CA2460685C - Cyclosporine analogue mixtures and their use as immunomodulating agents - Google Patents

Cyclosporine analogue mixtures and their use as immunomodulating agents Download PDF

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Publication number
CA2460685C
CA2460685C CA2460685A CA2460685A CA2460685C CA 2460685 C CA2460685 C CA 2460685C CA 2460685 A CA2460685 A CA 2460685A CA 2460685 A CA2460685 A CA 2460685A CA 2460685 C CA2460685 C CA 2460685C
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Prior art keywords
mixture
composition
isomer
cyclosporine
day
Prior art date
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Expired - Lifetime
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CA2460685A
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English (en)
French (fr)
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CA2460685A1 (en
Inventor
Selvaraj Naicker
Randall W. Yatscoff
Robert T. Foster
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Paladin Labs Inc
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Isotechnika Inc
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Publication of CA2460685A1 publication Critical patent/CA2460685A1/en
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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
    • 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
    • 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
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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
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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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    • 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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • 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
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    • A—HUMAN NECESSITIES
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides 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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dispersion Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
CA2460685A 2001-10-19 2002-10-17 Cyclosporine analogue mixtures and their use as immunomodulating agents Expired - Lifetime CA2460685C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34620101P 2001-10-19 2001-10-19
US60/346,201 2001-10-19
PCT/CA2002/001560 WO2003033527A2 (en) 2001-10-19 2002-10-17 Cyclosporine analogue mixtures and their use as immunomodulating agents

Publications (2)

Publication Number Publication Date
CA2460685A1 CA2460685A1 (en) 2003-04-24
CA2460685C true CA2460685C (en) 2014-05-27

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Family Applications (2)

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CA2460685A Expired - Lifetime CA2460685C (en) 2001-10-19 2002-10-17 Cyclosporine analogue mixtures and their use as immunomodulating agents
CA2727642A Expired - Lifetime CA2727642C (en) 2001-10-19 2002-10-17 Synthesis of cyclosporin analogs

Family Applications After (1)

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CA2727642A Expired - Lifetime CA2727642C (en) 2001-10-19 2002-10-17 Synthesis of cyclosporin analogs

Country Status (37)

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US (2) US20110092669A1 (OSRAM)
EP (2) EP1436322B1 (OSRAM)
JP (4) JP2005511538A (OSRAM)
KR (1) KR100992850B1 (OSRAM)
CN (1) CN100344648C (OSRAM)
AR (1) AR036853A1 (OSRAM)
AT (1) ATE401339T1 (OSRAM)
AU (1) AU2002331510B2 (OSRAM)
BE (1) BE2022C547I2 (OSRAM)
BR (1) BR0213659A (OSRAM)
CA (2) CA2460685C (OSRAM)
CO (1) CO5570682A2 (OSRAM)
CY (2) CY1108410T1 (OSRAM)
DE (1) DE60227686D1 (OSRAM)
DK (1) DK1436322T3 (OSRAM)
EC (3) ECSP045061A (OSRAM)
ES (1) ES2310604T3 (OSRAM)
FI (1) FIC20220041I1 (OSRAM)
FR (1) FR22C1051I2 (OSRAM)
HR (1) HRP20040353B1 (OSRAM)
IL (2) IL160762A0 (OSRAM)
LT (1) LTC1436322I2 (OSRAM)
MA (1) MA26337A1 (OSRAM)
ME (1) ME00487B (OSRAM)
MX (1) MXPA04003624A (OSRAM)
MY (1) MY187182A (OSRAM)
NL (1) NL301200I2 (OSRAM)
NO (2) NO331745B1 (OSRAM)
NZ (1) NZ531945A (OSRAM)
PL (1) PL210697B1 (OSRAM)
PT (1) PT1436322E (OSRAM)
RU (1) RU2337106C2 (OSRAM)
SI (1) SI1436322T1 (OSRAM)
TN (1) TNSN04069A1 (OSRAM)
UY (1) UY27502A1 (OSRAM)
WO (1) WO2003033527A2 (OSRAM)
ZA (1) ZA200402270B (OSRAM)

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CA2460685C (en) * 2001-10-19 2014-05-27 Isotechnika Inc. Cyclosporine analogue mixtures and their use as immunomodulating agents
DE60231570D1 (de) 2001-10-19 2009-04-23 Isotechnika Inc Synthese von Cyclosporinanalogen
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US7378391B2 (en) 2004-09-29 2008-05-27 Amr Technology, Inc. Cyclosporin alkyne analogues and their pharmaceutical uses
US7511013B2 (en) 2004-09-29 2009-03-31 Amr Technology, Inc. Cyclosporin analogues and their pharmaceutical uses
EP1812037A4 (en) 2004-10-06 2009-11-11 Amr Technology Inc ALKYNES OF CYCLOSPORINE AND THEIR USEFUL AS PHARMACEUTICAL AGENTS
CA2592343A1 (en) * 2004-12-17 2006-06-22 Isotechnika Inc. Metabolites of cyclosporin analogs
BRPI0617781A2 (pt) * 2005-10-26 2011-08-09 Astellas Pharma Inc compostos de peptìdeos cìclicos
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
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ES2537385T3 (es) 2009-06-09 2015-06-08 Aurinia Pharmaceuticals Inc. Sistemas de suministro tópico para uso oftálmico
GB0912584D0 (en) * 2009-07-20 2009-08-26 Ucl Business Plc Cyclosporin conjugates
AU2011342284C1 (en) 2010-12-15 2017-07-13 Contravir Pharmaceuticals, Inc. Cyclosporine analogue molecules modified at amino acid 1 and 3
GB201222455D0 (en) * 2012-12-13 2013-01-30 Perioc Ltd Novel pharmaceutical formulations and their use in the treatment of periodontaldisease
WO2018102565A1 (en) * 2016-11-30 2018-06-07 Schrödinger, Inc. Graphical user interface for chemical transition state calculations
WO2018106931A1 (en) 2016-12-07 2018-06-14 Progenity Inc. Gastrointestinal tract detection methods, devices and systems
WO2018106928A1 (en) 2016-12-08 2018-06-14 Contravir Pharmaceuticals, Inc. Treatment and prevention of hbv diseases by cyclosporine analogue molecules modified at amino acides 1 and 3
US11523772B2 (en) 2016-12-14 2022-12-13 Biora Therapeutics, Inc. Treatment of a disease of the gastrointestinal tract with an immunosuppressant
US10286036B2 (en) * 2017-05-12 2019-05-14 Aurinia Pharmaceuticals Inc. Protocol for treatment of lupus nephritis
US20190224275A1 (en) 2017-05-12 2019-07-25 Aurinia Pharmaceuticals Inc. Protocol for treatment of lupus nephritis
US20230041197A1 (en) 2018-06-20 2023-02-09 Progenity, Inc. Treatment of a disease of the gastrointestinal tract with an immunomodulator
CA3172601A1 (en) * 2020-03-26 2021-09-30 Ching-Pong Mak Preparation of cyclosporin derivatives
EP4201952A1 (en) 2021-12-21 2023-06-28 Curia Spain, S.A.U. Process for the controlled synthesis of voclosporin
EP4584279A1 (en) * 2022-09-09 2025-07-16 Dr. Reddy's Laboratories Limited Improved process for the preparation of voclosporin
IT202300001116A1 (it) * 2023-01-25 2024-07-25 Indena Spa Processo per la preparazione di un intermedio utile per la sintesi di voclosporina
IT202300001056A1 (it) * 2023-01-25 2024-07-25 Procos Spa Nuovo processo per la preparazione di voclosporina amorfa
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DE60231570D1 (de) * 2001-10-19 2009-04-23 Isotechnika Inc Synthese von Cyclosporinanalogen
CA2460685C (en) * 2001-10-19 2014-05-27 Isotechnika Inc. Cyclosporine analogue mixtures and their use as immunomodulating agents

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BR0213659A (pt) 2004-10-26
FR22C1051I2 (fr) 2023-11-17
WO2003033527A3 (en) 2003-10-16
TNSN04069A1 (en) 2006-06-01
HK1062567A1 (en) 2004-11-12
KR100992850B1 (ko) 2010-11-09
MA26337A1 (fr) 2004-10-01
CY2022030I1 (el) 2023-01-27
JP2013136597A (ja) 2013-07-11
KR20050037421A (ko) 2005-04-21
MXPA04003624A (es) 2004-12-06
DE60227686D1 (de) 2008-08-28
RU2337106C2 (ru) 2008-10-27
CY2022030I2 (el) 2023-06-09
IL160762A (en) 2010-11-30
ATE401339T1 (de) 2008-08-15
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