[go: up one dir, main page]

EA200600315A1 - Пиримидиновые соединения, их применение в качестве a-селективных антагонистов и способ их получения - Google Patents

Пиримидиновые соединения, их применение в качестве a-селективных антагонистов и способ их получения

Info

Publication number
EA200600315A1
EA200600315A1 EA200600315A EA200600315A EA200600315A1 EA 200600315 A1 EA200600315 A1 EA 200600315A1 EA 200600315 A EA200600315 A EA 200600315A EA 200600315 A EA200600315 A EA 200600315A EA 200600315 A1 EA200600315 A1 EA 200600315A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
substituted
heterocyclic
monocyclic
heteroaryl
Prior art date
Application number
EA200600315A
Other languages
English (en)
Other versions
EA011809B1 (ru
Inventor
Арлиндо Л. Кастэлано
Брайан МакКиббен
Арно Г. Штайниг
Эрик Уилльям Коллингтон
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
Application filed by Оси Фармасьютикалз, Инк. filed Critical Оси Фармасьютикалз, Инк.
Publication of EA200600315A1 publication Critical patent/EA200600315A1/ru
Publication of EA011809B1 publication Critical patent/EA011809B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Настоящее изобретение относится к соединениям структурыгде Rпредставляет собой замещенный или незамещенный фенил, или 5-6-членное гетероциклическое или гетероароматическое кольцо; Rи Rпредставляют собой водород, или замещенный или незамещенный алкил, -С(O)-алкил, -С(O)-O-алкил, алкокси-, циклоалкокси, алкенил, моноцикический или бициклический арил, гетероарил или гетероциклический радикал, где пунктирная линия представляет собой вторую связь, которая может присутствовать или отсутствовать, Rи Rнезависимо представляют собой замещенный или незамещенный алкил, -С(O)-алкил, -С(О)-O-алкил, алкокси-, циклоалкил, алкенил, моноциклический или бициклический арил, гетероарил или гетероциклический радикал; Rпредставляет собой водород, алкил, галоген или цианогруппу; и n равно 0, 1, 2, 3 или 4, или их энантиомеру, или их конкретному таутомеру, или их фармацевтически приемлемой соли, и способу лечения ассоциированного с аденозиновым рецептором Aзаболевания путем введения терапевтически эффективного количества соединений по настоящему изобретению и способу их получения.
EA200600315A 2001-12-20 2002-12-20 Пиримидиновые соединения, их применение в качестве a-селективных антагонистов и способ их получения EA011809B1 (ru)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US34259501P 2001-12-20 2001-12-20

Publications (2)

Publication Number Publication Date
EA200600315A1 true EA200600315A1 (ru) 2006-06-30
EA011809B1 EA011809B1 (ru) 2009-06-30

Family

ID=23342484

Family Applications (2)

Application Number Title Priority Date Filing Date
EA200600315A EA011809B1 (ru) 2001-12-20 2002-12-20 Пиримидиновые соединения, их применение в качестве a-селективных антагонистов и способ их получения
EA200400830A EA007468B1 (ru) 2001-12-20 2002-12-20 Пиримидиновые соединения, относящиеся к a-селективным антагонистам, их синтез и применение

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA200400830A EA007468B1 (ru) 2001-12-20 2002-12-20 Пиримидиновые соединения, относящиеся к a-селективным антагонистам, их синтез и применение

Country Status (13)

Country Link
US (2) US6916804B2 (ru)
EP (1) EP1465631B1 (ru)
JP (1) JP4440642B2 (ru)
KR (1) KR20040068317A (ru)
CN (1) CN1620294A (ru)
AT (1) ATE458483T1 (ru)
AU (1) AU2002366811B2 (ru)
BR (1) BR0215202A (ru)
CA (1) CA2471059C (ru)
DE (1) DE60235500D1 (ru)
EA (2) EA011809B1 (ru)
MX (1) MXPA04005862A (ru)
WO (1) WO2003053366A2 (ru)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ508314A (en) 1998-06-02 2004-03-26 Osi Pharm Inc Pyrrolo[2,3d]pyrimidine compositions and their use
US6403567B1 (en) 1999-06-22 2002-06-11 Cv Therapeutics, Inc. N-pyrazole A2A adenosine receptor agonists
USRE47351E1 (en) 1999-06-22 2019-04-16 Gilead Sciences, Inc. 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
WO2001062979A2 (en) * 2000-02-23 2001-08-30 Cv Therapeutics, Inc. Dentification of partial agonists of the a2a adenosine receptor
US6680324B2 (en) * 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
DK1450811T3 (da) * 2001-11-30 2010-02-15 Osi Pharm Inc Forbindelser specifikke af adenosin A1- og A3-receptorer og anvendelser heraf
KR20040068317A (ko) 2001-12-20 2004-07-30 오에스아이 파마슈티컬스, 인코포레이티드 피리미딘 ａ₂ｂ 선택성 길항 화합물, 그의 합성 방법 및용도
US20030229067A1 (en) * 2001-12-20 2003-12-11 Arlindo Castelhano Pyrrolopyrimidine A2b selective antagonist compounds, their synthesis and use
US20050256130A1 (en) * 2002-06-12 2005-11-17 Chemocentryx, Inc. Substituted piperazines
MXPA04012959A (es) * 2002-06-29 2005-05-16 Zentaris Gmbh Arilcarbonilpiperacinas y heteroarilcarbonilpiperacinas y su uso para tratamiento de enfermedades de tumor benigno y maligno.
US20050020915A1 (en) * 2002-07-29 2005-01-27 Cv Therapeutics, Inc. Myocardial perfusion imaging methods and compositions
US7683037B2 (en) * 2002-07-29 2010-03-23 Gilead Palo Alto, Inc. Myocardial perfusion imaging method
US8470801B2 (en) 2002-07-29 2013-06-25 Gilead Sciences, Inc. Myocardial perfusion imaging methods and compositions
KR20050057226A (ko) * 2002-09-06 2005-06-16 얀센 파마슈티카 엔.브이. 알레르기성 비염 치료용 약제를 제조하기 위한 인돌릴 유도체의 용도
BRPI0413497B8 (pt) * 2003-08-11 2021-05-25 Hoffmann La Roche piperazina com ou que substitui grupo fenila, e seu uso e seu processo de preparação, bem como medicamento
AU2004283751B2 (en) * 2003-10-24 2011-05-19 Exelixis, Inc. p70S6 kinase modulators and method of use
ES2234433B1 (es) * 2003-12-15 2006-11-01 Almirall Prodesfarma, S.A. 4-aminopirimidinas como antagonistas de receptores de adenosina.
EP1799221A1 (en) * 2004-10-15 2007-06-27 Cv Therapeutics, Inc. Method of preventing and treating airway remodeling and pulmonary inflammation using a2b adenosine receptor antagonists
AU2005295437B2 (en) 2004-10-20 2011-05-19 Gilead Palo Alto, Inc. Use of A2A adenosine receptor agonists
NZ555290A (en) * 2004-12-09 2009-09-25 Hoffmann La Roche Phenyl-piperazin methanone derivatives
JP2008528573A (ja) * 2005-01-27 2008-07-31 アルマ マテル ストゥディオルム−ウニヴェルシタ ディ ボローニャ アルツハイマー病の処置に有用な有機化合物、それらの使用及び調製の方法
RS53668B1 (en) 2005-04-13 2015-04-30 Astex Therapeutics Limited HYDROXYBENZAMIDE DERIVATIVES AND THEIR APPLICATIONS AS HSP90 INHIBITORS
WO2006124897A2 (en) * 2005-05-13 2006-11-23 Lexicon Genetics Incorporated Methods and compositions for improving cognition
ES2434467T3 (es) * 2005-05-13 2013-12-16 Lexicon Pharmaceuticals, Inc. Compuestos multicíclicos y métodos para su uso
CA2612344A1 (en) * 2005-06-16 2006-12-28 Cv Therapeutics, Inc. Prodrugs of a2b adenosine receptor antagonists
US7601844B2 (en) * 2006-01-27 2009-10-13 Bristol-Myers Squibb Company Piperidinyl derivatives as modulators of chemokine receptor activity
US7615556B2 (en) * 2006-01-27 2009-11-10 Bristol-Myers Squibb Company Piperazinyl derivatives as modulators of chemokine receptor activity
ES2593028T3 (es) 2006-02-03 2016-12-05 Gilead Sciences, Inc. Proceso para preparar un agonista de receptor de adenosina A2A y sus polimorfos
US7935706B2 (en) 2006-02-23 2011-05-03 Shionogi & Co., Ltd. Nitrogen-containing heterocycle derivatives substituted with cyclic group
US7754725B2 (en) 2006-03-01 2010-07-13 Astex Therapeutics Ltd. Dihydroxyphenyl isoindolymethanones
RU2459626C2 (ru) * 2006-09-01 2012-08-27 Гайлид Сайэнсиз, Инк. Способы и композиции, повышающие переносимость пациентом методов визуализации миокарда
US20090081120A1 (en) * 2006-09-01 2009-03-26 Cv Therapeutics, Inc. Methods and Compositions for Increasing Patient Tolerability During Myocardial Imaging Methods
EP2066232A1 (en) * 2006-09-29 2009-06-10 Cv Therapeutics, Inc. Methods for myocardial imaging in patients having a history of pulmonary disease
US9730912B2 (en) 2006-10-12 2017-08-15 Astex Therapeutics Limited Pharmaceutical compounds
EP2073803B1 (en) 2006-10-12 2018-09-19 Astex Therapeutics Limited Pharmaceutical combinations
US8883790B2 (en) 2006-10-12 2014-11-11 Astex Therapeutics Limited Pharmaceutical combinations
US8277807B2 (en) 2006-10-12 2012-10-02 Astex Therapeutics Limited Pharmaceutical combinations
GB0620259D0 (en) 2006-10-12 2006-11-22 Astex Therapeutics Ltd Pharmaceutical compounds
EP2081891A2 (en) 2006-10-12 2009-07-29 Astex Therapeutics Limited Pharmaceutical compounds having hsp90 inhibitory or modulating activity
CA2668811A1 (en) * 2006-11-07 2008-06-05 Lexicon Pharmaceuticals, Inc. Methods of treating cognitive impairment and dementia
GB0806527D0 (en) 2008-04-11 2008-05-14 Astex Therapeutics Ltd Pharmaceutical compounds
US10517839B2 (en) 2008-06-09 2019-12-31 Cornell University Mast cell inhibition in diseases of the retina and vitreous
TWI433838B (zh) * 2008-06-25 2014-04-11 必治妥美雅史谷比公司 作為趨化因子受體活性調節劑之六氫吡啶衍生物
EP2306838A4 (en) * 2008-07-16 2011-12-14 King Pharmaceuticals Res & Dev METHOD FOR THE TREATMENT OF ATHEROSCLEROSIS
CA2737077A1 (en) * 2008-09-29 2010-04-01 Gilead Sciences, Inc. Combinations of a rate control agent and an a-2-alpha receptor antagonist for use in multidetector computed tomography methods
US8642622B2 (en) 2010-06-16 2014-02-04 Bristol-Myers Squibb Company Piperidinyl compound as a modulator of chemokine receptor activity
CN101967209B (zh) * 2010-10-20 2012-11-07 南京大学 一种n-乙酰基乙二胺螯合树脂及其制备方法
WO2014065374A1 (ja) 2012-10-24 2014-05-01 参天製薬株式会社 未熟児網膜症の治療又は予防剤、未熟児網膜症の検査方法及び未熟児網膜症の治療又は予防物質のスクリーニング方法
US20160002188A1 (en) 2013-03-13 2016-01-07 Forma Therapeutics, Inc. Novel compounds and compositions for inhibition of fasn
WO2015051230A1 (en) * 2013-10-04 2015-04-09 Drexel University Novel compositions useful for inhibiting hiv-1 infection and methods using same
US20200352931A1 (en) * 2017-12-12 2020-11-12 Phenex Discovery Verwaltungs-GmbH Oxalamides as modulators of indoleamine 2,3-dioxygenase
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
CA3126735A1 (en) 2019-01-11 2020-07-16 Omeros Corporation Methods and compositions for treating cancer
CN115677596A (zh) * 2022-12-10 2023-02-03 江苏莱科化学有限公司 一种除草安全剂解草啶的制备工艺

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3037980A (en) 1955-08-18 1962-06-05 Burroughs Wellcome Co Pyrrolopyrimidine vasodilators and method of making them
GB915303A (en) 1958-03-13 1963-01-09 Wellcome Found Pyrrolo[2,3-d]pyrimidine derivatives and the manufacture thereof
US3910913A (en) 1969-11-04 1975-10-07 American Home Prod 4,5-Diamino-7H-pyrrolo{8 2,3-d{9 pyrimidine derivatives
DE3145287A1 (de) 1981-11-14 1983-05-19 Troponwerke GmbH & Co KG, 5000 Köln Pyrrolo (2.3-d)pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als arzneimittel
IN157280B (ru) 1983-07-15 1986-02-22 Hoechst India
GB8729994D0 (en) 1987-12-23 1988-02-03 Glaxo Group Ltd Chemical compounds
IL89028A0 (en) 1988-01-29 1989-08-15 Lilly Co Eli Quinoline,quinazoline and cinnoline derivatives
DE69027862T2 (de) 1989-09-19 1997-03-06 Teijin Ltd., Osaka Pyrrolo[2,3-d]pyrimidinderivate, verfahren zur herstellung und arzneimittelzusammensetzungen die diese enthalten
US5681941A (en) 1990-01-11 1997-10-28 Isis Pharmaceuticals, Inc. Substituted purines and oligonucleotide cross-linking
US5208240A (en) 1991-03-12 1993-05-04 Merrell Dow Pharmaceuticals Inc. 8-substituted purines as selective adenosine receptor agents
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5714493A (en) 1991-05-10 1998-02-03 Rhone-Poulenc Rorer Pharmaceuticals, Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
ES2108120T3 (es) 1991-05-10 1997-12-16 Rhone Poulenc Rorer Int Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf.
US5721237A (en) 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
US5516894A (en) 1992-03-11 1996-05-14 The General Hospital Corporation A2b -adenosine receptors
CA2130937A1 (en) 1992-04-03 1993-10-14 Gordon L. Bundy Pharmaceutically active bicyclic-heterocyclic amines
GB9323290D0 (en) 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
DK0674641T3 (da) 1992-12-17 1999-09-27 Pfizer Pyrrolopyrimidiner som CRF-antagonister
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
CA2155130C (en) 1993-02-26 1994-09-01 Janice M Hitchcock Xanthine derivatives as adenosine a1 receptor antagonists
DE69433379T2 (de) 1993-04-08 2004-10-14 The Trustees Of Columbia University In The City Of New York Verfahren zur Herstellung von 4- und/oder 5-(di)substituierten 2-Aminoimidazolen aus 2-Aminoimidazolen und Aldehyden
WO1995011681A1 (en) 1993-10-29 1995-05-04 Merck & Co., Inc. Human adenosine receptor antagonists
US5877218A (en) 1994-01-10 1999-03-02 Teva Pharmaceutical Industries, Ltd. Compositions containing and methods of using 1-aminoindan and derivatives thereof and process for preparing optically active 1-aminoindan derivatives
WO1995018617A1 (en) 1994-01-10 1995-07-13 Teva Pharmaceutical Industries Ltd. 1-aminoindan derivatives and compositions thereof
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
HU220423B (hu) 1994-01-26 2002-01-28 Novartis Ag. Módosított oligonukleotidok
US5646156A (en) 1994-04-25 1997-07-08 Merck & Co., Inc. Inhibition of eosinophil activation through A3 adenosine receptor antagonism
DE59500788D1 (de) 1994-05-03 1997-11-20 Ciba Geigy Ag Pyrrolopyrimidinderivate mit antiproliferativer Wirkung
US5877180A (en) 1994-07-11 1999-03-02 University Of Virginia Patent Foundation Method for treating inflammatory diseases with A2a adenosine receptor agonists
WO1996019478A1 (en) 1994-12-19 1996-06-27 Novartis Ag 6'-substituted carbocyclic nucleosides
EP0729758A3 (en) 1995-03-02 1997-10-29 Pfizer Pyrazolopyrimidines and pyrrolopyrimidines for the treatment of neuronal and other diseases
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
US5646130A (en) 1995-06-30 1997-07-08 Ocean University Of Oingdao Low molecular weight sulfated polysaccharides and uses thereof
DE69619114T2 (de) 1995-07-06 2002-10-02 Novartis Ag, Basel Pyrolopyrimidine und verfahren zu ihrer herstellung
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
US5780450A (en) 1995-11-21 1998-07-14 Alcon Laboratories, Inc. Use of adenosine uptake inhibitors for treating retinal or optic nerve head damage
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
WO1997033879A1 (en) 1996-03-15 1997-09-18 Merck & Co., Inc. Compounds and methods for selectively inhibiting activation of the human a3 adenosine receptor
JPH09291089A (ja) 1996-04-26 1997-11-11 Yamanouchi Pharmaceut Co Ltd 新規な５−チアゾリルウラシル誘導体又はその塩
AU2980797A (en) 1996-06-11 1998-01-07 Yoshitomi Pharmaceutical Industries, Ltd. Fused heterocyclic compounds and medicinal uses thereof
TW498067B (en) 1996-07-19 2002-08-11 Hoffmann La Roche 4-hydroxy-piperidine derivatives
US5780481A (en) 1996-08-08 1998-07-14 Merck & Co., Inc. Method for inhibiting activation of the human A3 adenosine receptor to treat asthma
ES2297864T3 (es) 1996-08-23 2008-05-01 Novartis Ag Pirrolopirimidinas sustituidas y procesos para su preparacion.
WO1998008382A1 (en) 1996-08-30 1998-03-05 Eli Lilly And Company Nonclassical pyrrolo[2,3-d]pyrimidine antifolates
US5786360A (en) 1996-11-19 1998-07-28 Link Technology Incorporated A1 adenosine receptor antagonists
WO1998029397A1 (fr) 1996-12-27 1998-07-09 Yoshitomi Pharmaceutical Industries, Ltd. Composes pyrimidine a anneaux condenses et leur utilisation medicinale
FR2763334A1 (fr) 1997-05-13 1998-11-20 Lipha Derives anthraniliques
EP1014995A4 (en) 1997-06-18 2005-02-16 Aderis Pharmaceuticals Inc COMPOSITIONS AND METHODS FOR PREVENTING RESTENOSES CONSECUTIVE TO REVASCULARIZATION INTERVENTIONS
EP1019427A4 (en) 1997-07-29 2000-07-19 Medco Res Inc N? 6 -SUBSTITUES-ADENOSINE-5'-URONAMIDES USEFUL AS MODULATORS OF ADENOSINE RECEPTORS
US6151484A (en) 1997-08-08 2000-11-21 Ericsson Inc. Communications apparatus and methods for adaptive signal processing based on mobility characteristics
US6436989B1 (en) 1997-12-24 2002-08-20 Vertex Pharmaceuticals, Incorporated Prodrugs of aspartyl protease inhibitors
US6117878A (en) 1998-02-24 2000-09-12 University Of Virginia 8-phenyl- or 8-cycloalkyl xanthine antagonists of A2B human adenosine receptors
US6878716B1 (en) 1998-06-02 2005-04-12 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptor and uses thereof
US6686366B1 (en) 1998-06-02 2004-02-03 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
NZ508314A (en) 1998-06-02 2004-03-26 Osi Pharm Inc Pyrrolo[2,3d]pyrimidine compositions and their use
WO2000003741A2 (en) 1998-07-16 2000-01-27 The Trustees Of The University Of Pennsylvania Methods for reducing intraocular pressure using a3-adenosine antagonists
JP2003519102A (ja) 1999-12-02 2003-06-17 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド アデノシンａ▲下１▼、ａ▲下２ａ▼およびａ▲下３▼受容体に対して特異的な化合物並びにその使用
US6680322B2 (en) 1999-12-02 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US6664252B2 (en) 1999-12-02 2003-12-16 Osi Pharmaceuticals, Inc. 4-aminopyrrolo[2,3-d]pyrimidine compounds specific to adenosine A2a receptor and uses thereof
US7160890B2 (en) 1999-12-02 2007-01-09 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
US6465456B2 (en) 2000-06-29 2002-10-15 Bristol-Myers Squibb Company Isoxazolinone antibacterial agents
US6680324B2 (en) 2000-12-01 2004-01-20 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A1 receptors and uses thereof
US6673802B2 (en) 2000-12-01 2004-01-06 Osi Pharmaceuticals, Inc. Compounds specific to adenosine A3 receptor and uses thereof
NZ525885A (en) 2000-12-01 2005-01-28 Osi Pharm Inc Compounds specific to adenosine A1, A2A, and A3 receptor and uses as ubiquitous modulators of physiological activities
DK1450811T3 (da) 2001-11-30 2010-02-15 Osi Pharm Inc Forbindelser specifikke af adenosin A1- og A3-receptorer og anvendelser heraf
US20030229067A1 (en) 2001-12-20 2003-12-11 Arlindo Castelhano Pyrrolopyrimidine A2b selective antagonist compounds, their synthesis and use
BR0215279A (pt) 2001-12-20 2005-05-10 Osi Pharmaceutical Inc Compostos antagonistas a2b seletivos da pirrolopirimidina, sua sìntese e uso
KR20040068317A (ko) * 2001-12-20 2004-07-30 오에스아이 파마슈티컬스, 인코포레이티드 피리미딘 ａ₂ｂ 선택성 길항 화합물, 그의 합성 방법 및용도
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
JP2006518390A (ja) 2003-02-19 2006-08-10 エンダシア，インコーポレイテッド Ａ１アデノシンレセプターアンタゴニスト
US7384885B2 (en) * 2003-03-31 2008-06-10 Exxonmobil Chemical Patents Inc. Catalyst activation and resins therefrom

Also Published As

Publication number Publication date
CN1620294A (zh) 2005-05-25
CA2471059A1 (en) 2003-07-03
EA011809B1 (ru) 2009-06-30
MXPA04005862A (es) 2004-11-01
BR0215202A (pt) 2004-10-13
US7501407B2 (en) 2009-03-10
DE60235500D1 (de) 2010-04-08
CA2471059C (en) 2011-04-26
ATE458483T1 (de) 2010-03-15
EP1465631A2 (en) 2004-10-13
EP1465631A4 (en) 2005-03-30
EP1465631B1 (en) 2010-02-24
US20030162764A1 (en) 2003-08-28
AU2002366811B2 (en) 2009-01-15
AU2002366811A1 (en) 2003-07-09
US20050119271A1 (en) 2005-06-02
EA007468B1 (ru) 2006-10-27
US6916804B2 (en) 2005-07-12
WO2003053366A2 (en) 2003-07-03
JP2005517659A (ja) 2005-06-16
JP4440642B2 (ja) 2010-03-24
KR20040068317A (ko) 2004-07-30
WO2003053366A3 (en) 2004-01-29
EA200400830A1 (ru) 2004-12-30

Similar Documents

Publication Publication Date Title
EA200600315A1 (ru) Пиримидиновые соединения, их применение в качестве a-селективных антагонистов и способ их получения
RU2353616C2 (ru) Производные 2-пиридона в качестве ингибиторов эластазы нейтрофилов и их применение
RU2373209C2 (ru) Пирролотриазиновые соединения как ингибиторы киназ
KR100476586B1 (ko) 치환된 피리미딘온 화합물과 이 화합물을 포함하는 제약학적 조성물 및 치료방법
PE20060197A1 (es) Heterociclos biciclicos como inhibidores de cinasa
ATE123771T1 (de) Stickstoff enthaltende heterozyklische verbindungen, ihre herstellung und verwendung.
PE20060374A1 (es) Inhibidores de cinasa heterociclicos fusionados
AU2005304040A1 (en) Aminoquinazolines compounds
CN1152870A (zh) 杂环化合物作为多巴胺d3配位体的用途
NO20033385D0 (no) Fuserte heterocykliske forbindelser
PE20020219A1 (es) Derivados de 6-fenilpirrolpirimidindiona como inhibidores de fosfodiesterasa 5
JP2005526068A (ja) 抗炎症剤としての単環式アロイルピリジノン類
ATE139233T1 (de) Annelierte thiophen-derivate, ihre herstellung und verwendung
DE60336576D1 (de) Hemmer der akt aktivität
RU2003129638A (ru) Новые соединения
PE20100737A1 (es) Nuevos compuestos
RU2006146632A (ru) Производные хиназолинона, полезные в качестве ванилоидных антагонистов
PE20060625A1 (es) Derivados de benzazepina como antagonistas y/o agonistas del receptor h3 de histamina
JP2000503987A (ja) 炎症処置用の異項環置換イミダゾール
JP7381602B2 (ja) 二環式及び三環式化合物
PE20060770A1 (es) Derivados de n-[(4,5-difenil-3-alquil-2-tienil)metil]amina como antagonistas de los receptores cannabinoides cb1
PE20071086A1 (es) DERIVADOS DE PIRAZOLOISOQUINOLINA COMO INHIBIDORES DE LA CINASA p38
KR20220016177A (ko) 트라이사이클릭 화합물
JO2307B1 (en) Papermidine derivatives
MXPA02011464A (es) Derivados 1,4-diazepan-2,5-diona y su uso como antagonistas del receptor de la nk-1.

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU