MX2021002380A - Conjugados de isoquinolina-esteroide y usos de los mismos. - Google Patents

Conjugados de isoquinolina-esteroide y usos de los mismos.

Info

Publication number
MX2021002380A
MX2021002380A MX2021002380A MX2021002380A MX2021002380A MX 2021002380 A MX2021002380 A MX 2021002380A MX 2021002380 A MX2021002380 A MX 2021002380A MX 2021002380 A MX2021002380 A MX 2021002380A MX 2021002380 A MX2021002380 A MX 2021002380A
Authority
MX
Mexico
Prior art keywords
methods
compounds
isoquinoline
subject
kinase activity
Prior art date
Application number
MX2021002380A
Other languages
English (en)
Inventor
Mitchell A Delong
Eric Carlson
Jill M Sturdivant
Casey Kopczynski
Cynthia L Lichorowic
Original Assignee
Aerie Pharmaceuticals Inc
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.)
Filing date
Publication date
Application filed by Aerie Pharmaceuticals Inc filed Critical Aerie Pharmaceuticals Inc
Publication of MX2021002380A publication Critical patent/MX2021002380A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • A61K31/573Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • 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
    • 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
    • A61K47/55Medicinal 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, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • A61K47/554Medicinal 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
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/0026Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031Oxygen-containing hetero ring cyclic ketals at positions 16, 17
    • 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

Abstract

Se proporcionan en la presente compuestos y composiciones farmacéuticas útiles para modular la actividad de cinasa y enfermedades relacionadas. También se proporcionan métodos para tratar una enfermedad o trastorno ocular en un sujeto. También se proporcionan en la presente métodos para reducir la presión intraocular en un sujeto. También se proporcionan en la presente métodos para modular la actividad de cinasa en una célula. También se proporcionan en la presente métodos para hacer los compuestos provistos en la presente y compuestos útiles para la preparación de los compuestos provistos en la presente.
MX2021002380A 2018-08-31 2019-08-30 Conjugados de isoquinolina-esteroide y usos de los mismos. MX2021002380A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862725941P 2018-08-31 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
MX2021002380A true MX2021002380A (es) 2021-07-15

Family

ID=69639319

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021002380A MX2021002380A (es) 2018-08-31 2019-08-30 Conjugados de isoquinolina-esteroide y usos de los mismos.

Country Status (10)

Country Link
US (2) US11059789B2 (es)
EP (1) EP3843736A4 (es)
JP (1) JP7437384B2 (es)
KR (1) KR20210053301A (es)
CN (1) CN112638386A (es)
AU (2) AU2019328590B2 (es)
BR (1) BR112021003613A2 (es)
MX (1) MX2021002380A (es)
SG (1) SG11202101517PA (es)
WO (1) WO2020047496A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11202101517PA (en) 2018-08-31 2021-03-30 Aerie Pharmaceuticals Inc Isoquinoline-steroid conjugates and uses thereof
US20230149387A1 (en) * 2020-04-08 2023-05-18 Aerie Pharmaceuticals, Inc. Treatments
CA3176134A1 (en) 2020-05-01 2021-11-04 Ripple Therapeutics Corporation Heterodimer compositions and methods for the treatment of ocular disorders
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

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
EP1910297B1 (en) 2005-07-11 2016-05-25 Aerie Pharmaceuticals, Inc. Isoquinoline compounds
US8455513B2 (en) * 2007-01-10 2013-06-04 Aerie Pharmaceuticals, Inc. 6-aminoisoquinoline compounds
US20100234334A1 (en) * 2007-02-05 2010-09-16 Nicox S.A. Nitric oxide releasing steroids
US8450344B2 (en) * 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
EP3354643B1 (en) * 2009-05-01 2020-10-28 Aerie Pharmaceuticals, Inc. Dual mechanism inhibitors for the treatment of disease
US20140256694A1 (en) 2013-03-08 2014-09-11 Allergan, Inc. Steroid antibiotic conjugates
EP2964266A1 (en) 2013-03-08 2016-01-13 Allergan, Inc. Antibiotic conjugates directly linked with steroid drugs
US20140275160A1 (en) * 2013-03-15 2014-09-18 Aerie Pharmaceuticals, Inc. Combination therapy
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
SG11202101517PA (en) 2018-08-31 2021-03-30 Aerie Pharmaceuticals Inc Isoquinoline-steroid conjugates and uses thereof

Also Published As

Publication number Publication date
WO2020047496A1 (en) 2020-03-05
EP3843736A4 (en) 2022-06-15
US20200071275A1 (en) 2020-03-05
EP3843736A1 (en) 2021-07-07
AU2019328590A1 (en) 2021-03-11
BR112021003613A2 (pt) 2021-05-18
KR20210053301A (ko) 2021-05-11
CN112638386A (zh) 2021-04-09
AU2023204624A1 (en) 2023-08-03
JP7437384B2 (ja) 2024-02-22
AU2019328590B2 (en) 2023-04-13
US11059789B2 (en) 2021-07-13
JP2021535147A (ja) 2021-12-16
US11691950B2 (en) 2023-07-04
SG11202101517PA (en) 2021-03-30
US20210300874A1 (en) 2021-09-30

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