PE20121499A1 - Formas cristalinas de 3-(2, 6-dicloro-3, 5-dimetoxi-fenil)-1-{6-4[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas - Google Patents

Formas cristalinas de 3-(2, 6-dicloro-3, 5-dimetoxi-fenil)-1-{6-4[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
PE20121499A1
PE20121499A1 PE2012000772A PE2012000772A PE20121499A1 PE 20121499 A1 PE20121499 A1 PE 20121499A1 PE 2012000772 A PE2012000772 A PE 2012000772A PE 2012000772 A PE2012000772 A PE 2012000772A PE 20121499 A1 PE20121499 A1 PE 20121499A1
Authority
PE
Peru
Prior art keywords
peaks
phenyl
approximately
theta
diffraction pattern
Prior art date
Application number
PE2012000772A
Other languages
English (en)
Inventor
Joerg Berghausen
Prasad Koteswara Kapa
Joseph Mckenna
Joel Slade
Raeann Wu
Zhengming Du
Frank Stowasser
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.)
Filing date
Publication date
Family has litigation
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=PE20121499(A1) "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 PE20121499A1 publication Critical patent/PE20121499A1/es

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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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA (I) DONDE: A) LA FORMA CRISTALINA ANHIDRA PRESENTA UN PATRON DE DIFRACCION EN POLVO DE RAYOS X QUE COMPRENDE UNO O MAS PICOS EN TERMINOS 2 THETA SELECCIONADOS A PARTIR DE PICOS A APROXIMADAMENTE 12º, 10.5º, 15.2º, 19.5º Y 21.0º; (B) LA FORMA DE MONOHIDRATO CRISTALINO PRESENTA UN PATRON DE DIFRACCION EN POLVO DE RAYOS X QUE COMPRENDE UNO O MAS PICOS EN TERMINOS 2 THETA SELECCIONADOS A PARTIR DE PICOS A APROXIMADAMENTE 20.3º, 21.3º, 18.8º, 4.7º, 9.4º Y 11.0º; (C) LA SAL CRISTALINA ANHIDRA DEL ACIDO MONOFOSFORICO PRESENTA UN PATRON DE DIFRACCION EN POLVO DE RAYOS X QUE COMPRENDE UNO O MAS PICOS EN TERMINOS 2 THETA SELECCIONADOS A PARTIR DE PICOS A APROXIMADAMENTE: 15º, 13.7º, 16.8º, 21.3º, 22.4º, 9.2º, 9.6º, 18.7º, 20.0º, 22.9º Y 27.2º; D) LA SAL DE CLORHIDRATO PRESENTA UN PATRON DE DIFRACCION EN POLVO DE RAYOS X QUE COMPRENDE UNO O MAS PICOS EN TERMINOS 2 THETA SELECCIONADOS A PARTIR DE PICOS A APROXIMADAMENTE 10.9º, 12.1º, 14.8º, 20.5º, 22º Y 25.1º. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO ES INHIBIDOR DE CINASA FGFR1, FGFR2, FGFR3, FGFR4, KDR, HER1, HER2, Bcr-Abl, Tie2 Y Ret. SIENDO UTIL PARA EL TRATAMIENTO DE CANCER
PE2012000772A 2009-12-07 2010-12-06 Formas cristalinas de 3-(2, 6-dicloro-3, 5-dimetoxi-fenil)-1-{6-4[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas PE20121499A1 (es)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
PE20121499A1 true PE20121499A1 (es) 2012-11-15

Family

ID=43983750

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012000772A PE20121499A1 (es) 2009-12-07 2010-12-06 Formas cristalinas de 3-(2, 6-dicloro-3, 5-dimetoxi-fenil)-1-{6-4[4-(4-etil-piperazin-1-il)-fenil-amino]-pirimidin-4-il}-1-metil-urea y sales de las mismas

Country Status (32)

Country Link
US (1) US9067896B2 (es)
EP (1) EP2509963B1 (es)
JP (2) JP5714024B2 (es)
KR (1) KR101787784B1 (es)
CN (5) CN111269186A (es)
AR (2) AR079257A1 (es)
AU (1) AU2010328391B2 (es)
CA (1) CA2781431C (es)
CL (1) CL2012001480A1 (es)
DK (1) DK2509963T3 (es)
EC (1) ECSP12012026A (es)
ES (1) ES2562462T3 (es)
GT (1) GT201200181A (es)
HK (1) HK1171016A1 (es)
HR (1) HRP20160126T1 (es)
HU (1) HUE026983T2 (es)
IL (1) IL220012B (es)
JO (1) JO3061B1 (es)
MA (1) MA33849B1 (es)
MX (1) MX2012006562A (es)
MY (1) MY158333A (es)
NZ (3) NZ700778A (es)
PE (1) PE20121499A1 (es)
PH (1) PH12014502593A1 (es)
PL (1) PL2509963T3 (es)
RU (1) RU2572848C2 (es)
SG (1) SG10201408063SA (es)
SI (1) SI2509963T1 (es)
TN (1) TN2012000263A1 (es)
TW (1) TWI526440B (es)
WO (1) WO2011071821A1 (es)
ZA (1) ZA201203612B (es)

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CN105899490B (zh) * 2013-10-18 2019-07-23 卫材R&D管理有限公司 嘧啶fgfr4抑制剂
CA2930055C (en) * 2013-12-13 2023-07-04 Novartis Ag Pharmaceutical dosage forms comprising protein kinase inhibitor
US9951047B2 (en) 2014-08-18 2018-04-24 Eisai R&D Management Co., Ltd. Salt of monocyclic pyridine derivative and crystal thereof
WO2016055916A1 (en) 2014-10-06 2016-04-14 Novartis Ag Therapeutic combination for the treatment of cancer
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 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
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
WO2016151501A1 (en) 2015-03-25 2016-09-29 Novartis Ag Pharmaceutical combinations
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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
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Also Published As

Publication number Publication date
CL2012001480A1 (es) 2014-09-05
NZ624315A (en) 2014-11-28
AR079257A1 (es) 2012-01-04
EP2509963A1 (en) 2012-10-17
CA2781431C (en) 2017-10-31
KR20130028045A (ko) 2013-03-18
HK1171016A1 (zh) 2013-03-15
HUE026983T2 (en) 2016-08-29
NZ700778A (en) 2015-04-24
CN111100077A (zh) 2020-05-05
RU2572848C2 (ru) 2016-01-20
KR101787784B1 (ko) 2017-10-18
MY158333A (en) 2016-09-30
JP2013512956A (ja) 2013-04-18
SG10201408063SA (en) 2015-01-29
IL220012A0 (en) 2012-07-31
JO3061B1 (ar) 2017-03-15
BR112012013784A8 (pt) 2017-12-26
ZA201203612B (en) 2013-01-30
DK2509963T3 (en) 2016-02-29
CN102639510A (zh) 2012-08-15
US9067896B2 (en) 2015-06-30
AU2010328391A1 (en) 2012-06-07
JP6019142B2 (ja) 2016-11-02
PL2509963T3 (pl) 2016-05-31
SI2509963T1 (sl) 2016-05-31
CN105061332A (zh) 2015-11-18
ECSP12012026A (es) 2012-08-31
AU2010328391B2 (en) 2014-07-03
NZ600070A (en) 2014-06-27
EP2509963B1 (en) 2015-11-25
PH12014502593A1 (en) 2015-09-21
MX2012006562A (es) 2012-07-04
TN2012000263A1 (en) 2013-12-12
JP5714024B2 (ja) 2015-05-07
TWI526440B (zh) 2016-03-21
RU2012128351A (ru) 2014-01-20
CN111100078A (zh) 2020-05-05
AR114946A2 (es) 2020-11-11
HRP20160126T1 (hr) 2016-03-25
MA33849B1 (fr) 2012-12-03
WO2011071821A1 (en) 2011-06-16
CA2781431A1 (en) 2011-06-16
TW201144297A (en) 2011-12-16
IL220012B (en) 2018-02-28
CN111269186A (zh) 2020-06-12
BR112012013784A2 (pt) 2016-05-03
ES2562462T3 (es) 2016-03-04
JP2015107996A (ja) 2015-06-11
US20120245182A1 (en) 2012-09-27
GT201200181A (es) 2013-12-03

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