CN113966337A - 调节nmda受体活性的化合物、其药物组合物及用途 - Google Patents
调节nmda受体活性的化合物、其药物组合物及用途 Download PDFInfo
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- 125000002950 monocyclic group Chemical group 0.000 description 1
- LNOPIUAQISRISI-UHFFFAOYSA-N n'-hydroxy-2-propan-2-ylsulfonylethanimidamide Chemical compound CC(C)S(=O)(=O)CC(N)=NO LNOPIUAQISRISI-UHFFFAOYSA-N 0.000 description 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 description 1
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- YZMHQCWXYHARLS-UHFFFAOYSA-N naphthalene-1,2-disulfonic acid Chemical compound C1=CC=CC2=C(S(O)(=O)=O)C(S(=O)(=O)O)=CC=C21 YZMHQCWXYHARLS-UHFFFAOYSA-N 0.000 description 1
- KVBGVZZKJNLNJU-UHFFFAOYSA-N naphthalene-2-sulfonic acid Chemical compound C1=CC=CC2=CC(S(=O)(=O)O)=CC=C21 KVBGVZZKJNLNJU-UHFFFAOYSA-N 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- 125000004433 nitrogen atom Chemical group N* 0.000 description 1
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- 238000010534 nucleophilic substitution reaction Methods 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
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- WLJNZVDCPSBLRP-UHFFFAOYSA-N pamoic acid Chemical compound C1=CC=C2C(CC=3C4=CC=CC=C4C=C(C=3O)C(=O)O)=C(O)C(C(O)=O)=CC2=C1 WLJNZVDCPSBLRP-UHFFFAOYSA-N 0.000 description 1
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- 230000036470 plasma concentration Effects 0.000 description 1
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- WSHYKIAQCMIPTB-UHFFFAOYSA-M potassium;2-oxo-3-(3-oxo-1-phenylbutyl)chromen-4-olate Chemical compound [K+].[O-]C=1C2=CC=CC=C2OC(=O)C=1C(CC(=O)C)C1=CC=CC=C1 WSHYKIAQCMIPTB-UHFFFAOYSA-M 0.000 description 1
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- 125000001501 propionyl group Chemical group O=C([*])C([H])([H])C([H])([H])[H] 0.000 description 1
- 125000004742 propyloxycarbonyl group Chemical group 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
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- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
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- 229960004889 salicylic acid Drugs 0.000 description 1
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
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- 230000019491 signal transduction Effects 0.000 description 1
- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
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- 238000007619 statistical method Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
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- 230000035882 stress Effects 0.000 description 1
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- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- CWXPZXBSDSIRCS-UHFFFAOYSA-N tert-butyl piperazine-1-carboxylate Chemical compound CC(C)(C)OC(=O)N1CCNCC1 CWXPZXBSDSIRCS-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-N triflic acid Chemical compound OS(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-N 0.000 description 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 description 1
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- 239000004474 valine Substances 0.000 description 1
Classifications
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- 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
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/10—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
提供调节NMDA受体活性的化合物、其药物组合物及用途。具体地，提供式Ⅰ表示的化合物、或其药学上可接受的盐或酯、立体异构体或溶剂合物。所述化合物具有增强NMDA受体活性的作用，可用于制备预防/治疗抑郁、焦虑、紧张、学习及认知缺陷、神经性疼痛等疾病的药物，
Description
PCT国内申请，说明书已公开。
Claims (15)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2020103972655 | 2020-05-12 | ||
| CN202010397265 | 2020-05-12 | ||
| PCT/CN2021/093264 WO2021228123A1 (zh) | 2020-05-12 | 2021-05-12 | 调节nmda受体活性的化合物、其药物组合物及用途 |
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| CN113966337A true CN113966337A (zh) | 2022-01-21 |
| CN113966337B CN113966337B (zh) | 2024-01-02 |
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| Country | Link |
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| US (1) | US20230348493A1 (zh) |
| EP (1) | EP4137496A4 (zh) |
| JP (1) | JP2023525860A (zh) |
| CN (1) | CN113966337B (zh) |
| AU (1) | AU2021270664B2 (zh) |
| CA (1) | CA3183111A1 (zh) |
| WO (1) | WO2021228123A1 (zh) |
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| CN1129942A (zh) * | 1993-07-20 | 1996-08-28 | 以色列国有生物学研究所 | 作用于胆碱能系统的具有毒蕈碱拮抗性的氮杂螺环化合物 |
| CN1244528A (zh) * | 1998-06-12 | 2000-02-16 | 弗·哈夫曼-拉罗切有限公司 | 双－或三氮杂－螺旋[4,5]癸烷衍生物 |
| CN1662506A (zh) * | 2002-05-03 | 2005-08-31 | 以色列生物研究所 | 治疗中枢和周围神经系统疾病的方法和组合物及其有用的新化合物 |
| CN105408336A (zh) * | 2013-01-29 | 2016-03-16 | 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 |
| CN109937204A (zh) * | 2016-08-01 | 2019-06-25 | 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 |
| CN110198944A (zh) * | 2017-01-23 | 2019-09-03 | 辉瑞大药厂 | 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS5750798B2 (zh) * | 1973-03-29 | 1982-10-28 | ||
| CA1032945A (en) * | 1973-05-28 | 1978-06-13 | Katsuo Arimura | Imidazolido (1,5-c) thiazolidine-3-spiro-4'-piperidines |
| DE3204373A1 (de) * | 1982-02-09 | 1983-08-18 | Luitpold-Werk, Chemisch-pharmazeutische Fabrik GmbH & Co, 8000 München | Thiazaspiranderivate, verfahren zu ihrer herstellung und arzneimittel |
| IL97726A (en) * | 1990-04-10 | 1994-12-29 | Israel Inst Biolog Res | Pharmaceutical preparations containing compounds with bridged and unbridged heterocyclic groups connected via spiro-atop with oxazoline and thiazoline groups, and sharp compounds |
| NZ508016A (en) * | 1998-05-08 | 2002-09-27 | Toyama Chemical Co Ltd | Spiro compounds for preventing and/or treating autoimmune diseases |
| TW200404796A (en) * | 2002-08-19 | 2004-04-01 | Ono Pharmaceutical Co | Nitrogen-containing compound |
| FR2856685B1 (fr) * | 2003-06-25 | 2005-09-23 | Merck Sante Sas | Derives de thiazolylpiperidine, leurs procedes de preparation et les compositions pharmaceutiques qui les contiennent |
| TW200827368A (en) * | 2006-11-21 | 2008-07-01 | Genelabs Tech Inc | Amido anti-viral compounds |
| KR101675174B1 (ko) * | 2009-01-26 | 2016-11-10 | 이스라엘 인스티튜트 포 바이올로지컬 리서치 | 이환형 헤테로사이클릭 스피로 화합물 |
-
2021
- 2021-05-12 US US17/998,626 patent/US20230348493A1/en active Pending
- 2021-05-12 JP JP2022569218A patent/JP2023525860A/ja active Pending
- 2021-05-12 AU AU2021270664A patent/AU2021270664B2/en active Active
- 2021-05-12 CA CA3183111A patent/CA3183111A1/en active Pending
- 2021-05-12 WO PCT/CN2021/093264 patent/WO2021228123A1/zh unknown
- 2021-05-12 CN CN202180003919.4A patent/CN113966337B/zh active Active
- 2021-05-12 EP EP21804453.5A patent/EP4137496A4/en active Pending
Patent Citations (6)
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|---|---|---|---|---|
| CN1129942A (zh) * | 1993-07-20 | 1996-08-28 | 以色列国有生物学研究所 | 作用于胆碱能系统的具有毒蕈碱拮抗性的氮杂螺环化合物 |
| CN1244528A (zh) * | 1998-06-12 | 2000-02-16 | 弗·哈夫曼-拉罗切有限公司 | 双－或三氮杂－螺旋[4,5]癸烷衍生物 |
| CN1662506A (zh) * | 2002-05-03 | 2005-08-31 | 以色列生物研究所 | 治疗中枢和周围神经系统疾病的方法和组合物及其有用的新化合物 |
| CN105408336A (zh) * | 2013-01-29 | 2016-03-16 | 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 |
| CN109937204A (zh) * | 2016-08-01 | 2019-06-25 | 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 |
| CN110198944A (zh) * | 2017-01-23 | 2019-09-03 | 辉瑞大药厂 | 作为单酰基甘油脂肪酶抑制剂的杂环螺环化合物 |
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| EP4137496A4 (en) | 2024-08-21 |
| US20230348493A1 (en) | 2023-11-02 |
| AU2021270664A1 (en) | 2023-01-19 |
| EP4137496A1 (en) | 2023-02-22 |
| AU2021270664B2 (en) | 2024-05-30 |
| CA3183111A1 (en) | 2021-11-18 |
| JP2023525860A (ja) | 2023-06-19 |
| CN113966337B (zh) | 2024-01-02 |
| WO2021228123A1 (zh) | 2021-11-18 |
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