KR20130122531A - Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드 - Google Patents

Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드 Download PDF

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KR20130122531A
KR20130122531A KR1020127033660A KR20127033660A KR20130122531A KR 20130122531 A KR20130122531 A KR 20130122531A KR 1020127033660 A KR1020127033660 A KR 1020127033660A KR 20127033660 A KR20127033660 A KR 20127033660A KR 20130122531 A KR20130122531 A KR 20130122531A
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optionally substituted
compound
alkyl
aryl
heteroaryl
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Korean (ko)
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피. 제프리. 콘
크레이그 더블유. 린즐리
숀 알. 스타우퍼
야 저우
제이슨 만카
그레고르 제임스 맥도날드
호세 마누엘 바르톨로메-네브레다
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벤더르빌트 유니버시티
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic 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
    • C07D213/02—Heterocyclic 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
    • C07D213/04—Heterocyclic 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
    • C07D213/60—Heterocyclic 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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    • 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]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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

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  • 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)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Anesthesiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
KR1020127033660A 2010-05-24 2011-05-24 Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드 Withdrawn KR20130122531A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34779510P 2010-05-24 2010-05-24
US61/347,795 2010-05-24
PCT/US2011/037775 WO2011149963A1 (en) 2010-05-24 2011-05-24 Substituted-6-methylnicotinamides as mglur5 positive allosteric modulators

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KR20130122531A true KR20130122531A (ko) 2013-11-07

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KR1020127033660A Withdrawn KR20130122531A (ko) 2010-05-24 2011-05-24 Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드

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

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Publication number Priority date Publication date Assignee Title
KR20130122531A (ko) 2010-05-24 2013-11-07 벤더르빌트 유니버시티 Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드
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
US9815850B2 (en) 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods
LT3552017T (lt) 2016-12-09 2022-05-10 Denali Therapeutics Inc. Junginiai, naudotini kaip ripk1 inhibitoriai
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
EP4463229A1 (en) 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide
WO2026072192A1 (en) 2024-09-27 2026-04-02 Alto Neuroscience, Inc. Effective treatment of depression in patients having poor cognition or impaired learning and/or memory with a mglur5 positive allosteric modulator

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JPH06508621A (ja) * 1991-06-12 1994-09-29 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 置換されたピリジン除草剤
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
WO2001078648A2 (en) 2000-04-17 2001-10-25 Dong Wha Pharm. Ind. Co., Ltd. 6-methylnicotinamide derivatives as antiviral agents
US7932272B2 (en) 2003-09-30 2011-04-26 Eisai R&D Management Co., Ltd. Antifungal agent containing heterocyclic compound
EP1715867A4 (en) * 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
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BRPI0620066A2 (pt) * 2005-12-20 2011-11-01 Novartis Ag derivados de ácido nicotìnico como moduladores do receptor de glutamato metabotrópico, processo para preparação dos mesmos, composição farmacêutica e uso dos referidos derivados
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
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KR20100033981A (ko) * 2007-06-03 2010-03-31 벤더르빌트 유니버시티 벤즈아미드 대사성 글루타민산염 수용체5 양성 알로스테릭 조절자 및 이의 제조 및 사용방법
US8034806B2 (en) * 2007-11-02 2011-10-11 Vanderbilt University Bicyclic mGluR5 positive allosteric modulators and methods of making and using same
CA2774981A1 (en) * 2009-09-21 2011-03-24 Vanderbilt University O-benzyl nicotinamide analogs as mglur5 positive allosteric modulators
EP2504279A4 (en) 2009-11-25 2016-07-27 Dynatec Engineering As REACTOR AND METHOD FOR THE PRODUCTION OF SILICONE
KR20130122531A (ko) 2010-05-24 2013-11-07 벤더르빌트 유니버시티 Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드

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Publication number Publication date
EP2575461A1 (en) 2013-04-10
JP2013526610A (ja) 2013-06-24
CA2799966A1 (en) 2011-12-01
CN103037693A (zh) 2013-04-10
US20110294858A1 (en) 2011-12-01
US8969389B2 (en) 2015-03-03
AU2011258389A1 (en) 2012-12-06
MX2012013560A (es) 2013-03-05
WO2011149963A1 (en) 2011-12-01
EA201291327A1 (ru) 2013-05-30
EP2575461A4 (en) 2013-12-18

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Patent event date: 20121224

Patent event code: PA01051R01D

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