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

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—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
    • A61P25/22—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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • 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
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P25/36—Opioid-abuse
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (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 (enExample)
EP (1) EP1912979B1 (enExample)
JP (2) JP2008540637A (enExample)
KR (1) KR20080014046A (enExample)
CN (1) CN101218234B (enExample)
AT (1) ATE513828T1 (enExample)
AU (1) AU2006248657B2 (enExample)
BR (1) BRPI0610059A2 (enExample)
CA (1) CA2608324A1 (enExample)
CY (1) CY1111859T1 (enExample)
DK (1) DK1912979T3 (enExample)
EA (1) EA014081B1 (enExample)
ES (1) ES2367663T3 (enExample)
GB (1) GB0510141D0 (enExample)
IL (1) IL187187A0 (enExample)
MX (1) MX2007014403A (enExample)
NO (1) NO20076480L (enExample)
NZ (1) NZ564202A (enExample)
PL (1) PL1912979T3 (enExample)
PT (1) PT1912979E (enExample)
UA (1) UA92494C2 (enExample)
WO (1) WO2006123257A2 (enExample)
ZA (1) ZA200710279B (enExample)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2006123255A2 (en) * 2005-05-18 2006-11-23 Addex Pharma Sa Substituted oxadiazole derivatives as positive allosteric modulators of metabotropic glutamate receptors
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
US20100144756A1 (en) 2007-07-13 2010-06-10 Bolea Christelle Novel heteroaromatic derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors
ES2499018T3 (es) 2007-09-20 2014-09-26 Irm Llc Compuestos y composiciones como moduladores de la actividad 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
EP2393780A1 (en) * 2009-02-04 2011-12-14 Recordati Ireland Limited Heterocyclic derivatives as m-glu5 antagonists
WO2010098866A1 (en) 2009-02-27 2010-09-02 Supergen, Inc. Cyclopentathiophene/cyclohexathiophene dna methyltransferase inhibitors
WO2010124055A1 (en) * 2009-04-23 2010-10-28 Merck Sharp & Dohme Corp. 2-alkyl piperidine mglur5 receptor modulators
GB0912946D0 (en) * 2009-07-24 2009-09-02 Addex Pharmaceuticals Sa New compounds 5
CA2784830C (en) 2009-12-18 2018-03-27 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
CN102762572A (zh) 2010-02-01 2012-10-31 诺瓦提斯公司 作为CRF-1受体拮抗剂的吡唑并[5,1b]*唑衍生物
EP2531490B1 (en) 2010-02-02 2014-10-15 Novartis AG Cyclohexyl amide derivatives as crf receptor antagonists
CA2798330A1 (en) 2010-05-05 2011-11-10 Infinity Pharmaceuticals, Inc. Tetrazolones as inhibitors of fatty acid synthase
NZ618795A (en) 2011-05-13 2015-07-31 Array Biopharma Inc Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
EP2744807A4 (en) 2011-08-15 2015-03-04 Intermune Inc COMPOUNDS AS LYSOPHOSPHIC ACID RECEPTOR ANTAGONISTS
EP2794565B1 (en) 2011-12-21 2017-07-26 Novira Therapeutics Inc. Hepatitis b antiviral agents
CA2881057C (en) 2012-08-28 2020-10-27 Janssen Sciences Ireland Uc Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis b
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl 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
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
CA2891334C (en) 2012-11-13 2021-10-19 Array Biopharma Inc. Bicyclic urea, thiourea, guanidine and cyanoguanidine compounds useful for the treatment of pain
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
ME02990B (me) 2012-11-13 2018-10-20 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze
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
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
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
JP6466348B2 (ja) 2013-02-28 2019-02-06 ヤンセン・サイエンシズ・アイルランド・アンリミテッド・カンパニー スルファモイル−アリールアミドおよびb型肝炎を処置するための医薬品としてのその使用
US8993771B2 (en) 2013-03-12 2015-03-31 Novira Therapeutics, Inc. Hepatitis B antiviral agents
HUE033542T2 (en) 2013-04-03 2017-12-28 Janssen Sciences Ireland Uc Their use as medicaments for the treatment of N-phenylcarboxamide derivatives and hepatitis B
TW202126620A (zh) 2013-05-17 2021-07-16 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
WO2015011281A1 (en) 2013-07-25 2015-01-29 Janssen R&D Ireland Glyoxamide substituted pyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b
MX368158B (es) 2013-10-23 2019-09-20 Janssen Sciences Ireland Uc Derivados de carboxamida y su uso como medicamentos para el tratamiento de la hepatitis b.
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
US9169212B2 (en) 2014-01-16 2015-10-27 Novira Therapeutics, Inc. Azepane derivatives and methods of treating hepatitis B infections
JP6553059B2 (ja) 2014-02-05 2019-07-31 ノヴィラ・セラピューティクス・インコーポレイテッド Hbv感染の治療のための併用療法
PL3102572T3 (pl) 2014-02-06 2019-04-30 Janssen Sciences Ireland Uc Pochodne sulfamoilopirolamidu i ich zastosowanie jako leki do leczenia wirusowego zapalenia wątroby typu B
US9400280B2 (en) 2014-03-27 2016-07-26 Novira Therapeutics, Inc. Piperidine derivatives and methods of treating hepatitis B infections
CN106459013B (zh) 2014-05-15 2019-10-25 阵列生物制药公司 作为trka激酶抑制剂的化合物及其用途
EP3271019A1 (en) 2015-03-19 2018-01-24 Novira Therapeutics Inc. Azocane and azonane derivatives and methods of treating hepatitis b infections
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
AR106192A1 (es) 2015-09-29 2017-12-20 Novira Therapeutics Inc Formas cristalinas de un agente antiviral contra la hepatitis b
WO2017181141A2 (en) 2016-04-15 2017-10-19 Novira Therapeutics, Inc. 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
WO2019160882A1 (en) 2018-02-13 2019-08-22 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
SG11202007097QA (en) 2018-03-14 2020-08-28 Janssen Sciences Ireland Unlimited Co Capsid assembly modulator dosing regimen
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
PE20210642A1 (es) 2018-07-13 2021-03-23 Gilead Sciences Inc Inhibidores de pd-1/pd-l1
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)
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
AU2019387370A1 (en) 2018-11-30 2021-06-10 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
AU2020223865A1 (en) 2019-02-22 2021-07-15 Janssen Sciences Ireland Unlimited Company Amide derivatives useful in the treatment of HBV infection or HBV-induced diseases
BR112021021454A2 (pt) 2019-05-06 2021-12-21 Janssen Sciences Ireland Unlimited Co Derivados de amida úteis no tratamento da infecção por hbv ou doenças induzidas por hbv
PH12022551379A1 (en) 2019-12-06 2023-05-03 Vertex Pharma Substituted tetrahydrofurans as modulators of sodium channels
WO2021138540A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer
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
SI4347031T1 (sl) 2021-06-04 2026-01-30 Vertex Pharmaceuticals Incorporated N-(hidroksialkil (hetero)aril) tetrahidrofuran karboksamidi kot modulatorji natrijevih kanalčkov
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
CN117756793A (zh) * 2022-12-16 2024-03-26 四川大学 1,2,4-杂二唑衍生物及其用途

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
WO2003093297A2 (en) * 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
WO2003093236A1 (en) * 2002-05-02 2003-11-13 Euro-Celtique, S.A. 1-(pyrid-2-yl)-piperazine compounds as metabotropic glutamate receptor inhibitor
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
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
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

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
DE60022386T2 (de) * 1999-12-16 2006-06-22 Schering Corp. Substituierte imidazole als neuropeptide y y5 rezeptor antagonisten
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
EP1289955B1 (en) * 2000-06-16 2005-04-13 Smithkline Beecham Plc Piperidines for use as orexin receptor antagonists
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
CA2462289C (en) * 2001-10-04 2010-02-23 Nicholas D. Cosford Heteroaryl substituted tetrazole modulators of metabotropic glutamate receptor-5
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
EP1658291B1 (en) * 2003-08-25 2013-10-02 Dogwood Pharmaceuticals, Inc. Substituted 8-heteroaryl xanthines
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
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
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
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
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

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

Similar Documents

Publication Publication Date Title
CN101218234B (zh) 作为代谢型谷氨酸受体的正变构调节剂的吡咯衍生物
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