AR121661A2 - Esteroides neuroactivos, composiciones y usos de los mismos - Google Patents

Esteroides neuroactivos, composiciones y usos de los mismos

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Publication number
AR121661A2
AR121661A2 ARP210100747A ARP210100747A AR121661A2 AR 121661 A2 AR121661 A2 AR 121661A2 AR P210100747 A ARP210100747 A AR P210100747A AR P210100747 A ARP210100747 A AR P210100747A AR 121661 A2 AR121661 A2 AR 121661A2
Authority
AR
Argentina
Prior art keywords
disorders
alkyl
alkoxy
xra
nrbrc
Prior art date
Application number
ARP210100747A
Other languages
English (en)
Inventor
Botella Gabriel Martinez
Boyd L Harrison
Albert Jean Robichaud
Richard Thomas Beresis
Original Assignee
Sage Therapeutics 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 Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of AR121661A2 publication Critical patent/AR121661A2/es

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Classifications

    • 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
    • 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
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0018Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J13/00Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C07J7/007Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified not substituted in position 17 alfa
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009Normal 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
    • 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
    • C07J71/001Oxiranes

Landscapes

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

Abstract

Se proveen esteroides 19-nor C3,3-disustituidos de fórmula (1) y sus sales farmacéuticamente aceptables; en donde R¹, R², R³ y R⁴ tienen los valores que se definen en la presente, y A es un sistema de anillos heteroarilo que comprende 3 ó 4 nitrógenos como aquí se define. Se contempla que dichos compuestos son útiles para la prevención y tratamiento de diversos trastornos relacionados con el sistema nervioso central, por ejemplo, el tratamiento de trastornos del sueño, trastornos del estado de ánimo, trastornos del espectro de la esquizofrenia, trastornos convulsivos, trastornos de la memoria y/o la cognición, trastornos del movimiento, trastornos de la personalidad, trastornos del espectro del autismo, dolor, lesiones traumáticas cerebrales, enfermedades vasculares, trastornos del abuso de sustancias y/o síndrome de abstinencia y tinnitus. Reivindicación 1: Un compuesto, caracterizado porque es de la fórmula (1) o una sal farmacéuticamente aceptable del mismo; en donde: A se selecciona del grupo: de compuestos (A-1) - (A-5) del grupo de fórmulas (2); R¹ es C₁-C₆ haloalquilo o C₁-C₆ alquilo; R² y R³ se seleccionan de manera independiente entre H, halo, C₁-C₆ alquilo o alcoxi; R⁴ es halo, ciano, nitro, -S(O)ˣRᵃ, -NRᵇRᶜ, C₁-C₆ alquilo, C₁-C₆ alcoxi, -C(O)Rᵃ, -C(O)ORᵃ o -C(O)NRᵇRᶜ; Rᵃ es H, arilo, heteroarilo o C₁-C₆ alquilo; cada Rᵇ y Rᶜ es de manera independiente H, -S(O)ˣRᵃ, -C(O)Rᵃ, C₁-C₆ alquilo o C₁-C₆ alcoxi, o Rᵇ y Rᶜ tomados junto con el átomo al cual están unidos forman un anillo; n es un número entero entre 0 y 2; y n es un número entero entre 0 y 2; en donde cuando A es (A-1) o (A-2), entonces R¹ se selecciona entre: -CHF₂, -CH₂F, -CCl₃, -CHCl₂, -CH₂Cl, -CBr₃, -CHBr₂, -CH₂Br o C₁-C₆ alquilo; o cuando A es (A-3) o (A-5), R¹ es -CH₃, -CH₂F, -CH₂OCH₃ o -CHF₂, y n es 0, entonces por lo menos uno entre R² y R³ no es H.
ARP210100747A 2014-05-29 2021-03-25 Esteroides neuroactivos, composiciones y usos de los mismos AR121661A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2014078820 2014-05-29

Publications (1)

Publication Number Publication Date
AR121661A2 true AR121661A2 (es) 2022-06-29

Family

ID=54698130

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP150101717A AR100691A1 (es) 2014-05-29 2015-05-29 Esteroides neuroactivos, composiciones, y usos de los mismos
ARP210100747A AR121661A2 (es) 2014-05-29 2021-03-25 Esteroides neuroactivos, composiciones y usos de los mismos

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP150101717A AR100691A1 (es) 2014-05-29 2015-05-29 Esteroides neuroactivos, composiciones, y usos de los mismos

Country Status (26)

Country Link
US (5) US20180179247A1 (es)
EP (3) EP3149018B1 (es)
JP (4) JP6652934B2 (es)
KR (3) KR20240066304A (es)
CN (3) CN106661078A (es)
AR (2) AR100691A1 (es)
AU (4) AU2015266447A1 (es)
CA (1) CA2949720A1 (es)
CY (1) CY1124109T1 (es)
DK (2) DK3705488T3 (es)
ES (2) ES2805598T3 (es)
HR (2) HRP20221294T1 (es)
HU (2) HUE059829T2 (es)
IL (3) IL304033A (es)
JO (1) JO3691B1 (es)
LT (2) LT3705488T (es)
MX (4) MX2016015532A (es)
PH (1) PH12016502342A1 (es)
PL (2) PL3705488T3 (es)
PT (2) PT3705488T (es)
RS (2) RS60529B1 (es)
RU (2) RU2019126637A (es)
SG (2) SG10201803812TA (es)
SI (2) SI3149018T1 (es)
TW (1) TW201625661A (es)
WO (1) WO2015180679A1 (es)

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JP2020073577A (ja) 2020-05-14
CN114133423A (zh) 2022-03-04
CA2949720A1 (en) 2015-12-03
TW201625661A (zh) 2016-07-16
IL292461B1 (en) 2023-11-01
JP2023123878A (ja) 2023-09-05
NZ764941A (en) 2023-11-24
AR100691A1 (es) 2016-10-26
RS60529B1 (sr) 2020-08-31
MX2021005099A (es) 2021-06-15
KR102494061B1 (ko) 2023-01-31
EP3705488A1 (en) 2020-09-09
KR20170003706A (ko) 2017-01-09
EP3705488B1 (en) 2022-08-03
AU2015266447A1 (en) 2016-12-01
ES2805598T3 (es) 2021-02-12
NZ726260A (en) 2023-11-24
SG11201609813XA (en) 2016-12-29
CN106661078A (zh) 2017-05-10
KR20230021165A (ko) 2023-02-13
LT3705488T (lt) 2022-09-26
HRP20221294T1 (hr) 2023-03-03
EP3149018A4 (en) 2017-12-06
JP2021130696A (ja) 2021-09-09
KR20240066304A (ko) 2024-05-14
EP4144746A1 (en) 2023-03-08
AU2019279910B2 (en) 2021-07-22
HRP20201126T1 (hr) 2020-12-11
RU2019126637A (ru) 2019-10-03
PT3149018T (pt) 2020-07-21
DK3149018T3 (da) 2020-07-20
US20180179247A1 (en) 2018-06-28
WO2015180679A1 (en) 2015-12-03
BR112016027508A2 (pt) 2018-06-26
MX2021005106A (es) 2021-06-15
RU2699359C2 (ru) 2019-09-05
CY1124109T1 (el) 2022-03-24
HUE050028T2 (hu) 2021-12-28
IL304033A (en) 2023-08-01
ES2927007T3 (es) 2022-10-31
CN114369135A (zh) 2022-04-19
RU2016151727A (ru) 2018-07-02
US20210061850A1 (en) 2021-03-04
JP6652934B2 (ja) 2020-02-26
SG10201803812TA (en) 2018-06-28
PL3705488T3 (pl) 2022-12-05
AU2023285755A1 (en) 2024-01-18
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EP3149018B1 (en) 2020-04-29
IL248948B (en) 2022-09-01
KR102664412B1 (ko) 2024-05-21
RS63554B1 (sr) 2022-09-30
SI3705488T1 (sl) 2022-10-28
US20200165291A1 (en) 2020-05-28
IL292461A (en) 2022-06-01
AU2019279910A1 (en) 2020-01-16
US20210061849A1 (en) 2021-03-04
MX2016015532A (es) 2017-02-27
PL3149018T3 (pl) 2021-01-25
IL292461B2 (en) 2024-03-01
TW202231652A (zh) 2022-08-16
HUE059829T2 (hu) 2022-12-28
US20240076310A1 (en) 2024-03-07
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AU2021204410A1 (en) 2021-07-22
LT3149018T (lt) 2020-08-10
RU2016151727A3 (es) 2018-12-03
JP6892936B2 (ja) 2021-06-23
PT3705488T (pt) 2022-09-30
DK3705488T3 (da) 2022-10-03
IL248948A0 (en) 2017-01-31
JO3691B1 (ar) 2020-08-27
JP7386204B2 (ja) 2023-11-24
AU2021204410B2 (en) 2023-09-21
PH12016502342A1 (en) 2017-02-13
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EP3149018A1 (en) 2017-04-05
JP2017516793A (ja) 2017-06-22

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