JP2018530593A5 - - Google Patents
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- Publication number
- JP2018530593A5 JP2018530593A5 JP2018519482A JP2018519482A JP2018530593A5 JP 2018530593 A5 JP2018530593 A5 JP 2018530593A5 JP 2018519482 A JP2018519482 A JP 2018519482A JP 2018519482 A JP2018519482 A JP 2018519482A JP 2018530593 A5 JP2018530593 A5 JP 2018530593A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- pyrrolidine
- pharmaceutical composition
- hydroxy
- carboxamide
- 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.)
- Pending
Links
- 239000008194 pharmaceutical composition Substances 0.000 claims 28
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 claims 15
- 239000003693 atypical antipsychotic agent Substances 0.000 claims 15
- 229940127236 atypical antipsychotics Drugs 0.000 claims 15
- VLJNHYLEOZPXFW-UHFFFAOYSA-N pyrrolidine-2-carboxamide Chemical compound NC(=O)C1CCCN1 VLJNHYLEOZPXFW-UHFFFAOYSA-N 0.000 claims 8
- 108010024875 GLYX-13 peptide Proteins 0.000 claims 6
- 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 6
- 229950000471 rapastinel Drugs 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 5
- 208000010877 cognitive disease Diseases 0.000 claims 5
- ZRDKPMDWWRFAAM-BJDJZHNGSA-N (2s)-n-[(2s)-1-amino-3-hydroxy-1-oxopropan-2-yl]-1-[(2s)-1-[(2s)-2-amino-3-hydroxypropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide Chemical compound OC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)N[C@@H](CO)C(N)=O)CCC1 ZRDKPMDWWRFAAM-BJDJZHNGSA-N 0.000 claims 4
- 208000028698 Cognitive impairment Diseases 0.000 claims 4
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims 3
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 3
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 3
- 239000005557 antagonist Substances 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 229960001432 lurasidone Drugs 0.000 claims 3
- PQXKDMSYBGKCJA-CVTJIBDQSA-N lurasidone Chemical compound C1=CC=C2C(N3CCN(CC3)C[C@@H]3CCCC[C@H]3CN3C(=O)[C@@H]4[C@H]5CC[C@H](C5)[C@@H]4C3=O)=NSC2=C1 PQXKDMSYBGKCJA-CVTJIBDQSA-N 0.000 claims 3
- YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical group C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 claims 2
- 229960003299 ketamine Drugs 0.000 claims 2
- 208000024714 major depressive disease Diseases 0.000 claims 2
- 239000003607 modifier Substances 0.000 claims 2
- VSWBSWWIRNCQIJ-GJZGRUSLSA-N (R,R)-asenapine Chemical compound O1C2=CC=CC=C2[C@@H]2CN(C)C[C@H]2C2=CC(Cl)=CC=C21 VSWBSWWIRNCQIJ-GJZGRUSLSA-N 0.000 claims 1
- DKMFBWQBDIGMHM-UHFFFAOYSA-N 1-(4-fluorophenyl)-4-(4-methyl-1-piperidinyl)-1-butanone Chemical compound C1CC(C)CCN1CCCC(=O)C1=CC=C(F)C=C1 DKMFBWQBDIGMHM-UHFFFAOYSA-N 0.000 claims 1
- GUJRSXAPGDDABA-NSHDSACASA-N 3-bromo-N-[[(2S)-1-ethyl-2-pyrrolidinyl]methyl]-2,6-dimethoxybenzamide Chemical compound CCN1CCC[C@H]1CNC(=O)C1=C(OC)C=CC(Br)=C1OC GUJRSXAPGDDABA-NSHDSACASA-N 0.000 claims 1
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000032170 Congenital Abnormalities Diseases 0.000 claims 1
- 206010010356 Congenital anomaly Diseases 0.000 claims 1
- 208000020358 Learning disease Diseases 0.000 claims 1
- -1 amino-3-hydroxybutanoyl Chemical group 0.000 claims 1
- 229960004372 aripiprazole Drugs 0.000 claims 1
- 229960005245 asenapine Drugs 0.000 claims 1
- 230000007698 birth defect Effects 0.000 claims 1
- 229960005123 cariprazine Drugs 0.000 claims 1
- KPWSJANDNDDRMB-QAQDUYKDSA-N cariprazine Chemical compound C1C[C@@H](NC(=O)N(C)C)CC[C@@H]1CCN1CCN(C=2C(=C(Cl)C=CC=2)Cl)CC1 KPWSJANDNDDRMB-QAQDUYKDSA-N 0.000 claims 1
- 229960004170 clozapine Drugs 0.000 claims 1
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010013932 dyslexia Diseases 0.000 claims 1
- 230000007613 environmental effect Effects 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- LHAPOGAFBLSJJQ-GUTACTQSSA-N iti007 Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.C([C@@H]1N2CCN(C=3C=CC=C(C2=3)[C@@H]1C1)C)CN1CCCC(=O)C1=CC=C(F)C=C1 LHAPOGAFBLSJJQ-GUTACTQSSA-N 0.000 claims 1
- 201000003723 learning disability Diseases 0.000 claims 1
- 229960001861 melperone Drugs 0.000 claims 1
- 239000003703 n methyl dextro aspartic acid receptor blocking agent Substances 0.000 claims 1
- 229960005017 olanzapine Drugs 0.000 claims 1
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims 1
- RKEWSXXUOLRFBX-UHFFFAOYSA-N pimavanserin Chemical compound C1=CC(OCC(C)C)=CC=C1CNC(=O)N(C1CCN(C)CC1)CC1=CC=C(F)C=C1 RKEWSXXUOLRFBX-UHFFFAOYSA-N 0.000 claims 1
- 229960003300 pimavanserin Drugs 0.000 claims 1
- 229960004431 quetiapine Drugs 0.000 claims 1
- URKOMYMAXPYINW-UHFFFAOYSA-N quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims 1
- 229960003448 remoxipride Drugs 0.000 claims 1
- 229960001534 risperidone Drugs 0.000 claims 1
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 229960000607 ziprasidone Drugs 0.000 claims 1
- MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022107539A JP2022140441A (ja) | 2015-10-16 | 2022-07-04 | 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 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562242633P | 2015-10-16 | 2015-10-16 | |
| US62/242,633 | 2015-10-16 | ||
| PCT/US2016/057071 WO2017066590A1 (en) | 2015-10-16 | 2016-10-14 | Pharmaceutical combination of an atypical antipsychotic and an nmda modulator for the treatment of schizophrenia,bipolar disorder, cognitive impairment and major depressive disorder |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022107539A Division JP2022140441A (ja) | 2015-10-16 | 2022-07-04 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018530593A JP2018530593A (ja) | 2018-10-18 |
| JP2018530593A5 true JP2018530593A5 (enExample) | 2019-11-28 |
Family
ID=57178579
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018519482A Pending JP2018530593A (ja) | 2015-10-16 | 2016-10-14 | 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 |
| JP2022107539A Pending JP2022140441A (ja) | 2015-10-16 | 2022-07-04 | 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022107539A Pending JP2022140441A (ja) | 2015-10-16 | 2022-07-04 | 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 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20180325893A1 (enExample) |
| EP (1) | EP3362080A1 (enExample) |
| JP (2) | JP2018530593A (enExample) |
| KR (1) | KR20180102052A (enExample) |
| CN (1) | CN108601814A (enExample) |
| AU (2) | AU2016340080A1 (enExample) |
| BR (1) | BR112018007681A2 (enExample) |
| CA (1) | CA3002070A1 (enExample) |
| MX (1) | MX2018004553A (enExample) |
| WO (1) | WO2017066590A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017100599A1 (en) | 2015-12-09 | 2017-06-15 | Luc Therapeutics | Thienopyrimidinone nmda receptor modulators and uses thereof |
| ES2821010T3 (es) | 2015-12-09 | 2021-04-23 | Cadent Therapeutics Inc | Moduladores heteroaromáticos del receptor NMDA y usos de los mismos |
| AU2017382339B2 (en) | 2016-12-22 | 2024-02-15 | Novartis Ag | NMDA receptor modulators and uses thereof |
| US20200199173A1 (en) * | 2017-07-28 | 2020-06-25 | Naurex, Inc. | Process and intermediates for synthesis of peptide compounds |
| BR112020009310A2 (pt) | 2017-11-14 | 2020-10-13 | Sk Biopharmaceuticals Co., Ltd. | combinação e composição farmacêutica para a prevenção, alívio ou tratamento da esquizofrenia. |
| DK3505157T3 (da) | 2017-12-29 | 2022-02-28 | Celon Pharma Sa | Tørpulver-ketaminsammensætning til pulmonal indgivelse ved behandlingsresistent depression |
| PT3830092T (pt) | 2018-08-03 | 2023-07-25 | Novartis Ag | Moduladores do recetor nmda heteroaromáticos e suas utilizações |
| US20220024976A1 (en) * | 2019-01-11 | 2022-01-27 | Naurex Inc. | Salt and crystalline forms of rapastinel |
| KR20210060843A (ko) | 2019-11-19 | 2021-05-27 | 뉴트라팜주식회사 | 기억력 및 인지기능 개선, 조현병 예방, 치료 또는 개선용 조성물 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5902815A (en) * | 1996-09-03 | 1999-05-11 | Washington University | Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction |
| KR20040105740A (ko) * | 2002-02-25 | 2004-12-16 | 엘란 파마슈티칼스, 인크. | 염증 치료제의 투여 방법 |
| WO2006066121A2 (en) * | 2004-12-16 | 2006-06-22 | Janssen Pharmaceutica N.V. | Combination of a glycine transporter (glyt1) inhibitor and an antipsychotic for the treatment of symptoms of schizophrenia as well as its preparation and use thereof |
| JP5838021B2 (ja) * | 2005-04-15 | 2015-12-24 | マクロジェニクス，インコーポレーテッド | 共有結合型ダイアボディとその使用 |
| EP2485751B1 (en) * | 2009-10-05 | 2014-05-21 | Northwestern University | GLYX-13 for use in a method of treating refractory depression |
| KR101692275B1 (ko) * | 2010-02-11 | 2017-01-04 | 노오쓰웨스턴 유니버시티 | ２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도 |
| SG10201501050RA (en) * | 2010-02-11 | 2015-04-29 | Univ Northwestern | Secondary Structure Stabilized NMDA Receptor Modulators And Uses Thereof |
| US9737531B2 (en) * | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| MX357761B (es) * | 2011-04-27 | 2018-07-23 | Univ Northwestern | Métodos para tratar la enfermedad de alzheimer, enfermedad de huntington, autismo u otros trastornos. |
| WO2013080046A1 (en) * | 2011-12-02 | 2013-06-06 | Dainippon Sumitomo Pharma Co., Ltd. | Lurasidone novel dosage regimens and use thereof for the treatment, prevention, and/or management of at least one cns disorder |
| EP2906722A4 (en) * | 2012-10-12 | 2016-07-20 | Univ Northwestern | METHOD FOR IDENTIFYING COMPOUNDS FOR THE TREATMENT OF DEPRESSIONS AND RELATED DISEASES |
| US20160345855A1 (en) * | 2013-12-13 | 2016-12-01 | Northwestern University | Methods of treating brain disorders or identifying biomarkers related thereto |
| BR112016025910A8 (pt) * | 2014-05-06 | 2021-07-13 | Univ Northwestern | uso de uma quantidade eficaz de glyx-13, uso de glyx-13 e um antagonista de nmdar e composição farmaceuticamente aceitável compreendendo os mesmos |
| KR20170040351A (ko) * | 2014-08-14 | 2017-04-12 | 노렉스, 인크. | Nmda 조절인자를 사용하여 우울증을 치료하는 방법 |
-
2016
- 2016-10-14 KR KR1020187013668A patent/KR20180102052A/ko not_active Ceased
- 2016-10-14 US US15/773,084 patent/US20180325893A1/en not_active Abandoned
- 2016-10-14 CA CA3002070A patent/CA3002070A1/en not_active Abandoned
- 2016-10-14 WO PCT/US2016/057071 patent/WO2017066590A1/en not_active Ceased
- 2016-10-14 EP EP16784754.0A patent/EP3362080A1/en not_active Withdrawn
- 2016-10-14 JP JP2018519482A patent/JP2018530593A/ja active Pending
- 2016-10-14 BR BR112018007681-3A patent/BR112018007681A2/en not_active IP Right Cessation
- 2016-10-14 CN CN201680064997.4A patent/CN108601814A/zh active Pending
- 2016-10-14 AU AU2016340080A patent/AU2016340080A1/en not_active Abandoned
- 2016-10-14 MX MX2018004553A patent/MX2018004553A/es unknown
-
2022
- 2022-07-04 JP JP2022107539A patent/JP2022140441A/ja active Pending
-
2023
- 2023-08-17 AU AU2023216827A patent/AU2023216827A1/en not_active Abandoned
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