FI20051271A - Compounds and compositions for allosteric modulation of the GABA receptor - Google Patents
Compounds and compositions for allosteric modulation of the GABA receptor Download PDFInfo
- Publication number
- FI20051271A FI20051271A FI20051271A FI20051271A FI20051271A FI 20051271 A FI20051271 A FI 20051271A FI 20051271 A FI20051271 A FI 20051271A FI 20051271 A FI20051271 A FI 20051271A FI 20051271 A FI20051271 A FI 20051271A
- Authority
- FI
- Finland
- Prior art keywords
- compositions
- compounds
- gaba receptor
- allosteric modulation
- receptor
- Prior art date
Links
Classifications
-
- 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
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- 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
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
-
- 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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- 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
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J33/002—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/005—Normal 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- 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
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal 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
- C07J7/0015—Normal 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
- C07J7/002—Normal 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
-
- 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
- C07J7/0085—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 an halogen atom
Abstract
Methods, compositions and compounds for modulating the GABAA receptor-chloride ionophore complex to alleviate stress, anxiety, seizures, mood disorders, PMS and PND and to induce anesthesia.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US19691994A | 1994-02-14 | 1994-02-14 | |
US19691994 | 1994-02-14 | ||
US34692794A | 1994-11-23 | 1994-11-23 | |
US34692794 | 1994-11-23 | ||
PCT/US1995/001712 WO1995021617A1 (en) | 1994-02-14 | 1995-02-14 | Androstanes and pregnanes for allosteric modulation of gaba receptor |
US9501712 | 1995-02-14 |
Publications (2)
Publication Number | Publication Date |
---|---|
FI20051271A true FI20051271A (en) | 2005-12-09 |
FI118687B FI118687B (en) | 2008-02-15 |
Family
ID=26892391
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI963174A FI118008B (en) | 1994-02-14 | 1996-08-13 | Androstanes and pregnanes for allosteric modulation of the GABA receptor |
FI20051271A FI118687B (en) | 1994-02-14 | 2005-12-09 | Compounds and compositions for allosteric modulation of the GABA receptor |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI963174A FI118008B (en) | 1994-02-14 | 1996-08-13 | Androstanes and pregnanes for allosteric modulation of the GABA receptor |
Country Status (18)
Country | Link |
---|---|
EP (2) | EP1038880B1 (en) |
JP (1) | JP4066272B2 (en) |
KR (1) | KR100338287B1 (en) |
AT (2) | ATE375993T1 (en) |
AU (1) | AU691905B2 (en) |
BR (1) | BR9506779A (en) |
CA (1) | CA2183231A1 (en) |
DE (2) | DE69518509T2 (en) |
DK (2) | DK0752860T3 (en) |
ES (2) | ES2296594T3 (en) |
FI (2) | FI118008B (en) |
GR (1) | GR3034810T3 (en) |
HK (1) | HK1014665A1 (en) |
IL (1) | IL112638A (en) |
NO (1) | NO308307B1 (en) |
NZ (1) | NZ282939A (en) |
PT (2) | PT752860E (en) |
WO (1) | WO1995021617A1 (en) |
Families Citing this family (70)
Publication number | Priority date | Publication date | Assignee | Title |
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US6780853B1 (en) | 1995-06-06 | 2004-08-24 | Euro-Celtique S.A. | Neuroactive steroids of the androstane and pregnane series |
AU725214B2 (en) * | 1995-06-06 | 2000-10-05 | 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 |
EP1449846A1 (en) * | 1999-04-29 | 2004-08-25 | Euro-Celtique S.A. | 3-alpha Hydroxy-3-beta methoxymethyl-21-heterocycle substituted steriods with anaesthetic activity |
MXPA01010915A (en) * | 1999-04-29 | 2002-11-07 | Purdue Pharma Ltd | 3alpha-HYDROXY-3beta METHOXYMETHYL-21-HETEROCYCLE SUBSTITUTED STEROIDS WITH ANESTHETIC ACTIVITY. |
JP2001039954A (en) * | 1999-05-24 | 2001-02-13 | Tomono Agrica Co Ltd | Heterocyclic derivative |
CA2669753C (en) | 1999-09-30 | 2012-06-26 | Hollis-Eden Pharmaceuticals, Inc. | Therapeutic treatment of androgen receptor driven conditions |
US8771740B2 (en) | 1999-12-20 | 2014-07-08 | Nicholas J. Kerkhof | Process for producing nanoparticles by spray drying |
AU2583401A (en) | 1999-12-20 | 2001-07-03 | Cocensys, Inc. | Process for producing nanometer particles by fluid bed spray-drying |
US8569275B2 (en) | 2002-08-28 | 2013-10-29 | Harbor Therapeutics, Inc. | Steroids having 7-oxgen and 17-heteroaryl substitution |
AU2006256851C1 (en) * | 2005-06-09 | 2010-07-15 | Euro-Celtique S.A. | Pharmaceutical compositions of a neuroactive steroid and uses thereof |
CA2620333A1 (en) | 2005-08-26 | 2007-03-01 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation |
EP2258359A3 (en) | 2005-08-26 | 2011-04-06 | Braincells, Inc. | Neurogenesis by muscarinic receptor modulation with sabcomelin |
CA2625153A1 (en) | 2005-10-21 | 2007-04-26 | Braincells, Inc. | Modulation of neurogenesis by pde inhibition |
EP1942879A1 (en) | 2005-10-31 | 2008-07-16 | Braincells, Inc. | Gaba receptor mediated modulation of neurogenesis |
US20100216734A1 (en) | 2006-03-08 | 2010-08-26 | Braincells, Inc. | Modulation of neurogenesis by nootropic agents |
JP2009536667A (en) | 2006-05-09 | 2009-10-15 | ブレインセルス,インコーポレイティド | 5HT receptor-mediated neurogenesis |
JP2009536669A (en) | 2006-05-09 | 2009-10-15 | ブレインセルス,インコーポレイティド | Neurogenesis by angiotensin regulation |
AU2007292848A1 (en) | 2006-09-08 | 2008-03-13 | Braincells, Inc. | Combinations containing a 4-acylaminopyridine derivative |
AU2007299010B2 (en) * | 2006-09-19 | 2013-01-31 | Solvay Pharmaceuticals Gmbh | Estratriene derivatives and their uses as 17beta-hydroxysteroid dehydrogenase inhibitors |
US20100184806A1 (en) | 2006-09-19 | 2010-07-22 | Braincells, Inc. | Modulation of neurogenesis by ppar agents |
EP2792681B1 (en) | 2006-11-21 | 2016-10-19 | Umecrine AB | The use of pregnane and androstane steroids for the manufacture of a pharmaceutical composition for the treatment of cns disorders |
US8575375B2 (en) | 2007-06-15 | 2013-11-05 | Research Triangle Institute | Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties |
WO2010099217A1 (en) | 2009-02-25 | 2010-09-02 | Braincells, Inc. | Modulation of neurogenesis using d-cycloserine combinations |
CZ302050B6 (en) * | 2009-08-04 | 2010-09-15 | Ústav organické chemie a biochemie, Akademie ved CR, v.v.i. | 3alpha-Hydroxy-21xi, 22-oxide-21-homo-5alpha-pregnan-20-one, process if its preparation and its use |
RU2665571C2 (en) | 2011-09-08 | 2018-08-31 | Сейдж Терапьютикс, Инк. | Neuroactive steroids, compositions and uses thereof |
US10478505B2 (en) | 2011-09-23 | 2019-11-19 | The Regents Of The University Of California | Edible oils to enhance delivery of orally administered steroids |
CN113234114A (en) * | 2011-10-14 | 2021-08-10 | 萨奇治疗股份有限公司 | 3, 3-disubstituted 19-norpregnane compounds, compositions, and uses thereof |
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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 |
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WO2015027227A1 (en) * | 2013-08-23 | 2015-02-26 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
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WO2016036724A1 (en) | 2014-09-02 | 2016-03-10 | The Texas A&M University System | Method of treating organophosphate intoxication |
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Family Cites Families (7)
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US3274179A (en) * | 1964-03-19 | 1966-09-20 | Merck & Co Inc | 3-haloethynyl-3-hydroxy derivatives of the androstane-17-one and pregnane-20-one series |
US3953429A (en) * | 1970-12-17 | 1976-04-27 | Glaxo Laboratories Limited | Anaesthetic steroids of the androstance and pregnane series |
GB1430942A (en) * | 1972-05-05 | 1976-04-07 | Glaxo Lab Ltd | 21-substituted 3alpha-hydroxy pregnanes |
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 |
US5120723A (en) * | 1987-08-25 | 1992-06-09 | University Of Southern California | Method, compositions, and compounds for modulating brain excitability |
JPH06510999A (en) * | 1991-09-13 | 1994-12-08 | コセンシス・インコーポレイテッド | Novel GABA↓a receptor with steroid binding site |
EP0701444B1 (en) * | 1993-05-24 | 2010-04-07 | Purdue Pharma Ltd. | Methods and compositions for inducing sleep |
-
1995
- 1995-02-14 DK DK95913478T patent/DK0752860T3/en active
- 1995-02-14 EP EP00200119A patent/EP1038880B1/en not_active Expired - Lifetime
- 1995-02-14 DE DE69518509T patent/DE69518509T2/en not_active Expired - Lifetime
- 1995-02-14 CA CA002183231A patent/CA2183231A1/en not_active Abandoned
- 1995-02-14 DE DE69535623T patent/DE69535623T2/en not_active Expired - Lifetime
- 1995-02-14 AT AT00200119T patent/ATE375993T1/en active
- 1995-02-14 IL IL11263895A patent/IL112638A/en not_active IP Right Cessation
- 1995-02-14 KR KR1019960704396A patent/KR100338287B1/en not_active IP Right Cessation
- 1995-02-14 JP JP52135695A patent/JP4066272B2/en not_active Expired - Fee Related
- 1995-02-14 WO PCT/US1995/001712 patent/WO1995021617A1/en active IP Right Grant
- 1995-02-14 DK DK00200119T patent/DK1038880T3/en active
- 1995-02-14 ES ES00200119T patent/ES2296594T3/en not_active Expired - Lifetime
- 1995-02-14 PT PT95913478T patent/PT752860E/en unknown
- 1995-02-14 NZ NZ282939A patent/NZ282939A/en not_active IP Right Cessation
- 1995-02-14 BR BR9506779A patent/BR9506779A/en not_active IP Right Cessation
- 1995-02-14 EP EP95913478A patent/EP0752860B1/en not_active Expired - Lifetime
- 1995-02-14 AT AT95913478T patent/ATE195654T1/en active
- 1995-02-14 ES ES95913478T patent/ES2151593T3/en not_active Expired - Lifetime
- 1995-02-14 AU AU20901/95A patent/AU691905B2/en not_active Ceased
- 1995-02-14 PT PT00200119T patent/PT1038880E/en unknown
-
1996
- 1996-08-12 NO NO963355A patent/NO308307B1/en not_active IP Right Cessation
- 1996-08-13 FI FI963174A patent/FI118008B/en not_active IP Right Cessation
-
1998
- 1998-12-28 HK HK98116032A patent/HK1014665A1/en not_active IP Right Cessation
-
2000
- 2000-11-10 GR GR20000402497T patent/GR3034810T3/en unknown
-
2005
- 2005-12-09 FI FI20051271A patent/FI118687B/en not_active IP Right Cessation
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