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CY1114007T1 - N - (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) N '- (4-fluorophenyl) cyclopropane-1,1-dicarboxylic acid, CANCER EDUCATION - Google Patents

N - (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) N '- (4-fluorophenyl) cyclopropane-1,1-dicarboxylic acid, CANCER EDUCATION

Info

Publication number
CY1114007T1
CY1114007T1 CY20131100420T CY131100420T CY1114007T1 CY 1114007 T1 CY1114007 T1 CY 1114007T1 CY 20131100420 T CY20131100420 T CY 20131100420T CY 131100420 T CY131100420 T CY 131100420T CY 1114007 T1 CY1114007 T1 CY 1114007T1
Authority
CY
Cyprus
Prior art keywords
methyloxy
quinolin
cyclopropane
fluorophenyl
oxy
Prior art date
Application number
CY20131100420T
Other languages
Greek (el)
Inventor
Adrian St Clair Brown
Peter Lamb
William P Gallagher
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
Priority claimed from EP10701175.1A external-priority patent/EP2387563B2/en
Application filed by Exelixis, Inc. filed Critical Exelixis, Inc.
Publication of CY1114007T1 publication Critical patent/CY1114007T1/en

Links

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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Εδώ αποκαλύπτονται μηλικά άλατα Ν-(4-{[6,7-δις(μεθυλοξυ)κινολιν-4-υλ]οξυ}φαινυλ)-Ν'-(4-φθοροφαινυλο)κυκλοπροπανο-1,1-δικαρβοξαμιδίου, συμπεριλαμβανομένου ενός (L)-μηλικού άλατος, ενός (D)-μηλικού άλατος, ενός (DL) μηλικού άλατος, και μιγμάτων αυτών˙ και κρυσταλλικές και μη κρυσταλλικές μορφές των μηλικών αλάτων. Επίσης αποκαλύπτονται φαρμακευτικές συνθέσεις περιέχουσες τουλάχιστον ένα μηλικό άλας Ν-(4-{[6,7-δις(μεθυλοξυ)κινολιν-4-υλ]οξυ}φαινυλ)-Ν'-(4-φθοροφαινυλο)-κυκλοπροπανο-1,1-δικαρβοξαμιδίου, και μέθοδοι θεραπείας του καρκίνου περιλαμβάνουσες τη χορήγηση τουλάχιστον ενός μηλικού άλατος Ν-(4-{[6,7-δις(μεθυλοξυ)κινολιν-4-υλ]οξυ}φαινυλ)-Ν'-(4-φθοροφαινυλο)κυκλοπροπανο-1,1 -δικαρβοξαμιδίου.N- (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) -N '- (4-fluorophenyl) cyclopropane-1,1-dicarboxamide maleate salts are disclosed herein, including (L ) -maltate, a (D) -maltate, a (DL) malate, and mixtures thereof; and crystalline and non-crystalline forms of malate. Also disclosed are pharmaceutical compositions containing at least one N- (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) -N '- (4-fluorophenyl) -cyclopropane-1,1-maleate. dicarboxamide, and methods of cancer treatment comprising administering at least one maleic salt of N- (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) -N '- (4-fluorophenyl) cyclopropane- 1,1-dicarboxamide.

CY20131100420T 2009-01-16 2013-05-29 N - (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) N '- (4-fluorophenyl) cyclopropane-1,1-dicarboxylic acid, CANCER EDUCATION CY1114007T1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14542109A 2009-01-16 2009-01-16
EP10701175.1A EP2387563B2 (en) 2009-01-16 2010-01-15 Malate salt of n- (4- { [ 6, 7-bis (methyloxy) quinolin-4-yl]oxy}phenyl-n' - (4 -fluorophenyl) cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer

Publications (1)

Publication Number Publication Date
CY1114007T1 true CY1114007T1 (en) 2016-07-27

Family

ID=58449012

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20131100420T CY1114007T1 (en) 2009-01-16 2013-05-29 N - (4 - {[6,7-bis (methyloxy) quinolin-4-yl] oxy} phenyl) N '- (4-fluorophenyl) cyclopropane-1,1-dicarboxylic acid, CANCER EDUCATION

Country Status (2)

Country Link
CY (1) CY1114007T1 (en)
SI (1) SI2387563T2 (en)

Also Published As

Publication number Publication date
SI2387563T1 (en) 2013-06-28
SI2387563T2 (en) 2022-08-31

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