JP2014520072A5 - - Google Patents
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- Publication number
- JP2014520072A5 JP2014520072A5 JP2014508130A JP2014508130A JP2014520072A5 JP 2014520072 A5 JP2014520072 A5 JP 2014520072A5 JP 2014508130 A JP2014508130 A JP 2014508130A JP 2014508130 A JP2014508130 A JP 2014508130A JP 2014520072 A5 JP2014520072 A5 JP 2014520072A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- group
- alkenyl
- hydrogen
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 26
- -1 cyano, amino, phenyl Chemical group 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 13
- GIBQQARAXHVEGD-BSOLPCOYSA-N rapastinel Chemical compound C[C@@H](O)[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)N[C@@H]([C@@H](C)O)C(N)=O)CCC1 GIBQQARAXHVEGD-BSOLPCOYSA-N 0.000 claims description 12
- 206010003805 Autism Diseases 0.000 claims description 7
- 208000020706 Autistic disease Diseases 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 108090000623 proteins and genes Proteins 0.000 claims description 4
- 230000003956 synaptic plasticity Effects 0.000 claims description 4
- 210000004027 cell Anatomy 0.000 claims description 3
- 102100035923 4-aminobutyrate aminotransferase, mitochondrial Human genes 0.000 claims description 2
- 102100039289 Glial fibrillary acidic protein Human genes 0.000 claims description 2
- 101710193519 Glial fibrillary acidic protein Proteins 0.000 claims description 2
- 102100029458 Glutamate receptor ionotropic, NMDA 2A Human genes 0.000 claims description 2
- 101001000686 Homo sapiens 4-aminobutyrate aminotransferase, mitochondrial Proteins 0.000 claims description 2
- 101001125242 Homo sapiens Glutamate receptor ionotropic, NMDA 2A Proteins 0.000 claims description 2
- 101000745167 Homo sapiens Neuronal acetylcholine receptor subunit alpha-4 Proteins 0.000 claims description 2
- 101000745175 Homo sapiens Neuronal acetylcholine receptor subunit alpha-5 Proteins 0.000 claims description 2
- 101001099423 Homo sapiens Proenkephalin-A Proteins 0.000 claims description 2
- 102100039909 Neuronal acetylcholine receptor subunit alpha-4 Human genes 0.000 claims description 2
- 102100039907 Neuronal acetylcholine receptor subunit alpha-5 Human genes 0.000 claims description 2
- 102100038931 Proenkephalin-A Human genes 0.000 claims description 2
- 102100024622 Proenkephalin-B Human genes 0.000 claims description 2
- 101100162976 Sus scrofa APOR gene Proteins 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 210000005046 glial fibrillary acidic protein Anatomy 0.000 claims description 2
- 108010074732 preproenkephalin Proteins 0.000 claims description 2
- WWJZWCUNLNYYAU-UHFFFAOYSA-N temephos Chemical group C1=CC(OP(=S)(OC)OC)=CC=C1SC1=CC=C(OP(=S)(OC)OC)C=C1 WWJZWCUNLNYYAU-UHFFFAOYSA-N 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 105
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 60
- 125000003342 alkenyl group Chemical group 0.000 claims 40
- 229910052739 hydrogen Inorganic materials 0.000 claims 40
- 239000001257 hydrogen Substances 0.000 claims 40
- 125000001424 substituent group Chemical group 0.000 claims 40
- 150000002431 hydrogen Chemical class 0.000 claims 30
- 125000003545 alkoxy group Chemical group 0.000 claims 25
- 229910052736 halogen Inorganic materials 0.000 claims 25
- 150000002367 halogens Chemical class 0.000 claims 25
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 25
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 10
- 150000001408 amides Chemical class 0.000 claims 10
- 150000001412 amines Chemical class 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 5
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 5
- 208000024891 symptom Diseases 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000006096 Attention Deficit Disorder with Hyperactivity Diseases 0.000 claims 2
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 2
- 206010012335 Dependence Diseases 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 208000001914 Fragile X syndrome Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000017442 Retinal disease Diseases 0.000 claims 2
- 206010038923 Retinopathy Diseases 0.000 claims 2
- 208000030507 AIDS Diseases 0.000 claims 1
- 208000000044 Amnesia Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 206010008027 Cerebellar atrophy Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 208000030990 Impulse-control disease Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000001089 Multiple system atrophy Diseases 0.000 claims 1
- 206010028570 Myelopathy Diseases 0.000 claims 1
- 206010057852 Nicotine dependence Diseases 0.000 claims 1
- 240000007817 Olea europaea Species 0.000 claims 1
- 208000003435 Optic Neuritis Diseases 0.000 claims 1
- 206010039897 Sedation Diseases 0.000 claims 1
- 208000025569 Tobacco Use disease Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 208000026911 Tuberous sclerosis complex Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 230000003542 behavioural effect Effects 0.000 claims 1
- 206010008129 cerebral palsy Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 1
- 230000003834 intracellular effect Effects 0.000 claims 1
- 238000010255 intramuscular injection Methods 0.000 claims 1
- 239000007927 intramuscular injection Substances 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 230000006984 memory degeneration Effects 0.000 claims 1
- 208000023060 memory loss Diseases 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 208000028173 post-traumatic stress disease Diseases 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 230000036280 sedation Effects 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000009999 tuberous sclerosis Diseases 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161479593P | 2011-04-27 | 2011-04-27 | |
| US61/479,593 | 2011-04-27 | ||
| US201161527744P | 2011-08-26 | 2011-08-26 | |
| US61/527,744 | 2011-08-26 | ||
| PCT/US2012/035547 WO2012149389A2 (en) | 2011-04-27 | 2012-04-27 | Methods of treating alzheimer's disease, huntington's disease, autism, or other disorders |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014520072A JP2014520072A (ja) | 2014-08-21 |
| JP2014520072A5 true JP2014520072A5 (enExample) | 2016-09-23 |
| JP6035326B2 JP6035326B2 (ja) | 2016-11-30 |
Family
ID=47073094
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014508130A Expired - Fee Related JP6035326B2 (ja) | 2011-04-27 | 2012-04-27 | アルツハイマー病、ハンチントン病、自閉症及びその他の疾患を治療する方法 |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US20140107037A1 (enExample) |
| EP (2) | EP3679931A3 (enExample) |
| JP (1) | JP6035326B2 (enExample) |
| KR (5) | KR20180095096A (enExample) |
| CN (2) | CN103974712A (enExample) |
| AU (1) | AU2012249397B2 (enExample) |
| BR (1) | BR112013027554A2 (enExample) |
| CA (1) | CA2834286A1 (enExample) |
| EA (2) | EA201790653A1 (enExample) |
| HK (1) | HK1258231A1 (enExample) |
| MX (1) | MX357761B (enExample) |
| SG (2) | SG10202010665YA (enExample) |
| WO (1) | WO2012149389A2 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2331571B1 (en) | 2008-09-18 | 2015-08-26 | Northwestern University | Nmda receptor modulators and uses thereof |
| KR101692275B1 (ko) | 2010-02-11 | 2017-01-04 | 노오쓰웨스턴 유니버시티 | ２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도 |
| RU2566821C2 (ru) | 2010-02-11 | 2015-10-27 | Нортвестерн Юниверсити | Модулятор nmda-рецептора со стабилизированной вторичной структурой и его применение |
| CN105408336B (zh) | 2013-01-29 | 2018-06-26 | 阿普廷伊克斯股份有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| BR112015018095A2 (pt) | 2013-01-29 | 2017-07-18 | Naurex Inc | moduladores de receptor nmda de espiro-lactama e usos dos mesmos |
| AU2014212487C1 (en) | 2013-01-29 | 2018-10-25 | Aptinyx, Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| WO2014120783A1 (en) | 2013-01-29 | 2014-08-07 | Naurex, Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| ES2618421T3 (es) | 2013-01-29 | 2017-06-21 | Aptinyx Inc. | Moduladores espiro-lactama del receptor NMDA y usos de los mismos |
| MX378668B (es) * | 2013-10-28 | 2025-03-10 | Naurex Inc | Profarmacos y moduladores de receptores nmda, sales y usos de estos. |
| US20160345855A1 (en) * | 2013-12-13 | 2016-12-01 | Northwestern University | Methods of treating brain disorders or identifying biomarkers related thereto |
| CN105327349A (zh) * | 2014-06-18 | 2016-02-17 | 上海翰森生物医药科技有限公司 | Nmda受体拮抗剂的医药用途及其药物组合物 |
| JP6688748B2 (ja) * | 2014-06-23 | 2020-04-28 | ノースウェスタン ユニバーシティ | 片頭痛の治療または改善方法 |
| EP3362080A1 (en) * | 2015-10-16 | 2018-08-22 | Northwestern University | Pharmaceutical combination of an atypical antipsychotic and an nmda modulator for the treatment of schizophrenia,bipolar disorder, cognitive impairment and major depressive disorder |
| WO2017201285A1 (en) | 2016-05-19 | 2017-11-23 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| AU2017267708B2 (en) | 2016-05-19 | 2020-02-20 | Aptinyx Inc. | Spiro-lactam NMDA receptor modulators and uses thereof |
| ES2972533T3 (es) | 2016-08-01 | 2024-06-13 | Tenacia Biotechnology Hong Kong Co Ltd | Moduladores del receptor de NMDA a base de espirolactama, y sus usos |
| AU2017306158B2 (en) | 2016-08-01 | 2021-10-14 | Aptinyx Inc. | Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof |
| EA201990424A1 (ru) | 2016-08-01 | 2019-08-30 | Аптиникс Инк. | Спиролактамовые модуляторы nmda-рецептора и их применение |
| WO2018026798A1 (en) | 2016-08-01 | 2018-02-08 | Aptinyx Inc. | Spiro-lactam nmda modulators and methods of using same |
| ES2973283T3 (es) | 2016-08-01 | 2024-06-19 | Tenacia Biotechnology Hong Kong Co Ltd | Moduladores de receptores de NMDA espirolactámicos y usos de los mismos |
| KR102761196B1 (ko) | 2018-01-31 | 2025-02-03 | 테나시아 바이오테크놀로지 (홍콩) 코., 리미티드 | 스피로-락탐 nmda 수용체 조정제 및 그의 용도 |
| US12012413B2 (en) | 2019-11-11 | 2024-06-18 | Tenacia Biotechnology (Hong Kong) Co., Limited | Methods of treating painful diabetic peripheral neuropathy |
| KR102415692B1 (ko) | 2020-09-01 | 2022-07-05 | 건국대학교 글로컬산학협력단 | 시냅스 불균형 조절에 의한 발달장애 예방, 개선 또는 치료용 조성물 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4086196A (en) | 1975-03-28 | 1978-04-25 | Armour Pharmaceutical Company | Parathyroid hormone |
| US5763393A (en) | 1996-05-17 | 1998-06-09 | Neurotherapeutics L.P. | Neuroactive peptides |
| GB0018272D0 (en) * | 2000-07-25 | 2000-09-13 | Vernalis Research Limited | Chemical compounds IV |
| EP1471909A4 (en) * | 2002-01-16 | 2007-07-25 | Endo Pharmaceuticals Inc | PHARMACEUTICAL COMPOSITION AND METHOD FOR THE TREATMENT OF DISEASES OF THE CENTRAL NERVOUS SYSTEM |
| US20060063707A1 (en) * | 2004-09-17 | 2006-03-23 | Lifelike Biomatic, Inc. | Compositions for enhancing memory and methods therefor |
| RS52471B (sr) * | 2005-03-24 | 2013-02-28 | Emory University | Režimi doziranja za lečenje traumatske povrede mozga progesteronom |
| US9783851B2 (en) * | 2008-02-20 | 2017-10-10 | The Children's Hospital Of Philadelphia | Genetic alterations associated with autism and the autistic phenotype and methods of use thereof for the diagnosis and treatment of autism |
| EP2331571B1 (en) * | 2008-09-18 | 2015-08-26 | Northwestern University | Nmda receptor modulators and uses thereof |
| HRP20140784T1 (hr) * | 2009-10-05 | 2014-10-10 | Northwestern University | Glyx-13 za uporabu u postupku tretiranja refraktornih depresija |
-
2012
- 2012-04-27 BR BR112013027554A patent/BR112013027554A2/pt not_active Application Discontinuation
- 2012-04-27 EA EA201790653A patent/EA201790653A1/ru unknown
- 2012-04-27 CN CN201280027349.3A patent/CN103974712A/zh active Pending
- 2012-04-27 EP EP20151676.2A patent/EP3679931A3/en not_active Withdrawn
- 2012-04-27 SG SG10202010665YA patent/SG10202010665YA/en unknown
- 2012-04-27 JP JP2014508130A patent/JP6035326B2/ja not_active Expired - Fee Related
- 2012-04-27 MX MX2013012526A patent/MX357761B/es active IP Right Grant
- 2012-04-27 KR KR1020187022910A patent/KR20180095096A/ko not_active Ceased
- 2012-04-27 CA CA2834286A patent/CA2834286A1/en not_active Abandoned
- 2012-04-27 KR KR1020207011211A patent/KR20200043534A/ko not_active Ceased
- 2012-04-27 EP EP12777016.2A patent/EP2701721A4/en not_active Ceased
- 2012-04-27 KR KR1020197008907A patent/KR20190037359A/ko not_active Ceased
- 2012-04-27 CN CN201711451914.XA patent/CN108283712A/zh active Pending
- 2012-04-27 KR KR1020137031028A patent/KR20140043078A/ko not_active Ceased
- 2012-04-27 WO PCT/US2012/035547 patent/WO2012149389A2/en not_active Ceased
- 2012-04-27 AU AU2012249397A patent/AU2012249397B2/en not_active Ceased
- 2012-04-27 KR KR1020217011613A patent/KR20210046843A/ko not_active Ceased
- 2012-04-27 SG SG2013079603A patent/SG194230A1/en unknown
- 2012-04-27 US US14/114,376 patent/US20140107037A1/en not_active Abandoned
- 2012-04-27 EA EA201391581A patent/EA029999B1/ru unknown
-
2016
- 2016-04-14 US US15/098,985 patent/US20170049845A1/en not_active Abandoned
-
2018
- 2018-10-23 US US16/168,242 patent/US20190209642A1/en not_active Abandoned
-
2019
- 2019-01-14 HK HK19100591.2A patent/HK1258231A1/zh unknown
-
2020
- 2020-05-05 US US16/867,324 patent/US20210169964A1/en not_active Abandoned
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