HRP20150225T1 - Derivati acilbenzena - Google Patents

Derivati acilbenzena Download PDF

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HRP20150225T1
HRP20150225T1 HRP20150225TT HRP20150225T HRP20150225T1 HR P20150225 T1 HRP20150225 T1 HR P20150225T1 HR P20150225T T HRP20150225T T HR P20150225TT HR P20150225 T HRP20150225 T HR P20150225T HR P20150225 T1 HRP20150225 T1 HR P20150225T1
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group
fluoro
hydroxy
oxadiazol
benzamide
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HRP20150225TT
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English (en)
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Shigeo Yamanoi
Takahiro Katagiri
Hidenori Namiki
Madoka Hatta
Koji Matsumoto
Kanako Takahashi
Tomomi Yoshitomi
Yuichi Ochiai
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Daiichi Sankyo Company, Limited
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Publication of HRP20150225T1 publication Critical patent/HRP20150225T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/12Ophthalmic agents for cataracts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Emergency Medicine (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (15)

1. Spoj predstavljen općom formulom (I): [Kemijska formula 1] [image] naznačen time, što R1 predstavlja neka hidroksi C1-C6 alkil grupa ili neka hidroksi C3-C6 cikloalkil grupa, od kojih svaka može biti supstituirana sa 1 do 3 supstituenta koji se biraju iz grupe supstituenata α, a subgrupu supstituenata α čine hidroksilna grupa i karbamoil grupa, R2 predstavlja metil grupa ili etil grupa, R3 predstavlja neka C1-C6 alkil grupa ili neka C3-C6 cikloalkil grupa, od kojih svaka može biti supstituirana sa 1 to 3 atoma halogena, i R4 predstavlja neki atom halogena; ili neka njegova farmaceutski prihvatljiva sol.
2. Spoj prema Zahtjevu 1, naznačen time, što R1 predstavlja neka hidroksi C1-C3 alkil grupa ili neka hidroksi C3-C4 cikloalkil grupa, od kojih svaka može biti supstituirana sa 1 do 3 supstituenta koji se biraju iz grupe supstituenata α.
3. Spoj prema Zahtjevu 1, naznačen time, što R1 predstavlja hidroksietil grupa, hidroksipropil grupa, hidroksiizopropil grupa ili hidroksiciklopentil grupa, od kojih svaka može biti supstituirana sa jednim substituentom koji se bira iz grupe supstituenata α.
4. Spoj prema bilo kojem od Zahtjeva 1 do 3, naznačen time, što R3 predstavlja neka C1-C4 alkil grupa ili neka C3-C4 cikloalkil grupa, od kojih svaka može biti supstituirana sa 1 do 3 atoma halogena.
5. Spoj prema bilo kojem od Zahtjeva 1 do 3, naznačen time, što R3 predstavlja izopropil grupa, terc-butil grupa, ciklopropil grupa ili ciklobutil grupa, od kojih svaka može biti supstituirana sa jednim atomom halogena.
6. Spoj prema bilo kojem od Zahtjeva 1 do 5, naznačen time, što R4 predstavlja atom fluora.
7. Spoj prema Zahtjevu 1, koje se bira iz grupe koju čine slijedeći spojevi: 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-N-[(2S)-2,3-dihidroksipropil]-2-fluoro benzamid; N-[(1S)-2-аmino-1-(hidroksimetil)-2-oksoеtil]-4-(5-{(1R)-1-[4-(ciklopropilkarbonil)-fenoksi]propil}-1,2,4-oksadazol-3-il)-2-fluorobenzamid; 4-((5-{(1R]-1-[4-(ciklopropilkarbonil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-[(1R)-2-hidroksi-1-metiletil]benzamid; 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N- [(1S)-2-hidroksi-1-metiletil]benzamid; 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-[(2R)-2,3-dihidroksipropil]-2-fluorobenzamid; 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N- [2-hidroksi-1-(hidroksimetil)etil]benzamid; 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-[(1S)-2-hidroksi-1-metiletil]benzamid; 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]etil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-[(1R,2R)-2-hidroksiciklopentil]benzamid; 4-((5-{(1R)-1-[9-(ciklopropilkarbonil)fenoksi]etil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-(1R)-2- hidroksi-1-metiletil]benzamid; 4-((5-{(1R)-1-[4-(ciklopropilkarbonil)fenoksi]etil}-1,2,4-oxadiazol-3-il)-2-fluоro-N-[(1S,2S)-2-hidroksiciklopentil]benzamid; 4-((5-[(1R]-1-[4-(2,2-dimetilpropanoil)fenoksi]propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-[2-hidroksi-1-(hidroksimetil)etil]benzamid; 4-((5-{(1R)-1-[4-(ciklobutilkarbonil)fenoksi)propil}-1,2,4-oksadiazol-3-il)-2-fluoro-N-[2-hidroksi-1-(hidroksimetil)etil]benzamid; 2-fluoro-4-{5-[(1R)-1-(4-[(1-fluorociklopropil)karbonil]fenoksi}propil]-1,2,4-oksadiаzol-3- il]-N-[2-hidroksi-1-(hidroksimetil)etil]benzamid; 2-fluoro-N-[(1R)-2-hidroksi-1-metiletil]-4-{5-[(1R)-1-(4-izobutirilfenoksi)propil]-1,2,4- oksadiazol-3-il]benzamid; i 2-fluoro-N-[2-hidroksi-1-(hidroksimetil)etil]-4-{5-[(1R)-1-(izobutirilfenoksi)propil]-1,2,9-oksadiazol-3-il]benzamid.
8. Farmaceutska kompozicija, naznačena time, što sadrži kao aktivni sastojak spoj prema bilo kojem od Zahtjeva 1 do 7, ili neku njegovu farmaceutski prihvatljivu sol.
9. Uporaba farmaceutske kompozicije prema Zahtjevu 8 za tretiranje tipa 1 dijabetesa, tipa 2 dijabetesa ili debljine.
10. Uporaba farmaceutske kompozicije prema Zahtjevu 8 za zaštitu β-stanica ili pankreasa.
11. Uporaba spoja prema bilo kojem od Zahtjeva 1 do 7, ili neke njegove farmaceutski prihvatljive soli, za dobijanje farmaceutske kompozicije.
12. Uporaba prema Zahtjevu 11, gdje je ta farmaceutska kompozicija za tretiranje tipa 1 dijabetesa, tipa 2 dijabetesa ili debljine.
13. Uporaba prema Zahtjevu 11, gdje je ta farmaceutska kompozicija za zaštitu stanica ili pankreasa.
14. Uporaba nekog spoja prema bilo kojem od Zahtjeva 1 do 7 u tretmanu tipa 1 dijabetesa, tipa 2 dijabetesa ili debljine.
15. Uporaba nekog spoja prema bilo kojem od Zahtjeva 1 do 7 za zaštitu β-stanica ili pankreasa.
HRP20150225TT 2010-10-14 2015-02-26 Derivati acilbenzena HRP20150225T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
JP2010231471 2010-10-14
JP2011022325 2011-02-04
EP11832583.6A EP2628733B1 (en) 2010-10-14 2011-10-13 Acylbenzene derivative
PCT/JP2011/073489 WO2012050151A1 (ja) 2010-10-14 2011-10-13 アシルベンゼン誘導体

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HRP20150225T1 true HRP20150225T1 (hr) 2015-06-19

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US (1) US8722711B2 (hr)
EP (1) EP2628733B1 (hr)
JP (2) JP5069813B2 (hr)
KR (1) KR101829086B1 (hr)
CN (1) CN103249726B (hr)
AU (1) AU2011314712B2 (hr)
BR (1) BR112013009043B8 (hr)
CA (1) CA2814628C (hr)
CO (1) CO6771403A2 (hr)
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DK (1) DK2628733T3 (hr)
ES (1) ES2532706T3 (hr)
HK (1) HK1185082A1 (hr)
HR (1) HRP20150225T1 (hr)
IL (1) IL225724A (hr)
MX (1) MX2013004176A (hr)
MY (1) MY160300A (hr)
NZ (1) NZ610145A (hr)
PL (1) PL2628733T3 (hr)
PT (1) PT2628733E (hr)
RS (1) RS53965B1 (hr)
RU (1) RU2585765C2 (hr)
SG (1) SG189320A1 (hr)
SI (1) SI2628733T1 (hr)
SM (1) SMT201500067B (hr)
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BR112014001767A2 (pt) 2011-07-29 2017-02-14 Daiichi Sankyo Co Ltd composto, composição farmaccêutica, uso de um composto, e, método para o tratamento de uma doença
WO2013108800A1 (ja) 2012-01-18 2013-07-25 第一三共株式会社 置換フェニルアゾール誘導体
JP2017119628A (ja) * 2014-05-09 2017-07-06 日産化学工業株式会社 置換アゾール化合物及び糖尿病治療薬
WO2017104782A1 (ja) * 2015-12-17 2017-06-22 第一三共株式会社 オキサジアゾール化合物の製造方法
TW201731506A (zh) * 2016-01-19 2017-09-16 第一三共股份有限公司 糖尿病治療劑之倂用

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JPWO2012050151A1 (ja) 2014-02-24
JP5069813B2 (ja) 2012-11-07
SG189320A1 (en) 2013-05-31
PL2628733T3 (pl) 2015-05-29
KR101829086B1 (ko) 2018-02-13
EP2628733B1 (en) 2014-12-24
RS53965B1 (en) 2015-08-31
CO6771403A2 (es) 2013-10-15
CN103249726B (zh) 2015-01-07
IL225724A0 (en) 2013-06-27
EP2628733A4 (en) 2014-02-26
JP2012224640A (ja) 2012-11-15
ES2532706T3 (es) 2015-03-31
BR112013009043B8 (pt) 2019-09-17
CN103249726A (zh) 2013-08-14
CA2814628C (en) 2015-06-16
TWI487699B (zh) 2015-06-11
SI2628733T1 (sl) 2015-10-30
IL225724A (en) 2015-10-29
MX2013004176A (es) 2013-10-25
RU2013121816A (ru) 2014-11-20
WO2012050151A1 (ja) 2012-04-19
AU2011314712A1 (en) 2013-05-02
NZ610145A (en) 2015-02-27
KR20130099094A (ko) 2013-09-05
EP2628733A1 (en) 2013-08-21
MY160300A (en) 2017-02-28
CY1116303T1 (el) 2017-02-08
US8722711B2 (en) 2014-05-13
BR112013009043A2 (pt) 2016-07-26
US20130217733A1 (en) 2013-08-22
RU2585765C2 (ru) 2016-06-10
DK2628733T3 (en) 2015-03-30
SMT201500067B (it) 2015-05-05
PT2628733E (pt) 2015-03-24
TW201305121A (zh) 2013-02-01
HK1185082A1 (en) 2014-02-07
JP5869985B2 (ja) 2016-02-24
BR112013009043B1 (pt) 2019-06-18
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CA2814628A1 (en) 2012-04-19

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