EA201890764A1 - Селективные антагонисты nr2b - Google Patents

Селективные антагонисты nr2b

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Publication number
EA201890764A1
EA201890764A1 EA201890764A EA201890764A EA201890764A1 EA 201890764 A1 EA201890764 A1 EA 201890764A1 EA 201890764 A EA201890764 A EA 201890764A EA 201890764 A EA201890764 A EA 201890764A EA 201890764 A1 EA201890764 A1 EA 201890764A1
Authority
EA
Eurasian Patent Office
Prior art keywords
nr2b
selective antagonists
formula
compounds according
nmda
Prior art date
Application number
EA201890764A
Other languages
English (en)
Inventor
Имадул Ислам
Сринивасан Тангатирупати
Джайакумар Санкара Варриер
Сринивас Черуку
Пурнима Шетти
Джон Е. Мэйкор
Original Assignee
Бристол-Майерс Сквибб Компани
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Бристол-Майерс Сквибб Компани filed Critical Бристол-Майерс Сквибб Компани
Publication of EA201890764A1 publication Critical patent/EA201890764A1/ru

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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

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)

Abstract

Настоящее изобретение относится к соединениям согласно формуле (I) и их фармацевтически приемлемым солям. Соединения согласно формуле (I) представляют собой лиганды для рецептора NR2B N-метил-D-аспартата (NMDA), что делает их применимыми для лечения различных нарушений центральной нервной системы.
EA201890764A 2015-10-14 2016-10-13 Селективные антагонисты nr2b EA201890764A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN3309DE2015 2015-10-14
PCT/US2016/056716 WO2017066368A1 (en) 2015-10-14 2016-10-13 Selective nr2b antagonists

Publications (1)

Publication Number Publication Date
EA201890764A1 true EA201890764A1 (ru) 2018-09-28

Family

ID=57208377

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201890764A EA201890764A1 (ru) 2015-10-14 2016-10-13 Селективные антагонисты nr2b

Country Status (13)

Country Link
US (2) US10501451B2 (ru)
EP (1) EP3362447B1 (ru)
JP (1) JP6843853B2 (ru)
KR (1) KR20180064507A (ru)
CN (1) CN108368101B (ru)
AU (1) AU2016340239A1 (ru)
BR (1) BR112018007181A2 (ru)
CA (1) CA3001894A1 (ru)
EA (1) EA201890764A1 (ru)
ES (1) ES2822830T3 (ru)
IL (1) IL258611A (ru)
MX (1) MX2018004257A (ru)
WO (1) WO2017066368A1 (ru)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3001890A1 (en) 2015-10-14 2017-04-20 Bristol-Myers Squibb Company Selective nr2b antagonists
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
TWI828779B (zh) * 2018-10-17 2024-01-11 德商百靈佳殷格翰國際股份有限公司 4-吡-2-基甲基-嗎啉衍生物及其作為醫藥之用途
EP3867245B1 (en) * 2018-10-17 2022-12-07 Boehringer Ingelheim International GmbH 4-pyrimidin-5-ylmethyl-morpholine derivatives and the use thereof as medicament
JP2023551943A (ja) * 2020-12-04 2023-12-13 ノバルティス アーゲー うつ病の処置のためのnr2b-nmda受容体namについての投薬レジメン
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

Family Cites Families (13)

* 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
JPWO2003035641A1 (ja) 2001-10-22 2005-02-10 塩野義製薬株式会社 新規カルバモイルピロリドン誘導体
RU2339630C2 (ru) 2003-06-04 2008-11-27 Мерк Энд Ко., Инк. 3-фторпиперидины в качестве антагонистов nmda/nr2b
CA2541162A1 (en) 2003-10-08 2005-04-21 Pfizer Inc. Fused lactam compounds
EP1736474A4 (en) * 2004-04-07 2010-04-21 Kyowa Hakko Kirin Co Ltd piperidine
WO2006137465A1 (ja) * 2005-06-24 2006-12-28 Shionogi & Co., Ltd. 含窒素複素環誘導体
EP1988077A4 (en) 2006-02-23 2009-09-02 Shionogi & Co NUCLEIC HETEROCYCLIC DERIVATIVES SUBSTITUTED BY CYCLIC GROUPS
US8420680B2 (en) 2007-06-29 2013-04-16 Emory University NMDA receptor antagonists for neuroprotection
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
CN102933226A (zh) * 2010-02-11 2013-02-13 西北大学 二级结构稳定化的nmda受体调节剂及其用途
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

Also Published As

Publication number Publication date
US20200115370A1 (en) 2020-04-16
EP3362447A1 (en) 2018-08-22
US10501451B2 (en) 2019-12-10
IL258611A (en) 2018-06-28
MX2018004257A (es) 2018-05-16
CA3001894A1 (en) 2017-04-20
BR112018007181A2 (pt) 2018-10-16
EP3362447B1 (en) 2020-08-26
JP2018530582A (ja) 2018-10-18
CN108368101A (zh) 2018-08-03
US10954225B2 (en) 2021-03-23
WO2017066368A1 (en) 2017-04-20
KR20180064507A (ko) 2018-06-14
CN108368101B (zh) 2022-03-15
AU2016340239A1 (en) 2018-05-31
JP6843853B2 (ja) 2021-03-17
US20180312495A1 (en) 2018-11-01
ES2822830T3 (es) 2021-05-05

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