HRP20070058B1 - Sinteza ciklosporinskih analoga - Google Patents

Sinteza ciklosporinskih analoga

Info

Publication number
HRP20070058B1
HRP20070058B1 HRP20070058AA HRP20070058A HRP20070058B1 HR P20070058 B1 HRP20070058 B1 HR P20070058B1 HR P20070058A A HRP20070058A A HR P20070058AA HR P20070058 A HRP20070058 A HR P20070058A HR P20070058 B1 HRP20070058 B1 HR P20070058B1
Authority
HR
Croatia
Prior art keywords
isomers
cyclosporin
isa247
derivatives
weight
Prior art date
Application number
HRP20070058AA
Other languages
English (en)
Inventor
Selvaraj Naicker
Randall W. Yatscoff
Robert T. Foster
Mark Abel
Seetharaman Jayaraman
Hans-Jurgen Mair
Jean-Michel Adam
Bruno Lohri
Original Assignee
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 HRP20070058A2 publication Critical patent/HRP20070058A2/hr
Publication of HRP20070058B1 publication Critical patent/HRP20070058B1/hr

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C07K7/645—Cyclosporins; Related peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B82—NANOTECHNOLOGY
    • B82Y—SPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00—Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10S—TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10S530/00—Chemistry: natural resins or derivatives; peptides or proteins; lignins or reaction products thereof
    • Y10S530/806—Antigenic peptides or proteins

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  • General Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
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  • Epidemiology (AREA)
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  • Molecular Biology (AREA)
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  • Proteomics, Peptides & Aminoacids (AREA)
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  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
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  • Hematology (AREA)
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Abstract

Izum je usmjeren prema izomernim smjesama ciklosporinskih analoga, strukturno sličnima ciklosporinu A. Smjese posjeduju povećanu djelotvornost i smanjenu toksičnost pred pojedinačnim izomerima i prirodnim i ostalim trenutno poznatim ciklosporinima i ciklosporinskim derivatima. Ostvarenja ovog izuma usmjerena su prema cis- i trans-izomerima analoga ciklosporina A, nazvanim ISA247, kao i njihovim derivatima. Smjese izomera ISA247 pokazuju kombinaciju povećane snage i smanjene toksičnosti pred prirodnim i trenutno poznatim ciklosporinima. Izomeri ISA247 i alkilirani, arilirani i deuterirani derivati sintetiziraju se stereoselektivnim putevima gdje određeni uvjeti reakcije određuju stupanj stereoselektivnosti. Stereoselektivni putevi mogu koristiti Wittigovu reakciju ili organometalni reagens, koji sadrži anorganske elemente, kao što su bor, silicij, titan i litij. Omjer izomera u smjesi može varirati od oko 10 do 90 posto mase (E)-izomera do oko 90 do 10 posto mase (Z)-izomera, na osnovi ukupne mase smjese.
HRP20070058AA 2001-10-19 2007-02-14 Sinteza ciklosporinskih analoga HRP20070058B1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34620101P 2001-10-19 2001-10-19
US37059602P 2002-04-05 2002-04-05
PCT/CA2002/001559 WO2003033526A2 (en) 2001-10-19 2002-10-17 Synthesis of cyclosporin analogs

Publications (2)

Publication Number Publication Date
HRP20070058A2 HRP20070058A2 (hr) 2008-09-30
HRP20070058B1 true HRP20070058B1 (hr) 2014-05-23

Family

ID=26994746

Family Applications (2)

Application Number Title Priority Date Filing Date
HRP20040355AA HRP20040355B1 (hr) 2001-10-19 2004-04-19 Sinteza ciklosporinskih analoga
HRP20070058AA HRP20070058B1 (hr) 2001-10-19 2007-02-14 Sinteza ciklosporinskih analoga

Family Applications Before (1)

Application Number Title Priority Date Filing Date
HRP20040355AA HRP20040355B1 (hr) 2001-10-19 2004-04-19 Sinteza ciklosporinskih analoga

Country Status (28)

Country Link
US (13) US6998385B2 (hr)
EP (2) EP1436321B9 (hr)
JP (3) JP4261355B2 (hr)
KR (2) KR100982466B1 (hr)
CN (1) CN100334106C (hr)
AT (2) ATE332917T1 (hr)
AU (2) AU2002331509B2 (hr)
BR (1) BRPI0213658A8 (hr)
CA (1) CA2461740C (hr)
CO (1) CO5580836A2 (hr)
CY (1) CY1105111T1 (hr)
DE (2) DE60213115T2 (hr)
DK (2) DK1436321T3 (hr)
ES (2) ES2326040T3 (hr)
HK (1) HK1062568A1 (hr)
HR (2) HRP20040355B1 (hr)
IL (3) IL160763A0 (hr)
MA (1) MA27293A1 (hr)
MX (1) MXPA04003625A (hr)
NO (1) NO332459B1 (hr)
NZ (1) NZ531944A (hr)
PL (2) PL210841B1 (hr)
PT (2) PT1714977E (hr)
RU (1) RU2321593C9 (hr)
SI (1) SI1436321T1 (hr)
TN (1) TNSN04068A1 (hr)
WO (1) WO2003033526A2 (hr)
ZA (1) ZA200402269B (hr)

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