CA2468248C - Pregnane steroids for use in the treatment of cns disorders - Google Patents
Pregnane steroids for use in the treatment of cns disorders Download PDFInfo
- Publication number
- CA2468248C CA2468248C CA2468248A CA2468248A CA2468248C CA 2468248 C CA2468248 C CA 2468248C CA 2468248 A CA2468248 A CA 2468248A CA 2468248 A CA2468248 A CA 2468248A CA 2468248 C CA2468248 C CA 2468248C
- Authority
- CA
- Canada
- Prior art keywords
- 3beta
- 5alpha
- hydroxy
- pregnan
- steroid
- 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 - Fee Related
Links
- -1 Pregnane steroids Chemical class 0.000 title abstract description 12
- 150000003431 steroids Chemical class 0.000 claims abstract description 92
- 238000004519 manufacturing process Methods 0.000 claims abstract description 29
- 230000001225 therapeutic effect Effects 0.000 claims abstract description 25
- 230000002265 prevention Effects 0.000 claims abstract description 23
- 208000015114 central nervous system disease Diseases 0.000 claims abstract description 17
- 230000000694 effects Effects 0.000 claims description 66
- 230000027758 ovulation cycle Effects 0.000 claims description 25
- GFHOQCXDABGYAL-POBGKJHXSA-N 3beta-Hydroxy-5alpha-pregnan-20-one acetate Chemical compound C1C[C@@H]2[C@@]3(C)CC[C@H](OC(=O)C)C[C@@H]3CC[C@H]2[C@@H]2CC[C@H](C(C)=O)[C@]21C GFHOQCXDABGYAL-POBGKJHXSA-N 0.000 claims description 24
- YWYQTGBBEZQBGO-HUTKLZKUSA-N 5beta-pregnane-3beta,20alpha-diol 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@@H](O)C)[C@@]2(C)CC1 YWYQTGBBEZQBGO-HUTKLZKUSA-N 0.000 claims description 24
- CYKYBWRSLLXBOW-PFIRBALFSA-N 2-hydroxy-1-[(3s,5r,8r,9s,10s,13s,14s,17s)-3-hydroxy-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 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-PFIRBALFSA-N 0.000 claims description 23
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
- DUHUCHOQIDJXAT-YUUPMBNKSA-N (3s,5s,8s,9s,10s,13s,14s,17s)-17-acetyl-3-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-11-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=O DUHUCHOQIDJXAT-YUUPMBNKSA-N 0.000 claims description 22
- 208000035475 disorder Diseases 0.000 claims description 22
- 230000003867 tiredness Effects 0.000 claims description 22
- 208000016255 tiredness Diseases 0.000 claims description 22
- 206010015037 epilepsy Diseases 0.000 claims description 20
- 208000019695 Migraine disease Diseases 0.000 claims description 17
- 206010027599 migraine Diseases 0.000 claims description 17
- 206010027940 Mood altered Diseases 0.000 claims description 15
- 230000007510 mood change Effects 0.000 claims description 15
- 206010036618 Premenstrual syndrome Diseases 0.000 claims description 12
- 230000015654 memory Effects 0.000 claims description 11
- 229940127234 oral contraceptive Drugs 0.000 claims description 10
- 239000003539 oral contraceptive agent Substances 0.000 claims description 10
- 159000000000 sodium salts Chemical class 0.000 claims description 10
- 230000005906 menstruation Effects 0.000 claims description 9
- 230000035945 sensitivity Effects 0.000 claims description 9
- 206010056465 Food craving Diseases 0.000 claims description 7
- 206010034759 Petit mal epilepsy Diseases 0.000 claims description 7
- 208000003554 absence epilepsy Diseases 0.000 claims description 7
- 206010021654 increased appetite Diseases 0.000 claims description 7
- 206010027175 memory impairment Diseases 0.000 claims description 7
- 230000007659 motor function Effects 0.000 claims description 7
- 206010009696 Clumsiness Diseases 0.000 claims description 6
- 206010022998 Irritability Diseases 0.000 claims description 6
- 208000037158 Partial Epilepsies Diseases 0.000 claims description 6
- 206010061334 Partial seizures Diseases 0.000 claims description 6
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 claims description 6
- 206010039897 Sedation Diseases 0.000 claims description 6
- 201000007186 focal epilepsy Diseases 0.000 claims description 6
- 230000005032 impulse control Effects 0.000 claims description 6
- 201000003723 learning disability Diseases 0.000 claims description 6
- 230000036651 mood Effects 0.000 claims description 6
- 230000036280 sedation Effects 0.000 claims description 6
- 230000037396 body weight Effects 0.000 claims description 5
- 230000001419 dependent effect Effects 0.000 claims description 5
- 238000001990 intravenous administration Methods 0.000 claims description 5
- 208000019116 sleep disease Diseases 0.000 claims description 5
- 239000003270 steroid hormone Substances 0.000 claims description 4
- 208000019022 Mood disease Diseases 0.000 claims description 3
- 230000001195 anabolic effect Effects 0.000 claims description 3
- 230000001548 androgenic effect Effects 0.000 claims description 3
- 238000002657 hormone replacement therapy Methods 0.000 claims description 3
- 208000027866 inflammatory disease Diseases 0.000 claims description 3
- 238000002360 preparation method Methods 0.000 claims description 3
- 210000000664 rectum Anatomy 0.000 claims description 3
- 238000002560 therapeutic procedure Methods 0.000 claims description 3
- 206010002091 Anaesthesia Diseases 0.000 claims description 2
- 230000037005 anaesthesia Effects 0.000 claims description 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 4
- 201000006152 substance dependence Diseases 0.000 claims 4
- 208000011117 substance-related disease Diseases 0.000 claims 4
- 208000030814 Eating disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- 208000016285 Movement disease Diseases 0.000 claims 2
- 208000010877 cognitive disease Diseases 0.000 claims 2
- 235000014632 disordered eating Nutrition 0.000 claims 2
- 239000000126 substance Substances 0.000 abstract description 28
- 230000009471 action Effects 0.000 abstract description 26
- 238000000034 method Methods 0.000 abstract description 22
- 239000003814 drug Substances 0.000 abstract description 18
- 239000000852 hydrogen donor Substances 0.000 abstract description 9
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 abstract description 7
- 102000004300 GABA-A Receptors Human genes 0.000 description 39
- 108090000839 GABA-A Receptors Proteins 0.000 description 39
- 150000001875 compounds Chemical class 0.000 description 39
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 27
- AURFZBICLPNKBZ-UHFFFAOYSA-N Pregnanolone Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 AURFZBICLPNKBZ-UHFFFAOYSA-N 0.000 description 25
- 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 24
- 230000000903 blocking effect Effects 0.000 description 23
- 230000008859 change Effects 0.000 description 22
- 241000700159 Rattus Species 0.000 description 21
- 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 18
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 13
- 239000000203 mixture Substances 0.000 description 13
- 238000012360 testing method Methods 0.000 description 13
- 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 description 12
- 210000003169 central nervous system Anatomy 0.000 description 12
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 12
- 241001465754 Metazoa Species 0.000 description 11
- 229940079593 drug Drugs 0.000 description 10
- 150000003839 salts Chemical class 0.000 description 10
- 208000024891 symptom Diseases 0.000 description 10
- 229960002200 flunitrazepam Drugs 0.000 description 9
- 239000000047 product Substances 0.000 description 9
- 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
- 230000007246 mechanism Effects 0.000 description 8
- 239000005557 antagonist Substances 0.000 description 7
- 230000008901 benefit Effects 0.000 description 7
- 210000004556 brain Anatomy 0.000 description 7
- 230000001965 increasing effect Effects 0.000 description 7
- 229940049706 benzodiazepine Drugs 0.000 description 6
- 238000011161 development Methods 0.000 description 6
- 230000018109 developmental process Effects 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 239000003981 vehicle Substances 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 206010052804 Drug tolerance Diseases 0.000 description 5
- 239000002671 adjuvant Substances 0.000 description 5
- 238000002474 experimental method Methods 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- 230000013016 learning Effects 0.000 description 5
- 102000005962 receptors Human genes 0.000 description 5
- 108020003175 receptors Proteins 0.000 description 5
- AURFZBICLPNKBZ-YZRLXODZSA-N 3alpha-hydroxy-5beta-pregnan-20-one Chemical group 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 4
- 238000012347 Morris Water Maze Methods 0.000 description 4
- 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 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 4
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical class [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 4
- 229940125717 barbiturate Drugs 0.000 description 4
- 230000006870 function Effects 0.000 description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 4
- 238000000338 in vitro Methods 0.000 description 4
- 230000010534 mechanism of action Effects 0.000 description 4
- 230000001537 neural effect Effects 0.000 description 4
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-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
- JWMFYGXQPXQEEM-NUNROCCHSA-N 5β-pregnane Chemical compound C([C@H]1CC2)CCC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](CC)[C@@]2(C)CC1 JWMFYGXQPXQEEM-NUNROCCHSA-N 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 230000002411 adverse Effects 0.000 description 3
- 238000000540 analysis of variance Methods 0.000 description 3
- 230000003042 antagnostic effect Effects 0.000 description 3
- 150000001557 benzodiazepines Chemical class 0.000 description 3
- 210000005257 cortical tissue Anatomy 0.000 description 3
- 230000002708 enhancing effect Effects 0.000 description 3
- 238000001727 in vivo Methods 0.000 description 3
- 230000003993 interaction Effects 0.000 description 3
- 230000029849 luteinization Effects 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 230000024664 tolerance induction Effects 0.000 description 3
- CYKYBWRSLLXBOW-DATPGIFZSA-N 2-hydroxy-1-[(3r,5r,8r,9s,10s,13s,14s,17s)-3-hydroxy-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 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-DATPGIFZSA-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
- CBMYJHIOYJEBSB-KHOSGYARSA-N 5alpha-androstane-3alpha,17beta-diol Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@H]21 CBMYJHIOYJEBSB-KHOSGYARSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 241000124008 Mammalia Species 0.000 description 2
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 230000001270 agonistic effect Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- 239000000872 buffer Substances 0.000 description 2
- 210000003710 cerebral cortex Anatomy 0.000 description 2
- 210000004246 corpus luteum Anatomy 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 230000003247 decreasing effect Effects 0.000 description 2
- 230000003828 downregulation Effects 0.000 description 2
- 230000001037 epileptic effect Effects 0.000 description 2
- 230000012173 estrus Effects 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 230000004907 flux Effects 0.000 description 2
- 230000036541 health Effects 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
- 125000004356 hydroxy functional group Chemical group O* 0.000 description 2
- 230000006698 induction Effects 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000002955 isolation Methods 0.000 description 2
- 230000000670 limiting effect Effects 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 230000002175 menstrual effect Effects 0.000 description 2
- 210000001672 ovary Anatomy 0.000 description 2
- 210000002826 placenta Anatomy 0.000 description 2
- 239000000186 progesterone Substances 0.000 description 2
- 229960003387 progesterone Drugs 0.000 description 2
- 238000011160 research Methods 0.000 description 2
- 238000012216 screening Methods 0.000 description 2
- 239000000932 sedative agent Substances 0.000 description 2
- 239000000377 silicon dioxide Substances 0.000 description 2
- QQVJEIZJHDPTSH-UTNKIXDHSA-M sodium;[(3s,8s,9s,10r,13s,14s,17s)-17-acetyl-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-3-yl] sulfate Chemical compound [Na+].C1C=C2C[C@@H](OS([O-])(=O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 QQVJEIZJHDPTSH-UTNKIXDHSA-M 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 238000003786 synthesis reaction Methods 0.000 description 2
- 230000000699 topical effect Effects 0.000 description 2
- 238000012549 training Methods 0.000 description 2
- OGNSCSPNOLGXSM-UHFFFAOYSA-N (+/-)-DABA Natural products NCCC(N)C(O)=O OGNSCSPNOLGXSM-UHFFFAOYSA-N 0.000 description 1
- IFHKDUOXEKUXGA-JHGMSEHPSA-N (5r,8s,9s,10s,13s,14s,17s)-17-acetyl-10,13-dimethyl-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-11-one 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=O IFHKDUOXEKUXGA-JHGMSEHPSA-N 0.000 description 1
- HWKJHWWGPNCBBN-XNKUGNQISA-N (8S,9S,10S,13R,14S,17S)-17-ethyl-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene sulfuric acid Chemical compound OS(O)(=O)=O.C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](CC)[C@@]1(C)CC2 HWKJHWWGPNCBBN-XNKUGNQISA-N 0.000 description 1
- AURFZBICLPNKBZ-JMTGGFPBSA-N 1-[(3r,8r,9s,10s,13s,14s,17s)-3-hydroxy-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 C1CC2C[C@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 AURFZBICLPNKBZ-JMTGGFPBSA-N 0.000 description 1
- YPEARZUTWVZHIZ-SRJHXTLLSA-N 1-[(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]ethanol Chemical compound C1CC2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(O)C)[C@@]1(C)CC2 YPEARZUTWVZHIZ-SRJHXTLLSA-N 0.000 description 1
- FUFLCEKSBBHCMO-UHFFFAOYSA-N 11-dehydrocorticosterone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 FUFLCEKSBBHCMO-UHFFFAOYSA-N 0.000 description 1
- ZESRJSPZRDMNHY-YFWFAHHUSA-N 11-deoxycorticosterone Chemical compound 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 1
- 239000003483 4 aminobutyric acid A receptor stimulating agent Substances 0.000 description 1
- AODPIQQILQLWGS-FDSHTENPSA-N 5a-Tetrahydrocortisol Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CC[C@H]21 AODPIQQILQLWGS-FDSHTENPSA-N 0.000 description 1
- CBMYJHIOYJEBSB-GCXXXECGSA-N 5beta-androstane-3alpha,17beta-diol Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CC[C@@H]21 CBMYJHIOYJEBSB-GCXXXECGSA-N 0.000 description 1
- JWMFYGXQPXQEEM-GCOKGBOCSA-N 5α-pregnane Chemical compound C([C@@H]1CC2)CCC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](CC)[C@@]2(C)CC1 JWMFYGXQPXQEEM-GCOKGBOCSA-N 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 108091006146 Channels Proteins 0.000 description 1
- 102000011045 Chloride Channels Human genes 0.000 description 1
- 108010062745 Chloride Channels Proteins 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- MFYSYFVPBJMHGN-ZPOLXVRWSA-N Cortisone Chemical compound O=C1CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 MFYSYFVPBJMHGN-ZPOLXVRWSA-N 0.000 description 1
- MFYSYFVPBJMHGN-UHFFFAOYSA-N Cortisone Natural products O=C1CCC2(C)C3C(=O)CC(C)(C(CC4)(O)C(=O)CO)C4C3CCC2=C1 MFYSYFVPBJMHGN-UHFFFAOYSA-N 0.000 description 1
- FMGSKLZLMKYGDP-UHFFFAOYSA-N Dehydroepiandrosterone Natural products C1C(O)CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CC=C21 FMGSKLZLMKYGDP-UHFFFAOYSA-N 0.000 description 1
- 102000002322 Egg Proteins Human genes 0.000 description 1
- 108010000912 Egg Proteins Proteins 0.000 description 1
- 102000005915 GABA Receptors Human genes 0.000 description 1
- 108010005551 GABA Receptors Proteins 0.000 description 1
- 206010020710 Hyperphagia Diseases 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 239000000853 adhesive Substances 0.000 description 1
- 230000001070 adhesive effect Effects 0.000 description 1
- 230000001919 adrenal effect Effects 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- AEMFNILZOJDQLW-QAGGRKNESA-N androst-4-ene-3,17-dione Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CCC2=C1 AEMFNILZOJDQLW-QAGGRKNESA-N 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 230000000949 anxiolytic effect Effects 0.000 description 1
- 230000003139 buffering effect Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 230000007012 clinical effect Effects 0.000 description 1
- 230000003920 cognitive function Effects 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- 239000003179 convulsant agent Substances 0.000 description 1
- 229960004544 cortisone Drugs 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- ZESRJSPZRDMNHY-UHFFFAOYSA-N de-oxy corticosterone Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 ZESRJSPZRDMNHY-UHFFFAOYSA-N 0.000 description 1
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 description 1
- KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid 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@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 description 1
- 230000000881 depressing effect Effects 0.000 description 1
- 229960003654 desoxycortone Drugs 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940000406 drug candidate Drugs 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 229950007402 eltanolone Drugs 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 230000000763 evoking effect Effects 0.000 description 1
- 238000013401 experimental design Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 238000007429 general method Methods 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 230000000971 hippocampal effect Effects 0.000 description 1
- 229940088597 hormone Drugs 0.000 description 1
- 239000005556 hormone Substances 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000004941 influx Effects 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 238000000670 ligand binding assay Methods 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 210000004379 membrane Anatomy 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000003821 menstrual periods Effects 0.000 description 1
- 239000002207 metabolite Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 210000004400 mucous membrane Anatomy 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 230000008587 neuronal excitability Effects 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000002611 ovarian Effects 0.000 description 1
- 210000002394 ovarian follicle Anatomy 0.000 description 1
- 210000004681 ovum Anatomy 0.000 description 1
- 230000032696 parturition Effects 0.000 description 1
- 238000010149 post-hoc-test Methods 0.000 description 1
- 229960002847 prasterone Drugs 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- ORNBQBCIOKFOEO-QGVNFLHTSA-N pregnenolone Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 ORNBQBCIOKFOEO-QGVNFLHTSA-N 0.000 description 1
- 150000003132 pregnenolones Chemical class 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 230000001739 rebound effect Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 230000003938 response to stress Effects 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 230000001624 sedative effect Effects 0.000 description 1
- 238000007391 self-medication Methods 0.000 description 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000009182 swimming Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 150000003515 testosterones Chemical class 0.000 description 1
- AODPIQQILQLWGS-GXBDJPPSSA-N tetrahydrocortisol Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CC[C@@H]21 AODPIQQILQLWGS-GXBDJPPSSA-N 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 230000031836 visual learning Effects 0.000 description 1
- 239000008215 water for injection Substances 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
- A61K31/573—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 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- 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
-
- 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
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- 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
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- 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
- A61P15/16—Masculine 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
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
- A61P25/10—Antiepileptics; Anticonvulsants for petit-mal
-
- 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
- A61P25/12—Antiepileptics; Anticonvulsants for grand-mal
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
-
- 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
- A61P25/26—Psychostimulants, e.g. nicotine, cocaine
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
-
- 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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Diabetes (AREA)
- Gynecology & Obstetrics (AREA)
- Addiction (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Pregnancy & Childbirth (AREA)
- Hematology (AREA)
- Child & Adolescent Psychology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0104423-9 | 2001-12-27 | ||
| SE0104423A SE0104423D0 (sv) | 2001-12-27 | 2001-12-27 | Pregnane steroids and their use in the treatment of CNS disorders |
| PCT/SE2002/002423 WO2003059357A1 (en) | 2001-12-27 | 2002-12-20 | Pregnane steroids for use in the treatment of cns disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2468248A1 CA2468248A1 (en) | 2003-07-24 |
| CA2468248C true CA2468248C (en) | 2011-08-16 |
Family
ID=20286518
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2468248A Expired - Fee Related CA2468248C (en) | 2001-12-27 | 2002-12-20 | Pregnane steroids for use in the treatment of cns disorders |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7960367B2 (enExample) |
| EP (2) | EP1458399B1 (enExample) |
| JP (2) | JP2005519893A (enExample) |
| CN (3) | CN101601674A (enExample) |
| AU (3) | AU2002359202C1 (enExample) |
| CA (1) | CA2468248C (enExample) |
| DK (1) | DK1458399T3 (enExample) |
| ES (1) | ES2394639T3 (enExample) |
| SE (1) | SE0104423D0 (enExample) |
| WO (1) | WO2003059357A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006054938A1 (en) * | 2004-11-18 | 2006-05-26 | Umecrine Ab | Gaba-steroid antagonists and their use for the treatment of cns disorders |
| RU2413516C2 (ru) * | 2004-11-18 | 2011-03-10 | Умекрин Аб | Гамк-стероидные антагонисты и их применение в лечении нарушений цнс |
| HUE036410T2 (hu) | 2006-11-21 | 2018-07-30 | Asarina Pharma Ab | Pregnán és androsztán szteroidok alkalmazása CNS rendellenességek kezelésére szolgáló gyógyszerkészítmény elõállítására |
| US20090269795A1 (en) * | 2007-03-09 | 2009-10-29 | The Research Foundation Of State University Of New York | Mutant alpha4betadelta GABAA receptor and methods of treating anxiety or irritability |
| CN101585862B (zh) * | 2008-05-20 | 2014-12-17 | 梅克芳股份公司 | 甾族化合物 |
| MX2012008257A (es) | 2010-01-14 | 2012-11-21 | Umecrine Mood Ab | Una composicion farmaceutica que comprende 3-beta-hidroxi-5-alfa-p regnan-20-ona con propiedades mejoradas de almacenamiento y solubilidad. |
| ES2621801T3 (es) * | 2011-05-20 | 2017-07-05 | Inserm - Institut National De La Santé Et De La Recherche Médicale | Antagonistas del receptor CB1 |
| NZ708086A (en) | 2012-11-28 | 2020-04-24 | Inst Nat Sante Rech Med | 3-(4’-substituted)-benzyl-ether derivatives of pregnenolone |
| KR102324667B1 (ko) * | 2014-01-29 | 2021-11-10 | 유메크린 코그니션 에이비 | 간성뇌증 치료용 스테로이드 화합물 |
| JOP20200195A1 (ar) * | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| TWI748936B (zh) | 2015-01-12 | 2021-12-11 | 瑞典商優鎂奎認知Ａｂ公司 | 新穎化合物 |
| US10278977B2 (en) | 2016-06-06 | 2019-05-07 | Umecrine Cognition Ab | Methods for treating hypersomnolence |
| DK3565528T3 (da) * | 2017-01-09 | 2025-05-26 | Relmada Therapeutics Inc | Injicerbare suspensioner |
| 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 |
| CN110430883A (zh) | 2017-02-10 | 2019-11-08 | 阿沙里那制药公司 | 用于医学治疗的3β-羟基-5α-孕烷-20-酮 |
| CA3094026A1 (en) * | 2018-04-05 | 2019-10-10 | Asarina Pharma Aps | Gaba-a antagonists for treating substance withdrawal disorders |
| US11969434B1 (en) | 2022-08-29 | 2024-04-30 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
| EP4429669A1 (en) | 2021-11-10 | 2024-09-18 | Umecrine AB | Steroid as a modulator of gabaa receptor |
| WO2023083979A1 (en) * | 2021-11-10 | 2023-05-19 | Umecrine Ab | 3.beta.-hydroxy, 3.alpha.-ethyl steroids for modulation of the alpha-3 subtype of the gaba-a receptor |
| US20240383941A1 (en) | 2021-11-10 | 2024-11-21 | Umecrine Ab | 3-alpha substituted 3-beta-hydroxy-17-oximated androstane compound for modulation of the alpha-3 subtype of the gabaa receptor |
| US12186327B2 (en) | 2022-08-29 | 2025-01-07 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US5439900A (en) | 1993-02-25 | 1995-08-08 | Bukusoglu; Cuneyt | Methods and compositions for providing analgesia and enhanced anesthesia |
| 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 |
| US5767117A (en) | 1994-11-18 | 1998-06-16 | The General Hospital Corporation | Method for treating vascular headaches |
| EP0980381B1 (en) * | 1997-05-02 | 2003-08-06 | Wyeth | Pharmaceutically acceptable salts of 5.alpha.-pregn-16-en-3.beta.-ol-20-one 3-sulphate ester with progestin activity and useful in the treatment of cns disorders |
| AU739146B2 (en) * | 1997-05-02 | 2001-10-04 | Wyeth | Pregnan-3-ol-20-ones |
| WO1998050411A1 (en) * | 1997-05-02 | 1998-11-12 | American Home Products Corporation | Pharmaceutically acceptable salts of 5alpha-pregnan-3beta, 16alp ha-diol-20-one 3-sulfate useful as progestins and cns disorders |
| WO1999045931A1 (en) | 1998-03-11 | 1999-09-16 | Baeckstroem Torbjoern | Epiallopregnanolone in the treatment of cns disorders |
| CN1330659A (zh) * | 1998-10-13 | 2002-01-09 | 美国家用产品公司 | 孕烷葡糖苷酸类化合物 |
| US20020072509A1 (en) * | 2000-10-11 | 2002-06-13 | Stein Donald Gerald | Methods for the treatment of a traumatic central nervous system injury |
-
2001
- 2001-12-27 SE SE0104423A patent/SE0104423D0/xx unknown
-
2002
- 2002-12-20 CN CNA2009101459536A patent/CN101601674A/zh active Pending
- 2002-12-20 JP JP2003559519A patent/JP2005519893A/ja active Pending
- 2002-12-20 CN CNA2009101459540A patent/CN101601675A/zh active Pending
- 2002-12-20 AU AU2002359202A patent/AU2002359202C1/en not_active Ceased
- 2002-12-20 EP EP02793723A patent/EP1458399B1/en not_active Expired - Lifetime
- 2002-12-20 WO PCT/SE2002/002423 patent/WO2003059357A1/en not_active Ceased
- 2002-12-20 DK DK02793723.4T patent/DK1458399T3/da active
- 2002-12-20 US US10/499,214 patent/US7960367B2/en not_active Expired - Fee Related
- 2002-12-20 EP EP10183670.8A patent/EP2275109B1/en not_active Expired - Lifetime
- 2002-12-20 CA CA2468248A patent/CA2468248C/en not_active Expired - Fee Related
- 2002-12-20 ES ES02793723T patent/ES2394639T3/es not_active Expired - Lifetime
- 2002-12-20 CN CNB028262751A patent/CN100518741C/zh not_active Expired - Fee Related
-
2009
- 2009-05-18 AU AU2009201956A patent/AU2009201956B2/en not_active Ceased
- 2009-05-18 AU AU2009201951A patent/AU2009201951A1/en not_active Abandoned
- 2009-11-10 JP JP2009256620A patent/JP5289281B2/ja not_active Expired - Fee Related
-
2011
- 2011-01-07 US US12/986,937 patent/US8119619B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| AU2009201956B2 (en) | 2010-11-25 |
| US7960367B2 (en) | 2011-06-14 |
| AU2002359202B2 (en) | 2009-02-19 |
| EP2275109A2 (en) | 2011-01-19 |
| WO2003059357A1 (en) | 2003-07-24 |
| JP2005519893A (ja) | 2005-07-07 |
| AU2009201951A1 (en) | 2009-06-04 |
| CN1607954A (zh) | 2005-04-20 |
| JP2010065052A (ja) | 2010-03-25 |
| ES2394639T3 (es) | 2013-02-04 |
| CN101601675A (zh) | 2009-12-16 |
| JP5289281B2 (ja) | 2013-09-11 |
| AU2002359202A1 (en) | 2003-07-30 |
| CN101601674A (zh) | 2009-12-16 |
| SE0104423D0 (sv) | 2001-12-27 |
| US20110098259A1 (en) | 2011-04-28 |
| EP2275109B1 (en) | 2013-07-24 |
| AU2002359202C1 (en) | 2011-03-31 |
| CN100518741C (zh) | 2009-07-29 |
| DK1458399T3 (da) | 2012-11-12 |
| US20050222099A1 (en) | 2005-10-06 |
| EP2275109A3 (en) | 2011-10-12 |
| AU2009201956A2 (en) | 2010-02-18 |
| EP1458399A1 (en) | 2004-09-22 |
| EP1458399B1 (en) | 2012-08-08 |
| US8119619B2 (en) | 2012-02-21 |
| AU2009201956A1 (en) | 2009-06-11 |
| CA2468248A1 (en) | 2003-07-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2009201956B2 (en) | Pregnane steroids for use in the treatment of CNS disorders | |
| CN1270718C (zh) | 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 | |
| HUE031390T2 (en) | Antagonists of cb1 receptor | |
| WO2009142594A9 (en) | The use of 3beta-ethenyl, methyl, 3alpha-hydroxy-steroids for the treatment of cns disorders | |
| US8372824B2 (en) | GABA-steroid antagonists and their use for the treatment of CNS disorders | |
| US6987101B1 (en) | Therapeutic gestagens for the treatment of premenstrual dysphoric disorder | |
| US11026953B2 (en) | 3-beta-hydroxy-5-alpha-pregnan-20-one for use in treatment of essential tremor | |
| RU2413516C2 (ru) | Гамк-стероидные антагонисты и их применение в лечении нарушений цнс |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20151221 |