CY1108410T1 - Μειγματα αναλογων κυκλοσπορινης και η χρηση τους ως ανοσορυθμιστικοι παραγοντες - Google Patents

Μειγματα αναλογων κυκλοσπορινης και η χρηση τους ως ανοσορυθμιστικοι παραγοντες

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Publication number
CY1108410T1
CY1108410T1 CY20081101130T CY081101130T CY1108410T1 CY 1108410 T1 CY1108410 T1 CY 1108410T1 CY 20081101130 T CY20081101130 T CY 20081101130T CY 081101130 T CY081101130 T CY 081101130T CY 1108410 T1 CY1108410 T1 CY 1108410T1
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CY
Cyprus
Prior art keywords
isomers
mixtures
cyclosporin
isatx247
derivatives
Prior art date
Application number
CY20081101130T
Other languages
English (en)
Inventor
Selvaraj Naicker
Randall W. Yatscoff
Robert T. Foster
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Isotechnika, Inc.
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 Isotechnika, Inc. filed Critical Isotechnika, Inc.
Publication of CY1108410T1 publication Critical patent/CY1108410T1/el

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64Cyclic peptides containing only normal peptide links
    • C07K7/645Cyclosporins; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13Cyclosporins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
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  • Neurology (AREA)
  • Dispersion Chemistry (AREA)
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Abstract

Η εφεύρεση απευθύνεται σε ισομερή μείγματα ανάλογων κυκλοσπορίνης που είναι δομικά παρόμοια με την κυκλοσπορίνη Α. Τα μείγματα διαθέτουν ενισχυμένη ισχύ και μειωμένη τοξικότητα σε σύγκριση με τα ξεχωριστά ισομερή και με τις φυσικές ή άλλες γνωστές προς το παρόν κυκλοσπορίνες και παράγωγα κυκλοσπορινών. Πραγματοποιήσεις της παρούσας εφεύρεσης απευθύνονται στα cis και trans ισομερή των ανάλογων κυκλοσπορίνης που αναφέρονται ως ISATX247, και παράγωγων τους. Μείγματα των ισομερών ISATX247 παρουσιάζουν ένα συνδυασμό ενισχυμένης ισχύος και μειωμένης τοξικότητας σε σύγκριση με τις φυσικές και γνωστές προς το παρόν κυκλοσπορίνες. Τα ισομερή ISATX247 και αλκυλιωμένα, αρυλιωμένα, και δευτεριωμένα παράγωγα συντίθενται με στερεοεκλεκτικές οδούς όπου οι ιδιαίτερες συνθήκες αντίδρασης καθορίζουν το βαθμό στερεοεκλεκτικότητας. Οι στερεοεκλεκτικές οδούς μπορούν να χρησιμοποιούν μια αντίδραση Wittig, ή ένα οργανομεταλλικό αντιδραστήριο που περιλαμβάνει ανόργανα στοιχεία τέτοια όπως, βόριο, πυρίτιο, τιτάνιο, και λίθιο. Το ποσοστό των ισομερών σε πρόσμειξη μπορεί να κυμαίνεται από περίπου 10 έως 90 τοις εκατό σε βάρος του (Ε)-ισομερούς έως περίπου 90 έως 10 τοις εκατό σε βάρος του (Ζ)-ισομερούς, με βάση το συνολικό βάρος του μείγματος.
CY20081101130T 2001-10-19 2008-10-13 Μειγματα αναλογων κυκλοσπορινης και η χρηση τους ως ανοσορυθμιστικοι παραγοντες CY1108410T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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

Publications (1)

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CY1108410T1 true CY1108410T1 (el) 2012-05-23

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Application Number Title Priority Date Filing Date
CY20081101130T CY1108410T1 (el) 2001-10-19 2008-10-13 Μειγματα αναλογων κυκλοσπορινης και η χρηση τους ως ανοσορυθμιστικοι παραγοντες
CY2022030C CY2022030I2 (el) 2001-10-19 2022-10-14 Μειγματα αναλογων κυκλοσπορινης και η χρηση τους ως ανοσορρυθμιστικοι παραγοντες

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US (2) US20110092669A1 (el)
EP (2) EP1436322B1 (el)
JP (4) JP2005511538A (el)
KR (1) KR100992850B1 (el)
CN (1) CN100344648C (el)
AR (1) AR036853A1 (el)
AT (1) ATE401339T1 (el)
AU (1) AU2002331510B2 (el)
BE (1) BE2022C547I2 (el)
BR (1) BR0213659A (el)
CA (2) CA2460685C (el)
CO (1) CO5570682A2 (el)
CY (2) CY1108410T1 (el)
DE (1) DE60227686D1 (el)
DK (1) DK1436322T3 (el)
EC (3) ECSP045060A (el)
ES (1) ES2310604T3 (el)
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NL301200I2 (nl) 2024-07-25
DK1436322T3 (da) 2008-11-03
CY2022030I2 (el) 2023-06-09
CN100344648C (zh) 2007-10-24
ZA200402270B (en) 2005-05-25
ECSP045060A (es) 2004-07-23
LTPA2022521I1 (el) 2022-11-10
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