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NO20055826L - HIV-prodroger spaltbare ved CD26 - Google Patents

HIV-prodroger spaltbare ved CD26

Info

Publication number
NO20055826L
NO20055826L NO20055826A NO20055826A NO20055826L NO 20055826 L NO20055826 L NO 20055826L NO 20055826 A NO20055826 A NO 20055826A NO 20055826 A NO20055826 A NO 20055826A NO 20055826 L NO20055826 L NO 20055826L
Authority
NO
Norway
Prior art keywords
prodrugs
acid
allyl
present
dipeptidyl
Prior art date
Application number
NO20055826A
Other languages
English (en)
Other versions
NO20055826D0 (no
Inventor
Jan Mr Balzarini
Piet Tom Bert Paul Wigerinck
Herman Augustinus De Kock
Original Assignee
Tibotec Pharm Ltd
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 Tibotec Pharm Ltd filed Critical Tibotec Pharm Ltd
Publication of NO20055826D0 publication Critical patent/NO20055826D0/no
Publication of NO20055826L publication Critical patent/NO20055826L/no

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    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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 a protein, peptide or polyamino acid
    • A61K47/64Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
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    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings
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    • C07C311/17Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the sulfonamide groups bound to hydrogen atoms or to an acyclic carbon atom to an acyclic carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
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Abstract

Foreliggende oppfinnelse tilveiebringer nye prodroger som er konjugater av en terapeutisk forbindelse og et peptid, hvori konjugatet kan spaltes ved dipeptidylpeptidaser, mer foretrukket ved CD26, også kjent som DPPIV (dipeptidyl aminodipeptidase IV). Foreliggende prodroger har formelen de stereoisomere formene og saltene derav, hvori n er 1 til 5, Y er prolin, alanin, hydroksyprolin, dihydroksyprolin, tiazolidinkarboksylsyre (tioprolin), dehydroprolin, pipecolinsyre (L-homoprolin), azetidinkarboksylsyre, aziridinkarboksylsyre, glysin, serin, valin, leucin, isoleucin og treonin, X velges fra enhver aminosyre i D- eller L-konfigurasjonen, X og Y i hver gjentagelse av [Y-X] velges uavhengig fra hverandre og uavhengig fra andre gjentagelser, Z er en direkte binding eller en bivalent rett eller forgrenet mettet hydrokarbongruppe med fra 1 til 4 karbonatomer. R' er et aryl, heteroaryl, aryloksy, heteroaryloksy, aryloksyCi.4alkyl, heterocykloalkyloksy, heterocykloalkylCMalkyloksy, heteroaryloksyCi. 4alkyl, heteroarylCi^allyloksy, R^ er arylCi^iallyl, R^ er Ci.ioallyl, ^.^alkei^l eller C3.7cykloalkylCi^allyl, R'' er hydrogen eller Ci^kyl. Foreliggende oppfinnelse tilveiebringer videre anvendelsen av prodrogene som medisin samt som en fremgangsmåte for å fremstille prodrogene.
NO20055826A 2003-05-08 2005-12-08 HIV-prodroger spaltbare ved CD26 NO20055826L (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0310593.9A GB0310593D0 (en) 2003-05-08 2003-05-08 Peptidic prodrugs
PCT/EP2004/050753 WO2004099135A2 (en) 2003-05-08 2004-05-10 Hiv prodrugs cleavable by cd26

Publications (2)

Publication Number Publication Date
NO20055826D0 NO20055826D0 (no) 2005-12-08
NO20055826L true NO20055826L (no) 2006-02-08

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Application Number Title Priority Date Filing Date
NO20055826A NO20055826L (no) 2003-05-08 2005-12-08 HIV-prodroger spaltbare ved CD26

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US (2) US20080214648A1 (no)
EP (2) EP1620130A1 (no)
JP (2) JP2007526872A (no)
KR (1) KR20060008300A (no)
CN (1) CN1784244A (no)
AP (1) AP2005003465A0 (no)
AT (1) ATE375172T1 (no)
AU (2) AU2004236371B2 (no)
BR (1) BRPI0410158A (no)
CA (2) CA2525191A1 (no)
DE (1) DE602004009435T2 (no)
DK (1) DK1624897T3 (no)
EA (1) EA009727B1 (no)
ES (1) ES2295879T3 (no)
GB (1) GB0310593D0 (no)
MX (1) MXPA05012019A (no)
NO (1) NO20055826L (no)
NZ (1) NZ543946A (no)
PT (1) PT1624897E (no)
UA (1) UA82221C2 (no)
WO (2) WO2004098644A1 (no)
ZA (1) ZA200509940B (no)

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CA2525191A1 (en) 2004-11-18
DE602004009435T2 (de) 2008-07-24
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JP2006525235A (ja) 2006-11-09
WO2004099135A3 (en) 2005-02-17
KR20060008300A (ko) 2006-01-26
DK1624897T3 (da) 2008-02-11
PT1624897E (pt) 2008-01-17
EA009727B1 (ru) 2008-02-28
ATE375172T1 (de) 2007-10-15
US20080214648A1 (en) 2008-09-04
ZA200509940B (en) 2007-04-25
CN1784244A (zh) 2006-06-07
AU2004236371B2 (en) 2009-12-17
GB0310593D0 (en) 2003-06-11
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AU2004236371A1 (en) 2004-11-18
US8236756B2 (en) 2012-08-07
EA200501768A1 (ru) 2006-04-28
NZ543946A (en) 2008-09-26
NO20055826D0 (no) 2005-12-08
CA2517338A1 (en) 2004-11-18
US20070275900A1 (en) 2007-11-29
EP1624897B1 (en) 2007-10-10
DE602004009435D1 (de) 2007-11-22
BRPI0410158A (pt) 2006-05-16
WO2004099135A2 (en) 2004-11-18
AP2005003465A0 (en) 2005-12-31
ES2295879T3 (es) 2008-04-16
JP2007526872A (ja) 2007-09-20
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AU2004235988A1 (en) 2004-11-18
EP1620130A1 (en) 2006-02-01

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