JP5727482B2 - 神経刺激性ピペラジンの合成 - Google Patents

神経刺激性ピペラジンの合成 Download PDF

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JP5727482B2
JP5727482B2 JP2012526928A JP2012526928A JP5727482B2 JP 5727482 B2 JP5727482 B2 JP 5727482B2 JP 2012526928 A JP2012526928 A JP 2012526928A JP 2012526928 A JP2012526928 A JP 2012526928A JP 5727482 B2 JP5727482 B2 JP 5727482B2
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formula
reaction
ambient temperature
alkyl
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JP2013502462A (ja
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スリパシー ベンカトラマン,
スリパシー ベンカトラマン,
サイエド マームード,
サイエド マームード,
ビンギディミ アイ. モベレ,
ビンギディミ アイ. モベレ,
オルガ ラピナ,
オルガ ラピナ,
ケリー バーコー,
ケリー バーコー,
イン リ,
イン リ,
ジョナサン サルズバリー,
ジョナサン サルズバリー,
マーク マクローズ,
マーク マクローズ,
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ニューラルステム, インコーポレイテッド
ニューラルステム, インコーポレイテッド
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (AREA)
JP2012526928A 2009-08-24 2010-08-24 神経刺激性ピペラジンの合成 Active JP5727482B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23647709P 2009-08-24 2009-08-24
US61/236,477 2009-08-24
PCT/US2010/046537 WO2011028548A1 (en) 2009-08-24 2010-08-24 Synthesis of a neurostimulative piperazine

Publications (2)

Publication Number Publication Date
JP2013502462A JP2013502462A (ja) 2013-01-24
JP5727482B2 true JP5727482B2 (ja) 2015-06-03

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ID=43649584

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JP2012526928A Active JP5727482B2 (ja) 2009-08-24 2010-08-24 神経刺激性ピペラジンの合成

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US (2) US9278933B2 (enExample)
EP (1) EP2470182B1 (enExample)
JP (1) JP5727482B2 (enExample)
KR (1) KR101701362B1 (enExample)
CN (2) CN105693601A (enExample)
AU (1) AU2010289802C1 (enExample)
BR (1) BR112012004161B1 (enExample)
CA (1) CA2772080C (enExample)
CL (1) CL2012000493A1 (enExample)
DK (1) DK2470182T3 (enExample)
ES (1) ES2475721T3 (enExample)
HR (1) HRP20140621T1 (enExample)
IL (1) IL218298A (enExample)
IN (1) IN2012DN02370A (enExample)
MX (1) MX2012002335A (enExample)
NZ (1) NZ598891A (enExample)
PL (1) PL2470182T3 (enExample)
PT (1) PT2470182E (enExample)
RU (1) RU2567390C2 (enExample)
SG (1) SG178867A1 (enExample)
SI (1) SI2470182T1 (enExample)
WO (1) WO2011028548A1 (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2012DN02370A (enExample) * 2009-08-24 2015-08-21 Neuralstem Inc
WO2018048927A1 (en) * 2016-09-12 2018-03-15 Neuralstem, Inc. Amelioration of neural deficits associated with diabetes
US20180104240A1 (en) * 2016-10-18 2018-04-19 Neuralstem, Inc. Amelioration of radiation-induced cognitive dysfunction
US10042957B2 (en) 2017-01-12 2018-08-07 Innovationdock, Inc. Devices and methods for implementing dynamic collaborative workflow systems
WO2018148733A1 (en) * 2017-02-13 2018-08-16 Neuralstem, Inc. Amelioration of certain deficiencies due to stroke
CN117377664A (zh) * 2020-12-23 2024-01-09 贝勒医学院 孤儿核受体tlx的小分子调节剂
JP2024520722A (ja) 2021-06-03 2024-05-24 オルト・ニューロサイエンス・インコーポレイテッド 不良な認知を有するうつ病患者の治療方法及びベンジルピペラジン-アミノピリジン剤の恩恵を受ける他の患者の選択
US12208096B2 (en) 2022-12-05 2025-01-28 Alto Neuroscience, Inc. Effective treatment of depression in patients having impaired learning and/or memory or certain EEG characteristics with a benzylpiperazine-aminopyridine agent
AU2023391488A1 (en) 2022-12-05 2025-05-22 Alto Neuroscience, Inc. Effective treatment of depression in patients having impaired learning and/or memory or certain eeg characteristics with a benzylpiperazine-aminopyridine agent
US12233059B2 (en) 2022-12-05 2025-02-25 Alto Neuroscience, Inc. Effective treatment of depression in patients having impaired learning and/or memory or certain EEG characteristics with a benzylpiperazine-aminopyridine agent

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU175075B (hu) * 1977-06-30 1980-05-28 Egyt Gyogyszervegyeszeti Gyar Sposob poluchenija piperazidov piridin-karbonovoj kisloty
JPS54122283A (en) * 1978-03-13 1979-09-21 Sumitomo Chem Co Ltd Novel quinazoline derivative and its preparation
US6995162B2 (en) * 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
DE60330323D1 (de) * 2002-03-29 2010-01-14 Schering Corp Stereoselektive alkylierung von chirale 2-methyl-4-geschützte piperazinen
GB0222493D0 (en) * 2002-09-27 2002-11-06 Glaxo Group Ltd Compounds
EP1576134B1 (en) * 2002-12-09 2013-03-06 Judith Kelleher-Andersson Method for discovering neurogenic agents
BRPI0414209B8 (pt) * 2003-09-09 2021-05-25 Hoffmann La Roche derivados de 1-(2-amino-benzol)-piperazina, seus processos de preparação e seu uso, e medicamento
EP1828165B1 (en) 2004-10-29 2013-03-20 Msd K.K. Novel aminopyridine derivatives having aurora a selective inhibitory action
US7754724B2 (en) * 2005-06-30 2010-07-13 Dow Agrosciences Llc N-substituted piperazines
AU2006329007A1 (en) * 2005-12-20 2007-06-28 Novartis Ag Nicotinic acid derivatives as modulators of metabotropic glutamate receptors
IN2012DN02370A (enExample) * 2009-08-24 2015-08-21 Neuralstem Inc

Also Published As

Publication number Publication date
RU2012111227A (ru) 2013-10-10
HK1172844A1 (en) 2013-05-03
US9278933B2 (en) 2016-03-08
JP2013502462A (ja) 2013-01-24
BR112012004161A2 (pt) 2016-03-29
AU2010289802B2 (en) 2014-10-02
IL218298A0 (en) 2012-04-30
EP2470182A4 (en) 2013-04-24
EP2470182B1 (en) 2014-06-04
PL2470182T3 (pl) 2015-05-29
BR112012004161B1 (pt) 2020-04-07
AU2010289802C1 (en) 2015-04-16
MX2012002335A (es) 2012-07-04
US20160090358A1 (en) 2016-03-31
IL218298A (en) 2017-03-30
CL2012000493A1 (es) 2012-09-28
US20130005974A1 (en) 2013-01-03
EP2470182A1 (en) 2012-07-04
CN102711764A (zh) 2012-10-03
AU2010289802A1 (en) 2012-04-12
KR20120054642A (ko) 2012-05-30
NZ598891A (en) 2014-05-30
DK2470182T3 (da) 2014-07-21
HRP20140621T1 (hr) 2014-11-21
ES2475721T3 (es) 2014-07-11
SI2470182T1 (sl) 2014-10-30
WO2011028548A1 (en) 2011-03-10
US9481649B2 (en) 2016-11-01
CN105693601A (zh) 2016-06-22
SG178867A1 (en) 2012-04-27
IN2012DN02370A (enExample) 2015-08-21
CA2772080A1 (en) 2011-03-10
KR101701362B1 (ko) 2017-02-01
CA2772080C (en) 2017-05-30
PT2470182E (pt) 2014-07-24
RU2567390C2 (ru) 2015-11-10

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