MXPA03009586A - Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma. - Google Patents

Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma.

Info

Publication number
MXPA03009586A
MXPA03009586A MXPA03009586A MXPA03009586A MXPA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A MX PA03009586 A MXPA03009586 A MX PA03009586A
Authority
MX
Mexico
Prior art keywords
group
linear
alkyl group
carbon atoms
alkyl
Prior art date
Application number
MXPA03009586A
Other languages
English (en)
Inventor
Wenger Roland
Original Assignee
Debiopharm Sa
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 Debiopharm Sa filed Critical Debiopharm Sa
Publication of MXPA03009586A publication Critical patent/MXPA03009586A/es

Links

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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invencion se refiere a un pro-farmaco que comprende un undecapeptido ciclico en donde la cadena del peptido del mismo comprende por lo menos un residuo de aminoacidos de la formula general (1) en donde el atomo de carbono Ca es uno de los enlaces en dicho ciclo undecapeptido; - substituyentes Y que representan individualmente un atomo de hidrogeno o forman un enlace juntos; - los substituyentes R1 y R3 representan independientemente un atomo de hidrogeno, un grupo aralquilo, un grupo alcarilo, un grupo heteroalquilo, un grupo heterociclico, un grupo alquilo heterociclico, un grupo heterociclico alquilo, o un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado, y que es opcionalmente sustituido por al menos uno de los grupos seleccionados entre -COOH, -CONHR8, -NHCO=NH(NH2), -NHC=NR8(NH2), -NH2, -NHR8, -NR82, -N+R83, -OH, -OPO(OR8)2, -OPO(OH)(OR8), -OPO(OH)2, -OSO(OR8)2, -OSO(OH)(OR8), -OSO(OH)2, y las diferentes sales producidas de los mismos, representando independientemente cada uno de los substituyentes R8 un grupo alquilo el cual es recto o ramificado que tiene de 1 a 6 atomos de carbono; - los substituyentes R2 y R4 representan independientemente un atomo de hidrogeno, un grupo alcarilo o un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado; - los substituyentes R5 y R6 representan individualmente un atomo de hidrogeno, un grupo aralquilo, un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado; y un substituyente R7 que representa un grupo alcarilo, un grupo heteroalquilo, un grupo heterociclico, un grupo alquilo heterociclico, un grupo heterociclico alquilo o un grupo alquilo que tiene de 1 a 6 atomos de carbono el cual es recto o ramificado.
MXPA03009586A 2001-04-20 2002-04-22 Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma. MXPA03009586A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH7202001 2001-04-20
PCT/CH2002/000222 WO2002085928A2 (fr) 2001-04-20 2002-04-22 Cyclosporine modifiee utilisable en tant que pro-drogue et son utilisation

Publications (1)

Publication Number Publication Date
MXPA03009586A true MXPA03009586A (es) 2004-05-24

Family

ID=4531478

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA03009586A MXPA03009586A (es) 2001-04-20 2002-04-22 Ciclosporina modificada que puede ser usada como un pro-farmaco y uso de la misma.

Country Status (17)

Country Link
US (1) US6995139B2 (es)
EP (1) EP1379547B1 (es)
JP (1) JP4588979B2 (es)
KR (1) KR100932859B1 (es)
CN (1) CN1507451A (es)
AT (1) ATE313557T1 (es)
AU (1) AU2002245996B8 (es)
BR (1) BR0208923A (es)
CA (1) CA2444278C (es)
DE (1) DE60208180T2 (es)
ES (1) ES2256450T3 (es)
IL (1) IL158385A0 (es)
MX (1) MXPA03009586A (es)
RU (1) RU2290196C2 (es)
UA (1) UA75136C2 (es)
WO (1) WO2002085928A2 (es)
ZA (1) ZA200307794B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7232924B2 (en) 2001-06-11 2007-06-19 Xenoport, Inc. Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7186855B2 (en) 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7354574B2 (en) 2002-11-07 2008-04-08 Advanced Ocular Systems Limited Treatment of ocular disease
AU2004222306A1 (en) 2003-03-17 2004-09-30 Albany Molecular Research, Inc. Novel cyclosporins
US7083803B2 (en) 2003-09-19 2006-08-01 Advanced Ocular Systems Limited Ocular solutions
US7087237B2 (en) 2003-09-19 2006-08-08 Advanced Ocular Systems Limited Ocular solutions
US20110104186A1 (en) 2004-06-24 2011-05-05 Nicholas Valiante Small molecule immunopotentiators and assays for their detection
WO2006039163A2 (en) 2004-09-29 2006-04-13 Amr Technology, Inc. Cyclosporin alkyne analogues and their pharmaceutical uses
JP2008514702A (ja) 2004-09-29 2008-05-08 エーエムアール テクノロジー インコーポレイテッド 新規シクロスポリン類似体およびそれらの薬学的使用
WO2006041631A2 (en) 2004-10-06 2006-04-20 Amr Technology, Inc. Novel cyclosporin alkynes and their utility as pharmaceutical agents
CA2615990A1 (en) 2005-07-18 2007-01-25 Minu, L.L.C. Enhanced ocular neuroprotection/neurostimulation
US7696165B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne analogues for preventing or treating viral-induced disorders
US7696166B2 (en) 2006-03-28 2010-04-13 Albany Molecular Research, Inc. Use of cyclosporin alkyne/alkene analogues for preventing or treating viral-induced disorders
WO2008013860A2 (en) 2006-07-28 2008-01-31 Xenoport, Inc. Acyloxyalkyl carbamate prodrugs of alpha-amino acids, methods of synthesis and use
WO2009042892A1 (en) 2007-09-26 2009-04-02 Oregon Health & Science University Cyclic undecapeptides and derivatives as multiple sclerosis therapies
WO2009098533A1 (en) * 2008-02-08 2009-08-13 Debiopharm Sa Non -immunosuppressive cyclosporin for the treatment of muscular dystrophy
GB0912584D0 (en) * 2009-07-20 2009-08-26 Ucl Business Plc Cyclosporin conjugates
LT2651965T (lt) 2010-12-15 2019-01-10 Contravir Pharmaceuticals, Inc. Ciklosporino analogo molekulės su modifikuotomis 1 ir 3 aminorūgštimis
AR090964A1 (es) * 2012-05-09 2014-12-17 Novartis Ag Proceso para la elaboracion de undecapeptidos ciclicos
CN113388002A (zh) * 2021-06-10 2021-09-14 梯尔希（南京）药物研发有限公司 一种环孢菌素相关化合物的制备方法

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4396542A (en) * 1980-02-14 1983-08-02 Sandoz Ltd. Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production
ATE43335T1 (de) * 1980-02-14 1989-06-15 Sandoz Ag Peptide die einen (1s,2r,3r)- oder (1r,2s,3s)-1nitrilo-1-carbonyl-3-methyl-2-oxyheptan oder hept-5-en-rest enthalten brauchbar in totaler synsthese von cyclosporinen, und verfahren zu ihrer herstellung.
US5169773A (en) * 1984-10-04 1992-12-08 Sandoz Ltd. Monoclonal antibodies to cyclosporins
DE3478398D1 (en) * 1984-10-10 1989-07-06 Ile De France Synergistic contraceptive mixture
US4764503A (en) * 1986-11-19 1988-08-16 Sandoz Ltd. Novel cyclosporins
GB8717300D0 (en) * 1987-07-22 1987-08-26 Nat Res Dev Cyclosporins
HU201577B (en) * 1988-12-20 1990-11-28 Gyogyszerkutato Intezet Process for producing cyclosporin antibiotics
DE69124459T3 (de) * 1990-11-02 2001-05-31 Novartis Ag, Basel Zyklosporine
GB9116836D0 (en) * 1991-08-05 1991-09-18 Sandoz Ltd Organic compounds
GB9204466D0 (en) * 1992-03-02 1992-04-15 Sandoz Ltd Improvements in or relating to organic compounds
US6187547B1 (en) * 1993-09-08 2001-02-13 Novartis Ag Assay kit
GB9624038D0 (en) * 1996-11-19 1997-01-08 Sandoz Ltd Organic compounds
US6017879A (en) * 1998-04-03 2000-01-25 B.M.R.A. Corporation B.V. Template associated NPY Y2-receptor agonists
USRE40987E1 (en) 1998-07-01 2009-11-17 Debiopharm S.A. Cyclosporin with improved activity profile
US6204257B1 (en) * 1998-08-07 2001-03-20 Universtiy Of Kansas Water soluble prodrugs of hindered alcohols
WO2000046239A1 (fr) * 1999-02-05 2000-08-10 Debiopharm S.A. Derives de cyclosporine et procede de preparation desdits derives
US6765019B1 (en) * 1999-05-06 2004-07-20 University Of Kentucky Research Foundation Permeable, water soluble, non-irritating prodrugs of chemotherapeutic agents with oxaalkanoic acids
WO2001005819A1 (en) * 1999-07-15 2001-01-25 Kuhnil Pharm. Co., Ltd. Novel water soluble-cyclosporine conjugated compounds
EP2269654A3 (en) * 1999-08-24 2011-04-13 Cellgate Inc. Enhancing drug delivery across and into epithelial tissues using oligo arginine moieties

Also Published As

Publication number Publication date
KR20030094357A (ko) 2003-12-11
AU2002245996B8 (en) 2005-07-14
ZA200307794B (en) 2004-07-19
RU2003133742A (ru) 2005-03-20
AU2002245996B2 (en) 2005-06-30
EP1379547A2 (fr) 2004-01-14
JP2004536051A (ja) 2004-12-02
KR100932859B1 (ko) 2009-12-23
US6995139B2 (en) 2006-02-07
EP1379547B1 (fr) 2005-12-21
CA2444278A1 (en) 2002-10-31
RU2290196C2 (ru) 2006-12-27
CA2444278C (en) 2011-11-22
DE60208180T2 (de) 2006-08-17
BR0208923A (pt) 2004-04-27
ATE313557T1 (de) 2006-01-15
ES2256450T3 (es) 2006-07-16
IL158385A0 (en) 2004-05-12
WO2002085928A3 (fr) 2003-04-17
CN1507451A (zh) 2004-06-23
DE60208180D1 (de) 2006-01-26
WO2002085928A2 (fr) 2002-10-31
JP4588979B2 (ja) 2010-12-01
US20040138108A1 (en) 2004-07-15
UA75136C2 (en) 2006-03-15

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