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Article Title

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Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH

Jagiellonian University Medical College

Calcitonin gene-related peptide receptor antagonists: new therapeutic agents for migraine.

Merck Research Laboratories

Serendipitous oxidation product of BIBN4096BS: a potent CGRP receptor antagonist.

Bristol-Myers Squibb

Identification of potent CNS-penetrant thiazolidinones as novel CGRP receptor antagonists.

Vertex Pharmaceuticals

(E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.

Merck

Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.

Bristol-Myers Squibb

[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.

Merck Research Labortories

Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery.

Bristol-Myers Squibb R & D

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.

Bristol-Myers Squibb Research & Development

Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine.

Glaxosmithkline

Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.

Bristol-Myers Squibb Research & Development

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.

TBA

Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor.

Bristol-Myers Squibb R & D

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.

Bristol-Myers Squibb Research & Development

MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.

Merck Research Laboratories

Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.

Bristol-Myers Squibb Research & Development

Calcitonin gene-related peptide (CGRP) receptor antagonists: novel aspartates and succinates.

Bristol-Myers Squibb Research & Development

The discovery of highly potent CGRP receptor antagonists.

Merck

Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.

Merck Research Laboratories

 

Synthesis of -helix substituted analogs of calcitonin gene-related peptide

TBA

Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.

Merck Research Laboratories

Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.

Merck

Identification of potent, highly constrained CGRP receptor antagonists.

Merck

Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.

Merck Research Laboratories

Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.

Merck

The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.

Merck Research Laboratories

 

Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists

TBA

Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability.

Bristol-Myers Squibb Research And Development

Potent benzimidazolone-based CGRP receptor antagonists.

Merck

Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and effic

Bristol-Myers Squibb Research & Development

Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974).

Merck Research Laboratories

Caprolactams as potent CGRP receptor antagonists for the treatment of migraine.

Merck Research Laboratories

Calcitonin gene-related peptide analogues with aza and indolizidinone amino acid residues reveal conformational requirements for antagonist activity at the human calcitonin gene-related peptide 1 receptor.

Université

Identification of novel, orally bioavailable spirohydantoin CGRP receptor antagonists.

Merck Research Laboratories

Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine.

Merck Research Laboratories

Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead.

Department Of Medicinal Chemistry Merck

Identification of the key residue of calcitonin gene related peptide (CGRP) 27-37 to obtain antagonists with picomolar affinity at the CGRP receptor.

University Of Leipzig

Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist

Boehringer Ingelheim Pharma

From micromolar to nanomolar affinity: a systematic approach to identify the binding site of CGRP at the human calcitonin gene-related peptide 1 receptor.

Eth ZüRich

Structure-activity study of hCGRP8-37, a calcitonin gene-related peptide receptor antagonist.

Université

Validation of flavonoids as potential dipeptidyl peptidase III inhibitors: Experimental and computational approach.

Josip Juraj Strossmayer University Of Osijek

Thymidine esters as substrate analogue inhibitors of angiogenic enzyme thymidine phosphorylase in vitro.

University Of Karachi

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

 

SYNTHESIS AND PHARMACOKINETICS OF POTENT CARBAMATE HIV-1 PROTEASE INHIBITORS CONTAINING NOVEL HIGH AFFINITY HYDROXYETHYLAMINE ISOSTERES

Eli Lilly