TWI792406B - B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 - Google Patents

B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 Download PDF

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TWI792406B
TWI792406B TW110125410A TW110125410A TWI792406B TW I792406 B TWI792406 B TW I792406B TW 110125410 A TW110125410 A TW 110125410A TW 110125410 A TW110125410 A TW 110125410A TW I792406 B TWI792406 B TW I792406B
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crystalline form
compound
dihydro
salt
sesquimaleate
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TW110125410A
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English (en)
Chinese (zh)
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TW202138370A (zh
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張國良
昌友 周
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英屬開曼群島商百濟神州有限公司
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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
    • 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
    • A61K31/435—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

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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)
TW110125410A 2015-04-15 2016-04-14 B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途 TWI792406B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
WOPCT/CN2015/076639 2015-04-15
CN2015076639 2015-04-15

Publications (2)

Publication Number Publication Date
TW202138370A TW202138370A (zh) 2021-10-16
TWI792406B true TWI792406B (zh) 2023-02-11

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TW113101605A TWI876835B (zh) 2015-04-15 2016-04-14 B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途
TW110125410A TWI792406B (zh) 2015-04-15 2016-04-14 B-raf激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途
TW112101259A TWI832668B (zh) 2015-04-15 2016-04-14 Ｂ-ｒａｆ激酶抑制劑的無定形形式、鹽酸鹽、甲磺酸鹽、２-羥基乙磺酸鹽、ｌ-酒石酸鹽或草酸鹽及其用途
TW105111715A TWI736531B (zh) 2015-04-15 2016-04-14 B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途

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TW113101605A TWI876835B (zh) 2015-04-15 2016-04-14 B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途

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TW112101259A TWI832668B (zh) 2015-04-15 2016-04-14 Ｂ-ｒａｆ激酶抑制劑的無定形形式、鹽酸鹽、甲磺酸鹽、２-羥基乙磺酸鹽、ｌ-酒石酸鹽或草酸鹽及其用途
TW105111715A TWI736531B (zh) 2015-04-15 2016-04-14 B-raf 激酶抑制劑的馬來酸鹽、其結晶形式、製備方法及用途

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US (1) US10351559B2 (enExample)
EP (2) EP4119559A1 (enExample)
JP (3) JP7320741B2 (enExample)
KR (2) KR102643609B1 (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) TWI876835B (enExample)
WO (1) WO2016165626A1 (enExample)
ZA (1) ZA201706392B (enExample)

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JP5885670B2 (ja) 2009-12-11 2016-03-15 アルデイラ セラピューティクス， インコーポレイテッド 黄斑変性の処置のための組成物および方法
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JP6514114B2 (ja) 2013-01-23 2019-05-15 アルデイラ セラピューティクス， インコーポレイテッド 毒性アルデヒド関連疾患および処置
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
WO2017035077A1 (en) 2015-08-21 2017-03-02 Aldeyra Therapeutics, Inc. Deuterated compounds and uses thereof
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
CN110494166B (zh) 2017-05-02 2022-11-08 诺华股份有限公司 组合疗法
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
LT3873894T (lt) * 2018-10-31 2023-06-26 Les Laboratoires Servier Naujoji bcl-2 inhibitoriaus druska, susijusi kristalinė forma, jos gamybos būdas ir farmacinės kompozicijos, kurių sudėtyje ji yra
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
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
BR112021016921A2 (pt) * 2019-03-15 2021-11-03 Forma Therapeutics Inc Inibição de proteína de ligação a elemento responsivo a amp cíclico (creb)
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
EP3962894A4 (en) 2019-05-02 2023-01-11 Aldeyra Therapeutics, Inc. POLYMORPHIC COMPOUNDS AND USES THEREOF
BR112021022335A2 (pt) 2019-05-13 2021-12-28 Novartis Ag Formas cristalinas de n-(3-(2-(2-hidroxietoxi)-6-morfolinopiridin-4-il)-4-metilfenil)-2 (trifluorome-til)isonicotinamida como inibidores raf para o tratamento de câncer
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
KR20230048476A (ko) * 2020-04-03 2023-04-11 베이진 리미티드 암 치료 시에 사용하기 위한 미르다메티닙과 리피라페닙의 공동 투여
EP4149470A4 (en) 2020-05-13 2024-04-24 Aldeyra Therapeutics, Inc. 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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TWI736531B (zh) * 2015-04-15 2021-08-21 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、製備方法及用途

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CN103596926A (zh) * 2011-12-31 2014-02-19 百济神州有限公司 作为raf激酶抑制剂的稠合三环化合物
TWI736531B (zh) * 2015-04-15 2021-08-21 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、製備方法及用途

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IL287740B2 (en) 2025-11-01
CA2981746C (en) 2023-08-01
EA035680B1 (ru) 2020-07-24
TW202138370A (zh) 2021-10-16
IL255555B (en) 2021-12-01
WO2016165626A1 (en) 2016-10-20
JP2024012540A (ja) 2024-01-30
US10351559B2 (en) 2019-07-16
EA201792254A1 (ru) 2018-02-28
MX381053B (es) 2025-03-12
TWI876835B (zh) 2025-03-11
ZA201706392B (en) 2019-05-29
EP3283486A1 (en) 2018-02-21
TW202330526A (zh) 2023-08-01
CN107531682A (zh) 2018-01-02
KR20170139073A (ko) 2017-12-18
TWI736531B (zh) 2021-08-21
JP7383652B2 (ja) 2023-11-20
KR20240049684A (ko) 2024-04-16
TW202434587A (zh) 2024-09-01
TW201702241A (zh) 2017-01-16
KR102643609B1 (ko) 2024-03-05
MX2017013219A (es) 2018-02-15
JP2021073246A (ja) 2021-05-13
EP3283486A4 (en) 2018-08-22
CN107531682B (zh) 2021-05-04
IL255555A (en) 2018-01-31
EP3283486B1 (en) 2022-07-27
EP4119559A1 (en) 2023-01-18
JP7320741B2 (ja) 2023-08-04
CN113307805A (zh) 2021-08-27
US20180127412A1 (en) 2018-05-10
IL287740B1 (en) 2025-07-01
SG11201707984TA (en) 2017-11-29
IL287740A (en) 2021-12-01
CA2981746A1 (en) 2016-10-20
TWI832668B (zh) 2024-02-11
AU2016248376A1 (en) 2017-10-12
NZ735715A (en) 2022-09-30
AU2016248376B2 (en) 2020-10-08
JP2018511634A (ja) 2018-04-26
BR112017020945A2 (pt) 2018-07-10

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