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
Priority date (The priority date 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 date listed.)
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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    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis

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  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (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)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (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 (https=)
EP (1) EP2776033A1 (https=)
JP (2) JP2014532766A (https=)
KR (1) KR20140088610A (https=)
CN (1) CN104159585A (https=)
AU (2) AU2012335737A1 (https=)
BR (1) BR112014011009A2 (https=)
CA (1) CA2854336A1 (https=)
EA (1) EA201490944A1 (https=)
HK (1) HK1202062A1 (https=)
IL (1) IL232421A0 (https=)
IN (1) IN2014CN04067A (https=)
MX (1) MX2014005458A (https=)
TW (2) TW201818937A (https=)
WO (1) WO2013070890A1 (https=)

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
CA2812750C (en) 2010-09-27 2020-10-06 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration-resistant prostate cancer and osteoblastic bone metastases
JP2014505109A (ja) 2011-02-10 2014-02-27 エクセリクシス， インク． キノリン化合物およびそのような化合物を含有する医薬組成物の調製方法
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR20140025496A (ko) 2011-05-02 2014-03-04 엑셀리시스, 인코포레이티드 암 및 뼈 암 통증의 치료방법
GEP201606523B (en) 2011-09-22 2016-08-10 Exelixis Inc Method for treating osteoporosis
DK2768796T3 (da) 2011-10-20 2020-02-24 Exelixis Inc Fremgangsmåde til fremstilling af quinolin-derivater
JP2015515988A (ja) * 2012-05-02 2015-06-04 エクセリクシス， インク． 溶骨性骨転移を治療するためのｍｅｔ−ｖｅｇｆ二重調節剤
AU2014232714B2 (en) 2013-03-15 2018-07-19 Exelixis, Inc. Metabolites of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
EP2981263B1 (en) 2013-04-04 2022-06-29 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
US9149471B2 (en) * 2013-09-30 2015-10-06 National University Corporation Tokyo University Of Agriculture And Technology Therapeutic agent for osteoporosis
KR102354963B1 (ko) 2014-02-14 2022-01-21 엑셀리시스, 인코포레이티드 N-｛4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐｝-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법
EA201691850A1 (ru) 2014-03-17 2016-12-30 Экселиксис, Инк. Дозирование составов, содержащих кабозантиниб
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
ES2929888T3 (es) 2014-07-31 2022-12-02 Exelixis Inc Procedimiento para preparar cabozantinib marcado con flúor 18 y sus análogos
BR112017002318A2 (pt) 2014-08-05 2018-07-17 Exelixis, Inc. combinações de fármacos para tratar mieloma múltiplo.
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
US10723701B2 (en) * 2016-10-18 2020-07-28 Beijing Konruns Pharmaceutical Co., Ltd. Quinolyl-substituted carboxylic acid compound or pharmaceutically acceptable salt thereof, pharmaceutical composition of the same, and use of the same
AU2018272088C1 (en) 2017-05-26 2022-09-22 Exelixis, Inc. Crystalline solid forms of salts of N-{4-[(6,7-dimethoxyquinolin-4-yl) oxy]phenyl}-N'-(4-fluorphenyl) cyclopropane-1,1-dicarboxamide, processes for making, and methods of use
UA128476C2 (uk) 2018-01-26 2024-07-24 Екселіксіс, Інк. Сполуки для лікування кіназозалежних розладів
CN113292537B (zh) 2018-06-15 2024-04-05 汉达癌症医药责任有限公司 激酶抑制剂的盐类及其组合物
TW202444365A (zh) 2023-01-31 2024-11-16 漢達生技醫藥股份有限公司 改良之卡博替尼組合物及其使用方法

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
PT2213661E (pt) 2003-09-26 2011-12-15 Exelixis Inc Moduladores de c-met e métodos de uso
WO2008083319A1 (en) 2006-12-29 2008-07-10 Il Yang Pharmaceutical Company, Ltd. 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
EP2621483A1 (en) * 2010-09-27 2013-08-07 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration resistant prostate cancer and osteoblastic bone metastases

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

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Application publication date: 20141119