JP6553615B2 - 疼痛に対して多重モードの活性を有するピペラジン誘導体 - Google Patents

疼痛に対して多重モードの活性を有するピペラジン誘導体 Download PDF

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JP6553615B2
JP6553615B2 JP2016539896A JP2016539896A JP6553615B2 JP 6553615 B2 JP6553615 B2 JP 6553615B2 JP 2016539896 A JP2016539896 A JP 2016539896A JP 2016539896 A JP2016539896 A JP 2016539896A JP 6553615 B2 JP6553615 B2 JP 6553615B2
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methyl
substituted
phenyl
triazol
unsubstituted
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JP2016540792A5 (enExample
JP2016540792A (ja
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コルドベス,フェリックス クエバス
コルドベス,フェリックス クエバス
アルマンサ−ロサレス,カルメン
ロペス,モニカ ガルシア
ロペス,モニカ ガルシア
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Esteve Pharmaceuticals SA
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/18Sulfonamides
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41921,2,3-Triazoles
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C07D249/101,2,4-Triazoles; Hydrogenated 1,2,4-triazoles 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
    • C07D249/14Nitrogen atoms
    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
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    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2016539896A 2013-12-20 2014-12-19 疼痛に対して多重モードの活性を有するピペラジン誘導体 Expired - Fee Related JP6553615B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13384006.6 2013-12-20
EP13384006 2013-12-20
PCT/EP2014/078852 WO2015092009A1 (en) 2013-12-20 2014-12-19 Piperazine derivatives having multimodal activity against pain

Publications (3)

Publication Number Publication Date
JP2016540792A JP2016540792A (ja) 2016-12-28
JP2016540792A5 JP2016540792A5 (enExample) 2018-02-01
JP6553615B2 true JP6553615B2 (ja) 2019-07-31

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JP2016539896A Expired - Fee Related JP6553615B2 (ja) 2013-12-20 2014-12-19 疼痛に対して多重モードの活性を有するピペラジン誘導体

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US (2) US10351535B2 (enExample)
EP (1) EP3083563A1 (enExample)
JP (1) JP6553615B2 (enExample)
KR (1) KR20160098506A (enExample)
CN (1) CN105829287B (enExample)
AU (1) AU2014368368C1 (enExample)
CA (1) CA2932051A1 (enExample)
IL (1) IL245808B (enExample)
MA (1) MA39145B1 (enExample)
MX (1) MX2016008130A (enExample)
MY (1) MY179509A (enExample)
PH (1) PH12016500978A1 (enExample)
RU (1) RU2709482C1 (enExample)
SG (1) SG10201805267UA (enExample)
TN (1) TN2016000203A1 (enExample)
UA (1) UA120754C2 (enExample)
WO (1) WO2015092009A1 (enExample)

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MX2018000419A (es) * 2015-07-29 2018-05-07 Esteve Labor Dr Derivados de amida sustituida que tienen actividad multimodal contra el dolor.
MX2018000418A (es) * 2015-07-29 2018-08-14 Esteve Labor Dr Derivados de amida que tienen actividad multimodal contra el dolor.
TW201808937A (zh) * 2016-05-20 2018-03-16 艾斯提夫博士實驗股份有限公司 針對疼痛具有多模態活性的四氫哌喃和噻喃衍生物
US11220505B2 (en) * 2017-03-21 2022-01-11 Temple University-Of The Commonwealth System Of Higher Education 5-hydroxytryptamine receptor 7 modulators and their use as therapeutic agents
JP7365237B2 (ja) * 2017-03-21 2023-10-19 テンプル・ユニバーシティ-オブ・ザ・コモンウェルス・システム・オブ・ハイアー・エデュケイション シグマ-2受容体の新規調節物質およびその使用方法
PT3762368T (pt) 2018-03-08 2022-05-06 Incyte Corp Compostos de aminopirazina diol como inibidores de pi3k-y
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
WO2020089400A1 (en) * 2018-10-31 2020-05-07 Esteve Pharmaceuticals, S.A. Piperazinyl and piperidinyl quinazolin-4(3h)-one derivatives having activity against pain
EP3753932A1 (en) * 2019-06-17 2020-12-23 Esteve Pharmaceuticals, S.A. Substituted bicyclic derivatives having multimodal activity against pain
WO2022187206A1 (en) * 2021-03-01 2022-09-09 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Dual-target mu opioid and dopamine d3 receptors ligands; preparation and use thereof
WO2024105225A1 (en) 2022-11-18 2024-05-23 Universitat De Barcelona Synergistic combinations of a sigma receptor 1 (s1r) antagonist and a soluble epoxide hydrolase inhibitor (sehi) and their use in the treatment of pain
CN117800942B (zh) * 2023-12-13 2025-04-25 徐州医科大学 一种噻吩哌嗪酰胺类衍生物、组合物及其应用

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IL245808B (en) 2020-03-31
IL245808A0 (en) 2016-08-02
CA2932051A1 (en) 2015-06-25
EP3083563A1 (en) 2016-10-26
MA39145B1 (fr) 2018-05-31
CN105829287A (zh) 2016-08-03
US20190276415A1 (en) 2019-09-12
SG10201805267UA (en) 2018-07-30
UA120754C2 (uk) 2020-02-10
US10351535B2 (en) 2019-07-16
RU2709482C1 (ru) 2019-12-18
CN105829287B (zh) 2019-08-27
US20170001967A1 (en) 2017-01-05
AU2014368368C1 (en) 2019-06-27
AU2014368368A1 (en) 2016-07-07
TN2016000203A1 (en) 2017-10-06
AU2014368368B2 (en) 2019-01-31
PH12016500978A1 (en) 2016-06-20
US10745361B2 (en) 2020-08-18
KR20160098506A (ko) 2016-08-18
MY179509A (en) 2020-11-09
JP2016540792A (ja) 2016-12-28
MA39145A1 (fr) 2017-10-31
MX2016008130A (es) 2016-10-13
WO2015092009A1 (en) 2015-06-25
RU2016129110A (ru) 2018-01-23

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