KR20180064507A - 선택적 nr2b 길항제 - Google Patents
선택적 nr2b 길항제 Download PDFInfo
- Publication number
- KR20180064507A KR20180064507A KR1020187013128A KR20187013128A KR20180064507A KR 20180064507 A KR20180064507 A KR 20180064507A KR 1020187013128 A KR1020187013128 A KR 1020187013128A KR 20187013128 A KR20187013128 A KR 20187013128A KR 20180064507 A KR20180064507 A KR 20180064507A
- Authority
- KR
- South Korea
- Prior art keywords
- mmol
- column
- flow rate
- compound
- substituted
- 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
- 102000034527 Retinoid X Receptors Human genes 0.000 title abstract 2
- 108010038912 Retinoid X Receptors Proteins 0.000 title abstract 2
- 239000005557 antagonist Substances 0.000 title 1
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 239000003446 ligand Substances 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 0 Cc1ccc(CN2OC[C@@](*)C2=O)cc1 Chemical compound Cc1ccc(CN2OC[C@@](*)C2=O)cc1 0.000 description 2
- VVPOMSQLXYLPSB-UHFFFAOYSA-N CC(C)(C)OC(NC(CON1Cc(cc2)ccc2F)C1=O)=O Chemical compound CC(C)(C)OC(NC(CON1Cc(cc2)ccc2F)C1=O)=O VVPOMSQLXYLPSB-UHFFFAOYSA-N 0.000 description 1
- VNNOMGVHZFZWLD-RXMQYKEDSA-N CC(C)(C)OC(N[C@H](CON1)C1=O)=O Chemical compound CC(C)(C)OC(N[C@H](CON1)C1=O)=O VNNOMGVHZFZWLD-RXMQYKEDSA-N 0.000 description 1
- WNVXFJFXBQATDY-SCSAIBSYSA-N CCOC(N[C@H](CON1)C1=O)=O Chemical compound CCOC(N[C@H](CON1)C1=O)=O WNVXFJFXBQATDY-SCSAIBSYSA-N 0.000 description 1
- KNLAYFWTYNWJDW-UHFFFAOYSA-N Cc1ccc(CN(C2=O)OCCC2N(CC2)CCN2c(nc2)ccc2O)cc1 Chemical compound Cc1ccc(CN(C2=O)OCCC2N(CC2)CCN2c(nc2)ccc2O)cc1 KNLAYFWTYNWJDW-UHFFFAOYSA-N 0.000 description 1
- LFAIBZXNQLLZCD-ATKRNPRHSA-N Cc1ccc(CN(C2=O)OCCC2N(CCC2c(cc3)ccc3O)C[C@H]2F)cc1 Chemical compound Cc1ccc(CN(C2=O)OCCC2N(CCC2c(cc3)ccc3O)C[C@H]2F)cc1 LFAIBZXNQLLZCD-ATKRNPRHSA-N 0.000 description 1
- NVNPLEPBDPJYRZ-UHFFFAOYSA-N Fc1ccc(CBr)cc1 Chemical compound Fc1ccc(CBr)cc1 NVNPLEPBDPJYRZ-UHFFFAOYSA-N 0.000 description 1
- DYDCUQKUCUHJBH-UWTATZPHSA-N N[C@H](CON1)C1=O Chemical compound N[C@H](CON1)C1=O DYDCUQKUCUHJBH-UWTATZPHSA-N 0.000 description 1
- QFTXNHSEWOULGJ-UHFFFAOYSA-N Oc1ccc(C(CC2)CCN2C(CON2Cc(cc3)ccc3F)C2=O)cc1 Chemical compound Oc1ccc(C(CC2)CCN2C(CON2Cc(cc3)ccc3F)C2=O)cc1 QFTXNHSEWOULGJ-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/09—Geometrical isomers
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN3309/DEL/2015 | 2015-10-14 | ||
| IN3309DE2015 | 2015-10-14 | ||
| PCT/US2016/056716 WO2017066368A1 (en) | 2015-10-14 | 2016-10-13 | Selective nr2b antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20180064507A true KR20180064507A (ko) | 2018-06-14 |
Family
ID=57208377
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187013128A Pending KR20180064507A (ko) | 2015-10-14 | 2016-10-13 | 선택적 nr2b 길항제 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US10501451B2 (enExample) |
| EP (1) | EP3362447B1 (enExample) |
| JP (1) | JP6843853B2 (enExample) |
| KR (1) | KR20180064507A (enExample) |
| CN (1) | CN108368101B (enExample) |
| AU (1) | AU2016340239A1 (enExample) |
| BR (1) | BR112018007181A2 (enExample) |
| CA (1) | CA3001894A1 (enExample) |
| EA (1) | EA201890764A1 (enExample) |
| ES (1) | ES2822830T3 (enExample) |
| IL (1) | IL258611A (enExample) |
| MX (1) | MX2018004257A (enExample) |
| WO (1) | WO2017066368A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112018006537A2 (pt) * | 2015-10-14 | 2018-10-16 | Bristol-Myers Squibb Company | antagonistas seletivos de nr2b |
| US11104670B2 (en) * | 2018-10-17 | 2021-08-31 | Boehringer Ingelheim International Gmbh | 4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament |
| CN112888685B (zh) * | 2018-10-17 | 2023-09-22 | 勃林格殷格翰国际有限公司 | 4-吡嗪-2-基甲基-吗啉衍生物及其作为药物的用途 |
| JP7093469B2 (ja) * | 2018-10-17 | 2022-06-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ４－ピリジニルメチル－モルホリン誘導体および医薬としてのその使用 |
| US12398143B2 (en) | 2019-06-04 | 2025-08-26 | Boehringer Ingelheim International Gmbh | Imidazopyrazine derivatives and the use thereof as medicament |
| TW202237103A (zh) * | 2020-12-04 | 2022-10-01 | 瑞士商諾華公司 | 用於治療抑鬱症的ｎｒ２ｂ－ｎｍｄａ受體ｎａｍ之劑量方案 |
| CN113620896A (zh) * | 2021-08-31 | 2021-11-09 | 青岛科技大学 | 2-(2-氯苯基)甲基-4,4-二甲基-3-异恶唑酮的制备方法 |
| CN116063200A (zh) * | 2022-12-12 | 2023-05-05 | 华南理工大学 | 一种异噁唑啉宠物用杀虫剂氟雷拉纳中间体及其制备方法 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| US7022728B2 (en) | 2001-03-09 | 2006-04-04 | Abbott Laboratories | Benzimidazoles that are useful in treating male sexual dysfunction |
| WO2003035641A1 (en) | 2001-10-22 | 2003-05-01 | Shionogi & Co., Ltd. | Novel carbamoylpyrrolidone derivative |
| MXPA05013151A (es) | 2003-06-04 | 2006-03-17 | Merck & Co Inc | 3-fluoro-piperidinas como antagonistas de n-metil-d-aspartato/nr2b. |
| JP2007508288A (ja) | 2003-10-08 | 2007-04-05 | ファイザー株式会社 | 縮合ラクタム化合物 |
| US20070185168A1 (en) * | 2004-04-07 | 2007-08-09 | Takai Haruki S | Piperidine derivatives |
| JPWO2006137465A1 (ja) * | 2005-06-24 | 2009-01-22 | 塩野義製薬株式会社 | 含窒素複素環誘導体 |
| US7935706B2 (en) | 2006-02-23 | 2011-05-03 | Shionogi & Co., Ltd. | Nitrogen-containing heterocycle derivatives substituted with cyclic group |
| CN101815518B (zh) | 2007-06-29 | 2013-01-09 | 埃莫里大学 | 用于神经保护的nmda受体拮抗剂 |
| JP2009067784A (ja) * | 2007-08-21 | 2009-04-02 | Shionogi & Co Ltd | 環式基で置換された含窒素複素環誘導体を含有する鎮痛剤 |
| US9101612B2 (en) * | 2010-02-11 | 2015-08-11 | Northwestern University | Secondary structure stabilized NMDA receptor modulators and uses thereof |
| US9221796B2 (en) * | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
| US9187506B2 (en) * | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
-
2016
- 2016-10-13 AU AU2016340239A patent/AU2016340239A1/en not_active Abandoned
- 2016-10-13 US US15/767,385 patent/US10501451B2/en active Active
- 2016-10-13 CA CA3001894A patent/CA3001894A1/en not_active Abandoned
- 2016-10-13 WO PCT/US2016/056716 patent/WO2017066368A1/en not_active Ceased
- 2016-10-13 ES ES16787974T patent/ES2822830T3/es active Active
- 2016-10-13 KR KR1020187013128A patent/KR20180064507A/ko active Pending
- 2016-10-13 EA EA201890764A patent/EA201890764A1/ru unknown
- 2016-10-13 EP EP16787974.1A patent/EP3362447B1/en active Active
- 2016-10-13 JP JP2018519276A patent/JP6843853B2/ja not_active Expired - Fee Related
- 2016-10-13 MX MX2018004257A patent/MX2018004257A/es unknown
- 2016-10-13 BR BR112018007181A patent/BR112018007181A2/pt not_active Application Discontinuation
- 2016-10-13 CN CN201680073103.8A patent/CN108368101B/zh active Active
-
2018
- 2018-04-10 IL IL258611A patent/IL258611A/en unknown
-
2019
- 2019-12-09 US US16/707,382 patent/US10954225B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| EA201890764A1 (ru) | 2018-09-28 |
| WO2017066368A1 (en) | 2017-04-20 |
| EP3362447B1 (en) | 2020-08-26 |
| EP3362447A1 (en) | 2018-08-22 |
| BR112018007181A2 (pt) | 2018-10-16 |
| IL258611A (en) | 2018-06-28 |
| MX2018004257A (es) | 2018-05-16 |
| CA3001894A1 (en) | 2017-04-20 |
| AU2016340239A1 (en) | 2018-05-31 |
| ES2822830T3 (es) | 2021-05-05 |
| JP6843853B2 (ja) | 2021-03-17 |
| US10501451B2 (en) | 2019-12-10 |
| CN108368101A (zh) | 2018-08-03 |
| US20180312495A1 (en) | 2018-11-01 |
| US20200115370A1 (en) | 2020-04-16 |
| US10954225B2 (en) | 2021-03-23 |
| JP2018530582A (ja) | 2018-10-18 |
| CN108368101B (zh) | 2022-03-15 |
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| KR102311518B1 (ko) | 선택적 nr2b 길항제 | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20180509 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20211012 Comment text: Request for Examination of Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20231201 Patent event code: PE09021S01D |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20240820 |