WO2016101912A1 - Forme cristalline d'un sel d'un inhibiteur de kinase du récepteur du facteur de croissance épidermique et son procédé de préparation - Google Patents

Forme cristalline d'un sel d'un inhibiteur de kinase du récepteur du facteur de croissance épidermique et son procédé de préparation Download PDF

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Publication number
WO2016101912A1
WO2016101912A1 PCT/CN2015/098901 CN2015098901W WO2016101912A1 WO 2016101912 A1 WO2016101912 A1 WO 2016101912A1 CN 2015098901 W CN2015098901 W CN 2015098901W WO 2016101912 A1 WO2016101912 A1 WO 2016101912A1
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WO
WIPO (PCT)
Prior art keywords
formula
compound
salt
crystalline form
hydrobromide salt
Prior art date
Application number
PCT/CN2015/098901
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English (en)
Chinese (zh)
Inventor
陈敏华
张炎锋
刘凯
张晓宇
Original Assignee
苏州晶云药物科技有限公司
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
Priority claimed from CN201410821405.1A external-priority patent/CN104961688A/zh
Priority claimed from CN201510019173.2A external-priority patent/CN105837518A/zh
Application filed by 苏州晶云药物科技有限公司 filed Critical 苏州晶云药物科技有限公司
Publication of WO2016101912A1 publication Critical patent/WO2016101912A1/fr

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    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids

Abstract

L'invention concerne une forme cristalline d'un sel d'un inhibiteur de kinase du récepteur du facteur de croissance épidermique et un procédé de préparation de celle-ci, et, en particulier, les formes cristallines d'un bromhydrate et d'un phosphate d'un composé de formule (I).
PCT/CN2015/098901 2014-12-25 2015-12-25 Forme cristalline d'un sel d'un inhibiteur de kinase du récepteur du facteur de croissance épidermique et son procédé de préparation WO2016101912A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201410821405.1A CN104961688A (zh) 2014-12-25 2014-12-25 一种表皮生长因子受体激酶抑制剂的磷酸盐及其制备方法
CN201410821405.1 2014-12-25
CN201510019173.2A CN105837518A (zh) 2015-01-14 2015-01-14 一种表皮生长因子受体抑制剂的氢溴酸盐新晶型及其制备方法
CN201510019173.2 2015-01-14

Publications (1)

Publication Number Publication Date
WO2016101912A1 true WO2016101912A1 (fr) 2016-06-30

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ID=56149292

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2015/098901 WO2016101912A1 (fr) 2014-12-25 2015-12-25 Forme cristalline d'un sel d'un inhibiteur de kinase du récepteur du facteur de croissance épidermique et son procédé de préparation

Country Status (1)

Country Link
WO (1) WO2016101912A1 (fr)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013138502A1 (fr) * 2012-03-15 2013-09-19 Celgene Avilomics Research, Inc. Sels d'inhibiteur de kinases du récepteur de facteur de croissance épidermique
WO2013138495A1 (fr) * 2012-03-15 2013-09-19 Celgene Avilomics Research, Inc. Formes solides d'un inhibiteur de kinases du récepteur du facteur de croissance épidermique

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013138502A1 (fr) * 2012-03-15 2013-09-19 Celgene Avilomics Research, Inc. Sels d'inhibiteur de kinases du récepteur de facteur de croissance épidermique
WO2013138495A1 (fr) * 2012-03-15 2013-09-19 Celgene Avilomics Research, Inc. Formes solides d'un inhibiteur de kinases du récepteur du facteur de croissance épidermique

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