BR112021003613A2 - conjugados de isoquinolina-esteróides e seus usos - Google Patents

conjugados de isoquinolina-esteróides e seus usos Download PDF

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Publication number
BR112021003613A2
BR112021003613A2 BR112021003613-0A BR112021003613A BR112021003613A2 BR 112021003613 A2 BR112021003613 A2 BR 112021003613A2 BR 112021003613 A BR112021003613 A BR 112021003613A BR 112021003613 A2 BR112021003613 A2 BR 112021003613A2
Authority
BR
Brazil
Prior art keywords
compound
alkylene
formula
compound according
alkyl
Prior art date
Application number
BR112021003613-0A
Other languages
English (en)
Portuguese (pt)
Inventor
Mitchell A. deLong
Eric Carlson
Casey Kopczynski
Jill M. Sturdivant
Cynthia L. Lichorowic
Original Assignee
Aerie Pharmaceuticals, Inc.
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 Aerie Pharmaceuticals, Inc. filed Critical Aerie Pharmaceuticals, Inc.
Publication of BR112021003613A2 publication Critical patent/BR112021003613A2/pt

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/545Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • A61K31/573Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/554Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • 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
    • A61P27/06Antiglaucoma agents or miotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/0026Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031Oxygen-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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (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)
BR112021003613-0A 2018-08-31 2019-08-30 conjugados de isoquinolina-esteróides e seus usos BR112021003613A2 (pt)

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

Publications (1)

Publication Number Publication Date
BR112021003613A2 true BR112021003613A2 (pt) 2021-05-18

Family

ID=69639319

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021003613-0A BR112021003613A2 (pt) 2018-08-31 2019-08-30 conjugados de isoquinolina-esteróides e seus usos

Country Status (10)

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

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7437384B2 (ja) 2018-08-31 2024-02-22 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 イソキノリンステロイド抱合体およびその使用
US12509469B2 (en) 2019-08-07 2025-12-30 Ripple Therapeutics Corporation Compositions and methods for the treatment of pain and dependence disorders
US20230149387A1 (en) * 2020-04-08 2023-05-18 Aerie Pharmaceuticals, Inc. Treatments
WO2021220061A2 (en) 2020-05-01 2021-11-04 Ripple Therapeutics Corporation Heterodimer compositions and methods for the treatment of ocular disorders
JP2024516193A (ja) * 2021-04-29 2024-04-12 エアリー ファーマシューティカルズ インコーポレイテッド 安定なイソキノリン-コルチコステロイドコンジュゲートおよびその使用
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

Family Cites Families (11)

* 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
US7470787B2 (en) * 2005-07-11 2008-12-30 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US8455513B2 (en) * 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
EP2109617A1 (en) * 2007-02-05 2009-10-21 Nicox S.A. Nitric oxide releasing steroids
US8450344B2 (en) * 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
EP3828172A1 (en) * 2009-05-01 2021-06-02 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
BR112015021388A2 (pt) * 2013-03-08 2017-07-18 Allergan Inc conjugados esteroides de ciclosporina a
RU2015138891A (ru) * 2013-03-08 2017-04-11 Аллерган, Инк. Конъюгаты антибиотиков, напрямую связанные со стероидными препаратами
ES2852377T3 (es) * 2013-03-15 2021-09-13 Aerie Pharmaceuticals Inc Sales dimesilato de 4-(3-amino-1-(isoquinolin-6-ilamino)-1-oxopropan-2-il)bencilo, sus combinaciones con prostaglandinas y el uso de las mismas en el tratamiento de trastornos oculares
EP3500251A4 (en) * 2016-08-19 2020-04-08 Aerie Pharmaceuticals, Inc. BETA AMINO ISOCHINOLINYL AMIDE COMPOUNDS
JP7437384B2 (ja) 2018-08-31 2024-02-22 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 イソキノリンステロイド抱合体およびその使用

Also Published As

Publication number Publication date
EP3843736A1 (en) 2021-07-07
US11691950B2 (en) 2023-07-04
CN112638386A (zh) 2021-04-09
US11059789B2 (en) 2021-07-13
US20200071275A1 (en) 2020-03-05
MX2021002380A (es) 2021-07-15
AU2019328590A1 (en) 2021-03-11
SG11202101517PA (en) 2021-03-30
AU2023204624A1 (en) 2023-08-03
JP7437384B2 (ja) 2024-02-22
WO2020047496A1 (en) 2020-03-05
KR20210053301A (ko) 2021-05-11
AU2019328590B2 (en) 2023-04-13
JP2021535147A (ja) 2021-12-16
EP3843736A4 (en) 2022-06-15
US20210300874A1 (en) 2021-09-30

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B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]