EA201291327A1 - Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5 - Google Patents

Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5

Info

Publication number
EA201291327A1
EA201291327A1 EA201291327A EA201291327A EA201291327A1 EA 201291327 A1 EA201291327 A1 EA 201291327A1 EA 201291327 A EA201291327 A EA 201291327A EA 201291327 A EA201291327 A EA 201291327A EA 201291327 A1 EA201291327 A1 EA 201291327A1
Authority
EA
Eurasian Patent Office
Prior art keywords
mglur5
substituted
compounds
positive allosteric
allosteric modulators
Prior art date
Application number
EA201291327A
Other languages
English (en)
Inventor
П. Джеффри Конн
Крейг У. Линдсли
Шон Р. Стоффер
Я Чжоу
Джейсон Манка
Грегор Джеймс Макдоналд
Хосе Мануэль Бартоломе-Небреда
Original Assignee
Вандербилт Юниверсити
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 Вандербилт Юниверсити filed Critical Вандербилт Юниверсити
Publication of EA201291327A1 publication Critical patent/EA201291327A1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P3/08Drugs 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

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

Abstract

В одном аспекте изобретение относится к замещенным аналогам 6-метилникотинамида, их производным и родственным соединениям, которые можно использовать в качестве позитивных аллостерических модуляторов метаботропного глутаматного рецептора подтипа 5 (mGluR5); способам синтеза соединений; фармацевтическим композициям, содержащим соединения; и способам лечения неврологических и психиатрических расстройств, связанных с дисфункцией глутамата, с использованием соединений и композиций. Этот реферат предназначен для быстрого ознакомления при поиске информации в конкретной области и не подразумевает какого-либо ограничения настоящего изобретения.
EA201291327A 2010-05-24 2011-05-24 Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5 EA201291327A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US34779510P 2010-05-24 2010-05-24
PCT/US2011/037775 WO2011149963A1 (en) 2010-05-24 2011-05-24 Substituted-6-methylnicotinamides as mglur5 positive allosteric modulators

Publications (1)

Publication Number Publication Date
EA201291327A1 true EA201291327A1 (ru) 2013-05-30

Family

ID=45004338

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201291327A EA201291327A1 (ru) 2010-05-24 2011-05-24 Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5

Country Status (10)

Country Link
US (1) US8969389B2 (ru)
EP (1) EP2575461A4 (ru)
JP (1) JP2013526610A (ru)
KR (1) KR20130122531A (ru)
CN (1) CN103037693A (ru)
AU (1) AU2011258389A1 (ru)
CA (1) CA2799966A1 (ru)
EA (1) EA201291327A1 (ru)
MX (1) MX2012013560A (ru)
WO (1) WO2011149963A1 (ru)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8969389B2 (en) 2010-05-24 2015-03-03 Vanderbilt University Substituted 6-methylnicotinamides as mGluR5 positive allosteric modulators

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130252943A1 (en) * 2012-02-29 2013-09-26 Vanderbilt University Bicyclic oxazole lactams as allosteric modulators of mglur5 receptors
CN106146391A (zh) * 2015-04-15 2016-11-23 中国科学院上海药物研究所 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途
US9987242B2 (en) 2015-05-05 2018-06-05 Northwestern University Treatment of Levodopa-induced Dyskinesias
CN109071504B (zh) 2016-02-05 2022-03-08 戴纳立制药公司 受体相互作用蛋白激酶1的抑制剂
DK3552017T3 (da) 2016-12-09 2022-05-16 Denali Therapeutics Inc Forbindelser, der er anvendelige som ripk1-inhibitorer
CN114437025B (zh) * 2020-11-05 2023-08-25 上海零诺生物科技有限公司 消旋6-甲基烟碱及其制备方法、以及应用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1992022203A1 (en) * 1991-06-12 1992-12-23 E.I. Du Pont De Nemours And Company Substituted pyridine herbicides
EP0533130A1 (de) * 1991-09-19 1993-03-24 Hoechst Aktiengesellschaft 2-Hydroxymethylpyridine, die entsprechenden Pyridin-N-oxide und ihre Derivate, Verfahren zu ihrer Herstellung sowie deren Verwendung
GB9417532D0 (en) 1994-08-31 1994-10-19 Zeneca Ltd Aromatic compounds
AU4890301A (en) * 2000-04-17 2001-10-30 Dong Wha Pharmaceutical Industrial Co., Ltd. 6-methylnicotinamide derivatives as antiviral agents
WO2005033079A1 (ja) 2003-09-30 2005-04-14 Eisai Co., Ltd. ヘテロ環化合物を含有する新規な抗真菌剤
CA2555402A1 (en) * 2004-02-12 2005-09-01 Celine Bonnefous Bipyridyl amides as modulators of metabotropic glutamate receptor-5
AU2006329007A1 (en) * 2005-12-20 2007-06-28 Novartis Ag Nicotinic acid derivatives as modulators of metabotropic glutamate receptors
CN101321731A (zh) * 2005-12-20 2008-12-10 诺瓦提斯公司 作为代谢型谷氨酸受体调节剂的烟酸衍生物
CN101600715A (zh) * 2006-12-21 2009-12-09 辉瑞产品公司 具有血管紧张素II受体拮抗作用和PPARγ活化活性的化合物
CA2671943A1 (en) * 2006-12-21 2008-07-17 Pfizer Products Inc. Compounds having both angiotensin ii receptor antagonism and ppary activating activities
WO2008151184A1 (en) 2007-06-03 2008-12-11 Vanderbilt University Benzamide mglur5 positive allosteric modulators and methods of making and using same
US8034806B2 (en) * 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
IN2012DN03322A (ru) * 2009-09-21 2015-10-23 Univ Vanderbilt
US20120251427A1 (en) 2009-11-25 2012-10-04 Josef Filtvedt Reactor and method for production of silicon
KR20130122531A (ko) 2010-05-24 2013-11-07 벤더르빌트 유니버시티 Mglur5 양성 알로스테릭 조절물로서 치환된 6­메틸니코틴아미드

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8969389B2 (en) 2010-05-24 2015-03-03 Vanderbilt University Substituted 6-methylnicotinamides as mGluR5 positive allosteric modulators

Also Published As

Publication number Publication date
KR20130122531A (ko) 2013-11-07
MX2012013560A (es) 2013-03-05
EP2575461A1 (en) 2013-04-10
US20110294858A1 (en) 2011-12-01
WO2011149963A1 (en) 2011-12-01
JP2013526610A (ja) 2013-06-24
CN103037693A (zh) 2013-04-10
EP2575461A4 (en) 2013-12-18
AU2011258389A1 (en) 2012-12-06
CA2799966A1 (en) 2011-12-01
US8969389B2 (en) 2015-03-03

Similar Documents

Publication Publication Date Title
EA200971143A1 (ru) Бензамидные mglur5 позитивные аллостерические модуляторы и способы их получения и применения
EA201291327A1 (ru) Замещенные 6-метилникотинамиды как позитивные аллостерические модуляторы mglur5
WO2012118563A3 (en) 6-alkyl-n-(pyridin-2-yl)-4-aryloxypicolinamide analogs as mglur5 negative allosteric modulators and methods of making and using the same
EA201190302A1 (ru) ПРОИЗВОДНЫЕ 7-АРИЛ-1,2,4-ТРИАЗОЛО[4,3-а]ПИРИДИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЛОЖИТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2
MX2011005242A (es) Derivados de indol y benzoxazina como moduladores de los receptores de glutamato metabotropicos.
EA201001724A1 (ru) Производные изоксазола и их применение в качестве потенциирующих средств для метаботропных глутаматных рецепторов
MA34078B1 (fr) Derives d'arylethynyle
EA200870423A1 (ru) Производные триазолпиразинов, применимые в качестве противораковых агентов
EA201390947A1 (ru) Соединения 2-амино-4-арилтиазола в качестве антагонистов trpa1
EA201592252A1 (ru) 6,7-ДИГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИН-4(5H)-ОНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ОТРИЦАТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ MGLUR2
EA200970612A1 (ru) Производные индола в качестве агонистов рецептора s1p1
EA200901160A1 (ru) Производные 3-циано-4-(4-тетрагидропиранфенил)пиридин-2-она
EA200901098A1 (ru) Производные тиазола в качестве модуляторов сопряженных с g-белком рецепторов
WO2015200682A8 (en) Substituted 4-alkoxypicolinamide analogs ds mglur5 negative allosteric modulators
MX2010002760A (es) Derivados de isoquinolinilo e isoindolinilo como antagonistas de la histamina-3.
EA201590228A1 (ru) Антагонисты 5-ht3 рецептора
WO2014055928A3 (en) Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
WO2014055934A3 (en) Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
EA201270428A1 (ru) Замещенные n-фенил-1-(4-пиридинил)-1н-пиразол-3-амины
WO2012125732A8 (en) Substituted imadazapyrinidin-5(6h)-ones as allosteric modulators of mglur5 receptors
EA201290534A1 (ru) Бициклические тиазолы в качестве аллостерических модуляторов mglur5 рецепторов
MX2013006768A (es) Moduladores de receptor de glucagon.
IN2012DN03322A (ru)
EA201690162A1 (ru) Этинильные производные в качестве антагонистов метаботропного глутаматного рецептора
EA201690535A1 (ru) 1,2,4-ТРИАЗОЛО[4,3-a]ПИРИДИНОВЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ПОЛОЖИТЕЛЬНЫХ АЛЛОСТЕРИЧЕСКИХ МОДУЛЯТОРОВ РЕЦЕПТОРОВ mGluR2