CA2836946C - A crystalline form of cyclosporine a, methods of preparation, and methods for use thereof - Google Patents

A crystalline form of cyclosporine a, methods of preparation, and methods for use thereof Download PDF

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Publication number
CA2836946C
CA2836946C CA2836946A CA2836946A CA2836946C CA 2836946 C CA2836946 C CA 2836946C CA 2836946 A CA2836946 A CA 2836946A CA 2836946 A CA2836946 A CA 2836946A CA 2836946 C CA2836946 C CA 2836946C
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Canada
Prior art keywords
cyclosporine
crystalline form
eye
methods
csa
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CA2836946A
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English (en)
French (fr)
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CA2836946A1 (en
Inventor
Kiomars Karami
Richard S. Graham
Anuradha V. Gore
Scott W. Smith
Ke Wu
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.)
Allergan Inc
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Allergan Inc
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Application filed by Allergan Inc filed Critical Allergan Inc
Publication of CA2836946A1 publication Critical patent/CA2836946A1/en
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Publication of CA2836946C publication Critical patent/CA2836946C/en
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Classifications

    • 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
    • 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
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/30Extraction; Separation; Purification by precipitation
    • C07K1/306Extraction; Separation; Purification by precipitation by crystallization
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Analytical Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
CA2836946A 2011-05-27 2012-05-25 A crystalline form of cyclosporine a, methods of preparation, and methods for use thereof Active CA2836946C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161490887P 2011-05-27 2011-05-27
US61/490,887 2011-05-27
PCT/US2012/039611 WO2012166610A1 (en) 2011-05-27 2012-05-25 A crystalline form of cyclosporine a, methods of preparation, and methods for use thereof

Publications (2)

Publication Number Publication Date
CA2836946A1 CA2836946A1 (en) 2012-12-06
CA2836946C true CA2836946C (en) 2017-08-01

Family

ID=46178866

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2836946A Active CA2836946C (en) 2011-05-27 2012-05-25 A crystalline form of cyclosporine a, methods of preparation, and methods for use thereof

Country Status (19)

Country Link
US (4) US8772245B2 (https=)
EP (2) EP3521302A1 (https=)
JP (1) JP6163482B2 (https=)
KR (1) KR102079402B1 (https=)
CN (1) CN103649108B (https=)
AR (1) AR086586A1 (https=)
AU (4) AU2012262513B2 (https=)
BR (1) BR112013030554B1 (https=)
CA (1) CA2836946C (https=)
CL (1) CL2013003400A1 (https=)
IL (2) IL229475A0 (https=)
MX (1) MX362271B (https=)
MY (1) MY180581A (https=)
RU (1) RU2602062C2 (https=)
SG (1) SG10201607344UA (https=)
TW (1) TWI554522B (https=)
UA (1) UA113627C2 (https=)
WO (1) WO2012166610A1 (https=)
ZA (1) ZA201308665B (https=)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6363506B2 (ja) * 2011-11-15 2018-07-25 アラーガン、インコーポレイテッドAllergan,Incorporated シクロスポリンa2型の懸濁剤
ES2666191T3 (es) * 2011-11-15 2018-05-03 Allergan, Inc. Un proceso para la cristalización de la forma 2 de la ciclosporina A
RU2630970C2 (ru) * 2011-11-15 2017-09-15 Аллерган, Инк. Автоклавируемые взвеси циклоспорина а формы 2
RU2639393C2 (ru) * 2011-11-15 2017-12-21 Аллерган, Инк. Состав пролонгированного действия циклоспорина формы 2
JP2015519368A (ja) 2012-06-01 2015-07-09 アラーガン インコーポレイテッドAllergan,Incorporated シクロスポリンa類似体
GB201222455D0 (en) * 2012-12-13 2013-01-30 Perioc Ltd Novel pharmaceutical formulations and their use in the treatment of periodontaldisease
US10524661B2 (en) * 2013-06-12 2020-01-07 Proactive Live, Inc. Sleep monitoring and stimulation
MY196111A (en) 2014-07-18 2023-03-15 Allergan Inc Suspension Compositions of Cyclosporin a for Subconjunctival and Periocular Injection
US9914755B2 (en) 2015-01-08 2018-03-13 Allergan, Inc. Cyclosporin derivatives wherein the MeBmt sidechain has been cyclized
US10443292B2 (en) * 2016-04-25 2019-10-15 Magna Closures, Inc. Non-contact obstacle detection system for motor vehicles
KR102287226B1 (ko) 2017-05-17 2021-08-11 주식회사 유유제약 신규한 펩타이드 및 이를 유효성분으로 포함하는 안구질환 치료용 약학 조성물
US11613558B2 (en) 2018-11-14 2023-03-28 Yuyu Pharma, Inc. Peptides and pharmaceutical compositions for treating eye diseases
WO2021224901A2 (en) * 2021-08-20 2021-11-11 Sun Pharmaceutical Industries Limited Stable cyclosporine ophthalmic formulation and manufacturing process thereof
EP4585605A1 (en) * 2022-10-20 2025-07-16 Chugai Seiyaku Kabushiki Kaisha Method for producing cyclic peptide crystals
KR20250160895A (ko) 2023-03-20 2025-11-14 추가이 세이야쿠 가부시키가이샤 고리형 펩타이드의 공결정을 제조하는 방법

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU203564B (en) * 1987-12-21 1991-08-28 Sandoz Ag Process for producing new orthorombos cyclosporin without solvatation
GB9105705D0 (en) * 1991-03-18 1991-05-01 Sandoz Ltd Improvements in or relating to organic compounds
US5474979A (en) 1994-05-17 1995-12-12 Allergan, Inc. Nonirritating emulsions for sensitive tissue
US6254860B1 (en) 1999-04-13 2001-07-03 Allergan Sales, Inc. Ocular treatment using cyclosporin-A derivatives
US6656504B1 (en) * 1999-09-09 2003-12-02 Elan Pharma International Ltd. Nanoparticulate compositions comprising amorphous cyclosporine and methods of making and using such compositions
CA2686234A1 (en) * 2007-05-04 2008-11-13 Allergan, Inc. Use of cyclosporines in the treatment of patients with intraocular lenses
JP2011508776A (ja) * 2008-01-04 2011-03-17 アルコン ファーマシューティカルズ リミテッド 安定な水性シクロスポリン組成物

Also Published As

Publication number Publication date
CN103649108A (zh) 2014-03-19
UA113627C2 (xx) 2017-02-27
MY180581A (en) 2020-12-02
TWI554522B (zh) 2016-10-21
NZ719272A (en) 2017-10-27
EP3521302A1 (en) 2019-08-07
BR112013030554B1 (pt) 2020-12-15
MX2013013855A (es) 2014-02-17
EP2714720A1 (en) 2014-04-09
US20160083432A1 (en) 2016-03-24
IL290158A (en) 2022-03-01
JP6163482B2 (ja) 2017-07-12
SG10201607344UA (en) 2016-10-28
RU2602062C2 (ru) 2016-11-10
AU2012262513A1 (en) 2013-12-12
US8772245B2 (en) 2014-07-08
KR102079402B1 (ko) 2020-02-19
US9206228B2 (en) 2015-12-08
MX362271B (es) 2019-01-10
RU2013155033A (ru) 2015-07-20
US20140315827A1 (en) 2014-10-23
WO2012166610A1 (en) 2012-12-06
US20130023482A1 (en) 2013-01-24
ZA201308665B (en) 2014-07-30
AR086586A1 (es) 2014-01-08
AU2019204192A1 (en) 2019-07-04
BR112013030554A2 (pt) 2016-09-06
EP2714720B1 (en) 2018-12-26
US20210269484A1 (en) 2021-09-02
TW201311730A (zh) 2013-03-16
CA2836946A1 (en) 2012-12-06
AU2017265008A1 (en) 2017-12-07
AU2016203990A1 (en) 2016-06-30
NZ618213A (en) 2016-05-27
JP2014515372A (ja) 2014-06-30
AU2019204192B2 (en) 2021-02-04
AU2012262513B2 (en) 2016-03-17
CN103649108B (zh) 2017-03-29
KR20140047054A (ko) 2014-04-21
CL2013003400A1 (es) 2014-08-18
IL229475A0 (en) 2014-01-30

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