, functional characterization, and structure modeling.

Max Planck Institute of Biophysics
The SUMO1-E67 interacting loop peptide is an allosteric inhibitor of the dipeptidyl peptidases 8 and 9.

Georg-August-University of Goettingen
Amino-substituted imidazopyridazines

Bayer Pharma Aktiengesellschaft
Gamma secretase inhibitors

Merck Sharp & Dohme
Histone deacetylase 6 structure and molecular basis of catalysis and inhibition

University of Pennsylvania
Bicarbocyclic and tricarbocyclic ethynyl derivatives and uses of same

H. Lundbeck
Some Anticancer Agents Act on Human Serum Paraoxonase-1 to Reduce Its Activity.

Ahi Evran University
4-piperidinyl compounds for use as tankyrase inhibitors

Novartis
2-(1,2,3-triazol-2-yl)benzamide and 3-(1,2,3-triazol-2-YL)picolinamide derivatives as orexin receptor antagonists

Actelion Pharmaceuticals
Tri-aryl/heteroaromatic cannabinoids and use thereof

The University of Tennessee Research Foundation
Spiroepoxytriazoles Are Fumagillin-like Irreversible Inhibitors of MetAP2 with Potent Cellular Activity.

German Cancer Research Center (Dkfz)
Novel biphenyl bis-sulfonamides as acetyl and butyrylcholinesterase inhibitors: Synthesis, biological evaluation and molecular modeling studies.

Government College University
2-heteroaryl carboxamides

Bayer Intellectual Property
Method for enhancing anti-tumor effect of a microtubule-targeting drug, and a method for treatment of tumor

Taiho Pharmaceutical
Oxazine derivatives

Shionogi
Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs

University of South Florida
Morpholinone compounds as factor IXA inhibitors

Merck Sharp & Dohme
Inhibition of fucosyltransferase VII by gallic acid and its derivatives.

Schering-Plough Research Institute
N-substituted-5-substituted phthalamic acids as sortilin inhibitors

H. Lundbeck
Toll-like receptor 7 (TLR7) agonists having a tricyclic moiety, conjugates thereof, and methods and uses therefor

Bristol_Myers Squibb
Synthesis and structure-activity relationships of beta- and alpha-piperidine sulfone hydroxamic acid matrix metalloproteinase inhibitors with oral antitumor efficacy.

Pfizer
Discovery of novel aspartyl ketone dipeptides as potent and selective caspase-3 inhibitors.

Merck Frosst Canada
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.

Schering-Plough Research Institute