Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): a Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist For Acute Treatment of Migraine.

S.J. Bucknell,Mark A. Ator,Alastair J. H. Brown,J D Brown,Andrew Cansfield,Julie Elaine Cansfield,John A. Christopher,Miles Congreve,G Cseke,Francesca Deflorian,Chris Jones,Jonathan S. Mason,A OBrien,Gregory R. Ott,Mark Pickworth,Stacey M. Southall

Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1H-indazol-5-yl)-1-oxo-1-(((S)-1-oxo-3-(piperidin-4-yl)-1-(4-(pyridin-4-yl)piperazin-1-yl)propan-2-yl)amino)propan-2-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,4'-pyrido[2,3-d][1,3]oxazine]-1-carboxamide (HTL22562): a Calcitonin Gene-Related Peptide (CGRP) Receptor Antagonist For Acute Treatment of Migraine.

2020

S.J. Bucknell
Mark A. Ator
Alastair J. H. Brown
J D Brown
Andrew Cansfield
Julie Elaine Cansfield
John A. Christopher
Miles Congreve
G Cseke
Francesca Deflorian
Chris Jones
Jonathan S. Mason
A OBrien
Gregory R. Ott
Mark Pickworth
Stacey M. Southall

Structure-based drug design enabled the discovery of 8, HTL22562, a CGRP receptor antagonist. The structure of 8 complexed with the CGRP receptor was determined at 1.6 A resolution. Compound 8 is a...

Keywords:

Calcitonin gene-related peptide
CGRP receptor
Stereochemistry
Migraine
Organic chemistry
Chemistry
D-1
Antagonist
Drug discovery
Carboxamide
Piperidine

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