CN102834100A - 新型pan-CDK抑制剂用于治疗肿瘤的用途 - Google Patents

新型pan-CDK抑制剂用于治疗肿瘤的用途 Download PDF

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Publication number
CN102834100A
CN102834100A CN2011800166124A CN201180016612A CN102834100A CN 102834100 A CN102834100 A CN 102834100A CN 2011800166124 A CN2011800166124 A CN 2011800166124A CN 201180016612 A CN201180016612 A CN 201180016612A CN 102834100 A CN102834100 A CN 102834100A
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CN
China
Prior art keywords
amino
methyl
trifluoromethyl
phenyl
base
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Pending
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CN2011800166124A
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English (en)
Chinese (zh)
Inventor
U·吕金
G·西迈斯特
A·M·温内尔
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Bayer Pharma AG
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Bayer Pharma AG
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Filing date
Publication date
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of CN102834100A publication Critical patent/CN102834100A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2011800166124A 2010-04-01 2011-03-28 新型pan-CDK抑制剂用于治疗肿瘤的用途 Pending CN102834100A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102010014426A DE102010014426A1 (de) 2010-04-01 2010-04-01 Verwendung neuer pan-CDK-Inhibitoren zur Behandlung von Tumoren
DE102010014426.6 2010-04-01
PCT/EP2011/054733 WO2011120922A1 (de) 2010-04-01 2011-03-28 Verwendung neuer pan-cdk-inhibitoren zur behandlung von tumoren

Publications (1)

Publication Number Publication Date
CN102834100A true CN102834100A (zh) 2012-12-19

Family

ID=43858236

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2011800166124A Pending CN102834100A (zh) 2010-04-01 2011-03-28 新型pan-CDK抑制剂用于治疗肿瘤的用途

Country Status (21)

Country Link
US (1) US20130210846A1 (enExample)
EP (1) EP2552450A1 (enExample)
JP (1) JP5816259B2 (enExample)
KR (1) KR20130014678A (enExample)
CN (1) CN102834100A (enExample)
AU (1) AU2011234654B2 (enExample)
BR (1) BR112012024422A2 (enExample)
CA (1) CA2794996A1 (enExample)
CL (1) CL2012002753A1 (enExample)
CR (1) CR20120502A (enExample)
DE (1) DE102010014426A1 (enExample)
DO (1) DOP2012000260A (enExample)
EC (1) ECSP12012198A (enExample)
MA (1) MA34098B1 (enExample)
MX (1) MX337722B (enExample)
NZ (1) NZ602710A (enExample)
PH (1) PH12012501945A1 (enExample)
SG (2) SG10201502566SA (enExample)
TN (1) TN2012000469A1 (enExample)
UA (1) UA108494C2 (enExample)
WO (1) WO2011120922A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105007945A (zh) * 2013-03-07 2015-10-28 拜耳医药股份有限公司 (rs)-s-环丙基-s-(4-{[4-{[(1r,2r)-2-羟基-1-甲基丙基]氧基}-5-(三氟甲基)嘧啶-2-基]氨基}苯基)亚砜亚胺用于治疗特定肿瘤的用途
CN105530937A (zh) * 2013-03-13 2016-04-27 昂克希尔迪克斯有限公司 使用7-苄基-10-(2-甲基苄基)-2,6,7,8,9,10-六氢咪唑并[1,2-a]吡啶并[4,3-d]嘧啶-5(3h)-酮的联合疗法
CN116528869A (zh) * 2020-11-27 2023-08-01 安锐生物医药科技(广州)有限公司 氨基杂芳基激酶抑制剂

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2013234451A1 (en) * 2012-03-21 2014-09-25 Bayer Intellectual Property Gmbh Use of (RS)-S-cyclopropyl-S-(4-{[4-{[1R, 2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl] amino}phenyl)sulfoximide for treating specific tumours
WO2014173815A1 (en) * 2013-04-23 2014-10-30 Bayer Pharma Aktiengesellschaft Use of (rs)-s-cyclopropyl-s-(4-{[4-{[(1r, 2r)-2-hydroxy-1-methylpropyl]oxy}-5- (trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulphoximide for the treatment of specific tumours
US20160151370A1 (en) * 2013-06-21 2016-06-02 Bayer Pharma Aktiengesellschaft Substituted Benzylpyrazoles
WO2015071231A1 (de) * 2013-11-14 2015-05-21 Bayer Pharma Aktiengesellschaft Kombinationen von (rs)-s-cyclopropyl-s-(4-{[4-{[(1r, 2r)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluormethyl)pyrimidin-2-yl]amino}phenyl)sulfoximid zur behandlung von tumoren
CN109283263B (zh) * 2017-07-21 2019-06-25 南京正大天晴制药有限公司 用于雷替曲塞合成质量控制的检测分析方法
CN109283279B (zh) * 2017-07-21 2019-11-01 南京正大天晴制药有限公司 通过高效液相色谱法分离测定雷替曲塞及其对映异构体的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1867553A (zh) * 2003-10-16 2006-11-22 舍林股份公司 作为cdk 和/或vegf 抑制剂的氨基亚砜取代的嘧啶化合物、其制备方法以及作为药物的用途
CN101679310A (zh) * 2007-06-20 2010-03-24 拜耳先灵医药股份有限公司 作为Tie2激酶抑制剂的炔基嘧啶

Family Cites Families (15)

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DE4029650A1 (de) 1990-09-19 1992-03-26 Hoechst Ag 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide
WO1999002162A1 (en) 1997-07-12 1999-01-21 Cancer Research Campaign Technology Limited Cyclin dependent kinase inhibiting purine derivatives
US6440965B1 (en) 1997-10-15 2002-08-27 Krenitsky Pharmaceuticals, Inc. Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system
AU5438499A (en) 1998-08-29 2000-03-21 Astrazeneca Ab Pyrimidine compounds
GB9824579D0 (en) * 1998-11-10 1999-01-06 Novartis Ag Organic compounds
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
GB9919778D0 (en) 1999-08-21 1999-10-27 Zeneca Ltd Chemical compounds
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
EP1392662B1 (de) 2001-05-29 2009-01-07 Bayer Schering Pharma Aktiengesellschaft Cdk inhibitorische pyrimidine, deren herstellung und verwendung als arzneimittel
EP1483260A1 (de) 2002-03-11 2004-12-08 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
DE102005062742A1 (de) * 2005-12-22 2007-06-28 Bayer Schering Pharma Ag Sulfoximin substituierte Pyrimidine, Verfahren zu deren Herstellung und ihre Verwendung als Arzneimittel
DE102006027156A1 (de) * 2006-06-08 2007-12-13 Bayer Schering Pharma Ag Sulfimide als Proteinkinaseinhibitoren
EP1878726A1 (en) * 2006-07-12 2008-01-16 Bayer Schering Pharma Aktiengesellschaft Substituted sulphoximines as Tie2 inhibitors and salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same and uses of the same
WO2009100176A2 (en) * 2008-02-07 2009-08-13 Abbott Laboratories Pharmaceutical dosage form for oral administration of tyrosine kinase inhibitor
EP2179991A1 (de) 2008-10-21 2010-04-28 Bayer Schering Pharma Aktiengesellschaft Sulfoximinsubstituierte Anilino-Pyrimidinderivate als CDK-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1867553A (zh) * 2003-10-16 2006-11-22 舍林股份公司 作为cdk 和/或vegf 抑制剂的氨基亚砜取代的嘧啶化合物、其制备方法以及作为药物的用途
CN101679310A (zh) * 2007-06-20 2010-03-24 拜耳先灵医药股份有限公司 作为Tie2激酶抑制剂的炔基嘧啶

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105007945A (zh) * 2013-03-07 2015-10-28 拜耳医药股份有限公司 (rs)-s-环丙基-s-(4-{[4-{[(1r,2r)-2-羟基-1-甲基丙基]氧基}-5-(三氟甲基)嘧啶-2-基]氨基}苯基)亚砜亚胺用于治疗特定肿瘤的用途
CN105530937A (zh) * 2013-03-13 2016-04-27 昂克希尔迪克斯有限公司 使用7-苄基-10-(2-甲基苄基)-2,6,7,8,9,10-六氢咪唑并[1,2-a]吡啶并[4,3-d]嘧啶-5(3h)-酮的联合疗法
CN116528869A (zh) * 2020-11-27 2023-08-01 安锐生物医药科技(广州)有限公司 氨基杂芳基激酶抑制剂

Also Published As

Publication number Publication date
CR20120502A (es) 2012-11-20
WO2011120922A1 (de) 2011-10-06
SG10201502566SA (en) 2015-05-28
PH12012501945A1 (en) 2017-08-09
UA108494C2 (uk) 2015-05-12
US20130210846A1 (en) 2013-08-15
EP2552450A1 (de) 2013-02-06
AU2011234654B2 (en) 2015-08-06
MX337722B (es) 2016-03-16
DE102010014426A1 (de) 2011-10-06
CA2794996A1 (en) 2011-10-06
DOP2012000260A (es) 2013-03-31
AU2011234654A1 (en) 2012-10-25
SG183925A1 (en) 2012-10-30
JP5816259B2 (ja) 2015-11-18
ECSP12012198A (es) 2012-10-30
BR112012024422A2 (pt) 2016-05-31
NZ602710A (en) 2014-05-30
KR20130014678A (ko) 2013-02-08
JP2013523680A (ja) 2013-06-17
TN2012000469A1 (en) 2014-01-30
MX2012011427A (es) 2013-03-05
CL2012002753A1 (es) 2013-01-18
MA34098B1 (fr) 2013-03-05

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