CN107281491A - 作为认知和运动功能增强剂的a2a拮抗剂 - Google Patents

作为认知和运动功能增强剂的a2a拮抗剂 Download PDF

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Publication number
CN107281491A
CN107281491A CN201710583855.5A CN201710583855A CN107281491A CN 107281491 A CN107281491 A CN 107281491A CN 201710583855 A CN201710583855 A CN 201710583855A CN 107281491 A CN107281491 A CN 107281491A
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China
Prior art keywords
disease
patient
effective amount
dopamine
parkinson
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CN201710583855.5A
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English (en)
Chinese (zh)
Inventor
斯蒂芬·I·班达克
凯文·J·布拉克
梅格汉·C·坎贝尔
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Biotie Therapies Inc
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Biotie Therapies Inc
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Publication of CN107281491A publication Critical patent/CN107281491A/zh
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • 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
    • A61K31/428—Thiazoles condensed with carbocyclic 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
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    • 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
    • A61P25/24—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201710583855.5A 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂 Pending CN107281491A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
USPCT/US2010/055681 2010-11-05
PCT/US2010/055681 WO2012060844A1 (en) 2010-11-05 2010-11-05 A2a antagonists as cognition and motor function enhancers
CN2011800534450A CN103429221A (zh) 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂

Related Parent Applications (1)

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CN2011800534450A Division CN103429221A (zh) 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂

Publications (1)

Publication Number Publication Date
CN107281491A true CN107281491A (zh) 2017-10-24

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CN201811049033.XA Pending CN109223799A (zh) 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂
CN201710583855.5A Pending CN107281491A (zh) 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂
CN2011800534450A Pending CN103429221A (zh) 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂

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US (2) US20130317019A1 (enExample)
EP (1) EP2635256B1 (enExample)
JP (3) JP6315991B2 (enExample)
KR (2) KR101955045B1 (enExample)
CN (3) CN109223799A (enExample)
AU (3) AU2011323152A1 (enExample)
BR (1) BR112013011068A2 (enExample)
CA (1) CA2816834A1 (enExample)
EA (2) EA035900B1 (enExample)
ES (1) ES2842968T3 (enExample)
HK (1) HK1245138A1 (enExample)
IL (2) IL225868B (enExample)
MX (2) MX382823B (enExample)
NZ (2) NZ746118A (enExample)
WO (2) WO2012060844A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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US10653699B2 (en) 2015-06-19 2020-05-19 Biotie Therapies, Inc. Controlled-release tozadenant formulations

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JP6339758B2 (ja) * 2012-07-02 2018-06-06 国立研究開発法人国立長寿医療研究センター 軽度認知機能障害の有無の診断システム、認知機能検査用端末及び認知機能検査用プログラム
JO3544B1 (ar) * 2015-03-19 2020-07-05 Kyowa Kirin Co Ltd عامل علاجي للاختلال الوظيفي في الفص الجبهي
KR102413754B1 (ko) * 2016-04-19 2022-06-27 인트라바이오 리미티드 이동성 및 인지 기능을 개선시키기 위한 아세틸-류신 또는 이의 약제학적으로 허용되는 염
US11246871B2 (en) 2016-07-15 2022-02-15 Northwestern University Targeting adenosine A2A receptors for the treatment of levodopa-induced dyskinesias
WO2018059531A1 (zh) * 2016-09-30 2018-04-05 苏州晶云药物科技有限公司 一种腺苷a2a受体拮抗剂药物的晶型及其制备方法和用途
CN113727999A (zh) 2019-01-11 2021-11-30 奥默罗斯公司 用于治疗癌症的方法和组合物
WO2021113266A1 (en) * 2019-12-02 2021-06-10 Sinopia Biosciences, Inc. Treating cognitive disorders using trapidil

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KR20100056569A (ko) * 2002-01-28 2010-05-27 교와 핫꼬 기린 가부시키가이샤 운동성 질환에 걸린 환자의 치료 방법
US7576073B2 (en) * 2004-05-28 2009-08-18 UNIVERSITé LAVAL Combined therapy for the treatment of parkinson's disease
US8168785B2 (en) * 2009-06-17 2012-05-01 Biotie Therapies, Inc. Benzothiazole derivatives

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US20050261289A1 (en) * 2004-05-24 2005-11-24 Alexander Flohr 4-Hydroxy-4-methyl-piperidine-1-carboxylic acid (4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide

Non-Patent Citations (4)

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BOVE ET AL: "Adenosine A2A Antagonism Reverses Levodopa-Induced Motor Alterations in Hemiparkinsonian Rats", 《SYNAPSE》 *
KEVIN J BLACK ET AL: "A randomized，double-blind， placebo-controlled cross-over trial of the adenosine 2a antagonist SYN115 in parkinson disease", 《NEUROLOGY》 *
TAKAHASHI ET AL: "Adenosine receptor antagonists for cognitive dysfunction: a review of animal studies", 《FRONTIERS IN BIOSCIENCE》 *
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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10653699B2 (en) 2015-06-19 2020-05-19 Biotie Therapies, Inc. Controlled-release tozadenant formulations

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MX382823B (es) 2025-03-13
NZ746118A (en) 2020-03-27
EP2635256A4 (en) 2014-05-21
JP6611896B2 (ja) 2019-11-27
AU2017201446A1 (en) 2017-03-23
US20130317019A1 (en) 2013-11-28
EP2635256A1 (en) 2013-09-11
JP6444951B2 (ja) 2018-12-26
EP2635256B1 (en) 2020-10-21
US20220125772A1 (en) 2022-04-28
KR20190025734A (ko) 2019-03-11
EA035900B1 (ru) 2020-08-28
JP2019052163A (ja) 2019-04-04
ES2842968T3 (es) 2021-07-15
WO2012061787A1 (en) 2012-05-10
NZ609803A (en) 2016-08-26
WO2012060844A1 (en) 2012-05-10
KR102166229B1 (ko) 2020-10-15
KR101955045B1 (ko) 2019-03-06
JP2017019829A (ja) 2017-01-26
JP2013541593A (ja) 2013-11-14
AU2018286608B2 (en) 2020-07-30
IL225868A0 (en) 2013-07-31
IL266321A (en) 2019-06-30
BR112013011068A2 (pt) 2016-08-23
MX2013005014A (es) 2014-01-31
IL225868B (en) 2019-05-30
AU2011323152A1 (en) 2013-06-06
CN103429221A (zh) 2013-12-04
EA202091356A1 (ru) 2020-12-30
CA2816834A1 (en) 2012-05-10
HK1245138A1 (zh) 2018-08-24
EA201390653A1 (ru) 2013-12-30
AU2018286608A1 (en) 2019-01-24
CN109223799A (zh) 2019-01-18
KR20130143597A (ko) 2013-12-31
JP6315991B2 (ja) 2018-04-25

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