CN101861312B - 2-[4-(吡唑-4-基烷基)哌嗪-1-基]-3-苯基吡嗪和吡啶及3-[4-(吡唑-4-基烷基)哌嗪-1-基]-2-苯基吡啶作为5-ht7受体拮抗剂 - Google Patents

2-[4-(吡唑-4-基烷基)哌嗪-1-基]-3-苯基吡嗪和吡啶及3-[4-(吡唑-4-基烷基)哌嗪-1-基]-2-苯基吡啶作为5-ht7受体拮抗剂 Download PDF

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Publication number
CN101861312B
CN101861312B CN200880015741.XA CN200880015741A CN101861312B CN 101861312 B CN101861312 B CN 101861312B CN 200880015741 A CN200880015741 A CN 200880015741A CN 101861312 B CN101861312 B CN 101861312B
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China
Prior art keywords
ylmethyl
pyrazoles
tetrahydrochysene
phenyl
connection pyrazine
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Expired - Fee Related
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CN200880015741.XA
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English (en)
Chinese (zh)
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CN101861312A (zh
Inventor
V·O·巴德斯库
A·M·坎普
B·P·克拉克
M·P·科亨
S·A·费拉
P·T·加拉赫尔
S·L·赫尔曼
M·P·马扎内茨
M·M·皮内罗-努涅斯
J·M·肖斯
P·G·斯皮纳泽
M·A·华顿
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of CN101861312A publication Critical patent/CN101861312A/zh
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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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)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN200880015741.XA 2007-05-11 2008-05-07 2-[4-(吡唑-4-基烷基)哌嗪-1-基]-3-苯基吡嗪和吡啶及3-[4-(吡唑-4-基烷基)哌嗪-1-基]-2-苯基吡啶作为5-ht7受体拮抗剂 Expired - Fee Related CN101861312B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US91743107P 2007-05-11 2007-05-11
US60/917,431 2007-05-11
US97420907P 2007-09-21 2007-09-21
US60/974,209 2007-09-21
PCT/US2008/062834 WO2008141020A1 (en) 2007-05-11 2008-05-07 2-[4-(pyrazol-4-ylalkyl)piperazin-1-yl]-3-phenyl pyrazines and pyridines and 3-[4-(pyrazol-4-ylalkyl)piperazin-1-yl]-2-phenyl pyridines as 5-ht7 receptor antagonists

Publications (2)

Publication Number Publication Date
CN101861312A CN101861312A (zh) 2010-10-13
CN101861312B true CN101861312B (zh) 2014-09-03

Family

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CN200880015741.XA Expired - Fee Related CN101861312B (zh) 2007-05-11 2008-05-07 2-[4-(吡唑-4-基烷基)哌嗪-1-基]-3-苯基吡嗪和吡啶及3-[4-(吡唑-4-基烷基)哌嗪-1-基]-2-苯基吡啶作为5-ht7受体拮抗剂

Country Status (17)

Country Link
US (1) US8202873B2 (cg-RX-API-DMAC10.html)
EP (1) EP2155717B1 (cg-RX-API-DMAC10.html)
JP (1) JP5210375B2 (cg-RX-API-DMAC10.html)
KR (1) KR101119294B1 (cg-RX-API-DMAC10.html)
CN (1) CN101861312B (cg-RX-API-DMAC10.html)
AU (1) AU2008251584B2 (cg-RX-API-DMAC10.html)
BR (1) BRPI0811446A2 (cg-RX-API-DMAC10.html)
CA (1) CA2684563C (cg-RX-API-DMAC10.html)
CY (1) CY1113457T1 (cg-RX-API-DMAC10.html)
DK (1) DK2155717T3 (cg-RX-API-DMAC10.html)
EA (1) EA016529B1 (cg-RX-API-DMAC10.html)
ES (1) ES2395872T3 (cg-RX-API-DMAC10.html)
HR (1) HRP20120919T1 (cg-RX-API-DMAC10.html)
MX (1) MX2009012126A (cg-RX-API-DMAC10.html)
PL (1) PL2155717T3 (cg-RX-API-DMAC10.html)
PT (1) PT2155717E (cg-RX-API-DMAC10.html)
WO (1) WO2008141020A1 (cg-RX-API-DMAC10.html)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0821689A2 (pt) * 2007-12-26 2015-06-16 Eisai R&D Man Co Ltd Processo para a produção de derivados de piridina substituídos por heterociclo
WO2011012620A2 (en) * 2009-07-31 2011-02-03 Syngenta Participations Ag Processes for the alkylation of pyrazoles
WO2011062194A1 (ja) 2009-11-18 2011-05-26 武田薬品工業株式会社 アミノピリジン誘導体
EP2566333A4 (en) * 2010-05-07 2014-04-02 Univ Leland Stanford Junior IDENTIFICATION OF STABILIZERS OF MULTIMEDER PROTEINS
CN103052625B (zh) 2010-08-10 2016-04-13 先正达参股股份有限公司 制备3-卤烷基吡唑的方法
TN2016000203A1 (en) 2013-12-20 2017-10-06 Esteve Labor Dr Piperazine derivatives having multimodal activity against pain.
WO2016025129A1 (en) 2014-08-14 2016-02-18 Alhamadsheh Mamoun M Conjugation of pharmaceutically active agents with transthyretin ligands through adjustable linkers to increase serum half-life
CN104592199A (zh) * 2015-01-22 2015-05-06 杭州利巴医药科技有限公司 一种取代的1-(2-吡啶基)-吡唑-4-基乙酸及其衍生物和制备方法
CN104945325B (zh) * 2015-06-19 2017-04-05 浙江永太科技股份有限公司 一种吡唑甲酸衍生物的制备方法
NZ797281A (en) 2017-02-17 2025-10-31 Eidos Therapeutics Inc Processes for preparing ag-10, its intermediates, and salts thereof
MY208459A (en) 2018-03-23 2025-05-10 Eidos Therapeutics Inc Methods of treating ttr amyloidosis using ag10
FI3836920T3 (fi) 2018-08-17 2025-12-22 Eidos Therapeutics Inc AG10-formulaatioita
KR102514860B1 (ko) * 2020-12-01 2023-03-29 한국과학기술연구원 5-ht7 세로토닌 수용체 활성 저해용 바이페닐 피롤리딘 및 바이페닐 다이하이드로이미다졸 유도체 및 이를 유효성분으로 포함하는 약학 조성물
CN115974785A (zh) * 2022-12-09 2023-04-18 南京先进生物材料与过程装备研究院有限公司 一种3,5-二取代吡唑类化合物的制备方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995035293A1 (es) * 1994-06-21 1995-12-28 Vita-Invest, S.A. Derivados de indol utiles para el tratamiento de la migraña, composicion y uso correspondientes
WO2004067703A2 (en) * 2003-01-31 2004-08-12 Pfizer Products Inc. 5ht7 antagonists and inverse agonists
US20050080076A1 (en) * 2003-10-08 2005-04-14 Xanodyne Pharmacal, Inc. N-desmethyl levomepromazine
WO2006069776A1 (en) * 2004-12-28 2006-07-06 Laboratorios Del Dr. Esteve, S.A. 5-ht7 receptor antagonists

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995035293A1 (es) * 1994-06-21 1995-12-28 Vita-Invest, S.A. Derivados de indol utiles para el tratamiento de la migraña, composicion y uso correspondientes
WO2004067703A2 (en) * 2003-01-31 2004-08-12 Pfizer Products Inc. 5ht7 antagonists and inverse agonists
US20050080076A1 (en) * 2003-10-08 2005-04-14 Xanodyne Pharmacal, Inc. N-desmethyl levomepromazine
WO2006069776A1 (en) * 2004-12-28 2006-07-06 Laboratorios Del Dr. Esteve, S.A. 5-ht7 receptor antagonists

Also Published As

Publication number Publication date
WO2008141020A1 (en) 2008-11-20
PL2155717T3 (pl) 2013-03-29
CN101861312A (zh) 2010-10-13
AU2008251584B2 (en) 2013-04-11
US8202873B2 (en) 2012-06-19
CA2684563A1 (en) 2008-11-20
EP2155717B1 (en) 2012-10-24
BRPI0811446A2 (pt) 2014-10-29
CA2684563C (en) 2013-08-13
DK2155717T3 (da) 2012-11-19
CY1113457T1 (el) 2016-06-22
ES2395872T3 (es) 2013-02-15
JP5210375B2 (ja) 2013-06-12
JP2010526819A (ja) 2010-08-05
KR20090127436A (ko) 2009-12-11
EA200971052A1 (ru) 2010-04-30
US20100120785A1 (en) 2010-05-13
PT2155717E (pt) 2012-12-21
HRP20120919T1 (hr) 2012-12-31
EP2155717A1 (en) 2010-02-24
KR101119294B1 (ko) 2012-04-12
EA016529B1 (ru) 2012-05-30
MX2009012126A (es) 2009-11-23
AU2008251584A1 (en) 2008-11-20

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