JP2018505898A5 - - Google Patents
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- JP2018505898A5 JP2018505898A5 JP2017543767A JP2017543767A JP2018505898A5 JP 2018505898 A5 JP2018505898 A5 JP 2018505898A5 JP 2017543767 A JP2017543767 A JP 2017543767A JP 2017543767 A JP2017543767 A JP 2017543767A JP 2018505898 A5 JP2018505898 A5 JP 2018505898A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- compound according
- composition
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 136
- 150000003839 salts Chemical class 0.000 claims description 74
- 229910052739 hydrogen Inorganic materials 0.000 claims description 60
- 125000003118 aryl group Chemical group 0.000 claims description 32
- 125000001072 heteroaryl group Chemical group 0.000 claims description 32
- 229910052736 halogen Inorganic materials 0.000 claims description 28
- 150000002367 halogens Chemical class 0.000 claims description 28
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 24
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 22
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 22
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 20
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims description 19
- 208000035475 disorder Diseases 0.000 claims description 17
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims description 16
- 125000006728 (C1-C6) alkynyl group Chemical group 0.000 claims description 16
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 206010002091 Anaesthesia Diseases 0.000 claims description 9
- 206010039897 Sedation Diseases 0.000 claims description 9
- 230000037005 anaesthesia Effects 0.000 claims description 9
- 230000036280 sedation Effects 0.000 claims description 9
- 206010010904 Convulsion Diseases 0.000 claims description 7
- 210000003169 central nervous system Anatomy 0.000 claims description 7
- 208000019022 Mood disease Diseases 0.000 claims description 5
- 208000016285 Movement disease Diseases 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 4
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical group NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims description 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 208000009575 Angelman syndrome Diseases 0.000 claims description 3
- 208000001914 Fragile X syndrome Diseases 0.000 claims description 3
- 208000026139 Memory disease Diseases 0.000 claims description 3
- 208000002193 Pain Diseases 0.000 claims description 3
- 208000006289 Rett Syndrome Diseases 0.000 claims description 3
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims description 3
- 208000009205 Tinnitus Diseases 0.000 claims description 3
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 3
- 206010048010 Withdrawal syndrome Diseases 0.000 claims description 3
- 208000029560 autism spectrum disease Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 230000001939 inductive effect Effects 0.000 claims description 3
- 230000036407 pain Effects 0.000 claims description 3
- 208000022821 personality disease Diseases 0.000 claims description 3
- 201000000980 schizophrenia Diseases 0.000 claims description 3
- 208000019116 sleep disease Diseases 0.000 claims description 3
- 238000001228 spectrum Methods 0.000 claims description 3
- 201000009032 substance abuse Diseases 0.000 claims description 3
- 231100000736 substance abuse Toxicity 0.000 claims description 3
- 208000011117 substance-related disease Diseases 0.000 claims description 3
- 231100000886 tinnitus Toxicity 0.000 claims description 3
- 230000009529 traumatic brain injury Effects 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 241000124008 Mammalia Species 0.000 claims description 2
- 206010044565 Tremor Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 230000004064 dysfunction Effects 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015706 neuroendocrine disease Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 208000020685 sleep-wake disease Diseases 0.000 claims description 2
- 239000008247 solid mixture Substances 0.000 claims description 2
- 230000002792 vascular Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 33
- -1 C 1 -C 6 alkyl (eg Chemical group 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 80
- 238000000034 method Methods 0.000 description 30
- 125000003545 alkoxy group Chemical group 0.000 description 21
- 0 CC(CC1)(C(CC2)C(CC3)C1C(CC1)(C(*)OC)C3CC1(C)O)C2C(CN([N+])/N=C(\C)/*)=O Chemical compound CC(CC1)(C(CC2)C(CC3)C1C(CC1)(C(*)OC)C3CC1(C)O)C2C(CN([N+])/N=C(\C)/*)=O 0.000 description 7
- 125000001188 haloalkyl group Chemical group 0.000 description 7
- VMQODZOLIAGGSE-AJMFIOBFSA-N CCCC([C@H](CC1)C(C)(CC2)[C@H]1C(C[n]1c(C)ncc1)=O)[C@H]2[C@](COC)(CC1)CC[C@@]1(C)O Chemical compound CCCC([C@H](CC1)C(C)(CC2)[C@H]1C(C[n]1c(C)ncc1)=O)[C@H]2[C@](COC)(CC1)CC[C@@]1(C)O VMQODZOLIAGGSE-AJMFIOBFSA-N 0.000 description 1
- GFVHFBHMYPQSBW-QIZQWJJASA-N CCOC[C@](CC1)([C@H](CC2)C[C@]1(C)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(C[n]1nnc2c1ccc(F)c2F)=O Chemical compound CCOC[C@](CC1)([C@H](CC2)C[C@]1(C)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(C[n]1nnc2c1ccc(F)c2F)=O GFVHFBHMYPQSBW-QIZQWJJASA-N 0.000 description 1
- ZNUSUHPTIFXGGE-QLSPYGMDSA-N CCOc1c[n](CC([C@@H](CC2)C(C)(CC3)[C@@H]2C(CC2)[C@H]3[C@@](COC)(CC3)[C@@H]2C[C@]3(C)O)=O)nc1 Chemical compound CCOc1c[n](CC([C@@H](CC2)C(C)(CC3)[C@@H]2C(CC2)[C@H]3[C@@](COC)(CC3)[C@@H]2C[C@]3(C)O)=O)nc1 ZNUSUHPTIFXGGE-QLSPYGMDSA-N 0.000 description 1
- PTWOVFXCPWFCPZ-UXHHELFZSA-N CC[NH+](c1c[n](CC([C@@H](CC2)[C@@](C)(CC3)[C@@H]2C(CC2)[C@H]3C(COC)(CC3)C2C[C@]3(C)O)=O)nc1)[O-] Chemical compound CC[NH+](c1c[n](CC([C@@H](CC2)[C@@](C)(CC3)[C@@H]2C(CC2)[C@H]3C(COC)(CC3)C2C[C@]3(C)O)=O)nc1)[O-] PTWOVFXCPWFCPZ-UXHHELFZSA-N 0.000 description 1
- QFSNZTKYNCYYFG-MRBBWTDOSA-N C[C@@](CC[C@H]1C2(C)CC[C@@](C)(C3)C1[C@H](COC)CC[C@@]3(C)O)(C(CC1)C(CN/C=C(\C=N)/N)O)[C@]21N Chemical compound C[C@@](CC[C@H]1C2(C)CC[C@@](C)(C3)C1[C@H](COC)CC[C@@]3(C)O)(C(CC1)C(CN/C=C(\C=N)/N)O)[C@]21N QFSNZTKYNCYYFG-MRBBWTDOSA-N 0.000 description 1
- FKQAQJDAXUIGJZ-CFLHAHIFSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n](c1c2)nnc1ncc2Cl)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n](c1c2)nnc1ncc2Cl)=O FKQAQJDAXUIGJZ-CFLHAHIFSA-N 0.000 description 1
- CQERWFMVBUSUPZ-NJNSWNMJSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nc(cc(cc2)F)c2c1)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nc(cc(cc2)F)c2c1)=O CQERWFMVBUSUPZ-NJNSWNMJSA-N 0.000 description 1
- ZRDJOYYZXYBFCK-SKXUUBPOSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nc2c(F)cc(F)cc2n1)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nc2c(F)cc(F)cc2n1)=O ZRDJOYYZXYBFCK-SKXUUBPOSA-N 0.000 description 1
- SFYPYDOIEACSBV-CFLHAHIFSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nc2ncc(Cl)cc2n1)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nc2ncc(Cl)cc2n1)=O SFYPYDOIEACSBV-CFLHAHIFSA-N 0.000 description 1
- ZCZXKXRPDHXMNE-TXLWSPTFSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nnc(cc2)c1cc2Cl)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nnc(cc2)c1cc2Cl)=O ZCZXKXRPDHXMNE-TXLWSPTFSA-N 0.000 description 1
- CIYXWXIJFXRWRK-TXLWSPTFSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nnc2c1ccc(Cl)c2)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nnc2c1ccc(Cl)c2)=O CIYXWXIJFXRWRK-TXLWSPTFSA-N 0.000 description 1
- NWESTZPKTBDNON-CFLHAHIFSA-N C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nnc2cc(Cl)cnc12)=O Chemical compound C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1[C@@](COC)(CC1)[C@H]3C[C@]1(C)O)[C@H]2C(C[n]1nnc2cc(Cl)cnc12)=O NWESTZPKTBDNON-CFLHAHIFSA-N 0.000 description 1
- YDCMKTACEXKYAV-LLCFRCHKSA-N C[C@](CC1)([C@@H](CC2C3)C(CC4)[C@H]1[C@@](COC)(CC1)[C@@H]4C[C@]1(C)O)C23C(C[n]1ncc(C)c1)=O Chemical compound C[C@](CC1)([C@@H](CC2C3)C(CC4)[C@H]1[C@@](COC)(CC1)[C@@H]4C[C@]1(C)O)C23C(C[n]1ncc(C)c1)=O YDCMKTACEXKYAV-LLCFRCHKSA-N 0.000 description 1
- 239000003691 GABA modulator Substances 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021042532A JP7161558B2 (ja) | 2015-02-20 | 2021-03-16 | 神経刺激性ステロイド、組成物、およびその使用 |
| JP2022111940A JP2022137194A (ja) | 2015-02-20 | 2022-07-12 | 神経刺激性ステロイド、組成物、およびその使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562118884P | 2015-02-20 | 2015-02-20 | |
| US62/118,884 | 2015-02-20 | ||
| PCT/US2016/018748 WO2016134301A2 (en) | 2015-02-20 | 2016-02-19 | Neuroactive steroids, compositions, and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021042532A Division JP7161558B2 (ja) | 2015-02-20 | 2021-03-16 | 神経刺激性ステロイド、組成物、およびその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018505898A JP2018505898A (ja) | 2018-03-01 |
| JP2018505898A5 true JP2018505898A5 (enExample) | 2019-03-22 |
| JP6875996B2 JP6875996B2 (ja) | 2021-05-26 |
Family
ID=56692509
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017543767A Active JP6875996B2 (ja) | 2015-02-20 | 2016-02-19 | 神経刺激性ステロイド、組成物、およびその使用 |
| JP2021042532A Active JP7161558B2 (ja) | 2015-02-20 | 2021-03-16 | 神経刺激性ステロイド、組成物、およびその使用 |
| JP2022111940A Pending JP2022137194A (ja) | 2015-02-20 | 2022-07-12 | 神経刺激性ステロイド、組成物、およびその使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021042532A Active JP7161558B2 (ja) | 2015-02-20 | 2021-03-16 | 神経刺激性ステロイド、組成物、およびその使用 |
| JP2022111940A Pending JP2022137194A (ja) | 2015-02-20 | 2022-07-12 | 神経刺激性ステロイド、組成物、およびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (4) | US10329320B2 (enExample) |
| EP (2) | EP4155314A1 (enExample) |
| JP (3) | JP6875996B2 (enExample) |
| DK (1) | DK3258939T3 (enExample) |
| ES (1) | ES2935476T3 (enExample) |
| WO (1) | WO2016134301A2 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2766380B1 (en) | 2011-10-14 | 2019-04-24 | Sage Therapeutics, Inc. | 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof |
| MX2015002252A (es) | 2012-08-21 | 2015-07-21 | Sage Therapeutics Inc | Metodos para tratar epilepsia o estado de epilepsia. |
| MX362543B (es) | 2013-04-17 | 2019-01-24 | Sage Therapeutics Inc | Esteroides c21-n-pirazolilo 19-nor c3,3- disustituidos y metodos de uso de los mismos. |
| WO2014169831A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| RU2019126333A (ru) | 2013-04-17 | 2019-10-08 | Сейдж Терапьютикс, Инк. | 19-нор нейроактивные стероиды и способы их применения |
| SI3021852T1 (sl) | 2013-07-19 | 2021-07-30 | Sage Therapeutics, Inc. | Nevroaktivni steroidi, sestavki in uporabe le-teh |
| CN105579043B (zh) | 2013-08-23 | 2021-09-14 | 萨奇治疗股份有限公司 | 神经活性类固醇、组合物和其用途 |
| US10246482B2 (en) | 2014-06-18 | 2019-04-02 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| JOP20200195A1 (ar) | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| TW202426002A (zh) | 2014-10-16 | 2024-07-01 | 美商賽吉醫療公司 | 用於治療中樞神經系統(cns)病症之組合物及方法 |
| RS60642B1 (sr) | 2014-10-16 | 2020-09-30 | Sage Therapeutics Inc | Kompozicije i postupci za lečenje poremećaja cns-a |
| EP3719029A1 (en) | 2014-11-27 | 2020-10-07 | Sage Therapeutics, Inc. | Compositions for inducing sedation |
| DK3250210T3 (da) | 2015-01-26 | 2021-03-08 | Sage Therapeutics Inc | Sammensætninger og fremgangsmåder til behandling af cns-forstyrrelser |
| ES2935476T3 (es) * | 2015-02-20 | 2023-03-07 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones y usos de los mismos |
| EP3481844B1 (en) | 2016-07-11 | 2024-04-17 | Sage Therapeutics, Inc. | C7, c12, and c16 substituted neuroactive steroids and their methods of use |
| CN116162121A (zh) | 2016-07-11 | 2023-05-26 | 萨奇治疗股份有限公司 | C17、c20和c21取代的神经活性类固醇及其使用方法 |
| CN115974955A (zh) | 2016-08-23 | 2023-04-18 | 萨奇治疗股份有限公司 | 19-去甲c3,3-二取代的c21-n-吡唑基类固醇的晶体 |
| CN109666055A (zh) * | 2017-10-16 | 2019-04-23 | 张家口华健致远生物科技有限公司 | 调节中枢神经治疗抑郁症的化合物及其用途 |
| MA51046A (fr) * | 2017-12-08 | 2021-03-17 | Sage Therapeutics Inc | Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc |
| MA51315A (fr) | 2017-12-22 | 2020-10-28 | Sage Therapeutics Inc | Compositions et méthodes permettant de traiter des troubles du snc |
| EP3750909B1 (en) * | 2018-02-11 | 2025-03-05 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Steroid derivative regulators, method for preparing the same, and uses thereof |
| CN109503694A (zh) * | 2018-11-21 | 2019-03-22 | 苏州闻天医药科技有限公司 | 一种新型gabaa受体调节剂及其用途 |
| AU2019406803B2 (en) * | 2018-12-17 | 2025-04-24 | Intra-Cellular Therapies, Inc. | Organic compounds |
| US20220372067A1 (en) * | 2018-12-21 | 2022-11-24 | Sage Therapeutics, Inc. | 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof |
| WO2020150210A1 (en) * | 2019-01-14 | 2020-07-23 | Beijing Xuanyi Pharmasciences Co., Ltd. | Tetrazolone substituted steroids and use thereof |
| PH12021553005A1 (en) | 2019-05-31 | 2023-08-14 | Sage Therapeutics Inc | Neuroactive steroids and compositions thereof |
| TWI896548B (zh) | 2019-06-27 | 2025-09-11 | 美商賽吉醫療公司 | 用於治療cns病症之組合物及方法 |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| IL296645A (en) | 2020-03-25 | 2022-11-01 | Sage Therapeutics Inc | Use of agents for treatment of respiratory conditions |
Family Cites Families (114)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2856415A (en) | 1957-11-13 | 1958-10-14 | Searle & Co | 3,19-dihydroxy-5-androstene derivatives |
| FR1380417A (fr) | 1962-05-15 | 1964-12-04 | Roussel Uclaf | Nouveaux androstanyl-pyrazoles et procédé de préparation |
| US3206459A (en) | 1962-10-19 | 1965-09-14 | Syntex Corp | 10alpha-pregnan-19-ol derivatives |
| US3169134A (en) | 1963-03-21 | 1965-02-09 | Searle & Co | 2, 3-oxygenated-17alpha-methyl-5alpha-androstan-17beta-ols |
| BE754111A (fr) | 1969-07-29 | 1971-01-29 | Upjohn Co | Nouveaux 7alpha- et 7beta-methyl-3alpha,5alpha- cycloandrostanes et composes analogues 19-nor et leur procede de preparation |
| GB1434919A (en) | 1972-06-15 | 1976-05-12 | Glaxo Lab Ltd | 3alpha-hydroxy androstanes |
| GB1380246A (en) | 1970-12-17 | 1975-01-08 | Glaxo Lab Ltd | 3alpha-hydroxy-androstanes and esters thereof |
| US3943124A (en) | 1970-12-17 | 1976-03-09 | Gordon Hanley Phillipps | Chemical compounds |
| US3983111A (en) | 1972-05-05 | 1976-09-28 | Glaxo Laboratories Limited | Steroidal anaesthetics of the pregnane and 19-norpregnane series |
| GB1430942A (en) | 1972-05-05 | 1976-04-07 | Glaxo Lab Ltd | 21-substituted 3alpha-hydroxy pregnanes |
| GB1436324A (en) | 1972-05-12 | 1976-05-19 | Glaxo Lab Ltd | Anaesthetic 3alpha-hydroxy pregnanes |
| ES432106A1 (es) | 1973-11-30 | 1976-11-01 | Schering Ag | Procedimiento para la preparacion de d-homo-20-cetopregna- nos. |
| US4071625A (en) | 1974-05-13 | 1978-01-31 | Richardson-Merrell Inc. | 19-Oxygenated-5α-androstanes for the enhancement of libido |
| DE2438020A1 (de) | 1974-08-05 | 1976-02-26 | Schering Ag | 18-methyl-19-nor-20-keto-pregnane und verfahren zu ihrer herstellung |
| IL48628A0 (en) | 1974-12-23 | 1976-02-29 | Schering Ag | D-homo-20-keto-pregnanes and process for their manufactur |
| DE2526373C2 (de) | 1975-06-11 | 1983-11-10 | Schering AG, 1000 Berlin und 4709 Bergkamen | Verfahren zur Herstellung von Δ↑9↑↑(↑↑1↑↑1↑↑)↑-5α-20-Ketosteroiden |
| GB1570394A (en) | 1976-01-06 | 1980-07-02 | Glaxo Lab Ltd | 11-acyloxy-3-hydroxy steroids |
| US4192871A (en) | 1976-01-06 | 1980-03-11 | Glaxo Laboratories Limited | Chemical compounds |
| GB1581234A (en) | 1976-04-05 | 1980-12-10 | Glaxo Operations Ltd | 11a - amino - 3a - hydroxysteroids |
| DE2632677A1 (de) | 1976-07-16 | 1978-01-26 | Schering Ag | Verfahren zur herstellung von androstan-17-on-derivaten und deren verwendung |
| GB1581235A (en) | 1977-04-04 | 1980-12-10 | Glaxo Operations Ltd | 11a-amino-3a-hydroxy-steroids |
| US4389345A (en) | 1981-10-09 | 1983-06-21 | G.D. Searle & Co. | 3-Oxoestra-17-acetonitrile and unsaturated analogs |
| US4495102A (en) | 1982-09-03 | 1985-01-22 | G. D. Searle & Co. | Aminoalkyl steroids |
| US5232917A (en) | 1987-08-25 | 1993-08-03 | University Of Southern California | Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series |
| US5120723A (en) | 1987-08-25 | 1992-06-09 | University Of Southern California | Method, compositions, and compounds for modulating brain excitability |
| US5319115A (en) | 1987-08-25 | 1994-06-07 | Cocensys Inc. | Method for making 3α-hydroxy, 3β-substituted-pregnanes |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| WO1993005786A1 (en) | 1991-09-13 | 1993-04-01 | Cocensys, Inc. | Novel gabaa receptor with steroid binding sites |
| DE4232681C2 (de) | 1992-09-29 | 1994-11-24 | Sigma Tau Ind Farmaceuti | 17-Phenyl- und 17-Furyl-14beta,5alpha-androstan- und androsten- Derivate, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Zusammensetzung |
| AU698834B2 (en) | 1993-05-24 | 1998-11-12 | Purdue Pharma Ltd. | Methods and compositions for inducing sleep |
| EP0656365B1 (en) | 1993-12-02 | 1997-04-09 | Akzo Nobel N.V. | Substituted 2beta-morpholinoandrostane derivatives |
| CZ300694A3 (en) | 1993-12-02 | 1996-05-15 | Akzo Nobel Nv | Substituted 2beta-morpholinandrostane derivatives, process of their preparation, their use for preparing pharmaceutical preparations and pharmaceutical compositions containing thereof |
| EP1038880B1 (en) | 1994-02-14 | 2007-10-17 | Euro-Celtique S.A. | Androstanes and pregnanes for allosteric modulation of GABA receptor |
| 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 |
| AU3125695A (en) | 1994-07-21 | 1996-02-22 | Pharmacia & Upjohn Company | Neurologically active aminosteroids |
| NZ298567A (en) | 1994-11-23 | 2000-01-28 | Cocensys Inc | Androstane and pregnane derivatives, pharmaceutical compositions and methods of treatment |
| EP0837874B1 (en) | 1995-06-06 | 2004-12-15 | Euro-Celtique S.A. | Neuroactive steroids of the androstane and pregnane series |
| WO1998005337A1 (en) * | 1996-08-01 | 1998-02-12 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| US5994334A (en) | 1997-02-05 | 1999-11-30 | University Of Maryland | Androgen synthesis inhibitors |
| US5935545A (en) | 1997-07-11 | 1999-08-10 | E. I. Du Pont De Nemours And Company | Process for producing an aqueous solution comprising ferric chloride |
| EP1177206A1 (en) | 1999-04-29 | 2002-02-06 | Purdue Pharma Ltd. | 3alpha-hydroxy-3beta methoxymethyl-21-heterocycle substituted steroids with anaesthetic activity |
| US7018406B2 (en) | 1999-11-17 | 2006-03-28 | Corevalve Sa | Prosthetic valve for transluminal delivery |
| EP1172371B1 (en) | 2000-02-18 | 2005-06-08 | Taiho Pharmaceutical Company Limited | Process for the preparation of steroid derivatives |
| US6855836B2 (en) | 2000-10-26 | 2005-02-15 | Jenapharm Gmbh & Co. Kg | 17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds |
| ES2287184T3 (es) | 2000-11-03 | 2007-12-16 | Washington University | Estructuras aromaticas modificadas con sustituyentes hidroxi-, que tienen actividad citoprotectora. |
| GR1003861B (el) | 2000-12-29 | 2002-04-11 | Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa. | |
| ES2339450T3 (es) | 2003-03-24 | 2010-05-20 | Sterix Limited | Derivados de estrogenos como inhibidores de esteroide sulfatasa. |
| CA2527019A1 (en) | 2003-05-29 | 2005-01-06 | Washington University | Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally-related pentacyclic steroids |
| JP2007512344A (ja) | 2003-11-24 | 2007-05-17 | メルク エンド カムパニー インコーポレーテッド | エストロゲン受容体調節剤 |
| WO2005105822A2 (en) | 2004-04-23 | 2005-11-10 | Euro-Celtique S.A. | 3-alpha-hydroxy 21-n- heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof |
| US8604011B2 (en) | 2004-09-27 | 2013-12-10 | The Regents Of The University Of California | Therapy for treatment of chronic degenerative brain diseases and nervous system injury |
| EP2471536A1 (en) | 2004-09-29 | 2012-07-04 | Harbor BioSciences, Inc. | Steroid analogs and characterization and treatment methods |
| BRPI0612921A2 (pt) | 2005-06-09 | 2010-12-07 | Euro Celtique Sa | composições farmacêuticas de um esteróide neuroativo e métodos de uso do mesmo |
| US20090203658A1 (en) | 2007-01-08 | 2009-08-13 | Duke University | Neuroactive steroid compositions and methods of use therefor |
| DE102007027636A1 (de) | 2007-06-12 | 2008-12-18 | Bayer Schering Pharma Aktiengesellschaft | 17ß-Cyano-18a-homo-19-nor-androst-4-en-Derivat, dessen Verwendung und das Derivat enthaltende Arzneimittel |
| JP5663303B2 (ja) | 2007-06-15 | 2015-02-04 | リサーチ トライアングル インスティテュート | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
| GB0711948D0 (en) | 2007-06-20 | 2007-08-01 | Bionature E A Ltd | Neurosteriod compounds |
| CN101412742B (zh) | 2007-10-19 | 2013-07-31 | 天津金耀集团有限公司 | 一种抑制血管新生的硝酸酯药物 |
| US20090264443A1 (en) | 2008-04-18 | 2009-10-22 | David Helton | Treatment of organophosphate exposure with tetrahydroindolone arylpiperazine compounds |
| CN101624414B (zh) | 2008-07-07 | 2013-02-13 | 天津金耀集团有限公司 | 一种抑制血管新生的硝酸酯药物 |
| CZ2008434A3 (cs) | 2008-07-10 | 2009-12-09 | Ústav organické chemie a biochemie Akademie ved CR, v. v. i. | Pregnanové anionické slouceniny, zpusob jejich výroby a jejich použití |
| US20100120733A1 (en) | 2008-11-07 | 2010-05-13 | Auspex Pharmaceuticals, Inc. | Steroid modulators of glucocorticoid receptor |
| WO2011079047A1 (en) | 2009-12-23 | 2011-06-30 | Drugtech Corporation | Methods for reducing the occurrence of preterm delivery and other pregnancy-related conditions |
| AU2011284606A1 (en) | 2010-07-30 | 2013-03-14 | Pharmacellion Ltd | Compounds and methods for treating neoplasia |
| US20120214987A1 (en) | 2010-12-15 | 2012-08-23 | Yu Ge | Methods and compounds for preparing 3alpha-oxygen substituted steroids |
| EP2675822A4 (en) | 2011-02-15 | 2014-07-30 | Socpra Sciences Et Génie S E C | STEROID ALKALOIDS AND THEIR USE AS ANTIMICROBIAL AGENTS AGAINST MICROORGANISMS WITH ELECTRON TRANSPORT FAILURE AND AS MICROBIAL AGENT EXHAUSTERS AGAINST PATHOGENIC BACTERIA |
| CZ303443B6 (cs) | 2011-02-15 | 2012-09-12 | Ústav organické chemie a biochemie Akademie ved CR, v.v.i. | Deriváty pregnanolonu substituované v poloze 3alfa kationickou skupinou, zpusob jejich výroby, jejich použití a prostredek je obsahující |
| WO2012116290A2 (en) | 2011-02-25 | 2012-08-30 | Washington University | Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same |
| EP3296405B1 (en) | 2011-03-23 | 2019-10-09 | Etsuro Ito | Method and kit for super-high-sensitivity measurement of protein and nucleic acid, and novel enzyme substrate |
| WO2013019711A2 (en) | 2011-07-29 | 2013-02-07 | The Regents Of The University Of California | NOVEL 17β-HETEROARYL-SUBSTITUTED STEROIDS AS MODULATORS OF GABAA RECEPTORS |
| PT2753632T (pt) | 2011-09-08 | 2023-08-17 | Sage Therapeutics Inc | Esteróides neuroactivos, composições e respectivas utilizações |
| EP2766380B1 (en) * | 2011-10-14 | 2019-04-24 | Sage Therapeutics, Inc. | 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof |
| US20150175651A1 (en) | 2012-06-15 | 2015-06-25 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| CN111228278A (zh) | 2012-06-19 | 2020-06-05 | 英特塞普特医药品公司 | 奥贝胆酸的制备、用途和固体形式 |
| US20140050789A1 (en) | 2012-08-13 | 2014-02-20 | The Regents Of The University Of California | Mitigation of epileptic seizures by combination therapy using benzodiazepines and neurosteroids |
| WO2014058736A1 (en) | 2012-10-08 | 2014-04-17 | Washington University | Neuroactive 19-alkoxy-17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same |
| US9757391B2 (en) | 2012-11-09 | 2017-09-12 | Goodchild Investments Pty Ltd | Neuroactive steroids and their use to facilitate neuroprotection |
| SG11201504848QA (en) | 2012-12-18 | 2015-07-30 | Univ Washington | Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same |
| US8939545B2 (en) | 2012-12-20 | 2015-01-27 | Eastman Kodak Company | Inkjet printing with managed airflow for condensation control |
| WO2014108808A2 (en) | 2013-01-09 | 2014-07-17 | Henry James Lorne | Pharmaceutical formulations for the treatment and prevention of trauma-induced neuropathology and neurodegeneration |
| CA2831054C (en) | 2013-01-09 | 2016-08-30 | Sapna Life Sciences Corp. | Formulations, and methods for their use in treatment of neuropathology and neurodegeneration as a result of traumatic injury |
| GB201302368D0 (en) | 2013-02-11 | 2013-03-27 | Univ Bath | Compound |
| US9512170B2 (en) | 2013-03-01 | 2016-12-06 | Washington University | Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors |
| US9562026B2 (en) | 2013-03-14 | 2017-02-07 | Washington University | Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors |
| WO2014169831A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof |
| RU2019126333A (ru) | 2013-04-17 | 2019-10-08 | Сейдж Терапьютикс, Инк. | 19-нор нейроактивные стероиды и способы их применения |
| MX362543B (es) | 2013-04-17 | 2019-01-24 | Sage Therapeutics Inc | Esteroides c21-n-pirazolilo 19-nor c3,3- disustituidos y metodos de uso de los mismos. |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| SI3021852T1 (sl) | 2013-07-19 | 2021-07-30 | Sage Therapeutics, Inc. | Nevroaktivni steroidi, sestavki in uporabe le-teh |
| CN105579043B (zh) * | 2013-08-23 | 2021-09-14 | 萨奇治疗股份有限公司 | 神经活性类固醇、组合物和其用途 |
| EP4144746A1 (en) | 2014-05-29 | 2023-03-08 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions and uses thereof |
| US10246482B2 (en) * | 2014-06-18 | 2019-04-02 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| MA40498A (fr) | 2014-09-02 | 2021-05-19 | Texas A & M Univ Sys | Méthode de traitement de l'intoxication par organophosphates |
| TW202426002A (zh) | 2014-10-16 | 2024-07-01 | 美商賽吉醫療公司 | 用於治療中樞神經系統(cns)病症之組合物及方法 |
| RS60642B1 (sr) | 2014-10-16 | 2020-09-30 | Sage Therapeutics Inc | Kompozicije i postupci za lečenje poremećaja cns-a |
| EP3719029A1 (en) | 2014-11-27 | 2020-10-07 | Sage Therapeutics, Inc. | Compositions for inducing sedation |
| DK3250210T3 (da) | 2015-01-26 | 2021-03-08 | Sage Therapeutics Inc | Sammensætninger og fremgangsmåder til behandling af cns-forstyrrelser |
| CN105985396A (zh) | 2015-02-16 | 2016-10-05 | 苏州泽璟生物制药有限公司 | 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物 |
| ES2935476T3 (es) | 2015-02-20 | 2023-03-07 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones y usos de los mismos |
| UY36741A (es) | 2015-06-21 | 2016-12-30 | Prevacus Inc | Compuesto de esteroide c-20, sus composiciones y usos para tratar la lesión cerebral traumática (tbi), que incluye las conmociones cerebrales |
| JP2018526423A (ja) | 2015-09-08 | 2018-09-13 | ビューポイント セラピューティクス， インコーポレイテッド | 眼科疾患を処置するための化合物および製剤 |
| CN108135838A (zh) | 2015-10-16 | 2018-06-08 | 马瑞纳斯制药公司 | 包含纳米粒的可注射神经类固醇制剂 |
| US20200306262A1 (en) | 2015-11-20 | 2020-10-01 | Sage Therapeutics, Inc. | Compounds and methods of their use |
| RU2766155C2 (ru) | 2016-03-08 | 2022-02-08 | Сейдж Терапьютикс, Инк. | Нейроактивные стероиды, их композиции и применения |
| US10226550B2 (en) | 2016-03-11 | 2019-03-12 | Brigham Young University | Cationic steroidal antimicrobial compositions for the treatment of dermal tissue |
| EP3481844B1 (en) | 2016-07-11 | 2024-04-17 | Sage Therapeutics, Inc. | C7, c12, and c16 substituted neuroactive steroids and their methods of use |
| CN116162121A (zh) | 2016-07-11 | 2023-05-26 | 萨奇治疗股份有限公司 | C17、c20和c21取代的神经活性类固醇及其使用方法 |
| CN115974955A (zh) | 2016-08-23 | 2023-04-18 | 萨奇治疗股份有限公司 | 19-去甲c3,3-二取代的c21-n-吡唑基类固醇的晶体 |
| US10391105B2 (en) | 2016-09-09 | 2019-08-27 | Marinus Pharmaceuticals Inc. | Methods of treating certain depressive disorders and delirium tremens |
| CN108727453A (zh) | 2017-04-20 | 2018-11-02 | 华东理工大学 | 新型pd-1抑制剂及其应用 |
| WO2019018119A1 (en) | 2017-07-18 | 2019-01-24 | Pairnomix, Llc | METHODS FOR TREATING EPILEPSY AND DISORDERS ASSOCIATED WITH KCNTI |
| JP7196157B2 (ja) | 2017-08-31 | 2022-12-26 | 武田薬品工業株式会社 | Ｃｎｓ状態の治療 |
| IL303250A (en) | 2017-09-07 | 2023-07-01 | Sage Therapeutics Inc | Neuroactive steroids and their methods of use |
| WO2019094724A1 (en) | 2017-11-10 | 2019-05-16 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treating genetic epileptic disoders |
-
2016
- 2016-02-19 ES ES16753177T patent/ES2935476T3/es active Active
- 2016-02-19 WO PCT/US2016/018748 patent/WO2016134301A2/en not_active Ceased
- 2016-02-19 JP JP2017543767A patent/JP6875996B2/ja active Active
- 2016-02-19 US US15/552,201 patent/US10329320B2/en active Active
- 2016-02-19 EP EP22193689.1A patent/EP4155314A1/en active Pending
- 2016-02-19 EP EP16753177.1A patent/EP3258939B1/en active Active
- 2016-02-19 DK DK16753177.1T patent/DK3258939T3/da active
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2019
- 2019-04-30 US US16/399,529 patent/US11124538B2/en active Active
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2021
- 2021-01-08 US US17/144,302 patent/US20210347812A1/en not_active Abandoned
- 2021-03-16 JP JP2021042532A patent/JP7161558B2/ja active Active
-
2022
- 2022-07-12 JP JP2022111940A patent/JP2022137194A/ja active Pending
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2023
- 2023-07-10 US US18/349,218 patent/US20240025942A1/en active Pending
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