BR112017018580A2 - p-toluenossulfonato para inibidor de mek quinase, e forma cristalina do mesmo e método de preparação para tal - Google Patents

p-toluenossulfonato para inibidor de mek quinase, e forma cristalina do mesmo e método de preparação para tal

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Publication number
BR112017018580A2
BR112017018580A2 BR112017018580-6A BR112017018580A BR112017018580A2 BR 112017018580 A2 BR112017018580 A2 BR 112017018580A2 BR 112017018580 A BR112017018580 A BR 112017018580A BR 112017018580 A2 BR112017018580 A2 BR 112017018580A2
Authority
BR
Brazil
Prior art keywords
preparation
kinase inhibitor
crystalline form
mek kinase
toluene sulfonate
Prior art date
Application number
BR112017018580-6A
Other languages
English (en)
Chinese (zh)
Inventor
Wu Guaili
Gao Xiaohui
Bian Lin
JIA Junlei
Original Assignee
Jiangsu Hengrui Medicine Co., Ltd.
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
Application filed by Jiangsu Hengrui Medicine Co., Ltd. filed Critical Jiangsu Hengrui Medicine Co., Ltd.
Publication of BR112017018580A2 publication Critical patent/BR112017018580A2/pt

Links

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

a presente invenção refere-se a um p-toluenossulfonato para um inibidor de mek quinase, e uma forma cristalina deste e um método de preparação para tal, que são descritos. especificamente, um p-toluenossulfonato de 2-((2-flúor-4-iodofenil)amino)-1-metil-4-((6-metilpiridina-3-grupo)oxigrupo)-6-carbonila-1,6-di-hidropiridina-3-formamida (um composto representado pela fórmula (i)), e um cristal de forma i e um método de preparação para tal são descritos. o cristal de forma i obtido do composto representado pela fórmula (i) (i) tem boa estabilidade de forma cristalina e estabilidade química, e um solvente de cristalização usado tem toxicidade baixa e resíduo baixo e pode ser mais bem usado no tratamento clínico.
BR112017018580-6A 2015-03-27 2016-03-08 p-toluenossulfonato para inibidor de mek quinase, e forma cristalina do mesmo e método de preparação para tal BR112017018580A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510141303 2015-03-27
CN201510141303.X 2015-03-27
PCT/CN2016/075853 WO2016155473A1 (zh) 2015-03-27 2016-03-08 一种mek激酶抑制剂的对甲苯磺酸盐、其结晶形式及制备方法

Publications (1)

Publication Number Publication Date
BR112017018580A2 true BR112017018580A2 (pt) 2018-04-24

Family

ID=57005438

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017018580-6A BR112017018580A2 (pt) 2015-03-27 2016-03-08 p-toluenossulfonato para inibidor de mek quinase, e forma cristalina do mesmo e método de preparação para tal

Country Status (12)

Country Link
US (2) US10118911B2 (pt)
EP (1) EP3275866B1 (pt)
JP (1) JP2018509407A (pt)
KR (1) KR20170131506A (pt)
CN (1) CN106795116B (pt)
AU (1) AU2016239028B2 (pt)
BR (1) BR112017018580A2 (pt)
CA (1) CA2978796A1 (pt)
MX (1) MX2017011392A (pt)
RU (1) RU2704251C2 (pt)
TW (1) TWI705060B (pt)
WO (1) WO2016155473A1 (pt)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3545957A4 (en) 2016-11-25 2020-07-22 Jiangsu Hengrui Medicine Co., Ltd. PHARMACEUTICAL PYRIDONE DERIVATIVE COMPOSITION AND PRODUCTION METHOD THEREFOR
TW201821408A (zh) * 2016-12-01 2018-06-16 大陸商江蘇恆瑞醫藥股份有限公司 一種吡啶酮類衍生物的製備方法及其中間體
WO2020156162A1 (zh) * 2019-01-29 2020-08-06 贝达药业股份有限公司 Mek抑制剂及其在医药上的应用
TW202114994A (zh) * 2019-07-29 2021-04-16 大陸商江蘇恆瑞醫藥股份有限公司 一種１，６－二氫吡啶－３－甲醯胺衍生物的製備方法
TW202404581A (zh) * 2022-05-25 2024-02-01 美商醫肯納腫瘤學公司 Ｍｅｋ抑制劑及其用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1272290B (it) * 1994-06-20 1997-06-16 Avantgarde Spa Sale della l-carnitina e composizioni farmaceutiche che lo contengono per il trattamento di affezioni cutanee
US7732616B2 (en) * 2003-11-19 2010-06-08 Array Biopharma Inc. Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof
EP2279166A1 (en) 2008-04-22 2011-02-02 Bayer Schering Pharma Aktiengesellschaft Substituted phenoxybenzamides
TWI508965B (zh) * 2008-12-23 2015-11-21 Boehringer Ingelheim Int 有機化合物的鹽形式
CN102459188A (zh) 2009-06-15 2012-05-16 凯美隆(北京)药业技术有限公司 新型6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂
US20120238599A1 (en) * 2011-03-17 2012-09-20 Chemizon, A Division Of Optomagic Co., Ltd. Heterocyclic compounds as mek inhibitors
WO2014204263A1 (en) * 2013-06-20 2014-12-24 The Asan Foundation Substituted pyridinone compounds as mek inhibitors
MX2016004742A (es) * 2013-10-25 2016-12-09 Shanghai hengrui pharmaceutical co ltd Derivados de piridil cetona, metodo de preparacion de los mismos, y la aplicacion farmaceutica de los mismos.

Also Published As

Publication number Publication date
WO2016155473A1 (zh) 2016-10-06
RU2017134709A (ru) 2019-04-29
CN106795116A (zh) 2017-05-31
EP3275866A4 (en) 2018-08-15
EP3275866B1 (en) 2019-12-04
RU2704251C2 (ru) 2019-10-25
US20180118715A1 (en) 2018-05-03
CA2978796A1 (en) 2016-10-06
EP3275866A1 (en) 2018-01-31
KR20170131506A (ko) 2017-11-29
MX2017011392A (es) 2018-01-15
JP2018509407A (ja) 2018-04-05
US20180370948A1 (en) 2018-12-27
AU2016239028B2 (en) 2019-09-19
TW201634459A (zh) 2016-10-01
RU2017134709A3 (pt) 2019-07-17
CN106795116B (zh) 2019-11-01
TWI705060B (zh) 2020-09-21
AU2016239028A1 (en) 2017-09-14
US10118911B2 (en) 2018-11-06

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B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
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B350 Update of information on the portal [chapter 15.35 patent gazette]
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