CN105612162B - 作为nmda受体活性的调节剂的噻唑并嘧啶酮类 - Google Patents

作为nmda受体活性的调节剂的噻唑并嘧啶酮类 Download PDF

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Publication number
CN105612162B
CN105612162B CN201480055668.4A CN201480055668A CN105612162B CN 105612162 B CN105612162 B CN 105612162B CN 201480055668 A CN201480055668 A CN 201480055668A CN 105612162 B CN105612162 B CN 105612162B
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methyl
pyrimidine
trifluoromethyl
ketone
oxo
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CN105612162A (zh
Inventor
于江
吴国胜
袁步伟
伊莱沙·维尔缪
雅各布·施瓦茨
C·李
本杰明·塞勒斯
马修·沃尔格拉夫
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F Hoffmann La Roche AG
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14Ortho-condensed systems
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/429Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
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    • 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
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    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P9/00Drugs for disorders of the cardiovascular system
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Biomedical Technology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201480055668.4A 2013-10-11 2014-10-08 作为nmda受体活性的调节剂的噻唑并嘧啶酮类 Active CN105612162B (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201480055668.4A CN105612162B (zh) 2013-10-11 2014-10-08 作为nmda受体活性的调节剂的噻唑并嘧啶酮类
CN201810852075.0A CN108929336A (zh) 2013-10-11 2014-10-08 作为nmda受体活性的调节剂的噻唑并嘧啶酮类

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CN2013085031 2013-10-11
CNPCT/CN2013/085031 2013-10-11
CN2014085959 2014-09-05
CNPCT/CN2014/085959 2014-09-05
CN201480055668.4A CN105612162B (zh) 2013-10-11 2014-10-08 作为nmda受体活性的调节剂的噻唑并嘧啶酮类
PCT/EP2014/071522 WO2015052226A1 (en) 2013-10-11 2014-10-08 Thiazolopyrimidinones as modulators of nmda receptor activity

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CN105612162B true CN105612162B (zh) 2018-08-21

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US (2) US9988400B2 (https=)
EP (2) EP3415519A1 (https=)
JP (2) JP6419800B2 (https=)
KR (1) KR102361108B1 (https=)
CN (2) CN105612162B (https=)
BR (1) BR112016007563B1 (https=)
CA (1) CA2926830C (https=)
DK (1) DK3055315T3 (https=)
ES (1) ES2690355T3 (https=)
HR (1) HRP20181596T1 (https=)
HU (1) HUE040651T2 (https=)
LT (1) LT3055315T (https=)
MX (1) MX2016004540A (https=)
PL (1) PL3055315T3 (https=)
PT (1) PT3055315T (https=)
RS (1) RS58047B1 (https=)
RU (1) RU2703273C2 (https=)
SI (1) SI3055315T1 (https=)
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EP3283487B1 (en) * 2015-04-15 2019-10-16 H. Hoffnabb-La Roche Ag Pyridopyrimidinones and their use as nmda receptor modulators
SMT202000534T1 (it) 2015-12-09 2020-11-10 Cadent Therapeutics Inc Modulatori eteroaromatici del recettore nmda e loro usi
EP4006038A1 (en) 2015-12-09 2022-06-01 Cadent Therapeutics, Inc. Thienopyrimidinone nmda receptor modulators and uses thereof
WO2017109709A2 (en) 2015-12-22 2017-06-29 Novartis Ag A high-throughput assay method for identifying allosteric nmda receptor modulators
ES2975336T3 (es) * 2016-12-22 2024-07-04 Novartis Ag Moduladores del receptor NMDA y usos de los mismos
BR112021001967A2 (pt) 2018-08-03 2021-04-27 Cadent Therapeutics, Inc. moduladores de receptor nmda heteroaromáticos e usos dos mesmos
CN111840296B (zh) * 2020-07-22 2021-05-04 华中农业大学 一种5H-噻唑并[3,2-a]嘧啶-5-酮类化合物在制备单胺氧化酶抑制剂中的用途
CN112094267B (zh) * 2020-08-14 2025-06-06 贵州省中国科学院天然产物化学重点实验室(贵州医科大学天然产物化学重点实验室) 1-苯基-吡咯并异喹啉-3-酮类化合物及其制备方法和应用
EP4032896A1 (en) * 2021-01-20 2022-07-27 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Thiazolopyrimidones as inhibitors of ddr1/2 and therapeutic uses thereof
CN112724157B (zh) * 2021-01-23 2022-04-19 中国科学院新疆理化技术研究所 二氢噁唑并[5,4-d]吡咯并[1,2-a]嘧啶-9(5H)-酮类衍生物及用途
US20250073242A1 (en) * 2021-07-30 2025-03-06 The Regents Of The University Of California Slc26a3 inhibitors and use thereof

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WO2004074270A2 (en) * 2003-02-21 2004-09-02 Pfizer Inc. Inhibitors of hepatitis c virus rna-dependent rna polymerase, and compositions and treatments using the same
US20070155779A1 (en) * 2006-01-05 2007-07-05 Pfizer Inc Bicyclic heteroaryl compounds as pde10 inhibitors

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US5902815A (en) * 1996-09-03 1999-05-11 Washington University Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction
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WO2007006175A1 (en) 2005-07-11 2007-01-18 Zte Corporation Method for implementing channel shared ring protection supported easy failure prevention
JP6130061B2 (ja) 2013-06-19 2017-05-17 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft インドリン−2−オン又はピロロ−ピリジン/ピリミジン−2−オン誘導体
EP3283487B1 (en) 2015-04-15 2019-10-16 H. Hoffnabb-La Roche Ag Pyridopyrimidinones and their use as nmda receptor modulators

Patent Citations (2)

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WO2004074270A2 (en) * 2003-02-21 2004-09-02 Pfizer Inc. Inhibitors of hepatitis c virus rna-dependent rna polymerase, and compositions and treatments using the same
US20070155779A1 (en) * 2006-01-05 2007-07-05 Pfizer Inc Bicyclic heteroaryl compounds as pde10 inhibitors

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"A Novel Family of Negative and Positive Allosteric Modulators of NMDA Receptors";Blaise Mathias Costa et al.;《THE JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS》;20101201;第335卷(第3期);第614-621页 *
"Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as Novel PKM2 Activators";Chuangxing Guo et al.;《Bioorganic & Medicinal Chemistry Letters》;20130401;第23卷(第11期);第3358-3363页 *

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SI3055315T1 (sl) 2018-11-30
RU2016115487A3 (https=) 2018-06-21
US20160222033A1 (en) 2016-08-04
BR112016007563A2 (pt) 2020-04-28
ES2690355T3 (es) 2018-11-20
CN108929336A (zh) 2018-12-04
RU2703273C2 (ru) 2019-10-16
US20180244694A1 (en) 2018-08-30
RS58047B1 (sr) 2019-02-28
CA2926830A1 (en) 2015-04-16
MX2016004540A (es) 2016-07-21
RU2016115487A (ru) 2017-11-16
HUE040651T2 (hu) 2019-03-28
CA2926830C (en) 2023-08-01
US10647731B2 (en) 2020-05-12
CN105612162A (zh) 2016-05-25
KR102361108B1 (ko) 2022-02-10
WO2015052226A1 (en) 2015-04-16
PL3055315T3 (pl) 2018-12-31
LT3055315T (lt) 2018-10-25
JP6419800B2 (ja) 2018-11-07
JP2019023217A (ja) 2019-02-14
EP3055315B1 (en) 2018-07-25
BR112016007563B1 (pt) 2022-12-20
US9988400B2 (en) 2018-06-05
PT3055315T (pt) 2018-10-25
JP2016532669A (ja) 2016-10-20
KR20160068898A (ko) 2016-06-15
EP3055315A1 (en) 2016-08-17
HRP20181596T1 (hr) 2018-12-14
HK1220202A1 (zh) 2017-04-28
EP3415519A1 (en) 2018-12-19
DK3055315T3 (en) 2018-10-22

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