AU2003304527B2 - Uses of adenosine A2a receptor antagonists - Google Patents

Uses of adenosine A2a receptor antagonists Download PDF

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Publication number
AU2003304527B2
AU2003304527B2 AU2003304527A AU2003304527A AU2003304527B2 AU 2003304527 B2 AU2003304527 B2 AU 2003304527B2 AU 2003304527 A AU2003304527 A AU 2003304527A AU 2003304527 A AU2003304527 A AU 2003304527A AU 2003304527 B2 AU2003304527 B2 AU 2003304527B2
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AU
Australia
Prior art keywords
alkyl
alkoxy
phenyl
hydrogen
group
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Ceased
Application number
AU2003304527A
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English (en)
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AU2003304527A1 (en
Inventor
Michael Grzelak
John C. Hunter
Annamarie Pond
Geoffrey Varty
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Merck Sharp & Dohme LLC
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Merck Sharp and Dohme Ltd
Merck Sharp & Dohme LLC
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Publication of AU2003304527A1 publication Critical patent/AU2003304527A1/en
Priority to AU2010214749A priority Critical patent/AU2010214749B2/en
Application granted granted Critical
Publication of AU2003304527B2 publication Critical patent/AU2003304527B2/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: SCHERING CORPORATION
Anticipated expiration legal-status Critical
Ceased 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
    • A61K31/185—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
    • 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
    • A61K31/395—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4166—1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4515—Non condensed piperidines, e.g. piperocaine having a butyrophenone group in position 1, e.g. haloperidol
    • 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
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • 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
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    • 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
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415—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 sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • A61P25/08—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
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    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
AU2003304527A 2002-12-19 2003-12-17 Uses of adenosine A2a receptor antagonists Ceased AU2003304527B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2010214749A AU2010214749B2 (en) 2002-12-19 2010-08-31 Uses of adenosine A2a receptor antagonists

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US43532102P 2002-12-19 2002-12-19
US60/435,321 2002-12-19
PCT/US2003/040456 WO2005044245A1 (en) 2002-12-19 2003-12-17 USES OF ADENOSINE A2a RECEPTOR ANTAGONISTS

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2010214749A Division AU2010214749B2 (en) 2002-12-19 2010-08-31 Uses of adenosine A2a receptor antagonists

Publications (2)

Publication Number Publication Date
AU2003304527A1 AU2003304527A1 (en) 2005-05-26
AU2003304527B2 true AU2003304527B2 (en) 2010-09-09

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
AU2003304527A Ceased AU2003304527B2 (en) 2002-12-19 2003-12-17 Uses of adenosine A2a receptor antagonists
AU2010214749A Ceased AU2010214749B2 (en) 2002-12-19 2010-08-31 Uses of adenosine A2a receptor antagonists

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2010214749A Ceased AU2010214749B2 (en) 2002-12-19 2010-08-31 Uses of adenosine A2a receptor antagonists

Country Status (15)

Country Link
US (2) US7414058B2 (enExample)
EP (3) EP1578409B1 (enExample)
JP (3) JP2006514697A (enExample)
CN (2) CN100415217C (enExample)
AT (1) ATE490775T1 (enExample)
AU (2) AU2003304527B2 (enExample)
BR (1) BR0317436A (enExample)
DE (1) DE60335294D1 (enExample)
ES (1) ES2354875T3 (enExample)
MX (1) MXPA05006790A (enExample)
NO (1) NO20053509L (enExample)
NZ (1) NZ540493A (enExample)
TW (1) TWI331036B (enExample)
WO (1) WO2005044245A1 (enExample)
ZA (1) ZA200504478B (enExample)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1283839E (pt) * 2000-05-26 2005-08-31 Schering Corp Antagonistas do receptor a2a da adenosina
DE10043321B4 (de) * 2000-08-24 2005-07-28 Neurobiotec Gmbh Verwendung eines transdermalen therapeutischen Systems zur Behandlung der Parkinsonschen Krankheit, zur Behandlung und Prävention des prämenstruellen Syndroms und zur Lactationshemmung
DE10053397A1 (de) * 2000-10-20 2002-05-02 Schering Ag Verwendung eines dopaminergen Wirkstoffes zur Behandlung von dopaminerg behandelbaren Erkrankungen
DE10064453A1 (de) * 2000-12-16 2002-07-04 Schering Ag Verwendung eines dopaminergen Wirkstoffes zur Behandlung von dopaminerg behandelbaren Erkrankungen
US20060106040A1 (en) * 2002-12-19 2006-05-18 Michael Grzelak Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
US20060128694A1 (en) * 2002-12-19 2006-06-15 Michael Grzelak Adenosine A2a receptor antagonists for the treatment of extra-pyramidal syndrome and other movement disorders
MXPA05006790A (es) * 2002-12-19 2005-09-08 Schering Corp Usos de antagonistas del receptor adenosina a2a.
EP1622912B1 (en) * 2003-04-23 2009-05-27 Schering Corporation 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists
NZ527142A (en) 2003-07-23 2006-03-31 Douglas Pharmaceuticals Ltd A stable suspension formulation
ATE461932T1 (de) * 2004-04-21 2010-04-15 Schering Corp Pyrazoloä4,3-eü-1,2,4-triazoloä1,5-cüpyrimidine als antagonisten des adenosin-a2a-rezeptors
WO2006032273A1 (en) 2004-09-22 2006-03-30 H. Lundbeck A/S 2-acylaminothiazole derivatives
US8455437B2 (en) * 2005-02-04 2013-06-04 The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services Method to predict and prevent oxygen-induced inflammatory tissue injury
US7674912B2 (en) * 2005-04-25 2010-03-09 H. Lundbeck A/S Pro-drugs of N-thiazol-2-yl-benzamide derivatives
JPWO2006132275A1 (ja) * 2005-06-07 2009-01-08 協和醗酵工業株式会社 運動障害の予防および／または治療剤
AR057817A1 (es) * 2005-09-19 2007-12-19 Schering Corp Antagonistas del receptor a2a de 2-heteroaril-pirazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pirimidin adenosina. composiciones farmaceuticas
AR056080A1 (es) * 2005-09-23 2007-09-19 Schering Corp 7-[2-[4-(6-fluoro-3-metil-1,2-benciosoxazol-5-il)-1-piperazinil]etil]-2-(1-propinil)-7h-pirazol-[4,3-e]-[1,2,4]-triazol-[1,5-c] -pirimidin-5-amine
ES2273599B1 (es) 2005-10-14 2008-06-01 Universidad De Barcelona Compuestos para el tratamiento de la fibrilacion auricular.
JP2011513417A (ja) 2008-03-04 2011-04-28 シェーリング コーポレイション アデノシンＡ２ａ受容体アンタゴニストとして使用するための１，２，４−トリアゾロ［４，３−ｃ］ピリミジン−３−オンおよびピラゾロ［４，３−ｅ］−１，２，４−トリアゾロ［４，３−ｃ］ピリミジン−３−オン化合物
TWI473614B (zh) * 2008-05-29 2015-02-21 Kyowa Hakko Kirin Co Ltd Anti-analgesic inhibitors
BRPI1009398A2 (pt) 2009-03-13 2016-03-08 Advinus Therapeutics Private Ltd compostos de pirimidina fundida substituída
EP2499142B1 (en) 2009-11-09 2016-09-21 Advinus Therapeutics Limited Substituted fused pyrimidine compounds, its preparation and uses thereof
WO2011060207A1 (en) 2009-11-16 2011-05-19 Schering Corporation FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
US8473582B2 (en) * 2009-12-16 2013-06-25 International Business Machines Corporation Disconnected file operations in a scalable multi-node file system cache for a remote cluster file system
WO2011101861A1 (en) 2010-01-29 2011-08-25 Msn Laboratories Limited Process for preparation of dpp-iv inhibitors
ES2579949T3 (es) 2010-02-05 2016-08-17 Heptares Therapeutics Limited Derivados de 1,2,4-triazin-4-amina
CN103261202B (zh) * 2010-09-24 2016-01-20 阿迪维纳斯疗法有限公司 作为腺苷受体拮抗剂的稠合三环化合物
WO2012066330A1 (en) 2010-11-17 2012-05-24 Heptares Therapeutics Limited Compounds useful as a2a receptor inhibitors
WO2012135084A1 (en) * 2011-03-31 2012-10-04 Merck Sharp & Dohme Corp. METABOLITES OF 2-(FURAN-2-YL)-7-(2-(4-(4-(2-METHOXYETHOXY)PHENYL)PIPERAZIN-1-YL)ETHYL)-7H-PYRAZOLO[4,3-e][1,2,4]TRIAZOLO[1,5-c]PYRIMIDIN-5-AMINE AND THEIR UTILITY AS ADENOSINE A2a RECEPTOR ANTAGONISTS
WO2014101113A1 (en) * 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Piperazine-substituted 7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
WO2014101120A1 (en) 2012-12-28 2014-07-03 Merck Sharp & Dohme Corp. Heterobicyclo-substituted-7-methoxy-[1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds with a2a antagonist properties
US11246871B2 (en) 2016-07-15 2022-02-15 Northwestern University Targeting adenosine A2A receptors for the treatment of levodopa-induced dyskinesias
AU2018294557A1 (en) * 2017-06-30 2020-01-02 Ryvu Therapeutics S.A. Imidazo(1,2-a)pyrazine modulators of the adenosine A2A receptor
AU2018389313B2 (en) 2017-12-19 2021-08-19 Impetis Biosciences Ltd. Pharmaceutical composition for the treatment of cancer
AU2019205661B2 (en) 2018-01-04 2022-06-30 Impetis Biosciences Ltd. Tricyclic compounds, compositions and medicinal applications thereof
DE102019116986A1 (de) 2019-06-24 2020-12-24 Helmholtz-Zentrum Dresden-Rossendorf E. V. Deuterierte 7-(3-(4-(2-([18F]Fluor)ethoxy)phenyl)propyl)-2-(furan-2-yl)-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amin-Derivate
WO2021011670A1 (en) * 2019-07-17 2021-01-21 Teon Therapeutics, Inc. Adenosine a2a receptor antagonists and uses thereof
US11806350B2 (en) * 2020-11-19 2023-11-07 Ildong Pharmaceutical Co., Ltd. Prevention and/or treatment of CNS disorders

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999026627A1 (en) * 1997-11-26 1999-06-03 Cerebrus Limited (-)-mefloquine to block purinergic receptors and to treat movement or neurodegenerative disorders
WO2000013682A2 (en) * 1998-09-04 2000-03-16 Vernalis Research Limited 4-quinolinemethanol derivatives as purine receptor antagonists.(ii)
WO2001002409A1 (en) * 1999-07-01 2001-01-11 Vernalis Research Limited Thieno- and furopyrimidine derivatives as a2a-receptor antagonists
WO2001092264A1 (en) * 2000-05-26 2001-12-06 Schering Corporation Adenosine a2a receptor antagonists
WO2002055083A1 (en) * 2001-01-10 2002-07-18 Vernalis Research Limited TRIAZOLO[4,5-d] PYRIMIDINE DERIVATIVES AND THEIR USE AS PURINERGIC RECEPTOR ANTAGONISTS

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1264901B1 (it) 1993-06-29 1996-10-17 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(15-c)pirimidine ad attivita' antagonista per il recettore a2 dell'adenosina
US5565460A (en) 1993-07-27 1996-10-15 Kyowa Hakko Koygo Co., Ltd. Therapeutic purine agents for parkinson's disease
IT1277392B1 (it) 1995-07-28 1997-11-10 Schering Plough S P A Analoghi eterociclici di 1,2,4-triazolo(1,5-c]pirimidine ad attivita' antagonista per il recettore a2a dell'adenosina
US5933964A (en) * 1996-07-17 1999-08-10 Wahl Clipper Corporation Cutter blade for hair clippers
ATE424194T1 (de) 2001-04-09 2009-03-15 Neurosearch As Adenosin-a2a-rezeptor-antagonisten in kombination mit verbindungen mit neurotrophischer aktivität bei der behandlung von morbus parkinson
EP1425017A1 (en) * 2001-09-13 2004-06-09 Schering Corporation Combination of an adenosine a2a receptor antagonist and an antidepressant or anxiolytic
JP4545437B2 (ja) 2001-10-15 2010-09-15 シェーリング コーポレイション アデノシンａ２ａ受容体アンタゴニストとしてのイミダゾ（４，３−ｅ）−１，２，４−トリアゾロ（１，５−ｃ）ピリミジン
AU2002346503A1 (en) 2001-11-30 2003-06-17 Schering Corporation Adenosine A2a receptor antagonists
CA2468658C (en) 2001-11-30 2009-04-14 Schering Corporation [1,2,4]-triazole bicyclic adenosine a2a receptor antagonists
TW200300686A (en) 2001-11-30 2003-06-16 Schering Corp Adenosine A2a receptor antagonists
ES2716404T3 (es) * 2002-01-28 2019-06-12 Kyowa Hakko Kogyo Kk Antagonistas de receptores A2A para su uso en el tratamiento de trastornos del movimiento
ATE400275T1 (de) * 2002-08-30 2008-07-15 Kyowa Hakko Kogyo Kk Adenosin-a2a-rezeptorantagonisten zur behandlung des syndroms der unruhigen beine oder nächtlichen myoklonus
MXPA05006790A (es) * 2002-12-19 2005-09-08 Schering Corp Usos de antagonistas del receptor adenosina a2a.
EP1622912B1 (en) 2003-04-23 2009-05-27 Schering Corporation 2-alkynyl-and 2-alkenyl-pyrazolo- [4,3-e ] -1,2,4-triazolo- [1,5-c] -pyrimidine adenosine a2a receptor antagonists

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999026627A1 (en) * 1997-11-26 1999-06-03 Cerebrus Limited (-)-mefloquine to block purinergic receptors and to treat movement or neurodegenerative disorders
WO2000013682A2 (en) * 1998-09-04 2000-03-16 Vernalis Research Limited 4-quinolinemethanol derivatives as purine receptor antagonists.(ii)
WO2001002409A1 (en) * 1999-07-01 2001-01-11 Vernalis Research Limited Thieno- and furopyrimidine derivatives as a2a-receptor antagonists
WO2001092264A1 (en) * 2000-05-26 2001-12-06 Schering Corporation Adenosine a2a receptor antagonists
WO2002055083A1 (en) * 2001-01-10 2002-07-18 Vernalis Research Limited TRIAZOLO[4,5-d] PYRIMIDINE DERIVATIVES AND THEIR USE AS PURINERGIC RECEPTOR ANTAGONISTS

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
Eur J Pharm, 1994, 256(3): 263-8 *
Neuropsychopharm, 1999, 20(1): 44-51 *
Neurosci, 1999,89(3): 927-38 *
Neurotox Res, 2001, 3(6): 545-56 *
Synapse, 2001, 41(2): 160-71 *

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BR0317436A (pt) 2005-11-16
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CN1728990A (zh) 2006-02-01
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