CN113307805A - B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途 - Google Patents

B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途 Download PDF

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Publication number
CN113307805A
CN113307805A CN202110419671.1A CN202110419671A CN113307805A CN 113307805 A CN113307805 A CN 113307805A CN 202110419671 A CN202110419671 A CN 202110419671A CN 113307805 A CN113307805 A CN 113307805A
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degrees
crystalline form
compound
dihydro
diffraction pattern
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CN202110419671.1A
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Chinese (zh)
Inventor
张国良
周昌友
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BeOne Medicines Ltd
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Beigene Ltd
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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
    • A61K31/41—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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CN202110419671.1A 2015-04-15 2016-04-14 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途 Pending CN113307805A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/076639 2015-04-15
CN2015076639 2015-04-15
CN201680021109.0A CN107531682B (zh) 2015-04-15 2016-04-14 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途

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CN201680021109.0A Division CN107531682B (zh) 2015-04-15 2016-04-14 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途

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CN113307805A true CN113307805A (zh) 2021-08-27

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CN202110419671.1A Pending CN113307805A (zh) 2015-04-15 2016-04-14 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途
CN201680021109.0A Active CN107531682B (zh) 2015-04-15 2016-04-14 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途

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US (1) US10351559B2 (cg-RX-API-DMAC7.html)
EP (2) EP4119559A1 (cg-RX-API-DMAC7.html)
JP (3) JP7320741B2 (cg-RX-API-DMAC7.html)
KR (2) KR102643609B1 (cg-RX-API-DMAC7.html)
CN (2) CN113307805A (cg-RX-API-DMAC7.html)
AU (1) AU2016248376B2 (cg-RX-API-DMAC7.html)
CA (1) CA2981746C (cg-RX-API-DMAC7.html)
EA (1) EA035680B1 (cg-RX-API-DMAC7.html)
IL (2) IL255555B (cg-RX-API-DMAC7.html)
MX (1) MX381053B (cg-RX-API-DMAC7.html)
NZ (1) NZ735715A (cg-RX-API-DMAC7.html)
SG (1) SG11201707984TA (cg-RX-API-DMAC7.html)
TW (4) TWI876835B (cg-RX-API-DMAC7.html)
WO (1) WO2016165626A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201706392B (cg-RX-API-DMAC7.html)

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ES2393768T3 (es) 2005-05-26 2012-12-27 Neuron Systems, Inc Derivado de quinolina para el tratamiento de enfermedades retinianas
WO2011072141A1 (en) 2009-12-11 2011-06-16 Neuron Systems, Inc. Compositions and methods for the treatment of macular degeneration
CN103596926B (zh) 2011-12-31 2015-11-25 百济神州有限公司 作为raf激酶抑制剂的稠合三环化合物
CA3195807A1 (en) 2013-01-23 2014-07-31 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
TWI876835B (zh) * 2015-04-15 2025-03-11 英屬開曼群島商百濟神州有限公司 B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途
CN118724806A (zh) 2015-08-21 2024-10-01 奥尔德拉医疗公司 氘化化合物和其用途
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
KR102641827B1 (ko) 2017-05-02 2024-03-04 노파르티스 아게 병용 요법
EP3694500A4 (en) 2017-10-10 2021-06-30 Aldeyra Therapeutics, Inc. TREATMENT OF INFLAMMATORY DISORDERS
US12006298B2 (en) 2018-08-06 2024-06-11 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
PL3873894T3 (pl) * 2018-10-31 2023-07-31 Les Laboratoires Servier Nowa sól inhibitora BCL-2, powiązana postać krystaliczna, sposób jej wytwarzania oraz zawierające ją kompozycje farmaceutyczne
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
BR112021016921A2 (pt) * 2019-03-15 2021-11-03 Forma Therapeutics Inc Inibição de proteína de ligação a elemento responsivo a amp cíclico (creb)
EP3962894A4 (en) 2019-05-02 2023-01-11 Aldeyra Therapeutics, Inc. POLYMORPHIC COMPOUNDS AND USES THEREOF
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
US12187703B2 (en) 2019-05-13 2025-01-07 Novartis Ag Crystalline forms of N-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as Raf inhibitors for the treatment of cancer
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
TWI893097B (zh) * 2020-04-03 2025-08-11 開曼群島商百濟神州有限公司 用於治療癌症之米達替尼與利非芬尼之共同投藥
EP4149470A4 (en) 2020-05-13 2024-04-24 Aldeyra Therapeutics, Inc. Pharmaceutical formulations and uses thereof
JP2025519981A (ja) * 2022-06-08 2025-06-30 マップキュア，エルエルシー Ｂ－ｒａｆ阻害剤によるがんの治療方法

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WO2006065703A1 (en) 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
WO2007067444A1 (en) 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
PE20080069A1 (es) 2006-05-15 2008-02-22 Merck & Co Inc Compuestos biciclicos como agonistas del receptor 40 acoplado a proteina g (gpr40)
ATE530540T1 (de) 2006-08-23 2011-11-15 Pfizer Prod Inc Pyrimidonverbindungen als gsk-3-inhibitoren
JP2010502706A (ja) 2006-09-07 2010-01-28 ミレニアム・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害活性を有するフェネチルアミド誘導体
BRPI0811517A2 (pt) 2007-05-04 2014-11-18 Irm Llc Compostos e composições como inibidores de c-kit e pdgfr cinase.
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CN103596926B (zh) * 2011-12-31 2015-11-25 百济神州有限公司 作为raf激酶抑制剂的稠合三环化合物
TWI876835B (zh) 2015-04-15 2025-03-11 英屬開曼群島商百濟神州有限公司 B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途

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AU2016248376A1 (en) 2017-10-12
TW202138370A (zh) 2021-10-16
ZA201706392B (en) 2019-05-29
JP7320741B2 (ja) 2023-08-04
NZ735715A (en) 2022-09-30
IL255555B (en) 2021-12-01
TWI876835B (zh) 2025-03-11
AU2016248376B2 (en) 2020-10-08
SG11201707984TA (en) 2017-11-29
KR102643609B1 (ko) 2024-03-05
TWI792406B (zh) 2023-02-11
EP4119559A1 (en) 2023-01-18
EA201792254A1 (ru) 2018-02-28
TW201702241A (zh) 2017-01-16
JP2021073246A (ja) 2021-05-13
BR112017020945A2 (pt) 2018-07-10
US10351559B2 (en) 2019-07-16
IL287740B1 (en) 2025-07-01
TWI736531B (zh) 2021-08-21
EP3283486A4 (en) 2018-08-22
MX2017013219A (es) 2018-02-15
EP3283486A1 (en) 2018-02-21
IL255555A (en) 2018-01-31
EA035680B1 (ru) 2020-07-24
MX381053B (es) 2025-03-12
WO2016165626A1 (en) 2016-10-20
TWI832668B (zh) 2024-02-11
KR20240049684A (ko) 2024-04-16
JP7383652B2 (ja) 2023-11-20
EP3283486B1 (en) 2022-07-27
IL287740A (en) 2021-12-01
US20180127412A1 (en) 2018-05-10
TW202330526A (zh) 2023-08-01
CN107531682A (zh) 2018-01-02
KR20170139073A (ko) 2017-12-18
CA2981746C (en) 2023-08-01
CA2981746A1 (en) 2016-10-20
IL287740B2 (en) 2025-11-01
JP2024012540A (ja) 2024-01-30
JP2018511634A (ja) 2018-04-26
CN107531682B (zh) 2021-05-04
TW202434587A (zh) 2024-09-01

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