CN102209539B - P70 s6激酶抑制剂和mtor抑制剂的组合治疗剂 - Google Patents

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

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Publication number
CN102209539B
CN102209539B CN2009801449528A CN200980144952A CN102209539B CN 102209539 B CN102209539 B CN 102209539B CN 2009801449528 A CN2009801449528 A CN 2009801449528A CN 200980144952 A CN200980144952 A CN 200980144952A CN 102209539 B CN102209539 B CN 102209539B
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Prior art keywords
trifluoromethyl
phenyl
fluoro
pyrimidine
pyrazolo
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Expired - Fee Related
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CN2009801449528A
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English (en)
Chinese (zh)
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CN102209539A (zh
Inventor
S.吉加纳奇
G.P.多诺霍
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Eli Lilly and Co
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Eli Lilly and Co
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    • 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
    • A61K31/435—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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2009801449528A 2008-11-11 2009-11-04 P70 s6激酶抑制剂和mtor抑制剂的组合治疗剂 Expired - Fee Related CN102209539B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US11327908P 2008-11-11 2008-11-11
US61/113279 2008-11-11
PCT/US2009/063188 WO2010056574A1 (en) 2008-11-11 2009-11-04 P70 s6 kinase inhibitor and mtor inhibitor combination therapy

Publications (2)

Publication Number Publication Date
CN102209539A CN102209539A (zh) 2011-10-05
CN102209539B true CN102209539B (zh) 2013-06-12

Family

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CN2009801449528A Expired - Fee Related CN102209539B (zh) 2008-11-11 2009-11-04 P70 s6激酶抑制剂和mtor抑制剂的组合治疗剂

Country Status (11)

Country Link
US (1) US20110212977A1 (enExample)
EP (1) EP2355820A1 (enExample)
JP (1) JP2012508239A (enExample)
KR (1) KR20110075014A (enExample)
CN (1) CN102209539B (enExample)
AU (1) AU2009314335B2 (enExample)
BR (1) BRPI0921840A2 (enExample)
CA (1) CA2743242A1 (enExample)
EA (1) EA018824B1 (enExample)
MX (1) MX2011005003A (enExample)
WO (1) WO2010056574A1 (enExample)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013116735A1 (en) * 2012-02-01 2013-08-08 20/20 Gene Systems, Inc. Methods for predicting tumor response to targeted therapies
US9458134B2 (en) 2013-03-11 2016-10-04 Merck Patent Gmbh Heterocycles as modulators of kinase activity
US10202373B2 (en) 2014-01-14 2019-02-12 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2015108861A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
GB201918815D0 (en) * 2019-12-19 2020-02-05 Imperial College Innovations Ltd Treatment of cancer
KR20220125310A (ko) * 2020-01-10 2022-09-14 코이뮨, 인크. 종양 치료 방법

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 (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA83484C2 (uk) * 2003-03-05 2008-07-25 Уайт Спосіб лікування раку грудей комбінацією похідного рапаміцину і інгібітора ароматази - летрозолу, фармацевтична композиція
US8076338B2 (en) * 2004-04-23 2011-12-13 Exelixis, Inc. Kinase modulators and methods of use
ATE543821T1 (de) * 2004-12-28 2012-02-15 Exelixis Inc Ä1h-pyrazoloä3,4-düpyrimidin-4-ylü-piperidin- oder piperazinverbindungen als serin-threonin- kinasemodulatoren (p70s6k, atk1 und atk2) zur behandlung von immunologischen, entzündlichen und proliferativen erkrankungen
JP2009511935A (ja) * 2005-10-18 2009-03-19 ジョージ メイソン インテレクチュアル プロパティーズ インク． ｍＴＯＲ経路テラノスティック
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),第21页. *

Also Published As

Publication number Publication date
EP2355820A1 (en) 2011-08-17
US20110212977A1 (en) 2011-09-01
WO2010056574A1 (en) 2010-05-20
AU2009314335B2 (en) 2013-09-12
CA2743242A1 (en) 2010-05-20
EA201170681A1 (ru) 2011-10-31
BRPI0921840A2 (pt) 2018-10-09
EA018824B1 (ru) 2013-10-30
CN102209539A (zh) 2011-10-05
MX2011005003A (es) 2011-05-25
AU2009314335A1 (en) 2010-05-20
KR20110075014A (ko) 2011-07-05
JP2012508239A (ja) 2012-04-05

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