JP5599791B2 - 5−アルキニル−ピリミジン - Google Patents

5−アルキニル−ピリミジン Download PDF

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JP5599791B2
JP5599791B2 JP2011520491A JP2011520491A JP5599791B2 JP 5599791 B2 JP5599791 B2 JP 5599791B2 JP 2011520491 A JP2011520491 A JP 2011520491A JP 2011520491 A JP2011520491 A JP 2011520491A JP 5599791 B2 JP5599791 B2 JP 5599791B2
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mmol
amino
pyrimidin
methyl
pyridin
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Japanese (ja)
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JP2011529468A5 (OSRAM
JP2011529468A (ja
Inventor
トビアス ヴンベルク
ラルフ ブリュックナー
ディルク ケスラー
オリヴァー クレーマー
ダリル マコーネル
ジークフリート シュナイダー
デル フェーン ラルス ファン
Original Assignee
ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • 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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon 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
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • C07D409/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Laminated Bodies (AREA)
  • Application Of Or Painting With Fluid Materials (AREA)
JP2011520491A 2008-07-29 2009-07-28 5−アルキニル−ピリミジン Active JP5599791B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08161369.7 2008-07-29
EP08161369 2008-07-29
PCT/EP2009/059763 WO2010012740A1 (en) 2008-07-29 2009-07-28 5-alkynyl-pyrimidines

Publications (3)

Publication Number Publication Date
JP2011529468A JP2011529468A (ja) 2011-12-08
JP2011529468A5 JP2011529468A5 (OSRAM) 2012-08-30
JP5599791B2 true JP5599791B2 (ja) 2014-10-01

Family

ID=40202900

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2011520491A Active JP5599791B2 (ja) 2008-07-29 2009-07-28 5−アルキニル−ピリミジン

Country Status (25)

Country Link
US (1) US8916548B2 (OSRAM)
EP (1) EP2323992B1 (OSRAM)
JP (1) JP5599791B2 (OSRAM)
KR (1) KR20110041536A (OSRAM)
CN (1) CN102112450A (OSRAM)
AR (1) AR072845A1 (OSRAM)
AU (1) AU2009275957A1 (OSRAM)
BR (1) BRPI0916679A2 (OSRAM)
CA (1) CA2731909A1 (OSRAM)
CL (1) CL2011000195A1 (OSRAM)
CO (1) CO6341617A2 (OSRAM)
DK (1) DK2323992T3 (OSRAM)
EA (1) EA201100255A1 (OSRAM)
EC (1) ECSP11010786A (OSRAM)
ES (1) ES2597903T3 (OSRAM)
HU (1) HUE029837T2 (OSRAM)
IL (1) IL210343A0 (OSRAM)
MA (1) MA32505B1 (OSRAM)
MX (1) MX2011000729A (OSRAM)
NZ (1) NZ590558A (OSRAM)
PE (1) PE20110196A1 (OSRAM)
PL (1) PL2323992T3 (OSRAM)
TW (1) TW201010984A (OSRAM)
UY (1) UY32009A (OSRAM)
WO (1) WO2010012740A1 (OSRAM)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR072845A1 (es) 2008-07-29 2010-09-22 Boehringer Ingelheim Int 5-alquil-pirimidinas y su uso en el tratamiento de enfermedades mediadas por la actividad de quinasas.
US8853420B2 (en) 2008-07-29 2014-10-07 Boehringer Ingelheim International Gmbh Compounds
AR076332A1 (es) 2009-04-21 2011-06-01 Boehringer Ingelheim Int Derivados heterociclicos de 5-alquinil-piridinas, composiciones farmaceuticas que los comprenden y uso de los mismos para el tratamiento y/o prevencion del cancer, procesos inflamatorios, autoinmunes, y/o infecciones.
UY33199A (es) * 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.
US8618111B2 (en) * 2010-01-26 2013-12-31 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
TW201245176A (en) * 2011-01-26 2012-11-16 Boehringer Ingelheim Int New 5-alkynyl-pyridines
US8466162B2 (en) * 2011-01-26 2013-06-18 Boehringer Ingelheim International Gmbh 5-alkynyl-pyridines
JP6016915B2 (ja) * 2011-07-28 2016-10-26 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性なアルキニル置換ピリミジニルピロール
UA110995C2 (uk) * 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як модулятори метаботропного глутаматного рецептора
SI3080100T1 (sl) * 2013-12-11 2023-04-28 Celgene Quanticel Research, Inc. Inhibitorji lizin specifične demetilaze-1
WO2015168466A1 (en) 2014-05-01 2015-11-05 Quanticel Pharmaceuticals, Inc. Inhibitors of lysine specific demethylase-1
JP6692350B2 (ja) * 2014-09-05 2020-05-13 セルジーン クオンティセル リサーチ,インク. リジン特異的なデメチラーゼ−1の阻害剤
CN104803921A (zh) * 2015-03-14 2015-07-29 长沙深橙生物科技有限公司 一种苯取代嘧啶衍生物的制备方法
CN104744376A (zh) * 2015-03-14 2015-07-01 长沙深橙生物科技有限公司 一种2-异丙基嘧啶衍生物的制备方法

Family Cites Families (21)

* Cited by examiner, † Cited by third party
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DE3832570A1 (de) * 1988-09-24 1990-03-29 Hoechst Ag 7-substituierte derivate der 3,5-dihydroxyhept-6-insaeure, verfahren zur ihrer herstellung, ihre verwendung als arzneimittel, sowie zwischenprodukte
JPH08504798A (ja) 1992-12-18 1996-05-21 ザ ウエルカム ファウンデーション リミテッド 酵素阻害薬としての,ピリミジン,ピリジン,プテリジノンおよびインダゾール誘導体
US5622954A (en) 1994-05-11 1997-04-22 Fmc Corporation 5[W(substituted aryl)alkenylene and alkynylene]-2,4-diaminopyrimidines as pesticides
BR0108611A (pt) * 2000-02-25 2003-05-06 Hoffmann La Roche Moduladores de receptor de adenosina
JP5154728B2 (ja) * 2000-07-24 2013-02-27 クレニツキー・ファーマシューティカルズ,インコーポレイテッド 神経栄養活性を有する置換5−アルキニルピリミジン
WO2005016245A2 (en) * 2003-06-13 2005-02-24 Zentaris Gmbh Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof
JP2007517006A (ja) 2003-12-24 2007-06-28 アストラゼネカ アクチボラグ Tie2(tek)活性のあるピリミジン
ES2873875T3 (es) * 2004-05-13 2021-11-04 Icos Corp Quinazolinonas como inhibidores de fosfatidilinositol 3-quinasa delta humano
US7776869B2 (en) * 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
US20100048543A1 (en) 2005-02-01 2010-02-25 Astrazeneca Ab Pyrimidine compounds having ties (tek) inhibitory activity
US20080146599A1 (en) 2005-02-01 2008-06-19 Astrazeneca Ab Pyrimidine Compounds Having Tie-2 (Tek) Inhibitory Activity
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JP4993205B2 (ja) 2005-03-30 2012-08-08 塩野義製薬株式会社 チロシンキナーゼ阻害作用を有するピリミジン誘導体
WO2006103449A2 (en) 2005-03-31 2006-10-05 Astrazeneca Ab Saminopyrimidine derivates with tie2 inhibiting activity
CN101282948A (zh) * 2005-10-07 2008-10-08 埃克塞里艾克西斯公司 N-(3-氨基-喹喔啉-2-基)-磺酰胺衍生物及其作为磷脂酰肌醇3-激酶抑制剂的用途
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
US20090325957A1 (en) 2006-08-24 2009-12-31 Astrazeneca Ab Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders
EA020749B1 (ru) 2006-12-29 2015-01-30 Тиботек Фармасьютикалз Лтд. Вич-ингибирующие 5,6-замещенные пиримидины
EP2022785A1 (en) 2007-06-20 2009-02-11 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as Tie2 kinase inhibitors
AR072845A1 (es) 2008-07-29 2010-09-22 Boehringer Ingelheim Int 5-alquil-pirimidinas y su uso en el tratamiento de enfermedades mediadas por la actividad de quinasas.
UY33199A (es) 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.

Also Published As

Publication number Publication date
PL2323992T3 (pl) 2017-01-31
US20110281838A1 (en) 2011-11-17
CL2011000195A1 (es) 2011-07-08
TW201010984A (en) 2010-03-16
PE20110196A1 (es) 2011-04-03
WO2010012740A1 (en) 2010-02-04
IL210343A0 (en) 2011-03-31
ECSP11010786A (es) 2011-02-28
HUE029837T2 (en) 2017-04-28
EA201100255A1 (ru) 2011-08-30
JP2011529468A (ja) 2011-12-08
DK2323992T3 (en) 2016-10-31
CA2731909A1 (en) 2010-02-04
CN102112450A (zh) 2011-06-29
CO6341617A2 (es) 2011-11-21
EP2323992B1 (en) 2016-07-20
KR20110041536A (ko) 2011-04-21
US8916548B2 (en) 2014-12-23
AU2009275957A1 (en) 2010-02-04
ES2597903T3 (es) 2017-01-24
MA32505B1 (fr) 2011-07-03
BRPI0916679A2 (pt) 2015-11-17
UY32009A (es) 2010-02-26
MX2011000729A (es) 2011-03-15
EP2323992A1 (en) 2011-05-25
AR072845A1 (es) 2010-09-22
NZ590558A (en) 2012-12-21

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