CN108368101B - 选择性nr2b拮抗剂 - Google Patents

选择性nr2b拮抗剂 Download PDF

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Publication number
CN108368101B
CN108368101B CN201680073103.8A CN201680073103A CN108368101B CN 108368101 B CN108368101 B CN 108368101B CN 201680073103 A CN201680073103 A CN 201680073103A CN 108368101 B CN108368101 B CN 108368101B
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CN108368101A (zh
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I.伊斯拉姆
S.桑加蒂鲁帕蒂
J.S.瓦里尔
S.彻鲁库
P.舍蒂
J.E.马科
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Bristol Myers Squibb Co
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/09Geometrical isomers

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  • 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)
CN201680073103.8A 2015-10-14 2016-10-13 选择性nr2b拮抗剂 Active CN108368101B (zh)

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 (2)

Publication Number Publication Date
CN108368101A CN108368101A (zh) 2018-08-03
CN108368101B true CN108368101B (zh) 2022-03-15

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CN201680073103.8A Active CN108368101B (zh) 2015-10-14 2016-10-13 选择性nr2b拮抗剂

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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)

* Cited by examiner, † Cited by third party
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

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070185168A1 (en) * 2004-04-07 2007-08-09 Takai Haruki S Piperidine derivatives
WO2011100585A1 (en) * 2010-02-11 2011-08-18 Joseph Moskal Secondary structure stabilized nmda receptor modulators and uses thereof
WO2015105929A1 (en) * 2014-01-09 2015-07-16 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
WO2015105772A1 (en) * 2014-01-09 2015-07-16 Bristol-Myers Squibb Company Selective nr2b antagonists

Family Cites Families (9)

* Cited by examiner, † Cited by third party
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
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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070185168A1 (en) * 2004-04-07 2007-08-09 Takai Haruki S Piperidine derivatives
WO2011100585A1 (en) * 2010-02-11 2011-08-18 Joseph Moskal Secondary structure stabilized nmda receptor modulators and uses thereof
WO2015105929A1 (en) * 2014-01-09 2015-07-16 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
WO2015105772A1 (en) * 2014-01-09 2015-07-16 Bristol-Myers Squibb Company Selective nr2b antagonists

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Novel analogues of ketamine and phencyclidine as NMDA receptor antagonists;Paola Zarantonello et al.,;《Bioorganic & Medicinal Chemistry Letters》;20110218;第21卷;第2059-2063页 *
芳甲酰烷基哌嗪类化合物的合成及抗脑缺氧缺血活性;李建其等;《中国药物化学杂志》;20060228;第16卷(第1期);第6-14页 *

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
KR20180064507A (ko) 2018-06-14
US20180312495A1 (en) 2018-11-01
US20200115370A1 (en) 2020-04-16
US10954225B2 (en) 2021-03-23
JP2018530582A (ja) 2018-10-18

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