CO5631438A2 - Profarmacos de aminoacidos excitadores - Google Patents

Profarmacos de aminoacidos excitadores

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Publication number
CO5631438A2
CO5631438A2 CO04122695A CO04122695A CO5631438A2 CO 5631438 A2 CO5631438 A2 CO 5631438A2 CO 04122695 A CO04122695 A CO 04122695A CO 04122695 A CO04122695 A CO 04122695A CO 5631438 A2 CO5631438 A2 CO 5631438A2
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CO
Colombia
Prior art keywords
group
aromatic
optionally substituted
hydrogen
fluoro
Prior art date
Application number
CO04122695A
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English (en)
Inventor
Eric David Moher
James Allen Monn
Original Assignee
Lilly Co Eli
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Filing date
Publication date
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of CO5631438A2 publication Critical patent/CO5631438A2/es

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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
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    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/12—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
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    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/18—All rings being cycloaliphatic the ring system containing six carbon atoms

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  • Proteomics, Peptides & Aminoacids (AREA)
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Abstract

1.- Un compuesto de Fórmula I en la que:A es H-(Q)p-;Q se selecciona independientemente, cada vez que aparece, del grupo aminoacilo;p es un número entero de 1 a 10;X es O, S, SO, SO2 o CR3R4;R3 es fluoro, XAND#39OR5, SO3H, tetrazol-5-ilo, CN, PO3R62, hidroxi, NO2, N3, (CH2)mCOOR5a, (CH2)mPO3R6a2, NHCONHR5b o NHSO2R5c y R4 es hidrógeno; o cada uno de R3 y R4 representa fluoro; o R3 y R4 representan juntos =O, =NOR7, =CR8R9, =CHCOOR5b, =CHPO3R6a2 o =CHCN; o uno de R3 o R4 representa amino y el otro representa carboxilo;XAND#39 representa un enlace, CH2 o CO;m es un número entero de 1 a 3; R5, R5a, R5b, R5c, R7, R8 y R9 son independientemente un átomo de hidrógeno; un grupo alquilo (1-6C) opcionalmente sustituido; un grupo alquenilo (2-6C) opcionalmente sustituido; un grupo alquinilo (2-6C) opcionalmente sustituido; un grupo aromático opcionalmente sustituido; un grupo heteroaromático opcionalmente sustituido; un grupo carbocíclico no aromático; un grupo heterocíclico no aromático; un grupo carbocíclico monocíclico no aromático condensado con uno o dos grupos aromáticos o heteroaromáticos monocíclicos; o un grupo heterocíclico monocíclico no aromático condensado con uno o dos grupos aromáticos o heteroaromáticos monocíclicos;R6 y R6a representan independientemente hidrógeno o un grupo alquilo (1-6C);R10 es hidrógeno o fluoro; y R11 es hidrógeno, fluoro, o hidroxi;o una de sus sales farmacéuticamente aceptables.
CO04122695A 2002-06-11 2004-12-07 Profarmacos de aminoacidos excitadores CO5631438A2 (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP02380120 2002-06-11
EP02380121 2002-06-11
US41593602P 2002-10-03 2002-10-03
US41593702P 2002-10-03 2002-10-03

Publications (1)

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CO5631438A2 true CO5631438A2 (es) 2006-04-28

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CO04122695A CO5631438A2 (es) 2002-06-11 2004-12-07 Profarmacos de aminoacidos excitadores

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US (5) US7371872B2 (es)
EP (2) EP1897550A3 (es)
JP (2) JP4342437B2 (es)
KR (1) KR20080058509A (es)
AR (1) AR040257A1 (es)
AT (1) ATE421526T1 (es)
AU (1) AU2003232146B2 (es)
BR (1) BR0311558A (es)
CA (1) CA2488167C (es)
CO (1) CO5631438A2 (es)
CR (2) CR7616A (es)
CY (1) CY1108976T1 (es)
DE (1) DE60325968D1 (es)
DK (1) DK1517915T3 (es)
EA (2) EA011231B1 (es)
EC (1) ECSP085481A (es)
ES (1) ES2319116T3 (es)
HK (1) HK1075259A1 (es)
HR (2) HRP20041179B1 (es)
IL (2) IL165100A0 (es)
MX (1) MXPA04012518A (es)
MY (1) MY146238A (es)
NO (2) NO331780B1 (es)
NZ (3) NZ536459A (es)
PE (1) PE20040555A1 (es)
PL (1) PL221489B1 (es)
PT (1) PT1517915E (es)
SI (1) SI1517915T1 (es)
WO (1) WO2003104217A2 (es)
ZA (1) ZA200409553B (es)

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JP5656848B2 (ja) 2008-10-16 2015-01-21 ジャンセン ファーマシューティカルズ， インコーポレイテッド． 代謝型グルタミン酸受容体モジュレーターとしてのインドールおよびベンゾモルホリンの誘導体
RU2512283C2 (ru) 2008-11-28 2014-04-10 Янссен Фармасьютикалз, Инк. Производные индола и бензоксазина в качестве модуляторов метаботропных глутаматных рецепторов
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PT2430022E (pt) 2009-05-12 2013-12-26 Janssen Pharmaceuticals Inc Derivados de 1,2,3-triazolo[4,3-a]piridina e a sua utilização para o tratamento ou prevenção de doenças neurológicas e psiquiátricas
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