WO2000078779A3 - N-pyrazole a2a receptor agonists - Google Patents

N-pyrazole a2a receptor agonists Download PDF

Info

Publication number
WO2000078779A3
WO2000078779A3 PCT/US2000/040281 US0040281W WO0078779A3 WO 2000078779 A3 WO2000078779 A3 WO 2000078779A3 US 0040281 W US0040281 W US 0040281W WO 0078779 A3 WO0078779 A3 WO 0078779A3
Authority
WO
WIPO (PCT)
Prior art keywords
receptor agonists
pyrazole
compounds
purposes
adenosine
Prior art date
Application number
PCT/US2000/040281
Other languages
French (fr)
Other versions
WO2000078779A2 (en
Inventor
Jeff A Zablocki
Elfatih O Elzein
Venkata P Palle
Original Assignee
Cv Therapeutics Inc
Jeff A Zablocki
Elfatih O Elzein
Venkata P Palle
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 to NZ516334A priority Critical patent/NZ516334A/en
Priority to AT00960112T priority patent/ATE256141T1/en
Application filed by Cv Therapeutics Inc, Jeff A Zablocki, Elfatih O Elzein, Venkata P Palle filed Critical Cv Therapeutics Inc
Priority to AU71324/00A priority patent/AU760806B2/en
Priority to DE122011000010C priority patent/DE122011000010I1/en
Priority to JP2001515876A priority patent/JP4727880B2/en
Priority to IL14719800A priority patent/IL147198A0/en
Priority to DE60007127T priority patent/DE60007127T2/en
Priority to BRPI0011856A priority patent/BRPI0011856B8/en
Priority to EP00960112A priority patent/EP1189916B1/en
Priority to DK00960112T priority patent/DK1189916T3/en
Priority to US10/018,446 priority patent/US6642210B1/en
Priority to CA002377746A priority patent/CA2377746C/en
Priority to US15/635,017 priority patent/USRE47351E1/en
Priority to MXPA01013325A priority patent/MXPA01013325A/en
Publication of WO2000078779A2 publication Critical patent/WO2000078779A2/en
Publication of WO2000078779A3 publication Critical patent/WO2000078779A3/en
Priority to IL147198A priority patent/IL147198A/en
Priority to NO20016350A priority patent/NO322457B1/en
Priority to HK02106507.1A priority patent/HK1044952B/en
Priority to US10/652,378 priority patent/US7183264B2/en
Priority to US11/252,760 priority patent/US7144872B2/en
Priority to US11/588,834 priority patent/US7655637B2/en
Priority to US12/637,311 priority patent/US20100160620A1/en
Priority to US12/968,110 priority patent/US8278435B2/en
Priority to LU91785C priority patent/LU91785I2/en
Priority to FR11C0004C priority patent/FR11C0004I2/en
Priority to NO2011002C priority patent/NO2011002I2/en
Priority to CY2011002C priority patent/CY2011002I1/en
Priority to US13/598,451 priority patent/US8569260B2/en
Priority to US14/020,736 priority patent/US9045519B2/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Abstract

2-Adenosine N-pyrazole compounds having formula (1) and methods for using compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
PCT/US2000/040281 1999-06-22 2000-06-21 N-pyrazole a2a receptor agonists WO2000078779A2 (en)

Priority Applications (28)

Application Number Priority Date Filing Date Title
DE60007127T DE60007127T2 (en) 1999-06-22 2000-06-21 N-PYRAZOLE A2A RECEPTOR AGONISTS
MXPA01013325A MXPA01013325A (en) 1999-06-22 2000-06-21 N-pyrazole a2.
AU71324/00A AU760806B2 (en) 1999-06-22 2000-06-21 N-pyrazole A2A receptor agonists
DE122011000010C DE122011000010I1 (en) 1999-06-22 2000-06-21 N-PYRAZOL A2A RECEPTOR AGONISTS
JP2001515876A JP4727880B2 (en) 1999-06-22 2000-06-21 N-pyrazole A2A receptor agonist
IL14719800A IL147198A0 (en) 1999-06-22 2000-06-21 N-pyrazole a2a receptor agonists
AT00960112T ATE256141T1 (en) 1999-06-22 2000-06-21 N-PYRAZOLE A2A RECEPTOR AGONISTS
BRPI0011856A BRPI0011856B8 (en) 1999-06-22 2000-06-21 n-pyrazole a2a receptor agonists
EP00960112A EP1189916B1 (en) 1999-06-22 2000-06-21 N-pyrazole a 2a receptor agonists
DK00960112T DK1189916T3 (en) 1999-06-22 2000-06-21 N-pyrazole A 2A receptor agonists
US10/018,446 US6642210B1 (en) 1999-06-22 2000-06-21 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
CA002377746A CA2377746C (en) 1999-06-22 2000-06-21 N-pyrazole a2a receptor agonists
US15/635,017 USRE47351E1 (en) 1999-06-22 2000-06-21 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
NZ516334A NZ516334A (en) 1999-06-22 2000-06-21 N-pyrazole A2A receptor agonists
IL147198A IL147198A (en) 1999-06-22 2001-12-19 N-pyrazole a2a receptor agonists
NO20016350A NO322457B1 (en) 1999-06-22 2001-12-21 N-pyrazole A2A receptor agonists, pharmaceutical composition comprising the same and use of the same for the preparation of drug.
HK02106507.1A HK1044952B (en) 1999-06-22 2002-09-04 N-pyrazole a2a receptor agonists
US10/652,378 US7183264B2 (en) 1999-06-22 2003-08-29 N-pyrazole A2A receptor agonists
US11/252,760 US7144872B2 (en) 1999-06-22 2005-10-18 N-pyrazole A2A receptor agonists
US11/588,834 US7655637B2 (en) 1999-06-22 2006-10-27 N-pyrazole A2A receptor agonists
US12/637,311 US20100160620A1 (en) 1999-06-22 2009-12-14 N-pyrazole a2a receptor agonists
US12/968,110 US8278435B2 (en) 1999-06-22 2010-12-14 N-pyrazole A2A receptor agonists
LU91785C LU91785I2 (en) 1999-06-22 2011-01-31 Rapiscan - regadenoson and its salts.
FR11C0004C FR11C0004I2 (en) 1999-06-22 2011-02-07 N-PYRAZOLE 2A RECEPTOR AGONISTS
NO2011002C NO2011002I2 (en) 1999-06-22 2011-02-09 Regadenosone and its salts
CY2011002C CY2011002I1 (en) 1999-06-22 2011-02-16 N-PYRRAZOLE A2A RECEPTOR AGENTS
US13/598,451 US8569260B2 (en) 1999-06-22 2012-08-29 N-pyrazole A2A receptor agonists
US14/020,736 US9045519B2 (en) 1999-06-22 2013-09-06 N-pyrazole A2A receptor agonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US09/338,185 US6403567B1 (en) 1999-06-22 1999-06-22 N-pyrazole A2A adenosine receptor agonists
US09/338,185 1999-06-22

Related Parent Applications (3)

Application Number Title Priority Date Filing Date
US09/338,185 Continuation-In-Part US6403567B1 (en) 1999-06-22 1999-06-22 N-pyrazole A2A adenosine receptor agonists
US09/338,185 Continuation US6403567B1 (en) 1999-06-22 1999-06-22 N-pyrazole A2A adenosine receptor agonists
US09/388,185 Continuation-In-Part US6421138B1 (en) 1999-09-01 1999-09-01 Page allocation/deallocation procedure for a printer/copier with accessory media sheet handling apparatus

Related Child Applications (4)

Application Number Title Priority Date Filing Date
US10018446 A-371-Of-International 2000-06-21
US10018466 A-371-Of-International 2000-06-21
US10/018,446 A-371-Of-International US6642210B1 (en) 1999-06-22 2000-06-21 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
US10/652,378 Continuation US7183264B2 (en) 1999-06-22 2003-08-29 N-pyrazole A2A receptor agonists

Publications (2)

Publication Number Publication Date
WO2000078779A2 WO2000078779A2 (en) 2000-12-28
WO2000078779A3 true WO2000078779A3 (en) 2001-03-15

Family

ID=23323763

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2000/040281 WO2000078779A2 (en) 1999-06-22 2000-06-21 N-pyrazole a2a receptor agonists

Country Status (27)

Country Link
US (9) US6403567B1 (en)
EP (1) EP1189916B1 (en)
JP (1) JP4727880B2 (en)
KR (1) KR100463300B1 (en)
CN (1) CN1167709C (en)
AR (1) AR024441A1 (en)
AT (1) ATE256141T1 (en)
AU (1) AU760806B2 (en)
BE (1) BE2011C004I2 (en)
BR (1) BRPI0011856B8 (en)
CA (1) CA2377746C (en)
CY (1) CY2011002I1 (en)
DE (2) DE60007127T2 (en)
DK (1) DK1189916T3 (en)
ES (1) ES2209974T3 (en)
FR (1) FR11C0004I2 (en)
HK (1) HK1044952B (en)
IL (2) IL147198A0 (en)
LU (1) LU91785I2 (en)
MX (1) MXPA01013325A (en)
NO (2) NO322457B1 (en)
NZ (1) NZ516334A (en)
PT (1) PT1189916E (en)
TR (1) TR200200588T2 (en)
TW (1) TWI230161B (en)
WO (1) WO2000078779A2 (en)
ZA (1) ZA200200301B (en)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9085601B2 (en) 2006-02-03 2015-07-21 Gilead Sciences, Inc. Process for preparing an A2A-adenosine receptor agonist and its polymorphs
US9163057B2 (en) 2000-02-23 2015-10-20 Gilead Sciences, Inc. Methods of myocardial perfusion imaging

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6214807B1 (en) * 1999-06-22 2001-04-10 Cv Therapeutics, Inc. C-pyrazole 2A A receptor agonists
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
US20050059068A1 (en) * 2001-05-23 2005-03-17 Stratagene California Compositions and methods using dendrimer-treated microassays
US7262176B2 (en) 2001-08-08 2007-08-28 Cv Therapeutics, Inc. Adenosine A3 receptor agonists
US20030078232A1 (en) * 2001-08-08 2003-04-24 Elfatih Elzein Adenosine receptor A3 agonists
KR20040097126A (en) 2002-02-15 2004-11-17 씨브이 쎄러퓨틱스, 인코포레이티드 Polymer coating for medical devices
NZ537975A (en) * 2002-07-29 2007-08-31 Cv Therapeutics Inc Method of producing coronary vasodilation without peripheral vasodilation comprising administering at least 10 mcg of at least one A2A receptor agonist
US20050020915A1 (en) * 2002-07-29 2005-01-27 Cv Therapeutics, Inc. Myocardial perfusion imaging methods and compositions
US8470801B2 (en) * 2002-07-29 2013-06-25 Gilead Sciences, Inc. Myocardial perfusion imaging methods and compositions
DE60330250D1 (en) 2002-09-09 2010-01-07 Cv Therapeutics Inc ADENOSINE A3 RECEPTOR AGONISTS
CA2554169C (en) 2004-01-27 2010-03-16 Cv Therapeutics, Inc. Myocardial perfusion imaging using adenosine receptor agonists
TWI346109B (en) * 2004-04-30 2011-08-01 Otsuka Pharma Co Ltd 4-amino-5-cyanopyrimidine derivatives
KR101167342B1 (en) 2004-05-26 2012-07-19 이노텍 파마슈티컬스 코포레이션 Purine derivatives as adenosine a1 receptor agonists and methods of use thereof
MX2007003271A (en) * 2004-09-20 2007-06-05 Inotek Pharmaceuticals Corp Purine derivatives and methods of use thereof.
CN101076343A (en) * 2004-10-20 2007-11-21 Cv医药有限公司 Use of A2A adenosine receptor agonists
GT200500281A (en) * 2004-10-22 2006-04-24 Novartis Ag ORGANIC COMPOUNDS.
GB0500785D0 (en) * 2005-01-14 2005-02-23 Novartis Ag Organic compounds
GB0505219D0 (en) * 2005-03-14 2005-04-20 Novartis Ag Organic compounds
EP1883646A1 (en) * 2005-05-19 2008-02-06 Cv Therapeutics, Inc. A1 adenosine receptor agonists
WO2007064795A2 (en) * 2005-11-30 2007-06-07 Inotek Pharmaceuticals Corporation Purine derivatives and methods of use thereof
US20070183995A1 (en) * 2006-02-09 2007-08-09 Conopco, Inc., D/B/A Unilever Compounds useful as agonists of A2A adenosine receptors, cosmetic compositions with A2A agonists and a method for using the same
GB0607944D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607951D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
JP5373599B2 (en) 2006-04-21 2013-12-18 ノバルティス アーゲー Purine derivatives for use as adenosine A2A receptor agonists
GB0607950D0 (en) * 2006-04-21 2006-05-31 Novartis Ag Organic compounds
DE102006020349A1 (en) 2006-04-28 2007-10-31 Mahle International Gmbh Piston engine and associated operating method
US7691825B2 (en) * 2006-06-06 2010-04-06 King Pharmaceuticals Research And Development, Inc. Adenosine A2B receptor agonists
MX2008016254A (en) * 2006-06-22 2009-01-15 Cv Therapeutics Inc Use of a2a adenosine receptor agonists in the treatment of ischemia.
EP1889846A1 (en) * 2006-07-13 2008-02-20 Novartis AG Purine derivatives as A2a agonists
US20090081120A1 (en) * 2006-09-01 2009-03-26 Cv Therapeutics, Inc. Methods and Compositions for Increasing Patient Tolerability During Myocardial Imaging Methods
KR20090047499A (en) * 2006-09-01 2009-05-12 씨브이 쎄러퓨틱스, 인코포레이티드 Methods and compositions for increasing patient tolerability during myocardial imaging methods
EP1903044A1 (en) * 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
JP2011502101A (en) * 2006-09-29 2011-01-20 ギリアード・パロ・アルト・インコーポレイテッド Myocardial imaging in patients with a history of lung disease
MX2009004991A (en) * 2006-11-10 2009-05-20 Novartis Ag Cyclopentene diol monoacetate derivatives.
WO2008086096A2 (en) * 2007-01-03 2008-07-17 Cv Therapeutics, Inc. Myocardial perfusion imaging
JP2008285478A (en) * 2007-04-16 2008-11-27 Santen Pharmaceut Co Ltd Therapeutic agent for glaucoma comprising adenosine a2a receptor agonist as effective component
RU2443708C2 (en) * 2007-05-17 2012-02-27 Си Ви Терапьютикс, Инк. Method of producing a2a-adenosine receptor agonist and polymorphic modifications thereof
PT2158208E (en) * 2007-05-17 2015-06-11 Gilead Sciences Inc Process for preparing an a2a-adenosine receptor agonist and its polymorphs
US7868001B2 (en) * 2007-11-02 2011-01-11 Hutchison Medipharma Enterprises Limited Cytokine inhibitors
US7899039B2 (en) * 2008-02-15 2011-03-01 Cisco Technology, Inc. System and method for providing location and access network information support in a network environment
EP2300489B1 (en) * 2008-06-06 2015-11-11 Harbor Therapeutics, Inc. Methods for preparing 17-alkynyl-7-hydroxy steroids and related compounds
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
US7957314B2 (en) * 2008-12-12 2011-06-07 Cisco Technology, Inc. System and method for provisioning charging and policy control in a network environment
EP2523669B1 (en) 2010-01-11 2016-12-07 Inotek Pharmaceuticals Corporation Combination, kit and method of reducing intraocular pressure
SG184221A1 (en) 2010-03-26 2012-10-30 Inotek Pharmaceuticals Corp Method of reducing intraocular pressure in humans using n6 -cyclopentyladenosine (cpa), cpa derivatives or prodrugs thereof
US20130109645A1 (en) 2010-03-31 2013-05-02 The united States of America,as represented by Secretary,Dept.,of Health and Human Services Adenosine receptor agonists for the treatment and prevention of vascular or joint capsule calcification disorders
US9215588B2 (en) 2010-04-30 2015-12-15 Cisco Technology, Inc. System and method for providing selective bearer security in a network environment
JP2011098990A (en) * 2011-02-21 2011-05-19 Gilead Palo Alto Inc Myocardial perfusion imaging using adenosine receptor agonist
US8859522B2 (en) 2011-04-27 2014-10-14 Reliable Biopharmaceutical Corporation Processes for the preparation of regadenoson and a new crystalline form thereof
CZ308577B6 (en) 2011-08-18 2020-12-16 Farmak, A. S. Process for preparing 2- (4-methoxy carbonyl pyrazol-1-yl) adenosine and 2- (4-ethoxycarbonylpyrazol-1-yl) adenosine
CZ304053B6 (en) 2011-08-22 2013-09-04 Farmak, A. S. Process for preparing 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate
DK2807178T3 (en) 2012-01-26 2017-09-04 Inotek Pharmaceuticals Corp Anhydrous polymorphs of (2R, 3S, 4R, 5R) -5- (6- (cyclopentylamino) -9H-purin-9-yl) -3,4-dihydroxytetrahydrofuran-2-yl) methyl nitrate and processes for their preparation
US20150290236A1 (en) * 2012-11-30 2015-10-15 Leiutis Pharmaceuticals Pvt. Ltd. Pharmaceutical compositions of regadenoson
WO2014152723A1 (en) 2013-03-15 2014-09-25 Inotek Pharmaceuticals Corporation Ophthalmic formulations
EP2789624B1 (en) 2013-04-11 2020-09-23 AMRI Italy S.r.l. Stable solid forms of regadenoson
CZ305213B6 (en) * 2013-04-29 2015-06-10 Farmak, A. S. Polymorph E, 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine and process for its preparation
WO2014207758A2 (en) 2013-05-30 2014-12-31 Biophore India Pharmaceuticals Pvt. Ltd. Novel polymorph of regadenoson
CN104513241B (en) * 2013-09-30 2017-02-08 浙江海正药业股份有限公司 New regadenoson intermediate, preparation method and application thereof
CN104744540A (en) * 2013-12-26 2015-07-01 上海紫源制药有限公司 Preparation method for regadenoson
CN105085593A (en) * 2014-04-21 2015-11-25 上海紫源制药有限公司 Regadenoson crystal form and preparation method thereof
WO2016126734A1 (en) 2015-02-06 2016-08-11 Apicore Us Llc Process of making regadenoson and novel polymorph thereof
US9809617B2 (en) 2015-07-03 2017-11-07 Shanghai Ziyuan Pharmaceutical Co., Ltd. Crystal form of regadenoson and preparation method thereof
CN106397442B (en) * 2015-07-28 2020-03-27 国药集团国瑞药业有限公司 Purification method of regadenoson
TWI739983B (en) 2017-01-13 2021-09-21 日商東菱藥品工業股份有限公司 Neutrophil activation regulator
WO2019191389A1 (en) 2018-03-29 2019-10-03 Johnson Matthey Public Limited Company Solid-state forms of regadenoson, their use and preparation
US10815265B2 (en) 2018-06-29 2020-10-27 Usv Private Limited Process for preparation of regadenoson and polymorphs thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0354638A2 (en) * 1988-08-11 1990-02-14 Medco Research Inc Use of adenosine and its derivatives in diagnosis

Family Cites Families (85)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK135130B (en) 1970-12-28 1977-03-07 Takeda Chemical Industries Ltd Analogous process for the preparation of 2-substituted adenosine derivatives or acid addition salts thereof.
BE787064A (en) 1971-08-03 1973-02-01 Philips Nv MAGNETIC DEVICE CONTAINING DOMAINS
US3845770A (en) * 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US4120947A (en) * 1976-03-31 1978-10-17 Cooper Laboratories, Inc. Xanthine compounds and method of treating bronchospastic and allergic diseases
US4089959A (en) * 1976-03-31 1978-05-16 Cooper Laboratories, Inc. Long-acting xanthine bronchodilators and antiallergy agents
SE7810946L (en) * 1978-10-20 1980-04-21 Draco Ab METHOD OF TREATING CHRONIC OBSTRUCTIVE AIR DISEASE
US4326525A (en) * 1980-10-14 1982-04-27 Alza Corporation Osmotic device that improves delivery properties of agent in situ
US4593095A (en) * 1983-02-18 1986-06-03 The Johns Hopkins University Xanthine derivatives
US5364620A (en) * 1983-12-22 1994-11-15 Elan Corporation, Plc Controlled absorption diltiazem formulation for once daily administration
US4696932A (en) * 1984-10-26 1987-09-29 The United States Of America As Represented By The Department Of Health And Human Services Biologically-active xanthine derivatives
JPS6299395A (en) 1985-10-25 1987-05-08 Yamasa Shoyu Co Ltd 2-alkinyladenosine and antihypertensive
US4968697A (en) * 1987-02-04 1990-11-06 Ciba-Geigy Corporation 2-substituted adenosine 5'-carboxamides as antihypertensive agents
US5001139A (en) * 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) * 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US4990498A (en) * 1988-04-26 1991-02-05 Temple University-Of The Commonwealth System Of Higher Education 2- and 8-azido(2'-5')oligoadenylates and antiviral uses thereof
US4902514A (en) * 1988-07-21 1990-02-20 Alza Corporation Dosage form for administering nilvadipine for treating cardiovascular symptoms
DE3831430A1 (en) * 1988-09-15 1990-03-22 Bayer Ag SUBSTITUTED 4-HETEROCYCLYLOXIMINO-PYRAZOLIN-5-ONE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS A PEST CONTROL
KR0137786B1 (en) 1988-11-15 1998-05-15 하마구찌 미찌오 Agent for treatment and prophylaxis of ischemic disease of heart or brain
IT1229195B (en) 1989-03-10 1991-07-25 Poli Ind Chimica Spa XANTHINIC DERIVATIVES WITH BRONCODILATORY ACTIVITY AND THEIR THERAPEUTIC APPLICATIONS.
EP0429681B1 (en) 1989-06-20 1995-09-06 Yamasa Shoyu Kabushiki Kaisha (Yamasa Corporation) Intermediate for 2-alkynyladenosine synthesis, production of said intermediate, production of 2-alkynyladenosine from said intermediate, and stable 2-alkynyladenosine derivative
US5032252A (en) * 1990-04-27 1991-07-16 Mobil Oil Corporation Process and apparatus for hot catalyst stripping in a bubbling bed catalyst regenerator
DE4019892A1 (en) 1990-06-22 1992-01-02 Boehringer Ingelheim Kg New xanthine derivs. are selective A1 adenosine antagonists - useful for treating CNS disorders (e.g. senile dementia) and heart and circulation disorders
US5189027A (en) 1990-11-30 1993-02-23 Yamasa Shoyu Kabushiki Kaisha 2-substituted adenosine derivatives and pharmaceutical compositions for circulatory diseases
FR2671356B1 (en) 1991-01-09 1993-04-30 Inst Nat Sante Rech Med METHOD FOR DESCRIBING ANTIBODY (AB) DIRECTORIES AND T CELL RECEPTORS (TCR) IN THE INDIVIDUAL'S IMMUNE SYSTEM.
JP2740362B2 (en) 1991-02-12 1998-04-15 ヤマサ醤油株式会社 Stable solid 2-octynyl adenosine and process for its preparation
JP3053908B2 (en) 1991-06-28 2000-06-19 ヤマサ醤油株式会社 2-alkynyl adenosine derivatives
US5516894A (en) * 1992-03-11 1996-05-14 The General Hospital Corporation A2b -adenosine receptors
IT1254915B (en) 1992-04-24 1995-10-11 Gloria Cristalli ADENOSINE DERIVATIVES FOR ACTIVITY A2 AGONIST
GB9210839D0 (en) 1992-05-21 1992-07-08 Smithkline Beecham Plc Novel compounds
WO1993025677A1 (en) 1992-06-12 1993-12-23 Garvan Institute Of Medical Research DNA SEQUENCES ENCODING THE HUMAN A1, A2a and A2b ADENOSINE RECEPTORS
EP0601322A3 (en) 1992-10-27 1994-10-12 Nippon Zoki Pharmaceutical Co Adenosindeaminase inhibitor.
CA2112031A1 (en) * 1992-12-24 1994-06-25 Fumio Suzuki Xanthine derivatives
US5477857A (en) 1993-09-10 1995-12-26 Discovery Therapeutics, Inc. Diagnostic uses of hydrazinoadenosines
WO1995011681A1 (en) 1993-10-29 1995-05-04 Merck & Co., Inc. Human adenosine receptor antagonists
DE69526822T2 (en) * 1994-02-23 2003-01-23 Kyowa Hakko Kogyo Kk Xanthine derivatives
US5704491A (en) * 1995-07-21 1998-01-06 Cummins-Allison Corp. Method and apparatus for discriminating and counting documents
US5646156A (en) * 1994-04-25 1997-07-08 Merck & Co., Inc. Inhibition of eosinophil activation through A3 adenosine receptor antagonism
US6448235B1 (en) * 1994-07-11 2002-09-10 University Of Virginia Patent Foundation Method for treating restenosis with A2A adenosine receptor agonists
US6514949B1 (en) * 1994-07-11 2003-02-04 University Of Virginia Patent Foundation Method compositions for treating the inflammatory response
US5877180A (en) * 1994-07-11 1999-03-02 University Of Virginia Patent Foundation Method for treating inflammatory diseases with A2a adenosine receptor agonists
US5854081A (en) * 1996-06-20 1998-12-29 The University Of Patent Foundation Stable expression of human A2B adenosine receptors, and assays employing the same
US5780481A (en) * 1996-08-08 1998-07-14 Merck & Co., Inc. Method for inhibiting activation of the human A3 adenosine receptor to treat asthma
US5776960A (en) * 1996-10-16 1998-07-07 Buckman Laboratories International, Inc. Synergistic antimicrobial compositions containing an ionene polymer and a pyrithione salt and methods of using the same
US5770716A (en) 1997-04-10 1998-06-23 The Perkin-Elmer Corporation Substituted propargylethoxyamido nucleosides, oligonucleotides and methods for using same
WO1998052611A1 (en) 1997-05-23 1998-11-26 Nippon Shinyaku Co., Ltd. Medicinal composition for prevention or treatment of hepatopathy
CA2295195C (en) 1997-06-18 2009-12-15 Discovery Therapeutics, Inc. Compositions and methods for preventing restenosis following revascularization procedures
US6026317A (en) 1998-02-06 2000-02-15 Baylor College Of Medicine Myocardial perfusion imaging during coronary vasodilation with selective adenosine A2 receptor agonists
US6117878A (en) * 1998-02-24 2000-09-12 University Of Virginia 8-phenyl- or 8-cycloalkyl xanthine antagonists of A2B human adenosine receptors
AU4675699A (en) 1998-06-08 1999-12-30 Epigenesis Pharmaceuticals, Inc. Composition and method for prevention and treatment of cardiopulmonary and renal failure or damage associated with ischemia, endotoxin release, ards or brought about by administration of certain drugs
US6322771B1 (en) * 1999-06-18 2001-11-27 University Of Virginia Patent Foundation Induction of pharmacological stress with adenosine receptor agonists
US6403567B1 (en) 1999-06-22 2002-06-11 Cv Therapeutics, Inc. N-pyrazole A2A adenosine receptor agonists
US6214807B1 (en) * 1999-06-22 2001-04-10 Cv Therapeutics, Inc. C-pyrazole 2A A receptor agonists
PT1208100E (en) 1999-08-31 2003-07-31 Univ Vanderbilt SELECTIVE ANTAGONISTS OF A2B ADENOSIN RECEPTORS
US6368573B1 (en) * 1999-11-15 2002-04-09 King Pharmaceuticals Research And Development, Inc. Diagnostic uses of 2-substituted adenosine carboxamides
US6294522B1 (en) * 1999-12-03 2001-09-25 Cv Therapeutics, Inc. N6 heterocyclic 8-modified adenosine derivatives
US6605597B1 (en) * 1999-12-03 2003-08-12 Cv Therapeutics, Inc. Partial or full A1agonists-N-6 heterocyclic 5′-thio substituted adenosine derivatives
US6552023B2 (en) * 2000-02-22 2003-04-22 Cv Therapeutics, Inc. Aralkyl substituted piperazine compounds
US6677336B2 (en) * 2000-02-22 2004-01-13 Cv Therapeutics, Inc. Substituted piperazine compounds
US20020012946A1 (en) * 2000-02-23 2002-01-31 Luiz Belardinelli Method of identifying partial agonists of the A2A receptor
US6387913B1 (en) * 2000-12-07 2002-05-14 S. Jamal Mustafa Method of treating airway diseases with combined administration of A2B and A3 adenosine receptor antagonists
US6670334B2 (en) * 2001-01-05 2003-12-30 University Of Virginia Patent Foundation Method and compositions for treating the inflammatory response
US6995148B2 (en) * 2001-04-05 2006-02-07 University Of Pittsburgh Adenosine cyclic ketals: novel adenosine analogues for pharmacotherapy
US6599283B1 (en) * 2001-05-04 2003-07-29 Cv Therapeutics, Inc. Method of preventing reperfusion injury
US7109203B2 (en) * 2001-05-14 2006-09-19 Novartis Ag Sulfonamide derivatives
US7125993B2 (en) * 2001-11-09 2006-10-24 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
DK1444233T3 (en) * 2001-11-09 2011-10-17 Gilead Palo Alto Inc A 2B adenosine receptor antagonists
US6977300B2 (en) * 2001-11-09 2005-12-20 Cv Therapeutics, Inc. A2B adenosine receptor antagonists
WO2003053366A2 (en) * 2001-12-20 2003-07-03 Osi Pharmaceuticals, Inc. Pyrimidine a2b selective antagonist compounds, their synthesis and use
WO2003086451A1 (en) * 2002-04-05 2003-10-23 Centocor, Inc. Asthma-related anti-il-13 immunoglobulin derived proteins, compositions, methods and uses
EP1494685B1 (en) 2002-04-18 2008-12-31 Cv Therapeutics, Inc. Method of treating arrhythmias comprising administration of an a1 adenosine agonist with a beta blocker
NZ537975A (en) * 2002-07-29 2007-08-31 Cv Therapeutics Inc Method of producing coronary vasodilation without peripheral vasodilation comprising administering at least 10 mcg of at least one A2A receptor agonist
US20050020915A1 (en) * 2002-07-29 2005-01-27 Cv Therapeutics, Inc. Myocardial perfusion imaging methods and compositions
CA2554169C (en) 2004-01-27 2010-03-16 Cv Therapeutics, Inc. Myocardial perfusion imaging using adenosine receptor agonists
JP2008516969A (en) * 2004-10-15 2008-05-22 シーブイ・セラピューティクス・インコーポレイテッド Methods of preventing and treating airway remodeling and lung inflammation using A2B adenosine receptor antagonists
CN101076343A (en) * 2004-10-20 2007-11-21 Cv医药有限公司 Use of A2A adenosine receptor agonists
AU2006204716A1 (en) 2005-01-12 2006-07-20 King Pharmaceuticals Reserch & Development, Inc. Method of detecting myocardial dysfunction in patients having a history of asthma or bronchospasm
US7732595B2 (en) * 2006-02-03 2010-06-08 Gilead Palo Alto, Inc. Process for preparing an A2A-adenosine receptor agonist and its polymorphs
MX2008016254A (en) * 2006-06-22 2009-01-15 Cv Therapeutics Inc Use of a2a adenosine receptor agonists in the treatment of ischemia.
US20090081120A1 (en) * 2006-09-01 2009-03-26 Cv Therapeutics, Inc. Methods and Compositions for Increasing Patient Tolerability During Myocardial Imaging Methods
KR20090047499A (en) * 2006-09-01 2009-05-12 씨브이 쎄러퓨틱스, 인코포레이티드 Methods and compositions for increasing patient tolerability during myocardial imaging methods
JP2011502101A (en) * 2006-09-29 2011-01-20 ギリアード・パロ・アルト・インコーポレイテッド Myocardial imaging in patients with a history of lung disease
WO2008086096A2 (en) 2007-01-03 2008-07-17 Cv Therapeutics, Inc. Myocardial perfusion imaging
PT2158208E (en) 2007-05-17 2015-06-11 Gilead Sciences Inc Process for preparing an a2a-adenosine receptor agonist and its polymorphs
US20100272711A1 (en) 2007-12-12 2010-10-28 Thomas Jefferson University Compositions and methods for the treatment and prevention of cardiovascular diseases
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0354638A2 (en) * 1988-08-11 1990-02-14 Medco Research Inc Use of adenosine and its derivatives in diagnosis

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
R. MARUMOTO ET AL.: "Synthesis and coronary vasodilating activity of 2-substituted adenosines", CHEM. PHARM. BULL., vol. 23, no. 4, 1975, pages 759 - 774, XP002154408 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9163057B2 (en) 2000-02-23 2015-10-20 Gilead Sciences, Inc. Methods of myocardial perfusion imaging
US9085601B2 (en) 2006-02-03 2015-07-21 Gilead Sciences, Inc. Process for preparing an A2A-adenosine receptor agonist and its polymorphs

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