RU2014148964A - Антиретровирусная композиция - Google Patents
Антиретровирусная композиция Download PDFInfo
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- RU2014148964A RU2014148964A RU2014148964A RU2014148964A RU2014148964A RU 2014148964 A RU2014148964 A RU 2014148964A RU 2014148964 A RU2014148964 A RU 2014148964A RU 2014148964 A RU2014148964 A RU 2014148964A RU 2014148964 A RU2014148964 A RU 2014148964A
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- Russia
- Prior art keywords
- oral administration
- pharmaceutical composition
- solid pharmaceutical
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- sprinkler
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- 230000000798 anti-retroviral effect Effects 0.000 title claims abstract 21
- 239000000203 mixture Substances 0.000 title claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 47
- 239000007787 solid Substances 0.000 claims abstract 47
- 239000003814 drug Substances 0.000 claims abstract 23
- 229940079593 drug Drugs 0.000 claims abstract 22
- 239000002245 particle Substances 0.000 claims abstract 18
- 229920000642 polymer Polymers 0.000 claims abstract 17
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 claims abstract 14
- 229960000311 ritonavir Drugs 0.000 claims abstract 14
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims abstract 14
- 239000012453 solvate Substances 0.000 claims abstract 11
- ZHNUHDYFZUAESO-UHFFFAOYSA-N Formamide Chemical compound NC=O ZHNUHDYFZUAESO-UHFFFAOYSA-N 0.000 claims abstract 8
- 229940123527 Nucleotide reverse transcriptase inhibitor Drugs 0.000 claims abstract 6
- 229940122313 Nucleoside reverse transcriptase inhibitor Drugs 0.000 claims abstract 3
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims abstract 3
- 229940124524 integrase inhibitor Drugs 0.000 claims abstract 3
- 239000002850 integrase inhibitor Substances 0.000 claims abstract 3
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims abstract 3
- 239000000651 prodrug Substances 0.000 claims abstract 3
- 229940002612 prodrug Drugs 0.000 claims abstract 3
- 239000003419 rna directed dna polymerase inhibitor Substances 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 3
- 150000002148 esters Chemical class 0.000 claims abstract 2
- HHFAWKCIHAUFRX-UHFFFAOYSA-N ethoxide Chemical compound CC[O-] HHFAWKCIHAUFRX-UHFFFAOYSA-N 0.000 claims abstract 2
- 239000003112 inhibitor Substances 0.000 claims abstract 2
- 230000035800 maturation Effects 0.000 claims abstract 2
- 239000008187 granular material Substances 0.000 claims 8
- KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 claims 7
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- 238000000576 coating method Methods 0.000 claims 6
- 239000007888 film coating Substances 0.000 claims 6
- 238000009501 film coating Methods 0.000 claims 6
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- 208000031886 HIV Infections Diseases 0.000 claims 4
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- 229960001997 adefovir Drugs 0.000 claims 4
- WOZSCQDILHKSGG-UHFFFAOYSA-N adefovir depivoxil Chemical compound N1=CN=C2N(CCOCP(=O)(OCOC(=O)C(C)(C)C)OCOC(=O)C(C)(C)C)C=NC2=C1N WOZSCQDILHKSGG-UHFFFAOYSA-N 0.000 claims 4
- 229920001577 copolymer Polymers 0.000 claims 4
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 4
- 229960000884 nelfinavir Drugs 0.000 claims 4
- QAGYKUNXZHXKMR-HKWSIXNMSA-N nelfinavir Chemical compound CC1=C(O)C=CC=C1C(=O)N[C@H]([C@H](O)CN1[C@@H](C[C@@H]2CCCC[C@@H]2C1)C(=O)NC(C)(C)C)CSC1=CC=CC=C1 QAGYKUNXZHXKMR-HKWSIXNMSA-N 0.000 claims 4
- NQDJXKOVJZTUJA-UHFFFAOYSA-N nevirapine Chemical group C12=NC=CC=C2C(=O)NC=2C(C)=CC=NC=2N1C1CC1 NQDJXKOVJZTUJA-UHFFFAOYSA-N 0.000 claims 4
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- 239000013543 active substance Substances 0.000 claims 3
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- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 3
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- 229920003169 water-soluble polymer Polymers 0.000 claims 3
- UDJZTGMLYITLIQ-UHFFFAOYSA-N 1-ethenylpyrrolidine Chemical compound C=CN1CCCC1 UDJZTGMLYITLIQ-UHFFFAOYSA-N 0.000 claims 2
- GWFOVSGRNGAGDL-FSDSQADBSA-N 2-amino-9-[(1r,2r,3s)-2,3-bis(hydroxymethyl)cyclobutyl]-3h-purin-6-one Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1C[C@H](CO)[C@H]1CO GWFOVSGRNGAGDL-FSDSQADBSA-N 0.000 claims 2
- HSBKFSPNDWWPSL-CAHLUQPWSA-N 4-amino-5-fluoro-1-[(2r,5s)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]pyrimidin-2-one Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1C=C[C@@H](CO)O1 HSBKFSPNDWWPSL-CAHLUQPWSA-N 0.000 claims 2
- HSBKFSPNDWWPSL-VDTYLAMSSA-N 4-amino-5-fluoro-1-[(2s,5r)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]pyrimidin-2-one Chemical compound C1=C(F)C(N)=NC(=O)N1[C@@H]1C=C[C@H](CO)O1 HSBKFSPNDWWPSL-VDTYLAMSSA-N 0.000 claims 2
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- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 claims 2
- XQSPYNMVSIKCOC-NTSWFWBYSA-N Emtricitabine Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1O[C@@H](CO)SC1 XQSPYNMVSIKCOC-NTSWFWBYSA-N 0.000 claims 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims 2
- XNKLLVCARDGLGL-JGVFFNPUSA-N Stavudine Chemical compound O=C1NC(=O)C(C)=CN1[C@H]1C=C[C@@H](CO)O1 XNKLLVCARDGLGL-JGVFFNPUSA-N 0.000 claims 2
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 claims 2
- WREGKURFCTUGRC-POYBYMJQSA-N Zalcitabine Chemical compound O=C1N=C(N)C=CN1[C@@H]1O[C@H](CO)CC1 WREGKURFCTUGRC-POYBYMJQSA-N 0.000 claims 2
- RLAHNGKRJJEIJL-RFZPGFLSSA-N [(2r,4r)-4-(2,6-diaminopurin-9-yl)-1,3-dioxolan-2-yl]methanol Chemical compound C12=NC(N)=NC(N)=C2N=CN1[C@H]1CO[C@@H](CO)O1 RLAHNGKRJJEIJL-RFZPGFLSSA-N 0.000 claims 2
- 229960004748 abacavir Drugs 0.000 claims 2
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- 229960001830 amprenavir Drugs 0.000 claims 2
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- 229960003277 atazanavir Drugs 0.000 claims 2
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- WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine mesylate Natural products CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 WHBIGIKBNXZKFE-UHFFFAOYSA-N 0.000 claims 2
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- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 claims 2
- 229960003586 elvitegravir Drugs 0.000 claims 2
- JUZYLCPPVHEVSV-LJQANCHMSA-N elvitegravir Chemical compound COC1=CC=2N([C@H](CO)C(C)C)C=C(C(O)=O)C(=O)C=2C=C1CC1=CC=CC(Cl)=C1F JUZYLCPPVHEVSV-LJQANCHMSA-N 0.000 claims 2
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- YXPVEXCTPGULBZ-WQYNNSOESA-N entecavir hydrate Chemical compound O.C1=NC=2C(=O)NC(N)=NC=2N1[C@H]1C[C@H](O)[C@@H](CO)C1=C YXPVEXCTPGULBZ-WQYNNSOESA-N 0.000 claims 2
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- 229960001936 indinavir Drugs 0.000 claims 2
- CBVCZFGXHXORBI-PXQQMZJSSA-N indinavir Chemical compound C([C@H](N(CC1)C[C@@H](O)C[C@@H](CC=2C=CC=CC=2)C(=O)N[C@H]2C3=CC=CC=C3C[C@H]2O)C(=O)NC(C)(C)C)N1CC1=CC=CN=C1 CBVCZFGXHXORBI-PXQQMZJSSA-N 0.000 claims 2
- 229960001627 lamivudine Drugs 0.000 claims 2
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims 2
- 229950005339 lobucavir Drugs 0.000 claims 2
- 239000000314 lubricant Substances 0.000 claims 2
- VPABMVYNSQRPBD-AOJMVMDXSA-N methyl (2r)-2-[[(4-bromophenoxy)-[[(2s,5r)-5-(5-methyl-2,4-dioxopyrimidin-1-yl)-2,5-dihydrofuran-2-yl]methoxy]phosphoryl]amino]propanoate Chemical compound N1([C@@H]2O[C@@H](C=C2)COP(=O)(N[C@H](C)C(=O)OC)OC=2C=CC(Br)=CC=2)C=C(C)C(=O)NC1=O VPABMVYNSQRPBD-AOJMVMDXSA-N 0.000 claims 2
- 229960000689 nevirapine Drugs 0.000 claims 2
- RXBWRFDZXRAEJT-SZNOJMITSA-N palinavir Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)C=1N=C2C=CC=CC2=CC=1)C(C)C)[C@H](O)CN1[C@@H](C[C@@H](CC1)OCC=1C=CN=CC=1)C(=O)NC(C)(C)C)C1=CC=CC=C1 RXBWRFDZXRAEJT-SZNOJMITSA-N 0.000 claims 2
- 229950006460 palinavir Drugs 0.000 claims 2
- 229960004742 raltegravir Drugs 0.000 claims 2
- CZFFBEXEKNGXKS-UHFFFAOYSA-N raltegravir Chemical group O1C(C)=NN=C1C(=O)NC(C)(C)C1=NC(C(=O)NCC=2C=CC(F)=CC=2)=C(O)C(=O)N1C CZFFBEXEKNGXKS-UHFFFAOYSA-N 0.000 claims 2
- 229960001852 saquinavir Drugs 0.000 claims 2
- QWAXKHKRTORLEM-UGJKXSETSA-N saquinavir Chemical group C([C@@H]([C@H](O)CN1C[C@H]2CCCC[C@H]2C[C@H]1C(=O)NC(C)(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)C=1N=C2C=CC=CC2=CC=1)C1=CC=CC=C1 QWAXKHKRTORLEM-UGJKXSETSA-N 0.000 claims 2
- 239000008137 solubility enhancer Substances 0.000 claims 2
- 229960001203 stavudine Drugs 0.000 claims 2
- 229960004556 tenofovir Drugs 0.000 claims 2
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical group OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims 2
- 229920002554 vinyl polymer Polymers 0.000 claims 2
- 229960000523 zalcitabine Drugs 0.000 claims 2
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- HBOMLICNUCNMMY-XLPZGREQSA-N zidovudine Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](CO)[C@@H](N=[N+]=[N-])C1 HBOMLICNUCNMMY-XLPZGREQSA-N 0.000 claims 2
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- 229920002472 Starch Polymers 0.000 claims 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 claims 1
- 150000001241 acetals Chemical class 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
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- 229920000233 poly(alkylene oxides) Polymers 0.000 claims 1
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Classifications
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
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- A61K9/5084—Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
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- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Application Number | Priority Date | Filing Date | Title |
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IN1380MU2012 | 2012-05-03 | ||
IN1380/MUM/2012 | 2012-05-03 | ||
IN2590MU2012 | 2012-09-06 | ||
IN2590/MUM/2012 | 2012-09-06 | ||
PCT/GB2013/000193 WO2013164559A1 (en) | 2012-05-03 | 2013-05-03 | Antiretroviral composition |
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Publication Number | Publication Date |
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RU2014148964A true RU2014148964A (ru) | 2016-06-27 |
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RU2014148964A RU2014148964A (ru) | 2012-05-03 | 2013-05-03 | Антиретровирусная композиция |
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US (1) | US20150086628A1 (OSRAM) |
EP (1) | EP2844231A1 (OSRAM) |
JP (1) | JP6314131B2 (OSRAM) |
KR (1) | KR20150021510A (OSRAM) |
CN (1) | CN104411300A (OSRAM) |
AU (1) | AU2013255666A1 (OSRAM) |
CA (1) | CA2871794A1 (OSRAM) |
IN (1) | IN2014MN02252A (OSRAM) |
JO (1) | JO3641B1 (OSRAM) |
MX (1) | MX2014013326A (OSRAM) |
RU (1) | RU2014148964A (OSRAM) |
WO (1) | WO2013164559A1 (OSRAM) |
ZA (1) | ZA201408281B (OSRAM) |
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RU2663466C1 (ru) * | 2017-03-20 | 2018-08-06 | Общество с ограниченной ответственностью "МБА-групп" | Композиция для профилактики и/или лечения вич-инфекции |
CN112220771B (zh) * | 2020-11-10 | 2023-03-31 | 成都大学 | 扎西他滨渗透泵型控释片及其制备方法 |
US20250242031A1 (en) * | 2022-02-14 | 2025-07-31 | Purdue Research Foundation | Polymer salts for improved drug delivery from amorphous solid dispersions |
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NZ226822A (en) * | 1987-11-16 | 1990-03-27 | Mcneil Consumer Prod | Chewable medicament tablet containing means for taste masking |
US5696270A (en) | 1989-05-23 | 1997-12-09 | Abbott Laboratories | Intermediate for making retroviral protease inhibiting compounds |
IL110752A (en) | 1993-09-13 | 2000-07-26 | Abbott Lab | Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor |
JP3693270B2 (ja) * | 1995-10-12 | 2005-09-07 | 旭化成ケミカルズ株式会社 | フィルムコーティング顆粒およびその製造方法 |
US5914332A (en) | 1995-12-13 | 1999-06-22 | Abbott Laboratories | Retroviral protease inhibiting compounds |
ZA9710071B (en) | 1996-11-21 | 1998-05-25 | Abbott Lab | Pharmaceutical composition. |
MXPA03010771A (es) | 2001-05-25 | 2004-07-01 | Abbott Lab | Capsulas elasticas blandas que comprenden ritonavir y/o lopinavir. |
US8377952B2 (en) * | 2003-08-28 | 2013-02-19 | Abbott Laboratories | Solid pharmaceutical dosage formulation |
BRPI0507372A (pt) * | 2004-02-06 | 2007-07-10 | Wyeth Corp | formulação de multiparticulados de um o-desmetilvenlafaxina (odv), métodos para tratar de depressão em um paciente em sua necessidade e para reduzir os efeitos colaterais gastrintestinais da venlafaxina em um paciente, formulação de liberação modificada de um multiparticulado, método para reduzir os efeitos colaterais gastrintestinais de um odv em um paciente, produto de venlafaxina de liberação modificada, métodos para reduzir os efeitos colaterais gastrintestinais associados com o tratamento da venlafaxina e para liberar odv a um paciente pediátrico ou geriátrico, formulações de multiparticulados de formiato ou succinato de odv e de liberação retardada de formiato ou succinato de odv, uso de uma formulação, e, pacote farmacêutico |
MXPA06010488A (es) * | 2004-03-31 | 2006-12-19 | Bpsi Holdings Inc | Revestimientos entericos para sustratos oralmente ingeribles. |
US20100173921A1 (en) * | 2006-08-10 | 2010-07-08 | Cipla Limited | Antiretroviral Solid Oral Composition |
CA2707418C (en) * | 2007-11-16 | 2013-11-19 | Boehringer Ingelheim International Gmbh | Inhibitors of human immunodeficiency virus replication |
PA8809601A1 (es) * | 2007-12-24 | 2009-07-23 | Cipla Ltd | Combinación anti-retroviral |
WO2009153654A1 (en) * | 2008-06-17 | 2009-12-23 | Aurobindo Pharma Limited | Solid dosage forms of antiretrovirals |
EP2568964B1 (en) * | 2010-05-10 | 2018-08-01 | Evonik Röhm GmbH | Pharmaceutical dosage form comprising one or more antiretroviral active ingredients |
WO2013057469A1 (en) * | 2011-10-20 | 2013-04-25 | Cipla Limited | Pharmaceutical antiretroviral compositions |
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2013
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2014
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CA2871794A1 (en) | 2013-11-07 |
JO3641B1 (ar) | 2020-08-27 |
EP2844231A1 (en) | 2015-03-11 |
JP2015519326A (ja) | 2015-07-09 |
WO2013164559A1 (en) | 2013-11-07 |
IN2014MN02252A (OSRAM) | 2015-07-24 |
JP6314131B2 (ja) | 2018-04-18 |
US20150086628A1 (en) | 2015-03-26 |
ZA201408281B (en) | 2019-06-26 |
AU2013255666A1 (en) | 2014-11-20 |
KR20150021510A (ko) | 2015-03-02 |
MX2014013326A (es) | 2015-08-10 |
CN104411300A (zh) | 2015-03-11 |
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