AP653A - Androstane and pregnane series for allosteric modulations of gaba receptor. - Google Patents

Androstane and pregnane series for allosteric modulations of gaba receptor. Download PDF

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Publication number
AP653A
AP653A APAP/P/1997/000998A AP9700998A AP653A AP 653 A AP653 A AP 653A AP 9700998 A AP9700998 A AP 9700998A AP 653 A AP653 A AP 653A
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AP
ARIPO
Prior art keywords
pregnan
hydroxy
dihydroxy
trifluoromethyl
compounds
Prior art date
Application number
APAP/P/1997/000998A
Other languages
English (en)
Other versions
AP9700998A0 (en
Inventor
Nancy C Lan
Kelvin W Gee
Michael B Bolger
Hassan F Tahir
Robetrt Purdy
Ravindra Upasani
Original Assignee
Cocensys 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 Cocensys Inc filed Critical Cocensys Inc
Publication of AP9700998A0 publication Critical patent/AP9700998A0/xx
Application granted granted Critical
Publication of AP653A publication Critical patent/AP653A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • 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
    • A61P25/08Antiepileptics; Anticonvulsants
    • A61P25/12Antiepileptics; Anticonvulsants for grand-mal
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J5/00Normal 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
    • C07J5/0007Normal 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
    • C07J5/0015Normal 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
    • 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
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
APAP/P/1997/000998A 1994-11-23 1995-11-22 Androstane and pregnane series for allosteric modulations of gaba receptor. AP653A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34692694A 1994-11-23 1994-11-23
PCT/US1995/015210 WO1996016076A1 (en) 1994-11-23 1995-11-22 Androstane and pregnane series for allosteric modulation of gaba receptor

Publications (2)

Publication Number Publication Date
AP9700998A0 AP9700998A0 (en) 1997-07-31
AP653A true AP653A (en) 1998-07-21

Family

ID=23361616

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1997/000998A AP653A (en) 1994-11-23 1995-11-22 Androstane and pregnane series for allosteric modulations of gaba receptor.

Country Status (27)

Country Link
EP (1) EP0808325B1 (da)
JP (1) JPH10509458A (da)
KR (1) KR100394548B1 (da)
CN (1) CN1171114A (da)
AP (1) AP653A (da)
AT (1) ATE198753T1 (da)
AU (1) AU707486B2 (da)
BR (1) BR9509764A (da)
CA (1) CA2205919A1 (da)
CZ (1) CZ292881B6 (da)
DE (1) DE69519945T2 (da)
DK (1) DK0808325T3 (da)
ES (1) ES2155543T3 (da)
FI (1) FI972202A (da)
GE (1) GEP20002033B (da)
GR (1) GR3035562T3 (da)
HU (1) HUT77087A (da)
IL (1) IL116108A (da)
IS (1) IS4488A (da)
MX (1) MX9703826A (da)
NO (1) NO308950B1 (da)
NZ (1) NZ298567A (da)
PL (1) PL182898B1 (da)
PT (1) PT808325E (da)
RU (1) RU2176248C2 (da)
UA (1) UA48154C2 (da)
WO (1) WO1996016076A1 (da)

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US6780853B1 (en) 1995-06-06 2004-08-24 Euro-Celtique S.A. Neuroactive steroids of the androstane and pregnane series
US20010051599A1 (en) 1997-05-02 2001-12-13 Michael Z. Kagan Pregnan-3-ol-20-ones
CN1270718C (zh) 1998-03-11 2006-08-23 托布乔恩·贝克斯托罗姆 表别孕烷醇酮在制备治疗甾族化合物诱导的疾病的药物中的应用
US8771740B2 (en) 1999-12-20 2014-07-08 Nicholas J. Kerkhof Process for producing nanoparticles by spray drying
ES2240222T3 (es) 1999-12-20 2005-10-16 Nicholas J. Kerkhof Procedimiento para producir particulas nanometricas mediante secado por pulverizacion en lecho fluidizado.
AR031473A1 (es) * 2000-11-20 2003-09-24 Lundbeck & Co As H Intensificadores de gaba en el tratamiento de enfermedades relacionadas con una reducida actividad neuroesteroide
WO2006012563A2 (en) * 2004-07-23 2006-02-02 The Regents Of The University Of California Method for the treatment and diagnosis of certain psychiatric disorders related to the menstrual cycle
CA2620333A1 (en) 2005-08-26 2007-03-01 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
CA2625210A1 (en) 2005-10-31 2007-05-10 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
PL2097437T3 (pl) 2006-11-21 2015-12-31 Umecrine Cognition Ab Zastosowanie steroidów pregnanowych i androstanowych do wytwarzania kompozycji farmaceutycznej do leczenia zaburzeń OUN
CN101585862B (zh) * 2008-05-20 2014-12-17 梅克芳股份公司 甾族化合物
CN103819525A (zh) * 2008-05-20 2014-05-28 梅克芳股份公司 甾族化合物
CN103880909A (zh) * 2008-05-20 2014-06-25 梅克芳股份公司 甾族化合物
US20100216805A1 (en) 2009-02-25 2010-08-26 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
AU2010282570B2 (en) * 2009-08-13 2014-04-24 Marinus Pharmaceuticals, Inc. Method for making 3alpha-hydroxy, 3beta- methyl-5alpha-pregnan-20-one (ganaxolone)
CN102753181B (zh) 2010-01-14 2014-09-17 优麦克里尼穆德公司 具有改进的储存特性和溶解度特性的包含3-β-羟基-5-α-孕烷-20-酮的药物组合物
WO2011120044A1 (en) * 2010-03-26 2011-09-29 Duke University Conjugated neuroactive steroid compositions and methods of use
WO2013019711A2 (en) * 2011-07-29 2013-02-07 The Regents Of The University Of California NOVEL 17β-HETEROARYL-SUBSTITUTED STEROIDS AS MODULATORS OF GABAA RECEPTORS
CN107936076B (zh) * 2011-09-08 2021-10-15 萨奇治疗股份有限公司 神经活性类固醇、组合物、及其用途
US10478505B2 (en) 2011-09-23 2019-11-19 The Regents Of The University Of California Edible oils to enhance delivery of orally administered steroids
CA3152410A1 (en) * 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3-disubstituted 19-nor pregnane compounds, compositions, and uses thereof for the treatment of cns related disorders
LT2806877T (lt) 2012-01-23 2019-12-10 Sage Therapeutics Inc Neuroaktyvios steroidų kompozicijos, apimančios alopregnanolono ir sulfobutilo eterio beta-ciklodekstrino kompleksą
IL275725B (en) * 2012-08-21 2022-08-01 Sage Therapeutics Inc Treatment methods for epilepsy and status epilepticus
EP2925327B1 (en) 2012-11-30 2024-01-10 The Regents of The University of California Allopregnanolone for treating, reducing or mitigating symptoms of post-partum depression
WO2014160480A1 (en) 2013-03-13 2014-10-02 Sage Therapeutics, Inc. Neuroactive steroids and methods of use thereof
CN113527400A (zh) 2013-04-17 2021-10-22 萨奇治疗股份有限公司 19-去甲c3,3-二取代的c21-n-吡唑基类固醇及其使用方法
US9725481B2 (en) 2013-04-17 2017-08-08 Sage Therapeutics, Inc. 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
CN112110976B (zh) 2013-04-17 2023-08-29 萨奇治疗股份有限公司 刺激神经活性的19-去甲类固醇及其使用方法
LT3021852T (lt) * 2013-07-19 2021-04-12 Sage Therapeutics, Inc. Neuroaktyvūs steroidai, jų kompozicijos ir panaudojimas
DK3488852T3 (da) 2013-08-23 2021-02-01 Sage Therapeutics Inc Neuroaktive steroider, sammensætninger og anvendelser deraf
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TW202235090A (zh) 2014-10-16 2022-09-16 美商賽吉醫療公司 用於治療中樞神經系統(cns)病症之組合物及方法
ES2808855T3 (es) * 2014-10-16 2021-03-02 Sage Therapeutics Inc Composiciones y métodos para tratar trastornos del SNC
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HUE054092T2 (hu) 2015-01-26 2021-08-30 Sage Therapeutics Inc Központi idegrendszeri zavarok kezelésére szolgáló kompozíciók és eljárások
ES2935476T3 (es) 2015-02-20 2023-03-07 Sage Therapeutics Inc Esteroides neuroactivos, composiciones y usos de los mismos
US11117924B2 (en) 2015-07-06 2021-09-14 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
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CN111410673A (zh) * 2019-01-08 2020-07-14 成都康弘药业集团股份有限公司 甾体类化合物、用途及其制备方法
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Citations (2)

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Publication number Priority date Publication date Assignee Title
US5120723A (en) * 1987-08-25 1992-06-09 University Of Southern California Method, compositions, and compounds for modulating brain excitability
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

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US3953429A (en) * 1970-12-17 1976-04-27 Glaxo Laboratories Limited Anaesthetic steroids of the androstance and pregnane series
WO1993005786A1 (en) * 1991-09-13 1993-04-01 Cocensys, Inc. Novel gabaa receptor with steroid binding sites
US5371077A (en) * 1992-08-03 1994-12-06 William Marsh Rice University Side chain derivatized 15-oxygenated sterols, methods of using them and a process for preparing them
AU698834B2 (en) * 1993-05-24 1998-11-12 Purdue Pharma Ltd. Methods and compositions for inducing sleep

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Publication number Priority date Publication date Assignee Title
US5120723A (en) * 1987-08-25 1992-06-09 University Of Southern California Method, compositions, and compounds for modulating brain excitability
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

Also Published As

Publication number Publication date
EP0808325A4 (da) 1997-12-17
RU2176248C2 (ru) 2001-11-27
CZ292881B6 (cs) 2003-12-17
ES2155543T3 (es) 2001-05-16
WO1996016076A1 (en) 1996-05-30
IL116108A0 (en) 1996-01-31
NZ298567A (en) 2000-01-28
PL320416A1 (en) 1997-09-29
PL182898B1 (pl) 2002-03-29
UA48154C2 (uk) 2002-08-15
PT808325E (pt) 2001-06-29
KR100394548B1 (ko) 2004-02-05
JPH10509458A (ja) 1998-09-14
IL116108A (en) 2002-08-14
FI972202A0 (fi) 1997-05-23
EP0808325B1 (en) 2001-01-17
NO972320D0 (no) 1997-05-21
DE69519945T2 (de) 2001-06-07
GEP20002033B (en) 2000-04-10
CN1171114A (zh) 1998-01-21
MX9703826A (es) 1998-02-28
CZ155397A3 (cs) 1998-03-18
BR9509764A (pt) 1998-07-07
NO972320L (no) 1997-07-23
DE69519945D1 (de) 2001-02-22
IS4488A (is) 1997-05-23
CA2205919A1 (en) 1996-05-30
DK0808325T3 (da) 2001-01-29
EP0808325A1 (en) 1997-11-26
AP9700998A0 (en) 1997-07-31
NO308950B1 (no) 2000-11-20
FI972202A (fi) 1997-07-17
AU4408596A (en) 1996-06-17
AU707486B2 (en) 1999-07-08
HUT77087A (hu) 1998-03-02
ATE198753T1 (de) 2001-02-15
GR3035562T3 (en) 2001-06-29

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