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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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

Related Parent Applications (1)

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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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Publication Number Publication Date
CN113307805A true CN113307805A (zh) 2021-08-27

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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
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

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US (1) US10351559B2 (enExample)
EP (2) EP4119559A1 (enExample)
JP (3) JP7320741B2 (enExample)
KR (2) KR20240049684A (enExample)
CN (2) CN107531682B (enExample)
AU (1) AU2016248376B2 (enExample)
CA (1) CA2981746C (enExample)
EA (1) EA035680B1 (enExample)
IL (2) IL255555B (enExample)
MX (1) MX381053B (enExample)
NZ (1) NZ735715A (enExample)
SG (1) SG11201707984TA (enExample)
TW (4) TWI792406B (enExample)
WO (1) WO2016165626A1 (enExample)
ZA (1) ZA201706392B (enExample)

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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
DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
CN117045653A (zh) 2013-01-23 2023-11-14 奥尔德拉医疗公司 与毒性醛相关的疾病和治疗
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
JP6947406B2 (ja) 2015-08-21 2021-10-13 アルデイラ セラピューティクス， インコーポレイテッド 重水素化化合物およびその使用
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
US11266653B2 (en) 2017-05-02 2022-03-08 Novartis Ag Combination therapy
JP7311162B2 (ja) 2017-10-10 2023-07-19 アルデイラ セラピューティクス， インコーポレイテッド 炎症性障害の処置
CN112714762A (zh) * 2018-08-06 2021-04-27 奥尔德拉医疗公司 多晶型化合物及其用途
JOP20210072A1 (ar) * 2018-10-31 2023-01-30 Servier Lab ملح جديد لمثبط bcl-2، صورة بلورية ذات صلة، طريقة تحضيره وتركيبات صيدلية تحتوي عليه
CN111484489B (zh) * 2019-01-25 2023-05-23 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
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
WO2020190780A1 (en) * 2019-03-15 2020-09-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (creb)
EP3962894A4 (en) 2019-05-02 2023-01-11 Aldeyra Therapeutics, Inc. POLYMORPHIC COMPOUNDS AND USES THEREOF
WO2020223717A1 (en) 2019-05-02 2020-11-05 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
CA3138123A1 (en) 2019-05-13 2020-11-19 Novartis Ag New 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
US20230128315A1 (en) * 2020-04-03 2023-04-27 Beigene, Ltd. Co-administration of mirdametinib and lifirafenib for use in treating cancers
CA3175856A1 (en) 2020-05-13 2021-11-18 Todd Brady Pharmaceutical formulations and uses thereof
WO2023240178A1 (en) * 2022-06-08 2023-12-14 Mapkure, Llc Methods of treating cancer with a b-raf inhibitor

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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
KR20080074220A (ko) 2005-12-08 2008-08-12 밀레니엄 파머슈티컬스 인코퍼레이티드 키나아제 억제 활성을 갖는 비시클릭 화합물
WO2007136572A2 (en) 2006-05-15 2007-11-29 Merck & Co., Inc. Antidiabetic bicyclic compounds
ATE530540T1 (de) 2006-08-23 2011-11-15 Pfizer Prod Inc Pyrimidonverbindungen als gsk-3-inhibitoren
EP2061761A1 (en) 2006-09-07 2009-05-27 Millennium Pharmaceuticals, Inc. Phenethylamide derivatives with kinase inhibitory activity
EP2148875A1 (en) 2007-05-04 2010-02-03 Irm Llc Compounds and compositions as c-kit and pdgfr kinase inhibitors
US20100197924A1 (en) * 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
KR20130105675A (ko) * 2010-11-25 2013-09-25 라티오팜 게엠베하 아파티닙의 신규 염 및 다형
DK2797888T3 (en) * 2011-12-31 2016-09-19 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

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

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