EA201391787A1 - Производные пиразола - Google Patents

Производные пиразола

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Publication number
EA201391787A1
EA201391787A1 EA201391787A EA201391787A EA201391787A1 EA 201391787 A1 EA201391787 A1 EA 201391787A1 EA 201391787 A EA201391787 A EA 201391787A EA 201391787 A EA201391787 A EA 201391787A EA 201391787 A1 EA201391787 A1 EA 201391787A1
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EA
Eurasian Patent Office
Prior art keywords
halogen
lower alkyl
substituted
hydrogen
disorders
Prior art date
Application number
EA201391787A
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English (en)
Other versions
EA024648B1 (ru
Inventor
Гуидо Галлей
Седрик Гелламалла
Роджер Норкросс
Филипп Пфлигер
Original Assignee
Ф.Хоффманн-Ля Рош Аг
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Application filed by Ф.Хоффманн-Ля Рош Аг filed Critical Ф.Хоффманн-Ля Рош Аг
Publication of EA201391787A1 publication Critical patent/EA201391787A1/ru
Publication of EA024648B1 publication Critical patent/EA024648B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • 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
    • A61P25/04Centrally 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/12Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям формулыгде Rпредставляет собой водород или фенил, возможно, содержащий в качестве заместителя галоген, CN или низшую алкоксигруппу или же низшую алкоксигруппу, замещенную галогеном; Rпредставляет собой водород или низший алкил; Rпредставляет собой водород или низший алкил или представляет собой фенил, возможно, содержащий один или более заместителей, выбранных из следующих: галоген, цианогруппа или низшая алкоксигруппа, замещенная галогеном, или представляет собой пиридинил, возможно, содержащий в качестве заместителя галоген или низший алкил, замещенный галогеном, или представляет собой пиримидинил, возможно, содержащий в качестве заместителя низший алкил, замещенный галогеном, или представляет собой пиразинил, возможно, содержащий в качестве заместителя галоген, цианогруппу или низший алкил, замещенный галогеном; Rпредставляет собой водород, низший алкил или фенил; Z представляет собой связь, -СН- или -О-; или к их фармацевтически приемлемым кислотно-аддитивным солям. Было показано, что соединения формулы IA и IB обладают высоким сродством по отношению к рецепторам следовых аминов (TAARs), в частности TAAR1. Эти соединения можно применять для лечения депрессии, тревожного невроза, биполярного расстройства, синдрома дефицита внимания и гиперактивности (СДВГ), расстройств, связанных со стрессом, психических расстройств, таких как шизофрения, неврологических заболеваний, таких как болезнь Паркинсона, нейродегенеративных расстройств, таких как болезнь Альцгеймера, эпилепсии, мигрени, гипертонии, наркотической зависимости и токсикомании и метаболических расстройств, таких как расстройства приема
EA201391787A 2011-06-09 2012-06-06 Производные пиразола EA024648B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP11169217 2011-06-09
PCT/EP2012/060627 WO2012168260A1 (en) 2011-06-09 2012-06-06 Pyrazole derivatives

Publications (2)

Publication Number Publication Date
EA201391787A1 true EA201391787A1 (ru) 2014-04-30
EA024648B1 EA024648B1 (ru) 2016-10-31

Family

ID=46298390

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201391787A EA024648B1 (ru) 2011-06-09 2012-06-06 Производные пиразола

Country Status (32)

Country Link
US (1) US9073911B2 (ru)
EP (1) EP2717873B1 (ru)
JP (1) JP5914642B2 (ru)
KR (1) KR101574905B1 (ru)
CN (1) CN103596567B (ru)
AR (1) AR088741A1 (ru)
AU (1) AU2012266457B2 (ru)
BR (1) BR112013031324B1 (ru)
CA (1) CA2837255C (ru)
CL (1) CL2013003484A1 (ru)
CO (1) CO6801764A2 (ru)
CY (1) CY1116778T1 (ru)
DK (1) DK2717873T3 (ru)
EA (1) EA024648B1 (ru)
EC (1) ECSP13013072A (ru)
ES (1) ES2546438T3 (ru)
HK (1) HK1191862A1 (ru)
HR (1) HRP20151077T1 (ru)
IL (1) IL229549B (ru)
MA (1) MA35192B1 (ru)
MX (1) MX347239B (ru)
MY (1) MY162160A (ru)
PE (1) PE20140934A1 (ru)
PL (1) PL2717873T3 (ru)
PT (1) PT2717873E (ru)
RS (1) RS54183B1 (ru)
SG (1) SG195156A1 (ru)
SI (1) SI2717873T1 (ru)
TW (1) TWI440636B (ru)
UA (1) UA110525C2 (ru)
WO (1) WO2012168260A1 (ru)
ZA (1) ZA201308939B (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2731095C2 (ru) * 2016-03-17 2020-08-28 Ф. Хоффманн-Ля Рош Аг Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar

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US9029370B2 (en) 2011-06-10 2015-05-12 Hoffmann-La Roche Inc. Substituted benzamide derivatives
KR101631003B1 (ko) 2012-01-12 2016-06-15 에프. 호프만-라 로슈 아게 미량 아민 결합 수용체(taar)로서 헤테로환형 유도체
HUE037689T2 (hu) 2012-09-14 2018-09-28 Hoffmann La Roche Pirazol-karboxamid származékok mint TAAR-modulátorok különféle rendellenességek, mint például depresszió, cukorbetegség és Parkinson-kór kezelésében történõ alkalmazásra
US9580407B2 (en) * 2012-12-07 2017-02-28 Merck Sharp & Dohme Corp. Regioselective N-2 arylation of indazoles
WO2015165085A1 (en) * 2014-04-30 2015-11-05 F.Hoffmann-La Roche Ag Morpholin-pyridine derivatives
IL270068B (en) 2017-04-24 2022-06-01 Tesaro Inc Manufacturing methods of Niraprib
CN112480005B (zh) * 2017-11-08 2022-08-19 北京嘉林药业股份有限公司 化合物及其治疗癌症的用途
CA3104053A1 (en) * 2018-06-18 2019-12-26 Janssen Pharmaceutica Nv Pyrazole derivatives as malt1 inhibitors
KR102161787B1 (ko) * 2018-07-02 2020-10-06 한국기초과학지원연구원 수면 장애의 예방 또는 치료용 약학적 조성물
CN112752755A (zh) 2018-09-27 2021-05-04 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的杂环基化合物
KR102396602B1 (ko) * 2019-02-28 2022-05-11 주식회사 마더스제약 피라졸 아마이드 유도체 화합물 및 이의 용도
AU2020274645A1 (en) * 2019-05-14 2021-12-16 Metabomed Ltd ACSS2 inhibitors and methods of use thereof
WO2023283369A1 (en) * 2021-07-08 2023-01-12 Vibliome Therapeutics, Llc Modulators of protein kinases
WO2023183444A1 (en) * 2022-03-24 2023-09-28 Vibliome Therapeutics, Llc Modulators of protein kinases
WO2024033459A1 (en) * 2022-08-12 2024-02-15 F. Hoffmann-La Roche Ag Pharmaceutical compositions comprising 5-ethyl-4-methyl- n-[4-[(2 s) morpholin-2-yl]phenyl]-1h-pyrazole-3-carboxamide

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GB9520150D0 (en) * 1995-10-03 1995-12-06 Orion Yhtymae Oy New imidazole derivatives
US6841684B2 (en) * 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
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CN101616902B (zh) 2007-02-15 2013-03-27 弗·哈夫曼-拉罗切有限公司 作为taar1配体的2-氨基*唑啉类化合物
US8354441B2 (en) 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
US9452980B2 (en) * 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
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CN102899314A (zh) 2011-07-29 2013-01-30 江汉大学 一种批量基因克隆的方法

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2731095C2 (ru) * 2016-03-17 2020-08-28 Ф. Хоффманн-Ля Рош Аг Производное 5-этил-4-метил-пиразол-3-карбоксамида, обладающее активностью агониста taar

Also Published As

Publication number Publication date
MX2013013853A (es) 2014-01-20
ECSP13013072A (es) 2014-01-31
MX347239B (es) 2017-04-20
BR112013031324B1 (pt) 2021-11-03
SG195156A1 (en) 2013-12-30
AU2012266457A1 (en) 2013-11-14
ZA201308939B (en) 2014-08-27
CL2013003484A1 (es) 2014-08-08
RS54183B1 (en) 2015-12-31
MA35192B1 (fr) 2014-06-02
EA024648B1 (ru) 2016-10-31
KR20140029517A (ko) 2014-03-10
PE20140934A1 (es) 2014-08-06
JP5914642B2 (ja) 2016-05-11
US20120316172A1 (en) 2012-12-13
EP2717873A1 (en) 2014-04-16
MY162160A (en) 2017-05-31
HRP20151077T1 (hr) 2015-11-06
SI2717873T1 (sl) 2015-09-30
US9073911B2 (en) 2015-07-07
ES2546438T3 (es) 2015-09-23
CN103596567B (zh) 2016-03-16
TW201302727A (zh) 2013-01-16
CA2837255C (en) 2020-10-27
IL229549A0 (en) 2014-01-30
AU2012266457B2 (en) 2016-09-08
PL2717873T3 (pl) 2015-12-31
AR088741A1 (es) 2014-07-02
BR112013031324A2 (pt) 2016-11-29
DK2717873T3 (en) 2015-07-27
PT2717873E (pt) 2015-09-18
CO6801764A2 (es) 2013-11-29
TWI440636B (zh) 2014-06-11
NZ617350A (en) 2016-01-29
KR101574905B1 (ko) 2015-12-04
IL229549B (en) 2019-06-30
CY1116778T1 (el) 2017-03-15
UA110525C2 (ru) 2016-01-12
CA2837255A1 (en) 2012-12-13
CN103596567A (zh) 2014-02-19
EP2717873B1 (en) 2015-07-15
WO2012168260A1 (en) 2012-12-13
HK1191862A1 (zh) 2014-08-08
JP2014516066A (ja) 2014-07-07

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