JP2019529495A5 - - Google Patents
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- JP2019529495A5 JP2019529495A5 JP2019517289A JP2019517289A JP2019529495A5 JP 2019529495 A5 JP2019529495 A5 JP 2019529495A5 JP 2019517289 A JP2019517289 A JP 2019517289A JP 2019517289 A JP2019517289 A JP 2019517289A JP 2019529495 A5 JP2019529495 A5 JP 2019529495A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- formula
- hydrogen
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 291
- 125000000217 alkyl group Chemical group 0.000 claims description 190
- 229910052739 hydrogen Inorganic materials 0.000 claims description 124
- 239000001257 hydrogen Substances 0.000 claims description 124
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 111
- 208000035475 disorder Diseases 0.000 claims description 96
- 150000003839 salts Chemical class 0.000 claims description 71
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 60
- 125000003342 alkenyl group Chemical group 0.000 claims description 50
- 125000000304 alkynyl group Chemical group 0.000 claims description 50
- 150000002431 hydrogen Chemical group 0.000 claims description 46
- 229910052799 carbon Inorganic materials 0.000 claims description 38
- 125000004432 carbon atom Chemical group C* 0.000 claims description 38
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 36
- 239000008194 pharmaceutical composition Substances 0.000 claims description 27
- 208000002193 Pain Diseases 0.000 claims description 24
- 125000003118 aryl group Chemical group 0.000 claims description 24
- 125000001072 heteroaryl group Chemical group 0.000 claims description 24
- 125000004043 oxo group Chemical group O=* 0.000 claims description 22
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 18
- 229930182558 Sterol Natural products 0.000 claims description 18
- 230000015572 biosynthetic process Effects 0.000 claims description 18
- 230000002496 gastric effect Effects 0.000 claims description 18
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 18
- 235000003702 sterols Nutrition 0.000 claims description 18
- 238000003786 synthesis reaction Methods 0.000 claims description 18
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 16
- 125000001188 haloalkyl group Chemical group 0.000 claims description 16
- 208000014617 hemorrhoid Diseases 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 16
- 208000028017 Psychotic disease Diseases 0.000 claims description 15
- 201000010099 disease Diseases 0.000 claims description 15
- 230000002265 prevention Effects 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 13
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 12
- 208000011231 Crohn disease Diseases 0.000 claims description 12
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 12
- 210000003169 central nervous system Anatomy 0.000 claims description 12
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 12
- 201000000980 schizophrenia Diseases 0.000 claims description 12
- 150000003432 sterols Chemical class 0.000 claims description 12
- 208000000094 Chronic Pain Diseases 0.000 claims description 9
- 230000001154 acute effect Effects 0.000 claims description 9
- 208000005298 acute pain Diseases 0.000 claims description 9
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims description 8
- 125000001475 halogen functional group Chemical group 0.000 claims description 8
- 208000016583 Anus disease Diseases 0.000 claims description 7
- 208000024827 Alzheimer disease Diseases 0.000 claims description 6
- 206010002091 Anaesthesia Diseases 0.000 claims description 6
- 206010048946 Anal abscess Diseases 0.000 claims description 6
- 206010002556 Ankylosing Spondylitis Diseases 0.000 claims description 6
- 208000008958 Anti-N-Methyl-D-Aspartate Receptor Encephalitis Diseases 0.000 claims description 6
- 208000019901 Anxiety disease Diseases 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 208000020925 Bipolar disease Diseases 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010010144 Completed suicide Diseases 0.000 claims description 6
- 208000024581 Compulsive Personality disease Diseases 0.000 claims description 6
- 206010010774 Constipation Diseases 0.000 claims description 6
- 206010012289 Dementia Diseases 0.000 claims description 6
- 208000030814 Eating disease Diseases 0.000 claims description 6
- 206010072378 Encephalitis autoimmune Diseases 0.000 claims description 6
- 208000019454 Feeding and Eating 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
- 208000016285 Movement disease Diseases 0.000 claims description 6
- 208000032580 NMDA receptor encephalitis 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
- 201000009916 Postpartum depression 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
- 208000004680 Rectal Fistula Diseases 0.000 claims description 6
- 102100030681 SH3 and multiple ankyrin repeat domains protein 3 Human genes 0.000 claims description 6
- 101710101741 SH3 and multiple ankyrin repeat domains protein 3 Proteins 0.000 claims description 6
- 206010039897 Sedation Diseases 0.000 claims description 6
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 6
- 206010041247 Social fear Diseases 0.000 claims description 6
- 208000006011 Stroke Diseases 0.000 claims description 6
- 208000009205 Tinnitus Diseases 0.000 claims description 6
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 6
- 230000006978 adaptation Effects 0.000 claims description 6
- 230000037005 anaesthesia Effects 0.000 claims description 6
- 206010002156 anal fistula Diseases 0.000 claims description 6
- 208000029188 anti-NMDA receptor encephalitis Diseases 0.000 claims description 6
- 208000029560 autism spectrum disease Diseases 0.000 claims description 6
- 201000011510 cancer Diseases 0.000 claims description 6
- 208000010877 cognitive disease Diseases 0.000 claims description 6
- 208000029742 colonic neoplasm Diseases 0.000 claims description 6
- 206010012601 diabetes mellitus Diseases 0.000 claims description 6
- 235000014632 disordered eating Nutrition 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 6
- 208000024732 dysthymic disease Diseases 0.000 claims description 6
- 206010015037 epilepsy Diseases 0.000 claims description 6
- 230000001037 epileptic effect Effects 0.000 claims description 6
- 230000001939 inductive effect Effects 0.000 claims description 6
- 206010022437 insomnia Diseases 0.000 claims description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 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
- 230000035772 mutation Effects 0.000 claims description 6
- 230000036407 pain Effects 0.000 claims description 6
- 230000002085 persistent effect Effects 0.000 claims description 6
- 208000022821 personality disease Diseases 0.000 claims description 6
- 208000014081 polyp of colon Diseases 0.000 claims description 6
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 6
- 102000004169 proteins and genes Human genes 0.000 claims description 6
- 108090000623 proteins and genes Proteins 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 230000036280 sedation Effects 0.000 claims description 6
- 208000019116 sleep disease Diseases 0.000 claims description 6
- 125000002328 sterol group Chemical group 0.000 claims description 6
- 208000011117 substance-related disease Diseases 0.000 claims description 6
- 208000011580 syndromic disease Diseases 0.000 claims description 6
- 230000009529 traumatic brain injury Effects 0.000 claims description 6
- 208000029028 brain injury Diseases 0.000 claims description 3
- 206010009887 colitis Diseases 0.000 claims description 3
- 230000002996 emotional effect Effects 0.000 claims description 3
- 208000007386 hepatic encephalopathy Diseases 0.000 claims description 3
- 230000000394 mitotic effect Effects 0.000 claims description 3
- 208000009999 tuberous sclerosis Diseases 0.000 claims description 3
- OZUCXGWYZVDFOU-UHFFFAOYSA-N 2-(diethylamino)ethyl 6-hydroxy-4,7-dimethoxy-1-benzofuran-5-carboxylate;hydrochloride Chemical compound [Cl-].CC[NH+](CC)CCOC(=O)C1=C(O)C(OC)=C2OC=CC2=C1OC OZUCXGWYZVDFOU-UHFFFAOYSA-N 0.000 claims description 2
- JCSGAUKCDAVARS-SOUFLCLCSA-N chembl2106517 Chemical compound C1([C@@H](O)[C@H]2C3)=CC=CC(O)=C1C(=O)C2=C(O)[C@@]1(O)[C@@H]3[C@H](N(C)C)C(O)=C(C(N)=O)C1=O JCSGAUKCDAVARS-SOUFLCLCSA-N 0.000 claims description 2
- -1 -OR C Chemical group 0.000 claims 4
- 206010002153 Anal fissure Diseases 0.000 claims 1
- 206010011878 Deafness Diseases 0.000 claims 1
- 208000009531 Fissure in Ano Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 230000001771 impaired effect Effects 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 0 CC(C[C@@](C)[C@@](CC1)C2(C)[C@@]1C1C(C)(*)C=C(C[C@](*)(CC3)O)[C@@]3(C)[C@]1CC2)C(C)C(C(*)(*)O)=C Chemical compound CC(C[C@@](C)[C@@](CC1)C2(C)[C@@]1C1C(C)(*)C=C(C[C@](*)(CC3)O)[C@@]3(C)[C@]1CC2)C(C)C(C(*)(*)O)=C 0.000 description 85
- 238000000034 method Methods 0.000 description 63
- 208000034693 Laceration Diseases 0.000 description 5
- 208000016354 hearing loss disease Diseases 0.000 description 5
- 206010047571 Visual impairment Diseases 0.000 description 4
- 208000029257 vision disease Diseases 0.000 description 4
- 230000004393 visual impairment Effects 0.000 description 4
- 208000014644 Brain disease Diseases 0.000 description 3
- 208000018152 Cerebral disease Diseases 0.000 description 3
- 208000032274 Encephalopathy Diseases 0.000 description 3
- 230000008993 bowel inflammation Effects 0.000 description 3
- 210000004185 liver Anatomy 0.000 description 3
- 230000001314 paroxysmal effect Effects 0.000 description 3
- 230000000069 prophylactic effect Effects 0.000 description 3
- 230000001568 sexual effect Effects 0.000 description 3
- 201000007772 internal hemorrhoid Diseases 0.000 description 2
- 230000003449 preventive effect Effects 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000006735 deficit Effects 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022003714A JP2022036260A (ja) | 2016-09-30 | 2022-01-13 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
| JP2024041201A JP2024069502A (ja) | 2016-09-30 | 2024-03-15 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662402797P | 2016-09-30 | 2016-09-30 | |
| US201662402789P | 2016-09-30 | 2016-09-30 | |
| US62/402,797 | 2016-09-30 | ||
| US62/402,789 | 2016-09-30 | ||
| PCT/US2017/054657 WO2018064649A1 (en) | 2016-09-30 | 2017-09-30 | C7 substituted oxysterols and methods as nmda modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022003714A Division JP2022036260A (ja) | 2016-09-30 | 2022-01-13 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019529495A JP2019529495A (ja) | 2019-10-17 |
| JP2019529495A5 true JP2019529495A5 (https=) | 2020-11-12 |
| JP7149266B2 JP7149266B2 (ja) | 2022-10-06 |
Family
ID=60117790
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517289A Active JP7149266B2 (ja) | 2016-09-30 | 2017-09-30 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
| JP2022003714A Withdrawn JP2022036260A (ja) | 2016-09-30 | 2022-01-13 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
| JP2024041201A Pending JP2024069502A (ja) | 2016-09-30 | 2024-03-15 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022003714A Withdrawn JP2022036260A (ja) | 2016-09-30 | 2022-01-13 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
| JP2024041201A Pending JP2024069502A (ja) | 2016-09-30 | 2024-03-15 | Ｃ７置換オキシステロールおよびｎｍｄａモジュレーターとしての方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (4) | US11149056B2 (https=) |
| EP (1) | EP3519422B1 (https=) |
| JP (3) | JP7149266B2 (https=) |
| CN (3) | CN115850361B (https=) |
| AU (1) | AU2017337121B2 (https=) |
| CA (1) | CA3038900A1 (https=) |
| ES (1) | ES2935057T3 (https=) |
| MA (1) | MA46351A (https=) |
| MX (1) | MX392270B (https=) |
| PT (1) | PT3519422T (https=) |
| WO (1) | WO2018064649A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20230747T1 (hr) | 2011-09-08 | 2024-01-05 | Sage Therapeutics, Inc. | Neuroaktivni steroidi, pripravci i njihova uporaba |
| SMT201800657T1 (it) | 2013-03-13 | 2019-01-11 | Sage Therapeutics Inc | Steroidi neuroattivi e loro metodi di utilizzo |
| WO2015195967A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| PL3319611T3 (pl) | 2015-07-06 | 2021-07-12 | Sage Therapeutics, Inc. | Oksysterole i sposoby ich stosowania |
| MX382122B (es) | 2015-07-06 | 2025-03-13 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| EP3436022B1 (en) | 2016-04-01 | 2022-03-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| WO2018009867A1 (en) | 2016-07-07 | 2018-01-11 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| PT3519422T (pt) | 2016-09-30 | 2022-12-05 | Sage Therapeutics Inc | Oxisteróis substituídos em c7 e métodos como moduladores nmda |
| CA3041088C (en) | 2016-10-18 | 2024-05-21 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| DK4105223T3 (da) | 2016-10-18 | 2025-07-07 | Sage Therapeutics Inc | Oxysteroler og fremgangsmåder til anvendelse deraf |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| IL308273A (en) * | 2021-05-04 | 2024-01-01 | Sage Therapeutics Inc | Neuroactive steroids for the treatment of mild cognitive impairment associated with Parkinson's disease |
| EP4405370A1 (en) * | 2021-09-22 | 2024-07-31 | Sage Therapeutics, Inc. | Deuterated positive nmda-modulating compounds and methods of use thereof |
| EP4671260A3 (en) * | 2024-06-28 | 2026-03-04 | Industriale Chimica S.r.l. | Process for the preparation of (3-beta,24s)-25,25,25-trifluoro-3-methyl-26,27-dinorergost-5-ene-3,24-diol |
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2017
- 2017-09-30 PT PT177847704T patent/PT3519422T/pt unknown
- 2017-09-30 CN CN202211226669.3A patent/CN115850361B/zh active Active
- 2017-09-30 CA CA3038900A patent/CA3038900A1/en active Pending
- 2017-09-30 JP JP2019517289A patent/JP7149266B2/ja active Active
- 2017-09-30 MX MX2019003724A patent/MX392270B/es unknown
- 2017-09-30 EP EP17784770.4A patent/EP3519422B1/en active Active
- 2017-09-30 WO PCT/US2017/054657 patent/WO2018064649A1/en not_active Ceased
- 2017-09-30 CN CN201780072617.6A patent/CN110023323A/zh active Pending
- 2017-09-30 AU AU2017337121A patent/AU2017337121B2/en active Active
- 2017-09-30 CN CN202511041222.2A patent/CN121085986A/zh active Pending
- 2017-09-30 US US16/338,315 patent/US11149056B2/en active Active
- 2017-09-30 MA MA046351A patent/MA46351A/fr unknown
- 2017-09-30 ES ES17784770T patent/ES2935057T3/es active Active
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2021
- 2021-09-15 US US17/476,153 patent/US11926646B2/en active Active
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- 2022-01-13 JP JP2022003714A patent/JP2022036260A/ja not_active Withdrawn
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- 2025-05-13 US US19/206,490 patent/US20250388622A1/en active Pending
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