HRP20140986T1 - Polimorfni oblik derivata 2-amino(nitroaril)tiazola - Google Patents
Polimorfni oblik derivata 2-amino(nitroaril)tiazola Download PDFInfo
- Publication number
- HRP20140986T1 HRP20140986T1 HRP20140986AT HRP20140986T HRP20140986T1 HR P20140986 T1 HRP20140986 T1 HR P20140986T1 HR P20140986A T HRP20140986A T HR P20140986AT HR P20140986 T HRP20140986 T HR P20140986T HR P20140986 T1 HRP20140986 T1 HR P20140986T1
- Authority
- HR
- Croatia
- Prior art keywords
- polymorphic form
- nitroaryl
- amino
- polymorph form
- thiazole derivative
- Prior art date
Links
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 title 1
- 125000004999 nitroaryl group Chemical group 0.000 title 1
- 150000007979 thiazole derivatives Chemical class 0.000 title 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 4
- 238000000034 method Methods 0.000 claims 3
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 229940098779 methanesulfonic acid Drugs 0.000 claims 2
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000002798 polar solvent Substances 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- 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
- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
- A61P37/08—Antiallergic agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Transplantation (AREA)
- Urology & Nephrology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Catalysts (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Claims (5)
1. Polimorfni oblik spoja (IX), koji ostaje suh kod 80%-tne relativne vlažnosti i termodinamički je stabilan na temperaturama ispod 200 °C:
[image]
,
naznačen time što uzorak difrakcije rendgenskih zraka ima karakteristične signale, izražene u stupnjevima 2θ, na 7,269, 9,120, 11,038, 13,704, 14,481, 15,483, 15,870, 16,718, 17,087, 17,473, 18,224, 19,248, 19,441, 19,940, 20,441, 21,469, 21,750, 22,111, 23,319, 23,763, 24,120, 24,681, 25,754, 26,777, 28,975, 29,609, 30,073.
2. Polimorfni oblik spoja (IX), u skladu s patentnim zahtjevom 1, naznačen time što diferencijalna skenirajuća kalorimetrija (DSC) pokazuje pojedinačni najveći signal na 237,49 ± 0,3 °C.
3. Postupak dobivanja polimorfnog oblika u skladu s bilo kojim od patentnih zahtjeva 1 do 2, naznačen time što se sastoji u obradi 4-(4-metilpiperazin-1-ilmetil)-N-[4-metil-3-(4-piridin-3-iltiazol-2-ilamino)fenil]benzamida metansulfonskom kiselinom, na temperaturi između 20 i 80 °C.
4. Postupak u skladu s patentnim zahtjevom 3, naznačen time što se reakcija provodi u polarnom otapalu.
5. Postupak u skladu s patentnim zahtjevom 3 ili patentnim zahtjevom 4, naznačen time što se reakcija provodi uz upotrebu 1,0 ekvivalenta metansulfonske kiseline.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88958707P | 2007-02-13 | 2007-02-13 |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20140986T1 true HRP20140986T1 (hr) | 2014-11-21 |
Family
ID=39332208
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20110709T HRP20110709T1 (hr) | 2007-02-13 | 2011-10-05 | Postupak sinteze spojeva 2-aminotioazola kao inhibitora kinaza |
HRP20140986AT HRP20140986T1 (hr) | 2007-02-13 | 2014-10-15 | Polimorfni oblik derivata 2-amino(nitroaril)tiazola |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20110709T HRP20110709T1 (hr) | 2007-02-13 | 2011-10-05 | Postupak sinteze spojeva 2-aminotioazola kao inhibitora kinaza |
Country Status (23)
Country | Link |
---|---|
US (3) | US8153792B2 (hr) |
EP (2) | EP2118099B1 (hr) |
JP (2) | JP5568312B2 (hr) |
KR (1) | KR20090110851A (hr) |
CN (2) | CN103342701B (hr) |
AR (1) | AR065337A1 (hr) |
AT (1) | ATE515506T1 (hr) |
AU (1) | AU2008214679A1 (hr) |
BR (1) | BRPI0807626B1 (hr) |
CA (2) | CA2970628C (hr) |
ES (2) | ES2522169T3 (hr) |
HR (2) | HRP20110709T1 (hr) |
IL (1) | IL200320A0 (hr) |
MA (1) | MA31180B1 (hr) |
MX (1) | MX2009008665A (hr) |
NZ (1) | NZ578944A (hr) |
PL (2) | PL2366703T3 (hr) |
RU (2) | RU2456285C2 (hr) |
SI (2) | SI2366703T1 (hr) |
TN (1) | TN2009000342A1 (hr) |
TW (1) | TWI406862B (hr) |
WO (1) | WO2008098949A2 (hr) |
ZA (1) | ZA200905981B (hr) |
Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
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US8450302B2 (en) | 2002-08-02 | 2013-05-28 | Ab Science | 2-(3-aminoaryl) amino-4-aryl-thiazoles and their use as c-kit inhibitors |
CN100491374C (zh) | 2002-08-02 | 2009-05-27 | Ab科学公司 | 2-(3-氨基芳基)氨基-4-芳基-噻唑及其作为c-kit抑制剂的应用 |
US20120302577A1 (en) | 2010-01-28 | 2012-11-29 | Ab Science | Treatment of gist with masitinib |
TW201130830A (en) | 2010-02-01 | 2011-09-16 | Ab Science | Combined treatment of pancreatic cancer with gemcitabine and masitinib |
AR080380A1 (es) | 2010-03-09 | 2012-04-04 | Ab Science | Tratamiento de la demencia tipo alzheimer con masitinib |
TW201204360A (en) | 2010-04-20 | 2012-02-01 | Ab Science | Treatment of multiple sclerosis with MASITINIB |
TW201204719A (en) | 2010-06-02 | 2012-02-01 | Ab Science | Treatment of rheumatoid arthritis with masitinib |
US10045978B2 (en) | 2010-11-05 | 2018-08-14 | Ab Science | Treatment of mastocytosis with masitinib |
US20140147415A1 (en) | 2010-11-05 | 2014-05-29 | Ab Science | Treatment of mastocytosis with masitinib |
US9078894B2 (en) | 2011-02-04 | 2015-07-14 | Ab Science | Treatment of severe persistant asthma with masitinib |
WO2012136732A1 (en) | 2011-04-08 | 2012-10-11 | Ab Science | Treatment of multiple myeloma with masitinib |
WO2014053650A1 (en) | 2012-10-04 | 2014-04-10 | Ab Science | Use of masitinib for treatment of cancer in patient subpopulations identified using predictor factors |
WO2015082496A1 (en) | 2013-12-02 | 2015-06-11 | Ab Science | Use of masitinib for treatment of colorectal cancer |
EP2886543A1 (en) | 2013-12-18 | 2015-06-24 | Sandoz Ag | Crystalline form of mastinib mesylate |
WO2015185958A1 (en) | 2014-06-02 | 2015-12-10 | Ab Science | Use of an inhibitor of kinase activity, particularly masitinib, for treatment of prostate cancer |
CN105585556A (zh) * | 2014-11-13 | 2016-05-18 | 连云港杰瑞药业有限公司 | 一种伊马替尼的合成方法 |
CN106794179A (zh) * | 2015-07-29 | 2017-05-31 | 苏州晶云药物科技有限公司 | 马赛替尼甲磺酸盐的新晶型及其制备方法 |
CA3000894A1 (en) | 2015-10-05 | 2017-04-13 | Ab Science | Treatment of severe systemic mastocytosis with masitinib |
HUE057398T2 (hu) | 2016-03-25 | 2022-05-28 | Ab Science | A masitinib alkalmazása egy amiotrófiás laterálszklerózisos beteg alpopuláció kezelésére |
EP3601278B1 (en) | 2017-03-31 | 2022-10-26 | Sandoz AG | Crystalline form of masitinib |
US10696638B2 (en) | 2017-12-26 | 2020-06-30 | Industrial Technology Research Institute | Compounds for inhibiting AGC kinase and pharmaceutical compositions comprising the same |
WO2021099616A1 (en) | 2019-11-22 | 2021-05-27 | Ab Science | Masitinib for the treatment of sickle cell disease |
EP3831384A1 (en) | 2019-12-02 | 2021-06-09 | AB Science | Use of masitinib for the treatment of eosinophilic asthma |
KR20220143020A (ko) | 2020-02-20 | 2022-10-24 | 에이비 사이언스 | 다발 경화증 환자 하위집단의 치료를 위한 마시티닙 |
US20230226043A1 (en) | 2020-04-10 | 2023-07-20 | Ab Science | Use of masitinib for the treatment of coronavirus disease 2019 (covid-19) |
CA3201259A1 (en) | 2020-12-16 | 2022-06-23 | Alain Moussy | Masitinib for the treatment of alzheimer's disease |
IL308088A (en) | 2021-05-17 | 2023-12-01 | Ab Science | Mestitinib for the treatment of castrate-resistant prostate cancer |
CN115850258A (zh) * | 2022-12-27 | 2023-03-28 | 东北林业大学 | 一种马赛替尼的合成方法 |
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DK1401413T3 (da) | 2001-06-29 | 2007-03-26 | Ab Science | Anvendelse af tyrosinkinaseinhibitorer til behandling af allergiske sygdomme |
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JP2005500041A (ja) | 2001-06-29 | 2005-01-06 | アブ サイエンス | 強力で選択的かつ非毒性のc−kit阻害剤 |
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WO2003039550A1 (en) | 2001-09-20 | 2003-05-15 | Ab Science | Use of tyrosine kinase inhibitors for whitening human skin and treating melanocyte dysfunction associated diseases |
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CN100491374C (zh) * | 2002-08-02 | 2009-05-27 | Ab科学公司 | 2-(3-氨基芳基)氨基-4-芳基-噻唑及其作为c-kit抑制剂的应用 |
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AU2004212490B2 (en) * | 2003-02-10 | 2008-05-15 | Amgen Inc. | Vanilloid receptor ligands and their use in treatments |
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2008
- 2008-02-13 JP JP2009549405A patent/JP5568312B2/ja active Active
- 2008-02-13 ES ES11170200.7T patent/ES2522169T3/es active Active
- 2008-02-13 CA CA2970628A patent/CA2970628C/en active Active
- 2008-02-13 EP EP08708929A patent/EP2118099B1/en active Active
- 2008-02-13 AT AT08708929T patent/ATE515506T1/de not_active IP Right Cessation
- 2008-02-13 CN CN201310141370.2A patent/CN103342701B/zh active Active
- 2008-02-13 CN CN2008800049044A patent/CN101657446B/zh active Active
- 2008-02-13 SI SI200831294T patent/SI2366703T1/sl unknown
- 2008-02-13 RU RU2009132186/04A patent/RU2456285C2/ru active
- 2008-02-13 AU AU2008214679A patent/AU2008214679A1/en not_active Abandoned
- 2008-02-13 BR BRPI0807626-0A patent/BRPI0807626B1/pt active IP Right Grant
- 2008-02-13 KR KR1020097016822A patent/KR20090110851A/ko not_active Application Discontinuation
- 2008-02-13 NZ NZ578944A patent/NZ578944A/en unknown
- 2008-02-13 SI SI200830399T patent/SI2118099T1/sl unknown
- 2008-02-13 PL PL11170200T patent/PL2366703T3/pl unknown
- 2008-02-13 CA CA2677586A patent/CA2677586C/en active Active
- 2008-02-13 AR ARP080100620A patent/AR065337A1/es active IP Right Grant
- 2008-02-13 PL PL08708929T patent/PL2118099T3/pl unknown
- 2008-02-13 MX MX2009008665A patent/MX2009008665A/es active IP Right Grant
- 2008-02-13 EP EP11170200.7A patent/EP2366703B1/en active Active
- 2008-02-13 US US12/526,827 patent/US8153792B2/en active Active
- 2008-02-13 ES ES08708929T patent/ES2369617T3/es active Active
- 2008-02-13 TW TW097105021A patent/TWI406862B/zh active
- 2008-02-13 WO PCT/EP2008/051704 patent/WO2008098949A2/en active Application Filing
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2009
- 2009-08-10 IL IL200320A patent/IL200320A0/en unknown
- 2009-08-11 TN TNP2009000342A patent/TN2009000342A1/fr unknown
- 2009-08-11 MA MA32161A patent/MA31180B1/fr unknown
- 2009-08-28 ZA ZA2009/05981A patent/ZA200905981B/en unknown
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2011
- 2011-10-05 HR HR20110709T patent/HRP20110709T1/hr unknown
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2012
- 2012-03-08 US US13/415,249 patent/US8492545B2/en active Active
- 2012-04-12 RU RU2012114234/04A patent/RU2491286C1/ru active
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2013
- 2013-05-10 US US13/891,639 patent/US8940894B2/en active Active
- 2013-05-30 JP JP2013113789A patent/JP5784073B2/ja active Active
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2014
- 2014-10-15 HR HRP20140986AT patent/HRP20140986T1/hr unknown
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