ZA200606880B - Diaminopyrimidines as P2X3 and P2X2/3 antagonists - Google Patents

Diaminopyrimidines as P2X3 and P2X2/3 antagonists Download PDF

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Publication number
ZA200606880B
ZA200606880B ZA200606880A ZA200606880A ZA200606880B ZA 200606880 B ZA200606880 B ZA 200606880B ZA 200606880 A ZA200606880 A ZA 200606880A ZA 200606880 A ZA200606880 A ZA 200606880A ZA 200606880 B ZA200606880 B ZA 200606880B
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South Africa
Prior art keywords
alkyl
hydrogen
formula
alkoxy
halo
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ZA200606880A
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English (en)
Inventor
Carter David Scott
Hawley Ronald Charles
Parish Daniel Warren
Jahangir Alam
Dillon Michael Patrick
Lin Clara Jeou Jen
Broka Chris Allen
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Hoffmann La Roche
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Publication of ZA200606880B publication Critical patent/ZA200606880B/en

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    • 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
    • C07D239/49—Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

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  • Urology & Nephrology (AREA)
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  • Tropical Medicine & Parasitology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Virology (AREA)
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  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA200606880A 2004-03-05 2006-08-17 Diaminopyrimidines as P2X3 and P2X2/3 antagonists ZA200606880B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US55049904P 2004-03-05 2004-03-05

Publications (1)

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ZA200606880B true ZA200606880B (en) 2008-04-30

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ZA200606880A ZA200606880B (en) 2004-03-05 2006-08-17 Diaminopyrimidines as P2X3 and P2X2/3 antagonists

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US (11) US7858632B2 (hr)
EP (2) EP1725540B1 (hr)
JP (4) JP4717876B2 (hr)
KR (1) KR100822530B1 (hr)
CN (1) CN1930135B (hr)
AR (1) AR047992A1 (hr)
AU (1) AU2005229331B2 (hr)
BE (1) BE2024C508I2 (hr)
BR (2) BR122018003623B8 (hr)
CA (1) CA2557372C (hr)
CY (1) CY1113450T1 (hr)
DK (1) DK1725540T5 (hr)
ES (2) ES2391636T3 (hr)
FI (1) FIC20240007I1 (hr)
FR (1) FR24C1011I1 (hr)
HK (1) HK1101074A1 (hr)
HR (1) HRP20120901T1 (hr)
HU (1) HUS2400005I1 (hr)
IL (2) IL177438A (hr)
LU (1) LUC00333I2 (hr)
MY (1) MY145465A (hr)
NL (1) NL301261I2 (hr)
NO (4) NO339497B1 (hr)
NZ (1) NZ549069A (hr)
PL (1) PL1725540T3 (hr)
PT (1) PT1725540E (hr)
RU (1) RU2422441C2 (hr)
SI (1) SI1725540T1 (hr)
TW (1) TWI313604B (hr)
WO (1) WO2005095359A1 (hr)
ZA (1) ZA200606880B (hr)

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WO2006050265A2 (en) * 2004-10-29 2006-05-11 Musc Foundation For Research Development Ceramides and apoptosis-signaling ligand
CN101296907B (zh) * 2005-09-01 2013-03-27 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
JP4850914B2 (ja) * 2005-09-01 2012-01-11 エフ．ホフマン−ラ ロシュ アーゲー Ｐ２ｘ３およびｐ２ｘ２／３モジュレーターとしてのジアミノピリミジン
CA2620129C (en) * 2005-09-01 2014-12-23 F. Hoffmann-La Roche Ag Diaminopyrimidines as p2x3 and p2x2/3 modulators
ES2601178T3 (es) * 2005-09-01 2017-02-14 F. Hoffmann-La Roche Ag Diaminopirimidinas como moduladores de P2X3 y P3X2/3
EP1926716B1 (en) 2005-09-01 2011-10-19 F. Hoffmann-La Roche AG Process for synthesis of aryloxy diaminopyrimidines
EP1770089A1 (en) * 2005-10-03 2007-04-04 Institut Pasteur Pyranodibenzofuran derivatives with antifungal and antibacterial activity
JP5128603B2 (ja) * 2006-10-04 2013-01-23 エフ．ホフマン−ラ ロシュ アーゲー フェノキシジアミノピリミジン誘導体の合成方法
BRPI0718714B8 (pt) * 2006-11-09 2021-05-25 Hoffmann La Roche arilamidas substituídas por tiazol e oxazol, seu uso e composição farmacêutica que as compreende
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
WO2008104474A1 (en) * 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Diaminopyrimidines
KR20100016076A (ko) 2007-03-30 2010-02-12 시오노기 앤드 컴파니, 리미티드 신규 피롤리논 유도체 및 그것을 함유하는 의약 조성물
US20090136473A1 (en) * 2007-11-21 2009-05-28 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
WO2010054223A1 (en) 2008-11-06 2010-05-14 Musc Foundation For Research Development Lysosomotropic inhibitors of acid ceramidase
CN102224140B (zh) 2008-11-24 2014-04-16 巴斯夫欧洲公司 包含热潜性碱的可固化组合物
AU2009332952A1 (en) * 2008-12-30 2011-07-21 Musc Foundation For Research Development Sphingo-guanidines and their use as inhibitors of sphingosine kinase
CA2752269C (en) 2009-02-13 2016-08-30 Hiroyuki Kai Novel triazine derivative and pharmaceutical composition comprising the same
NZ713361A (en) 2009-08-17 2017-06-30 Memorial Sloan Kettering Cancer Center Heat shock protein binding compounds, compositions, and methods for making and using same
WO2012020749A1 (ja) 2010-08-10 2012-02-16 塩野義製薬株式会社 トリアジン誘導体およびそれを含有する鎮痛作用を有する医薬組成物
JP6075621B2 (ja) * 2010-08-10 2017-02-08 塩野義製薬株式会社 新規複素環誘導体およびそれらを含有する医薬組成物
WO2013118855A1 (ja) * 2012-02-09 2013-08-15 塩野義製薬株式会社 複素環および炭素環誘導体
TWI637949B (zh) 2013-06-14 2018-10-11 塩野義製藥股份有限公司 胺基三衍生物及含有其等之醫藥組合物
JP6546592B2 (ja) * 2013-08-23 2019-07-17 アファレント ファーマシューティカルズ インコーポレイテッド 急性、亜急性または慢性の咳を治療するためのジアミノピリミジンｐ２ｘ３およびｐ２ｘ２／３受容体モジュレーター
EP3143013B1 (en) 2014-05-13 2019-12-18 Memorial Sloan Kettering Cancer Center Hsp70 modulators and methods for making and using the same
WO2016004358A1 (en) 2014-07-03 2016-01-07 Afferent Pharmaceuticals, Inc. Methods and compositions for treating diseases and conditions
AU2015313221B2 (en) 2014-09-09 2019-11-21 Cytokinetics Incorporated Novel pharmaceutical composition for prevention and/or treatment of urinary incontinence
RU2585727C1 (ru) * 2014-12-12 2016-06-10 Наталья Борисовна Гусева Способ лечения детей с гиперактивным мочевым пузырем
ES2942711T3 (es) 2015-09-29 2023-06-06 Afferent Pharmaceuticals Inc Moduladores de los receptores P2X3 y P2X2/3 de diaminopirimidina para su uso en el tratamiento de la tos
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