EA014081B1 - Производные пиррола в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов - Google Patents

Производные пиррола в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов Download PDF

Info

Publication number
EA014081B1
EA014081B1 EA200702470A EA200702470A EA014081B1 EA 014081 B1 EA014081 B1 EA 014081B1 EA 200702470 A EA200702470 A EA 200702470A EA 200702470 A EA200702470 A EA 200702470A EA 014081 B1 EA014081 B1 EA 014081B1
Authority
EA
Eurasian Patent Office
Prior art keywords
oxadiazol
piperidin
methanone
pyrrol
mmol
Prior art date
Application number
EA200702470A
Other languages
English (en)
Russian (ru)
Other versions
EA200702470A1 (ru
Inventor
Стефания Гаглиарди
Эммануэль Ле Поул
Йан Лингард
Джиованни Паломби
Сонья Мария Поли
Джен-Филиппе Рошер
Original Assignee
Аддекс Фарма Са
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 Аддекс Фарма Са filed Critical Аддекс Фарма Са
Publication of EA200702470A1 publication Critical patent/EA200702470A1/ru
Publication of EA014081B1 publication Critical patent/EA014081B1/ru

Links

Classifications

    • 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
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61P25/14Drugs 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
    • A61P25/14Drugs 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
    • A61P25/22Anxiolytics
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32Alcohol-abuse
    • 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
    • A61P25/34Tobacco-abuse
    • 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
    • A61P25/36Opioid-abuse
    • 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]
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Fats And Perfumes (AREA)
  • Pyrrole Compounds (AREA)
EA200702470A 2005-05-18 2006-05-17 Производные пиррола в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов EA014081B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0510141.5A GB0510141D0 (en) 2005-05-18 2005-05-18 Novel compounds B3
PCT/IB2006/002047 WO2006123257A2 (en) 2005-05-18 2006-05-17 Phenyl-3-{(3-(1h-pyrrol-2-yl)-[1, 2 , 4]0xadiaz0l-5-yl]piperidin-1-yl}-methanone derivatives and related compounds as positive allosteric modulators of metabotropic glutamate receptors

Publications (2)

Publication Number Publication Date
EA200702470A1 EA200702470A1 (ru) 2008-06-30
EA014081B1 true EA014081B1 (ru) 2010-08-30

Family

ID=34708379

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200702470A EA014081B1 (ru) 2005-05-18 2006-05-17 Производные пиррола в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов

Country Status (23)

Country Link
US (1) US20090203737A1 (https=)
EP (1) EP1912979B1 (https=)
JP (2) JP2008540637A (https=)
KR (1) KR20080014046A (https=)
CN (1) CN101218234B (https=)
AT (1) ATE513828T1 (https=)
AU (1) AU2006248657B2 (https=)
BR (1) BRPI0610059A2 (https=)
CA (1) CA2608324A1 (https=)
CY (1) CY1111859T1 (https=)
DK (1) DK1912979T3 (https=)
EA (1) EA014081B1 (https=)
ES (1) ES2367663T3 (https=)
GB (1) GB0510141D0 (https=)
IL (1) IL187187A0 (https=)
MX (1) MX2007014403A (https=)
NO (1) NO20076480L (https=)
NZ (1) NZ564202A (https=)
PL (1) PL1912979T3 (https=)
PT (1) PT1912979E (https=)
UA (1) UA92494C2 (https=)
WO (1) WO2006123257A2 (https=)
ZA (1) ZA200710279B (https=)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1893606A2 (en) * 2005-05-18 2008-03-05 Addex Pharma SA Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
GB0510141D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B3
GB0510140D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B2
GB0510139D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510142D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds A1
GB0622202D0 (en) * 2006-11-07 2006-12-20 Addex Pharmaceuticals Sa Novel compounds
JP2010533147A (ja) 2007-07-13 2010-10-21 アデックス ファルマ エス.エイ. 代謝調節型グルタミン酸レセプターのモジュレーターとしてのピラゾール誘導体
BRPI0817211A2 (pt) 2007-09-20 2017-05-16 Irm Llc composto composições como moduladores da atividade de gpr119
AR072297A1 (es) 2008-06-27 2010-08-18 Novartis Ag Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona.
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
US8349852B2 (en) 2009-01-13 2013-01-08 Novartis Ag Quinazolinone derivatives useful as vanilloid antagonists
US20100317630A1 (en) * 2009-02-04 2010-12-16 Recordati Ireland Limited Novel heterocyclic compounds as mglu5 antagonists
WO2010098866A1 (en) 2009-02-27 2010-09-02 Supergen, Inc. Cyclopentathiophene/cyclohexathiophene dna methyltransferase inhibitors
EP2421370A4 (en) * 2009-04-23 2012-12-12 Merck Sharp & Dohme 2-alkyl-piperidine-mGluR5 receptor MODULATORS
GB0912946D0 (en) 2009-07-24 2009-09-02 Addex Pharmaceuticals Sa New compounds 5
US8772301B2 (en) 2009-12-18 2014-07-08 Sunovion Pharmaceuticals, Inc. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
AR080056A1 (es) 2010-02-01 2012-03-07 Novartis Ag Derivados de ciclohexil-amida como antagonistas de los receptores de crf
JP2013518085A (ja) 2010-02-01 2013-05-20 ノバルティス アーゲー CRF−1受容体アンタゴニストとしてのピラゾロ[5,1b]オキサゾール誘導体
JP5748777B2 (ja) 2010-02-02 2015-07-15 ノバルティス アーゲー Crf受容体アンタゴニストとしてのシクロヘキシルアミド誘導体
CA2798330A1 (en) 2010-05-05 2011-11-10 Infinity Pharmaceuticals, Inc. Tetrazolones as inhibitors of fatty acid synthase
CA2835835C (en) 2011-05-13 2019-04-02 Array Biopharma Inc. Pyrrolidinyl urea and pyrrolidinyl thiourea compounds as trka kinase inhibitors
JP2014525932A (ja) 2011-08-15 2014-10-02 インターミューン, インコーポレイテッド リゾホスファチド酸レセプターアンタゴニスト
BR112014015197A8 (pt) 2011-12-21 2017-06-13 Novira Therapeutics Inc agentes antivirais de hepatite b
KR102271574B1 (ko) 2012-08-28 2021-07-01 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 설파모일-아릴아미드 및 b형 간염 치료제로서의 그 용도
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
MX374242B (es) 2012-11-13 2025-03-05 Array Biopharma Inc Compuestos de n-pirrolidinil, n' -pirazolil-urea, tiourea, guanidina y cianoguanidina como inhibidores de trka cinasa.
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
RS55593B1 (sr) 2012-11-13 2017-06-30 Array Biopharma Inc Jedinjenja biciklične uree, tiouree, guanidina i cijanoguanidina korisna za lečenje bola
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078378A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014131847A1 (en) 2013-02-28 2014-09-04 Janssen R&D Ireland Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
US8993771B2 (en) 2013-03-12 2015-03-31 Novira Therapeutics, Inc. Hepatitis B antiviral agents
MX353412B (es) 2013-04-03 2018-01-10 Janssen Sciences Ireland Uc Derivados de n-fenil-carboxamida y su uso como medicamentos para el tratamiento de la hepatitis b.
TWI733288B (zh) 2013-05-17 2021-07-11 愛爾蘭商健生科學愛爾蘭無限公司 胺磺醯基吡咯醯胺衍生物及其作為用於治療b型肝炎藥物的用途
HRP20180791T1 (hr) 2013-07-25 2018-09-07 Janssen Sciences Ireland Uc Glioksamid supstituirani derivati pirolamida i njihova uporaba kao lijekova za liječenje hepatitisa b
CA2923712C (en) 2013-10-23 2021-11-02 Janssen Sciences Ireland Uc Carboxamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US9181288B2 (en) 2014-01-16 2015-11-10 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
US10392349B2 (en) 2014-01-16 2019-08-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
CA2936947A1 (en) 2014-02-05 2015-08-13 Novira Therapeutics, Inc. Combination therapy for treatment of hbv infections
TW201620893A (zh) 2014-02-06 2016-06-16 健生科學愛爾蘭無限公司 磺醯胺基吡咯醯胺衍生物及其用作治療b型肝炎之醫藥品的用途
US9400280B2 (en) 2014-03-27 2016-07-26 Novira Therapeutics, Inc. Piperidine derivatives and methods of treating hepatitis B infections
MA40434B1 (fr) 2014-05-15 2019-09-30 Array Biopharma Inc 1-((3s,4r)-4-(3-fluorophényl)-1-(2-méthoxyéthyl)pyrrolidin-3-yl)-3-(4-méthyl-3-(2-méthylpyrimidin-5-yl)-1-phényl-1h-pyrazol-5-yl)urée comme inhibiteur de la kinase trka
JP2018510159A (ja) 2015-03-19 2018-04-12 ノヴィラ・セラピューティクス・インコーポレイテッド アゾカン及びアゾナン誘導体及びb型肝炎感染症の治療法
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
TW201718496A (zh) 2015-09-29 2017-06-01 諾維拉治療公司 B型肝炎抗病毒劑之晶型
AU2017248828A1 (en) 2016-04-15 2018-11-01 Janssen Sciences Ireland Uc Combinations and methods comprising a capsid assembly inhibitor
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
CR20200347A (es) 2018-02-13 2020-09-23 Gilead Sciences Inc Inhibidores pd-1/pd-l1
MX2020009531A (es) 2018-03-14 2020-10-05 Janssen Sciences Ireland Unlimited Co Regimen posologico del modulador del ensamblaje de la capside.
TWI712412B (zh) 2018-04-19 2020-12-11 美商基利科學股份有限公司 Pd‐1/pd‐l1抑制劑
SG11202012425QA (en) 2018-07-13 2021-01-28 Gilead Sciences Inc Pd-1/pd-l1 inhibitors
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
WO2020086556A1 (en) 2018-10-24 2020-04-30 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
CA3121202A1 (en) 2018-11-30 2020-06-04 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
US12590083B2 (en) * 2019-01-25 2026-03-31 University Of Virginia Patent Foundation Inhibitors of spinster homolog 2 (SPNS2) for use in therapy
WO2020169784A1 (en) 2019-02-22 2020-08-27 Janssen Sciences Ireland Unlimited Company Amide derivatives useful in the treatment of hbv infection or hbv-induced diseases
AR119732A1 (es) 2019-05-06 2022-01-05 Janssen Sciences Ireland Unlimited Co Derivados de amida útiles en el tratamiento de la infección por vhb o de enfermedades inducidas por vhb
BR112022010924A2 (pt) 2019-12-06 2022-09-06 Vertex Pharma Tetra-hidrofuranos substituídos como moduladores de canais de sódio
CN115210229A (zh) 2020-01-03 2022-10-18 博格有限责任公司 多环酰胺作为治疗癌症的ube2k调节剂
WO2022069953A1 (en) * 2020-09-29 2022-04-07 Ranjith Siddaraj Synthesis and characterization of (s)-3-(5- fluoropyridin-2-yl)-5-(piperidin-3-yl)-l,2,4-oxadiazole derivatives and their secretory phospholipase a2 (spla2) inhibitor activity
SMT202500481T1 (it) 2021-06-04 2026-01-12 Vertex Pharma N-(idrossialchil(etero)aril)tetraidrofuran carbossammidi come modulatori di canali del sodio
WO2024059207A2 (en) * 2022-09-15 2024-03-21 Vanderbilt University Pyrazoloether analogs as mglu5 negative allosteric modulators and methods of making and using the same

Citations (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003027080A1 (en) * 2001-09-21 2003-04-03 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
EP1300396A1 (en) * 2000-06-12 2003-04-09 Eisai Co., Ltd. 1,2-dihydropyridine compounds, process for preparation of the same and use thereof
WO2003037888A1 (en) * 2001-09-21 2003-05-08 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
WO2003087304A2 (en) * 2002-04-04 2003-10-23 Biogen, Inc. Tri-substituted heteroaryls and methods of making and using the same
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
WO2003093297A2 (en) * 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
WO2004014902A2 (en) * 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
WO2004029044A1 (en) * 2002-09-24 2004-04-08 Euro-Celtique, S.A. Pyrimidine compounds as therapeutic agents
WO2004048334A1 (en) * 2002-11-26 2004-06-10 Pfizer Products Inc. Phenyl substituted piperidine compounds for use as ppar activators
WO2004058754A1 (en) * 2002-12-24 2004-07-15 Euro-Celtique S.A. Benzoazolypiperazine derivatives having mglur1- and mglur5-antagonistic activity
WO2005009988A1 (en) * 2003-07-24 2005-02-03 Euro-Celtique S.A. Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain
WO2005044797A1 (en) * 2003-11-06 2005-05-19 Addex Pharmaceuticals Sa Allosteric modulators of metabotropic glutamate receptors
WO2005074934A1 (en) * 2004-02-04 2005-08-18 Merck Patent Gmbh Thiazolylimidazole derivatives and their use as inhibitors of microsmal triglyce ride transfer protein
WO2005115389A2 (en) * 2004-05-25 2005-12-08 Pfizer Products Inc. Specific ppar agonists for treating negative energy balance
WO2006036015A2 (en) * 2004-09-29 2006-04-06 Mitsubishi Pharma Corporation 6- (pyridinyl) -4-pyrimidone derivates as tau protein kinase 1 inhibitors
WO2006044509A2 (en) * 2004-10-15 2006-04-27 Biogen Idec Ma Inc. Methods of treating vascular injuries
WO2006048771A1 (en) * 2004-11-04 2006-05-11 Addex Pharmaceuticals Sa Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
WO2006065601A2 (en) * 2004-12-15 2006-06-22 Merck & Co., Inc. Inhibitors of akt activity
WO2006123255A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
WO2006123257A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Phenyl-3-{(3-(1h-pyrrol-2-yl)-[1, 2 , 4]0xadiaz0l-5-yl]piperidin-1-yl}-methanone derivatives and related compounds as positive allosteric modulators of metabotropic glutamate receptors
WO2006123249A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Novel oxadiazole derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3509153A (en) * 1967-03-24 1970-04-28 Miles Lab 5-phenyl (or 5-phenylalkyl)-2-(omega-(4-phenyl-1-piperazinyl)alkyl)tetrazoles
US3991064A (en) * 1975-01-17 1976-11-09 Warner-Lambert Company Benzonaphthyridines
US3966748A (en) * 1975-05-08 1976-06-29 American Cyanamid Company Para-fluorophenyl-N-heterocyclic substituted butanes
US5338969A (en) * 1991-06-27 1994-08-16 Texas Instruments, Incorporated Unerasable programmable read-only memory
US6846839B1 (en) * 1995-06-07 2005-01-25 Sugen, Inc. Methods for treating diseases and disorders related to unregulated angiogenesis and/or vasculogenesis
GB9603755D0 (en) * 1996-02-22 1996-04-24 Pfizer Ltd Therapeutic agents
US6437146B1 (en) * 1998-09-25 2002-08-20 Fujisawa Pharmaceutical Co., Ltd. Oxazole compounds as prostaglandin e2 agonists or antagonists
US7217714B1 (en) * 1998-12-23 2007-05-15 Agouron Pharmaceuticals, Inc. CCR5 modulators
AU2935200A (en) * 1999-04-30 2000-11-17 Pfizer Products Inc. Compounds for the treatment of obesity
EP1237875B1 (en) * 1999-12-16 2005-08-31 Schering Corporation Substituted imidazole neuropeptide y y5 receptor antagonists
AR033517A1 (es) * 2000-04-08 2003-12-26 Astrazeneca Ab Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos
ES2238458T3 (es) * 2000-06-16 2005-09-01 Smithkline Beecham Plc Piperidinas para uso como antagonistas de los receptores de orexina.
US6894063B2 (en) * 2000-09-14 2005-05-17 Schering Corporation Substituted urea neuropeptide Y Y5 Receptor antagonists
US6946476B2 (en) * 2000-12-21 2005-09-20 Schering Corporation Heteroaryl urea neuropeptide Y Y5 receptor antagonists
JP4303109B2 (ja) * 2001-10-04 2009-07-29 メルク エンド カムパニー インコーポレーテッド 代謝共役型グルタミン酸受容体−5のヘテロアリール置換テトラゾール調節剤
EP1452525A4 (en) * 2001-10-30 2005-01-26 Nippon Shinyaku Co Ltd AMIDE DERIVATIVES AND CORRESPONDING MEDICAMENTS
US6806279B2 (en) * 2001-12-17 2004-10-19 Sunesis Pharmaceuticals, Inc. Small-molecule inhibitors of interleukin-2
KR101222364B1 (ko) * 2003-08-25 2013-01-15 트로비스 파마슈티칼스 엘엘씨 치환된 8-헤테로아릴 크산틴
GB0510143D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds A1
US7713998B2 (en) * 2004-11-10 2010-05-11 Ono Pharmaceutical Co., Ltd. Nitrogenous heterocyclic compound and pharmaceutical use thereof
GB0510139D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
GB0510140D0 (en) * 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B2
GB0622202D0 (en) * 2006-11-07 2006-12-20 Addex Pharmaceuticals Sa Novel compounds

Patent Citations (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1300396A1 (en) * 2000-06-12 2003-04-09 Eisai Co., Ltd. 1,2-dihydropyridine compounds, process for preparation of the same and use thereof
WO2003027080A1 (en) * 2001-09-21 2003-04-03 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
WO2003037888A1 (en) * 2001-09-21 2003-05-08 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
WO2003087304A2 (en) * 2002-04-04 2003-10-23 Biogen, Inc. Tri-substituted heteroaryls and methods of making and using the same
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
WO2003093297A2 (en) * 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
WO2004014902A2 (en) * 2002-08-09 2004-02-19 Astrazeneca Ab Compounds having an activity at metabotropic glutamate receptors
WO2004029044A1 (en) * 2002-09-24 2004-04-08 Euro-Celtique, S.A. Pyrimidine compounds as therapeutic agents
WO2004048334A1 (en) * 2002-11-26 2004-06-10 Pfizer Products Inc. Phenyl substituted piperidine compounds for use as ppar activators
WO2004058754A1 (en) * 2002-12-24 2004-07-15 Euro-Celtique S.A. Benzoazolypiperazine derivatives having mglur1- and mglur5-antagonistic activity
WO2005009988A1 (en) * 2003-07-24 2005-02-03 Euro-Celtique S.A. Heteroaryl-tetrahydropiperidyl compounds useful for treating or preventing pain
WO2005044797A1 (en) * 2003-11-06 2005-05-19 Addex Pharmaceuticals Sa Allosteric modulators of metabotropic glutamate receptors
WO2005074934A1 (en) * 2004-02-04 2005-08-18 Merck Patent Gmbh Thiazolylimidazole derivatives and their use as inhibitors of microsmal triglyce ride transfer protein
WO2005115389A2 (en) * 2004-05-25 2005-12-08 Pfizer Products Inc. Specific ppar agonists for treating negative energy balance
WO2006036015A2 (en) * 2004-09-29 2006-04-06 Mitsubishi Pharma Corporation 6- (pyridinyl) -4-pyrimidone derivates as tau protein kinase 1 inhibitors
WO2006044509A2 (en) * 2004-10-15 2006-04-27 Biogen Idec Ma Inc. Methods of treating vascular injuries
WO2006048771A1 (en) * 2004-11-04 2006-05-11 Addex Pharmaceuticals Sa Novel tetrazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
WO2006065601A2 (en) * 2004-12-15 2006-06-22 Merck & Co., Inc. Inhibitors of akt activity
WO2006123255A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
WO2006123257A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Phenyl-3-{(3-(1h-pyrrol-2-yl)-[1, 2 , 4]0xadiaz0l-5-yl]piperidin-1-yl}-methanone derivatives and related compounds as positive allosteric modulators of metabotropic glutamate receptors
WO2006123249A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Novel oxadiazole derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE CA [Online], CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1989, VASVARI-DEBRECZY, LELLE ET AL.: "Nitrogen bridgehead compounds. Part 74. Cyclization of 2-[(2-pyridylamino)methylene]succinates in ethanolic sodium ethoxide. Part 2. Michael addition of pyridyldihydropyrrolones", XP002413099, retrieved from STN, Database accession no. 1989:75220, abstract & JOURNAL OF THE CHEMICAL SOCIETY, PERKIN TRANSACTIONS 1: ORGANIC AND BIO-ORGANIC CHEMISTRY (1972-1999), (7), 2019-22, CODEN: JCPRB4; ISSN: 0300-922X, 1988 *

Also Published As

Publication number Publication date
CN101218234A (zh) 2008-07-09
CA2608324A1 (en) 2006-11-23
ZA200710279B (en) 2009-03-25
WO2006123257A8 (en) 2007-03-15
HK1112909A1 (en) 2008-09-19
DK1912979T3 (da) 2011-08-22
GB0510141D0 (en) 2005-06-22
JP2012184254A (ja) 2012-09-27
US20090203737A1 (en) 2009-08-13
ATE513828T1 (de) 2011-07-15
PT1912979E (pt) 2011-08-22
KR20080014046A (ko) 2008-02-13
CY1111859T1 (el) 2015-11-04
IL187187A0 (en) 2008-02-09
AU2006248657A1 (en) 2006-11-23
JP2008540637A (ja) 2008-11-20
EP1912979A2 (en) 2008-04-23
MX2007014403A (es) 2008-04-21
BRPI0610059A2 (pt) 2010-05-25
UA92494C2 (ru) 2010-11-10
EP1912979B1 (en) 2011-06-22
NZ564202A (en) 2011-04-29
CN101218234B (zh) 2011-12-14
AU2006248657B2 (en) 2012-07-19
PL1912979T3 (pl) 2011-11-30
EA200702470A1 (ru) 2008-06-30
NO20076480L (no) 2008-01-28
WO2006123257A2 (en) 2006-11-23
WO2006123257A3 (en) 2007-05-03
ES2367663T3 (es) 2011-11-07

Similar Documents

Publication Publication Date Title
EA014081B1 (ru) Производные пиррола в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов
EA014904B1 (ru) Новые гетероциклические соединения в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов
CN101218232B (zh) 噁二唑衍生物和它们作为代谢型谷氨酸受体的正变构调节剂的用途
KR20220130127A (ko) Trpml 조절제
JP2008525478A (ja) 神経系及び精神医学系障害の治療のための代謝共役型グルタミン酸受容体アゴニストとしてのピラゾロン化合物
EA015813B1 (ru) Замещенные производные оксадиазола в качестве положительных аллостерических модуляторов метаботропных глутаматных рецепторов
CN102356065B (zh) 作为nk3受体拮抗剂的哌啶衍生物
CN101228155B (zh) 作为代谢型谷氨酸受体的正变构调节剂的取代的*二唑衍生物
HK1112909B (en) Phenyl-{3-(3-(1h-pyrrol-2-yl)-[1,2,4]oxadiazol-5-yl]piperidin-1-yl}-methanone derivatives and related compounds as positive allosteric modulators of metabotropic glutamate receptors

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KZ KG MD TJ TM

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): BY

MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU