KR20110041536A - 5-알키닐-피리미딘 - Google Patents

5-알키닐-피리미딘 Download PDF

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Publication number
KR20110041536A
KR20110041536A KR1020117003951A KR20117003951A KR20110041536A KR 20110041536 A KR20110041536 A KR 20110041536A KR 1020117003951 A KR1020117003951 A KR 1020117003951A KR 20117003951 A KR20117003951 A KR 20117003951A KR 20110041536 A KR20110041536 A KR 20110041536A
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KR
South Korea
Prior art keywords
mmol
membered
amino
pyrimidin
methyl
Prior art date
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Withdrawn
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KR1020117003951A
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English (en)
Korean (ko)
Inventor
토비아스 분버그
랄프 브루크너
더크 케슬러
올리버 크레이머
다릴 맥코넬
지그프리드 슈나이더
데르 빈 라스 반
Original Assignee
베링거 인겔하임 인터내셔날 게엠베하
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Application filed by 베링거 인겔하임 인터내셔날 게엠베하 filed Critical 베링거 인겔하임 인터내셔날 게엠베하
Publication of KR20110041536A publication Critical patent/KR20110041536A/ko
Withdrawn legal-status Critical Current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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • 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
    • 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)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Rheumatology (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)
KR1020117003951A 2008-07-29 2009-07-28 5-알키닐-피리미딘 Withdrawn KR20110041536A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08161369 2008-07-29
EP08161369.7 2008-07-29

Publications (1)

Publication Number Publication Date
KR20110041536A true KR20110041536A (ko) 2011-04-21

Family

ID=40202900

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020117003951A Withdrawn KR20110041536A (ko) 2008-07-29 2009-07-28 5-알키닐-피리미딘

Country Status (25)

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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5651110B2 (ja) 2008-07-29 2015-01-07 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 新規化合物
CA2731909A1 (en) 2008-07-29 2010-02-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
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
US8466162B2 (en) * 2011-01-26 2013-06-18 Boehringer Ingelheim International Gmbh 5-alkynyl-pyridines
TW201245176A (en) * 2011-01-26 2012-11-16 Boehringer Ingelheim Int New 5-alkynyl-pyridines
EP2736514B1 (en) * 2011-07-28 2017-10-18 Nerviano Medical Sciences S.r.l. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
UA110995C2 (uk) * 2011-10-07 2016-03-10 Ф. Хоффманн-Ля Рош Аг Етинільні похідні як модулятори метаботропного глутаматного рецептора
PL3080100T3 (pl) 2013-12-11 2023-03-06 Celgene Quanticel Research, Inc. Inhibitory lizyno-specyficznej demetylazy-1
HUE057895T2 (hu) 2014-05-01 2022-06-28 Celgene Quanticel Res Inc Lizinspecifikus demetiláz-1 inhibitorai
ES2935114T3 (es) * 2014-09-05 2023-03-01 Celgene Quanticel Res Inc Inhibidores de la desmetilasa 1 específica de lisina
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
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

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
ATE293962T1 (de) 2000-02-25 2005-05-15 Hoffmann La Roche Adenosin-rezeptor modulatoren
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
CA2528938A1 (en) * 2003-06-13 2005-02-24 Zentaris Gmbh Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof
EP1737462B1 (en) 2003-12-24 2008-07-30 AstraZeneca AB Pyrimidines with tie2 (tek) activity
EP1761540B1 (en) * 2004-05-13 2016-09-28 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
US7776869B2 (en) 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
WO2006082371A1 (en) 2005-02-01 2006-08-10 Astrazeneca Ab Pyrimidine compounds having tie2 (tek) inhibitory activity
EP1863805A1 (en) 2005-02-01 2007-12-12 AstraZeneca AB Pyrimidine compounds having tie2 (tek) inhibitory activity
US20070135437A1 (en) 2005-03-04 2007-06-14 Alsgen, Inc. Modulation of neurodegenerative diseases
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
US20080194552A1 (en) 2005-03-31 2008-08-14 Astrazeneca Ab Aminopyrimidine Derivatives With Tie2 Inhibiting Activity
AU2006302179C1 (en) * 2005-10-07 2013-06-20 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
JP2010501537A (ja) 2006-08-24 2010-01-21 アストラゼネカ アクチボラグ 増殖性障害の治療に有用なモルホリノピリミジン誘導体
CN106045965A (zh) 2006-12-29 2016-10-26 爱尔兰詹森科学公司 抑制hiv的5,6‑取代的嘧啶类化合物
EP2022785A1 (en) 2007-06-20 2009-02-11 Bayer Schering Pharma Aktiengesellschaft Alkynylpyrimidines as Tie2 kinase inhibitors
CA2731909A1 (en) 2008-07-29 2010-02-04 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
UY33199A (es) 2010-01-26 2011-08-31 Boehringer Ingelheim Int 5-alquinil-pirimidinas.

Also Published As

Publication number Publication date
CA2731909A1 (en) 2010-02-04
US8916548B2 (en) 2014-12-23
BRPI0916679A2 (pt) 2015-11-17
DK2323992T3 (en) 2016-10-31
PE20110196A1 (es) 2011-04-03
ES2597903T3 (es) 2017-01-24
UY32009A (es) 2010-02-26
AU2009275957A1 (en) 2010-02-04
WO2010012740A1 (en) 2010-02-04
ECSP11010786A (es) 2011-02-28
PL2323992T3 (pl) 2017-01-31
MX2011000729A (es) 2011-03-15
MA32505B1 (fr) 2011-07-03
HUE029837T2 (en) 2017-04-28
US20110281838A1 (en) 2011-11-17
CL2011000195A1 (es) 2011-07-08
NZ590558A (en) 2012-12-21
EP2323992B1 (en) 2016-07-20
JP2011529468A (ja) 2011-12-08
CO6341617A2 (es) 2011-11-21
AR072845A1 (es) 2010-09-22
EP2323992A1 (en) 2011-05-25
TW201010984A (en) 2010-03-16
JP5599791B2 (ja) 2014-10-01
EA201100255A1 (ru) 2011-08-30
IL210343A0 (en) 2011-03-31
CN102112450A (zh) 2011-06-29

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PA0105 International application

Patent event date: 20110221

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid