CN106414456B - 用于预防和治疗神经退行性疾病和疼痛的化合物 - Google Patents

用于预防和治疗神经退行性疾病和疼痛的化合物 Download PDF

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CN106414456B
CN106414456B CN201480058727.3A CN201480058727A CN106414456B CN 106414456 B CN106414456 B CN 106414456B CN 201480058727 A CN201480058727 A CN 201480058727A CN 106414456 B CN106414456 B CN 106414456B
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base
adenosine
methyl
pain
compound
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CN106414456A (zh
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方俊民
林云莲
林荣信
林君荣
陈仪庄
黄乃瑰
王鸿利
邦宪·B·杜
陈志成
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Academia Sinica
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero 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
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    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
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    • 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
    • A61K31/52—Purines, e.g. adenine
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7076—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines containing purines, e.g. adenosine, adenylic acid
    • 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
    • A61P25/14—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
    • A61P25/28—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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • C07H19/167—Purine radicals with ribosyl as the saccharide radical
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/582—Recycling of unreacted starting or intermediate materials

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  • Health & Medical Sciences (AREA)
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  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
CN201480058727.3A 2013-10-23 2014-10-22 用于预防和治疗神经退行性疾病和疼痛的化合物 Active CN106414456B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361894699P 2013-10-23 2013-10-23
US61/894,699 2013-10-23
PCT/US2014/061734 WO2015061426A1 (en) 2013-10-23 2014-10-22 Compounds for use in prevention and treatment of neurodegenerative diseases and pain

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CN106414456A CN106414456A (zh) 2017-02-15
CN106414456B true CN106414456B (zh) 2018-12-14

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US (1) US10301348B2 (https=)
EP (1) EP3060566B1 (https=)
JP (1) JP6534997B2 (https=)
KR (1) KR102313314B1 (https=)
CN (1) CN106414456B (https=)
AU (1) AU2014340114B2 (https=)
BR (1) BR112016008901B1 (https=)
CA (1) CA2927699C (https=)
IL (1) IL245103B (https=)
MX (1) MX367707B (https=)
RU (1) RU2695358C2 (https=)
SG (1) SG11201603063WA (https=)
WO (1) WO2015061426A1 (https=)
ZA (1) ZA201603118B (https=)

Families Citing this family (6)

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Publication number Priority date Publication date Assignee Title
US10675293B2 (en) * 2015-05-29 2020-06-09 The Board Of Trustees Of The Leland Stanford Junior University Nucleoside agents for the reduction of the deleterious activity of extended nucleotide repeat containing genes
US11753432B2 (en) 2017-01-27 2023-09-12 Academia Sinica Compound with analgesic effect for use in prevention and treatment of pain
EP4476235A4 (en) * 2022-02-10 2026-02-18 Academia Sinica METHOD FOR TREATMENT OF A SPINAL CORD INJURY AND CORRESPONDING COMPOSITION
TWI910441B (zh) * 2022-07-07 2026-01-01 中央研究院 治療思覺失調症之方法及用於其中之組成物
CA3275345A1 (en) * 2022-12-29 2024-07-04 Academia Sinica METHODS FOR TREATING SLEEP DISORDERS AND COMPOSITION INTENDED FOR USE THEREOF
TW202500138A (zh) * 2023-03-17 2025-01-01 中央研究院 治療結節性硬化症或癲癇之方法及用於其中之組成物

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988003148A2 (en) * 1986-10-31 1988-05-05 Warner-Lambert Company Heteroaromatic derivatives of adenoside
US5034381A (en) * 1988-01-07 1991-07-23 Ciba-Geigy Corporation 2-(substituted amino) adenosines as antihypertensives
CN1148811A (zh) * 1994-04-19 1997-04-30 罗纳·布朗克罗尔药制品有限公司 具有抗高血压、保护心脏、抗局部缺血和抗脂解性质的化合物
WO2012064340A1 (en) * 2009-11-13 2012-05-18 Academia Sinica Dual-action compounds targeting adenosine a2a receptor and adenosine transporter for prevention and treatment of neurodegenerative diseases
WO2013120078A1 (en) * 2012-02-11 2013-08-15 Academia Sinica Methods and compositions for treating pain

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SG80526A1 (en) * 1990-09-25 2001-05-22 Rhone Poulenc Rorer Int Compounds having antihypertensive and anti- ischemic properies
UY27939A1 (es) * 2002-08-21 2004-03-31 Glaxo Group Ltd Compuestos
CA2783859A1 (en) * 2009-12-10 2011-06-16 Institute Of Materia Medica, Chinese Academy Of Medical Sciences N6-substituted adenosine derivatives and n6-substituted adenine derivatives and uses thereof
WO2013120076A1 (en) 2012-02-09 2013-08-15 Brand Bumps, LLC Decorative detectable warning panel having improved grip

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1988003148A2 (en) * 1986-10-31 1988-05-05 Warner-Lambert Company Heteroaromatic derivatives of adenoside
US5034381A (en) * 1988-01-07 1991-07-23 Ciba-Geigy Corporation 2-(substituted amino) adenosines as antihypertensives
CN1148811A (zh) * 1994-04-19 1997-04-30 罗纳·布朗克罗尔药制品有限公司 具有抗高血压、保护心脏、抗局部缺血和抗脂解性质的化合物
WO2012064340A1 (en) * 2009-11-13 2012-05-18 Academia Sinica Dual-action compounds targeting adenosine a2a receptor and adenosine transporter for prevention and treatment of neurodegenerative diseases
WO2013120078A1 (en) * 2012-02-11 2013-08-15 Academia Sinica Methods and compositions for treating pain

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"Caffeine and Adenosine A2A Receptor Inactivation Decrease Striatal Neuropathology in a Lentiviral-Based Model of Machado–Joseph Disease";Nelio Goncalves et al.;《ANNALS of Neurology》;20130426;第73卷(第5期);第655-666页 *
"D- and L-2",3"-Didehydro-2",3"-dideoxy-3"-fluoro-carbocyclic Nucleosides: Synthesis, Anti-HIV Activity and Mechanism of Resistance";Jianing Wang et al.;《Journal of Medicinal Chemistry》;20070321;第50卷(第8期);第1828-1839页 *
"Synthesis of 6-15N and 1-15N labeled adenosine monophosphates";Simon R. Scarfati et al.;《Tetrahedron》;19881231;第44卷(第20期);第6368页Scheme 1，第6371页化合物6-8的制备 *

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WO2015061426A1 (en) 2015-04-30
US20160264613A1 (en) 2016-09-15
NZ719740A (en) 2021-02-26
JP6534997B2 (ja) 2019-06-26
CA2927699C (en) 2022-07-05
BR112016008901B1 (pt) 2022-08-23
EP3060566A4 (en) 2017-06-14
RU2016118282A (ru) 2017-11-28
CA2927699A1 (en) 2015-04-30
ZA201603118B (en) 2019-04-24
MX367707B (es) 2019-09-03
IL245103B (en) 2019-02-28
RU2016118282A3 (https=) 2018-06-18
AU2014340114A1 (en) 2016-05-26
IL245103A0 (en) 2016-06-30
KR20160086852A (ko) 2016-07-20
MX2016005174A (es) 2016-08-11
EP3060566A1 (en) 2016-08-31
AU2014340114B2 (en) 2018-10-18
JP2016535019A (ja) 2016-11-10
CN106414456A (zh) 2017-02-15
US10301348B2 (en) 2019-05-28
BR112016008901A2 (pt) 2020-05-12
RU2695358C2 (ru) 2019-07-23
KR102313314B1 (ko) 2021-10-19
SG11201603063WA (en) 2016-05-30
EP3060566B1 (en) 2018-09-05

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