DE69927960T2 - Epiallopregnanolon zur behandlung von krankheiten des cns - Google Patents
Epiallopregnanolon zur behandlung von krankheiten des cns Download PDFInfo
- Publication number
- DE69927960T2 DE69927960T2 DE69927960T DE69927960T DE69927960T2 DE 69927960 T2 DE69927960 T2 DE 69927960T2 DE 69927960 T DE69927960 T DE 69927960T DE 69927960 T DE69927960 T DE 69927960T DE 69927960 T2 DE69927960 T2 DE 69927960T2
- Authority
- DE
- Germany
- Prior art keywords
- pregnan
- hydroxy
- 5alpha
- 3beta
- treatment
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
Links
- AURFZBICLPNKBZ-FZCSVUEKSA-N 3beta-hydroxy-5alpha-pregnan-20-one Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-FZCSVUEKSA-N 0.000 title claims abstract description 46
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 7
- AURFZBICLPNKBZ-UHFFFAOYSA-N Pregnanolone Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 AURFZBICLPNKBZ-UHFFFAOYSA-N 0.000 title abstract description 30
- 201000010099 disease Diseases 0.000 title description 4
- 150000003431 steroids Chemical class 0.000 claims abstract description 29
- 208000019022 Mood disease Diseases 0.000 claims abstract description 8
- 238000004519 manufacturing process Methods 0.000 claims abstract description 7
- 230000000694 effects Effects 0.000 claims description 34
- 230000027758 ovulation cycle Effects 0.000 claims description 20
- 210000003169 central nervous system Anatomy 0.000 claims description 12
- 230000002265 prevention Effects 0.000 claims description 12
- 206010016256 fatigue Diseases 0.000 claims description 11
- 206010036618 Premenstrual syndrome Diseases 0.000 claims description 9
- 206010015037 epilepsy Diseases 0.000 claims description 9
- 206010002091 Anaesthesia Diseases 0.000 claims description 7
- 230000037005 anaesthesia Effects 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 7
- 229940127234 oral contraceptive Drugs 0.000 claims description 6
- 239000003539 oral contraceptive agent Substances 0.000 claims description 6
- 206010027951 Mood swings Diseases 0.000 claims description 5
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- 208000019695 Migraine disease Diseases 0.000 claims description 4
- 206010027599 migraine Diseases 0.000 claims description 4
- 208000019116 sleep disease Diseases 0.000 claims description 4
- 238000002560 therapeutic procedure Methods 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 3
- 230000003867 tiredness Effects 0.000 claims description 3
- 208000016255 tiredness Diseases 0.000 claims description 3
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 claims description 2
- 230000003637 steroidlike Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 7
- 208000015114 central nervous system disease Diseases 0.000 abstract description 6
- 208000024891 symptom Diseases 0.000 abstract 1
- 230000027455 binding Effects 0.000 description 15
- 230000008859 change Effects 0.000 description 13
- 102000004300 GABA-A Receptors Human genes 0.000 description 11
- 108090000839 GABA-A Receptors Proteins 0.000 description 11
- 238000001727 in vivo Methods 0.000 description 10
- AURFZBICLPNKBZ-YZRLXODZSA-N 3alpha-hydroxy-5beta-pregnan-20-one Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-YZRLXODZSA-N 0.000 description 9
- 229960002200 flunitrazepam Drugs 0.000 description 9
- 238000001802 infusion Methods 0.000 description 9
- 241000700159 Rattus Species 0.000 description 8
- PPTYJKAXVCCBDU-UHFFFAOYSA-N Rohypnol Chemical compound N=1CC(=O)N(C)C2=CC=C([N+]([O-])=O)C=C2C=1C1=CC=CC=C1F PPTYJKAXVCCBDU-UHFFFAOYSA-N 0.000 description 8
- 230000003444 anaesthetic effect Effects 0.000 description 8
- 238000001990 intravenous administration Methods 0.000 description 8
- 239000000126 substance Substances 0.000 description 7
- RJKFOVLPORLFTN-LEKSSAKUSA-N Progesterone Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 RJKFOVLPORLFTN-LEKSSAKUSA-N 0.000 description 6
- 230000029849 luteinization Effects 0.000 description 6
- AURFZBICLPNKBZ-SYBPFIFISA-N brexanolone Chemical compound C([C@@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-SYBPFIFISA-N 0.000 description 5
- 229940079593 drug Drugs 0.000 description 5
- 229950007402 eltanolone Drugs 0.000 description 5
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 5
- 230000035945 sensitivity Effects 0.000 description 5
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 4
- 229920000858 Cyclodextrin Polymers 0.000 description 4
- 239000005557 antagonist Substances 0.000 description 4
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 4
- AURFZBICLPNKBZ-GRWISUQFSA-N 3beta-hydroxy-5beta-pregnan-20-one Chemical compound C([C@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-GRWISUQFSA-N 0.000 description 3
- VTBHBNXGFPTBJL-UHFFFAOYSA-N 4-tert-butyl-1-sulfanylidene-2,6,7-trioxa-1$l^{5}-phosphabicyclo[2.2.2]octane Chemical compound C1OP2(=S)OCC1(C(C)(C)C)CO2 VTBHBNXGFPTBJL-UHFFFAOYSA-N 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 229940035674 anesthetics Drugs 0.000 description 3
- 229940049706 benzodiazepine Drugs 0.000 description 3
- 230000000903 blocking effect Effects 0.000 description 3
- 210000004556 brain Anatomy 0.000 description 3
- 230000001419 dependent effect Effects 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 230000004907 flux Effects 0.000 description 3
- 230000006870 function Effects 0.000 description 3
- 239000003193 general anesthetic agent Substances 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 230000001537 neural effect Effects 0.000 description 3
- 239000000186 progesterone Substances 0.000 description 3
- 229960003387 progesterone Drugs 0.000 description 3
- CYKYBWRSLLXBOW-GDYGHMJCSA-N 5-alpha-THDOC Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CC[C@H]21 CYKYBWRSLLXBOW-GDYGHMJCSA-N 0.000 description 2
- 206010001497 Agitation Diseases 0.000 description 2
- 102000005915 GABA Receptors Human genes 0.000 description 2
- 108010005551 GABA Receptors Proteins 0.000 description 2
- 206010022998 Irritability Diseases 0.000 description 2
- 230000004075 alteration Effects 0.000 description 2
- 150000001557 benzodiazepines Chemical class 0.000 description 2
- 150000001875 compounds Chemical class 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- 230000002611 ovarian Effects 0.000 description 2
- 150000003146 progesterones Chemical class 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 description 1
- RSRDWHPVTMQUGZ-QYYVTAPASA-N 1-[(5r,8r,9s,10s,13s,14s,17s)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]ethanone Chemical compound C([C@@H]1CC2)CCC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 RSRDWHPVTMQUGZ-QYYVTAPASA-N 0.000 description 1
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
- 239000003148 4 aminobutyric acid receptor blocking agent Substances 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 238000012404 In vitro experiment Methods 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 208000026139 Memory disease Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- LHNKBXRFNPMIBR-UHFFFAOYSA-N Picrotoxin Natural products CC(C)(O)C1(O)C2OC(=O)C1C3(O)C4OC4C5C(=O)OC2C35C LHNKBXRFNPMIBR-UHFFFAOYSA-N 0.000 description 1
- 206010035148 Plague Diseases 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- 241000607479 Yersinia pestis Species 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 230000001270 agonistic effect Effects 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 230000003042 antagnostic effect Effects 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 230000002460 anti-migrenic effect Effects 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 239000002246 antineoplastic agent Substances 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 229940125717 barbiturate Drugs 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 239000003874 central nervous system depressant Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000008094 contradictory effect Effects 0.000 description 1
- 230000002920 convulsive effect Effects 0.000 description 1
- 210000004246 corpus luteum Anatomy 0.000 description 1
- 238000013016 damping Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 230000003828 downregulation Effects 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 238000009164 estrogen replacement therapy Methods 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 206010027175 memory impairment Diseases 0.000 description 1
- 230000002175 menstrual effect Effects 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 230000001722 neurochemical effect Effects 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 230000008587 neuronal excitability Effects 0.000 description 1
- 230000011599 ovarian follicle development Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 230000002974 pharmacogenomic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- VJKUPQSHOVKBCO-AHMKVGDJSA-N picrotoxin Chemical compound O=C([C@@]12O[C@@H]1C[C@]1(O)[C@@]32C)O[C@@H]3[C@H]2[C@@H](C(=C)C)[C@@H]1C(=O)O2.O=C([C@@]12O[C@@H]1C[C@]1(O)[C@@]32C)O[C@@H]3[C@H]2[C@@H](C(C)(O)C)[C@@H]1C(=O)O2 VJKUPQSHOVKBCO-AHMKVGDJSA-N 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 229960000249 pregnenolone Drugs 0.000 description 1
- 230000000757 progestagenic effect Effects 0.000 description 1
- 102000003998 progesterone receptors Human genes 0.000 description 1
- 108090000468 progesterone receptors Proteins 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000028527 righting reflex Effects 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 238000007391 self-medication Methods 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 208000022925 sleep disturbance Diseases 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 238000012453 sprague-dawley rat model Methods 0.000 description 1
- 238000010025 steaming Methods 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 238000005728 strengthening Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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
- A61K31/57—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/28—Drugs 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Anesthesiology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US3786998A | 1998-03-11 | 1998-03-11 | |
| US37869 | 1998-03-11 | ||
| PCT/EP1999/001496 WO1999045931A1 (en) | 1998-03-11 | 1999-03-10 | Epiallopregnanolone in the treatment of cns disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE69927960D1 DE69927960D1 (de) | 2005-12-01 |
| DE69927960T2 true DE69927960T2 (de) | 2006-07-20 |
Family
ID=21896803
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE69927960T Expired - Lifetime DE69927960T2 (de) | 1998-03-11 | 1999-03-10 | Epiallopregnanolon zur behandlung von krankheiten des cns |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US6455516B1 (https=) |
| EP (1) | EP1063999B1 (https=) |
| JP (1) | JP3877961B2 (https=) |
| CN (1) | CN1270718C (https=) |
| AT (1) | ATE307592T1 (https=) |
| AU (1) | AU756001B2 (https=) |
| CA (1) | CA2321728C (https=) |
| DE (1) | DE69927960T2 (https=) |
| WO (1) | WO1999045931A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20020072509A1 (en) * | 2000-10-11 | 2002-06-13 | Stein Donald Gerald | Methods for the treatment of a traumatic central nervous system injury |
| SE0104423D0 (sv) * | 2001-12-27 | 2001-12-27 | Umecrine Ab | Pregnane steroids and their use in the treatment of CNS disorders |
| CN101076340B (zh) * | 2004-11-18 | 2011-01-12 | 梅克芳股份公司 | Gaba-类固醇拮抗剂及其治疗cns障碍的用途 |
| RU2413516C2 (ru) * | 2004-11-18 | 2011-03-10 | Умекрин Аб | Гамк-стероидные антагонисты и их применение в лечении нарушений цнс |
| DE102006003508A1 (de) * | 2006-01-24 | 2007-07-26 | Grünenthal GmbH | Arzneimittel umfassend eine Hormonkombination |
| DE102006003509A1 (de) * | 2006-01-24 | 2007-07-26 | Grünenthal GmbH | Kontrazeptivum |
| US20070203216A1 (en) * | 2006-02-14 | 2007-08-30 | Bjarke Ebert | Method of treating inflammatory diseases |
| DK2792681T3 (en) | 2006-11-21 | 2017-01-23 | Umecrine Ab | Use of Pregnancy and Androstan Steroids in the Preparation of a Pharmaceutical Composition for the Treatment of CNS Disorders. |
| US20100204192A1 (en) | 2007-06-11 | 2010-08-12 | University Of Sourthern California | Agents, compositions and methods for enhancing neurological function |
| EP2167098B1 (en) * | 2007-06-11 | 2018-09-05 | University Of Southern California | Allopregnanolone in a method for enhancing neurological function (alzheimer disease) |
| US20090048288A1 (en) * | 2007-08-13 | 2009-02-19 | H. Lundbeck A/S | Method of treating stress-mediated depression |
| RU2012133627A (ru) * | 2010-01-14 | 2014-04-20 | Умекрине Муд Аб | Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, с улучшенными свойствами хранения и растворимости |
| PL2709631T3 (pl) | 2011-05-20 | 2017-07-31 | Inserm - Institut National De La Santé Et De La Recherche Médicale | Antagoniści receptora cb1 |
| WO2013043985A1 (en) | 2011-09-23 | 2013-03-28 | The Regents Of The University Of California | Edible oils to enhance delivery of orally administered steroids |
| EP2806877B2 (en) * | 2012-01-23 | 2025-01-29 | Sage Therapeutics, Inc. | Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin |
| US20140050789A1 (en) | 2012-08-13 | 2014-02-20 | The Regents Of The University Of California | Mitigation of epileptic seizures by combination therapy using benzodiazepines and neurosteroids |
| CA2882708A1 (en) | 2012-08-21 | 2014-02-27 | Sage Therapeutics, Inc. | Methods of treating epilepsy or status epilepticus |
| ES2621528T3 (es) | 2012-11-28 | 2017-07-04 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Derivados de 3-(4-sustituido)-bencil éter de pregnenolona |
| AU2013352141B2 (en) * | 2012-11-30 | 2018-04-05 | The Regents Of The University Of California | Anticonvulsant activity of steroids |
| RU2684616C2 (ru) | 2014-01-29 | 2019-04-10 | Умекрин Когнишн Аб | Стероидное соединение для применения в лечении печеночной энцефалопатии |
| JOP20200195A1 (ar) | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| WO2016082789A1 (en) * | 2014-11-27 | 2016-06-02 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| AR103384A1 (es) | 2015-01-12 | 2017-05-03 | Umecrine Cognition Ab | 3a-ETINILO, 3b-HIDROXI, 5a-PREGNAN-20-OXIMA COMO MODULADOR DE GABA |
| KR20240157128A (ko) | 2016-03-08 | 2024-10-31 | 세이지 테라퓨틱스, 인크. | 신경활성 스테로이드, 조성물, 및 그의 용도 |
| US10278977B2 (en) | 2016-06-06 | 2019-05-07 | Umecrine Cognition Ab | Methods for treating hypersomnolence |
| RS67063B1 (sr) * | 2017-01-09 | 2025-08-29 | Relmada Therapeutics Inc | Injektabilne suspenzije |
| WO2018147792A1 (en) * | 2017-02-10 | 2018-08-16 | Asarina Pharma Ab | 3-beta-hydroxy-5-alpha-pregnan-20-one for use in medical treatment |
| WO2018147791A1 (en) * | 2017-02-10 | 2018-08-16 | Asarina Pharma Ab | 3-beta-hydroxy-5-alpha-pregnan-20-one for use in treatment of essential tremor |
| US20210228596A1 (en) * | 2017-10-12 | 2021-07-29 | Sage Therapeutics, Inc. | Method of treating cns disorders with neurosteroids and gabaergic compounds |
| JP2021519799A (ja) | 2018-04-05 | 2021-08-12 | アサリナ ファーマ エーピーエス | 物質離脱障害を治療するためのｇａｂａ−ａアンタゴニスト |
| KR20240050372A (ko) | 2021-09-14 | 2024-04-18 | 난징 미노바 파마슈티컬 컴퍼니, 리미티드 | 수용성 알로프레그나놀론 유도체 및 이의 제조 방법과 용도 |
| US20250387409A1 (en) | 2021-11-10 | 2025-12-25 | Umecrine Cognition Ab | 3-beta-hydroxy-3-alpha-ethyl steroids for modulation of the alpha-3 subtype of the gabaa receptor |
| CA3237550A1 (en) | 2021-11-10 | 2023-05-19 | Umecrine Ab | 3.alpha.-substituted 3.beta.-hydroxy 17-oximated androstane compound for modulation of the alpha-3 subtype of the gaba-a receptor |
| WO2023083980A1 (en) | 2021-11-10 | 2023-05-19 | Umecrine Ab | Steroid as a modulator of gabaa receptor |
Family Cites Families (6)
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|---|---|---|---|---|
| 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 |
| WO1995005826A1 (en) * | 1993-08-20 | 1995-03-02 | Jackson Meyer B | Method for regulating neuropeptide hormone secretion |
| US5939545A (en) * | 1994-02-14 | 1999-08-17 | Cocensys, Inc. | Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series |
| NZ298567A (en) * | 1994-11-23 | 2000-01-28 | Cocensys Inc | Androstane and pregnane derivatives, pharmaceutical compositions and methods of treatment |
| BR9809376A (pt) * | 1997-05-02 | 2000-07-04 | American Home Prod | Pregnan-3-ol-20-onas |
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1999
- 1999-03-10 AU AU33292/99A patent/AU756001B2/en not_active Ceased
- 1999-03-10 AT AT99914491T patent/ATE307592T1/de not_active IP Right Cessation
- 1999-03-10 CN CNB998060283A patent/CN1270718C/zh not_active Expired - Fee Related
- 1999-03-10 WO PCT/EP1999/001496 patent/WO1999045931A1/en not_active Ceased
- 1999-03-10 EP EP99914491A patent/EP1063999B1/en not_active Expired - Lifetime
- 1999-03-10 CA CA002321728A patent/CA2321728C/en not_active Expired - Fee Related
- 1999-03-10 DE DE69927960T patent/DE69927960T2/de not_active Expired - Lifetime
- 1999-03-10 JP JP2000535346A patent/JP3877961B2/ja not_active Expired - Fee Related
- 1999-03-11 US US09/266,035 patent/US6455516B1/en not_active Expired - Lifetime
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|---|---|
| CA2321728A1 (en) | 1999-09-16 |
| EP1063999B1 (en) | 2005-10-26 |
| DE69927960D1 (de) | 2005-12-01 |
| CN1270718C (zh) | 2006-08-23 |
| CA2321728C (en) | 2008-12-09 |
| JP2002506034A (ja) | 2002-02-26 |
| CN1300219A (zh) | 2001-06-20 |
| ATE307592T1 (de) | 2005-11-15 |
| JP3877961B2 (ja) | 2007-02-07 |
| AU3329299A (en) | 1999-09-27 |
| AU756001B2 (en) | 2003-01-02 |
| WO1999045931A1 (en) | 1999-09-16 |
| US6455516B1 (en) | 2002-09-24 |
| EP1063999A1 (en) | 2001-01-03 |
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Owner name: UMECRINE MOOD AB, STOCKHOLM, SE |