CN104159585A - 用于治疗癌症的met和vegf双重抑制剂 - Google Patents

用于治疗癌症的met和vegf双重抑制剂 Download PDF

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Publication number
CN104159585A
CN104159585A CN201280066410.5A CN201280066410A CN104159585A CN 104159585 A CN104159585 A CN 104159585A CN 201280066410 A CN201280066410 A CN 201280066410A CN 104159585 A CN104159585 A CN 104159585A
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CN
China
Prior art keywords
compound
formula
bone
acid
pharmaceutically acceptable
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.)
Pending
Application number
CN201280066410.5A
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English (en)
Chinese (zh)
Inventor
D.T.阿夫塔布
F.施莫尔勒
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Exelixis Inc
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Exelixis Inc
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Filing date
Publication date
Application filed by Exelixis Inc filed Critical Exelixis Inc
Publication of CN104159585A publication Critical patent/CN104159585A/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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • 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
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P35/04Antineoplastic agents specific for metastasis

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)
CN201280066410.5A 2011-11-08 2012-11-08 用于治疗癌症的met和vegf双重抑制剂 Pending CN104159585A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161557358P 2011-11-08 2011-11-08
US61/557358 2011-11-08
PCT/US2012/064116 WO2013070890A1 (en) 2011-11-08 2012-11-08 Dual inhibitor of met and vegf for treating cancer

Publications (1)

Publication Number Publication Date
CN104159585A true CN104159585A (zh) 2014-11-19

Family

ID=47179011

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280066410.5A Pending CN104159585A (zh) 2011-11-08 2012-11-08 用于治疗癌症的met和vegf双重抑制剂

Country Status (15)

Country Link
US (1) US20140323522A1 (enExample)
EP (1) EP2776033A1 (enExample)
JP (2) JP2014532766A (enExample)
KR (1) KR20140088610A (enExample)
CN (1) CN104159585A (enExample)
AU (2) AU2012335737A1 (enExample)
BR (1) BR112014011009A2 (enExample)
CA (1) CA2854336A1 (enExample)
EA (1) EA201490944A1 (enExample)
HK (1) HK1202062A1 (enExample)
IL (1) IL232421A0 (enExample)
IN (1) IN2014CN04067A (enExample)
MX (1) MX2014005458A (enExample)
TW (2) TWI662962B (enExample)
WO (1) WO2013070890A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109069499A (zh) * 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法

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UA108618C2 (uk) 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
PL2621481T5 (pl) 2010-09-27 2023-03-13 Exelixis, Inc. Podwójne inhibitory MET i VEGF do leczenia opornego na kastrację raka prostaty i osteoblastycznych przerzutów do kości
CA2826751C (en) 2011-02-10 2021-05-18 Exelixis, Inc. Processes for preparing quinoline compounds and pharmaceutical compositions containing such compounds
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
JP2014513129A (ja) 2011-05-02 2014-05-29 エクセリクシス, インク. 癌および骨癌疼痛の治療方法
EP2758057B1 (en) 2011-09-22 2017-05-31 Exelixis, Inc. Method for treating osteoporosis
CN104395284A (zh) 2011-10-20 2015-03-04 埃克塞里艾克西斯公司 制备喹啉衍生物的方法
HK1207587A1 (en) * 2012-05-02 2016-02-05 Exelixis, Inc. A dual met - vegf modulator for treating osteolytic bone metastases
GEP20196995B (en) 2013-03-15 2019-07-25 Inc Exelixis Metabolites of n-(4-{[6,7-bis (methyloxy)quinolin-4-yl] oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
ES2927651T3 (es) 2013-04-04 2022-11-10 Exelixis Inc Forma de dosificación de cabozantinib y uso en el tratamiento del cáncer
US9149471B2 (en) * 2013-09-30 2015-10-06 National University Corporation Tokyo University Of Agriculture And Technology Therapeutic agent for osteoporosis
EP3738952A1 (en) 2014-02-14 2020-11-18 Exelixis, Inc. Crystalline solid forms of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
WO2015142928A1 (en) 2014-03-17 2015-09-24 Exelixis, Inc. Dosing of cabozantinib formulations
CN104788372B (zh) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体
MA40386A (fr) 2014-07-31 2016-02-04 Exelixis Inc Procédé de préparation de cabozantinib marqué au fluor-18 et d'analogues de celui-ci
EA034992B1 (ru) 2014-08-05 2020-04-15 Экселиксис, Инк. Комбинации лекарственных средств для лечения множественной миеломы
CN105503717A (zh) * 2014-09-24 2016-04-20 江苏奥赛康药业股份有限公司 一种苹果酸卡博替尼化合物及其药物组合物
CN109496212B (zh) * 2016-10-18 2020-08-14 北京康辰药业股份有限公司 一种喹啉基取代的羧酸化合物或其药学上可接受的盐、其药物组合物及应用
CA3060370A1 (en) 2017-05-26 2018-11-29 Exelixis, Inc. Crystalline solid forms of salts of n-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
MY210421A (en) 2018-01-26 2025-09-22 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
AU2019285066B2 (en) 2018-06-15 2024-06-13 Handa Pharmaceuticals, Inc. Kinase inhibitor salts and compositions thereof
EP4658271A1 (en) 2023-01-31 2025-12-10 Handa Oncology, LLC Improved cabozantinib compositions and methods of use

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103402505A (zh) * 2010-09-27 2013-11-20 埃克塞里艾克西斯公司 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂

Family Cites Families (6)

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US4107288A (en) 1974-09-18 1978-08-15 Pharmaceutical Society Of Victoria Injectable compositions, nanoparticles useful therein, and process of manufacturing same
US5145684A (en) 1991-01-25 1992-09-08 Sterling Drug Inc. Surface modified drug nanoparticles
EP2392565B1 (en) 2003-09-26 2014-03-19 Exelixis, Inc. c-Met modulators and methods of use
US20080200515A1 (en) 2006-12-29 2008-08-21 Tap Pharmaceutical Products Inc. Solid state forms of enantiopure ilaprazole
UA108618C2 (uk) * 2009-08-07 2015-05-25 Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку
JP2013537918A (ja) * 2010-09-27 2013-10-07 エクセリクシス, インク. 去勢抵抗性前立腺癌および骨芽細胞骨転移の治療のためのmetおよびvegfの二元阻害薬

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103402505A (zh) * 2010-09-27 2013-11-20 埃克塞里艾克西斯公司 用于治疗去势抵抗性前列腺癌和成骨性骨转移的met和vegf的双重抑制剂

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109069499A (zh) * 2016-04-15 2018-12-21 埃克塞里艾克西斯公司 使用 n-(4-(6,7-二甲氧基喹啉-4-基氧基)苯基)-n’-(4-氟苯基)环丙烷-1,1-二甲酰胺,(2s)-羟基丁二酸盐治疗肾细胞癌的方法

Also Published As

Publication number Publication date
KR20140088610A (ko) 2014-07-10
IN2014CN04067A (enExample) 2015-10-23
JP2018048154A (ja) 2018-03-29
AU2017225103A1 (en) 2017-09-28
IL232421A0 (en) 2014-06-30
TWI662962B (zh) 2019-06-21
US20140323522A1 (en) 2014-10-30
TW201818937A (zh) 2018-06-01
BR112014011009A2 (pt) 2017-06-06
MX2014005458A (es) 2015-04-16
CA2854336A1 (en) 2013-05-16
AU2012335737A1 (en) 2014-06-05
TW201322981A (zh) 2013-06-16
JP2014532766A (ja) 2014-12-08
WO2013070890A1 (en) 2013-05-16
HK1202062A1 (en) 2015-09-18
EP2776033A1 (en) 2014-09-17
EA201490944A1 (ru) 2014-10-30

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Application publication date: 20141119