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
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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)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (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 (cg-RX-API-DMAC10.html)
EP (1) EP2355820A1 (cg-RX-API-DMAC10.html)
JP (1) JP2012508239A (cg-RX-API-DMAC10.html)
KR (1) KR20110075014A (cg-RX-API-DMAC10.html)
CN (1) CN102209539B (cg-RX-API-DMAC10.html)
AU (1) AU2009314335B2 (cg-RX-API-DMAC10.html)
BR (1) BRPI0921840A2 (cg-RX-API-DMAC10.html)
CA (1) CA2743242A1 (cg-RX-API-DMAC10.html)
EA (1) EA018824B1 (cg-RX-API-DMAC10.html)
MX (1) MX2011005003A (cg-RX-API-DMAC10.html)
WO (1) WO2010056574A1 (cg-RX-API-DMAC10.html)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140378500A1 (en) * 2012-02-01 2014-12-25 20/20 Gene Systems, Inc. Methods for predicting tumor reponse to targeted therapies
MX370448B (es) 2013-03-11 2019-12-13 Merck Patent Gmbh Derivados de 6- [4- (1h-imidazol-2-il) piperidin-1-il] pirimidin-4-amina como moduladores de la actividad de cinasa.
WO2015108881A1 (en) 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
TN2016000270A1 (en) 2014-01-14 2017-10-06 Millennium Pharm Inc Heteroaryls and uses thereof.
GB201918815D0 (en) * 2019-12-19 2020-02-05 Imperial College Innovations Ltd Treatment of cancer
CA3162074A1 (en) * 2020-01-10 2021-07-15 Joseph HORVATINOVICH Methods of treating tumors

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
WO2005117909A2 (en) * 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
AU2005322085B2 (en) * 2004-12-28 2012-07-19 Exelixis, Inc. [1H-pyrazolo[3, 4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70S6K, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases
CA2626456C (en) * 2005-10-18 2018-01-09 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),第21页. *

Also Published As

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

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