CA2377746A1 - N-pyrazole a2a receptor agonists - Google Patents

N-pyrazole a2a receptor agonists Download PDF

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Publication number
CA2377746A1
CA2377746A1 CA002377746A CA2377746A CA2377746A1 CA 2377746 A1 CA2377746 A1 CA 2377746A1 CA 002377746 A CA002377746 A CA 002377746A CA 2377746 A CA2377746 A CA 2377746A CA 2377746 A1 CA2377746 A1 CA 2377746A1
Authority
CA
Canada
Prior art keywords
receptor agonists
pyrazole
compounds
purposes
adenosine
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002377746A
Other languages
French (fr)
Other versions
CA2377746C (en
Inventor
Jeff A. Zablocki
Elfatih O. Elzein
Venkata P. Palle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
Original Assignee
Cv Therapeutics, Inc.
Jeff A. Zablocki
Elfatih O. Elzein
Venkata P. Palle
Gilead Palo Alto, Inc.
Gilead Sciences, Inc.
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 Cv Therapeutics, Inc., Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle, Gilead Palo Alto, Inc., Gilead Sciences, Inc. filed Critical Cv Therapeutics, Inc.
Publication of CA2377746A1 publication Critical patent/CA2377746A1/en
Application granted granted Critical
Publication of CA2377746C publication Critical patent/CA2377746C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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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 the following formula:

(see formula I) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilation for therapeutic purposes and for purposes of imaging the heart.
CA002377746A 1999-06-22 2000-06-21 N-pyrazole a2a receptor agonists Expired - Lifetime CA2377746C (en)

Applications Claiming Priority (3)

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
PCT/US2000/040281 WO2000078779A2 (en) 1999-06-22 2000-06-21 N-pyrazole a2a receptor agonists

Publications (2)

Publication Number Publication Date
CA2377746A1 true CA2377746A1 (en) 2000-12-28
CA2377746C CA2377746C (en) 2007-04-10

Family

ID=23323763

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002377746A Expired - Lifetime CA2377746C (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) CY2011002I2 (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)

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US8071566B2 (en) 2000-02-23 2011-12-06 Gilead Sciences, Inc. Methods of coronary imaging
US8106183B2 (en) 2006-02-03 2012-01-31 Gilead Sciences, Inc. Process for preparing an A2A-adenosine receptor agonist and its polymorphs
US8133879B2 (en) 2002-07-29 2012-03-13 Gilead Sciences, Inc. Myocardial perfusion imaging methods and compositions
US8183226B2 (en) 2002-07-29 2012-05-22 Gilead Sciences, Inc. Myocardial perfusion imaging method
US8278435B2 (en) 1999-06-22 2012-10-02 Gilead Sciences, Inc. N-pyrazole A2A receptor agonists
US8470801B2 (en) 2002-07-29 2013-06-25 Gilead Sciences, Inc. Myocardial perfusion imaging methods and compositions
USRE47351E1 (en) 1999-06-22 2019-04-16 Gilead Sciences, Inc. 2-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists

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