EA007254B1 - Соединения, специфические к аденозиновому а, аи арецептору, и их применение - Google Patents

Соединения, специфические к аденозиновому а, аи арецептору, и их применение Download PDF

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Publication number
EA007254B1
EA007254B1 EA200300628A EA200300628A EA007254B1 EA 007254 B1 EA007254 B1 EA 007254B1 EA 200300628 A EA200300628 A EA 200300628A EA 200300628 A EA200300628 A EA 200300628A EA 007254 B1 EA007254 B1 EA 007254B1
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EA
Eurasian Patent Office
Prior art keywords
receptor
compound
compound according
substituted
agonists
Prior art date
Application number
EA200300628A
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English (en)
Russian (ru)
Other versions
EA200300628A1 (ru
Inventor
Арлиндо Л. Кастэлано
Брайан МакКиббен
Дэвид Дж. Уиттер
Original Assignee
Оси Фармасьютикалз, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US09/728,607 external-priority patent/US6664252B2/en
Priority claimed from US09/728,616 external-priority patent/US7160890B2/en
Priority claimed from US09/728,316 external-priority patent/US6680322B2/en
Application filed by Оси Фармасьютикалз, Инк. filed Critical Оси Фармасьютикалз, Инк.
Publication of EA200300628A1 publication Critical patent/EA200300628A1/ru
Publication of EA007254B1 publication Critical patent/EA007254B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00—General protective or antinoxious agents
    • A61P39/06—Free radical scavengers or antioxidants
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/08—Vasodilators for multiple indications

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Toxicology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Anesthesiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EA200300628A 2000-12-01 2001-11-30 Соединения, специфические к аденозиновому а, аи арецептору, и их применение EA007254B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US09/728,607 US6664252B2 (en) 1999-12-02 2000-12-01 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
US09/728,616 US7160890B2 (en) 1999-12-02 2000-12-01 Compounds specific to adenosine A3 receptor and uses thereof
US09/728,316 US6680322B2 (en) 1999-12-02 2000-12-01 Compounds specific to adenosine A1 receptors and uses thereof
PCT/US2001/045280 WO2002057267A1 (en) 2000-12-01 2001-11-30 Compounds specific to adenosine a1, a2a, and a3 receptor and uses thereof

Publications (2)

Publication Number Publication Date
EA200300628A1 EA200300628A1 (ru) 2003-12-25
EA007254B1 true EA007254B1 (ru) 2006-08-25

Family

ID=27419112

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200300628A EA007254B1 (ru) 2000-12-01 2001-11-30 Соединения, специфические к аденозиновому а, аи арецептору, и их применение

Country Status (20)

Country Link
EP (1) EP1347980A4 (cs)
JP (1) JP4579497B2 (cs)
CN (1) CN1263757C (cs)
AP (1) AP1893A (cs)
AU (1) AU2002248151B2 (cs)
BR (1) BR0115847A (cs)
CA (1) CA2430577A1 (cs)
CZ (1) CZ20031831A3 (cs)
EA (1) EA007254B1 (cs)
HU (1) HUP0400692A3 (cs)
IL (1) IL155962A0 (cs)
ME (1) MEP35308A (cs)
MX (1) MXPA03004717A (cs)
NO (1) NO327207B1 (cs)
NZ (1) NZ525885A (cs)
OA (1) OA13295A (cs)
PL (1) PL363245A1 (cs)
WO (1) WO2002057267A1 (cs)
YU (1) YU42703A (cs)
ZA (1) ZA200303729B (cs)

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US5090531A (en) * 1990-01-10 1992-02-25 Lord Corporation Electrophoretic fluid differential
WO1999062518A1 (en) 1998-06-02 1999-12-09 Osi Pharmaceuticals, Inc. PYRROLO[2,3d]PYRIMIDINE COMPOSITIONS AND THEIR USE
US6680324B2 (en) 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
DE10148883A1 (de) 2001-10-04 2003-04-10 Merck Patent Gmbh Pyrimidinderivate
AU2002360436A1 (en) 2001-11-30 2003-06-17 Osi Pharmaceuticals, Inc. 2-aryl pyrrologpyrimidines for a1 and a3 receptors
DE60236322D1 (de) * 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
US20030229067A1 (en) 2001-12-20 2003-12-11 Arlindo Castelhano Pyrrolopyrimidine A2b selective antagonist compounds, their synthesis and use
BR0215202A (pt) 2001-12-20 2004-10-13 Osi Pharm Inc Compostos antagonistas seletivos a2b de pirimidina, sua sìntese e uso
WO2004041285A1 (en) * 2002-10-31 2004-05-21 Amgen Inc. Antiinflammation agents
HUP0203976A3 (en) * 2002-11-15 2004-08-30 Sanofi Aventis Adenozine a3 receptors, process for their preparation and pharmaceutical compositions containing them
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
BRPI0608184A2 (pt) * 2005-02-18 2009-11-17 Solvay Pharm Gmbh composições farmacêuticas compreendendo inibidores da nep, inibidores da nep, inibidores do sistema de produção de endotelina endógena e diuréticos
US8796293B2 (en) 2006-04-25 2014-08-05 Astex Therapeutics Limited Purine and deazapurine derivatives as pharmaceutical compounds
US20070260203A1 (en) * 2006-05-04 2007-11-08 Allergan, Inc. Vasoactive agent intraocular implant
TW200808819A (en) * 2006-06-19 2008-02-16 Solvay Pharm Gmbh Use of adenosine A1 antagonists in radiocontrast media induced nephrophaty
WO2009047563A1 (en) 2007-10-11 2009-04-16 Astrazeneca Ab Pyrrolo [2, 3 -d] pyrimidin derivatives as protein kinase b inhibitors
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
EP2247596A2 (en) 2008-01-11 2010-11-10 Natco Pharma Limited Novel pyrazolo [3, 4 -d] pyrimidine derivatives as anti -cancer agents
BR112013025410A2 (pt) 2011-04-01 2016-12-20 Astrazeneca Ab tratamento terapêutico
LT2785349T (lt) 2011-11-30 2019-12-10 Astrazeneca Ab Kombinuotas vėžio gydymas
AU2013204533B2 (en) 2012-04-17 2017-02-02 Astrazeneca Ab Crystalline forms
CN104350056A (zh) * 2012-06-07 2015-02-11 霍夫曼-拉罗奇有限公司 端锚聚合酶的吡咯并嘧啶酮和吡咯并吡啶酮抑制剂
PL3010503T3 (pl) 2013-06-21 2020-08-24 Zenith Epigenetics Ltd. Nowe bicykliczne inhibitory bromodomen
WO2015004534A2 (en) * 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
WO2015015318A2 (en) 2013-07-31 2015-02-05 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
US10292968B2 (en) 2014-12-11 2019-05-21 Zenith Epigenetics Ltd. Substituted heterocycles as bromodomain inhibitors
JP2017538721A (ja) 2014-12-17 2017-12-28 ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． ブロモドメインの阻害剤
PL3248980T3 (pl) * 2015-01-20 2024-03-04 Wuxi Fortune Pharmaceutical Co., Ltd Inhibitor jak
EP3290418B1 (en) 2015-04-29 2019-05-15 Wuxi Fortune Pharmaceutical Co., Ltd Janus kinase (jak) inhibitors
CA2983481C (en) 2015-05-29 2020-04-14 Wuxi Fortune Pharmaceutical Co., Ltd Janus kinase inhibitor
CN105771672B (zh) * 2016-04-18 2018-03-02 天津工业大学 一种抗污染抗菌芳香聚酰胺反渗透复合膜及制备方法
EP3594216B1 (en) * 2017-03-07 2022-04-06 Guangzhou Maxinovel Pharmaceuticals Co., Ltd. Aminopyrimidine five-membered heterocyclic compound, and intermediate, preparation method, pharmaceutical composition and application thereof
CN108017584B (zh) * 2017-06-20 2021-03-23 南开大学 A3腺苷受体的小分子拮抗剂
CN118834214A (zh) * 2018-06-04 2024-10-25 爱克思科技有限公司 作为腺苷受体拮抗剂的吡唑并嘧啶化合物
CN110128316B (zh) * 2019-05-22 2021-08-31 北京大学深圳研究生院 5位取代的β-脯氨酸及其衍生物的制备方法
CN110272373B (zh) * 2019-07-02 2022-07-29 天津国际生物医药联合研究院 一种具有选择性的腺苷a1受体拮抗剂及其应用
CN114085178A (zh) * 2021-12-29 2022-02-25 苏州楚凯药业有限公司 一种4-甲基-1-丙基-2-氨基-1h-吡咯-3-腈的制备方法

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ES2128544T3 (es) * 1992-12-17 1999-05-16 Pfizer Pirrolopirimidinas como antagonistas del crf.
US5780450A (en) * 1995-11-21 1998-07-14 Alcon Laboratories, Inc. Use of adenosine uptake inhibitors for treating retinal or optic nerve head damage
WO1999062518A1 (en) * 1998-06-02 1999-12-09 Osi Pharmaceuticals, Inc. PYRROLO[2,3d]PYRIMIDINE COMPOSITIONS AND THEIR USE
AU784878B2 (en) * 1999-12-02 2006-07-13 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 A2A and A3 receptors and uses thereof
AU2002360436A1 (en) * 2001-11-30 2003-06-17 Osi Pharmaceuticals, Inc. 2-aryl pyrrologpyrimidines for a1 and a3 receptors

Also Published As

Publication number Publication date
IL155962A0 (en) 2003-12-23
JP4579497B2 (ja) 2010-11-10
AU2002248151B2 (en) 2008-02-21
WO2002057267A1 (en) 2002-07-25
NO327207B1 (no) 2009-05-11
OA13295A (en) 2007-04-13
PL363245A1 (en) 2004-11-15
EA200300628A1 (ru) 2003-12-25
YU42703A (sh) 2006-03-03
ZA200303729B (en) 2004-05-14
CN1489590A (zh) 2004-04-14
MEP35308A (en) 2011-02-10
EP1347980A1 (en) 2003-10-01
EP1347980A4 (en) 2005-02-09
NO20032482D0 (no) 2003-06-02
NZ525885A (en) 2005-01-28
JP2004517896A (ja) 2004-06-17
HUP0400692A3 (en) 2007-09-28
NO20032482L (no) 2003-07-28
AP1893A (en) 2008-09-23
CA2430577A1 (en) 2002-07-25
MXPA03004717A (es) 2004-06-30
AP2003002807A0 (en) 2003-06-30
BR0115847A (pt) 2004-02-25
CN1263757C (zh) 2006-07-12
HUP0400692A2 (hu) 2004-07-28
CZ20031831A3 (cs) 2004-05-12

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