CN103429221A - 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
CN103429221A
CN103429221A CN2011800534450A CN201180053445A CN103429221A CN 103429221 A CN103429221 A CN 103429221A CN 2011800534450 A CN2011800534450 A CN 2011800534450A CN 201180053445 A CN201180053445 A CN 201180053445A CN 103429221 A CN103429221 A CN 103429221A
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China
Prior art keywords
dopamine
patient
treatment
parkinson
levodopa
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CN2011800534450A
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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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Priority to CN201710583855.5A priority Critical patent/CN107281491A/zh
Priority to CN201811049033.XA priority patent/CN109223799A/zh
Publication of CN103429221A publication Critical patent/CN103429221A/zh
Pending legal-status Critical Current

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    • 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
    • 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
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    • 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
    • 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
    • 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
    • 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
    • A61P25/24—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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (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)
CN2011800534450A 2010-11-05 2011-11-04 作为认知和运动功能增强剂的a2a拮抗剂 Pending CN103429221A (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN201710583855.5A 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
CN201811049033.XA 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

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
PCT/US2011/059466 WO2012061787A1 (en) 2010-11-05 2011-11-04 A2a antagonists as cognition and motor function enhancers

Related Child Applications (2)

Application Number Title Priority Date Filing Date
CN201710583855.5A Division 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
CN201811049033.XA Division 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

Publications (1)

Publication Number Publication Date
CN103429221A true CN103429221A (zh) 2013-12-04

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Application Number Title Priority Date Filing Date
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
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
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

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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
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

Country Status (15)

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US (2) US20130317019A1 (OSRAM)
EP (1) EP2635256B1 (OSRAM)
JP (3) JP6315991B2 (OSRAM)
KR (2) KR102166229B1 (OSRAM)
CN (3) CN103429221A (OSRAM)
AU (3) AU2011323152A1 (OSRAM)
BR (1) BR112013011068A2 (OSRAM)
CA (1) CA2816834A1 (OSRAM)
EA (2) EA035900B1 (OSRAM)
ES (1) ES2842968T3 (OSRAM)
HK (1) HK1245138A1 (OSRAM)
IL (2) IL225868B (OSRAM)
MX (2) MX2013005014A (OSRAM)
NZ (2) NZ746118A (OSRAM)
WO (2) WO2012060844A1 (OSRAM)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN109069463A (zh) * 2016-04-19 2018-12-21 内在生物技术有限公司 用于改善运动能力和认知功能的乙酰亮氨酸或其药学上可接受的盐

Families Citing this family (6)

* Cited by examiner, † Cited by third party
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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
CA2988918A1 (en) 2015-06-19 2016-12-22 Biotie Therapies, Inc. Controlled-release tozadenant formulations
WO2018013951A1 (en) * 2016-07-15 2018-01-18 Northwestern University Targeting adenosine a2a receptors for the treatment of levodopa-induced dyskinesias
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
CA3163242A1 (en) * 2019-12-02 2021-06-10 Aarash BORDBAR Treating cognitive disorders using trapidil

Citations (1)

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CN101543497A (zh) * 2002-01-28 2009-09-30 协和发酵工业株式会社 治疗运动疾病患者的方法

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CN1956983B (zh) * 2004-05-24 2010-05-26 弗·哈夫曼-拉罗切有限公司 4-羟基-4-甲基-哌啶-1-甲酸(4-甲氧基-7-吗啉-4-基-苯并噻唑-2-基)-酰胺
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

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
CN101543497A (zh) * 2002-01-28 2009-09-30 协和发酵工业株式会社 治疗运动疾病患者的方法

Non-Patent Citations (3)

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Title
KEVIN J BLACK,ET AL: "A randomized,double-blind,placebo-controlled cross-over trial of the adenosine 2a antagonist SYN115 in parkinson disease", 《NEUROLOGY》 *
REINALDO NAOTO TAKAHASHI, ET AL: "Adenosine receptor antagonists for cognitive dysfunction: a review of animal studies", 《FRONTIERS IN BIOSCIENCE》 *
侯训尧: "PD认知功能障碍", 《山东医药》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109069463A (zh) * 2016-04-19 2018-12-21 内在生物技术有限公司 用于改善运动能力和认知功能的乙酰亮氨酸或其药学上可接受的盐
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

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AU2017201446A1 (en) 2017-03-23
KR20130143597A (ko) 2013-12-31
EP2635256B1 (en) 2020-10-21
IL225868B (en) 2019-05-30
AU2011323152A1 (en) 2013-06-06
BR112013011068A2 (pt) 2016-08-23
US20220125772A1 (en) 2022-04-28
EA201390653A1 (ru) 2013-12-30
EA035900B1 (ru) 2020-08-28
KR102166229B1 (ko) 2020-10-15
NZ746118A (en) 2020-03-27
MX382823B (es) 2025-03-13
CA2816834A1 (en) 2012-05-10
ES2842968T3 (es) 2021-07-15
KR101955045B1 (ko) 2019-03-06
JP6611896B2 (ja) 2019-11-27
JP2013541593A (ja) 2013-11-14
NZ609803A (en) 2016-08-26
EP2635256A1 (en) 2013-09-11
EA202091356A1 (ru) 2020-12-30
JP6315991B2 (ja) 2018-04-25
EP2635256A4 (en) 2014-05-21
MX2013005014A (es) 2014-01-31
IL266321A (en) 2019-06-30
CN107281491A (zh) 2017-10-24
JP2017019829A (ja) 2017-01-26
JP2019052163A (ja) 2019-04-04
KR20190025734A (ko) 2019-03-11
US20130317019A1 (en) 2013-11-28
AU2018286608A1 (en) 2019-01-24
CN109223799A (zh) 2019-01-18
WO2012060844A1 (en) 2012-05-10
WO2012061787A1 (en) 2012-05-10
IL225868A0 (en) 2013-07-31
HK1245138A1 (zh) 2018-08-24
JP6444951B2 (ja) 2018-12-26
AU2018286608B2 (en) 2020-07-30

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Application publication date: 20131204