KR102361108B1 - N-메틸-d-아스파르테이트 수용체 활성의 조절자로서의 티아졸로피리미딘온 - Google Patents

N-메틸-d-아스파르테이트 수용체 활성의 조절자로서의 티아졸로피리미딘온 Download PDF

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KR102361108B1
KR102361108B1 KR1020167012236A KR20167012236A KR102361108B1 KR 102361108 B1 KR102361108 B1 KR 102361108B1 KR 1020167012236 A KR1020167012236 A KR 1020167012236A KR 20167012236 A KR20167012236 A KR 20167012236A KR 102361108 B1 KR102361108 B1 KR 102361108B1
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methyl
thiazolo
trifluoromethyl
oxo
pyrimidin
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KR20160068898A (ko
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지앙 유
구오솅 우
포-와이 유엔
엘리시아 빌레무어
야콥 슈바츠
쿠옹 리
벤자민 셀레스
매튜 볼그라프
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에프. 호프만-라 로슈 아게
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/12—Heterocyclic 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
    • C07D513/14—Ortho-condensed systems
    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic ring systems
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • 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)
KR1020167012236A 2013-10-11 2014-10-08 N-메틸-d-아스파르테이트 수용체 활성의 조절자로서의 티아졸로피리미딘온 Active KR102361108B1 (ko)

Applications Claiming Priority (5)

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
PCT/EP2014/071522 WO2015052226A1 (en) 2013-10-11 2014-10-08 Thiazolopyrimidinones as modulators of nmda receptor activity

Publications (2)

Publication Number Publication Date
KR20160068898A KR20160068898A (ko) 2016-06-15
KR102361108B1 true KR102361108B1 (ko) 2022-02-10

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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=)
WO (1) WO2015052226A1 (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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US5902815A (en) * 1996-09-03 1999-05-11 Washington University Use of 5HT-2A serotonin agonists to prevent adverse effects of NMDA receptor hypofunction
EP0891978B1 (en) 1997-07-18 2002-03-20 F. Hoffmann-La Roche Ag 5H-Thiazolo (3,2-a) pyrimidine derivatives
US7148226B2 (en) * 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
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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

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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
CN105612162B (zh) 2018-08-21
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
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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