KR101845931B1 - 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 - Google Patents

헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 Download PDF

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KR101845931B1
KR101845931B1 KR1020160067210A KR20160067210A KR101845931B1 KR 101845931 B1 KR101845931 B1 KR 101845931B1 KR 1020160067210 A KR1020160067210 A KR 1020160067210A KR 20160067210 A KR20160067210 A KR 20160067210A KR 101845931 B1 KR101845931 B1 KR 101845931B1
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South Korea
Prior art keywords
pyrimidin
amino
oxo
chloro
dihydroquinazolin
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KR1020160067210A
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Korean (ko)
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KR20160150006A (ko
Inventor
이계형
임희종
조희영
박우규
김성환
최정환
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한국화학연구원
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Priority to US15/567,692 priority Critical patent/US10526337B2/en
Priority to CN201680030953.XA priority patent/CN107690433B/zh
Priority to PCT/KR2016/005798 priority patent/WO2016204429A1/ko
Priority to ES16811842T priority patent/ES2816050T3/es
Priority to PH1/2017/501989A priority patent/PH12017501989B1/en
Priority to MX2017014478A priority patent/MX385704B/es
Priority to BR112017025518-9A priority patent/BR112017025518B1/pt
Priority to HUE16811842A priority patent/HUE052332T2/hu
Priority to HK18110179.2A priority patent/HK1250714B/zh
Priority to RU2017140446A priority patent/RU2719367C2/ru
Priority to EP16811842.0A priority patent/EP3312175B1/en
Priority to CA2979815A priority patent/CA2979815C/en
Priority to PL16811842T priority patent/PL3312175T3/pl
Priority to AU2016279661A priority patent/AU2016279661B2/en
Priority to JP2017565779A priority patent/JP6808905B2/ja
Priority to PT168118420T priority patent/PT3312175T/pt
Priority to SG11201707448SA priority patent/SG11201707448SA/en
Priority to MYPI2017001544A priority patent/MY189345A/en
Priority to TW105118848A priority patent/TWI616446B/zh
Publication of KR20160150006A publication Critical patent/KR20160150006A/ko
Priority to ZA2017/07096A priority patent/ZA201707096B/en
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Publication of KR101845931B1 publication Critical patent/KR101845931B1/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23L—FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES, NOT OTHERWISE PROVIDED FOR; PREPARATION OR TREATMENT THEREOF
    • A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
    • A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
    • 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
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
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    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
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    • A61P17/06—Antipsoriatics
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D497/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
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    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
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    • A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23V—INDEXING SCHEME RELATING TO FOODS, FOODSTUFFS OR NON-ALCOHOLIC BEVERAGES AND LACTIC OR PROPIONIC ACID BACTERIA USED IN FOODSTUFFS OR FOOD PREPARATION
    • A23V2200/00—Function of food ingredients
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  • Medicinal Chemistry (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Diabetes (AREA)
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  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Coloring Foods And Improving Nutritive Qualities (AREA)
KR1020160067210A 2015-06-18 2016-05-31 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물 Active KR101845931B1 (ko)

Priority Applications (20)

Application Number Priority Date Filing Date Title
PL16811842T PL3312175T3 (pl) 2015-06-18 2016-06-01 Pochodne heteroarylowe lub ich farmaceutycznie dopuszczalna sól, sposób ich wytwarzania, i kompozycja farmaceutyczna zawierająca je jako substancję czynną do zapobiegania lub leczenia chorób związanych z kinazą PI3
PCT/KR2016/005798 WO2016204429A1 (ko) 2015-06-18 2016-06-01 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물.
ES16811842T ES2816050T3 (es) 2015-06-18 2016-06-01 Derivado heteroarilo o sal farmacéuticamente aceptable del mismo, método de preparación del mismo y composición farmacéutica para prevenir o tratar enfermedades asociadas con PI3 quinasas, que contiene el mismo como principio activo
PH1/2017/501989A PH12017501989B1 (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with pi3 kinases, containing same as active ingredient
MX2017014478A MX385704B (es) 2015-06-18 2016-06-01 Derivado de heteroarilo o su sal farmacéuticamente aceptable, su método de preparación y composición farmacéutica para la prevención o tratamiento de enfermedades asociadas con pi3 cinasas que contiene el mismo como ingrediente activo.
BR112017025518-9A BR112017025518B1 (pt) 2015-06-18 2016-06-01 Compostos derivado de heteroarila, isômero óptico do mesmo ou sal farmaceuticamente aceitável do mesmo, uso dos mesmos e composição farmacêutica para a prevenção ou tratamento de doença relacionada à pi3 quinase, bem como métodos para preparar os ditos compostos
HUE16811842A HUE052332T2 (hu) 2015-06-18 2016-06-01 Heteroaril-származék vagy gyógyászatilag elfogadható sója, eljárás annak elõállítására, és az ezeket hatóanyagént tartalmazó gyógyászati készítmény PI3 kinázokkal összefüggõ betegségek megelõzésére vagy kezelésére
HK18110179.2A HK1250714B (zh) 2015-06-18 2016-06-01 杂芳基衍生物或其药学上可接受的盐、其制备方法以及包含其作为活性成分的用於预防或治疗pi3激酶相关疾病的药物组合物
CN201680030953.XA CN107690433B (zh) 2015-06-18 2016-06-01 杂芳基衍生物或其药学上可接受的盐、其制备方法以及包含其作为活性成分的用于预防或治疗pi3激酶相关疾病的药物组合物
EP16811842.0A EP3312175B1 (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with pi3 kinases, containing same as active ingredient
US15/567,692 US10526337B2 (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing same as active ingredient
JP2017565779A JP6808905B2 (ja) 2015-06-18 2016-06-01 ヘテロアリール誘導体またはその薬学的に許容可能な塩、その製造方法、及びそれを有効成分として含むｐｉ３キナーゼ関連疾患の予防または治療用薬学的組成物
CA2979815A CA2979815C (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with pi3 kinases, containing same as active ingredient
AU2016279661A AU2016279661B2 (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing same as active ingredient
PT168118420T PT3312175T (pt) 2015-06-18 2016-06-01 Derivado de heteroarilo ou seu sal farmaceuticamente aceitável, respetivo método de preparação e composição farmacêutica para a prevenção ou tratamento de doenças associadas com pi3 cinases, que contêm o mesmo como ingrediente ativo
SG11201707448SA SG11201707448SA (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with pi3 kinases, containing same as active ingredient
MYPI2017001544A MY189345A (en) 2015-06-18 2016-06-01 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with pi3 kinases, containing same as active ingredient
RU2017140446A RU2719367C2 (ru) 2015-06-18 2016-06-01 Гетероарильное производное или его фармацевтически приемлемая соль, способ их получения и фармацевтическая композиция для профилактики или лечения заболеваний, связанных с pi3 киназами, содержащая данное действующее вещество
TW105118848A TWI616446B (zh) 2015-06-18 2016-06-15 雜芳基衍生物或其醫藥上可接受之鹽類、其製備方法以及用於預防或治療ｐｉ３激酶相關疾病之醫藥組成物
ZA2017/07096A ZA201707096B (en) 2015-06-18 2017-10-19 Heteroaryl derivative or pharmaceutically acceptable salt thereof, preparation method therefor, and pharmaceutical composition for preventing or treating diseases associated with pi3 kinases, containing same as active ingredient

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR20150086372 2015-06-18
KR1020150086372 2015-06-18

Publications (2)

Publication Number Publication Date
KR20160150006A KR20160150006A (ko) 2016-12-28
KR101845931B1 true KR101845931B1 (ko) 2018-04-05

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KR1020160067210A Active KR101845931B1 (ko) 2015-06-18 2016-05-31 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물

Country Status (18)

Country Link
US (1) US10526337B2 (https=)
EP (1) EP3312175B1 (https=)
JP (1) JP6808905B2 (https=)
KR (1) KR101845931B1 (https=)
CN (1) CN107690433B (https=)
AU (1) AU2016279661B2 (https=)
CA (1) CA2979815C (https=)
ES (1) ES2816050T3 (https=)
HU (1) HUE052332T2 (https=)
MX (1) MX385704B (https=)
MY (1) MY189345A (https=)
PH (1) PH12017501989B1 (https=)
PL (1) PL3312175T3 (https=)
PT (1) PT3312175T (https=)
RU (1) RU2719367C2 (https=)
SG (1) SG11201707448SA (https=)
TW (1) TWI616446B (https=)
ZA (1) ZA201707096B (https=)

Cited By (1)

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