BR112012013784A8 - 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 uréia e seus sais - Google Patents

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 uréia e seus sais

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Publication number
BR112012013784A8
BR112012013784A8 BR112012013784A BR112012013784A BR112012013784A8 BR 112012013784 A8 BR112012013784 A8 BR 112012013784A8 BR 112012013784 A BR112012013784 A BR 112012013784A BR 112012013784 A BR112012013784 A BR 112012013784A BR 112012013784 A8 BR112012013784 A8 BR 112012013784A8
Authority
BR
Brazil
Prior art keywords
dimethoxyphenyl
phenylamino
pyrimidin
dichloro
salts
Prior art date
Application number
BR112012013784A
Other languages
English (en)
Other versions
BR112012013784A2 (pt
BR112012013784B1 (pt
Inventor
Stowasser Frank
Slade Joel
Berghausen Joerg
Mckenna Joseph
Koteswara Kapa Prasad
Wu Raeann
Du Zhengming
Original Assignee
Novartis Ag
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.)
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43983750&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012013784(A8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of BR112012013784A2 publication Critical patent/BR112012013784A2/pt
Publication of BR112012013784A8 publication Critical patent/BR112012013784A8/pt
Publication of BR112012013784B1 publication Critical patent/BR112012013784B1/pt

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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)
  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Hematology (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)
BR112012013784-0A 2009-12-07 2010-12-06 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 uréia, seus sais, seu uso e seu método de preparação, e composição BR112012013784B1 (pt)

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.

Publications (3)

Publication Number Publication Date
BR112012013784A2 BR112012013784A2 (pt) 2016-05-03
BR112012013784A8 true BR112012013784A8 (pt) 2017-12-26
BR112012013784B1 BR112012013784B1 (pt) 2021-11-03

Family

ID=43983750

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012013784-0A BR112012013784B1 (pt) 2009-12-07 2010-12-06 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 uréia, seus sais, seu uso e seu método de preparação, e composição

Country Status (33)

Country Link
US (1) US9067896B2 (pt)
EP (1) EP2509963B1 (pt)
JP (2) JP5714024B2 (pt)
KR (1) KR101787784B1 (pt)
CN (5) CN111100078A (pt)
AR (2) AR079257A1 (pt)
AU (1) AU2010328391B2 (pt)
BR (1) BR112012013784B1 (pt)
CA (1) CA2781431C (pt)
CL (1) CL2012001480A1 (pt)
DK (1) DK2509963T3 (pt)
EC (1) ECSP12012026A (pt)
ES (1) ES2562462T3 (pt)
GT (1) GT201200181A (pt)
HK (1) HK1171016A1 (pt)
HR (1) HRP20160126T1 (pt)
HU (1) HUE026983T2 (pt)
IL (1) IL220012B (pt)
JO (1) JO3061B1 (pt)
MA (1) MA33849B1 (pt)
MX (1) MX2012006562A (pt)
MY (1) MY158333A (pt)
NZ (3) NZ600070A (pt)
PE (1) PE20121499A1 (pt)
PH (1) PH12014502593A1 (pt)
PL (1) PL2509963T3 (pt)
RU (1) RU2572848C2 (pt)
SG (1) SG10201408063SA (pt)
SI (1) SI2509963T1 (pt)
TN (1) TN2012000263A1 (pt)
TW (1) TWI526440B (pt)
WO (1) WO2011071821A1 (pt)
ZA (1) ZA201203612B (pt)

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WO2012088266A2 (en) 2010-12-22 2012-06-28 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3
RU2643326C2 (ru) * 2012-03-30 2018-01-31 Новартис Аг Ингибитор рецептора фрф для применения в лечении гипофосфатемических заболеваний
WO2014007951A2 (en) 2012-06-13 2014-01-09 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
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EP2968337B1 (en) 2013-03-15 2021-07-21 Celgene CAR LLC Heteroaryl compounds and uses thereof
TWI647220B (zh) 2013-03-15 2019-01-11 美商西建卡爾有限責任公司 雜芳基化合物及其用途
KR102350704B1 (ko) 2013-03-15 2022-01-13 셀젠 카르 엘엘씨 헤테로아릴 화합물 및 이의 용도
WO2014155268A2 (en) 2013-03-25 2014-10-02 Novartis Ag Fgf-r tyrosine kinase activity inhibitors - use in diseases associated with lack of or reduced snf5 activity
DK2986610T5 (en) 2013-04-19 2018-12-10 Incyte Holdings Corp BICYCLIC HETEROCYCLES AS FGFR INHIBITORS
CA2917667A1 (en) * 2013-07-09 2015-01-15 Dana-Farber Cancer Institute, Inc. Kinase inhibitors for the treatment of disease
RS57444B1 (sr) * 2013-10-18 2018-09-28 Eisai R&D Man Co Ltd Pirimidin fgfr4 inhibitori
SI3079667T1 (sl) 2013-12-13 2019-10-30 Novartis Ag Farmacevtske dozirne oblike
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
US20170304313A1 (en) 2014-10-06 2017-10-26 Novartis Ag Therapeutic Combination For The Treatment Of Cancer
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
NZ773116A (en) 2015-02-20 2024-05-31 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
JP2018509448A (ja) * 2015-03-25 2018-04-05 ノバルティス アーゲー 組合せ医薬
EP3283465B1 (en) 2015-04-14 2021-01-06 Eisai R&D Management Co., Ltd. Crystalline fgfr4 inhibitor compound and uses thereof
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
WO2017196854A1 (en) 2016-05-10 2017-11-16 Eisai R&D Management Co., Ltd. Drug combinations for reducing cell viability and/or cell proliferation
EP3459952B1 (en) * 2016-05-20 2022-01-05 Zhejiang Hisun Pharmaceutical Co., Ltd. Pyrimidine derivative, method for preparing same and use thereof in medicine
CN109803684B (zh) * 2016-08-23 2022-08-23 卫材 R&D 管理有限公司 用于治疗肝细胞癌的组合疗法
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN107176954B (zh) 2017-06-02 2019-01-11 无锡双良生物科技有限公司 一种egfr抑制剂的药用盐及其晶型、制备方法和应用
US11440903B2 (en) 2017-11-01 2022-09-13 Guangdong Zhongsheng Pharmaceutical Co., Ltd Salt form and crystal form of compound as FGFR4 inhibitor and preparation method thereof
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BR112020022373A2 (pt) 2018-05-04 2021-02-02 Incyte Corporation sais de um inibidor de fgfr
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
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JP2023505258A (ja) 2019-12-04 2023-02-08 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式複素環
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WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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CN115785001B (zh) * 2022-11-23 2023-09-15 斯坦德药典标准物质研发(湖北)有限公司 一种英菲格拉替尼的制备方法
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GB0512324D0 (en) 2005-06-16 2005-07-27 Novartis Ag Organic compounds
CN101242843A (zh) * 2005-06-10 2008-08-13 詹森药业有限公司 作为激酶调节剂的氨基嘧啶类化合物
KR101486490B1 (ko) * 2005-11-08 2015-01-27 제이더블유중외제약 주식회사 α-헬릭스 유사체 및 암 줄기세포의 치료에 관한 방법
ME00011A (me) * 2005-12-21 2009-02-10 Novartis Ag Derivati pirimidinilaril uree kao fgf inhibitori
CN102016592A (zh) * 2008-04-29 2011-04-13 诺瓦提斯公司 监测成纤维细胞生长因子受体的激酶活性的调节的方法及所述方法的应用
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

Also Published As

Publication number Publication date
TWI526440B (zh) 2016-03-21
NZ600070A (en) 2014-06-27
JP2015107996A (ja) 2015-06-11
EP2509963B1 (en) 2015-11-25
ZA201203612B (en) 2013-01-30
AU2010328391A1 (en) 2012-06-07
MA33849B1 (fr) 2012-12-03
CN111100078A (zh) 2020-05-05
SG10201408063SA (en) 2015-01-29
EP2509963A1 (en) 2012-10-17
JP5714024B2 (ja) 2015-05-07
AR114946A2 (es) 2020-11-11
JP6019142B2 (ja) 2016-11-02
IL220012A0 (en) 2012-07-31
KR20130028045A (ko) 2013-03-18
ES2562462T3 (es) 2016-03-04
JO3061B1 (ar) 2017-03-15
IL220012B (en) 2018-02-28
JP2013512956A (ja) 2013-04-18
MY158333A (en) 2016-09-30
KR101787784B1 (ko) 2017-10-18
DK2509963T3 (en) 2016-02-29
AU2010328391B2 (en) 2014-07-03
CN105061332A (zh) 2015-11-18
PL2509963T3 (pl) 2016-05-31
RU2012128351A (ru) 2014-01-20
HRP20160126T1 (hr) 2016-03-25
GT201200181A (es) 2013-12-03
PH12014502593A1 (en) 2015-09-21
CN102639510A (zh) 2012-08-15
CA2781431A1 (en) 2011-06-16
RU2572848C2 (ru) 2016-01-20
NZ624315A (en) 2014-11-28
NZ700778A (en) 2015-04-24
HUE026983T2 (en) 2016-08-29
ECSP12012026A (es) 2012-08-31
US20120245182A1 (en) 2012-09-27
MX2012006562A (es) 2012-07-04
BR112012013784A2 (pt) 2016-05-03
CN111269186A (zh) 2020-06-12
BR112012013784B1 (pt) 2021-11-03
CN111100077A (zh) 2020-05-05
US9067896B2 (en) 2015-06-30
TW201144297A (en) 2011-12-16
AR079257A1 (es) 2012-01-04
CA2781431C (en) 2017-10-31
WO2011071821A1 (en) 2011-06-16
HK1171016A1 (zh) 2013-03-15
PE20121499A1 (es) 2012-11-15
SI2509963T1 (sl) 2016-05-31
CL2012001480A1 (es) 2014-09-05
TN2012000263A1 (en) 2013-12-12

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