RU2016114540A - Соль азотсодержащего гетероциклического соединения или ее кристаллическая форма, фармацевтическая композиция и ингибитор flt3 - Google Patents

Соль азотсодержащего гетероциклического соединения или ее кристаллическая форма, фармацевтическая композиция и ингибитор flt3 Download PDF

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RU2016114540A
RU2016114540A RU2016114540A RU2016114540A RU2016114540A RU 2016114540 A RU2016114540 A RU 2016114540A RU 2016114540 A RU2016114540 A RU 2016114540A RU 2016114540 A RU2016114540 A RU 2016114540A RU 2016114540 A RU2016114540 A RU 2016114540A
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salt
amino
crystalline form
enamide
oxopropan
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RU2016114540A
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RU2641106C2 (ru
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Синсуке МИДЗУМОТО
Такуя МАЦУМОТО
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Фуджифилм Корпорэйшн
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    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/18—Sulfonamides
    • 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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
    • C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two 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
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (12)

1. Соль карбоновой кислоты (карбоксилат), соль минеральной кислоты или соль сульфоновой кислоты (сульфонат) (S,E)-N-(1-((5-(2-((4-цианофенил)амино)-4-(пропиламино)пиримидин-5-ил)пент-4-ин-1-ил)амино)-1-оксопропан-2-ил)-4-(диметиламино)-N-метилбут-2-енамида.
2. Соль по п. 1, представляющая собой карбоксилат.
3. Соль по п. 1, представляющая собой соль минеральной кислоты.
4. Соль по п. 2, где карбоксилатом является формиат, ацетат, лактат, бензоат, цитрат, оксалат, фумарат, малеат, сукцинат, малат, тартрат, аспартат, трихлорацетат, трифторацетат или памоат.
5. Соль по п.2, где карбоксилатом является фумарат, сукцинат или памоат.
6. Соль по п. 3, где солью минеральной кислоты является гидрохлорид, гидробромид, гидройодид, нитрат, фосфат или сульфат.
7. Соль по п. 3, где солью минеральной кислоты является гидрохлорид или гидробромид.
8. Кристаллическая форма сукцината (S,E)-N-(1-((5-(2-((4-цианофенил)амино)-4-(пропиламино)пиримидин-5-ил)пент-4-ин-1-ил)амино)-1-оксопропан-2-ил)-4-(диметиламино)-N-метилбут-2-енамида, которая демонстрирует пики дифракции при углах дифракции (2θ) 10,5, 17,1, 19,1 и 22,4° на порошковой рентгеновской дифрактограмме.
9. Кристаллическая форма сукцината S,E)-N-(1-((5-(2-((4-цианофенил)амино)-4-(пропиламино)пиримидин-5-ил)пент-4-ин-1-ил)амино)-1-оксопропан-2-ил)-4-(диметиламино)-N-метилбут-2-енамида, которая демонстрирует пики дифракции при углах дифракции (2θ) 12,8, 16,1, 21,4 и 28,0° на порошковой рентгеновской дифрактограмме.
10. Кристаллическая форма фумарата S,E)-N-(1-((5-(2-((4-цианофенил)амино)-4-(пропиламино)пиримидин-5-ил)пент-4-ин-1-ил)амино)-1-оксопропан-2-ил)-4-(диметиламино)-N-метилбут-2-енамида, которая демонстрирует пики дифракции при углах дифракции (2θ) 8,6, 13,7, 17,8 и 23,0° на порошковой рентгеновской дифрактограмме.
11. Фармацевтическая композиция, содержащая соль по любому из п.п. 1-7 или кристаллическую форму по любому из п.п. 8-10.
12. Ингибитор FLT3, содержащий соль по любому из п.п.1-7 или ее кристаллическую форму по любому из п.п. 8-10.
RU2016114540A 2013-10-16 2014-10-15 Соль азотсодержащего гетероциклического соединения или ее кристаллическая форма, фармацевтическая композиция и ингибитор flt3 RU2641106C2 (ru)

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JP2013215755 2013-10-16
JP2013-215755 2013-10-16
PCT/JP2014/077368 WO2015056683A1 (ja) 2013-10-16 2014-10-15 含窒素複素環化合物の塩またはその結晶、医薬組成物およびｆｌｔ３阻害剤

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KR (1) KR101744033B1 (ru)
CN (1) CN105683167B (ru)
AU (1) AU2014335312B9 (ru)
BR (1) BR112016008080B1 (ru)
CA (1) CA2927079C (ru)
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HK (1) HK1219946A1 (ru)
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AU2014335312B9 (en) 2017-05-25
WO2015056683A1 (ja) 2015-04-23
EP3059227A4 (en) 2016-09-07
BR112016008080B1 (pt) 2021-02-23
CA2927079C (en) 2017-05-23
CN105683167A (zh) 2016-06-15
ES2738573T3 (es) 2020-01-23
HK1219946A1 (zh) 2017-04-21
CN105683167B (zh) 2018-10-23
CA2927079A1 (en) 2015-04-23
JPWO2015056683A1 (ja) 2017-03-09
EP3059227A1 (en) 2016-08-24
KR101744033B1 (ko) 2017-06-07
KR20160049009A (ko) 2016-05-04
US20160229812A1 (en) 2016-08-11
PL3059227T3 (pl) 2019-11-29
US9701644B2 (en) 2017-07-11
BR112016008080A8 (pt) 2020-03-17
EP3059227B1 (en) 2019-06-26
RU2641106C2 (ru) 2018-01-16
AU2014335312B2 (en) 2017-01-05
AU2014335312A1 (en) 2016-05-05
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