PMID
Cmpds
Data
Article Title
Organization
9
Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.

Merck
19
Novel tricyclic pyrazolo[1,5-d][1,4]benzoxazepin-5(6H)-one: Design, synthesis, model and use as hMAO-B inhibitors.

Anhui Medical University
11
Design and synthesis of celastrol derivatives as anticancer agents.

Anhui Medical University
36
Design and synthesis of novel 2-pyrazoline-1-ethanone derivatives as selective MAO inhibitors.

Anhui Medical University
22
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.

Merck Research Laboratories
25
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.

Merck Research Laboratories
22
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.

Merck Research Laboratories
77
Discovery of novel oxazolidinedione derivatives as potent and selective mineralocorticoid receptor antagonists.

Merck Research Laboratories
2
2-[(3aR,4R,5S,7aS)-5-{(1S)-1-[3,5-bis(trifluoromethyl)phenyl]-2-hydroxyethoxy}-4-(2-methylphenyl)octahydro-2H-isoindol-2-yl]-1,3-oxazol-4(5H)-one: a potent human NK1 receptor antagonist with multiple clearance pathways.

Merck Research Laboratories
31
Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-ß-alanine (MK-0893) for the treatment of type II diabetes.

Merck Research Laboratories
100
1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.

Merck Research Laboratories
23
A new class of prolylcarboxypeptidase inhibitors, part 2: the aminocyclopentanes.

Merck Research Laboratories
37
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.

Merck Research Laboratories
31
Tetrahydroindolizinone NK1 antagonists.

Merck Research Laboratories
26
Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.

Merck Research Laboratories
13
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.

Merck Research Laboratories
38
Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
24
Discovery of benzodihydroisofurans as novel, potent, bioavailable and brain-penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
26
Discovery of a new class of potent prolylcarboxypeptidase inhibitors derived from alanine.

Merck Research Laboratories
46
The discovery of non-benzimidazole and brain-penetrant prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
24
SAR studies on the central phenyl ring of substituted biphenyl oxazolidinone-potent CETP inhibitors.

Merck Sharp & Dohme
11
Biphenyl-substituted oxazolidinones as cholesteryl ester transfer protein inhibitors: modifications of the oxazolidinone ring leading to the discovery of anacetrapib.

Merck Research Laboratories
33
Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.

Merck Research Laboratories
42
2-Arylbenzoxazoles as CETP inhibitors: raising HDL-C in cynoCETP transgenic mice.

Merck Research Laboratories
41
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.

Merck Research Laboratories
18
Design of a novel class of biphenyl CETP inhibitors.

Merck Sharp & Dohme
62
Design and synthesis of prolylcarboxypeptidase (PrCP) inhibitors to validate PrCP as a potential target for obesity.

Merck Research Laboratories
19
Fused tricyclic pyrrolizinones that exhibit pseudo-irreversible blockade of the NK1 receptor.

Merck Research Laboratories
34
Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.

Merck Research Laboratories
26
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.

Merck Research Laboratories
29
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.

Merck Research Laboratories
20
Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: synthesis and biological evaluation. Part 1.

Merck Research Laboratories
11
Discovery of a biaryl cyclohexene carboxylic acid (MK-6892): a potent and selective high affinity niacin receptor full agonist with reduced flushing profiles in animals as a preclinical candidate.

Merck Research Laboratories
14
Substituted fused bicyclic pyrrolizinones as potent, orally bioavailable hNK1 antagonists.

Merck Research Laboratories
36
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.

Merck Research Laboratories
49
2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety.

Merck Research Laboratories
46
A strategy of employing aminoheterocycles as amide mimics to identify novel, potent and bioavailable soluble epoxide hydrolase inhibitors.

Merck Research Laboratories
20
Discovery of spirocyclic secondary amine-derived tertiary ureas as highly potent, selective and bioavailable soluble epoxide hydrolase inhibitors.

Merck Research Laboratories
10
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.

Merck Research Laboratories
8
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.

Merck Research Laboratories
35
Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation.

Merck Research Laboratories
66
1-Sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists for the treatment of obesity.

Merck Research Laboratories
29
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.

Merck Research Laboratories
8
Molecular modeling aided design of nicotinic acid receptor GPR109A agonists.

Merck Research Laboratories
2
Discovery of cloxiquine derivatives as potent HDAC inhibitors for the treatment of melanoma via activating PPARγ.

Xinxiang Medical University
5
Development of novel antivrial agents that induce the degradation of the main protease of human-infecting coronaviruses.

Chinese Academy of Sciences
21
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.

Merck Research Laboratories
29
The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine.

Merck
12
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.

TBA
6
Synthesis, binding affinity, and inhibitory capacity of cyclodextrin-based multivalent glycan ligands for human galectin-3.

University of Maryland
34
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.

Merck Research Laboratories
37
Lead optimization of 5,6-diarylpyridines as CB1 receptor inverse agonists.

Merck Research Laboratories
32
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.

Merck Research Laboratories
18
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.

Merck Research Laboratories
32
Discovery of novel, potent, and orally active spiro-urea human glucagon receptor antagonists.

Merck Research Laboratories
36
Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists.

Merck Research Laboratories
54
Synthesis and SAR of 5,6-diarylpyridines as human CB1 inverse agonists.

Merck Research Laboratories
10
Discovery of Pyrazolo[3,4-

Bytedance Ai Lab
8
Bioisosteric replacement of anilide with benzoxazole: potent and orally bioavailable antagonists of VLA-4.

Merck Research Laboratories
27
Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.

Merck Research Laboratories
30
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.

Merck And
30
The discovery of acylated beta-amino acids as potent and orally bioavailable VLA-4 antagonists.

Merck Research Laboratories
7
Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.

Merck
61
Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors

Forma Therapeutics
8
Aniline derivatives, their preparation and their therapeutic application

Sanofi
27
Pyrazolyl-substituted heteroaryls and their use as medicaments

Boehringer Ingelheim International
192
Benzamide imidazopyrazine Btk inhibitors

Merck Sharp & Dohme
10
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.

Shanghai Institute of Materia Medica