WO2014192865A1 - Dérivé phénylpipérazine - Google Patents

Dérivé phénylpipérazine Download PDF

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Publication number
WO2014192865A1
WO2014192865A1 PCT/JP2014/064254 JP2014064254W WO2014192865A1 WO 2014192865 A1 WO2014192865 A1 WO 2014192865A1 JP 2014064254 W JP2014064254 W JP 2014064254W WO 2014192865 A1 WO2014192865 A1 WO 2014192865A1
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WO
WIPO (PCT)
Prior art keywords
group
piperazin
atom
halogen atom
alkyloxy
Prior art date
Application number
PCT/JP2014/064254
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English (en)
Japanese (ja)
Inventor
英史 吉永
拓士 中川
龍 永田
森　泰生
Original Assignee
大日本住友製薬株式会社
国立大学法人京都大学
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Application filed by 大日本住友製薬株式会社, 国立大学法人京都大学 filed Critical 大日本住友製薬株式会社
Publication of WO2014192865A1 publication Critical patent/WO2014192865A1/fr

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne un agent thérapeutique pour les maladies neurodégénératives et les maladies mentales, qui comprend, comme ingrédient actif, un composé représenté par la formule (1) [dans laquelle Z1 représente un atome d'halogène, un groupe alkyle ou similaires ; R11 à R25 représentent indépendamment un atome d'hydrogène, un atome d'halogène, un groupe alkyle ou similaire ; et X2 représente un atome d'halogène], un sel pharmaceutiquement acceptable du composé ou similaire.
PCT/JP2014/064254 2013-05-30 2014-05-29 Dérivé phénylpipérazine WO2014192865A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2013114287 2013-05-30
JP2013-114287 2013-05-30

Publications (1)

Publication Number Publication Date
WO2014192865A1 true WO2014192865A1 (fr) 2014-12-04

Family

ID=51988888

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/JP2014/064254 WO2014192865A1 (fr) 2013-05-30 2014-05-29 Dérivé phénylpipérazine

Country Status (1)

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WO (1) WO2014192865A1 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017046794A1 (fr) 2015-09-14 2017-03-23 The National Institute for Biotechnology in the Negev Ltd. Nouveaux dérivés de pipérazine et pipéridine, leur synthèse et utilisation associée pour inhiber l'oligomérisation de vdac, l'apoptose et le dysfonctionnement mitochondrial
US10434099B2 (en) 2016-09-22 2019-10-08 The National Institute for Biotechnology in the Negev Ltd. Methods for treating central nervous system disorders using VDAC inhibitors
US10787423B2 (en) 2015-09-14 2020-09-29 The National Institute For Biotechnolgy In The Negev Ltd. Piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
JP2021513984A (ja) * 2018-02-15 2021-06-03 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 Ｔｒｐｃ６阻害剤
WO2021210650A1 (fr) * 2020-04-16 2021-10-21 帝人ファーマ株式会社 Dérivé aryle ou hétéroaryle
WO2022118966A1 (fr) * 2020-12-04 2022-06-09 国立大学法人京都大学 Agent favorisant l'absorption de molécules d'acide nucléique dans les cellules, composition pharmaceutique et nouveau composé
WO2023233994A1 (fr) * 2022-05-30 2023-12-07 国立大学法人京都大学 Composition pharmaceutique et activateur d'autophagie

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005014563A1 (fr) * 2003-08-11 2005-02-17 F. Hoffmann-La Roche Ag Piperazine avec groupe phenyle substitue de type or et leur utilisation comme inhibiteurs de glyt1
WO2005023261A1 (fr) * 2003-09-09 2005-03-17 F. Hoffmann-La Roche Ag Derives de 1-benzoyl-piperazine comme inhibiteurs du recaptage de la glycine pour le traitement de psychoses
JP2009046464A (ja) * 2007-08-21 2009-03-05 Abbott Lab 中枢神経系障害を治療するための医薬組成物
WO2009132454A1 (fr) * 2008-04-28 2009-11-05 Neuromed Pharmaceuticals Ltd. Di-t-butylphényle piperazines utilisées comme inhibiteurs des canaux calciques
WO2013033037A2 (fr) * 2011-08-26 2013-03-07 The Regents Of The University Of California Nouveaux composés d'antiprion
JP2013116858A (ja) * 2011-12-01 2013-06-13 Dainippon Sumitomo Pharma Co Ltd Ｂｄｎｆ様低分子化合物を含有する治療薬

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005014563A1 (fr) * 2003-08-11 2005-02-17 F. Hoffmann-La Roche Ag Piperazine avec groupe phenyle substitue de type or et leur utilisation comme inhibiteurs de glyt1
WO2005023261A1 (fr) * 2003-09-09 2005-03-17 F. Hoffmann-La Roche Ag Derives de 1-benzoyl-piperazine comme inhibiteurs du recaptage de la glycine pour le traitement de psychoses
JP2009046464A (ja) * 2007-08-21 2009-03-05 Abbott Lab 中枢神経系障害を治療するための医薬組成物
WO2009132454A1 (fr) * 2008-04-28 2009-11-05 Neuromed Pharmaceuticals Ltd. Di-t-butylphényle piperazines utilisées comme inhibiteurs des canaux calciques
WO2013033037A2 (fr) * 2011-08-26 2013-03-07 The Regents Of The University Of California Nouveaux composés d'antiprion
JP2013116858A (ja) * 2011-12-01 2013-06-13 Dainippon Sumitomo Pharma Co Ltd Ｂｄｎｆ様低分子化合物を含有する治療薬

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY 2009, accession no. 181045-68-0 *
DATABASE REGISTRY 2012, accession no. 390496-47-5 *
KUMAR, S. ET AL.: "Synthesis and preliminary pharmacological evaluation of 2-[4-(aryl substituted)piperazin-1-yl]-N-phenylacetamides: potential antipsychotics", TROPICAL JOURNAL OF PHARMACEUTICAL RESEARCH, vol. 10, no. 3, 2011, pages 265 - 272 *
KUMAR, S. ET AL.: "Synthesis, computational studies and preliminary pharmacological evaluation of new arylpiperazines", E-JOURNAL OF CHEMISTRY, vol. 8, no. 3, 2011, pages 1044 - 1051 *

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11472777B2 (en) 2015-09-14 2022-10-18 The National Institute for Biotechnology in the Negev Ltd. Piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
CN108290889A (zh) * 2015-09-14 2018-07-17 内盖夫国家生物技术研究所 新的哌嗪和哌啶衍生物、它们的合成及其在抑制vdac寡聚化、细胞凋亡和线粒体功能障碍中的用途
US10508091B2 (en) 2015-09-14 2019-12-17 The National Institute for Biotechnology in the Negev Ltd. Piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
IL273816A (en) * 2015-09-14 2020-05-31 Nat Inst Biotechnology Negev Ltd Innovative derivatives of piperazine and piperidine, methods for their synthesis and uses as inhibitors of vdac oligomerization, apoptosis and disruption of mitochondrial activity
US10787423B2 (en) 2015-09-14 2020-09-29 The National Institute For Biotechnolgy In The Negev Ltd. Piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
AU2016325108B2 (en) * 2015-09-14 2020-10-22 The National Institute for Biotechnology in the Negev Ltd. Novel piperazine and piperidine derivatives, their synthesis and use thereof in inhibiting VDAC oligomerization, apoptosis and mitochondria dysfunction
US10946013B2 (en) 2015-09-14 2021-03-16 The National Institute for Biotechnology in the Negev Ltd. Methods for treating central nervous system disorders using vdac inhibitors
WO2017046794A1 (fr) 2015-09-14 2017-03-23 The National Institute for Biotechnology in the Negev Ltd. Nouveaux dérivés de pipérazine et pipéridine, leur synthèse et utilisation associée pour inhiber l'oligomérisation de vdac, l'apoptose et le dysfonctionnement mitochondrial
CN108290889B (zh) * 2015-09-14 2021-08-10 内盖夫国家生物技术研究所 新的哌嗪和哌啶衍生物、它们的合成及其在抑制vdac寡聚化、细胞凋亡和线粒体功能障碍中的用途
CN113620863B (zh) * 2015-09-14 2024-04-05 内盖夫国家生物技术研究所 新的哌嗪和哌啶衍生物、它们的合成及其用途
CN113620863A (zh) * 2015-09-14 2021-11-09 内盖夫国家生物技术研究所 新的哌嗪和哌啶衍生物、它们的合成及其用途
US10434099B2 (en) 2016-09-22 2019-10-08 The National Institute for Biotechnology in the Negev Ltd. Methods for treating central nervous system disorders using VDAC inhibitors
JP2021513984A (ja) * 2018-02-15 2021-06-03 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 Ｔｒｐｃ６阻害剤
JP7291711B2 (ja) 2018-02-15 2023-06-15 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 Ｔｒｐｃ６阻害剤
WO2021210650A1 (fr) * 2020-04-16 2021-10-21 帝人ファーマ株式会社 Dérivé aryle ou hétéroaryle
WO2022118966A1 (fr) * 2020-12-04 2022-06-09 国立大学法人京都大学 Agent favorisant l'absorption de molécules d'acide nucléique dans les cellules, composition pharmaceutique et nouveau composé
WO2023233994A1 (fr) * 2022-05-30 2023-12-07 国立大学法人京都大学 Composition pharmaceutique et activateur d'autophagie

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