EA201290520A1 - Производные дифенилпиразолопиридинов, их получение и применение в качестве модуляторов нуклеарного рецептора not - Google Patents

Производные дифенилпиразолопиридинов, их получение и применение в качестве модуляторов нуклеарного рецептора not

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Publication number
EA201290520A1
EA201290520A1 EA201290520A EA201290520A EA201290520A1 EA 201290520 A1 EA201290520 A1 EA 201290520A1 EA 201290520 A EA201290520 A EA 201290520A EA 201290520 A EA201290520 A EA 201290520A EA 201290520 A1 EA201290520 A1 EA 201290520A1
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Eurasian Patent Office
Prior art keywords
alkyl
alkyls
hydroxy
halogen
oxo
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EA201290520A
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English (en)
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EA020652B1 (ru
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Флориан Оже
Люк Эвен
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Санофи
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Publication of EA201290520A1 publication Critical patent/EA201290520A1/ru
Publication of EA020652B1 publication Critical patent/EA020652B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/06—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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
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  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Формула (I), в которой: R представляет собой атом водорода или галогена или (С-С)алкил; X представляет собой один или несколько заместителей, выбранных из атомов водорода или галогена, (С-С)алкилов, галоген(С-С)алкилов, (С-С)алкоксигрупп, галоген(С-С)алкоксигрупп, циано-, гидрокси- группы или гидрокси(С-С)алкилов; Y представляет собой атом водорода, галогена или (С-С)алкил; R1 представляет собой NR2R3 или OR4; R2 и R3 независимо друг от друга представляют собой атомы водорода, (С-С)алкилы, гидрокси(С-С)алкилы или оксо(С-С) алкилы или R2 и R3 с атомом азота, с которым они связаны, образуют гетероцикл, необязательно замещенный С-С)алкилом, гидрокси- или оксогруппой; R4 представляет собой (С-С)алкил, гидрокси(С-С)алкил или оксо(С-С)алкил; в виде основания или кислотно-аддитивной соли. Применение в терапии при лечении или профилактике заболеваний, затрагивающих нуклеарные рецепторы Nurr-1, называемые также NR4A2, NOT, TINUR, RNR-1 и HZF3.
EA201290520A 2009-12-04 2010-12-03 Производные дифенилпиразолопиридинов, их получение и применение в качестве модуляторов нуклеарного рецептора not EA020652B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0958651A FR2953520B1 (fr) 2009-12-04 2009-12-04 Derives de diphenyl-pyrazolopyridines, leur preparation et leur application en therapeutique
PCT/FR2010/052605 WO2011067544A1 (fr) 2009-12-04 2010-12-03 Derives de diphenyl - pyrazolopyrdines, leur preparation et leur application en tant que modulateurs du recepteur nucleaire not

Publications (2)

Publication Number Publication Date
EA201290520A1 true EA201290520A1 (ru) 2013-01-30
EA020652B1 EA020652B1 (ru) 2014-12-30

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EA201290520A EA020652B1 (ru) 2009-12-04 2010-12-03 Производные дифенилпиразолопиридинов, их получение и применение в качестве модуляторов нуклеарного рецептора not

Country Status (24)

Country Link
US (1) US8680096B2 (ru)
EP (1) EP2507238B1 (ru)
JP (1) JP5738310B2 (ru)
KR (1) KR101696959B1 (ru)
CN (1) CN102762559B (ru)
AR (1) AR079250A1 (ru)
AU (1) AU2010326429B2 (ru)
BR (1) BR112012013511A2 (ru)
CA (1) CA2782704C (ru)
CL (1) CL2012001461A1 (ru)
CO (1) CO6551713A2 (ru)
EA (1) EA020652B1 (ru)
FR (1) FR2953520B1 (ru)
HK (1) HK1169984A1 (ru)
IL (1) IL220060A (ru)
JO (1) JO3098B1 (ru)
MA (1) MA33893B1 (ru)
MX (1) MX2012006421A (ru)
MY (1) MY157676A (ru)
NZ (1) NZ600368A (ru)
SG (1) SG181138A1 (ru)
TW (1) TWI481606B (ru)
UY (1) UY33079A (ru)
WO (1) WO2011067544A1 (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2950345B1 (fr) * 2009-09-18 2011-09-23 Sanofi Aventis Derives acetyleniques de 5-phenyl-pyrazolopyridine, leur preparation et leur application en therapeutique
FR2950344B1 (fr) * 2009-09-18 2011-11-25 Sanofi Aventis Derives de 5-phenyl-pyrazolopyridine, leur preparation et leur aplication en therapeutique.
US11261188B2 (en) 2016-11-28 2022-03-01 Praxis Precision Medicines, Inc. Fused heteroaryl compounds, and methods thereof for treating diseases, disorders, and conditions relating to aberrant function of a sodium channel
CN110337295B (zh) 2016-11-28 2023-06-09 普拉克西斯精密药物股份有限公司 化合物以及它们的使用方法
WO2018098500A1 (en) * 2016-11-28 2018-05-31 Praxis Precision Medicines, Inc. Compounds and their methods of use
CN110049975B (zh) * 2016-12-08 2023-01-31 拜耳作物科学股份公司 制备5-(1-苯基-1h-吡唑-4-基)烟酰胺衍生物的方法
US11492345B2 (en) 2017-02-13 2022-11-08 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11731966B2 (en) 2017-04-04 2023-08-22 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11278535B2 (en) 2017-08-15 2022-03-22 Praxis Precision Medicines, Inc. Compounds and their methods of use
TWI831786B (zh) 2018-05-30 2024-02-11 美商普雷西斯精密藥品公司 離子通道調節劑
US11773099B2 (en) 2019-05-28 2023-10-03 Praxis Precision Medicines, Inc. Compounds and their methods of use
US11505554B2 (en) 2019-05-31 2022-11-22 Praxis Precision Medicines, Inc. Substituted pyridines as ion channel modulators
US11279700B2 (en) 2019-05-31 2022-03-22 Praxis Precision Medicines, Inc. Ion channel modulators
US11767325B2 (en) 2019-11-26 2023-09-26 Praxis Precision Medicines, Inc. Substituted [1,2,4]triazolo[4,3-a]pyrazines as ion channel modulators
CN111138325B (zh) * 2019-12-20 2021-11-30 台州学院 一种(Z)-β-磺酰基烯胺类化合物的制备方法

Family Cites Families (8)

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JP2001139575A (ja) * 1999-11-15 2001-05-22 Fujisawa Pharmaceut Co Ltd 新規ピラゾロピリジン誘導体
FR2906250B1 (fr) * 2006-09-22 2008-10-31 Sanofi Aventis Sa Derives de 2-aryl-6phenyl-imidazo(1,2-a) pyridines, leur preparation et leur application en therapeutique
CN101679409B (zh) * 2006-12-22 2014-11-26 Astex治疗学有限公司 双环杂环衍生化合物、其医药组合物和其用途
FR2928921B1 (fr) * 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 2-aryl-6-phenyl-imidazo°1,2-a!pyridines, leur preparation et leur application en therapeutique
FR2928923B1 (fr) * 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 2-heteroaryl-6-phenyl-imidazo °1,2-a!pyridines, leur preparation et leur application en therapeutiques
FR2928924B1 (fr) * 2008-03-21 2010-04-23 Sanofi Aventis Derives polysubstitues de 6-heteroaryle-imidazo°1,2-a! pyridines, leur preparation et leur application en therapeutique
US8198449B2 (en) * 2008-09-11 2012-06-12 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
FR2950344B1 (fr) * 2009-09-18 2011-11-25 Sanofi Aventis Derives de 5-phenyl-pyrazolopyridine, leur preparation et leur aplication en therapeutique.

Also Published As

Publication number Publication date
FR2953520A1 (fr) 2011-06-10
MY157676A (en) 2016-07-15
EA020652B1 (ru) 2014-12-30
JO3098B1 (ar) 2017-03-15
AU2010326429A1 (en) 2012-06-21
KR20120103672A (ko) 2012-09-19
CL2012001461A1 (es) 2012-10-12
TW201129564A (en) 2011-09-01
EP2507238B1 (fr) 2013-07-31
AU2010326429B2 (en) 2016-07-14
TWI481606B (zh) 2015-04-21
CN102762559A (zh) 2012-10-31
US20120245164A1 (en) 2012-09-27
EP2507238A1 (fr) 2012-10-10
JP5738310B2 (ja) 2015-06-24
JP2013512884A (ja) 2013-04-18
CN102762559B (zh) 2014-11-05
CO6551713A2 (es) 2012-10-31
MX2012006421A (es) 2012-10-09
KR101696959B1 (ko) 2017-01-16
FR2953520B1 (fr) 2011-11-25
NZ600368A (en) 2013-12-20
CA2782704C (fr) 2018-01-02
MA33893B1 (fr) 2013-01-02
UY33079A (es) 2011-06-01
WO2011067544A1 (fr) 2011-06-09
BR112012013511A2 (pt) 2016-06-07
IL220060A (en) 2015-05-31
US8680096B2 (en) 2014-03-25
CA2782704A1 (fr) 2011-06-09
SG181138A1 (en) 2012-07-30
AR079250A1 (es) 2012-01-04
HK1169984A1 (en) 2013-02-15

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