EA202191075A1 - Соединения для применения в качестве терапевтически активных веществ при лечении и/или предотвращении нейроретинальных заболеваний - Google Patents

Соединения для применения в качестве терапевтически активных веществ при лечении и/или предотвращении нейроретинальных заболеваний

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Publication number
EA202191075A1
EA202191075A1 EA202191075A EA202191075A EA202191075A1 EA 202191075 A1 EA202191075 A1 EA 202191075A1 EA 202191075 A EA202191075 A EA 202191075A EA 202191075 A EA202191075 A EA 202191075A EA 202191075 A1 EA202191075 A1 EA 202191075A1
Authority
EA
Eurasian Patent Office
Prior art keywords
group
difluoromethoxy
trifluoromethyl
methoxy
chlorine
Prior art date
Application number
EA202191075A
Other languages
English (en)
Inventor
Маттиас Штегер
Алекс Мюллер
Мауро Мариго
Бернард Фашинг
Дафна Мокади
Original Assignee
Эндогена Терапьютикс, Инк.
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.)
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Publication date
Application filed by Эндогена Терапьютикс, Инк. filed Critical Эндогена Терапьютикс, Инк.
Publication of EA202191075A1 publication Critical patent/EA202191075A1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41961,2,4-Triazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Изобретение относится к новым соединениям и к способу лечения заболевания сетчатки, приводящего к потере фоторецепторов или дегенерации наружных слоев сетчатки, включающему введение соединения формулы (I)или его фармацевтически приемлемой соли, рацемической смеси, соответствующего энантиомера или, если применимо, соответствующего диастереомера, где A выбран из группы, состоящей 5-оксазолильного, пиридин-4-ильного, триазолильного, оксадиазолильного, имидазолильного и 2-метилоксазол-5-ильного остатка, R1 и R12 независимо выбраны из группы, состоящей из водорода, фтора, хлора, метокси, трифторметила, метила и дифторметокси, В выбран из группы, состоящей из остатка формулы (II), (III), (IV), (V), (VI), (VII), (VIII) и (IX)где "*" указывает место присоединения к остальной части молекулы, и R2, R3, R4, R5, R2I, R3I, R4I, R5I, R2II, R3II, R4II, R5II, R2III, R3III, R4III, R5III, R2IV, R3IV, R4IV, R5IV, R2V, R3V, R4V, R5V, R2VI, R3VI, R4VI, R5VI, R2VII, R3VII, R4VII и R5VII независимо выбраны из группы, состоящей из водорода, линейного или разветвленного алкила, содержащего от 1 до 3 атомов углерода, фтора, хлора, брома, метокси, этокси, пропокси, 2,2,2-трифторметила и дифторметокси.
EA202191075A 2018-12-28 2019-12-27 Соединения для применения в качестве терапевтически активных веществ при лечении и/или предотвращении нейроретинальных заболеваний EA202191075A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16/235,429 US10807973B2 (en) 2018-12-28 2018-12-28 Compounds for use as therapeutically active substances in the treatment of retinal diseases
PCT/US2019/068768 WO2020140050A1 (en) 2018-12-28 2019-12-27 N-(4-(oxazol-5-yl)phenyl)chromane-3-carboxamide derivatives and related compounds as stimulators of the production of retinal precursor cells for the treatment of neuroretinal diseases

Publications (1)

Publication Number Publication Date
EA202191075A1 true EA202191075A1 (ru) 2021-10-06

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ID=69191293

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EA202191075A EA202191075A1 (ru) 2018-12-28 2019-12-27 Соединения для применения в качестве терапевтически активных веществ при лечении и/или предотвращении нейроретинальных заболеваний

Country Status (15)

Country Link
US (2) US10807973B2 (ru)
EP (1) EP3902798B1 (ru)
JP (1) JP7492964B2 (ru)
KR (1) KR20210110652A (ru)
CN (1) CN113227086A (ru)
AU (1) AU2019413682B2 (ru)
BR (1) BR112021011633A2 (ru)
CA (1) CA3125327A1 (ru)
CL (1) CL2021001698A1 (ru)
EA (1) EA202191075A1 (ru)
IL (1) IL284302A (ru)
MX (1) MX2021007815A (ru)
PH (1) PH12021551133A1 (ru)
SG (1) SG11202105229TA (ru)
WO (1) WO2020140050A1 (ru)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4167999A4 (en) * 2020-06-19 2024-03-06 Endogena Therapeutics Inc NOVEL COMPOUNDS AND THEIR USE AS THERAPEUTICALLY ACTIVE SUBSTANCES IN THE TREATMENT AND/OR PREVENTION OF DISEASES INVOLVING THE RETINAL PIGMENTED EPITHELIUM
US11541039B2 (en) 2020-10-08 2023-01-03 Endogena Therapeutics, Inc. Compounds and their use as therapeutically active substances in the treatment and/or reducing signs or symptoms of diseases involving the retinal pigment epithelium

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2216439A1 (en) 1996-09-25 1998-03-25 Derek Van Der Kooy Pharmaceuticals containing retinal stem cells
US6342516B1 (en) 1998-07-31 2002-01-29 Nippon Soda Co., Ltd. Phenylazole compounds, process for producing the same and drugs for hyperlipemia
TWI243164B (en) * 2001-02-13 2005-11-11 Aventis Pharma Gmbh Acylated indanyl amines and their use as pharmaceuticals
ES2453950T3 (es) 2007-08-27 2014-04-09 AbbVie Deutschland GmbH & Co. KG 4-(4-Piridinil)-benzamidas y su uso como moduladores de la actividad de ROCK
JP2011506445A (ja) * 2007-12-13 2011-03-03 アムジエン・インコーポレーテツド γ−セクレターゼ調節剤
EP2234618A4 (en) 2007-12-21 2011-04-27 Scripps Research Inst BENZOPYRANE AND ANALOGUE AS RHO KINASE INHIBITORS
US9018202B2 (en) * 2010-12-03 2015-04-28 Allergan, Inc. Methods for treating diseases of the retina
US20130046003A1 (en) 2011-07-22 2013-02-21 Mohammed I. Dibas Pharmaceutical compositions comprising 4-bromo-n-(imidazolidin-2-ylidene)-1h-benzimidazol-5-amine for treating retinal diseases
WO2014079850A1 (en) 2012-11-23 2014-05-30 F. Hoffmann-La Roche Ag Substituted heterocyclic derivatives
DE102013110714A1 (de) 2013-09-27 2015-04-02 Eberhard Karls Universität Tübingen Medizinische Fakultät Prophylaxe und Behandlung einer nicht auf einer Proteinfaltungsstörung beruhenden neurodegenerativen Erkrankung
WO2015070170A1 (en) 2013-11-08 2015-05-14 The Translational Genomics Research Institute Compounds for cognitive enhancement and methods of use thereof
KR20220039853A (ko) 2014-11-07 2022-03-29 더 존스 홉킨스 유니버시티 N-아세틸시스테인 아미드를 사용한 색소성 망막염의 치료
CA2986692A1 (en) 2015-05-29 2016-12-08 Edge Therapeutics, Inc. Compositions and methods for reducing visual loss

Also Published As

Publication number Publication date
SG11202105229TA (en) 2021-07-29
JP7492964B2 (ja) 2024-05-30
US10807973B2 (en) 2020-10-20
EP3902798A1 (en) 2021-11-03
WO2020140050A1 (en) 2020-07-02
KR20210110652A (ko) 2021-09-08
EP3902798B1 (en) 2023-12-20
AU2019413682B2 (en) 2023-11-23
US20220089583A1 (en) 2022-03-24
AU2019413682A1 (en) 2021-06-03
EP3902798C0 (en) 2023-12-20
PH12021551133A1 (en) 2022-02-21
MX2021007815A (es) 2021-10-01
IL284302A (en) 2021-08-31
JP2022516087A (ja) 2022-02-24
CA3125327A1 (en) 2020-07-02
US20200207749A1 (en) 2020-07-02
CN113227086A (zh) 2021-08-06
CL2021001698A1 (es) 2021-12-17
BR112021011633A2 (pt) 2021-09-08

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