AR116659A1 - Derivados de neuroesteroides y usos de estos - Google Patents

Derivados de neuroesteroides y usos de estos

Info

Publication number
AR116659A1
AR116659A1 ARP190101187A ARP190101187A AR116659A1 AR 116659 A1 AR116659 A1 AR 116659A1 AR P190101187 A ARP190101187 A AR P190101187A AR P190101187 A ARP190101187 A AR P190101187A AR 116659 A1 AR116659 A1 AR 116659A1
Authority
AR
Argentina
Prior art keywords
hydrogen
neurosteroids
derivatives
functions
derived
Prior art date
Application number
ARP190101187A
Other languages
English (en)
Inventor
Avinash Chander Sharma
Nathan Bryson
Original Assignee
Acerus Pharmaceuticals Corp
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 Acerus Pharmaceuticals Corp filed Critical Acerus Pharmaceuticals Corp
Publication of AR116659A1 publication Critical patent/AR116659A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by only one oxygen atom doubly bound
    • 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
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05—Phenols
    • 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
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/0043—Nose
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dispersion Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Otolaryngology (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos derivados de neuroesteroides, tales como derivados de ganaxolona y alopregnanolona, que tienen una solubilidad y biodisponibilidad mejoradas. Los compuestos derivados de neuroesteroides están caracterizados por las fórmulas (1) y (2), en donde R¹ es metilo o hidrógeno, R² es una función éster (R-C(O)O-), R³ es hidrógeno, R⁴ es hidrógeno a o b, R⁵ es R-CO- o cualquier estructura de hidrocarburo (R-), y en donde R (en R² o R⁵) se selecciona independientemente de cualquier estructura que comprenda 10 átomos de carbono o menos, que sea lineal o ramificada, saturada o insaturada, que pueda comprender funciones cíclicas o aromáticas dentro de la estructura, y en donde R no contiene más de 1 OH o NR₂, o 2 funciones de éter o tioéter.
ARP190101187A 2018-05-04 2019-05-03 Derivados de neuroesteroides y usos de estos AR116659A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201862667100P 2018-05-04 2018-05-04

Publications (1)

Publication Number Publication Date
AR116659A1 true AR116659A1 (es) 2021-06-02

Family

ID=68384780

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190101187A AR116659A1 (es) 2018-05-04 2019-05-03 Derivados de neuroesteroides y usos de estos

Country Status (10)

Country Link
US (2) US20190337975A1 (es)
EP (1) EP3788055A4 (es)
JP (1) JP2021523938A (es)
CN (1) CN112823164A (es)
AR (1) AR116659A1 (es)
AU (1) AU2019264032A1 (es)
CA (1) CA3099089A1 (es)
TW (1) TW202014192A (es)
UY (1) UY38213A (es)
WO (1) WO2019211668A2 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2806877T1 (sl) 2012-01-23 2020-01-31 Sage Therapeutics, Inc. Nevroaktivne steroidne formulacije, ki obsegajo kompleks alopregnanolona in sulfobutil etra beta-ciklodekstrina
US9512165B2 (en) 2013-04-17 2016-12-06 Sage Therapeutics, Inc. 19-nor C3, 3-disubstituted C21-N-pyrazolyl steroids and methods of use thereof
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
LT3488852T (lt) 2013-08-23 2021-02-25 Sage Therapeutics, Inc. Neuroaktyvūs steroidai, kompozicijos, ir jų naudojimas
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
HUE051488T2 (hu) 2014-10-16 2021-03-01 Sage Therapeutics Inc Készítmények és eljárások központi idegrendszeri rendellenességek kezelésére
MY190408A (en) 2014-10-16 2022-04-21 Sage Therapeutics Inc Compositions and methods for treating cns disorders
ES2857082T3 (es) 2015-01-26 2021-09-28 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos del SNC
JOP20170059B1 (ar) 2016-03-08 2021-08-17 Sage Therapeutics Inc ستيرويدات وتركيبات نشطة عصبيًا واستخداماتها
DK3481845T3 (da) 2016-07-11 2023-11-27 Sage Therapeutics Inc C17, c20 og c21 substituerede neuroaktive steroider og deres anvendelsesmetoder
KR20220016098A (ko) 2019-05-31 2022-02-08 세이지 테라퓨틱스, 인크. 신경활성 스테로이드 및 이의 조성물
CA3172901A1 (en) * 2020-02-27 2021-09-02 Brii Biosciences, Inc. Prodrugs of neuroactive steroids
WO2023178299A1 (en) * 2022-03-18 2023-09-21 Marinus Pharmaceuticals, Inc. Prodrugs of ganaxolone

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB748846A (en) * 1953-10-28 1956-05-09 Vitamins Ltd A process for the manufacture of pregnan-3(-a)-ol-20-one and derivatives thereof
US5232917A (en) * 1987-08-25 1993-08-03 University Of Southern California Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series
EP0752860B1 (en) * 1994-02-14 2000-08-23 Euro-Celtique S.A. Androstanes and pregnanes for allosteric modulation of gaba receptor
US20060009432A1 (en) * 2004-07-09 2006-01-12 Roger Whiting Use of neurosteroids to treat neuropathic pain
WO2011120044A1 (en) * 2010-03-26 2011-09-29 Duke University Conjugated neuroactive steroid compositions and methods of use
FR2973031B1 (fr) * 2011-03-23 2013-11-29 Univ Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
WO2015081170A2 (en) * 2013-11-26 2015-06-04 Systamedic Inc. Ganaxolone derivatives for treatment of central nervous systems disorders
CA3068462A1 (en) * 2017-06-23 2019-12-27 The Board Of Trustees Of The University Of Illinois Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof
CN109666055A (zh) * 2017-10-16 2019-04-23 张家口华健致远生物科技有限公司 调节中枢神经治疗抑郁症的化合物及其用途

Also Published As

Publication number Publication date
UY38213A (es) 2019-10-31
JP2021523938A (ja) 2021-09-09
US20210363173A1 (en) 2021-11-25
AU2019264032A1 (en) 2020-12-03
TW202014192A (zh) 2020-04-16
CA3099089A1 (en) 2019-11-07
EP3788055A2 (en) 2021-03-10
WO2019211668A2 (en) 2019-11-07
CN112823164A (zh) 2021-05-18
WO2019211668A3 (en) 2019-12-12
EP3788055A4 (en) 2022-03-30
US20190337975A1 (en) 2019-11-07

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