CN102209538B - P70 s6激酶抑制剂和egfr抑制剂的组合治疗剂 - Google Patents

P70 s6激酶抑制剂和egfr抑制剂的组合治疗剂 Download PDF

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Publication number
CN102209538B
CN102209538B CN2009801448775A CN200980144877A CN102209538B CN 102209538 B CN102209538 B CN 102209538B CN 2009801448775 A CN2009801448775 A CN 2009801448775A CN 200980144877 A CN200980144877 A CN 200980144877A CN 102209538 B CN102209538 B CN 102209538B
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CN
China
Prior art keywords
fluoro
trifluoromethyl
phenyl
pyrimidine
pyrazolo
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
CN2009801448775A
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English (en)
Chinese (zh)
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CN102209538A (zh
Inventor
S.吉加纳奇
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of CN102209538A publication Critical patent/CN102209538A/zh
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Publication of CN102209538B publication Critical patent/CN102209538B/zh
Expired - Fee Related legal-status Critical Current
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2009801448775A 2008-11-11 2009-11-04 P70 s6激酶抑制剂和egfr抑制剂的组合治疗剂 Expired - Fee Related CN102209538B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US11327608P 2008-11-11 2008-11-11
US61/113,276 2008-11-11
US61/113276 2008-11-11
PCT/US2009/063189 WO2010056575A1 (en) 2008-11-11 2009-11-04 P70 s6 kinase inhibitor and egfr inhibitor combination therapy

Publications (2)

Publication Number Publication Date
CN102209538A CN102209538A (zh) 2011-10-05
CN102209538B true CN102209538B (zh) 2013-06-12

Family

ID=41664868

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2009801448775A Expired - Fee Related CN102209538B (zh) 2008-11-11 2009-11-04 P70 s6激酶抑制剂和egfr抑制剂的组合治疗剂

Country Status (11)

Country Link
US (1) US8334293B2 (enExample)
EP (1) EP2355821A1 (enExample)
JP (1) JP2012508240A (enExample)
KR (1) KR20110075015A (enExample)
CN (1) CN102209538B (enExample)
AU (1) AU2009314336B2 (enExample)
BR (1) BRPI0921888A2 (enExample)
CA (1) CA2743295A1 (enExample)
EA (1) EA018624B1 (enExample)
MX (1) MX2011005002A (enExample)
WO (1) WO2010056575A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2777707A1 (en) 2013-03-11 2014-09-17 Wake Forest University Health Sciences Method of Treating Brain Tumors
KR20150124957A (ko) * 2013-03-11 2015-11-06 메르크 파텐트 게엠베하 키나아제 활성의 조절인자로서 (6-[4-1h-이미다졸-2-일)피페리딘-1-일]피리미딘-4-아민 유도체
US9457019B2 (en) * 2013-11-07 2016-10-04 Deciphera Pharmaceuticals, Llc Methods for inhibiting tie-2 kinase useful in the treatment of cancer
WO2015150826A1 (en) * 2014-04-04 2015-10-08 Astrazeneca Ab Combination of egfr inhibitor and mek inhibitor for use in the treatment of nras mutated cancer
EP3749290A4 (en) * 2018-01-29 2022-01-26 Jonathan Sackner-Bernstein METHODS OF DOPAMINE MODULATION IN HUMAN NEUROLOGICAL DISEASES
DE102018205152A1 (de) 2018-04-05 2019-10-10 Glatt Ingenieurtechnik Gmbh Verfahren und Reaktor zur Herstellung von Partikeln

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101679439A (zh) * 2007-05-11 2010-03-24 伊莱利利公司 P70 s6激酶抑制剂

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69522717T2 (de) 1995-03-30 2002-02-14 Pfizer Inc., New York Chinazolinderivate
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
JP5274842B2 (ja) * 2004-12-28 2013-08-28 エグゼリクシス， インコーポレイテッド 免疫疾患、炎症疾患および増殖疾患の処置のためのセリン−スレオニンキナーゼモジュレーター（ｐ７０Ｓ６Ｋ、Ａｋｔ−１およびＡｋｔ−２）としての［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジンまたは［１Ｈ−ピペラゾ［３，４−ｄ］ピリミジン−４−イル］−ピペラジン化合物
US8628931B2 (en) 2005-10-18 2014-01-14 George Mason Intellectual Properties, Inc. mTOR pathway theranostic
AR064416A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101679439A (zh) * 2007-05-11 2010-03-24 伊莱利利公司 P70 s6激酶抑制剂

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Doherty L.;et al.egfr和mtor抑制剂联合应用治疗复发性恶性胶质瘤的先导性研究.《世界核心医学期刊文摘(神经病学分册)》.2006,(第12期),21页. *

Also Published As

Publication number Publication date
US8334293B2 (en) 2012-12-18
CA2743295A1 (en) 2010-05-20
WO2010056575A1 (en) 2010-05-20
BRPI0921888A2 (pt) 2015-12-29
AU2009314336B2 (en) 2013-09-12
EA201170682A1 (ru) 2011-10-31
EA018624B1 (ru) 2013-09-30
EP2355821A1 (en) 2011-08-17
US20110207752A1 (en) 2011-08-25
CN102209538A (zh) 2011-10-05
AU2009314336A1 (en) 2010-05-20
MX2011005002A (es) 2011-05-25
KR20110075015A (ko) 2011-07-05
JP2012508240A (ja) 2012-04-05

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