AU2008251584B2 - 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 - Google Patents

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 Download PDF

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Publication number
AU2008251584B2
AU2008251584B2 AU2008251584A AU2008251584A AU2008251584B2 AU 2008251584 B2 AU2008251584 B2 AU 2008251584B2 AU 2008251584 A AU2008251584 A AU 2008251584A AU 2008251584 A AU2008251584 A AU 2008251584A AU 2008251584 B2 AU2008251584 B2 AU 2008251584B2
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AU
Australia
Prior art keywords
alkyl
mmol
methyl
tetrahydro
pyrazol
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU2008251584A
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English (en)
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AU2008251584A1 (en
Inventor
Valentina O. Badescu
Anne Marie Camp
Barry Peter Clark
Michael Philip Cohen
Sandra Ann Filla
Peter Thaddeus Gallagher
Sarah Lynne Hellman
Michael Philip Mazanetz
Marta Maria Pineiro-Nunez
John Mehnert Schaus
Patrick Gianpietro Spinazze
Maria Ann Whatton
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Eli Lilly and Co
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Eli Lilly and Co
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Publication date
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Publication of AU2008251584A1 publication Critical patent/AU2008251584A1/en
Application granted granted Critical
Publication of AU2008251584B2 publication Critical patent/AU2008251584B2/en
Ceased legal-status Critical Current
Anticipated expiration legal-status Critical

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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

Landscapes

  • 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)
AU2008251584A 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 Ceased AU2008251584B2 (en)

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
AU2008251584A1 AU2008251584A1 (en) 2008-11-20
AU2008251584B2 true AU2008251584B2 (en) 2013-04-11

Family

ID=39629131

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2008251584A Ceased AU2008251584B2 (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

Country Status (17)

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

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009081970A1 (ja) * 2007-12-26 2009-07-02 Eisai R & D Management Co., Ltd. ヘテロ環置換ピリジン誘導体の製造方法
WO2011012620A2 (en) * 2009-07-31 2011-02-03 Syngenta Participations Ag Processes for the alkylation of pyrazoles
JPWO2011062194A1 (ja) 2009-11-18 2013-04-04 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
CA2806436C (en) 2010-08-10 2019-09-10 Syngenta Participations Ag Process for the preparation of 3-haloalkylpyrazoles
KR20160098506A (ko) 2013-12-20 2016-08-18 라보라토리오스 델 드라. 에스테브.에스.에이. 통증에 대한 다양한 활성을 갖는 피페라진 유도체
US20160045609A1 (en) 2014-08-14 2016-02-18 Mamoun M. Alhamadsheh 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
EP3582773A4 (en) 2017-02-17 2021-03-10 Eidos Therapeutics, Inc. PROCESS FOR THE MANUFACTURING OF AG-10, ITS INTERMEDIATES AND SALTS THEREOF
WO2019183463A1 (en) 2018-03-23 2019-09-26 Eidos Therapeutics, Inc. Methods of treating ttr amyloidosis using ag10
LT3836920T (lt) 2018-08-17 2026-01-26 Eidos Therapeutics, Inc. Ag10 farmacinės formos
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
US20240210412A1 (en) * 2021-04-13 2024-06-27 University Of Virginia Patent Foundation Sulfonyl-triazole compounds useful as ligands and inhibitors of prostaglandin reductase 2
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004067703A2 (en) * 2003-01-31 2004-08-12 Pfizer Products Inc. 5ht7 antagonists and inverse agonists

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2079323B1 (es) * 1994-06-21 1996-10-16 Vita Invest Sa Derivados de indol utiles para el tratamiento de la migraña, composicion y uso correspondientes.
EP1676844A1 (en) * 2004-12-28 2006-07-05 Laboratorios Del Dr. Esteve, S.A. 5-HT7 receptor antagonists
US20050080076A1 (en) * 2003-10-08 2005-04-14 Xanodyne Pharmacal, Inc. N-desmethyl levomepromazine

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004067703A2 (en) * 2003-01-31 2004-08-12 Pfizer Products Inc. 5ht7 antagonists and inverse agonists

Also Published As

Publication number Publication date
DK2155717T3 (da) 2012-11-19
HRP20120919T1 (hr) 2012-12-31
KR20090127436A (ko) 2009-12-11
US20100120785A1 (en) 2010-05-13
EP2155717A1 (en) 2010-02-24
EP2155717B1 (en) 2012-10-24
PL2155717T3 (pl) 2013-03-29
BRPI0811446A2 (pt) 2014-10-29
CY1113457T1 (el) 2016-06-22
CA2684563A1 (en) 2008-11-20
CN101861312B (zh) 2014-09-03
WO2008141020A1 (en) 2008-11-20
JP5210375B2 (ja) 2013-06-12
KR101119294B1 (ko) 2012-04-12
EA200971052A1 (ru) 2010-04-30
AU2008251584A1 (en) 2008-11-20
CA2684563C (en) 2013-08-13
US8202873B2 (en) 2012-06-19
MX2009012126A (es) 2009-11-23
ES2395872T3 (es) 2013-02-15
JP2010526819A (ja) 2010-08-05
EA016529B1 (ru) 2012-05-30
CN101861312A (zh) 2010-10-13
PT2155717E (pt) 2012-12-21

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