862805-23-0Relevant academic research and scientific papers
Structure-Based Drug Discovery of N-((R)-3-(7-Methyl-1 H-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-carboxam
Bucknell, Sarah J.,Ator, Mark A.,Brown, Alastair J. H.,Brown, Jason,Cansfield, Andrew D.,Cansfield, Julie E.,Christopher, John A.,Congreve, Miles,Cseke, Gabriella,Deflorian, Francesca,Jones, Christopher R.,Mason, Jonathan S.,O'Brien, M. Alistair,Ott, Gregory R.,Pickworth, Mark,Southall, Stacey M.
, p. 7906 - 7920 (2020/08/21)
Structure-based drug design enabled the discovery of 8, HTL22562, a calcitonin gene-related peptide (CGRP) receptor antagonist. The structure of 8 complexed with the CGRP receptor was determined at a 1.6 ? resolution. Compound 8 is a highly potent, select
CGRP RECEPTOR ANTAGONISTS
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Paragraph 0077; 0081, (2018/10/25)
The disclosures herein relate to novel compounds of formula (IA) wherein R1, R2, R3and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function. The disclosures herein also relates to novel compounds of formula(IB) wherein R1, R2 and R3 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function. The disclosures herein also relate to novel compounds of formula (IC) wherein Ar1 and R1 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
CGRP RECEPTOR ANTAGONISTS
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Paragraph 0055, (2017/05/17)
The disclosures herein relate to novel compounds of formula (I) wherein R1, R2, R3 and R4 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
Serendipitous oxidation product of BIBN4096BS: A potent CGRP receptor antagonist
Dasgupta, Bireshwar,Kozlowski, Edward,Schroeder, Daniel R.,Torrente, John R.,Xu, Cen,Pin, Sokhom,Conway, Charlie M.,Dubowchik, Gene M.,Macor, John E.,Vrudhula, Vivekananda M.
, p. 2744 - 2748 (2014/06/09)
An oxidation product (5) formed during the synthesis of BIBN-4096BS (1) was found to be a potent CGRP antagonist (IC50 = 0.11 nM). While 5 was found to be ten-fold less potent than 1, another analog 8 with lower molecular weight containing the
Serendipitous oxidation product of BIBN4096BS: A potent CGRP receptor antagonist
Dasgupta, Bireshwar,Kozlowski, Edward,Schroeder, Daniel R.,Torrente, John R.,Xu, Cen,Pin, Sokhom,Conway, Charlie M.,Dubowchik, Gene M.,Macor, John E.,Vrudhula, Vivekananda M.
, p. 2744 - 2748 (2015/02/19)
An oxidation product (5) formed during the synthesis of BIBN-4096BS (1) was found to be a potent CGRP antagonist (IC50 = 0.11 nM). While 5 was found to be ten-fold less potent than 1, another analog 8 with lower molecular weight containing the
Process for preparing 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
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Page/Page column 8, (2010/02/13)
The present application relates to a process for preparing the CGRP-antagonist 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 of formula by means of which this compound can be prepared in large amounts, in high yields and with high purity.
METHOD FOR THE PRODUCTION OF 1-[N2-[3,5-DIBROMO-N-[[4-(3,4-DIHYDRO-2(1H)-OXOQUINAZOLINE-3-YL)-1-PIPERIDINYL]CARBONYL]-D-TYROSYL]-L-LYSYL]-4-(4-PYRIDINYL)-PIPERAZINE
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Page/Page column 19-20, (2010/02/13)
The invention relates to a method for producing the CGRP antagonist 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazoline-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-L-Iysyl]-4-(4-pyridinyl)-piperazine of formula (I). The disclosed method allows said compound to be produced in great quantities, at great yields, and at a high degree of purity.
