FI111730B - Förfarande för framställning av ej-immunosuppresiva cyklosporiner - Google Patents

Förfarande för framställning av ej-immunosuppresiva cyklosporiner Download PDF

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Publication number
FI111730B
FI111730B FI915135A FI915135A FI111730B FI 111730 B FI111730 B FI 111730B FI 915135 A FI915135 A FI 915135A FI 915135 A FI915135 A FI 915135A FI 111730 B FI111730 B FI 111730B
Authority
FI
Finland
Prior art keywords
meleu
cyclosporin
mebmt
ciclosporin
hydroxy
Prior art date
Application number
FI915135A
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English (en)
Finnish (fi)
Other versions
FI915135A0 (fi
FI915135A (fi
Inventor
Dieter Seebach
Hans Kobel
Roland Wenger
Pietro Bollinger
Soo Young Ko
Brigitte Rosenwirth
Rene P Traber
Original Assignee
Novartis Ag
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=27517009&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=FI111730(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GB909023859A external-priority patent/GB9023859D0/en
Priority claimed from GB909023972A external-priority patent/GB9023972D0/en
Priority claimed from GB909023971A external-priority patent/GB9023971D0/en
Priority claimed from GB909023970A external-priority patent/GB9023970D0/en
Priority claimed from GB919116836A external-priority patent/GB9116836D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of FI915135A0 publication Critical patent/FI915135A0/fi
Publication of FI915135A publication Critical patent/FI915135A/fi
Application granted granted Critical
Publication of FI111730B publication Critical patent/FI111730B/sv

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • Y10S435/00—Chemistry: molecular biology and microbiology
    • Y10S435/8215—Microorganisms
    • Y10S435/911—Microorganisms using fungi
    • 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
    • Y10S930/00—Peptide or protein sequence
    • Y10S930/01—Peptide or protein sequence
    • Y10S930/27—Cyclic peptide or cyclic protein

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • AIDS & HIV (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Cephalosporin Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (5)

1. Förfarande för framställning av en ej-immunosuppressiv cyklosporin enligt formel II
5 -V' X R Y-Z—MeLeu-Ala- ( D ) Ala-MeLeu-MeLeu-Me Vai-, 1 2 3 A 5 6 7 8 9 10 11 II väri W är MeBmt eller dihydro-MeBmt;
10 X är aAbu, Vai, Thr, Nva eller MeOthr; R är Sar eller (D)-MeAla; Y är MeLeu, γ-hydroxi-MeLeu, Melle, MeVal, MeThr, MeAla, Mealle eller MeaThr; och Z är Vai, Leu, MeVal eller MeLeu; 15 pä det villkor att 1. dä Y är MeLeu elle MeAla, är Z MeVal eller MeLeu; och 2. dä W är MeBmt, är R Sar och Y är γ-hydroxi-MeLeu, sä är Z nägot annan än Vai; 20 kännetecknat därav, att förfarandet omfattar ett eller flere av följande skeden: a) en svampstam av arten Tolypocladium infla- • ·. turn odlas och produkten isoleras; . b) cyklosporinet med en eller flera MeLeu- 25 rester hydroxyleras genom att tillföra det tili en • ; svampkultur av arten Sebekia benihana och isolera pro dukten; , ’ c) cyklosporinet, med en Val-rest i 5-ställ- ning, N-alkyleras; 30 d) cyklosporinet med en MeBmt i 1-ställning hydreras, . e) en lineär peptid med 11 aminosyror synte- • · tiseras och peptidens tvä ändar förenas för bildande ’ * av cyklosporinet. 35
2. Förfarande enligt patentkrav 1 för fram- ställning av en förening enligt formel II' 30 111730 -W' -ocAbu-Sar-Y' Z' —MeLeu-Ala- (D)Ala-MeLeu-MeLeu-MeVal— 1 2 3 4 5 6 7 8 9 10 11 II' 5 _ kännetecknat därav, att W är MeBmt eller dihydro-MeBmt; Y’ är γ-hydroxi-MeLeu, MeVal, MeThr eller 10 Melle; och Z1 är Vai eller MeVal; pä det villkor att, dä W är MeBmt, är Y' nä-gon annan än γ-hydroxi-MeLeu.
3. Förfarande enligt patentkrav 1 eller 2, 15 for framställning av [Melle] 4-cyklosporin, k ä n n e - t e c k n a t därav, att en Tylopocladium inflatum DSM 6627-svampstam odlas i ett näringssubstrat och produk-ten isoleras ur jäsningslösningen.
4. En ren kultur av svampstammen DSM 6627. 20
5. Förfarande enligt patentkrav 1 eller 2 för framställning av cyklosporiner, vilka innehäller en eller flere γ-hydroxi-MeLeu-rester, känneteck-• · n a t därav, att en Sebekia benihana DSM 6182- svampstam odlas i ett näringssubstrat, cyklosporin, · 25 vilket innehäller en eller flere MeLeu-rester till- ,· · sätts, och produkten isoleras ur jäsningslösningen.
FI915135A 1990-11-02 1991-10-30 Förfarande för framställning av ej-immunosuppresiva cyklosporiner FI111730B (sv)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
GB909023859A GB9023859D0 (en) 1990-11-02 1990-11-02 Chemical products
GB9023859 1990-11-02
GB909023972A GB9023972D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB909023971A GB9023971D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB9023972 1990-11-05
GB909023970A GB9023970D0 (en) 1990-11-05 1990-11-05 New use of a cyclosporin derivative
GB9023971 1990-11-05
GB9023970 1990-11-05
GB919116836A GB9116836D0 (en) 1991-08-05 1991-08-05 Organic compounds
GB9116836 1991-08-05

Publications (3)

Publication Number Publication Date
FI915135A0 FI915135A0 (fi) 1991-10-30
FI915135A FI915135A (fi) 1992-05-03
FI111730B true FI111730B (sv) 2003-09-15

Family

ID=27517009

Family Applications (1)

Application Number Title Priority Date Filing Date
FI915135A FI111730B (sv) 1990-11-02 1991-10-30 Förfarande för framställning av ej-immunosuppresiva cyklosporiner

Country Status (25)

Country Link
US (3) US5767069A (sv)
EP (1) EP0484281B2 (sv)
JP (1) JP2740775B2 (sv)
KR (1) KR100203556B1 (sv)
AT (1) ATE148469T1 (sv)
AU (1) AU649277B2 (sv)
CA (1) CA2054590C (sv)
CY (1) CY2159B1 (sv)
CZ (1) CZ280909B6 (sv)
DE (1) DE69124459T3 (sv)
DK (1) DK0484281T4 (sv)
ES (1) ES2095926T5 (sv)
FI (1) FI111730B (sv)
GR (2) GR3022592T3 (sv)
HK (1) HK1005741A1 (sv)
HU (1) HU212674B (sv)
IE (1) IE913824A1 (sv)
IL (1) IL99912A (sv)
MX (1) MX9101869A (sv)
MY (1) MY134806A (sv)
NZ (1) NZ240421A (sv)
PL (1) PL168609B1 (sv)
PT (1) PT99410B (sv)
SA (1) SA92120344B1 (sv)
SK (1) SK278808B6 (sv)

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IL99912A0 (en) 1992-08-18
SK278808B6 (sk) 1998-03-04
US5981479A (en) 1999-11-09
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HK1005741A1 (en) 1999-01-22
GR3022592T3 (en) 1997-05-31
DE69124459D1 (de) 1997-03-13
DE69124459T2 (de) 1997-07-10
AU8692391A (en) 1992-05-07
PT99410A (pt) 1992-09-30
EP0484281B2 (en) 2000-11-22
HUT62337A (en) 1993-04-28
SA92120344B1 (ar) 2004-01-24
FI915135A0 (fi) 1991-10-30
EP0484281A2 (en) 1992-05-06
US6255100B1 (en) 2001-07-03
ATE148469T1 (de) 1997-02-15
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PT99410B (pt) 1999-04-30
EP0484281A3 (en) 1993-02-24
FI915135A (fi) 1992-05-03
DK0484281T4 (da) 2001-02-05
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CA2054590A1 (en) 1992-05-03
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CZ280909B6 (cs) 1996-05-15
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ES2095926T5 (es) 2001-02-16
KR920009390A (ko) 1992-06-25
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HU212674B (en) 1996-09-30
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