EA201792254A1 - Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения - Google Patents

Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения

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Publication number
EA201792254A1
EA201792254A1 EA201792254A EA201792254A EA201792254A1 EA 201792254 A1 EA201792254 A1 EA 201792254A1 EA 201792254 A EA201792254 A EA 201792254A EA 201792254 A EA201792254 A EA 201792254A EA 201792254 A1 EA201792254 A1 EA 201792254A1
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EA
Eurasian Patent Office
Prior art keywords
salts
maleatic
kinazes
methods
receiving
Prior art date
Application number
EA201792254A
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English (en)
Other versions
EA035680B1 (ru
Inventor
Голян Чжан
Чаню Чжоу
Original Assignee
Бейджин, Лтд.
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Application filed by Бейджин, Лтд. filed Critical Бейджин, Лтд.
Publication of EA201792254A1 publication Critical patent/EA201792254A1/ru
Publication of EA035680B1 publication Critical patent/EA035680B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/558—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
    • A61K31/5585—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes having five-membered rings containing oxygen as the only ring hetero atom, e.g. prostacyclin
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42—Separation; Purification; Stabilisation; Use of additives
    • C07C51/43—Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
    • 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
    • C07C57/145—Maleic acid
    • 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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)

Abstract

Изобретение относится к малеатным солям 5-(((1R,1aS,6bR)-1-(6-(трифторметил)-1H-бензо[d]имидазол-2-ил)-1a,6b-дигидро-1H-циклопропа[b]бензофуран-5-ил)окси)-3,4-дигидро-1,8-нафтиридин-2(1H)-она (соединение 1), в частности сескви-малеатной соли и ее кристаллическим формам, способам получения, фармацевтическим композициям и терапевтическим применениям для лечения заболеваний или расстройств, опосредованных BRAF или другими киназами.
EA201792254A 2015-04-15 2016-04-14 Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения EA035680B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2015076639 2015-04-15
PCT/CN2016/079251 WO2016165626A1 (en) 2015-04-15 2016-04-14 Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

Publications (2)

Publication Number Publication Date
EA201792254A1 true EA201792254A1 (ru) 2018-02-28
EA035680B1 EA035680B1 (ru) 2020-07-24

Family

ID=57125563

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201792254A EA035680B1 (ru) 2015-04-15 2016-04-14 Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения

Country Status (15)

Country Link
US (1) US10351559B2 (ru)
EP (2) EP4119559A1 (ru)
JP (3) JP7320741B2 (ru)
KR (2) KR20240049684A (ru)
CN (2) CN107531682B (ru)
AU (1) AU2016248376B2 (ru)
CA (1) CA2981746C (ru)
EA (1) EA035680B1 (ru)
IL (2) IL255555B (ru)
MX (1) MX2017013219A (ru)
NZ (1) NZ735715A (ru)
SG (1) SG11201707984TA (ru)
TW (3) TWI792406B (ru)
WO (1) WO2016165626A1 (ru)
ZA (1) ZA201706392B (ru)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2006249866B2 (en) 2005-05-26 2011-10-13 Aldeyra Therapeutics, Inc. Compositions and methods of treating retinal disease
WO2013097224A1 (en) 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors
CN107531682B (zh) * 2015-04-15 2021-05-04 百济神州有限公司 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途
EP3481393B1 (en) 2016-07-05 2021-04-14 Beigene, Ltd. Combination of a pd-1 antagonist and a raf inhibitor for treating cancer
CN111356451A (zh) 2017-10-10 2020-06-30 奥尔德拉医疗公司 炎性病症的治疗
WO2020033344A1 (en) * 2018-08-06 2020-02-13 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
AR116921A1 (es) * 2018-10-31 2021-06-30 Servier Lab Sal de un inhibidor de bcl-2, forma cristalina relacionada, método para preparar la misma y composiciones farmacéuticas que contienen la misma
CN111484488A (zh) * 2019-01-25 2020-08-04 百济神州(北京)生物科技有限公司 一种b-raf激酶二聚体抑制剂的稳定结晶形式a
CN116715662A (zh) * 2019-01-25 2023-09-08 百济神州(北京)生物科技有限公司 无定形的b-raf激酶二聚体抑制剂
CN111184693B (zh) * 2019-05-29 2023-07-21 百济神州(苏州)生物科技有限公司 一种raf激酶抑制剂制剂及其制备方法
WO2023240178A1 (en) * 2022-06-08 2023-12-14 Mapkure, Llc Methods of treating cancer with a b-raf inhibitor

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5111113B2 (ja) 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ， インコーポレイテッド Ｒａｆキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
CA2632512A1 (en) 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
EP2021327B1 (en) 2006-05-15 2012-04-04 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
CA2661334C (en) 2006-08-23 2011-11-29 Pfizer Products Inc. Pyrimidone compounds as gsk-3 inhibitors
WO2008030448A1 (en) 2006-09-07 2008-03-13 Millennium Pharmaceuticals, Inc. Phenethylamide derivatives with kinase inhibitory activity
MX2009011952A (es) 2007-05-04 2009-12-11 Irm Llc Compuestos y composiciones como inhibidores de cinasa c-kit y pdgfr.
US20100197924A1 (en) * 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
EP2643314B1 (en) * 2010-11-25 2016-07-13 ratiopharm GmbH Novel salts and polymorphic forms of afatinib
WO2013097224A1 (en) 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors
CN107531682B (zh) * 2015-04-15 2021-05-04 百济神州有限公司 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途

Also Published As

Publication number Publication date
TWI792406B (zh) 2023-02-11
EP3283486B1 (en) 2022-07-27
CN107531682B (zh) 2021-05-04
EA035680B1 (ru) 2020-07-24
KR102643609B1 (ko) 2024-03-05
CA2981746A1 (en) 2016-10-20
JP7320741B2 (ja) 2023-08-04
MX2017013219A (es) 2018-02-15
IL255555A (en) 2018-01-31
CN113307805A (zh) 2021-08-27
KR20240049684A (ko) 2024-04-16
BR112017020945A2 (pt) 2018-07-10
TWI832668B (zh) 2024-02-11
TW202330526A (zh) 2023-08-01
ZA201706392B (en) 2019-05-29
AU2016248376B2 (en) 2020-10-08
JP2024012540A (ja) 2024-01-30
EP3283486A4 (en) 2018-08-22
TW202138370A (zh) 2021-10-16
TW201702241A (zh) 2017-01-16
TWI736531B (zh) 2021-08-21
CA2981746C (en) 2023-08-01
IL287740A (en) 2021-12-01
JP2018511634A (ja) 2018-04-26
US10351559B2 (en) 2019-07-16
KR20170139073A (ko) 2017-12-18
IL255555B (en) 2021-12-01
EP4119559A1 (en) 2023-01-18
SG11201707984TA (en) 2017-11-29
NZ735715A (en) 2022-09-30
AU2016248376A1 (en) 2017-10-12
CN107531682A (zh) 2018-01-02
JP7383652B2 (ja) 2023-11-20
EP3283486A1 (en) 2018-02-21
WO2016165626A1 (en) 2016-10-20
JP2021073246A (ja) 2021-05-13
US20180127412A1 (en) 2018-05-10

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