CN101601675A - 用于治疗中枢神经系统功能紊乱的孕烷类固醇 - Google Patents
用于治疗中枢神经系统功能紊乱的孕烷类固醇 Download PDFInfo
- Publication number
- CN101601675A CN101601675A CNA2009101459540A CN200910145954A CN101601675A CN 101601675 A CN101601675 A CN 101601675A CN A2009101459540 A CNA2009101459540 A CN A2009101459540A CN 200910145954 A CN200910145954 A CN 200910145954A CN 101601675 A CN101601675 A CN 101601675A
- Authority
- CN
- China
- Prior art keywords
- alpha
- hydroxies
- pregnane
- beta
- 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.)
- Pending
Links
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 27
- 210000003169 central nervous system Anatomy 0.000 title description 25
- -1 pregnane steroids Chemical class 0.000 title description 7
- 150000003431 steroids Chemical class 0.000 claims abstract description 90
- 230000000694 effects Effects 0.000 claims abstract description 70
- 230000004064 dysfunction Effects 0.000 claims abstract description 28
- 239000003814 drug Substances 0.000 claims abstract description 26
- 239000000463 material Substances 0.000 claims abstract description 18
- 238000002560 therapeutic procedure Methods 0.000 claims abstract description 4
- 150000001875 compounds Chemical class 0.000 claims description 45
- 238000000034 method Methods 0.000 claims description 44
- 102000004300 GABA-A Receptors Human genes 0.000 claims description 43
- 108090000839 GABA-A Receptors Proteins 0.000 claims description 43
- 150000002148 esters Chemical class 0.000 claims description 30
- 230000027758 ovulation cycle Effects 0.000 claims description 21
- 230000001419 dependent effect Effects 0.000 claims description 18
- 159000000000 sodium salts Chemical class 0.000 claims description 18
- 206010015037 epilepsy Diseases 0.000 claims description 17
- 201000010099 disease Diseases 0.000 claims description 15
- 208000035475 disorder Diseases 0.000 claims description 11
- 208000019695 Migraine disease Diseases 0.000 claims description 10
- 206010036618 Premenstrual syndrome Diseases 0.000 claims description 10
- 238000011161 development Methods 0.000 claims description 10
- 230000018109 developmental process Effects 0.000 claims description 10
- 238000004519 manufacturing process Methods 0.000 claims description 10
- 206010027599 migraine Diseases 0.000 claims description 10
- 238000001990 intravenous administration Methods 0.000 claims description 9
- 229940127234 oral contraceptive Drugs 0.000 claims description 9
- 239000003539 oral contraceptive agent Substances 0.000 claims description 9
- 206010027940 Mood altered Diseases 0.000 claims description 8
- 230000037396 body weight Effects 0.000 claims description 8
- 230000000994 depressogenic effect Effects 0.000 claims description 8
- 230000007510 mood change Effects 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 8
- 208000012661 Dyskinesia Diseases 0.000 claims description 6
- 230000036528 appetite Effects 0.000 claims description 6
- 235000019789 appetite Nutrition 0.000 claims description 6
- 230000000977 initiatory effect Effects 0.000 claims description 6
- 229940000406 drug candidate Drugs 0.000 claims description 5
- 208000019116 sleep disease Diseases 0.000 claims description 5
- 208000020685 sleep-wake disease Diseases 0.000 claims description 5
- 239000000126 substance Substances 0.000 claims description 5
- 206010022998 Irritability Diseases 0.000 claims description 4
- 208000020358 Learning disease Diseases 0.000 claims description 4
- 206010034759 Petit mal epilepsy Diseases 0.000 claims description 4
- 208000003554 absence epilepsy Diseases 0.000 claims description 4
- 239000012141 concentrate Substances 0.000 claims description 4
- 201000003723 learning disability Diseases 0.000 claims description 4
- 230000009245 menopause Effects 0.000 claims description 4
- 206010009696 Clumsiness Diseases 0.000 claims description 3
- 208000024732 dysthymic disease Diseases 0.000 claims description 3
- 210000000664 rectum Anatomy 0.000 claims description 3
- 239000003270 steroid hormone Substances 0.000 claims description 3
- 206010002091 Anaesthesia Diseases 0.000 claims description 2
- 230000037005 anaesthesia Effects 0.000 claims description 2
- 239000003098 androgen Substances 0.000 claims description 2
- 239000007795 chemical reaction product Substances 0.000 claims description 2
- 238000002657 hormone replacement therapy Methods 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- 230000004936 stimulating effect Effects 0.000 claims description 2
- 230000002951 depilatory effect Effects 0.000 claims 2
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000006866 deterioration Effects 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 238000001794 hormone therapy Methods 0.000 claims 1
- 239000000852 hydrogen donor Substances 0.000 abstract description 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract description 7
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 abstract description 6
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 description 29
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 24
- 241000700159 Rattus Species 0.000 description 20
- 230000008859 change Effects 0.000 description 13
- 238000012360 testing method Methods 0.000 description 13
- 230000006870 function Effects 0.000 description 12
- 239000000203 mixture Substances 0.000 description 11
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 10
- 150000003839 salts Chemical class 0.000 description 10
- 208000024891 symptom Diseases 0.000 description 10
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 10
- 230000000903 blocking effect Effects 0.000 description 9
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 9
- 230000007246 mechanism Effects 0.000 description 9
- 239000000047 product Substances 0.000 description 9
- 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 8
- 241001465754 Metazoa Species 0.000 description 8
- 238000011160 research Methods 0.000 description 8
- 239000005557 antagonist Substances 0.000 description 7
- 210000004556 brain Anatomy 0.000 description 7
- 230000008901 benefit Effects 0.000 description 6
- 238000002474 experimental method Methods 0.000 description 6
- 239000008194 pharmaceutical composition Substances 0.000 description 6
- 239000000546 pharmaceutical excipient Substances 0.000 description 6
- 238000002360 preparation method Methods 0.000 description 6
- 102000005962 receptors Human genes 0.000 description 6
- 108020003175 receptors Proteins 0.000 description 6
- 230000001105 regulatory effect Effects 0.000 description 6
- 206010013754 Drug withdrawal syndrome Diseases 0.000 description 5
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 5
- 239000002671 adjuvant Substances 0.000 description 5
- 230000008485 antagonism Effects 0.000 description 5
- 230000005764 inhibitory process Effects 0.000 description 5
- 230000035479 physiological effects, processes and functions Effects 0.000 description 5
- AURFZBICLPNKBZ-UHFFFAOYSA-N Pregnanolone Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 AURFZBICLPNKBZ-UHFFFAOYSA-N 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
- 229940125717 barbiturate Drugs 0.000 description 4
- 230000010534 mechanism of action Effects 0.000 description 4
- 230000003821 menstrual periods Effects 0.000 description 4
- 230000008569 process Effects 0.000 description 4
- 230000028327 secretion Effects 0.000 description 4
- 229930193551 sterin Natural products 0.000 description 4
- 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
- 206010052804 Drug tolerance Diseases 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 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 3
- 238000010171 animal model Methods 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 3
- 230000003203 everyday effect Effects 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- 238000011534 incubation Methods 0.000 description 3
- 230000002045 lasting effect Effects 0.000 description 3
- 230000029849 luteinization Effects 0.000 description 3
- 230000001537 neural effect Effects 0.000 description 3
- 230000035945 sensitivity Effects 0.000 description 3
- 238000012549 training Methods 0.000 description 3
- 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 2
- 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 description 2
- 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 2
- 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 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
- 239000000556 agonist Substances 0.000 description 2
- 238000000540 analysis of variance Methods 0.000 description 2
- 238000004458 analytical method Methods 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
- 210000003710 cerebral cortex Anatomy 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 210000004246 corpus luteum Anatomy 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 206010013663 drug dependence Diseases 0.000 description 2
- 238000002651 drug therapy Methods 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- 230000003862 health status 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
- 238000001727 in vivo Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 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
- 230000005906 menstruation Effects 0.000 description 2
- 210000002826 placenta Anatomy 0.000 description 2
- 229960003387 progesterone Drugs 0.000 description 2
- 239000000186 progesterone Substances 0.000 description 2
- 230000009467 reduction Effects 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
- 208000011117 substance-related disease Diseases 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 230000009182 swimming Effects 0.000 description 2
- LTYZUJSCZCPGHH-DCSYEGIMSA-N (2s,3r,4s,5r,6r)-2-[[(1r,2s,3r,4r,5r)-3,4-dihydroxy-6,8-dioxabicyclo[3.2.1]octan-2-yl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]2OC[C@H]1O2 LTYZUJSCZCPGHH-DCSYEGIMSA-N 0.000 description 1
- SFXPZLCQRZASKK-UHFFFAOYSA-N (3alpha,5alpha)-3-Hydroxypregn-16-en-20-one Natural products C1CC2CC(O)CCC2(C)C2C1C1CC=C(C(=O)C)C1(C)CC2 SFXPZLCQRZASKK-UHFFFAOYSA-N 0.000 description 1
- SFXPZLCQRZASKK-CKBUFISISA-N 1-[(3s,5s,8r,9s,10s,13s,14s)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl]ethanone Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC=C(C(=O)C)[C@@]2(C)CC1 SFXPZLCQRZASKK-CKBUFISISA-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
- 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 1
- 239000003483 4 aminobutyric acid A receptor stimulating agent Substances 0.000 description 1
- 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 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
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 102000011045 Chloride Channels Human genes 0.000 description 1
- 108010062745 Chloride Channels Proteins 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
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 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
- 206010021703 Indifference Diseases 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 238000012347 Morris Water Maze Methods 0.000 description 1
- 241001597008 Nomeidae Species 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 150000004703 alkoxides Chemical class 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
- 229960005471 androstenedione Drugs 0.000 description 1
- AEMFNILZOJDQLW-UHFFFAOYSA-N androstenedione Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)=O)C4C3CCC2=C1 AEMFNILZOJDQLW-UHFFFAOYSA-N 0.000 description 1
- 230000003556 anti-epileptic effect Effects 0.000 description 1
- 239000001961 anticonvulsive agent Substances 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 230000001174 ascending effect Effects 0.000 description 1
- 230000006399 behavior Effects 0.000 description 1
- 244000309464 bull Species 0.000 description 1
- 238000004422 calculation algorithm Methods 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 210000004027 cell Anatomy 0.000 description 1
- 239000013626 chemical specie Substances 0.000 description 1
- 230000003920 cognitive function Effects 0.000 description 1
- 239000008119 colloidal silica Substances 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 229940126214 compound 3 Drugs 0.000 description 1
- 238000004590 computer program Methods 0.000 description 1
- 230000000985 convulsing effect Effects 0.000 description 1
- 229960004544 cortisone Drugs 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
- 229940119740 deoxycorticosterone Drugs 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 229950007402 eltanolone Drugs 0.000 description 1
- 238000005516 engineering process Methods 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
- 238000009472 formulation Methods 0.000 description 1
- 229960005150 glycerol Drugs 0.000 description 1
- 210000001879 hippocampal ca1 region Anatomy 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
- 230000000147 hypnotic effect Effects 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002452 interceptive effect Effects 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 125000000468 ketone group Chemical group 0.000 description 1
- 150000002576 ketones Chemical class 0.000 description 1
- 238000002372 labelling 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
- 239000012528 membrane Substances 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
- 231100000219 mutagenic Toxicity 0.000 description 1
- 230000003505 mutagenic effect Effects 0.000 description 1
- 239000003887 narcotic antagonist Substances 0.000 description 1
- 208000020470 nervous system symptom Diseases 0.000 description 1
- 230000000926 neurological effect Effects 0.000 description 1
- 210000002569 neuron Anatomy 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
- 230000001151 other effect Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 210000004681 ovum Anatomy 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229960002847 prasterone Drugs 0.000 description 1
- 230000035935 pregnancy Effects 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
- 230000007115 recruitment Effects 0.000 description 1
- 239000012744 reinforcing agent Substances 0.000 description 1
- 230000010076 replication Effects 0.000 description 1
- 210000002345 respiratory system Anatomy 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- CBXWGGFGZDVPNV-UHFFFAOYSA-N so4-so4 Chemical group OS(O)(=O)=O.OS(O)(=O)=O CBXWGGFGZDVPNV-UHFFFAOYSA-N 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 238000000528 statistical test Methods 0.000 description 1
- 239000008227 sterile water for injection Substances 0.000 description 1
- 238000005728 strengthening Methods 0.000 description 1
- 239000000375 suspending agent Substances 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
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 210000001215 vagina Anatomy 0.000 description 1
- 229940099259 vaseline Drugs 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000008215 water for injection Substances 0.000 description 1
Images
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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE01044239 | 2001-12-27 | ||
| SE0104423A SE0104423D0 (sv) | 2001-12-27 | 2001-12-27 | Pregnane steroids and their use in the treatment of CNS disorders |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB028262751A Division CN100518741C (zh) | 2001-12-27 | 2002-12-20 | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101601675A true CN101601675A (zh) | 2009-12-16 |
Family
ID=20286518
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2009101459540A Pending CN101601675A (zh) | 2001-12-27 | 2002-12-20 | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 |
| CNB028262751A Expired - Fee Related CN100518741C (zh) | 2001-12-27 | 2002-12-20 | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 |
| CNA2009101459536A Pending CN101601674A (zh) | 2001-12-27 | 2002-12-20 | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB028262751A Expired - Fee Related CN100518741C (zh) | 2001-12-27 | 2002-12-20 | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 |
| CNA2009101459536A Pending CN101601674A (zh) | 2001-12-27 | 2002-12-20 | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7960367B2 (https=) |
| EP (2) | EP2275109B1 (https=) |
| JP (2) | JP2005519893A (https=) |
| CN (3) | CN101601675A (https=) |
| AU (3) | AU2002359202C1 (https=) |
| CA (1) | CA2468248C (https=) |
| DK (1) | DK1458399T3 (https=) |
| ES (1) | ES2394639T3 (https=) |
| SE (1) | SE0104423D0 (https=) |
| WO (1) | WO2003059357A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111918657A (zh) * | 2018-04-05 | 2020-11-10 | 阿沙里那制药有限公司 | 用于治疗物质戒断障碍的gaba-a拮抗剂 |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2413516C2 (ru) * | 2004-11-18 | 2011-03-10 | Умекрин Аб | Гамк-стероидные антагонисты и их применение в лечении нарушений цнс |
| 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 |
| 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. |
| 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 |
| 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 |
| 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 |
| 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 |
| AR103384A1 (es) | 2015-01-12 | 2017-05-03 | Umecrine Cognition Ab | 3a-ETINILO, 3b-HIDROXI, 5a-PREGNAN-20-OXIMA COMO MODULADOR DE GABA |
| 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 |
| US11969434B1 (en) | 2022-08-29 | 2024-04-30 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
| 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 |
| 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 |
| WO2023083980A1 (en) | 2021-11-10 | 2023-05-19 | Umecrine Ab | Steroid as a modulator of 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 |
| BR9809376A (pt) * | 1997-05-02 | 2000-07-04 | American Home Prod | Pregnan-3-ol-20-onas |
| ATE246705T1 (de) | 1997-05-02 | 2003-08-15 | Wyeth Corp | Pharamezeutische anwendbare sälze von 5.alpha.- pregn-16-en-3.beta.-ol-20-on 3-sulphate ester mit gestagen aktivität und verwendbar zur behandlung von störungen des zns |
| CA2289096A1 (en) * | 1997-05-02 | 1998-11-12 | Reinhold H. W. Bender | Pharmaceutically acceptable salts of 5alpha-pregnan-3beta, 16alpha-diol-20-one 3-sulfate useful as progestins and cns disorders |
| AU756001B2 (en) * | 1998-03-11 | 2003-01-02 | Umecrine Mood Ab | Epiallopregnanolone in the treatment of CNS disorders |
| IL142441A0 (en) | 1998-10-13 | 2002-03-10 | American Home Prod | Pregnane glucuronides |
| 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 CNA2009101459540A patent/CN101601675A/zh active Pending
- 2002-12-20 EP EP10183670.8A patent/EP2275109B1/en not_active Expired - Lifetime
- 2002-12-20 CN CNB028262751A patent/CN100518741C/zh not_active Expired - Fee Related
- 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 ES ES02793723T patent/ES2394639T3/es not_active Expired - Lifetime
- 2002-12-20 AU AU2002359202A patent/AU2002359202C1/en not_active Ceased
- 2002-12-20 US US10/499,214 patent/US7960367B2/en not_active Expired - Fee Related
- 2002-12-20 CN CNA2009101459536A patent/CN101601674A/zh active Pending
- 2002-12-20 CA CA2468248A patent/CA2468248C/en not_active Expired - Fee Related
- 2002-12-20 DK DK02793723.4T patent/DK1458399T3/da active
- 2002-12-20 JP JP2003559519A patent/JP2005519893A/ja active Pending
-
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
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111918657A (zh) * | 2018-04-05 | 2020-11-10 | 阿沙里那制药有限公司 | 用于治疗物质戒断障碍的gaba-a拮抗剂 |
Also Published As
| Publication number | Publication date |
|---|---|
| US7960367B2 (en) | 2011-06-14 |
| JP5289281B2 (ja) | 2013-09-11 |
| EP1458399A1 (en) | 2004-09-22 |
| AU2009201951A1 (en) | 2009-06-04 |
| WO2003059357A1 (en) | 2003-07-24 |
| EP1458399B1 (en) | 2012-08-08 |
| US8119619B2 (en) | 2012-02-21 |
| EP2275109B1 (en) | 2013-07-24 |
| CN101601674A (zh) | 2009-12-16 |
| AU2009201956B2 (en) | 2010-11-25 |
| AU2009201956A2 (en) | 2010-02-18 |
| CN1607954A (zh) | 2005-04-20 |
| US20050222099A1 (en) | 2005-10-06 |
| CA2468248A1 (en) | 2003-07-24 |
| DK1458399T3 (da) | 2012-11-12 |
| JP2005519893A (ja) | 2005-07-07 |
| EP2275109A3 (en) | 2011-10-12 |
| CA2468248C (en) | 2011-08-16 |
| AU2002359202B2 (en) | 2009-02-19 |
| JP2010065052A (ja) | 2010-03-25 |
| AU2002359202C1 (en) | 2011-03-31 |
| ES2394639T3 (es) | 2013-02-04 |
| AU2002359202A1 (en) | 2003-07-30 |
| SE0104423D0 (sv) | 2001-12-27 |
| US20110098259A1 (en) | 2011-04-28 |
| CN100518741C (zh) | 2009-07-29 |
| AU2009201956A1 (en) | 2009-06-11 |
| EP2275109A2 (en) | 2011-01-19 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN101601675A (zh) | 用于治疗中枢神经系统功能紊乱的孕烷类固醇 | |
| Behan et al. | Sex steroid hormones and the neural control of breathing | |
| Panay et al. | Progestogen intolerance and compliance with hormone replacement therapy in menopausal women | |
| Bäckström et al. | Ovarian steroid hormones: effects on mood, behaviour and brain excitability | |
| US8372824B2 (en) | GABA-steroid antagonists and their use for the treatment of CNS disorders | |
| REIFENSTEIN | The rationale for the use of anabolic steroids in controlling the adverse effects of corticoid hormones upon protein and osseous tissues | |
| JPH09501409A (ja) | ヒト視床下部機能の変化の神経化学イニシエーターとしてのアンドロスタンステロイド及びそれに関する医薬組成物及び方法 | |
| Korneyev | The role of the hypothalamic–pituitary–adrenocortical axis in memory-related effects of anxiolytics | |
| JP2001505574A (ja) | １７α−ジヒドロエキレニンを使用した神経退化および認識機能障害の予防方法 | |
| EP0565674B1 (en) | Method for memory enhancement and quality of life improvement | |
| Bass | Sex difference in the mechanisms that modulate social learning in male and female mice: The interaction between dorsal hippocampal d2-type dopamine receptors and gonadal steroid hormones | |
| RU2413516C2 (ru) | Гамк-стероидные антагонисты и их применение в лечении нарушений цнс | |
| CN101229174B (zh) | 一种含有盐酸依匹斯汀的抗过敏组合物 | |
| Panay et al. | Hormone replacement therapy and progestogen intolerance |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| ASS | Succession or assignment of patent right |
Owner name: MICPHONE RECOGNITION CO., LTD. Free format text: FORMER OWNER: MICPHONE JOINT-STOCK CO., LTD. Effective date: 20091023 |
|
| C06 | Publication | ||
| C41 | Transfer of patent application or patent right or utility model | ||
| PB01 | Publication | ||
| TA01 | Transfer of patent application right |
Effective date of registration: 20091023 Address after: Stockholm Applicant after: Mei Kefang identification Ltd Address before: Swedish chicken Applicant before: Umecrine AB |
|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C12 | Rejection of a patent application after its publication | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20091216 |