ES2562462T3 - Formas cristalinas de 3-(2,6-dicloro-3,5-dimetoxifenil)-1-{6-[4-(4-etilpiperazin-1-il)-fenilamino]-pirimidin-4-il}-1-metilurea y sus sales - Google Patents

Formas cristalinas de 3-(2,6-dicloro-3,5-dimetoxifenil)-1-{6-[4-(4-etilpiperazin-1-il)-fenilamino]-pirimidin-4-il}-1-metilurea y sus sales Download PDF

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Publication number
ES2562462T3
ES2562462T3 ES10788479.3T ES10788479T ES2562462T3 ES 2562462 T3 ES2562462 T3 ES 2562462T3 ES 10788479 T ES10788479 T ES 10788479T ES 2562462 T3 ES2562462 T3 ES 2562462T3
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ES
Spain
Prior art keywords
approximately
free base
anhydrous crystalline
crystalline form
water
Prior art date
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Active
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ES10788479.3T
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English (en)
Spanish (es)
Inventor
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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Novartis AG
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Application filed by Novartis AG filed Critical Novartis AG
Application granted granted Critical
Publication of ES2562462T3 publication Critical patent/ES2562462T3/es
Active legal-status Critical Current
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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)
  • 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)
ES10788479.3T 2009-12-07 2010-12-06 Formas cristalinas de 3-(2,6-dicloro-3,5-dimetoxifenil)-1-{6-[4-(4-etilpiperazin-1-il)-fenilamino]-pirimidin-4-il}-1-metilurea y sus sales Active ES2562462T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US26715509P 2009-12-07 2009-12-07
US267155P 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.

Publications (1)

Publication Number Publication Date
ES2562462T3 true ES2562462T3 (es) 2016-03-04

Family

ID=43983750

Family Applications (1)

Application Number Title Priority Date Filing Date
ES10788479.3T Active ES2562462T3 (es) 2009-12-07 2010-12-06 Formas cristalinas de 3-(2,6-dicloro-3,5-dimetoxifenil)-1-{6-[4-(4-etilpiperazin-1-il)-fenilamino]-pirimidin-4-il}-1-metilurea y sus sales

Country Status (32)

Country Link
US (1) US9067896B2 (enExample)
EP (1) EP2509963B1 (enExample)
JP (2) JP5714024B2 (enExample)
KR (1) KR101787784B1 (enExample)
CN (5) CN111100078A (enExample)
AR (2) AR079257A1 (enExample)
AU (1) AU2010328391B2 (enExample)
BR (1) BR112012013784B1 (enExample)
CA (1) CA2781431C (enExample)
CL (1) CL2012001480A1 (enExample)
DK (1) DK2509963T3 (enExample)
EC (1) ECSP12012026A (enExample)
ES (1) ES2562462T3 (enExample)
GT (1) GT201200181A (enExample)
HR (1) HRP20160126T1 (enExample)
HU (1) HUE026983T2 (enExample)
IL (1) IL220012B (enExample)
JO (1) JO3061B1 (enExample)
MA (1) MA33849B1 (enExample)
MX (1) MX2012006562A (enExample)
MY (1) MY158333A (enExample)
NZ (3) NZ700778A (enExample)
PE (1) PE20121499A1 (enExample)
PH (2) PH12014502593A1 (enExample)
PL (1) PL2509963T3 (enExample)
RU (1) RU2572848C2 (enExample)
SG (1) SG10201408063SA (enExample)
SI (1) SI2509963T1 (enExample)
TN (1) TN2012000263A1 (enExample)
TW (1) TWI526440B (enExample)
WO (1) WO2011071821A1 (enExample)
ZA (1) ZA201203612B (enExample)

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US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
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WO2016027781A1 (ja) 2014-08-18 2016-02-25 エーザイ・アール・アンド・ディー・マネジメント株式会社 単環ピリジン誘導体の塩およびその結晶
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CN114984013A (zh) 2015-03-25 2022-09-02 国立癌症研究中心 胆管癌治疗剂
CN107660200B (zh) 2015-04-14 2022-01-11 卫材R&D管理有限公司 结晶fgfr4抑制剂化合物和其用途
CN104803925B (zh) * 2015-04-16 2018-01-12 温州医科大学 一类以fgfr为靶点的2,4,5‑三取代嘧啶类化合物及其制备方法和用途
WO2016189472A1 (en) 2015-05-28 2016-12-01 Novartis Ag Fgfr inhibitor for use in the treatment of the phosphaturic mesenchymal tumor
AU2016374441B2 (en) 2015-12-17 2021-10-21 Eisai R&D Management Co., Ltd. Therapeutic agent for breast cancer
JP7372740B2 (ja) 2016-05-10 2023-11-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 細胞生存性及び/又は細胞増殖を低減するための薬物の組み合わせ
TWI669300B (zh) * 2016-05-20 2019-08-21 浙江海正藥業股份有限公司 嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途
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AR079257A1 (es) * 2009-12-07 2012-01-04 Novartis Ag Formas cristalinas de 3-(2,6-dicloro-3-5-dimetoxi-fenil)-1-{6-[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas

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Publication number Publication date
IL220012A0 (en) 2012-07-31
CA2781431A1 (en) 2011-06-16
MY158333A (en) 2016-09-30
MA33849B1 (fr) 2012-12-03
ECSP12012026A (es) 2012-08-31
PE20121499A1 (es) 2012-11-15
JP2015107996A (ja) 2015-06-11
BR112012013784B1 (pt) 2021-11-03
CL2012001480A1 (es) 2014-09-05
NZ700778A (en) 2015-04-24
PH12012501146A1 (en) 2012-10-22
SG10201408063SA (en) 2015-01-29
EP2509963A1 (en) 2012-10-17
AU2010328391A1 (en) 2012-06-07
TW201144297A (en) 2011-12-16
US9067896B2 (en) 2015-06-30
TN2012000263A1 (en) 2013-12-12
CA2781431C (en) 2017-10-31
HK1171016A1 (zh) 2013-03-15
PL2509963T3 (pl) 2016-05-31
HUE026983T2 (en) 2016-08-29
CN111100078A (zh) 2020-05-05
US20120245182A1 (en) 2012-09-27
NZ600070A (en) 2014-06-27
PH12014502593A1 (en) 2015-09-21
CN111269186A (zh) 2020-06-12
JP5714024B2 (ja) 2015-05-07
CN102639510A (zh) 2012-08-15
HRP20160126T1 (hr) 2016-03-25
AR114946A2 (es) 2020-11-11
KR101787784B1 (ko) 2017-10-18
DK2509963T3 (en) 2016-02-29
MX2012006562A (es) 2012-07-04
BR112012013784A8 (pt) 2017-12-26
AU2010328391B2 (en) 2014-07-03
RU2572848C2 (ru) 2016-01-20
IL220012B (en) 2018-02-28
KR20130028045A (ko) 2013-03-18
RU2012128351A (ru) 2014-01-20
WO2011071821A1 (en) 2011-06-16
JP6019142B2 (ja) 2016-11-02
EP2509963B1 (en) 2015-11-25
ZA201203612B (en) 2013-01-30
GT201200181A (es) 2013-12-03
NZ624315A (en) 2014-11-28
TWI526440B (zh) 2016-03-21
JP2013512956A (ja) 2013-04-18
JO3061B1 (ar) 2017-03-15
CN105061332A (zh) 2015-11-18
AR079257A1 (es) 2012-01-04
BR112012013784A2 (pt) 2016-05-03
SI2509963T1 (sl) 2016-05-31
CN111100077A (zh) 2020-05-05

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