JP2019532078A5 - - Google Patents
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- JP2019532078A5 JP2019532078A5 JP2019520736A JP2019520736A JP2019532078A5 JP 2019532078 A5 JP2019532078 A5 JP 2019532078A5 JP 2019520736 A JP2019520736 A JP 2019520736A JP 2019520736 A JP2019520736 A JP 2019520736A JP 2019532078 A5 JP2019532078 A5 JP 2019532078A5
- Authority
- JP
- Japan
- Prior art keywords
- hydrogen
- unsubstituted
- substituted
- alkyl
- pharmaceutically acceptable
- 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 329
- 229910052739 hydrogen Inorganic materials 0.000 claims description 213
- 239000001257 hydrogen Substances 0.000 claims description 213
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 118
- 125000000217 alkyl group Chemical group 0.000 claims description 109
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 96
- 208000035475 disorder Diseases 0.000 claims description 90
- 150000002431 hydrogen Chemical class 0.000 claims description 90
- 150000003839 salts Chemical class 0.000 claims description 76
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 46
- 150000001721 carbon Chemical group 0.000 claims description 38
- 229910052799 carbon Inorganic materials 0.000 claims description 38
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 29
- 125000000623 heterocyclic group Chemical group 0.000 claims description 26
- 125000003118 aryl group Chemical group 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 24
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 22
- 230000002496 gastric effect Effects 0.000 claims description 22
- 239000008194 pharmaceutical composition Substances 0.000 claims description 22
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 21
- 125000001475 halogen functional group Chemical group 0.000 claims description 21
- 125000004043 oxo group Chemical group O=* 0.000 claims description 20
- 208000002193 Pain Diseases 0.000 claims description 18
- 229930182558 Sterol Natural products 0.000 claims description 17
- 230000015572 biosynthetic process Effects 0.000 claims description 17
- 235000003702 sterols Nutrition 0.000 claims description 17
- 238000003786 synthesis reaction Methods 0.000 claims description 17
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 16
- 208000028017 Psychotic disease Diseases 0.000 claims description 16
- 210000003169 central nervous system Anatomy 0.000 claims description 15
- 125000001188 haloalkyl group Chemical group 0.000 claims description 15
- 239000000203 mixture Substances 0.000 claims description 14
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 14
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 14
- 230000002265 prevention Effects 0.000 claims description 13
- 150000003432 sterols Chemical class 0.000 claims description 12
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 11
- 208000011231 Crohn disease Diseases 0.000 claims description 11
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 11
- 208000012826 adjustment disease Diseases 0.000 claims description 11
- 125000004432 carbon atom Chemical group C* 0.000 claims description 11
- 125000004076 pyridyl group Chemical group 0.000 claims description 10
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 9
- 208000010877 cognitive disease Diseases 0.000 claims description 8
- 208000016285 Movement disease Diseases 0.000 claims description 7
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 7
- 208000022821 personality disease Diseases 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 7
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 6
- 208000016583 Anus disease Diseases 0.000 claims description 6
- 208000019901 Anxiety disease Diseases 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 6
- 208000023105 Huntington disease Diseases 0.000 claims description 6
- 208000003456 Juvenile Arthritis Diseases 0.000 claims description 6
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims description 6
- 208000019022 Mood disease Diseases 0.000 claims description 6
- 206010028980 Neoplasm Diseases 0.000 claims description 6
- 208000029726 Neurodevelopmental disease Diseases 0.000 claims description 6
- 208000018737 Parkinson disease Diseases 0.000 claims description 6
- 201000004681 Psoriasis Diseases 0.000 claims description 6
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims description 6
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims description 6
- 208000009205 Tinnitus Diseases 0.000 claims description 6
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 6
- 208000029560 autism spectrum disease Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 201000010099 disease Diseases 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 6
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 6
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims description 6
- 208000030159 metabolic disease Diseases 0.000 claims description 6
- 201000006417 multiple sclerosis Diseases 0.000 claims description 6
- 230000001314 paroxysmal effect Effects 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 201000000980 schizophrenia Diseases 0.000 claims description 6
- 208000011117 substance-related disease Diseases 0.000 claims description 6
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 6
- 230000009529 traumatic brain injury Effects 0.000 claims description 6
- 208000014644 Brain disease Diseases 0.000 claims description 5
- 206010009887 colitis Diseases 0.000 claims description 5
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 4
- 206010047571 Visual impairment Diseases 0.000 claims description 4
- 208000029257 vision disease Diseases 0.000 claims description 4
- 230000004393 visual impairment Effects 0.000 claims description 4
- LVZWSLJZHVFIQJ-UHFFFAOYSA-N Cyclopropane Chemical compound C1CC1 LVZWSLJZHVFIQJ-UHFFFAOYSA-N 0.000 claims description 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 2
- 206010011878 Deafness Diseases 0.000 claims 1
- 208000018460 Feeding disease Diseases 0.000 claims 1
- 208000018459 dissociative disease Diseases 0.000 claims 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 1
- 208000022131 polyp of large intestine Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 59
- 125000005843 halogen group Chemical group 0.000 description 20
- 208000014617 hemorrhoid Diseases 0.000 description 14
- 206010015037 epilepsy Diseases 0.000 description 10
- 208000002551 irritable bowel syndrome Diseases 0.000 description 10
- 208000000094 Chronic Pain Diseases 0.000 description 6
- 230000001154 acute effect Effects 0.000 description 6
- 208000005298 acute pain Diseases 0.000 description 6
- 206010048946 Anal abscess Diseases 0.000 description 5
- 208000008958 Anti-N-Methyl-D-Aspartate Receptor Encephalitis Diseases 0.000 description 5
- 208000020925 Bipolar disease Diseases 0.000 description 5
- 206010009944 Colon cancer Diseases 0.000 description 5
- 206010010144 Completed suicide Diseases 0.000 description 5
- 206010010774 Constipation Diseases 0.000 description 5
- 206010012289 Dementia Diseases 0.000 description 5
- 208000030814 Eating disease Diseases 0.000 description 5
- 206010072378 Encephalitis autoimmune Diseases 0.000 description 5
- 208000017605 Hodgkin disease nodular sclerosis Diseases 0.000 description 5
- 208000034693 Laceration Diseases 0.000 description 5
- 208000032580 NMDA receptor encephalitis Diseases 0.000 description 5
- 201000009916 Postpartum depression Diseases 0.000 description 5
- 208000004680 Rectal Fistula Diseases 0.000 description 5
- 102100030681 SH3 and multiple ankyrin repeat domains protein 3 Human genes 0.000 description 5
- 101710101741 SH3 and multiple ankyrin repeat domains protein 3 Proteins 0.000 description 5
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 5
- 206010041247 Social fear Diseases 0.000 description 5
- 206010002156 anal fistula Diseases 0.000 description 5
- 208000029188 anti-NMDA receptor encephalitis Diseases 0.000 description 5
- 208000029742 colonic neoplasm Diseases 0.000 description 5
- 235000014632 disordered eating Nutrition 0.000 description 5
- 208000016354 hearing loss disease Diseases 0.000 description 5
- 206010022437 insomnia Diseases 0.000 description 5
- 230000002085 persistent effect Effects 0.000 description 5
- 208000014081 polyp of colon Diseases 0.000 description 5
- 208000028173 post-traumatic stress disease Diseases 0.000 description 5
- 102000004169 proteins and genes Human genes 0.000 description 5
- 108090000623 proteins and genes Proteins 0.000 description 5
- 208000019116 sleep disease Diseases 0.000 description 5
- 125000002328 sterol group Chemical group 0.000 description 5
- 208000011580 syndromic disease Diseases 0.000 description 5
- 208000024581 Compulsive Personality disease Diseases 0.000 description 4
- 208000007386 hepatic encephalopathy Diseases 0.000 description 4
- 230000035772 mutation Effects 0.000 description 4
- 230000000394 mitotic effect Effects 0.000 description 3
- 230000006735 deficit Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 230000000698 schizophrenic effect Effects 0.000 description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 description 1
- 208000018152 Cerebral disease Diseases 0.000 description 1
- 241000004297 Draba Species 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 238000013400 design of experiment Methods 0.000 description 1
- 230000002440 hepatic effect Effects 0.000 description 1
- 201000007772 internal hemorrhoid Diseases 0.000 description 1
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022039315A JP2022069555A (ja) | 2016-10-18 | 2022-03-14 | オキシステロールおよびその使用方法 |
| JP2024009591A JP2024028631A (ja) | 2016-10-18 | 2024-01-25 | オキシステロールおよびその使用方法 |
| JP2025097029A JP2025123284A (ja) | 2016-10-18 | 2025-06-10 | オキシステロールおよびその使用方法 |
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662409772P | 2016-10-18 | 2016-10-18 | |
| US201662409767P | 2016-10-18 | 2016-10-18 | |
| US201662409774P | 2016-10-18 | 2016-10-18 | |
| US201662409764P | 2016-10-18 | 2016-10-18 | |
| US201662409761P | 2016-10-18 | 2016-10-18 | |
| US62/409,764 | 2016-10-18 | ||
| US62/409,774 | 2016-10-18 | ||
| US62/409,761 | 2016-10-18 | ||
| US62/409,772 | 2016-10-18 | ||
| US62/409,767 | 2016-10-18 | ||
| PCT/US2017/057277 WO2018075699A1 (en) | 2016-10-18 | 2017-10-18 | Oxysterols and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022039315A Division JP2022069555A (ja) | 2016-10-18 | 2022-03-14 | オキシステロールおよびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019532078A JP2019532078A (ja) | 2019-11-07 |
| JP2019532078A5 true JP2019532078A5 (enExample) | 2020-11-26 |
| JP7118957B2 JP7118957B2 (ja) | 2022-08-16 |
Family
ID=60263023
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019520736A Active JP7118957B2 (ja) | 2016-10-18 | 2017-10-18 | オキシステロールおよびその使用方法 |
| JP2022039315A Withdrawn JP2022069555A (ja) | 2016-10-18 | 2022-03-14 | オキシステロールおよびその使用方法 |
| JP2024009591A Pending JP2024028631A (ja) | 2016-10-18 | 2024-01-25 | オキシステロールおよびその使用方法 |
| JP2025097029A Pending JP2025123284A (ja) | 2016-10-18 | 2025-06-10 | オキシステロールおよびその使用方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022039315A Withdrawn JP2022069555A (ja) | 2016-10-18 | 2022-03-14 | オキシステロールおよびその使用方法 |
| JP2024009591A Pending JP2024028631A (ja) | 2016-10-18 | 2024-01-25 | オキシステロールおよびその使用方法 |
| JP2025097029A Pending JP2025123284A (ja) | 2016-10-18 | 2025-06-10 | オキシステロールおよびその使用方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (3) | US11149054B2 (enExample) |
| EP (2) | EP3529257B1 (enExample) |
| JP (4) | JP7118957B2 (enExample) |
| KR (2) | KR102583278B1 (enExample) |
| CN (4) | CN114478677B (enExample) |
| AU (3) | AU2017345400B2 (enExample) |
| BR (1) | BR112019008032A2 (enExample) |
| CA (2) | CA3041088C (enExample) |
| DK (1) | DK3529257T3 (enExample) |
| ES (1) | ES2952106T3 (enExample) |
| IL (2) | IL266093B2 (enExample) |
| MA (1) | MA46566A (enExample) |
| MX (4) | MX2019004578A (enExample) |
| RU (1) | RU2019115113A (enExample) |
| TW (3) | TWI815800B (enExample) |
| WO (1) | WO2018075699A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107936076B (zh) | 2011-09-08 | 2021-10-15 | 萨奇治疗股份有限公司 | 神经活性类固醇、组合物、及其用途 |
| AU2014243773B2 (en) | 2013-03-13 | 2018-12-13 | Sage Therapeutics, Inc. | Neuroactive steroids and methods of use thereof |
| US10259840B2 (en) | 2014-06-18 | 2019-04-16 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| CA2991214C (en) | 2015-07-06 | 2024-04-30 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US11117924B2 (en) | 2015-07-06 | 2021-09-14 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| MA44526A (fr) * | 2016-04-01 | 2021-06-02 | Sage Therapeutics Inc | Oxystérols et leurs méthodes d'utilisation |
| WO2017193046A1 (en) | 2016-05-06 | 2017-11-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| MA45598B1 (fr) | 2016-07-07 | 2021-09-30 | Sage Therapeutics Inc | Stéroles 24-hydroxylés substitués en position 11 pour le traitement des maladies liées au récepteur nmda |
| MA46351A (fr) | 2016-09-30 | 2021-06-02 | Sage Therapeutics Inc | Oxystérols substitués en c7 et procédés en tant que modulateurs nmda |
| RU2019115113A (ru) | 2016-10-18 | 2020-11-24 | Сейдж Терапьютикс, Инк. | Оксистеролы и способы их применения |
| US11111266B2 (en) | 2016-10-18 | 2021-09-07 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| WO2020260558A1 (en) | 2019-06-27 | 2020-12-30 | Phenex Pharmaceuticals Ag | 3-modified iso-/isoallo-lithocholic acid derivatives or their homo-analogs for preventing and treating clostridioides difficile-associated diseases |
| GB201913752D0 (en) | 2019-09-24 | 2019-11-06 | Syngenta Crop Protection Ag | Herbicidal compounds |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| GB201914277D0 (en) | 2019-10-03 | 2019-11-20 | Syngenta Crop Protection Ag | Herbicidal compounds |
| GB201917898D0 (en) | 2019-12-06 | 2020-01-22 | Syngenta Crop Protection Ag | Herbicidal compounds |
| US20230233580A1 (en) * | 2020-06-26 | 2023-07-27 | Durect Corporation | Use of oxygenated cholesterol sulfates for cancers and non-cancerous transformations related to epstein-barr virus |
| CA3223179A1 (en) | 2021-06-11 | 2022-12-15 | Sage Therapeutics, Inc. | Neuroactive steroid for the treatment of alzheimer's disease |
| JP2024534558A (ja) | 2021-09-22 | 2024-09-20 | セージ セラピューティクス， インコーポレイテッド | 重水素化ｎｍｄａ正調節化合物及びその使用方法 |
| 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 |
| EP4447953A1 (en) | 2021-12-13 | 2024-10-23 | Sage Therapeutics, Inc. | Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators |
| CN116143859A (zh) * | 2022-12-09 | 2023-05-23 | 江苏佳尔科药业集团股份有限公司 | 5α-孕甾-3,20-二酮的制备方法 |
| WO2025221731A1 (en) * | 2024-04-15 | 2025-10-23 | Sage Therapeutics, Inc. | Nmda receptor-modulating compounds and methods of use thereof |
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