CN112638386A - 异喹啉-类固醇缀合物及其用途 - Google Patents

异喹啉-类固醇缀合物及其用途 Download PDF

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Publication number
CN112638386A
CN112638386A CN201980056414.7A CN201980056414A CN112638386A CN 112638386 A CN112638386 A CN 112638386A CN 201980056414 A CN201980056414 A CN 201980056414A CN 112638386 A CN112638386 A CN 112638386A
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China
Prior art keywords
compound
subject
alkylene
formula
alkyl
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Pending
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CN201980056414.7A
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English (en)
Chinese (zh)
Inventor
米切尔·A·德隆
埃里克·卡尔森
凯西·科普琴斯基
吉尔·M·斯特迪文特
辛西娅·L·利科罗威克
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Aerie Pharmaceuticals Inc
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Aerie Pharmaceuticals Inc
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Publication of CN112638386A publication Critical patent/CN112638386A/zh
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    • 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
    • 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
    • A61K47/55—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
CN201980056414.7A 2018-08-31 2019-08-30 异喹啉-类固醇缀合物及其用途 Pending CN112638386A (zh)

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
CN112638386A true CN112638386A (zh) 2021-04-09

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Family Applications (1)

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CN201980056414.7A Pending CN112638386A (zh) 2018-08-31 2019-08-30 异喹啉-类固醇缀合物及其用途

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=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115340472A (zh) * 2022-09-19 2022-11-15 合肥工业大学 一种谷氨酸衍生物及其合成方法和应用

Families Citing this family (6)

* 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
WO2021024041A1 (en) 2019-08-07 2021-02-11 Ripple Therapeutics Corporation Controlled release drug dimers
WO2021207486A1 (en) * 2020-04-08 2021-10-14 Aerie Pharmaceuticals, Inc. Treatments
MX2022013665A (es) 2020-05-01 2022-11-30 Ripple Therapeutics Corp Composiciones y metodos heterodimeros para el tratamiento de trastornos oculares.
WO2022232602A1 (en) * 2021-04-29 2022-11-03 Aerie Pharmaceuticals, Inc. Stable isoquinoline-corticosteroid conjugates and uses thereof
WO2023079362A1 (en) * 2021-11-03 2023-05-11 Ripple Therapeutics Corporation Processable compositions and use for the same

Citations (4)

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CN101652380A (zh) * 2007-02-05 2010-02-17 尼科克斯公司 释放一氧化氮的类固醇
US20150119419A1 (en) * 2007-01-10 2015-04-30 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
CN105263494A (zh) * 2013-03-15 2016-01-20 爱瑞制药公司 联合治疗
US20180050990A1 (en) * 2016-08-19 2018-02-22 Aerie Pharmaceuticals, Inc. Beta-amino-isoquinolinyl amide compounds

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US3193459A (en) 1955-07-01 1965-07-06 Upjohn Co Steroid hemisuccinate compositions and method for extemporaneous administration
WO2007008926A1 (en) * 2005-07-11 2007-01-18 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US8450344B2 (en) * 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
EP3053913B1 (en) * 2009-05-01 2018-03-07 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
MX2015011948A (es) * 2013-03-08 2015-12-09 Allergan Inc Antibioticos conjugados directamente relacionados con farmacos esteroides.
WO2014138425A1 (en) * 2013-03-08 2014-09-12 Allergan, Inc. Cyclosporine a-steroid conjugates
WO2020047496A1 (en) 2018-08-31 2020-03-05 Aerie Pharmaceuticals, Inc. Isoquinoline-steroid conjugates and uses thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150119419A1 (en) * 2007-01-10 2015-04-30 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
CN101652380A (zh) * 2007-02-05 2010-02-17 尼科克斯公司 释放一氧化氮的类固醇
CN105263494A (zh) * 2013-03-15 2016-01-20 爱瑞制药公司 联合治疗
US20180050990A1 (en) * 2016-08-19 2018-02-22 Aerie Pharmaceuticals, Inc. Beta-amino-isoquinolinyl amide compounds

Non-Patent Citations (1)

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BAHRAM KHOOBEHI等: "Enhanced Oxygen Saturation in Optic Nerve Head of Non-Human Primate Eyes Following the Intravitreal Injection of NCX 434, an Innovative Nitric Oxide-Donating Glucocorticoid" *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN115340472A (zh) * 2022-09-19 2022-11-15 合肥工业大学 一种谷氨酸衍生物及其合成方法和应用
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

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Publication number Publication date
AU2019328590A1 (en) 2021-03-11
MX2021002380A (es) 2021-07-15
EP3843736A1 (en) 2021-07-07
EP3843736A4 (en) 2022-06-15
WO2020047496A1 (en) 2020-03-05
KR20210053301A (ko) 2021-05-11
AU2019328590B2 (en) 2023-04-13
AU2023204624A1 (en) 2023-08-03
US11059789B2 (en) 2021-07-13
SG11202101517PA (en) 2021-03-30
BR112021003613A2 (pt) 2021-05-18
JP7437384B2 (ja) 2024-02-22
US11691950B2 (en) 2023-07-04
US20210300874A1 (en) 2021-09-30
JP2021535147A (ja) 2021-12-16
US20200071275A1 (en) 2020-03-05

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