IN2014CN02971A - - Google Patents

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Publication number
IN2014CN02971A
IN2014CN02971A IN2971CHN2014A IN2014CN02971A IN 2014CN02971 A IN2014CN02971 A IN 2014CN02971A IN 2971CHN2014 A IN2971CHN2014 A IN 2971CHN2014A IN 2014CN02971 A IN2014CN02971 A IN 2014CN02971A
Authority
IN
India
Prior art keywords
formula
compound
alkyl
halo
orn
Prior art date
Application number
Inventor
Jo Ann Wilson
Sriram Naganathan
Matthew Pfeiffer
Neil G Andersen
Original Assignee
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 IN2014CN02971A publication Critical patent/IN2014CN02971A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/233—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/02—Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/58—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/57—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C233/59—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3

Abstract

1231616416A process for preparing a compound of Formula I is disclosed comprising the steps: wherein: R is halo; R is halo; R is (C C)alkyl or (C C)alkyl optionally substituted with heterocycloalkyl; R is (C C)alkyl; and Q is CH orN; comprising: (a) contacting 1 1 cyclopropane dicarboxylic acid with thionyl chloride in a polar aprotic solvent; (b) adding and a tertiary amine base to the mixture of step (a) to form a compound of Formula A; and (c) coupling a compound of Formula A with an amine of Formula B to form a compound of Formula I.
IN2971CHN2014 2011-10-20 2012-10-22 IN2014CN02971A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161549312P 2011-10-20 2011-10-20
PCT/US2012/061320 WO2013059788A1 (en) 2011-10-20 2012-10-22 Process for preparing quinoline derivatives

Publications (1)

Publication Number Publication Date
IN2014CN02971A true IN2014CN02971A (en) 2015-07-03

Family

ID=47146705

Family Applications (1)

Application Number Title Priority Date Filing Date
IN2971CHN2014 IN2014CN02971A (en) 2011-10-20 2012-10-22

Country Status (24)

Country Link
US (3) US9365516B2 (en)
EP (1) EP2768796B1 (en)
JP (2) JP6208140B2 (en)
KR (1) KR102075371B1 (en)
CN (2) CN110511158A (en)
AR (1) AR088483A1 (en)
AU (2) AU2012325768B2 (en)
BR (1) BR112014009302B1 (en)
CA (1) CA2852771C (en)
DK (1) DK2768796T3 (en)
EA (1) EA031485B1 (en)
ES (1) ES2765013T3 (en)
GE (1) GEP20207110B (en)
HK (1) HK1201517A1 (en)
HU (1) HUE048023T2 (en)
IL (1) IL232139A (en)
IN (1) IN2014CN02971A (en)
MX (1) MX343288B (en)
PL (1) PL2768796T3 (en)
PT (1) PT2768796T (en)
TW (2) TWI619694B (en)
UA (1) UA116876C2 (en)
WO (1) WO2013059788A1 (en)
ZA (1) ZA201402579B (en)

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CN106420743A (en) 2010-07-16 2017-02-22 埃克塞里艾克西斯公司 C-MET modulator pharmaceutical compositions
WO2012044572A1 (en) 2010-09-27 2012-04-05 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration- resistant prostate cancer and osteoblastic bone metastases
BR112013020362A2 (en) 2011-02-10 2018-05-29 Exelixis Inc processes for the preparation of quinoline compounds, compounds and pharmaceutical combinations containing them
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR20140025496A (en) 2011-05-02 2014-03-04 엑셀리시스, 인코포레이티드 Method of treating cancer and bone cancer pain
BR112014006702A2 (en) 2011-09-22 2017-06-13 Exelixis Inc method to treat osteoporosis
CA2852771C (en) * 2011-10-20 2019-11-26 Exelixis, Inc. Process for preparing quinoline derivatives
JP2015515988A (en) 2012-05-02 2015-06-04 エクセリクシス， インク． MET-VEGF dual regulator for the treatment of osteolytic bone metastases
MX366003B (en) 2013-03-15 2019-06-24 Exelixis Inc Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl) -n'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide.
US11564915B2 (en) 2013-04-04 2023-01-31 Exelixis, Inc. Cabozantinib dosage form and use in the treatment of cancer
CN104649969B (en) * 2013-11-22 2019-02-12 广东东阳光药业有限公司 A kind of salt and preparation method thereof for Buddhist nun's class drug
MX2021001583A (en) 2014-02-14 2023-02-08 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.
US10159666B2 (en) 2014-03-17 2018-12-25 Exelixis, Inc. Dosing of cabozantinib formulations
CN104788372B (en) * 2014-07-25 2018-01-30 上海圣考医药科技有限公司 A kind of deuterated card is rich to replace Buddhist nun's derivative, its preparation method, application and its intermediate
CN106715397B (en) 2014-07-31 2021-07-23 埃克塞里艾克西斯公司 Method for preparing fluorine-18 labeled cabozantinib and analogs thereof
EP3177311A1 (en) 2014-08-05 2017-06-14 Exelixis, Inc. Drug combinations to treat multiple myeloma
EP3345894B1 (en) * 2015-09-02 2021-12-29 Chen, Kuenfeng Compound having protein tyrosine phosphatase shp-1 agonist activity
EP3442531A1 (en) 2016-04-15 2019-02-20 Exelixis, Inc. Method of treating renal cell carcinoma using n-(4-(6,7-dimethoxyquinolin-4-yloxy) phenyl)-n'-(4-fluoropheny)cyclopropane-1,1-dicarboxamide, (2s)-hydroxybutanedioate
CN109836382B (en) * 2017-11-29 2021-11-05 江苏豪森药业集团有限公司 Preparation method of cabozantinib malate and intermediate thereof
CR20230287A (en) 2018-01-26 2023-07-26 Exelixis Inc Compounds for the treatment of kinase-dependent disorders
CN112142619B (en) * 2020-10-20 2023-01-10 浙江工业大学 1, 1-cyclopropane dicarboxylic acid amide compound and preparation method and application thereof

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DK2392564T3 (en) 2003-09-26 2014-01-13 Exelixis Inc c-Met modulators and methods of application
WO2006014325A2 (en) * 2004-07-02 2006-02-09 Exelixis, Inc. C-met modulators and method of use
WO2006108059A1 (en) 2005-04-06 2006-10-12 Exelixis, Inc. C-met modulators and methods of use
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
UY31800A (en) 2008-05-05 2009-11-10 Smithkline Beckman Corp CANCER TREATMENT METHOD USING A CMET AND AXL INHIBITOR AND AN ERBB INHIBITOR
US8445509B2 (en) * 2008-05-08 2013-05-21 Takeda Pharmaceutical Company Limited Fused heterocyclic derivatives and use thereof
AR075084A1 (en) * 2008-09-26 2011-03-09 Smithkline Beecham Corp PREPARATION METHOD OF QUINOLINIL -OXIDIFENIL - CYCLOPROPANODICARBOXAMIDS AND CORRESPONDING INTERMEDIARIES
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WO2010065838A1 (en) 2008-12-04 2010-06-10 Exelixis, Inc. Methods of preparing quinoline derivatives
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UA108618C2 (en) 2009-08-07 2015-05-25 APPLICATION OF C-MET-MODULATORS IN COMBINATION WITH THEMOSOLOMID AND / OR RADIATION THERAPY FOR CANCER TREATMENT
MX2012010506A (en) 2010-03-12 2012-10-15 Exelixis Inc Hydrated crystalline forms of n-[3-fluoro-4-({6-(methyloxy)-7-[(3 -morpholin-4-ylpropyl)oxy]-quinolin-4-yl}oxy)phenyl]-n'-(4-fluor ophenyl)cyclopropane-1,1-dicarboxamide.
US20120070368A1 (en) 2010-04-16 2012-03-22 Exelixis, Inc. Methods of Using C-Met Modulators
CN106420743A (en) 2010-07-16 2017-02-22 埃克塞里艾克西斯公司 C-MET modulator pharmaceutical compositions
EP2593091A1 (en) 2010-07-16 2013-05-22 Exelixis, Inc. C-met modulator pharmaceutical compositions
AU2011307306A1 (en) 2010-09-27 2013-05-02 Exelixis, Inc. Dual inhibitors of MET and VEGF for the treatment of castration resistant prostate cancer and osteoblastic bone metastases
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
WO2012044572A1 (en) 2010-09-27 2012-04-05 Exelixis, Inc. Dual inhibitors of met and vegf for the treatment of castration- resistant prostate cancer and osteoblastic bone metastases
EP2643001A4 (en) 2010-11-22 2014-02-19 Glaxosmithkline Ip Dev Ltd Method of treating cancer
BR112013020362A2 (en) 2011-02-10 2018-05-29 Exelixis Inc processes for the preparation of quinoline compounds, compounds and pharmaceutical combinations containing them
US20120252840A1 (en) 2011-04-04 2012-10-04 Exelixis, Inc. Method of Treating Cancer
KR20140025496A (en) 2011-05-02 2014-03-04 엑셀리시스, 인코포레이티드 Method of treating cancer and bone cancer pain
TW201306842A (en) 2011-06-15 2013-02-16 Exelixis Inc Combination therapies for treating hematologic malignancies using pyridopyrimidinone inhibitors of PI3K/MTOR with bendamustine and/or rituximab
BR112014006702A2 (en) 2011-09-22 2017-06-13 Exelixis Inc method to treat osteoporosis
CA2852771C (en) * 2011-10-20 2019-11-26 Exelixis, Inc. Process for preparing quinoline derivatives
TW201818937A (en) 2011-11-08 2018-06-01 美商艾克塞里克斯公司 Method of treating cancer
JP2015515988A (en) 2012-05-02 2015-06-04 エクセリクシス， インク． MET-VEGF dual regulator for the treatment of osteolytic bone metastases
CN114129566A (en) 2012-09-07 2022-03-04 埃克塞里艾克西斯公司 Inhibitors of MET, VEGFR and RET for the treatment of lung adenocarcinoma

Also Published As

Publication number Publication date
IL232139A (en) 2017-11-30
US20180230100A1 (en) 2018-08-16
WO2013059788A1 (en) 2013-04-25
PL2768796T3 (en) 2020-05-18
KR102075371B1 (en) 2020-02-10
JP2014530880A (en) 2014-11-20
TW201321342A (en) 2013-06-01
AU2012325768B2 (en) 2017-08-10
US20140256938A1 (en) 2014-09-11
EA201490831A1 (en) 2014-09-30
MX343288B (en) 2016-11-01
PT2768796T (en) 2020-02-21
CN104395284A (en) 2015-03-04
AR088483A1 (en) 2014-06-11
DK2768796T3 (en) 2020-02-24
EP2768796B1 (en) 2019-11-20
MX2014004583A (en) 2014-10-06
US9365516B2 (en) 2016-06-14
GEAP201913471A (en) 2019-10-25
CN110511158A (en) 2019-11-29
JP6208140B2 (en) 2017-10-04
UA116876C2 (en) 2018-05-25
CA2852771A1 (en) 2013-04-25
NZ723880A (en) 2018-03-23
BR112014009302B1 (en) 2020-04-28
HUE048023T2 (en) 2020-05-28
US9969692B2 (en) 2018-05-15
CA2852771C (en) 2019-11-26
IL232139A0 (en) 2014-05-28
BR112014009302A2 (en) 2017-05-23
TWI642650B (en) 2018-12-01
EP2768796A1 (en) 2014-08-27
KR20140088874A (en) 2014-07-11
JP2017222648A (en) 2017-12-21
HK1201517A1 (en) 2015-09-04
AU2017254982A1 (en) 2017-11-23
ZA201402579B (en) 2015-03-25
AU2012325768A1 (en) 2014-05-22
GEP20207110B (en) 2020-05-25
TW201731812A (en) 2017-09-16
TWI619694B (en) 2018-04-01
ES2765013T3 (en) 2020-06-05
US20160229805A1 (en) 2016-08-11
NZ624328A (en) 2016-10-28
EA031485B1 (en) 2019-01-31

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