EA200971052A1 - 2-[4-(пиразол-4-илалкил)пиперазин-1-ил]-3-фенил пиразины и пиридины и 3-[4-(пиразол-4-илалкил)пиперазин-1-ил]-2-фенил пиридины в качестве антагонистов рецепторов 5-ht - Google Patents

2-[4-(пиразол-4-илалкил)пиперазин-1-ил]-3-фенил пиразины и пиридины и 3-[4-(пиразол-4-илалкил)пиперазин-1-ил]-2-фенил пиридины в качестве антагонистов рецепторов 5-ht

Info

Publication number
EA200971052A1
EA200971052A1 EA200971052A EA200971052A EA200971052A1 EA 200971052 A1 EA200971052 A1 EA 200971052A1 EA 200971052 A EA200971052 A EA 200971052A EA 200971052 A EA200971052 A EA 200971052A EA 200971052 A1 EA200971052 A1 EA 200971052A1
Authority
EA
Eurasian Patent Office
Prior art keywords
ilalkil
piperazin
pyrazol
phenyl
antagonists
Prior art date
Application number
EA200971052A
Other languages
English (en)
Other versions
EA016529B1 (ru
Inventor
Валентина О. Бадеску
Энн Мари Кэмп
Барри Питер Кларк
Майкл Филип Коэн
Сандра Энн Филла
Питер Таддеуш Галлахер
Сара Линн Хеллман
Майкл Филип Мазанетц
Марта Мария Пинейро-Нуньес
Джон Менерт Шаус
Патрик Джанпьетро Спинадзе
Мария Энн Ваттон
Original Assignee
Эли Лилли Энд Компани
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA200971052A1 publication Critical patent/EA200971052A1/ru
Publication of EA016529B1 publication Critical patent/EA016529B1/ru

Links

Classifications

    • 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)

Abstract

В настоящем изобретении предложены соединения формулы I, являющиеся селективными антагонистами рецептора 5-НТ, и их применение в лечении мигрени, персистирующей боли и тревожностигде каждый из А и В независимо представляет собой -С(Н)= или -N=, при условии, что по меньшей мере один из А и В представляет собой -N=, n имеет значение 1-3, m имеет значение 0-3 и Rявляются такими, как определено в данном описании.
EA200971052A 2007-05-11 2008-05-07 2-[4-(пиразол-4-илалкил)пиперазин-1-ил]-3-фенилпиразины и -пиридины и 3-[4-(пиразол-4-илалкил)пиперазин-1-ил]-2-фенилпиридины в качестве антагонистов рецепторов 5-ht EA016529B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US91743107P 2007-05-11 2007-05-11
US97420907P 2007-09-21 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
EA200971052A1 true EA200971052A1 (ru) 2010-04-30
EA016529B1 EA016529B1 (ru) 2012-05-30

Family

ID=39629131

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200971052A EA016529B1 (ru) 2007-05-11 2008-05-07 2-[4-(пиразол-4-илалкил)пиперазин-1-ил]-3-фенилпиразины и -пиридины и 3-[4-(пиразол-4-илалкил)пиперазин-1-ил]-2-фенилпиридины в качестве антагонистов рецепторов 5-ht

Country Status (17)

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

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8410277B2 (en) 2007-12-26 2013-04-02 Eisai R&D Managment Co., Ltd. Method for manufacturing heterocycle substituted pyridine derivatives
BR112012008128B8 (pt) * 2009-07-31 2019-07-16 Syngenta Participations Ag processos para a preparação de um composto da fórmula | e processo para a alquilação regiosseletiva de um composto da fórmula ||
US20130005710A1 (en) 2009-11-18 2013-01-03 Tetsuya Tsukamoto Aminopyridine derivative
WO2011140333A1 (en) 2010-05-07 2011-11-10 The Board Of Trustees Of The Leland Stanford Junior University Identification of stabilizers of multimeric proteins
WO2012019950A1 (en) * 2010-08-10 2012-02-16 Syngenta Participations Ag Process for the preparation of 3-haloalkylpyrazoles
MY179509A (en) * 2013-12-20 2020-11-09 Esteve Pharmaceuticals Sa Piperazine derivatives having multimodal activity against pain
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
SG11201906922TA (en) 2017-02-17 2019-09-27 Eidos Therapeutics Inc Processes for preparing ag-10, its intermediates, and salts thereof
CA3094711A1 (en) 2018-03-23 2019-09-26 Eidos Therapeutics, Inc. Methods of treating ttr amyloidosis using ag10
TWI834708B (zh) 2018-08-17 2024-03-11 美商文涵治療有限公司 Ag10之調配物

Family Cites Families (4)

* 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
BRPI0406704A (pt) * 2003-01-31 2005-12-20 Pfizer Prod Inc Antagonistas de 5ht~7~ e agonistas inversos
US20050080076A1 (en) * 2003-10-08 2005-04-14 Xanodyne Pharmacal, Inc. N-desmethyl levomepromazine

Also Published As

Publication number Publication date
PL2155717T3 (pl) 2013-03-29
BRPI0811446A2 (pt) 2014-10-29
AU2008251584A1 (en) 2008-11-20
EP2155717A1 (en) 2010-02-24
US20100120785A1 (en) 2010-05-13
CA2684563C (en) 2013-08-13
EA016529B1 (ru) 2012-05-30
US8202873B2 (en) 2012-06-19
JP5210375B2 (ja) 2013-06-12
KR20090127436A (ko) 2009-12-11
AU2008251584B2 (en) 2013-04-11
CN101861312B (zh) 2014-09-03
ES2395872T3 (es) 2013-02-15
WO2008141020A1 (en) 2008-11-20
DK2155717T3 (da) 2012-11-19
PT2155717E (pt) 2012-12-21
JP2010526819A (ja) 2010-08-05
KR101119294B1 (ko) 2012-04-12
CA2684563A1 (en) 2008-11-20
MX2009012126A (es) 2009-11-23
EP2155717B1 (en) 2012-10-24
CY1113457T1 (el) 2016-06-22
HRP20120919T1 (hr) 2012-12-31
CN101861312A (zh) 2010-10-13

Similar Documents

Publication Publication Date Title
EA200971052A1 (ru) 2-[4-(пиразол-4-илалкил)пиперазин-1-ил]-3-фенил пиразины и пиридины и 3-[4-(пиразол-4-илалкил)пиперазин-1-ил]-2-фенил пиридины в качестве антагонистов рецепторов 5-ht
CY1118096T1 (el) Ρυθμιστες υποδοχεα οπιοειδους
EA200870521A1 (ru) Замещенные спироциклические антагонисты cgrp-рецепторов
EA201100524A1 (ru) Азаиндазолы в качестве антагонистов рецептора ccr1
EA201100523A1 (ru) Соединения сульфонила, которые селективно модулируют рецептор св2
EA200601895A1 (ru) 3-(4-гетероарилциклогексиламино)циклопентанкарбоксамиды в качестве модуляторов хемокиновых рецепторов
EA200970341A1 (ru) Пиразолиновые соединения в качестве антагонистов минералокортикоидных рецепторов
EA200900606A1 (ru) Новые сульфониламидные производные в качестве антагонистов брадикининовых рецепторов
EA201071264A1 (ru) Аминодигидротиазиновые производные в качестве ингибиторов bace для лечения болезни альцгеймера
EA201171063A1 (ru) Фармацевтические составы олмесартана
ATE469144T1 (de) Substituierte pyridonverbindungen und anwendungsverfahren
DK1716152T3 (da) Kondenserade heterocykliske forbindelser og deres anvendelse som metabotrope receptorantagonister til behandling af gastrointentinde lidelser
DE602006007556D1 (de) Heteroarylsulfonylstilbene als 5-ht2a-antagonisten
ATE537170T1 (de) Cgrp-rezeptorantagonisten
NO20076479L (no) Nye oksadiazolderivater og anvendelse derav som positive allosteriske metabotropiske modulatorer av glutamatreseptorer
EA200900831A1 (ru) Модуляторы никотиновых ацетилхолиновых рецепторов
ATE478856T1 (de) Spirobenzodioxole und deren verwendung als cb1- antagonisten
NO20080445L (no) Nye azetidinderivater som neurokininreseptorantagonister for behandling av gastrointestinale sykdommer
EA201100517A1 (ru) Способ получения дабигатрана и его промежуточные соединения
EA201190207A1 (ru) Соединения для лечения метаболических расстройств
ATE505468T1 (de) N-gebundene heterocyclische antagonisten des p2y1-rezeptors zur behandlung von thromboseleiden
EA201171211A1 (ru) Производные оксадиазола
EA201070321A1 (ru) Замещённые пиперазинил-пиразины и пиридины в качестве антагонистов рецепторов 5-нт
ATE511500T1 (de) Sulfonamide als orexin-antagonisten
ATE466853T1 (de) Cgrp-rezeptorantagonisten

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM BY KZ KG MD TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ TJ

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU