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CO5631438A2 - Profarmacos de aminoacidos excitadores - Google Patents

Profarmacos de aminoacidos excitadores

Info

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
Authority
CO
Colombia
Prior art keywords
group
aromatic
optionally substituted
hydrogen
fluoro
Prior art date
Application number
CO04122695A
Other languages
English (en)
Inventor
Eric David Moher
James Allen Monn
Original Assignee
Lilly Co Eli
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
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    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
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    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
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    • A61K47/555—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound pre-targeting systems involving an organic compound, other than a peptide, protein or antibody, for targeting specific cells
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • 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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    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
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    • C07—ORGANIC CHEMISTRY
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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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/14—All rings being cycloaliphatic
    • C07C2602/18—All rings being cycloaliphatic the ring system containing six carbon atoms

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  • Organic Chemistry (AREA)
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  • Psychiatry (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
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  • Diabetes (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Hospice & Palliative Care (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
US41593702P 2002-10-03 2002-10-03
US41593602P 2002-10-03 2002-10-03

Publications (1)

Publication Number Publication Date
CO5631438A2 true CO5631438A2 (es) 2006-04-28

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

Country Status (30)

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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) NZ564692A (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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EA017648B1 (ru) 2007-09-14 2013-02-28 Орто-Макнейл-Янссен Фармасьютикалз, Инк. 1',3'-двузамещенные-4-фенил-3,4,5,6-тетрагидро-2н,1'н-[1,4']бипириди-нил-2'-оны
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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
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