CA2882743C - Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes - Google Patents

Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes Download PDF

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Publication number
CA2882743C
CA2882743C CA2882743A CA2882743A CA2882743C CA 2882743 C CA2882743 C CA 2882743C CA 2882743 A CA2882743 A CA 2882743A CA 2882743 A CA2882743 A CA 2882743A CA 2882743 C CA2882743 C CA 2882743C
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Canada
Prior art keywords
unsubstituted
substituted
compound
alkyl
hydroxyl
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CA2882743A
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English (en)
French (fr)
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CA2882743A1 (en
Inventor
Wha Bin Im
Robert M. Burk
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Allergan Inc
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Allergan Inc
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Publication of CA2882743A1 publication Critical patent/CA2882743A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2882743A 2012-08-27 2013-08-23 Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes Active CA2882743C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261693437P 2012-08-27 2012-08-27
US61/693,437 2012-08-27
PCT/US2013/056418 WO2014035827A1 (en) 2012-08-27 2013-08-23 Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes

Publications (2)

Publication Number Publication Date
CA2882743A1 CA2882743A1 (en) 2014-03-06
CA2882743C true CA2882743C (en) 2021-11-30

Family

ID=49117974

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2882743A Active CA2882743C (en) 2012-08-27 2013-08-23 Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes

Country Status (11)

Country Link
US (2) US9024042B2 (https=)
EP (1) EP2888239B1 (https=)
JP (1) JP6270848B2 (https=)
KR (2) KR102304111B1 (https=)
CN (1) CN104684904B (https=)
AU (1) AU2013309124B2 (https=)
CA (1) CA2882743C (https=)
DK (1) DK2888239T3 (https=)
ES (1) ES2711425T3 (https=)
TR (1) TR201900863T4 (https=)
WO (1) WO2014035827A1 (https=)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR201900863T4 (tr) 2012-08-27 2019-02-21 Allergan Inc Beta-klorosiklopentanların hidrofilik ester ön ilaçlarının kullanılmasıyla merkezi korneal kalınlaşmanın azaltılması.
TR201902864T4 (tr) * 2014-02-20 2019-03-21 Allergan Inc Beta-klorosiklopentanların hidrofilik ester ön ilaçlarının kullanımı ile azaltılmış merkezi korneal kalınlaşma.
US9981938B2 (en) 2014-05-12 2018-05-29 Allergan, Inc. Quaternary ammonium alkyl esters as stable prodrugs
WO2015179815A1 (en) * 2014-05-22 2015-11-26 Allergan, Inc. Amidoalkylenyl and amidoaryl esters, compositions thereof, and methods for their use
CA2962766A1 (en) * 2014-10-02 2016-04-07 Allergan, Inc. Ester prodrugs of gamma-lactams and their use
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
TWI707849B (zh) 2018-02-13 2020-10-21 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
EP3820572B1 (en) 2018-07-13 2023-08-16 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors

Family Cites Families (19)

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Publication number Priority date Publication date Assignee Title
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
ATE141502T1 (de) 1991-01-15 1996-09-15 Alcon Lab Inc Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
US6353000B1 (en) 1996-11-12 2002-03-05 Alcon Laboratories, Inc. 11-halo prostaglandins for the treatment of glaucoma or ocular hypertension
DE10322843A1 (de) 2003-05-19 2004-12-16 Clariant Gmbh Verfahren zur Herstellung von Anilinboronsäuren und ihren Derivaten
WO2006047466A2 (en) 2004-10-21 2006-05-04 Duke University Ophthamological drugs
US7091231B2 (en) * 2004-12-10 2006-08-15 Allergan, Inc. 12-Aryl prostaglandin analogs
US20070254920A1 (en) 2006-04-26 2007-11-01 Aerie Pharmaceuticals, Inc. Prodrug derivatives of acids using alcohols with homotopic hydroxy groups and methods for their preparation and use
JP5570807B2 (ja) * 2006-07-11 2014-08-13 アラーガン インコーポレイテッド 抗緑内障薬としてのシクロペンタン誘導体
US7947732B2 (en) * 2007-07-13 2011-05-24 Allergan, Inc. Therapeutic substituted chlorocyclopentanols
US7732443B2 (en) * 2008-03-18 2010-06-08 Yariv Donde Therapeutic substituted cyclopentanes
US7737140B2 (en) 2008-04-24 2010-06-15 Allergan, Inc. Therapeutic compounds
US8592413B2 (en) * 2008-05-15 2013-11-26 Allergan, Inc. Therapeutic substituted cyclopentanes
PH12012500928A1 (en) 2009-11-09 2012-11-26 Allergan Inc Compositions and methods for stimulating hair growth
US20110136872A1 (en) 2009-12-09 2011-06-09 Burk Robert M Stable aqueous compositions of prostglandin agonist prodrugs and methods for use thereof
US9090595B2 (en) 2012-08-27 2015-07-28 Allergan, Inc. Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes
TR201900863T4 (tr) 2012-08-27 2019-02-21 Allergan Inc Beta-klorosiklopentanların hidrofilik ester ön ilaçlarının kullanılmasıyla merkezi korneal kalınlaşmanın azaltılması.

Also Published As

Publication number Publication date
US20140057975A1 (en) 2014-02-27
KR20150046269A (ko) 2015-04-29
AU2013309124B2 (en) 2018-03-01
CN104684904A (zh) 2015-06-03
AU2013309124A1 (en) 2015-03-12
US20150322036A1 (en) 2015-11-12
KR20200110820A (ko) 2020-09-25
CN104684904B (zh) 2017-10-13
DK2888239T3 (en) 2019-03-04
CA2882743A1 (en) 2014-03-06
EP2888239A1 (en) 2015-07-01
WO2014035827A1 (en) 2014-03-06
EP2888239B1 (en) 2018-11-28
JP2015528463A (ja) 2015-09-28
US9024042B2 (en) 2015-05-05
ES2711425T3 (es) 2019-05-03
US9427401B2 (en) 2016-08-30
KR102304111B1 (ko) 2021-09-23
JP6270848B2 (ja) 2018-01-31
HK1211031A1 (en) 2016-05-13
TR201900863T4 (tr) 2019-02-21

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CA2882743C (en) Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes
AU2015259752B2 (en) Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes
US9090595B2 (en) Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes
AU2015327817B2 (en) Ester prodrugs of gamma-lactams and their use
HK1211031B (en) Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes
HK40041854A (en) Ester prodrugs of gamma-lactams and their use
HK1229812A1 (en) Reduced central corneal thickening by use of hydrophilic ester prodrugs of beta-chlorocyclopentanes

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Effective date: 20180731

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Effective date: 20250224