AU2005229331B2 - Diaminopyrimidines as P2X3 and P2X2/3 antagonists - Google Patents

Diaminopyrimidines as P2X3 and P2X2/3 antagonists Download PDF

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Publication number
AU2005229331B2
AU2005229331B2 AU2005229331A AU2005229331A AU2005229331B2 AU 2005229331 B2 AU2005229331 B2 AU 2005229331B2 AU 2005229331 A AU2005229331 A AU 2005229331A AU 2005229331 A AU2005229331 A AU 2005229331A AU 2005229331 B2 AU2005229331 B2 AU 2005229331B2
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Prior art keywords
isopropyl
methoxy
phenoxy
pyrimidine
diamine
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AU2005229331A
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AU2005229331A1 (en
Inventor
Chris Allen Broka
David Scott Carter
Michael Patrick Dillon
Ronald Charles Hawley
Alam Jahangir
Clara Jeou Jen Lin
Daniel Warren Parish
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Priority to AU2012200211A priority Critical patent/AU2012200211B2/en
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Expired legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • C07D239/49Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • AHUMAN NECESSITIES
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
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    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
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    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
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  • Communicable Diseases (AREA)
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  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Toxicology (AREA)
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  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
AU2005229331A 2004-03-05 2005-02-25 Diaminopyrimidines as P2X3 and P2X2/3 antagonists Expired AU2005229331B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2012200211A AU2012200211B2 (en) 2004-03-05 2012-01-13 Diaminopyrimidines as P2X3 and P2X2/3 antagonists

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US55049904P 2004-03-05 2004-03-05
US60/550,499 2004-03-05
PCT/EP2005/002020 WO2005095359A1 (en) 2004-03-05 2005-02-25 Diaminopyrimidines as p2x3 and p2x2/3 antagonists

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AU2005229331A1 AU2005229331A1 (en) 2005-10-13
AU2005229331B2 true AU2005229331B2 (en) 2011-10-13

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US (12) US7858632B2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
EP (2) EP2343282B1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
JP (4) JP4717876B2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
KR (1) KR100822530B1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
CN (1) CN1930135B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
AR (1) AR047992A1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
AU (1) AU2005229331B2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
BE (1) BE2024C508I2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
BR (2) BRPI0508461B8 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
CA (1) CA2557372C (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
CY (2) CY1113450T1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
DK (1) DK1725540T5 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
ES (2) ES2391636T3 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
FI (1) FIC20240007I1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
FR (1) FR24C1011I2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
HR (1) HRP20120901T1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
HU (1) HUS2400005I1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
IL (2) IL177438A (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
LU (1) LUC00333I2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
MY (1) MY145465A (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
NL (1) NL301261I2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
NO (4) NO339497B1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
NZ (1) NZ549069A (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
PL (1) PL1725540T3 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
PT (1) PT1725540E (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
RU (1) RU2422441C2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
SI (1) SI1725540T1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
TW (1) TWI313604B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
WO (1) WO2005095359A1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
ZA (1) ZA200606880B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)

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WO2005095359A1 (en) * 2004-03-05 2005-10-13 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 antagonists
US8592419B2 (en) * 2004-10-29 2013-11-26 Musc Foundation For Research Development Ceramides and apoptosis-signaling ligand
EP1924264B9 (en) 2005-09-01 2014-02-19 F.Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
ES2374750T3 (es) * 2005-09-01 2012-02-21 F. Hoffmann-La Roche Ag Proceso de síntesis de ariloxidiaminopirimidinas.
CN101300235B (zh) * 2005-09-01 2011-12-07 弗·哈夫曼-拉罗切有限公司 作为p2x3和p2x2/3调节剂的二氨基嘧啶类化合物
CN101253159B (zh) * 2005-09-01 2011-12-07 弗·哈夫曼-拉罗切有限公司 作为p2x3和p2x2/3调节剂的二氨基嘧啶类化合物
ES2612890T3 (es) * 2005-09-01 2017-05-19 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P2X2/3
EP1770089A1 (en) * 2005-10-03 2007-04-04 Institut Pasteur Pyranodibenzofuran derivatives with antifungal and antibacterial activity
ES2461595T3 (es) 2006-10-04 2014-05-20 F. Hoffmann-La Roche Ag Proceso para la síntesis de derivados de fenoxi-diaminopirimidina
CA2668399C (en) * 2006-11-09 2015-01-27 Li Chen Thiazole and oxazole-substituted arylamides
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
WO2008104472A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag 2, 4 -diaminopyrimidine derivatives and their use as p2x antagonists or as prodrugs thereof
US8101644B2 (en) 2007-03-30 2012-01-24 Shionogi & Co., Ltd. Pyrrolinone derivative and pharmaceutical composition comprising the same
EP2628727A3 (en) * 2007-11-21 2013-12-25 Decode Genetics EHF Biaryl PDE4 inhibitors for treating pulmonary and cardiovascular disorders
EP2336109A4 (en) * 2008-09-25 2012-05-02 Shionogi & Co NOVEL PYRROLINONE DERIVATIVE AND DRUG COMPOSITION CONTAINING THE SAME
CA2742866C (en) 2008-11-06 2017-10-24 Musc Foundation For Research Development Lysosomotropic inhibitors of acid ceramidase
JP5250116B2 (ja) 2008-11-24 2013-07-31 ビーエーエスエフ ソシエタス・ヨーロピア 熱潜在性塩基を含む硬化性組成物
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