JP2001513800A - 医薬組成物調製のためのピバガビンの使用 - Google Patents
医薬組成物調製のためのピバガビンの使用Info
- Publication number
- JP2001513800A JP2001513800A JP53816898A JP53816898A JP2001513800A JP 2001513800 A JP2001513800 A JP 2001513800A JP 53816898 A JP53816898 A JP 53816898A JP 53816898 A JP53816898 A JP 53816898A JP 2001513800 A JP2001513800 A JP 2001513800A
- Authority
- JP
- Japan
- Prior art keywords
- pivagabine
- pharmaceutical composition
- anxiety
- day
- gaba
- 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.)
- Pending
Links
- SRPNQDXRVRCTNK-UHFFFAOYSA-N pivagabine Chemical compound CC(C)(C)C(=O)NCCCC(O)=O SRPNQDXRVRCTNK-UHFFFAOYSA-N 0.000 title claims abstract description 34
- 229960003084 pivagabine Drugs 0.000 title claims abstract description 33
- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 23
- 238000002360 preparation method Methods 0.000 title description 2
- 208000019901 Anxiety disease Diseases 0.000 claims abstract description 23
- 230000036506 anxiety Effects 0.000 claims abstract description 8
- 208000020401 Depressive disease Diseases 0.000 claims description 5
- 230000005856 abnormality Effects 0.000 claims description 5
- 208000019022 Mood disease Diseases 0.000 claims description 3
- 230000000694 effects Effects 0.000 description 16
- 241000700159 Rattus Species 0.000 description 11
- 230000001773 anti-convulsant effect Effects 0.000 description 10
- 239000002552 dosage form Substances 0.000 description 10
- 206010054089 Depressive symptom Diseases 0.000 description 9
- 239000001961 anticonvulsive agent Substances 0.000 description 8
- 229960003965 antiepileptics Drugs 0.000 description 8
- 210000004556 brain Anatomy 0.000 description 8
- 241001465754 Metazoa Species 0.000 description 7
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical class NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 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
- 230000000949 anxiolytic effect Effects 0.000 description 6
- 102000005962 receptors Human genes 0.000 description 6
- 108020003175 receptors Proteins 0.000 description 6
- 150000003431 steroids Chemical class 0.000 description 6
- 239000003826 tablet Substances 0.000 description 6
- AURFZBICLPNKBZ-UHFFFAOYSA-N Pregnanolone Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 AURFZBICLPNKBZ-UHFFFAOYSA-N 0.000 description 5
- 241000699670 Mus sp. Species 0.000 description 4
- 239000004615 ingredient Substances 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 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 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
- IYGYMKDQCDOMRE-QRWMCTBCSA-N Bicculine Chemical compound O([C@H]1C2C3=CC=4OCOC=4C=C3CCN2C)C(=O)C2=C1C=CC1=C2OCO1 IYGYMKDQCDOMRE-QRWMCTBCSA-N 0.000 description 3
- AACMFFIUYXGCOC-UHFFFAOYSA-N bicuculline Natural products CN1CCc2cc3OCOc3cc2C1C4OCc5c6OCOc6ccc45 AACMFFIUYXGCOC-UHFFFAOYSA-N 0.000 description 3
- 230000015572 biosynthetic process Effects 0.000 description 3
- 210000003710 cerebral cortex Anatomy 0.000 description 3
- IYGYMKDQCDOMRE-UHFFFAOYSA-N d-Bicucullin Natural products CN1CCC2=CC=3OCOC=3C=C2C1C1OC(=O)C2=C1C=CC1=C2OCO1 IYGYMKDQCDOMRE-UHFFFAOYSA-N 0.000 description 3
- 230000003111 delayed effect Effects 0.000 description 3
- 201000010099 disease Diseases 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 238000000537 electroencephalography Methods 0.000 description 3
- 206010015037 epilepsy Diseases 0.000 description 3
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000002858 neurotransmitter agent Substances 0.000 description 3
- 239000000902 placebo Substances 0.000 description 3
- 229940068196 placebo Drugs 0.000 description 3
- 229960003387 progesterone Drugs 0.000 description 3
- 239000000186 progesterone Substances 0.000 description 3
- 210000002700 urine Anatomy 0.000 description 3
- ZESRJSPZRDMNHY-YFWFAHHUSA-N 11-deoxycorticosterone Chemical class O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 ZESRJSPZRDMNHY-YFWFAHHUSA-N 0.000 description 2
- 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
- 206010010904 Convulsion Diseases 0.000 description 2
- 206010067482 No adverse event Diseases 0.000 description 2
- -1 alpha-hydroxylated pregnane steroids Chemical class 0.000 description 2
- 230000001430 anti-depressive effect Effects 0.000 description 2
- 239000000935 antidepressant agent Substances 0.000 description 2
- 229940005513 antidepressants Drugs 0.000 description 2
- 230000008499 blood brain barrier function Effects 0.000 description 2
- 210000001218 blood-brain barrier Anatomy 0.000 description 2
- 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 2
- 239000002775 capsule Substances 0.000 description 2
- 230000036461 convulsion Effects 0.000 description 2
- CZWCKYRVOZZJNM-USOAJAOKSA-N dehydroepiandrosterone sulfate Chemical compound C1[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 CZWCKYRVOZZJNM-USOAJAOKSA-N 0.000 description 2
- 239000003995 emulsifying agent Substances 0.000 description 2
- 230000001037 epileptic effect Effects 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 239000000796 flavoring agent Substances 0.000 description 2
- 235000019634 flavors Nutrition 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- 230000002209 hydrophobic effect Effects 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 231100000252 nontoxic Toxicity 0.000 description 2
- 230000003204 osmotic effect Effects 0.000 description 2
- 239000002831 pharmacologic agent Substances 0.000 description 2
- 230000000144 pharmacologic effect Effects 0.000 description 2
- 229950009829 prasterone sulfate Drugs 0.000 description 2
- 239000003755 preservative agent Substances 0.000 description 2
- 150000003146 progesterones Chemical class 0.000 description 2
- 208000020016 psychiatric disease Diseases 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000003381 stabilizer Substances 0.000 description 2
- 239000008174 sterile solution Substances 0.000 description 2
- 230000001954 sterilising effect Effects 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 239000006188 syrup Substances 0.000 description 2
- 235000020357 syrup Nutrition 0.000 description 2
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
- HFUCNMPQEAYQDJ-UHFFFAOYSA-N 4-(4-ethynylphenyl)-1-propyl-3,5,8-trioxabicyclo[2.2.2]octane Chemical compound O1CC(CCC)(CO2)COC12C1=CC=C(C#C)C=C1 HFUCNMPQEAYQDJ-UHFFFAOYSA-N 0.000 description 1
- 229930000680 A04AD01 - Scopolamine Natural products 0.000 description 1
- 102000004092 Amidohydrolases Human genes 0.000 description 1
- 108090000531 Amidohydrolases Proteins 0.000 description 1
- 208000000044 Amnesia Diseases 0.000 description 1
- 208000031091 Amnestic disease Diseases 0.000 description 1
- 208000014644 Brain disease Diseases 0.000 description 1
- 108010062745 Chloride Channels Proteins 0.000 description 1
- 102000011045 Chloride Channels Human genes 0.000 description 1
- 208000030453 Drug-Related Side Effects and Adverse reaction Diseases 0.000 description 1
- 102000027484 GABAA receptors Human genes 0.000 description 1
- 108091008681 GABAA receptors Proteins 0.000 description 1
- STECJAGHUSJQJN-GAUPFVANSA-N Hyoscine Natural products C1([C@H](CO)C(=O)OC2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-GAUPFVANSA-N 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 241000257159 Musca domestica Species 0.000 description 1
- STECJAGHUSJQJN-UHFFFAOYSA-N N-Methyl-scopolamin Natural products C1C(C2C3O2)N(C)C3CC1OC(=O)C(CO)C1=CC=CC=C1 STECJAGHUSJQJN-UHFFFAOYSA-N 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 241000404883 Pisa Species 0.000 description 1
- 229940123142 Steroid sulfatase inhibitor Drugs 0.000 description 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 1
- IUJDSEJGGMCXSG-UHFFFAOYSA-N Thiopental Chemical compound CCCC(C)C1(CC)C(=O)NC(=S)NC1=O IUJDSEJGGMCXSG-UHFFFAOYSA-N 0.000 description 1
- 206010070863 Toxicity to various agents Diseases 0.000 description 1
- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 description 1
- 206010048010 Withdrawal syndrome Diseases 0.000 description 1
- 230000003213 activating effect Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000003470 adrenal cortex hormone Substances 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 230000006986 amnesia Effects 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000002249 anxiolytic agent Substances 0.000 description 1
- 229940049706 benzodiazepine Drugs 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 230000002490 cerebral effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000007012 clinical effect Effects 0.000 description 1
- 230000001149 cognitive effect Effects 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000004040 coloring Methods 0.000 description 1
- 230000001276 controlling effect Effects 0.000 description 1
- 239000003179 convulsant agent Substances 0.000 description 1
- 210000003618 cortical neuron Anatomy 0.000 description 1
- ZESRJSPZRDMNHY-UHFFFAOYSA-N de-oxy corticosterone Chemical class O=C1CCC2(C)C3CCC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 ZESRJSPZRDMNHY-UHFFFAOYSA-N 0.000 description 1
- 229940119740 deoxycorticosterone Drugs 0.000 description 1
- 229950007402 eltanolone Drugs 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 239000003163 gonadal steroid hormone Substances 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 230000000971 hippocampal effect Effects 0.000 description 1
- 210000001320 hippocampus Anatomy 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 230000001127 hyperphagic effect Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 239000002917 insecticide Substances 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 230000004060 metabolic process Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 230000036651 mood Effects 0.000 description 1
- 230000000877 morphologic effect Effects 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 229940024999 proteolytic enzymes for treatment of wounds and ulcers Drugs 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- STECJAGHUSJQJN-FWXGHANASA-N scopolamine Chemical compound C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3N([C@H](C2)[C@@H]2[C@H]3O2)C)=CC=CC=C1 STECJAGHUSJQJN-FWXGHANASA-N 0.000 description 1
- 229960002646 scopolamine Drugs 0.000 description 1
- 238000002798 spectrophotometry method Methods 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 230000007428 synaptic transmission, GABAergic Effects 0.000 description 1
- 231100000440 toxicity profile Toxicity 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IT97MI000456A IT1290003B1 (it) | 1997-03-03 | 1997-03-03 | Uso di pivagabina per preparare composizioni farmaceutiche |
| IT97A000456 | 1997-03-03 | ||
| PCT/EP1998/001279 WO1998038988A1 (fr) | 1997-03-03 | 1998-02-25 | Utilisation de la pivagabine dans la preparation de compositions pharmaceutiques |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2001513800A true JP2001513800A (ja) | 2001-09-04 |
Family
ID=11376246
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP53816898A Pending JP2001513800A (ja) | 1997-03-03 | 1998-02-25 | 医薬組成物調製のためのピバガビンの使用 |
Country Status (7)
| Country | Link |
|---|---|
| JP (1) | JP2001513800A (fr) |
| AR (1) | AR011907A1 (fr) |
| AU (1) | AU7031798A (fr) |
| IL (1) | IL131355A0 (fr) |
| IT (1) | IT1290003B1 (fr) |
| WO (1) | WO1998038988A1 (fr) |
| ZA (1) | ZA981729B (fr) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010511615A (ja) * | 2006-11-30 | 2010-04-15 | セナークス、バイオファーマ、インコーポレーテッド | 中枢神経系障害用薬剤としてのピバガビンのジアルキルアミノアルキルエステル |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP3441382B1 (fr) * | 2016-04-05 | 2023-08-30 | Moresco Corporation | Composé d'oxa-acide |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IT1202402B (it) * | 1977-06-01 | 1989-02-09 | Galzigna Lauro | Derivati idrofobici dell'acido 4-aminobutirrico |
-
1997
- 1997-03-03 IT IT97MI000456A patent/IT1290003B1/it active IP Right Grant
-
1998
- 1998-02-25 JP JP53816898A patent/JP2001513800A/ja active Pending
- 1998-02-25 WO PCT/EP1998/001279 patent/WO1998038988A1/fr active Application Filing
- 1998-02-25 IL IL13135598A patent/IL131355A0/xx unknown
- 1998-02-25 AU AU70317/98A patent/AU7031798A/en not_active Abandoned
- 1998-03-02 ZA ZA981729A patent/ZA981729B/xx unknown
- 1998-03-02 AR ARP980100917A patent/AR011907A1/es unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2010511615A (ja) * | 2006-11-30 | 2010-04-15 | セナークス、バイオファーマ、インコーポレーテッド | 中枢神経系障害用薬剤としてのピバガビンのジアルキルアミノアルキルエステル |
Also Published As
| Publication number | Publication date |
|---|---|
| AU7031798A (en) | 1998-09-22 |
| IL131355A0 (en) | 2001-01-28 |
| IT1290003B1 (it) | 1998-10-19 |
| WO1998038988A1 (fr) | 1998-09-11 |
| ITMI970456A1 (it) | 1998-09-03 |
| ZA981729B (en) | 1998-08-28 |
| AR011907A1 (es) | 2000-09-13 |
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