ES2187393T1 - Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos. - Google Patents

Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos.

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Publication number
ES2187393T1
ES2187393T1 ES00965687T ES00965687T ES2187393T1 ES 2187393 T1 ES2187393 T1 ES 2187393T1 ES 00965687 T ES00965687 T ES 00965687T ES 00965687 T ES00965687 T ES 00965687T ES 2187393 T1 ES2187393 T1 ES 2187393T1
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Spain
Prior art keywords
useful
bivalent radical
macrociclic
pharmacos
discovery
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Pending
Application number
ES00965687T
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English (en)
Inventor
Pierre Deslongchamps
Yves Dory
Gilles Berthiaume
Luc Ouellet
Ruoxi Lan
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Neokimia Inc
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Neokimia Inc
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Publication of ES2187393T1 publication Critical patent/ES2187393T1/es
Pending legal-status Critical Current

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    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • A—HUMAN NECESSITIES
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    • A61P25/20—Hypnotics; Sedatives
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/12—Antivirals
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    • C07K1/04—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length on carriers
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    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
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    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
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    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
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    • C07K5/08—Tripeptides
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Abstract

Un compuesto macrocíclico de fórmula (I) **(Ver fórmula I)** - en la que la parte (A) es un radical bivalente **(Ver fórmula)** que tiene su grupo -NH- unido al grupo carbonilo de la parte **(Ver fórmula)**, un radical bivalente a -(CH2)y-, o un enlace covalente; en la que la parte (B) es a radical bivalente **(Ver fórmula)** que tiene su grupo -NH- unido a la parte (A), un radical bivalente -(CH2)z-, o un enlace covalente; - en la que la parte (C) es un radical bivalente **(Ver fórmula)** que tiene su grupo -NH- unido a la parte (B), un radical bivalente -(CH2)t-, o un enlace covalente; en la que la parte (T) es un radical - Y - L - Z -; y en la que x es un grupo monovalente seleccionado del grupo que consiste en: -SO2-Ar, -SO2CH3, -SO2-CF3, -H, -COH, -CO-CH3, -CO-Ar, -CO-R, -CO-NHR-, -CO-NHAr, -CO-O-tBu, -CO-O-CH2-Ar.
ES00965687T 1999-10-04 2000-10-04 Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos. Pending ES2187393T1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CA2284459A CA2284459C (en) 1999-10-04 1999-10-04 Combinatorial synthesis of libraries of macrocyclic compounds useful in drug discovery

Publications (1)

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ES2187393T1 true ES2187393T1 (es) 2003-06-16

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ES00965687T Pending ES2187393T1 (es) 1999-10-04 2000-10-04 Sintesis combinatoria de librerias de compuestos macrociclicos utiles en el descubrimiento de farmacos.

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US (5) US7169899B1 (es)
EP (1) EP1218403B1 (es)
JP (5) JP5005865B2 (es)
AT (1) ATE346857T1 (es)
AU (1) AU7636100A (es)
CA (1) CA2284459C (es)
DE (1) DE60032159T2 (es)
DK (1) DK1218403T3 (es)
ES (1) ES2187393T1 (es)
WO (1) WO2001025257A2 (es)

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US20070117154A1 (en) 2007-05-24
US20120046441A1 (en) 2012-02-23
US7169899B1 (en) 2007-01-30
US9018419B2 (en) 2015-04-28
US9409945B2 (en) 2016-08-09
US8188216B2 (en) 2012-05-29
WO2001025257A2 (en) 2001-04-12
WO2001025257A3 (en) 2001-12-06
ATE346857T1 (de) 2006-12-15
JP2012140400A (ja) 2012-07-26
AU7636100A (en) 2001-05-10
JP2003511387A (ja) 2003-03-25
DE60032159T2 (de) 2007-10-25
JP6407942B2 (ja) 2018-10-17
EP1218403B1 (en) 2006-11-29
US8008440B2 (en) 2011-08-30
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JP5005865B2 (ja) 2012-08-22
DE60032159D1 (de) 2007-01-11
JP6373699B2 (ja) 2018-08-15
JP5755530B2 (ja) 2015-07-29
JP5680577B2 (ja) 2015-03-04
JP2017075154A (ja) 2017-04-20
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