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 (https=) | 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 (https=) |
| EP (2) | EP2701721A4 (https=) |
| JP (1) | JP6035326B2 (https=) |
| KR (5) | KR20210046843A (https=) |
| CN (2) | CN103974712A (https=) |
| AU (1) | AU2012249397B2 (https=) |
| BR (1) | BR112013027554A2 (https=) |
| CA (1) | CA2834286A1 (https=) |
| EA (2) | EA029999B1 (https=) |
| HK (1) | HK1258231A1 (https=) |
| MX (1) | MX357761B (https=) |
| SG (2) | SG10202010665YA (https=) |
| WO (1) | WO2012149389A2 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011003015A (es) | 2008-09-18 | 2011-11-18 | Univ Northwestern | Moduladores del receptor de n-metil-d-aspartato, y usos de los mismos. |
| CN105037492A (zh) | 2010-02-11 | 2015-11-11 | 西北大学 | 二级结构稳定化的nmda受体调节剂及其用途 |
| KR101692275B1 (ko) | 2010-02-11 | 2017-01-04 | 노오쓰웨스턴 유니버시티 | ２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도 |
| KR20150110787A (ko) | 2013-01-29 | 2015-10-02 | 노렉스, 인크. | 스피로-락탐 nmda 수용체 조절인자 및 그의 용도 |
| EA032649B1 (ru) | 2013-01-29 | 2019-06-28 | Аптиникс Инк. | Спиролактамные модуляторы nmda-рецептора и их применение |
| SG11201505862TA (en) | 2013-01-29 | 2015-08-28 | Naurex Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| SG11201505942YA (en) | 2013-01-29 | 2015-08-28 | Naurex Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| KR20150110586A (ko) | 2013-01-29 | 2015-10-02 | 노렉스, 인크. | 스피로-락탐 nmda 수용체 조절인자 및 그의 용도 |
| AU2014342624A1 (en) * | 2013-10-28 | 2016-06-02 | Naurex, Inc. | NMDA receptor modulators and prodrugs, salts, and uses thereof |
| MX2016007716A (es) * | 2013-12-13 | 2017-03-31 | Univ Northwestern | Metodos para el tratamiento de trastornos cerebrales o la identificacion de biomarcadores relacionados con estos. |
| 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 |
| CN106661085A (zh) * | 2014-06-23 | 2017-05-10 | 西北大学 | 治疗或改善偏头痛的方法 |
| JP2018530593A (ja) * | 2015-10-16 | 2018-10-18 | ノースウェスタン ユニバーシティ | 統合失調症、双極性障害、認知障害及び大うつ病性障害の治療のための非定型的抗精神病薬ならびにｎｍｄａ調節剤の医薬品の組み合わせ |
| WO2017201285A1 (en) | 2016-05-19 | 2017-11-23 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| BR112018073663A2 (pt) | 2016-05-19 | 2019-04-30 | Aptinyx Inc. | moduladores de receptores nmda spiro-lactâmicos e seus usos |
| WO2018026782A1 (en) | 2016-08-01 | 2018-02-08 | Aptinyx Inc. | Spiro-lactam nmda receptor modulators and uses thereof |
| SG10202101055VA (en) | 2016-08-01 | 2021-03-30 | Aptinyx Inc | Spiro-lactam nmda receptor modulators and uses thereof |
| JP2019527232A (ja) | 2016-08-01 | 2019-09-26 | アプティニックス インコーポレイテッド | スピロ−ラクタムｎｍｄａ修飾因子及びこれを用いた方法 |
| MX385336B (es) | 2016-08-01 | 2025-03-18 | Aptinyx Inc | Moduladores del receptor nmda espiro-lactam y uso de los mismos. |
| EP3490994B8 (en) | 2016-08-01 | 2024-03-13 | Tenacia Biotechnology (Hong Kong) Co., Limited | Spiro-lactam and bis-spiro-lactam nmda receptor modulators and uses thereof |
| CN112204031B (zh) | 2018-01-31 | 2024-05-24 | 元羿生物科技(香港)有限公司 | 螺-内酰胺nmda受体调节剂及其用途 |
| 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 |
| WO2006034196A1 (en) * | 2004-09-17 | 2006-03-30 | Lifelike Biomatic Inc. | Compositions for enhancing memory and methods therefor |
| US20090325920A1 (en) * | 2005-03-24 | 2009-12-31 | Emory University | Methods for the treatment of a traumatic central nervous system injury |
| WO2009105718A1 (en) * | 2008-02-20 | 2009-08-27 | The Children's Hospital Of Philadelphia | Genetic alterations associated with autism and the autistic phenotype and methods of use thereof for the diagnosis and treatmemt of autism |
| MX2011003015A (es) * | 2008-09-18 | 2011-11-18 | Univ Northwestern | Moduladores del receptor de n-metil-d-aspartato, y usos de los mismos. |
| PL2485751T3 (pl) * | 2009-10-05 | 2014-10-31 | Univ Northwestern | GLYX-13 do stosowania w sposobie leczenia depresji opornej na leczenie |
-
2012
- 2012-04-27 US US14/114,376 patent/US20140107037A1/en not_active Abandoned
- 2012-04-27 EP EP12777016.2A patent/EP2701721A4/en not_active Ceased
- 2012-04-27 AU AU2012249397A patent/AU2012249397B2/en not_active Ceased
- 2012-04-27 SG SG10202010665YA patent/SG10202010665YA/en unknown
- 2012-04-27 CN CN201280027349.3A patent/CN103974712A/zh active Pending
- 2012-04-27 KR KR1020217011613A patent/KR20210046843A/ko not_active Ceased
- 2012-04-27 EP EP20151676.2A patent/EP3679931A3/en not_active Withdrawn
- 2012-04-27 KR KR1020187022910A patent/KR20180095096A/ko not_active Ceased
- 2012-04-27 CN CN201711451914.XA patent/CN108283712A/zh active Pending
- 2012-04-27 EA EA201391581A patent/EA029999B1/ru unknown
- 2012-04-27 BR BR112013027554A patent/BR112013027554A2/pt not_active Application Discontinuation
- 2012-04-27 JP JP2014508130A patent/JP6035326B2/ja not_active Expired - Fee Related
- 2012-04-27 CA CA2834286A patent/CA2834286A1/en not_active Abandoned
- 2012-04-27 WO PCT/US2012/035547 patent/WO2012149389A2/en not_active Ceased
- 2012-04-27 KR KR1020197008907A patent/KR20190037359A/ko not_active Ceased
- 2012-04-27 EA EA201790653A patent/EA201790653A1/ru unknown
- 2012-04-27 SG SG2013079603A patent/SG194230A1/en unknown
- 2012-04-27 KR KR1020207011211A patent/KR20200043534A/ko not_active Ceased
- 2012-04-27 MX MX2013012526A patent/MX357761B/es active IP Right Grant
- 2012-04-27 KR KR1020137031028A patent/KR20140043078A/ko not_active Ceased
-
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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