WO2003086408A1 - Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases - Google Patents

Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases Download PDF

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Publication number
WO2003086408A1
WO2003086408A1 PCT/US2003/011146 US0311146W WO03086408A1 WO 2003086408 A1 WO2003086408 A1 WO 2003086408A1 US 0311146 W US0311146 W US 0311146W WO 03086408 A1 WO03086408 A1 WO 03086408A1
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WO
WIPO (PCT)
Prior art keywords
carboxylic acid
piperidine
aryl
alkyl
alkylene
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.)
Ceased
Application number
PCT/US2003/011146
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English (en)
French (fr)
Other versions
WO2003086408A8 (en
Inventor
Joel M. Linden
Gail W. Sullivan
Timothy L. Macdonald
W. Michael Scheld
Tom G. Obrig
Jayson M. Rieger
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.)
UVA Licensing and Ventures Group
University of Virginia UVA
Original Assignee
University of Virginia UVA
University of Virginia Patent Foundation
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Publication date
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Application filed by University of Virginia UVA, University of Virginia Patent Foundation filed Critical University of Virginia UVA
Priority to DE60318192T priority Critical patent/DE60318192T2/de
Priority to AU2003234716A priority patent/AU2003234716A1/en
Priority to EP03728372A priority patent/EP1496911B1/en
Priority to JP2003583427A priority patent/JP2006515829A/ja
Publication of WO2003086408A1 publication Critical patent/WO2003086408A1/en
Anticipated expiration legal-status Critical
Publication of WO2003086408A8 publication Critical patent/WO2003086408A8/en
Ceased legal-status Critical Current

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Classifications

    • 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
    • A61K31/495—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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Definitions

  • Figure 7 illustrates the reduction of the Renal IL-6 in mice exposed to LPS/Stx2 for 6 hours using ATL-146e and ATL-203.
  • Figure 8 illustrates the reduction of chemokine Renal RANTES in kidney samples in mice exposed to LPS/Stx2 for 6 hours using ATL-146e and ATL-203.
  • R a is methyl, ethyl, i-propyl, i-butyl or tert-butyl.
  • R 7 is H, or methyl.
  • X is -CH 2 OR a or -C(O)NR b R c .
  • a more specific value for X is -CH 2 OH or -C(O)NHCH 2 CH 3 .
  • rings comprising R 4 , R 5 and the atom to which they are connected include:
  • R 7 is H
  • X is ethylaminocarbonyl
  • R 1 and R 2 are each hydrogen
  • Z is a 4-piperazine-l -carboxylic acid or ester group wherein R a is methyl, ethyl, isopropyl, isobutyl, or t-butyl, 18; or R 1 and R 9 together are oxo
  • Z is a 4- piperazine-1 -carboxylic acid or ester group wherein R a is methyl, ethyl, isopropyl, isobutyl, or t-butyl, 19.
  • agonists of A 2 A adenosine receptors that are useful in the practice of the present invention include compounds having the formula (IT):
  • R c is H, methyl or phenyl.
  • a specific value for X is CO 2 R a , (C 2 -C 5 )alkanoylmethyl or amido.
  • a specific value for Y is CO 2 R a , (C 2 -C 5 )alkanoylmethyl or amido.
  • a specific value for m is 1.
  • Z 2 is a group of the formula (iii)
  • Suitable Type IN phosphodiesterase (PDE) inhibitors include racemic and optically active 4-(polyalkoxyphenyl)-2-pyrrolidones of general formula (VI):
  • Example 55 Treatment of mice with E. Coli.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Diabetes (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (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)
PCT/US2003/011146 2002-04-10 2003-04-10 Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases Ceased WO2003086408A1 (en)

Priority Applications (4)

Application Number Priority Date Filing Date Title
DE60318192T DE60318192T2 (de) 2002-04-10 2003-04-10 Verwendung von a2a adenosin rezeptor agonisten und anti-pathogene mittel enthaltenden kombinationen zur behandlung von entzündungskrankheiten
AU2003234716A AU2003234716A1 (en) 2002-04-10 2003-04-10 Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases
EP03728372A EP1496911B1 (en) 2002-04-10 2003-04-10 Use of a combination comprising a2a adenosine receptor agonists and anti-pathogenic agents for the treatment of inflammatory diseases
JP2003583427A JP2006515829A (ja) 2002-04-10 2003-04-10 炎症性疾病の処置のための、ａ２ａアデノシン受容体アゴニストの使用

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US37143402P 2002-04-10 2002-04-10
US60/371,434 2002-04-10
US38718402P 2002-06-07 2002-06-07
US60/387,184 2002-06-07

Publications (2)

Publication Number Publication Date
WO2003086408A1 true WO2003086408A1 (en) 2003-10-23
WO2003086408A8 WO2003086408A8 (en) 2005-01-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2003/011146 Ceased WO2003086408A1 (en) 2002-04-10 2003-04-10 Use of a2a adenosine receptor agonists for the treatment of inflammatory diseases

Country Status (7)

Country Link
US (1) US20090170803A1 (enExample)
EP (1) EP1496911B1 (enExample)
JP (1) JP2006515829A (enExample)
AT (1) ATE381336T1 (enExample)
AU (1) AU2003234716A1 (enExample)
DE (1) DE60318192T2 (enExample)
WO (1) WO2003086408A1 (enExample)

Cited By (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006056471A1 (en) 2004-11-29 2006-06-01 Novartis Ag 5-hydroxy-benzothiazole derivatives having beta-2-adrenorecptor agonist activity
US7214665B2 (en) 2001-10-01 2007-05-08 University Of Virginia Patent Foundation 2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
WO2007121920A2 (en) 2006-04-21 2007-11-01 Novartis Ag Purine derivatives for use as adenosin a2a receptor agonists
JP2007536241A (ja) * 2004-05-03 2007-12-13 ユニバーシティ オブ バージニア パテント ファウンデーション 糖尿病性腎症の処置のためのａ２ａアデノシンレセプターアゴニスト
WO2008037477A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as p13k lipid kinase inhibitors
WO2007121918A3 (en) * 2006-04-21 2008-04-10 Novartis Ag Use of 2-(purin-9-yl)-tetrahydofuran-3,4-diol derivatives as adenosine a2a receptor agonists
WO2008052734A1 (en) 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
US7378400B2 (en) 1999-02-01 2008-05-27 University Of Virginia Patent Foundation Method to reduce an inflammatory response from arthritis
US7442687B2 (en) 2004-08-02 2008-10-28 The University Of Virginia Patent Foundation 2-polycyclic propynyl adenosine analogs having A2A agonist activity
WO2009087224A1 (en) 2008-01-11 2009-07-16 Novartis Ag Pyrimidines as kinase inhibitors
US7576069B2 (en) 2004-08-02 2009-08-18 University Of Virginia Patent Foundation 2-polycyclic propynyl adenosine analogs having A2A agonist activity
US7605143B2 (en) 2004-08-02 2009-10-20 University Of Virginia Patent Foundation 2-propynyl adenosine analogs with modified 5′-ribose groups having A2A agonist activity
EP2157091A1 (en) 2003-05-02 2010-02-24 Novartis AG Inhibitors of phosphatidylinositol 3-kinase
EP2206499A1 (en) 2004-11-02 2010-07-14 Novartis AG Quinuclidine derivatives and their use as muscarinic m3 receptor antagonists
WO2010088335A1 (en) 2009-01-29 2010-08-05 Novartis Ag Substituted benzimidazoles for the treatment of astrocytomas
EP2270008A1 (en) 2005-05-20 2011-01-05 Novartis AG 1,3-dihydro-imidazo[4,5-c]quinolin-2-ones as lipid kinase and/or pi3 kinases inhibitors
WO2011004166A1 (en) 2009-07-09 2011-01-13 Cbt Development Limited Combined preparation for use as a medicament
EP2281819A1 (en) 2004-01-21 2011-02-09 Novartis AG Benzimidazolyl or benzoxazolyl derivatives
WO2011015652A1 (en) 2009-08-07 2011-02-10 Novartis Ag 3-heteroarylmethyl-imidazo[1,2-b]pyridazin-6-yl derivatives as c-met tyrosine kinase modulators
WO2011018454A1 (en) 2009-08-12 2011-02-17 Novartis Ag Heterocyclic hydrazone compounds and their uses to treat cancer and inflammation
EP2286813A2 (en) 2006-01-31 2011-02-23 Novartis AG Use of naphthyridine derivatives as medicaments
WO2011020861A1 (en) 2009-08-20 2011-02-24 Novartis Ag Heterocyclic oxime compounds
WO2011022439A1 (en) 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof
US8071565B2 (en) 2006-07-13 2011-12-06 Novartis Ag Purine derivatives as a2a agonists
US8114877B2 (en) 2005-01-14 2012-02-14 Novartis Ag Organic compounds
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
WO2012034091A1 (en) 2010-09-09 2012-03-15 Irm Llc Imidazo [1, 2] pyridazin compounds and compositions as trk inhibitors
US8163754B2 (en) 2004-10-22 2012-04-24 Novartis Ag Purine derivatives for use as adenosine A-2A receptor agonists
US8188100B2 (en) 2006-09-14 2012-05-29 Novartis Ag Adenosine derivatives as A2A receptor agonists
US8193164B2 (en) 2006-04-21 2012-06-05 Novartis Ag Organic compounds
WO2012107500A1 (en) 2011-02-10 2012-08-16 Novartis Ag [1, 2, 4] triazolo [4, 3 -b] pyridazine compounds as inhibitors of the c-met tyrosine kinase
WO2012116237A2 (en) 2011-02-23 2012-08-30 Intellikine, Llc Heterocyclic compounds and uses thereof
WO2012116217A1 (en) 2011-02-25 2012-08-30 Irm Llc Compounds and compositions as trk inhibitors
EP2532677A1 (en) 2005-10-21 2012-12-12 Novartis AG Human antibodies against il13 and therapeutic uses
WO2013038362A1 (en) 2011-09-15 2013-03-21 Novartis Ag 6 - substituted 3 - (quinolin- 6 - ylthio) - [1,2,4] triazolo [4, 3 -a] pyradines as tyrosine kinase
WO2013149581A1 (en) 2012-04-03 2013-10-10 Novartis Ag Combination products with tyrosine kinase inhibitors and their use
WO2014151147A1 (en) 2013-03-15 2014-09-25 Intellikine, Llc Combination of kinase inhibitors and uses thereof
WO2015084804A1 (en) 2013-12-03 2015-06-11 Novartis Ag Combination of mdm2 inhibitor and braf inhibitor and their use
US9174994B2 (en) 2011-11-23 2015-11-03 Intellikine, Llc Enhanced treatment regimens using mTor inhibitors
WO2016011956A1 (en) 2014-07-25 2016-01-28 Novartis Ag Combination therapy
WO2016016822A1 (en) 2014-07-31 2016-02-04 Novartis Ag Combination therapy
US9415058B2 (en) 2008-07-03 2016-08-16 University Of Virginia Patent Foundation Unit dosage of Apadenoson
US9505796B2 (en) 2006-03-21 2016-11-29 Crozet Medical Gmbh Phosphorylated A2A receptor agonists
EP3603634A1 (en) 2004-05-18 2020-02-05 Novartis AG Pharmaceutical composition containing glycopyrrolate and a beta2 adrenoceptor agonist
WO2021152488A1 (en) 2020-01-29 2021-08-05 Novartis Ag Methods of treating an inflammatory or obstructive airway disease using anti-tslp antibody

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8178509B2 (en) * 2006-02-10 2012-05-15 University Of Virginia Patent Foundation Method to treat sickle cell disease
US8188063B2 (en) * 2006-06-19 2012-05-29 University Of Virginia Patent Foundation Use of adenosine A2A modulators to treat spinal cord injury
US8058259B2 (en) * 2007-12-20 2011-11-15 University Of Virginia Patent Foundation Substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters as A2AR agonists
US8293720B2 (en) * 2007-12-20 2012-10-23 Dogwood Pharmaceuticals, Inc. Substituted 4-{3-[6-amino-9-(3, 4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters as A2AR agonists

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5877180A (en) * 1994-07-11 1999-03-02 University Of Virginia Patent Foundation Method for treating inflammatory diseases with A2a adenosine receptor agonists
WO1999034804A1 (en) * 1998-01-08 1999-07-15 The University Of Virginia Patent Foundation A2a adenosine receptor agonists
WO2000072799A2 (en) * 1999-05-27 2000-12-07 The University Of Virginia Patent Foundation Method and compositions for treating the inflammatory response
WO2001094368A1 (en) * 2000-06-06 2001-12-13 Pfizer Limited 2-aminocarbonyl-9h-purine derivatives
US6350735B1 (en) * 1999-10-14 2002-02-26 Pfizer Inc Purine derivatives

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2413935A1 (de) * 1974-03-20 1975-10-16 Schering Ag 4-(polyalkoxy-phenyl)-2-pyrrolidone
US4559157A (en) * 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
LU84979A1 (fr) * 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
US4968697A (en) * 1987-02-04 1990-11-06 Ciba-Geigy Corporation 2-substituted adenosine 5'-carboxamides as antihypertensive agents
US4820508A (en) * 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
US5593973A (en) * 1987-09-04 1997-01-14 Hemispherx Biopharma Inc. Treatment of viral hepatitis with mismatched dsRNA
US4992478A (en) * 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US5561134A (en) * 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
CA2151741C (en) * 1991-12-30 2001-12-11 Alan Justice Methods of producing analgesia and enhancing opiate analgesia
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
GB9415529D0 (en) * 1994-08-01 1994-09-21 Wellcome Found Phenyl xanthine derivatives
GB9723566D0 (en) * 1997-11-08 1998-01-07 Glaxo Group Ltd Chemical compounds
JP2002173427A (ja) * 1998-09-01 2002-06-21 Yamasa Shoyu Co Ltd 眼疾患治療用医薬組成物
BR9914526A (pt) * 1998-10-16 2001-07-03 Pfizer Derivados de adenina
US6232297B1 (en) * 1999-02-01 2001-05-15 University Of Virginia Patent Foundation Methods and compositions for treating inflammatory response
US7378400B2 (en) * 1999-02-01 2008-05-27 University Of Virginia Patent Foundation Method to reduce an inflammatory response from arthritis
US7427606B2 (en) * 1999-02-01 2008-09-23 University Of Virginia Patent Foundation Method to reduce inflammatory response in transplanted tissue
AU2001278708A1 (en) * 2000-09-08 2002-03-22 Toa Eiyo Ltd. Adenosine derivatives and use thereof
GB0022695D0 (en) * 2000-09-15 2000-11-01 Pfizer Ltd Purine Derivatives
US6670334B2 (en) * 2001-01-05 2003-12-30 University Of Virginia Patent Foundation Method and compositions for treating the inflammatory response
BRPI0211932B1 (pt) * 2001-08-17 2016-12-06 Novartis Ag composição farmacêutica na forma de dosagem sólida para liberação oral, e uso de sal dissódio de ácido n-(5-cloro-saliciloil)-8-aminocaprílico (5-cnac)
EP1434782A2 (en) * 2001-10-01 2004-07-07 University of Virginia Patent Foundation 2-propynyl adenosine analogs having a2a agonist activity and compositions thereof
AU2005231440B9 (en) * 2004-04-02 2012-02-23 Dogwood Pharmaceuticals, Inc. Selective antagonists of A2A adenosine receptors
EP1746885A4 (en) * 2004-05-03 2010-09-08 Univ Virginia AGONISTS OF A2A ADENOSINE RECEPTORS FOR THE TREATMENT OF NEEDLE INJURY IN DIABETES
US7605143B2 (en) * 2004-08-02 2009-10-20 University Of Virginia Patent Foundation 2-propynyl adenosine analogs with modified 5′-ribose groups having A2A agonist activity
WO2006028618A1 (en) * 2004-08-02 2006-03-16 University Of Virginia Patent Foundation 2-polycyclic propynyl adenosine analogs with modified 5'-ribose groups having a2a agonist activity
US7442687B2 (en) * 2004-08-02 2008-10-28 The University Of Virginia Patent Foundation 2-polycyclic propynyl adenosine analogs having A2A agonist activity
WO2007092936A2 (en) * 2006-02-08 2007-08-16 University Of Virginia Patent Foundation Method to treat gastric lesions
US8178509B2 (en) * 2006-02-10 2012-05-15 University Of Virginia Patent Foundation Method to treat sickle cell disease
US8188063B2 (en) * 2006-06-19 2012-05-29 University Of Virginia Patent Foundation Use of adenosine A2A modulators to treat spinal cord injury
WO2008124150A1 (en) * 2007-04-09 2008-10-16 University Of Virginia Patent Foundation Method of treating enteritis, intestinal damage, and diarrhea from c. difficile with an a2a adenosine receptor agonist
US20080262001A1 (en) * 2007-04-23 2008-10-23 Adenosine Therapeutics, Llc Agonists of a2a adenosine receptors for treating recurrent tumor growth in the liver following resection

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5877180A (en) * 1994-07-11 1999-03-02 University Of Virginia Patent Foundation Method for treating inflammatory diseases with A2a adenosine receptor agonists
WO1999034804A1 (en) * 1998-01-08 1999-07-15 The University Of Virginia Patent Foundation A2a adenosine receptor agonists
WO2000072799A2 (en) * 1999-05-27 2000-12-07 The University Of Virginia Patent Foundation Method and compositions for treating the inflammatory response
US6350735B1 (en) * 1999-10-14 2002-02-26 Pfizer Inc Purine derivatives
WO2001094368A1 (en) * 2000-06-06 2001-12-13 Pfizer Limited 2-aminocarbonyl-9h-purine derivatives

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
BUSTER B(A) ET AL: "The effect of adenosine receptor agonists on neutrophil pleocytosis and blood-brain barrier pathophysiology in experimental bacterial meningitis", PROGRAM AND ABSTRACTS OF THE INTERSCIENCE CONFERENCE ON ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, XX, XX, vol. 37, 1997, pages 39, XP002104913 *
SULLIVAN G W ET AL: "NEUTROPHIL A2A ADENOSINE RECEPTOR INHIBITS INFLAMMATION IN A RAT MODEL OF MENINGITIS: SYNERGY WITH THE TYPE IV PHOSPHODIESTERASE INHIBITOR, ROLIPRAM", JOURNAL OF INFECTIOUS DISEASES, CHICAGO, IL, US, vol. 180, no. 5, November 1999 (1999-11-01), pages 1550 - 1560, XP000978330, ISSN: 0022-1899 *
SULLIVAN G W ET AL: "ROLE OF A2A ADENOSINE RECEPTORS IN INFLAMMATION", DRUG DEVELOPMENT RESEARCH, NEW YORK, NY, US, vol. 45, no. 3/4, November 1998 (1998-11-01), pages 103 - 112, XP000978332, ISSN: 0272-4391 *
SULLIVAN GW ET AL: "The specific type IV phosphodiesterase inhibitor rolipram combined with adenosine reduces tumor necrosis factor-alpha-primed neutrophil oxidative activity", INTERNATIONAL JOURNAL OF IMMUNOPHARMACOLOGY, ELMSFORD,NY, US, vol. 17, no. 10, 1995, pages 793 - 803, XP002104914, ISSN: 0192-0561 *

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