AR036853A1 - Mezclas de analogos de ciclosporina y su uso como agentes inmunomoduladores. - Google Patents

Mezclas de analogos de ciclosporina y su uso como agentes inmunomoduladores.

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Publication number
AR036853A1
AR036853A1 ARP020103918A ARP020103918A AR036853A1 AR 036853 A1 AR036853 A1 AR 036853A1 AR P020103918 A ARP020103918 A AR P020103918A AR P020103918 A ARP020103918 A AR P020103918A AR 036853 A1 AR036853 A1 AR 036853A1
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AR
Argentina
Prior art keywords
isomers
isomer
isatx247
mixtures
derivatives
Prior art date
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ARP020103918A
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English (en)
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Isotechnika Inc
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Publication of AR036853A1 publication Critical patent/AR036853A1/es

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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
    • C07K7/645Cyclosporins; Related peptides
    • 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
    • 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
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
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    • 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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    • 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
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    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
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    • A61P31/12Antivirals
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    • AHUMAN NECESSITIES
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
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    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
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  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
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  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Dispersion Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Emergency Medicine (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)

Abstract

Mezclas isoméricas de análogos de ciclosporina que son estructuralmente similares a la ciclosporina A. Las mezclas poseen una eficacia mejorada y una toxicidad reducida respecto de los isómeros individuales y las ciclosporinas y derivados de ciclosporinas naturales y otros actualmente conocidos. Las realizaciones de la presente invención se refieren a los isómeros cis y trans de los análogos de la ciclosporina A conocidos como ISATX247, y derivados de los mismos. Las mezclas de isómeros ISATX247 muestran una combinación de potencia mejorada y toxicidad reducida respecto de las ciclospirinas naturales y actualmente conocidas. Los isómeros ISATX247 y los derivados alquilados, arilados y deuterados se sintentizan por medio de vías estereoselectivas donde las condiciones particulares de reacción determinan el grado de estereoselectividad. Las vías estereoselectivas pueden utilizar una reacción de Wittig o un reactivo organometálico que comprende elementos inorgánicos tales como boro, silicio, titanio y litio. La relación de los isómeros en una mezcla puede variar entre aproximadamente 10 y 90% en peso del isómero (E), entre aproximadamente 90 y 10% en peso del isómero (Z), sobre la base del peso total de la mezcla. Reivindicación 1: Una composición, caracterizada porque comprende una mezcla isomérica de un análogo de ciclosporina modificado en el residuo del aminoácido 1 con un sustituyente de 1,3-dieno, donde el rango de mezcla isomérica para el sustituyente de dieno comprende entre aproximadamente 10% y aproximadamente 90% para el isómero E y entre aproximadamente 90% y aproximadamente 10% del isómero Z. Reivindicación 2: La composición de la reivindicación 1, caracterizada porque los isómeros no deuterados son los isómeros E y Z, según se indica en fórmulas 1 y 2.
ARP020103918A 2001-10-19 2002-10-17 Mezclas de analogos de ciclosporina y su uso como agentes inmunomoduladores. AR036853A1 (es)

Applications Claiming Priority (1)

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US34620101P 2001-10-19 2001-10-19

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AR036853A1 true AR036853A1 (es) 2004-10-06

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US (2) US20110092669A1 (es)
EP (2) EP1436322B1 (es)
JP (4) JP2005511538A (es)
KR (1) KR100992850B1 (es)
CN (1) CN100344648C (es)
AR (1) AR036853A1 (es)
AT (1) ATE401339T1 (es)
AU (1) AU2002331510B2 (es)
BE (1) BE2022C547I2 (es)
BR (1) BR0213659A (es)
CA (2) CA2460685C (es)
CO (1) CO5570682A2 (es)
CY (2) CY1108410T1 (es)
DE (1) DE60227686D1 (es)
DK (1) DK1436322T3 (es)
EC (3) ECSP045060A (es)
ES (1) ES2310604T3 (es)
FI (1) FIC20220041I1 (es)
FR (1) FR22C1051I2 (es)
HK (1) HK1062567A1 (es)
HR (1) HRP20040353B1 (es)
IL (2) IL160762A0 (es)
LT (1) LTC1436322I2 (es)
MA (1) MA26337A1 (es)
ME (1) ME00487B (es)
MX (1) MXPA04003624A (es)
MY (1) MY187182A (es)
NL (1) NL301200I2 (es)
NO (2) NO331745B1 (es)
NZ (1) NZ531945A (es)
PL (1) PL210697B1 (es)
PT (1) PT1436322E (es)
RU (1) RU2337106C2 (es)
SI (1) SI1436322T1 (es)
TN (1) TNSN04069A1 (es)
UY (1) UY27502A1 (es)
WO (1) WO2003033527A2 (es)
ZA (1) ZA200402270B (es)

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WO2024052941A1 (en) * 2022-09-09 2024-03-14 Dr. Reddy's Laboratories Limited Improved process for the preparation of voclosporin
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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 (es) 2022-11-10
US20140288266A1 (en) 2014-09-25
WO2003033527A3 (en) 2003-10-16
US20110092669A1 (en) 2011-04-21
HRP20040353A2 (en) 2005-04-30
IL160762A (en) 2010-11-30
RU2004110941A (ru) 2005-08-10
NZ531945A (en) 2006-01-27
PT1436322E (pt) 2008-10-23
CN1571794A (zh) 2005-01-26
CY1108410T1 (el) 2012-05-23
ME00487B (me) 2011-10-10
ATE401339T1 (de) 2008-08-15
CY2022030I1 (el) 2023-01-27
PL210697B1 (pl) 2012-02-29
JP2011006417A (ja) 2011-01-13
BE2022C547I2 (es) 2022-10-19
DE60227686D1 (de) 2008-08-28
RU2337106C2 (ru) 2008-10-27
CA2460685C (en) 2014-05-27
MA26337A1 (fr) 2004-10-01
MXPA04003624A (es) 2004-12-06
SI1436322T1 (sl) 2008-12-31
ES2310604T3 (es) 2009-01-16
CA2460685A1 (en) 2003-04-24
HRP20040353B1 (hr) 2012-10-31
AU2002331510B2 (en) 2008-05-01
CO5570682A2 (es) 2005-10-31
BR0213659A (pt) 2004-10-26
NO2022042I1 (no) 2022-10-14
JP2013136597A (ja) 2013-07-11
KR100992850B1 (ko) 2010-11-09
UY27502A1 (es) 2003-04-30
EP1816138A1 (en) 2007-08-08
CA2727642A1 (en) 2003-04-24
IL160762A0 (en) 2004-08-31
LTC1436322I2 (es) 2023-06-26
PL370501A1 (en) 2005-05-30
MY187182A (en) 2021-09-08
JP2009197036A (ja) 2009-09-03
EP1436322A2 (en) 2004-07-14
FIC20220041I1 (fi) 2022-10-14
JP5272140B2 (ja) 2013-08-28
FR22C1051I1 (fr) 2022-12-16
KR20050037421A (ko) 2005-04-21
CA2727642C (en) 2014-02-04
ECSP045059A (es) 2004-07-23
WO2003033527A2 (en) 2003-04-24
NO20042029L (no) 2004-05-14
EP1436322B1 (en) 2008-07-16
HK1062567A1 (en) 2004-11-12
NO331745B1 (no) 2012-03-19
ECSP045061A (es) 2004-08-27
TNSN04069A1 (en) 2006-06-01
FR22C1051I2 (fr) 2023-11-17
JP2005511538A (ja) 2005-04-28

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