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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
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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
    • 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
    • A61P25/20—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
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    • 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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    • 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)
  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine 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

Publications (1)

Publication Number Publication Date
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

Country Status (10)

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)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012013560A (es) 2010-05-24 2013-03-05 Univ Vanderbilt 6-metilnicotinamidas sustituidas como moduladores alostéricos positivos de mglur5.
WO2013130639A1 (en) * 2012-02-29 2013-09-06 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
TWI781920B (zh) 2016-02-05 2022-11-01 美商戴納立製藥公司 化合物、組合物及方法
PL3552017T3 (pl) 2016-12-09 2022-08-08 Denali Therapeutics Inc. Związki użyteczne jako inhibitory RIPK1
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
IL314082A (en) 2022-01-12 2024-09-01 Denali Therapeutics Inc Crystal forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazapin-3-yl)- H4- 1,2,4-triazole-3-carboxamide

Family Cites Families (15)

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Publication number Priority date Publication date Assignee Title
AU2187492A (en) * 1991-06-12 1993-01-12 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
WO2001078648A2 (en) * 2000-04-17 2001-10-25 Dong Wha Pharm. Ind. Co., Ltd. 6-methylnicotinamide derivatives as antiviral agents
EP1669348A4 (en) * 2003-09-30 2009-03-11 Eisai R&D Man Co Ltd NEW ANTIPILIC AGENT CONTAINING A HETEROCYCLIC COMPOUND
JP2007524682A (ja) * 2004-02-12 2007-08-30 メルク　エンド　カムパニー　インコーポレーテッド 代謝調節型グルタミン酸受容体−５の調節物質としてのビピリジルアミド
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
WO2007071358A1 (en) * 2005-12-20 2007-06-28 Novartis Ag Nicotinic acid derivatives as modulators of metabotropic glutamate receptors
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
MX2009006795A (es) 2006-12-21 2009-07-03 Pfizer Prod Inc Compuestos que tienen tanto actividades de antagonismo de receptor de angiotensina ii como actividades activadoras de receptores activados por proliferizador de peroxisomas gamma.
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
EP2482657A4 (en) 2009-09-21 2013-05-15 Univ Vanderbilt O-BENZYL-NICOTINAMIDANALOGA AS POSITIVE ALLOSTERIC MGLUR5 MODULATORS
KR101792562B1 (ko) 2009-11-25 2017-11-02 다이나텍 엔지니어링 에이에스 실리콘의 제조를 위한 반응기 및 방법
MX2012013560A (es) 2010-05-24 2013-03-05 Univ Vanderbilt 6-metilnicotinamidas sustituidas como moduladores alostéricos positivos de mglur5.

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

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Patent event date: 20121224

Patent event code: PA01051R01D

Comment text: International Patent Application

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WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid