NO20042031L - Syntese av syklosporin analoger - Google Patents

Syntese av syklosporin analoger

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Publication number
NO20042031L
NO20042031L NO20042031A NO20042031A NO20042031L NO 20042031 L NO20042031 L NO 20042031L NO 20042031 A NO20042031 A NO 20042031A NO 20042031 A NO20042031 A NO 20042031A NO 20042031 L NO20042031 L NO 20042031L
Authority
NO
Norway
Prior art keywords
cyclosporin
isomers
isa247
mixture
derivatives
Prior art date
Application number
NO20042031A
Other languages
English (en)
Other versions
NO332459B1 (no
Inventor
Selvaraj Naicker
Randall W Yatscoff
Robert T Foster
Mark Abel
Seetharaman Jayaraman
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 NO20042031L publication Critical patent/NO20042031L/no
Publication of NO332459B1 publication Critical patent/NO332459B1/no

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    • 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
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    • 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
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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
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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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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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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nanotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Dispersion Chemistry (AREA)
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  • Crystallography & Structural Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
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Abstract

Oppfinnelsen angår isomeriske blandinger av syklosporin-analoger som strukturelt er lik syklosporin A. Blandingen innehar forbedret effektivitet og redusert toksisitet overfor de individuelle isomerene, og overfor de naturlig forekommende og andre nåværende kjente syklosporinene og syklosporin-derivatene. Utførelser av den foreliggende oppfinnelsen er rettet mot cis og trans-isomere av syklosporin A - analoger, omtalt som ISA247, og derivater av det. Blandinger av ISA247 isomere oppviser en kombinasjon av forbedret kraft og redusert toksisitet overfor de naturlig forekommende og ellers kjente syklosporinene. ISA247 isomere og alkylerte, arylerte og deuterierte derivater syntetiseres via stereoselektive baner hvor de særlige forholdene for en reaksjon bestemmer graden av stereoselektivitet. Stereoselektive baner kan utnytte en Wittig reaksjon, eller en organometallisk reagent omfattende uorganiske elementer så som bor, silisium, titan og litium. Forholdet mellom isomere i en blanding kan variere fra omtrent 10 til 90 vektprosent, basert på den totale vekten av blandingen.
NO20042031A 2001-10-19 2004-05-14 Fremgangsmate for framstilling av en blanding av (E)- og (Z)-isomere av ISATX247. NO332459B1 (no)

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
NO20042031L true NO20042031L (no) 2004-05-19
NO332459B1 NO332459B1 (no) 2012-09-24

Family

ID=26994746

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20042031A NO332459B1 (no) 2001-10-19 2004-05-14 Fremgangsmate for framstilling av en blanding av (E)- og (Z)-isomere av ISATX247.

Country Status (27)

Country Link
US (13) US6998385B2 (no)
EP (2) EP1714977B1 (no)
JP (3) JP4261355B2 (no)
KR (2) KR101006206B1 (no)
CN (1) CN100334106C (no)
AT (2) ATE425178T1 (no)
AU (3) AU2002331509B2 (no)
BR (1) BRPI0213658A8 (no)
CA (1) CA2461740C (no)
CO (1) CO5580836A2 (no)
CY (1) CY1105111T1 (no)
DE (2) DE60213115T2 (no)
DK (2) DK1714977T3 (no)
ES (2) ES2326040T3 (no)
HR (2) HRP20040355B1 (no)
IL (3) IL160763A0 (no)
MA (1) MA27293A1 (no)
MX (1) MXPA04003625A (no)
NO (1) NO332459B1 (no)
NZ (1) NZ531944A (no)
PL (2) PL210841B1 (no)
PT (2) PT1436321E (no)
RU (1) RU2321593C9 (no)
SI (1) SI1436321T1 (no)
TN (1) TNSN04068A1 (no)
WO (1) WO2003033526A2 (no)
ZA (1) ZA200402269B (no)

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