KR20220003555A - 안구 장애의 치료를 위한 화합물 및 방법 - Google Patents

안구 장애의 치료를 위한 화합물 및 방법 Download PDF

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Publication number
KR20220003555A
KR20220003555A KR1020217037591A KR20217037591A KR20220003555A KR 20220003555 A KR20220003555 A KR 20220003555A KR 1020217037591 A KR1020217037591 A KR 1020217037591A KR 20217037591 A KR20217037591 A KR 20217037591A KR 20220003555 A KR20220003555 A KR 20220003555A
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South Korea
Prior art keywords
alkyl
heteroalkyl
optionally substituted
compound
heterocyclyl
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KR1020217037591A
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English (en)
Korean (ko)
Inventor
이안 홀메스
야이르 올스터
힐라 바라쉬
찰스 보즈워스
오머 라파엘리
마크 글레슨
마크 리차드 스튜어트
로버트 엠. 버크
조나단 둔
니콜라스 채프먼
Original Assignee
아주라 오프탈믹스 엘티디
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Priority claimed from PCT/IB2020/000288 external-priority patent/WO2020212755A1/en
Publication of KR20220003555A publication Critical patent/KR20220003555A/ko
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D211/60Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020217037591A 2019-04-18 2020-04-16 안구 장애의 치료를 위한 화합물 및 방법 Ceased KR20220003555A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962835963P 2019-04-18 2019-04-18
US62/835,963 2019-04-18
PCT/IB2020/000288 WO2020212755A1 (en) 2019-04-18 2020-04-16 Compounds and methods for the treatment of ocular disorders

Publications (1)

Publication Number Publication Date
KR20220003555A true KR20220003555A (ko) 2022-01-10

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217037591A Ceased KR20220003555A (ko) 2019-04-18 2020-04-16 안구 장애의 치료를 위한 화합물 및 방법

Country Status (6)

Country Link
US (3) US10875845B2 (https=)
EP (1) EP3955926A4 (https=)
JP (1) JP7700045B2 (https=)
KR (1) KR20220003555A (https=)
CN (1) CN114025759A (https=)
IL (1) IL287264A (https=)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7700045B2 (ja) * 2019-04-18 2025-06-30 アズーラ オフサルミックス エルティーディー. 眼障害を処置するための化合物および方法
IL302175A (en) * 2020-10-21 2023-06-01 Azura Ophthalmics Ltd Compounds and methods for the treatment of ocular disorders
EP4232034A4 (en) * 2020-10-21 2024-12-04 Azura Ophthalmics Ltd COMPOUNDS AND METHODS FOR TREATING EYE DISORDERS
US11459351B1 (en) 2021-04-05 2022-10-04 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders
EP4419502A4 (en) * 2021-10-20 2025-10-29 Azura Ophthalmics Ltd COMPOUNDS AND METHODS FOR THE TREATMENT OF SKIN AND OCULAR DISORDERS

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US6334997B1 (en) 1994-03-25 2002-01-01 Isotechnika, Inc. Method of using deuterated calcium channel blockers
ES2293638T3 (es) 1994-03-25 2008-03-16 Isotechnika, Inc. Mejora de la eficacia de farmacos por deuteracion.
US7056893B2 (en) 1999-03-31 2006-06-06 Insite Vision, Inc. Topical treatment for prevention of ocular infections
US6239113B1 (en) 1999-03-31 2001-05-29 Insite Vision, Incorporated Topical treatment or prevention of ocular infections
EP1483579A4 (en) 2002-02-15 2006-07-12 Merckle Gmbh CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, PROCESS FOR THEIR MANUFACTURE AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF
CA2544678C (en) 2003-11-05 2013-12-31 Sunesis Pharmaceuticals, Inc. Modulators of cellular adhesion
DK2444079T3 (en) 2005-05-17 2017-01-30 Sarcode Bioscience Inc Compositions and Methods for the Treatment of Eye Diseases
DE102005062987A1 (de) 2005-12-28 2007-07-05 Grünenthal GmbH Substituierte Propiolsäureamide und ihre Verwendung zur Herstellung von Arzneimitteln
WO2009128934A1 (en) * 2008-04-15 2009-10-22 Sarcode Corporation Topical lfa-1 antagonists for use in localized treatment of immune related disorders
WO2009139817A2 (en) 2008-04-15 2009-11-19 Sarcode Corporation Crystalline pharmaceutical and methods of preparation and use thereof
US20090257957A1 (en) * 2008-04-15 2009-10-15 John Burnier Aerosolized LFA-1 antagonists for use in localized treatment of immune related disorders
WO2011050175A1 (en) 2009-10-21 2011-04-28 Sarcode Corporation Crystalline pharmaceutical and methods of preparation and use thereof
KR20200108932A (ko) * 2012-07-25 2020-09-21 에스에이알코드 바이오사이언스 인코포레이티드 Lfa-1 저해제 및 그의 다형체
BR112015014367B1 (pt) * 2012-12-19 2022-11-22 Novartis Ag Composição inibidora de lfa-1, método para estabilizar a dita composição e uso da mesma para tratar uma doença ocular
US9463201B2 (en) 2014-10-19 2016-10-11 M.G. Therapeutics Ltd Compositions and methods for the treatment of meibomian gland dysfunction
JP2019513775A (ja) 2016-04-19 2019-05-30 アズーラ オフサルミックス エルティーディー. 角化症の処置のための組成物
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EP3955937A4 (en) 2019-04-18 2023-01-18 Azura Ophthalmics Ltd. COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF EYE DISEASES
WO2020212755A1 (en) 2019-04-18 2020-10-22 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders
JP7700045B2 (ja) 2019-04-18 2025-06-30 アズーラ オフサルミックス エルティーディー. 眼障害を処置するための化合物および方法
IL302173A (en) 2020-10-21 2023-06-01 Azura Ophthalmics Ltd Compounds and methods for the treatment of ocular disorders
US11459351B1 (en) 2021-04-05 2022-10-04 Azura Ophthalmics Ltd. Compounds and methods for the treatment of ocular disorders

Also Published As

Publication number Publication date
JP7700045B2 (ja) 2025-06-30
US20210107899A1 (en) 2021-04-15
CN114025759A (zh) 2022-02-08
EP3955926A4 (en) 2022-11-30
US11634411B2 (en) 2023-04-25
US20200331896A1 (en) 2020-10-22
EP3955926A1 (en) 2022-02-23
IL287264A (en) 2021-12-01
US10875845B2 (en) 2020-12-29
US20230357207A1 (en) 2023-11-09
JP2022530322A (ja) 2022-06-29

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