KR20210053301A - 이소퀴놀린-스테로이드 컨쥬게이트 및 이의 용도 - Google Patents

이소퀴놀린-스테로이드 컨쥬게이트 및 이의 용도 Download PDF

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Publication number
KR20210053301A
KR20210053301A KR1020217008114A KR20217008114A KR20210053301A KR 20210053301 A KR20210053301 A KR 20210053301A KR 1020217008114 A KR1020217008114 A KR 1020217008114A KR 20217008114 A KR20217008114 A KR 20217008114A KR 20210053301 A KR20210053301 A KR 20210053301A
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South Korea
Prior art keywords
compound
subject
alkylene
formula
haloalkyl
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Abandoned
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KR1020217008114A
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English (en)
Korean (ko)
Inventor
밋첼 에이. 데롱
에릭 칼슨
케이시 코프친스키
질 엠. 스터디번트
신시아 엘. 리초로윅
Original Assignee
에어리 파마슈티컬즈, 인코포레이티드
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Publication of KR20210053301A publication Critical patent/KR20210053301A/ko
Abandoned legal-status Critical Current

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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)
KR1020217008114A 2018-08-31 2019-08-30 이소퀴놀린-스테로이드 컨쥬게이트 및 이의 용도 Abandoned KR20210053301A (ko)

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
KR20210053301A true KR20210053301A (ko) 2021-05-11

Family

ID=69639319

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217008114A Abandoned KR20210053301A (ko) 2018-08-31 2019-08-30 이소퀴놀린-스테로이드 컨쥬게이트 및 이의 용도

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
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
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
WO2007008926A1 (en) * 2005-07-11 2007-01-18 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US8455513B2 (en) * 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
BRPI0807078A2 (pt) * 2007-02-05 2014-04-08 Nicox Sa Composto, e, formulação farmacêutica
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
DK3811943T3 (da) * 2013-03-15 2023-04-03 Aerie Pharmaceuticals Inc Forbindelse til anvendelse til behandling af øjenlidelser
BR112019003232A2 (pt) * 2016-08-19 2019-06-18 Aerie Pharmaceuticals Inc compostos de beta-amino-isoquinolinil amida, composições que o incluem e métodos de obtenção
WO2020047496A1 (en) 2018-08-31 2020-03-05 Aerie Pharmaceuticals, Inc. Isoquinoline-steroid conjugates and uses thereof

Also Published As

Publication number Publication date
AU2019328590A1 (en) 2021-03-11
CN112638386A (zh) 2021-04-09
MX2021002380A (es) 2021-07-15
EP3843736A1 (en) 2021-07-07
EP3843736A4 (en) 2022-06-15
WO2020047496A1 (en) 2020-03-05
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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