CL2021001698A1 - Derivados de n-(4-(oxazol-5-il)fenil)cromano-3-carboxamida y compuestos relacionados a manera de estimuladores de la producción de células precursoras de la retina para el tratamiento contra enfermedades neurorretinianas. - Google Patents

Derivados de n-(4-(oxazol-5-il)fenil)cromano-3-carboxamida y compuestos relacionados a manera de estimuladores de la producción de células precursoras de la retina para el tratamiento contra enfermedades neurorretinianas.

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Publication number
CL2021001698A1
CL2021001698A1 CL2021001698A CL2021001698A CL2021001698A1 CL 2021001698 A1 CL2021001698 A1 CL 2021001698A1 CL 2021001698 A CL2021001698 A CL 2021001698A CL 2021001698 A CL2021001698 A CL 2021001698A CL 2021001698 A1 CL2021001698 A1 CL 2021001698A1
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CL
Chile
Prior art keywords
vii
iii
group
chroman
stimulators
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CL2021001698A
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English (en)
Inventor
Matthias Steger
Alex Mueller
Mauro Marigo
Bernhard Fasching
Daphna Mokady
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Endogena Therapeutics Inc
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Publication of CL2021001698A1 publication Critical patent/CL2021001698A1/es

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

Abstract

Se describen nuevos compuestos y a un método para tratar una enfermedad de la retina que conlleva a la pérdida de fotorreceptores o degeneración de retina externa, que comprende que sea administrable el compuesto de la fórmula (I) (I) o una sal farmacéuticamente aceptable, una mezcla racémica, un enantiómero correspondiente o, si corresponde, un diastereómero correspondiente del mismo, en donde: A se selecciona a partir del grupo que consiste en un 5-oxazolilo, un piridin-4-ilo, un triazolilo, un oxadiazolilo, un imidazolilo y un residuo 2- metiloxazol-5-ilo, R1 y R12 se seleccionan indistintamente a partir del grupo que consiste en hidrógeno, fluoro, cloro, metoxilo, trifluorometilo, metilo y difluorometoxilo, B se selecciona a partir del grupo que consiste en un residuo de la fórmula (II), (III), (IV), (V), (VI), (VII), (VIII) y (IX) en donde, "*" denota el punto de unión al resto de la molécula. R2, R3, R4, R5, R2 I , R3 I , R4 I , R5 I , R2 II, R3 II, R4 II, R5 II, R2 III, R3 III, R4 III, R5 III, R2 IV, R3 IV, R4 IV, R5 IV, R2 V, R3 V, R4 V, R5 V, R2 VI, R3 VI, R4 VI, R5 VI, R2 VII, R3 VII, R4 VII, y R5 VII se seleccionan indistintamente a partir del grupo que consiste en hidrógeno, un alquilo lineal o ramificado que tiene 1 a 3 átomos de carbono, fluoro, cloro, bromo, metoxilo, etoxilo, propoxilo, 2,2,2-trifluorometilo y difluorometoxilo.
CL2021001698A 2018-12-28 2021-06-24 Derivados de n-(4-(oxazol-5-il)fenil)cromano-3-carboxamida y compuestos relacionados a manera de estimuladores de la producción de células precursoras de la retina para el tratamiento contra enfermedades neurorretinianas. CL2021001698A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

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CL2021001698A1 true CL2021001698A1 (es) 2021-12-17

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CL2021001698A CL2021001698A1 (es) 2018-12-28 2021-06-24 Derivados de n-(4-(oxazol-5-il)fenil)cromano-3-carboxamida y compuestos relacionados a manera de estimuladores de la producción de células precursoras de la retina para el tratamiento contra enfermedades neurorretinianas.

Country Status (15)

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

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* 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

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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
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CA2986692A1 (en) 2015-05-29 2016-12-08 Edge Therapeutics, Inc. Compositions and methods for reducing visual loss

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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
EA202191075A1 (ru) 2021-10-06
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
BR112021011633A2 (pt) 2021-09-08

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