AU2019328590B2 - Isoquinoline-steroid conjugates and uses thereof - Google Patents

Isoquinoline-steroid conjugates and uses thereof Download PDF

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Publication number
AU2019328590B2
AU2019328590B2 AU2019328590A AU2019328590A AU2019328590B2 AU 2019328590 B2 AU2019328590 B2 AU 2019328590B2 AU 2019328590 A AU2019328590 A AU 2019328590A AU 2019328590 A AU2019328590 A AU 2019328590A AU 2019328590 B2 AU2019328590 B2 AU 2019328590B2
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AU
Australia
Prior art keywords
compound
subject
alkylene
need
formula
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Legal status (The legal status 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 status listed.)
Ceased
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AU2019328590A
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English (en)
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AU2019328590A1 (en
Inventor
Eric Carlson
Mitchell A. Delong
Casey Kopczynski
Cynthia L. Lichorowic
Jill M. Sturdivant
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.)
Aerie Pharmaceuticals Inc
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Aerie Pharmaceuticals Inc
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Filing date
Publication date
Application filed by Aerie Pharmaceuticals Inc filed Critical Aerie Pharmaceuticals Inc
Publication of AU2019328590A1 publication Critical patent/AU2019328590A1/en
Application granted granted Critical
Publication of AU2019328590B2 publication Critical patent/AU2019328590B2/en
Priority to AU2023204624A priority Critical patent/AU2023204624A1/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/545—Heterocyclic compounds
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/55—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/0026—Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031—Oxygen-containing hetero ring cyclic ketals at positions 16, 17

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Botany (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
AU2019328590A 2018-08-31 2019-08-30 Isoquinoline-steroid conjugates and uses thereof Ceased AU2019328590B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2023204624A AU2023204624A1 (en) 2018-08-31 2023-07-12 Isoquinoline-steroid conjugates and uses thereof

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862725941P 2018-08-31 2018-08-31
US62/725,941 2018-08-31
PCT/US2019/049195 WO2020047496A1 (en) 2018-08-31 2019-08-30 Isoquinoline-steroid conjugates and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2023204624A Division AU2023204624A1 (en) 2018-08-31 2023-07-12 Isoquinoline-steroid conjugates and uses thereof

Publications (2)

Publication Number Publication Date
AU2019328590A1 AU2019328590A1 (en) 2021-03-11
AU2019328590B2 true AU2019328590B2 (en) 2023-04-13

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
AU2019328590A Ceased AU2019328590B2 (en) 2018-08-31 2019-08-30 Isoquinoline-steroid conjugates and uses thereof
AU2023204624A Abandoned AU2023204624A1 (en) 2018-08-31 2023-07-12 Isoquinoline-steroid conjugates and uses thereof

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2023204624A Abandoned AU2023204624A1 (en) 2018-08-31 2023-07-12 Isoquinoline-steroid conjugates and uses thereof

Country Status (10)

Country Link
US (2) US11059789B2 (enExample)
EP (1) EP3843736A4 (enExample)
JP (1) JP7437384B2 (enExample)
KR (1) KR20210053301A (enExample)
CN (1) CN112638386A (enExample)
AU (2) AU2019328590B2 (enExample)
BR (1) BR112021003613A2 (enExample)
MX (1) MX2021002380A (enExample)
SG (1) SG11202101517PA (enExample)
WO (1) WO2020047496A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2020047496A1 (en) 2018-08-31 2020-03-05 Aerie Pharmaceuticals, Inc. Isoquinoline-steroid conjugates and uses thereof
US12509469B2 (en) 2019-08-07 2025-12-30 Ripple Therapeutics Corporation Compositions and methods for the treatment of pain and dependence disorders
WO2021207486A1 (en) * 2020-04-08 2021-10-14 Aerie Pharmaceuticals, Inc. Treatments
CA3176134A1 (en) * 2020-05-01 2021-11-04 Ripple Therapeutics Corporation Heterodimer compositions and methods for the treatment of ocular disorders
AU2022264917A1 (en) * 2021-04-29 2023-11-02 Alcon Inc. Stable isoquinoline-corticosteroid conjugates and uses thereof
EP4426712A4 (en) * 2021-11-03 2026-04-08 Ripple Therapeutics Corp COMPOSITIONS SUITABLE FOR PROCESSING AND THEIR USE
CN115340472B (zh) * 2022-09-19 2024-05-07 合肥工业大学 一种谷氨酸衍生物及其合成方法和应用

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3193459A (en) * 1955-07-01 1965-07-06 Upjohn Co Steroid hemisuccinate compositions and method for extemporaneous administration
WO2010127329A1 (en) * 2009-05-01 2010-11-04 Aerie Pharmaceuticals, Inc. Dual-action inhibitors and methods of using same
US8450344B2 (en) * 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
US20150119419A1 (en) * 2007-01-10 2015-04-30 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US9402913B2 (en) * 2013-03-08 2016-08-02 Allergan, Inc. Cyclosporine A steroid conjugates
US9402912B2 (en) * 2013-03-08 2016-08-02 Allergan, Inc. Antibiotic conjugates directly linked with steroid drugs

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2580108T3 (es) * 2005-07-11 2016-08-19 Aerie Pharmaceuticals, Inc Compuestos de isoquinolina
MX2009008334A (es) * 2007-02-05 2009-08-12 Nicox Sa Esteroides que liberan oxido nitrico.
ES2776199T3 (es) * 2013-03-15 2020-07-29 Aerie Pharmaceuticals Inc Conjugados de compuestos de isoquinolina y prostaglandinas
JP2019529359A (ja) * 2016-08-19 2019-10-17 アエリエ ファーマシューティカルズ インコーポレイテッド ベータ−アミノ−イソキノリニルアミド化合物
WO2020047496A1 (en) 2018-08-31 2020-03-05 Aerie Pharmaceuticals, Inc. Isoquinoline-steroid conjugates and uses thereof

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3193459A (en) * 1955-07-01 1965-07-06 Upjohn Co Steroid hemisuccinate compositions and method for extemporaneous administration
US20150119419A1 (en) * 2007-01-10 2015-04-30 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US8450344B2 (en) * 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
WO2010127329A1 (en) * 2009-05-01 2010-11-04 Aerie Pharmaceuticals, Inc. Dual-action inhibitors and methods of using same
US9402913B2 (en) * 2013-03-08 2016-08-02 Allergan, Inc. Cyclosporine A steroid conjugates
US9402912B2 (en) * 2013-03-08 2016-08-02 Allergan, Inc. Antibiotic conjugates directly linked with steroid drugs

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Levine et al. 'Targeting the Androgen Receptor with Steroid Conjugates', J. Med. Chem. 2014, 57, 8224−8237. *
PUBCHEM, (2005-06-24), Database accession no. 656804 *

Also Published As

Publication number Publication date
WO2020047496A1 (en) 2020-03-05
US11059789B2 (en) 2021-07-13
AU2019328590A1 (en) 2021-03-11
EP3843736A1 (en) 2021-07-07
MX2021002380A (es) 2021-07-15
US20210300874A1 (en) 2021-09-30
JP7437384B2 (ja) 2024-02-22
JP2021535147A (ja) 2021-12-16
KR20210053301A (ko) 2021-05-11
AU2023204624A1 (en) 2023-08-03
US20200071275A1 (en) 2020-03-05
US11691950B2 (en) 2023-07-04
CN112638386A (zh) 2021-04-09
BR112021003613A2 (pt) 2021-05-18
SG11202101517PA (en) 2021-03-30
EP3843736A4 (en) 2022-06-15

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