JP6320379B2 - Ｃｄｋ４／６阻害剤およびｂ−ｒａｆ阻害剤の組合せ医薬 - Google Patents

Ｃｄｋ４／６阻害剤およびｂ−ｒａｆ阻害剤の組合せ医薬 Download PDF

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JP6320379B2
JP6320379B2 JP2015524444A JP2015524444A JP6320379B2 JP 6320379 B2 JP6320379 B2 JP 6320379B2 JP 2015524444 A JP2015524444 A JP 2015524444A JP 2015524444 A JP2015524444 A JP 2015524444A JP 6320379 B2 JP6320379 B2 JP 6320379B2
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cancer
combination
inhibitor
compound
raf
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JP2015523397A (ja
JP2015523397A5 (enExample
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カポニグロ，ジョルダーノ
スチュアート，ダリン
キム，スンキュ
ルー，アリス
デラック，スコット
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ノバルティス アーゲー
ノバルティス アーゲー
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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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015524444A 2012-07-26 2013-07-25 Ｃｄｋ４／６阻害剤およびｂ−ｒａｆ阻害剤の組合せ医薬 Active JP6320379B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261676134P 2012-07-26 2012-07-26
US61/676,134 2012-07-26
US201361830911P 2013-06-04 2013-06-04
US61/830,911 2013-06-04
PCT/US2013/051990 WO2014018725A1 (en) 2012-07-26 2013-07-25 Pharmaceutical combinations of a cdk4/6 inhibitor and a b-raf inhibitor

Publications (3)

Publication Number Publication Date
JP2015523397A JP2015523397A (ja) 2015-08-13
JP2015523397A5 JP2015523397A5 (enExample) 2016-08-25
JP6320379B2 true JP6320379B2 (ja) 2018-05-09

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JP2015524444A Active JP6320379B2 (ja) 2012-07-26 2013-07-25 Ｃｄｋ４／６阻害剤およびｂ−ｒａｆ阻害剤の組合せ医薬

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US (1) US9700557B2 (enExample)
EP (1) EP2877174B1 (enExample)
JP (1) JP6320379B2 (enExample)
KR (1) KR102113363B1 (enExample)
CN (1) CN104507474B (enExample)
AR (1) AR091876A1 (enExample)
AU (1) AU2013295771B2 (enExample)
CA (1) CA2874860C (enExample)
ES (1) ES2778059T3 (enExample)
IN (1) IN2015DN00376A (enExample)
JO (1) JO3776B1 (enExample)
MX (1) MX360045B (enExample)
RU (1) RU2685250C2 (enExample)
TW (1) TWI599357B (enExample)
WO (1) WO2014018725A1 (enExample)

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ES2676177T3 (es) * 2012-12-20 2018-07-17 Novartis Ag Una combinación farmacéutica que comprende binimetinib
WO2014130932A2 (en) * 2013-02-25 2014-08-28 Novartis Ag Novel androgen receptor mutation
PE20151785A1 (es) 2013-03-21 2015-12-20 Novartis Ag Terapia de combinacion
JP2018502089A (ja) * 2014-12-23 2018-01-25 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Ｍｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Ｒａｆ阻害剤及びａｕｒｏｒａキナーゼ阻害剤の組み合わせ
CN105753869B (zh) * 2015-04-01 2018-09-25 苏州晶云药物科技有限公司 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
EP3279201B1 (en) * 2015-04-01 2019-10-23 Crystal Pharmatech Co., Ltd. Cdk inhibitor, eutectic crystal of mek inhibitor, and preparation method therefor
WO2017037574A1 (en) * 2015-08-28 2017-03-09 Novartis Ag Combinations of the cdk4/6 inhibitor lee011 and the mek1/2 inhibitor trametinib, optionally further comprising the pi3k inhibitor byl719 to treat cancer
CN105732642B (zh) * 2015-11-18 2018-09-25 苏州晶云药物科技有限公司 一种cdk抑制剂和mek抑制剂的共晶及其制备方法
HUE060653T2 (hu) * 2016-06-03 2023-04-28 Array Biopharma Inc Gyógyászati kombinációk
AU2017315357B2 (en) * 2016-08-23 2022-12-01 Eisai R&D Management Co., Ltd. Combination therapies for the treatment of hepatocellular carcinoma
CN109715163B (zh) 2016-09-19 2022-11-22 诺华股份有限公司 包含raf抑制剂和erk抑制剂的治疗组合
WO2018081211A1 (en) * 2016-10-26 2018-05-03 Li George Y Deuterated 7-cyclopentyl-n, n-dimethyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-7h-pyrrolo[2,3-d]pyrimdine-6-carboxamide
US11395821B2 (en) 2017-01-30 2022-07-26 G1 Therapeutics, Inc. Treatment of EGFR-driven cancer with fewer side effects
TWI798218B (zh) 2017-05-02 2023-04-11 瑞士商諾華公司 組合療法
WO2018218633A1 (en) 2017-06-02 2018-12-06 Beijing Percans Oncology Co. Ltd. Combination therapies for treating cancers
WO2019136451A1 (en) 2018-01-08 2019-07-11 G1 Therapeutics, Inc. G1t38 superior dosage regimes
JP2021514359A (ja) 2018-02-15 2021-06-10 ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． キナーゼ阻害剤としての複素環式化合物
WO2019195959A1 (en) * 2018-04-08 2019-10-17 Cothera Biosciences, Inc. Combination therapy for cancers with braf mutation
WO2020010280A1 (en) * 2018-07-06 2020-01-09 Memorial Sloan Kettering Cancer Center Combination therapy with mek inhibitor and cdk4/6 inhibitor to treat pancreatic cancer
CA3123510A1 (en) * 2018-12-20 2020-06-25 Novartis Ag Combination therapy with a raf inhibitor and a cdk4/6 inhibitor for use in the treatment of cancer
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
TW202114667A (zh) * 2019-09-11 2021-04-16 大陸商江蘇恒瑞醫藥股份有限公司 Mek抑制劑與cdk4/6抑制劑聯合在製備治療腫瘤的藥物中的用途
EP4073065B1 (en) 2019-12-10 2025-02-19 F. Hoffmann-La Roche AG New methylquinazolinone derivatives
JP2023525100A (ja) * 2020-05-12 2023-06-14 ノバルティス アーゲー Ｃｒａｆ阻害剤を含む治療的組み合わせ
CA3257280A1 (en) 2022-05-25 2023-11-30 Msd International Gmbh COMBINATION OF A BRAF INHIBITOR, AN EGFR INHIBITOR AND A PD-1 ANTAGONIST FOR THE TREATMENT OF COLORECTAL CANCER MSI-H/DMMR, WITH BRAF V600E MUTATION
WO2025003956A1 (en) 2023-06-30 2025-01-02 Pfizer Inc. High drug loading formulations of encorafenib

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SI2130537T1 (sl) * 2002-03-13 2013-01-31 Array Biopharma, Inc. N3-alkilirani derivati benzimidazola kot inhibitorji mek
US7235537B2 (en) * 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
BRPI0509580A (pt) * 2004-03-30 2007-11-27 Pfizer Prod Inc combinações de inibidores de transdução de sinal
RU2508110C2 (ru) 2008-07-11 2014-02-27 Новартис Аг КОМБИНАЦИЯ (А) ИНГИБИТОРА ФОСФОИНОЗИТ-3-КИНАЗЫ И (Б) МОДУЛЯТОРА ПУТИ Ras/Raf/Mek
JO2924B1 (en) * 2008-08-22 2015-09-15 نوفارتيس ايه جي Pyroloperimidine compounds and their uses
JO3002B1 (ar) * 2009-08-28 2016-09-05 Irm Llc مركبات و تركيبات كمثبطات كيناز بروتين
WO2011130232A1 (en) 2010-04-13 2011-10-20 Novartis Ag Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase (cdk4/6) inhibitor and an mtor inhibitor for treating cancer

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KR102113363B1 (ko) 2020-05-21
IN2015DN00376A (enExample) 2015-06-12
AU2013295771A1 (en) 2014-12-11
CA2874860A1 (en) 2014-01-30
TWI599357B (zh) 2017-09-21
MX2015001122A (es) 2015-04-08
RU2685250C2 (ru) 2019-04-17
CN104507474A (zh) 2015-04-08
EP2877174A1 (en) 2015-06-03
AR091876A1 (es) 2015-03-04
CN104507474B (zh) 2018-01-02
AU2013295771B2 (en) 2016-08-11
JO3776B1 (ar) 2021-01-31
US20150164897A1 (en) 2015-06-18
ES2778059T3 (es) 2020-08-07
EP2877174B1 (en) 2020-01-01
JP2015523397A (ja) 2015-08-13
MX360045B (es) 2018-10-19
TW201412316A (zh) 2014-04-01
HK1210721A1 (en) 2016-05-06
US9700557B2 (en) 2017-07-11
BR112014033118A2 (pt) 2017-06-27
KR20150036146A (ko) 2015-04-07
WO2014018725A1 (en) 2014-01-30
CA2874860C (en) 2020-06-23
RU2015106524A (ru) 2016-09-20
BR112014033118A8 (pt) 2023-01-31

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