CA2781431C - Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof - Google Patents

Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof Download PDF

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CA2781431C
CA2781431C CA2781431A CA2781431A CA2781431C CA 2781431 C CA2781431 C CA 2781431C CA 2781431 A CA2781431 A CA 2781431A CA 2781431 A CA2781431 A CA 2781431A CA 2781431 C CA2781431 C CA 2781431C
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crystalline
diffraction pattern
powder diffraction
ray powder
peaks
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CA2781431A1 (en
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Joerg Berghausen
Prasad Koteswara Kapa
Joseph Mckenna
Joel Slade
Raeann Wu
Zhengming Du
Frank Stowasser
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Novartis AG
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48Two nitrogen atoms
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2781431A 2009-12-07 2010-12-06 Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof Active CA2781431C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26715509P 2009-12-07 2009-12-07
US61/267,155 2009-12-07
PCT/US2010/059108 WO2011071821A1 (en) 2009-12-07 2010-12-06 Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof.

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CA2781431A1 CA2781431A1 (en) 2011-06-16
CA2781431C true CA2781431C (en) 2017-10-31

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CA2781431A Active CA2781431C (en) 2009-12-07 2010-12-06 Crystalline forms of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea and salts thereof

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US (1) US9067896B2 (https=)
EP (1) EP2509963B1 (https=)
JP (2) JP5714024B2 (https=)
KR (1) KR101787784B1 (https=)
CN (5) CN105061332A (https=)
AR (2) AR079257A1 (https=)
AU (1) AU2010328391B2 (https=)
BR (1) BR112012013784B1 (https=)
CA (1) CA2781431C (https=)
CL (1) CL2012001480A1 (https=)
DK (1) DK2509963T3 (https=)
EC (1) ECSP12012026A (https=)
ES (1) ES2562462T3 (https=)
GT (1) GT201200181A (https=)
HR (1) HRP20160126T1 (https=)
HU (1) HUE026983T2 (https=)
IL (1) IL220012B (https=)
JO (1) JO3061B1 (https=)
MA (1) MA33849B1 (https=)
MX (1) MX2012006562A (https=)
MY (1) MY158333A (https=)
NZ (3) NZ600070A (https=)
PE (1) PE20121499A1 (https=)
PH (2) PH12014502593A1 (https=)
PL (1) PL2509963T3 (https=)
RU (1) RU2572848C2 (https=)
SG (1) SG10201408063SA (https=)
SI (1) SI2509963T1 (https=)
TN (1) TN2012000263A1 (https=)
TW (1) TWI526440B (https=)
WO (1) WO2011071821A1 (https=)
ZA (1) ZA201203612B (https=)

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HUE026983T2 (en) 2016-08-29
NZ700778A (en) 2015-04-24
US20120245182A1 (en) 2012-09-27
TN2012000263A1 (en) 2013-12-12
JP2013512956A (ja) 2013-04-18
RU2012128351A (ru) 2014-01-20
DK2509963T3 (en) 2016-02-29
MA33849B1 (fr) 2012-12-03
IL220012B (en) 2018-02-28
JP6019142B2 (ja) 2016-11-02
BR112012013784A8 (pt) 2017-12-26
JO3061B1 (ar) 2017-03-15
ZA201203612B (en) 2013-01-30
KR20130028045A (ko) 2013-03-18
PE20121499A1 (es) 2012-11-15
KR101787784B1 (ko) 2017-10-18
BR112012013784B1 (pt) 2021-11-03
BR112012013784A2 (pt) 2016-05-03
US9067896B2 (en) 2015-06-30
PL2509963T3 (pl) 2016-05-31
CN102639510A (zh) 2012-08-15
CN111100077A (zh) 2020-05-05
AU2010328391A1 (en) 2012-06-07
CN111100078A (zh) 2020-05-05
PH12012501146A1 (en) 2012-10-22
SG10201408063SA (en) 2015-01-29
HRP20160126T1 (hr) 2016-03-25
CA2781431A1 (en) 2011-06-16
WO2011071821A1 (en) 2011-06-16
CL2012001480A1 (es) 2014-09-05
ECSP12012026A (es) 2012-08-31
CN111269186A (zh) 2020-06-12
JP5714024B2 (ja) 2015-05-07
GT201200181A (es) 2013-12-03
AU2010328391B2 (en) 2014-07-03
RU2572848C2 (ru) 2016-01-20
SI2509963T1 (sl) 2016-05-31
NZ624315A (en) 2014-11-28
MX2012006562A (es) 2012-07-04
EP2509963B1 (en) 2015-11-25
IL220012A0 (en) 2012-07-31
TWI526440B (zh) 2016-03-21
HK1171016A1 (zh) 2013-03-15
TW201144297A (en) 2011-12-16
MY158333A (en) 2016-09-30
AR114946A2 (es) 2020-11-11
JP2015107996A (ja) 2015-06-11
PH12014502593A1 (en) 2015-09-21
AR079257A1 (es) 2012-01-04
ES2562462T3 (es) 2016-03-04
CN105061332A (zh) 2015-11-18
EP2509963A1 (en) 2012-10-17

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