RU2717665C2 - Пиридопиримидиноны и их применение в качестве модуляторов рецептора n-метил-d-аспартата - Google Patents

Пиридопиримидиноны и их применение в качестве модуляторов рецептора n-метил-d-аспартата Download PDF

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RU2717665C2
RU2717665C2 RU2017139254A RU2017139254A RU2717665C2 RU 2717665 C2 RU2717665 C2 RU 2717665C2 RU 2017139254 A RU2017139254 A RU 2017139254A RU 2017139254 A RU2017139254 A RU 2017139254A RU 2717665 C2 RU2717665 C2 RU 2717665C2
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methyl
pyrido
pyrimidin
oxo
trifluoromethyl
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RU2017139254A
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Russian (ru)
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RU2017139254A3 (enExample
RU2017139254A (ru
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Мэтью ВОЛЬГРАФ
Ю Цзян
Элизия ВИЛЛЕМУР
Бенджамин СЕЛЛЕРС
Гошэн У
Айцзюнь ЛУ
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Ф. Хоффманн-Ля Рош Аг
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08—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
    • A61P25/14—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/26—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring
    • C07C271/28—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a six-membered aromatic ring to a carbon atom of a non-condensed six-membered aromatic ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Addiction (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
RU2017139254A 2015-04-15 2016-04-12 Пиридопиримидиноны и их применение в качестве модуляторов рецептора n-метил-d-аспартата RU2717665C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/076617 2015-04-15
CN2015076617 2015-04-15
PCT/EP2016/057962 WO2016166078A1 (en) 2015-04-15 2016-04-12 Pyridopyrimidinones and their use as nmda receptor modulators

Publications (3)

Publication Number Publication Date
RU2017139254A RU2017139254A (ru) 2019-05-15
RU2017139254A3 RU2017139254A3 (enExample) 2019-09-30
RU2717665C2 true RU2717665C2 (ru) 2020-03-24

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RU2017139254A RU2717665C2 (ru) 2015-04-15 2016-04-12 Пиридопиримидиноны и их применение в качестве модуляторов рецептора n-метил-d-аспартата

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US (1) US10280165B2 (enExample)
EP (1) EP3283487B1 (enExample)
JP (2) JP6847851B2 (enExample)
KR (1) KR20170137137A (enExample)
CN (1) CN107531696B (enExample)
AU (1) AU2016248886B2 (enExample)
BR (1) BR112017021083A2 (enExample)
CA (1) CA2982217A1 (enExample)
CL (1) CL2017002498A1 (enExample)
CO (1) CO2017009989A2 (enExample)
CR (1) CR20170462A (enExample)
IL (1) IL254921B (enExample)
MX (1) MX373162B (enExample)
PE (1) PE20180316A1 (enExample)
PH (1) PH12017501876A1 (enExample)
RU (1) RU2717665C2 (enExample)
SG (1) SG11201708294YA (enExample)
UA (1) UA120647C2 (enExample)
WO (1) WO2016166078A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3055315T (pt) 2013-10-11 2018-10-25 Hoffmann La Roche Tiazolopirimidonas enquanto moduladores da atividade do recetor nmda
PE20180316A1 (es) 2015-04-15 2018-02-09 Hoffmann La Roche Compuestos piridopirimidinona y su uso como moduladores del receptor de nmda
ES2821010T3 (es) 2015-12-09 2021-04-23 Cadent Therapeutics Inc Moduladores heteroaromáticos del receptor NMDA y usos de los mismos
AU2017382339B2 (en) 2016-12-22 2024-02-15 Novartis Ag NMDA receptor modulators and uses thereof
PT3830092T (pt) 2018-08-03 2023-07-25 Novartis Ag Moduladores do recetor nmda heteroaromáticos e suas utilizações
CN116322696A (zh) 2020-05-04 2023-06-23 安进公司 作为髓样细胞上表达的触发受体2激动剂的杂环化合物和使用方法
TW202208355A (zh) 2020-05-04 2022-03-01 美商安進公司 作為骨髓細胞觸發受體2促效劑之雜環化合物及使用方法

Citations (2)

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Publication number Priority date Publication date Assignee Title
RU2004116473A (ru) * 2001-10-29 2005-11-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные пиридина в качестве блокаторов подтипа nmda- рецепторов
WO2014202493A1 (en) * 2013-06-19 2014-12-24 F. Hoffmann-La Roche Ag Indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives

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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
ES2339862T3 (es) * 2003-06-20 2010-05-26 Novartis Vaccines And Diagnostics, Inc. Compuestos de piridino 1,2-a-pirimidin-4-ona como agentes anticancerosos.
NL2000397C2 (nl) 2006-01-05 2007-10-30 Pfizer Prod Inc Bicyclische heteroarylverbindingen als PDE10 inhibitoren.
CA2677493A1 (en) * 2007-02-05 2008-08-14 Xenon Pharmaceuticals Inc. Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions
PT3055315T (pt) * 2013-10-11 2018-10-25 Hoffmann La Roche Tiazolopirimidonas enquanto moduladores da atividade do recetor nmda
PE20180316A1 (es) 2015-04-15 2018-02-09 Hoffmann La Roche Compuestos piridopirimidinona y su uso como moduladores del receptor de nmda

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
RU2004116473A (ru) * 2001-10-29 2005-11-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные пиридина в качестве блокаторов подтипа nmda- рецепторов
WO2014202493A1 (en) * 2013-06-19 2014-12-24 F. Hoffmann-La Roche Ag Indolin-2-one or pyrrolo-pyridin/pyrimidin-2-one derivatives

Non-Patent Citations (5)

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Title
Annamaria Molnar et al. "Suzuki-Miyaura cross-coupling reactions of halo derivatives of 4H-pyrido[1,2-a]pyrimidin-4-ones", Organic & Biomolecular Chemistry, 2011, Vol. 9, P. 6559-6565. *
Annamaria Molnar et al. "Suzuki-Miyaura cross-coupling reactions of halo derivatives of 4H-pyrido[1,2-a]pyrimidin-4-ones", Organic & Biomolecular Chemistry, 2011, Vol. 9, P. 6559-6565. Pier Luigi Ferrarini et al. "Study on Affinity Profile toward Native Human and Bovine Adenosine Receptors of a Series of 1,8-Naphthyridine Derivatives", Journal of Medicinal Chemistry, 2004, Vol. 47, No. 12, P. 3019-3031. Chuangxing Guo et al. "Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as Novel PKM2 Activators", Bioorganic & Medicinal Chemistry Letters, 2013, Vol. 23, No. 11, P. 3358-3363. Ludo E. J. Kennis et al. "New 2-Substituted 1,2,3,4-Tetrahydrobenzofuro[3,2-c]pyridine Having Highly Active and Potent Central α2-Antagonistic Activity as Potential Antidepressants", Bioorganic & Medicinal Chemistry Letters, 2000, Vol. 10, P. 71-74. *
Chuangxing Guo et al. "Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as Novel PKM2 Activators", Bioorganic & Medicinal Chemistry Letters, 2013, Vol. 23, No. 11, P. 3358-3363. *
Ludo E. J. Kennis et al. "New 2-Substituted 1,2,3,4-Tetrahydrobenzofuro[3,2-c]pyridine Having Highly Active and Potent Central α2-Antagonistic Activity as Potential Antidepressants", Bioorganic & Medicinal Chemistry Letters, 2000, Vol. 10, P. 71-74. *
Pier Luigi Ferrarini et al. "Study on Affinity Profile toward Native Human and Bovine Adenosine Receptors of a Series of 1,8-Naphthyridine Derivatives", Journal of Medicinal Chemistry, 2004, Vol. 47, No. 12, P. 3019-3031. *

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Publication number Publication date
CA2982217A1 (en) 2016-10-20
JP6847851B2 (ja) 2021-03-24
EP3283487A1 (en) 2018-02-21
CL2017002498A1 (es) 2018-04-20
RU2017139254A3 (enExample) 2019-09-30
US10280165B2 (en) 2019-05-07
JP2021046428A (ja) 2021-03-25
SG11201708294YA (en) 2017-11-29
CR20170462A (es) 2018-02-01
US20180127414A1 (en) 2018-05-10
UA120647C2 (uk) 2020-01-10
IL254921A0 (en) 2017-12-31
PH12017501876A1 (en) 2018-02-26
CN107531696B (zh) 2021-03-16
PE20180316A1 (es) 2018-02-09
EP3283487B1 (en) 2019-10-16
MX373162B (es) 2020-04-21
AU2016248886B2 (en) 2020-09-10
AU2016248886A1 (en) 2017-10-12
CO2017009989A2 (es) 2018-01-05
BR112017021083A2 (pt) 2018-07-03
MX2017013101A (es) 2018-01-30
HK1245259A1 (zh) 2018-08-24
CN107531696A (zh) 2018-01-02
RU2017139254A (ru) 2019-05-15
KR20170137137A (ko) 2017-12-12
JP2018511627A (ja) 2018-04-26
WO2016166078A1 (en) 2016-10-20
IL254921B (en) 2021-02-28

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