TWI876835B - B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途 - Google Patents

B-raf激酶抑制劑的馬來酸鹽、其結晶形式及用途 Download PDF

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TWI876835B
TWI876835B TW113101605A TW113101605A TWI876835B TW I876835 B TWI876835 B TW I876835B TW 113101605 A TW113101605 A TW 113101605A TW 113101605 A TW113101605 A TW 113101605A TW I876835 B TWI876835 B TW I876835B
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Taiwan
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compound
cancer
crystalline form
dihydro
maleate
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TW113101605A
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English (en)
Chinese (zh)
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TW202434587A (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
    • 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)
TW113101605A 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 TWI876835B (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
TW202434587A TW202434587A (zh) 2024-09-01
TWI876835B true TWI876835B (zh) 2025-03-11

Family

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Family Applications (4)

Application Number Title Priority Date Filing Date
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
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
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

Family Applications After (3)

Application Number Title Priority Date Filing Date
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
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

Country Status (15)

Country Link
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) IL287740B2 (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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CA2782015C (en) 2009-12-11 2020-08-25 Neuron Systems, Inc. Topical ophthalmic 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
CN111135171B (zh) 2013-01-23 2023-09-08 奥尔德拉医疗公司 与毒性醛相关的疾病和治疗
AU2016248376B2 (en) * 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
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
WO2018203219A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
CN111356451A (zh) 2017-10-10 2020-06-30 奥尔德拉医疗公司 炎性病症的治疗
CN112105349A (zh) * 2018-04-12 2020-12-18 阿纳韦克斯生命科学公司 A2-73结晶多晶型物质组合物及其使用方法
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
GEP20237494B (en) * 2018-10-31 2023-04-10 Servier Lab Novel salt of a bcl-2 inhibitor, related crystalline form, method for preparing the same and pharmaceutical compositions containing the same
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
EP3937936A4 (en) * 2019-03-15 2022-12-28 Forma Therapeutics, Inc. INHIBITION OF CYCLIC AMP-RESPONSIVE ELEMENT-BINDING PROTEIN (CREB)
CN113784954A (zh) 2019-05-02 2021-12-10 奥尔德拉医疗公司 多晶型化合物和其用途
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
EP4563150A3 (en) 2019-05-13 2025-07-23 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
PL4125842T3 (pl) * 2020-04-03 2024-10-14 Beigene, Ltd. Równoczesne podawanie mirdametynibu i lifirafenibu do stosowania w leczeniu nowotworów
WO2021231792A1 (en) 2020-05-13 2021-11-18 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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CN103476770A (zh) * 2010-11-25 2013-12-25 拉蒂欧制药有限责任公司 新的阿法替尼盐和多晶型物

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WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

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EA035680B1 (ru) 2020-07-24
CA2981746C (en) 2023-08-01
US20180127412A1 (en) 2018-05-10
ZA201706392B (en) 2019-05-29
KR20240049684A (ko) 2024-04-16
AU2016248376A1 (en) 2017-10-12
JP2021073246A (ja) 2021-05-13
EP3283486A4 (en) 2018-08-22
EP3283486A1 (en) 2018-02-21
IL287740B1 (en) 2025-07-01
IL287740A (en) 2021-12-01
TW202330526A (zh) 2023-08-01
JP2018511634A (ja) 2018-04-26
TWI736531B (zh) 2021-08-21
EP4119559A1 (en) 2023-01-18
TW201702241A (zh) 2017-01-16
CN107531682A (zh) 2018-01-02
TWI832668B (zh) 2024-02-11
CN113307805A (zh) 2021-08-27
WO2016165626A1 (en) 2016-10-20
IL287740B2 (en) 2025-11-01
IL255555A (en) 2018-01-31
AU2016248376B2 (en) 2020-10-08
IL255555B (en) 2021-12-01
NZ735715A (en) 2022-09-30
EP3283486B1 (en) 2022-07-27
BR112017020945A2 (pt) 2018-07-10
EA201792254A1 (ru) 2018-02-28
JP7383652B2 (ja) 2023-11-20
CN107531682B (zh) 2021-05-04
TWI792406B (zh) 2023-02-11
JP2024012540A (ja) 2024-01-30
JP7320741B2 (ja) 2023-08-04
KR20170139073A (ko) 2017-12-18
MX381053B (es) 2025-03-12
TW202138370A (zh) 2021-10-16
CA2981746A1 (en) 2016-10-20
SG11201707984TA (en) 2017-11-29
TW202434587A (zh) 2024-09-01
MX2017013219A (es) 2018-02-15
KR102643609B1 (ko) 2024-03-05
US10351559B2 (en) 2019-07-16

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