ME00487B - Smješa analoga ciklosporina i njihova upotreba u svojstvu imunomodulatornih supstanci - Google Patents

Smješa analoga ciklosporina i njihova upotreba u svojstvu imunomodulatornih supstanci

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Publication number
ME00487B
ME00487B MEP-2008-780A MEP78008A ME00487B ME 00487 B ME00487 B ME 00487B ME P78008 A MEP78008 A ME P78008A ME 00487 B ME00487 B ME 00487B
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Montenegro
Prior art keywords
isomers
isa
ciclosporin
derivatives
mixtures
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Application number
MEP-2008-780A
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English (en)
French (fr)
Inventor
Selvaraj Naicker
Randall W Yatscoff
Robert T Foster
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Aurinia Pharmaceuticals Inc
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Publication date
Application filed by Aurinia Pharmaceuticals Inc filed Critical Aurinia Pharmaceuticals Inc
Publication of ME00487B publication Critical patent/ME00487B/me

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    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
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Abstract

Pronalazak se bavi smešama izomera analoga ciklosporina koji imaju strukturu sličnu ciklosporinu A. Smeše poseduju poboljšanu delotvornost i smanjenu toksičnost u odnosu na pojedinačne izomere, kao i u odnosu na do sada poznate ciklosporine i derivate ciklosporina koji se nalaze u prirodi. Izvodjenja ovog pronalaska se odnose na cis i trans izomere analoga ciklosporina A. pod nazivom ISA TX 247, i derivata ovih jedinjenja. Smeše izomera ISA TX 247 pokazuju kako poboljšano delovanje, tako i smanjenu toksičnost u odnosu na do sada poznate ciklosporine, i one koji su prisutni u prirodi. Izomeri ISA TX 247, zatim alkilovani, arilovani i deuterijumom obeleženi derivati su sintetisani preko stereoselektivnih puteva u kojima odredjeni ušlo vi reakcije odredjuju stepen stereoselektivnosti. U stereoselektivnim putevima sinteze može da se koristi Wittig-ova reakcija, ili organometalni reagens koji sadrži neorganske elemente kao što su bor, silicijum, titanijum i litijum. Odnos izomera u smeši može da varira od približno 10 do 90 masenih procenata izomera (E) do približno 90 do 10 masenih procenata izomera (Z), u odnosu na ukupnu masu smeše.
MEP-2008-780A 2001-10-19 2002-10-17 Smješa analoga ciklosporina i njihova upotreba u svojstvu imunomodulatornih supstanci ME00487B (me)

Applications Claiming Priority (2)

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US34620101P 2001-10-19 2001-10-19
PCT/CA2002/001560 WO2003033527A2 (en) 2001-10-19 2002-10-17 Cyclosporine analogue mixtures and their use as immunomodulating agents

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US (2) US20110092669A1 (me)
EP (2) EP1436322B1 (me)
JP (4) JP2005511538A (me)
KR (1) KR100992850B1 (me)
CN (1) CN100344648C (me)
AR (1) AR036853A1 (me)
AT (1) ATE401339T1 (me)
AU (1) AU2002331510B2 (me)
BE (1) BE2022C547I2 (me)
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FR (1) FR22C1051I2 (me)
HK (1) HK1062567A1 (me)
HR (1) HRP20040353B1 (me)
IL (2) IL160762A0 (me)
LT (1) LTC1436322I2 (me)
MA (1) MA26337A1 (me)
ME (1) ME00487B (me)
MX (1) MXPA04003624A (me)
MY (1) MY187182A (me)
NO (2) NO331745B1 (me)
NZ (1) NZ531945A (me)
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JP2005511538A (ja) * 2001-10-19 2005-04-28 アイソテクニカ インコーポレーテッド シクロスポリン類似体混合物及びそれらの免疫調節剤としての使用

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FIC20220041I1 (fi) 2022-10-14
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WO2003033527A2 (en) 2003-04-24
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FR22C1051I1 (fr) 2022-12-16
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US20110092669A1 (en) 2011-04-21
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US20140288266A1 (en) 2014-09-25
ZA200402270B (en) 2005-05-25
AR036853A1 (es) 2004-10-06
BR0213659A (pt) 2004-10-26
LTPA2022521I1 (me) 2022-11-10
BE2022C547I2 (me) 2022-10-19
HRP20040353A2 (en) 2005-04-30

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