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Article Title
Organization
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.

Exploratory Chemistry Merck Sharp and Dohme Research Laboratories
Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted benzolactams.

Merck Sharp & Dohme Research Laboratories
Cholecystokinin antagonists. Synthesis and biological evaluation of 3-substituted 1,4-benzodiazepin-2-amines.

Merck Sharp & Dohme Research Laboratories
Cholecystokinin antagonists. Synthesis of asperlicin analogues with improved potency and water solubility.

TBA
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Merck Research Laboratories
Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Merck Research Laboratories
Benzodiazepines as potent and selective bradykinin B1 antagonists.

Merck Research Laboratories
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 4. Structure-activity relationship in the dihydropyrimidine series.

Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.

Synaptic Pharmaceutical
Novel glutamic acid derived cholecystokinin receptor ligands.

Merck Sharp & Dohme Research Laboratories
Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists.

Merck Sharp & Dohme Research Laboratories
Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.

Merck Research Laboratories
Design and synthesis of novel dihydropyridine alpha-1a antagonists.

Synaptic Pharmaceutical
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.

Merck
L-161,638: A potent AT2selective quinazolinone angiotensin II binding inhibitor

TBA
L-162,389: a potent orally active angiotensin II receptor antagonist with balanced affinity to both AT
1 and AT
2 receptor subtypes

TBA
AT
1 selective angiotensin II antagonists with phenoxyphenylacetic acid as a biphenyl replacement part I

TBA
The SAR of 6-(N-alkyl-N-acyl)-2-propyl-3-[(2′-tetrazol-5-yl)biphen-4-yl)methyl]-quinazolinones as balanced affinity antagonists of the human AT
1 and AT
2 receptors

TBA
Potent dual antagonists of endothelin and angiotensin II receptors derived from α-phenoxyphenylacetic acids (Part III)

TBA
α-Phenoxyphenylacetic acid derived angiotensin II antagonists with low nanomolar AT
1/AT
2 receptor subtype affinity (Part II)

TBA
Substituted 1,3-benzodioxole & 1,3-benzodithiole -2- carboxylates and their tetrazole analogs with potent binding affinity to the angiotensin II AT
1 receptor

TBA
Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT
1 and AT
2 subtypes

TBA
Development of angiotensin II antagonists with equipotent affinity for human AT
1 and AT
2 receptor subtypes.

TBA
A new class of balanced AT
1/AT
2 angiotensin II antagonists: quinazolinone AII antagonists with acylsulfonamide and sulfonylcarbamate acidic functionalities

TBA
Quinazolinone Biphenyl Acylsulfonamides: A potent new class of angiotensin-II receptor antagonists

TBA
Potent imidazole angiotensinII antagonists: acyl sulfonamides and acyl sulfamides as tetrazole replacements

TBA
Evaluation of heterocyclic acid equivalents as tetrazole replacements in imidazopyridine-based nonpeptide angiotensin II receptor antagonists

TBA
Synthesis of new imidazo[1,2-
b]pyridazine isosteres of potent imidazo[4,5-
b]pyridine angiotensin II antagonists

TBA
Acidic phenols: a new class of potent nonpeptide angiotensin II receptor antagonists

TBA
Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT
1 and AT
2 receptors

TBA
Imidazo[4,5-b]pyridine-based AT
1 / AT
2 angiotensin II receptor antagonists

TBA
Triazolinones as nonpeptide angiotensin II antagonists. 2. discovery of a potent and orally active triazolinone acylsulfonamide

TBA
Angiotensin II receptor antagonists containing a phenylpyridine element.

TBA
Quinazolinones 2: QSAR and in vivo characterization of AT1 selective AII antagonists

TBA
Quinazolinones 1: design and synthesis of potent quinazolinone- containing AT
1-selective angiotensin-II receptor antagonists

TBA
Benzolactams as non-peptide cholecystokinin receptor ligands

TBA
Multipurpose receptor ligands: β-carboline cholecystokinin antagonists

TBA
Synthesis and structure-activity relationships of a novel series of non-peptide AT
2-selective angiotensin II receptor antagonists

TBA
Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

Merck
Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

TBA
2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.

Merck Research Laboratories
2,3-diaminopyridine bradykinin B1 receptor antagonists.

Merck Research Laboratories
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.

Merck Research Laboratories
Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists.

Merck
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.

Synaptic Pharmaceutical
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

Merck
Phenylacetamides as selective alpha-1A adrenergic receptor antagonists.

Merck
In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.

Merck Research Laboratories
Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.

Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 3. Approaches to eliminate opioid agonist metabolites by using substituted phenylpiperazine side chains.

Synaptic Pharmaceutical
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety.

Synaptic Pharmaceutical
4-Oxospiro[benzopyran-2,4'-piperidines] as selective alpha 1a-adrenergic receptor antagonists.

Merck
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.

Merck
Design and synthesis of novel alpha1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia.

Synaptic Pharmaceutical
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.

Merck
Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles.

Merck Research Laboratories
Triazolinones as nonpeptide angiotensin II antagonists. 1. Synthesis and evaluation of potent 2,4,5-trisubstituted triazolinones.

Merck Research Laboratories
Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.

Merck Research Laboratories
Non-peptide angiotensin II receptor antagonists. 1. Design, synthesis, and biological activity of N-substituted indoles and dihydroindoles.

Merck Research Laboratories
(Dipropylphenoxy)phenylacetic acids: a new generation of nonpeptide angiotensin II receptor antagonists.

Merck Research Laboratories
Nonpeptide angiotensin II antagonists derived from 1H-pyrazole-5-carboxylates and 4-aryl-1H-imidazole-5-carboxylates.

Merck Research Laboratories
A potent, orally active, balanced affinity angiotensin II AT1 antagonist and AT2 binding inhibitor.

Merck Research Laboratories
A highly potent, orally active imidazo[4,5-b]pyridine biphenylacylsulfonamide (MK-996; L-159,282): a new AT1-selective angiotensin II receptor antagonist.

Merck Research Laboratories
Triazolinone biphenylsulfonamides as angiotensin II receptor antagonists with high affinity for both the AT1 and AT2 subtypes.

Merck Research Laboratories
Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.

Merck Research Laboratories
Cholecystokinin antagonists. Synthesis and biological evaluation of 4-substituted 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines.

Merck Sharp & Dohme Research Laboratories
Cholecystokinin-A receptor ligands based on the kappa-opioid agonist tifluadom.

Merck Sharp & Dohme Research Laboratories
Pyrrolidine-2, 5-dione derivatives, pharmaceutical compositions and methods for use as IDO1 inhibitors

Iteos Therapeutics
Use of pyrazolopyrimidine derivatives for the treatment of PI3K-delta related disorders

Incyte
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.

Methylgene