ME02815B - Biciklična heterociklična jedinjenja kao inhibitori protein tirozin kinaze - Google Patents
Biciklična heterociklična jedinjenja kao inhibitori protein tirozin kinazeInfo
- Publication number
- ME02815B ME02815B MEP-2016-141A MEP14116A ME02815B ME 02815 B ME02815 B ME 02815B ME P14116 A MEP14116 A ME P14116A ME 02815 B ME02815 B ME 02815B
- Authority
- ME
- Montenegro
- Prior art keywords
- alkyl
- compound according
- heterocyclyl
- groups
- optionally substituted
- Prior art date
Links
- 125000002618 bicyclic heterocycle group Chemical group 0.000 title 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- 239000001257 hydrogen Substances 0.000 claims 4
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 3
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- -1 triazinol Chemical group 0.000 claims 1
Classifications
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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
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- 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
- A61P7/06—Antianaemics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs 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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Otolaryngology (AREA)
- Obesity (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
Claims (12)
1. Jedinjenje formule (1): pri čemupredstavlja jednostruku ili dvostruku vezu, tako da je najmanje jedna veza u 5 članom prstenastom sistemu dvostruka veza;prsten A može biti opciono supstituisan sa 1, 2 ili 3 Ra grupe; B predstavlja -heterociklil grupu gde navedena heterociklil grupa može biti opciono supstituisane sa 1, 2 ili 3 Ra grupe;Ra predstavlja halogen, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3 – 8 cikloalkil, C3-8 cikloalkenil, -ORX, -O-(CH2)n-ORX, haloC1•6 alkil, haloC1-6 alkoksi, C1-6 alkanol, =0, =S, nitro, Si(Rx)4’’ (CH2)s-CN, -S-Rx, -SO-Rx, -S02-Rx, -CORx, -(CRxRy)s-COORz, -(CH2)s-CONRxRy, - (CH2)s-NRxRy, -(CH2)s·NRxCORy, -(CH2)s-NRxSO2-RY, - (CH2)s-NH-SO2-NRxRy, OCONRxRy, - (CH2)s-NRxCO2RY,-O-(CH2)s CRxRy-(CH2)t -ORz ili -(CH2)S-SO2NRxRy grupe;RX, RY i RZ nezavisno predstavljaju vodonik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6alkanol, hidroksi, C1-6 alkoksi, halo C1-6 alkil, -CO-(CH2)n-C1-6 alkoksi, C3-8 cikloalkil ili C3-8 cikloalkenil;R7 i R8 nezavisno predstavljaju vodonik, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C3-8 cikloalkil, C3-8 cikloalkenil, aril, heterociklil ili R7 i R8 zajedno sa atomom azota za koji su pričvršćeni mogu obrazovati heterociklil prsten koji sadrži azot, pri čemu pomenuti C1-6 alkil, aril i heterociklil može biti opciono supstituisan sa 1, 2 ili 3 Rb grupe;R1 i Rb nezavisno predstavlja Ra grupu ili -Y-karbocikličnu ili –Z heterociklil grupu, pri čemu pomenute karbociklične i heterociklil grupe mogu biti opciono supstituisane sa 1, 2 ili 3 Ra grupe; Y i Z nezavisno predstavljaju vezu, -CO-(CH2)S -, -COO-, -(CH2)n-, -NRx-(CH2)S -, -(CH2)S NRx-, -CONRx-, -NRxCO-, -SO2NRx-, -NRxSO 2-, -NRxCONRY-, -NRxCSNRY-, - O-(CH2)s ' -(CH2)s-O-, -S-, -SO- ili -(CH2)s-SO2-;n predstavljaju ceo broj od 1-4;s i t nezavisno predstavljaju ceo broj od 0-4;q nezavisno predstavljaju ceo broj od 0-2;ili njegova farmaceutski prihvatljiva so ili solvat.
2.Jedinjenje prema zahtjevu 1, pri čemu B predstavlja aromaticnu ili nearomaticnu heterociklil grupu; Ra predstavlja halogen, C1-6 alkil, C2.6 alkenil, C2.6 alkinil, C3-e cikloalkil, C3•8 cikloalkenil, - ORx, -O-(CH2)n-0Rx, haloC 1.6 alkil, haloC1. 6 alkoksi, C1. 6 alkanol, =0, =S, nitro, -(CH2)s-CN, -S-Rx, -SO-RX, -S02-Rx, -CORx, -(CRxRy)s-COORz, -(CH2)s-CONRxRy, -(CH2)s-NRxRy, - (CH2)s-NRxCORY, -(CH2)s-NRxS02-RY, -OCON-RxRy, - (CH2)s-NRxC02RY, -O-(CH2)s-CRxRy (CH2)t-ORz ili -(CH2)s-S02NRxRy grupe; Yi Z nezavisno predstavljaju vezu, -CO-, CH2-. -(CH2)2-. -CH2h-. - O-(CH2)s ili NH-(CH2)n--
3.Jedinjenje prema zahtjevu 2 pri čemu heterociklil grupa je 5 ili 6 člana monociklična heterociklil grupa.
4.Jedinjenje prema zahtjevu 3 pri čemu heterociklil grupa je piridil, pirazinil, triazinol, oksadiazolil, imidazolil ili tiadiazolil.
5.Jedinjenje prema zahtjevu 4 pri čemu heterociklil grupa je tiadiazolil.
6.Jedinjenje prema bilo kom od predhodnih zahtjeva pri čemu q predstavlja O.
7.Jedinjenje prema bilo kom od predhodnih zahtjeva pri cemu R7 i Re zajedno predstavljaju· vodonik ili C1-6 alkil; ili jedan od R7 i Re predstavlja vodonik i drugi predstavlja C1•6 alkil (opciono supstituisan sa -ORx grupom), C3-e cikloalkil ili heterociklil.
8.Jedinjenje prema bilo kom od predhodnih zahtjeva 1 - 6, pri čemu R 7 i Re zajedno sa atomom azota za koji su pričvršćeni obrazuju heterociklil prsten opciono supstituisan sa 1, 2 ,_ ili 3 Rb grupama.
9. Jedinjenje prema bilo kom od prethodnih zahtjeva koje ima sledeći prstenasti sistem:
10. Farmaceutska kompozicija koja sadrži jedinjenje formule (l) prema bilo kom od zahtjeva 1 do 9.
11.Jedinjenje prema bilo kom od zahtjeva 1 do 9 za primenu u terapiji.
12.Jedinjenje prema bilo kom od zahtjeva 1 do 9 za primjenu u profilaksi ili liječenju kancera.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97958907P | 2007-10-12 | 2007-10-12 | |
| GBGB0720038.9A GB0720038D0 (en) | 2007-10-12 | 2007-10-12 | New compounds |
| US6117208P | 2008-06-13 | 2008-06-13 | |
| EP08806575.0A EP2203449B1 (en) | 2007-10-12 | 2008-10-10 | Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors |
| PCT/GB2008/003439 WO2009047522A1 (en) | 2007-10-12 | 2008-10-10 | Bicyclic heterocyclic compounds as protein tyrosine kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ME02815B true ME02815B (me) | 2018-01-20 |
Family
ID=38788130
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MEP-2016-141A ME02815B (me) | 2007-10-12 | 2008-10-10 | Biciklična heterociklična jedinjenja kao inhibitori protein tirozin kinaze |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US8071614B2 (me) |
| EP (1) | EP2203449B1 (me) |
| JP (1) | JP5562858B2 (me) |
| AU (1) | AU2008309342C1 (me) |
| CA (1) | CA2701868C (me) |
| CY (1) | CY1117820T1 (me) |
| ES (1) | ES2585352T3 (me) |
| GB (1) | GB0720038D0 (me) |
| HR (1) | HRP20160852T1 (me) |
| HU (1) | HUE028999T2 (me) |
| ME (1) | ME02815B (me) |
| PL (1) | PL2203449T3 (me) |
| PT (1) | PT2203449T (me) |
| RS (1) | RS55045B1 (me) |
| SI (1) | SI2203449T1 (me) |
| WO (1) | WO2009047522A1 (me) |
Families Citing this family (59)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2114941B1 (en) | 2006-12-22 | 2015-03-25 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| JP5442449B2 (ja) | 2006-12-22 | 2014-03-12 | アステックス、セラピューティックス、リミテッド | 新規化合物 |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| GB0906470D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| LT3495367T (lt) | 2012-06-13 | 2021-02-25 | Incyte Holdings Corporation | Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| JP2016501203A (ja) | 2012-11-20 | 2016-01-18 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | インドールアミン２，３−ジオキシゲナーゼの阻害剤として有用な化合物 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| CA2907243C (en) | 2013-03-15 | 2021-12-28 | Celgene Avilomics Research, Inc. | Substituted dihydropyrimidopyrimidinone compounds and pharmaceutical compositions thereof use fgfr4 inhibitor |
| US9321786B2 (en) | 2013-03-15 | 2016-04-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| JP6576325B2 (ja) | 2013-03-15 | 2019-09-18 | セルジーン シーエーアール エルエルシー | ヘテロアリール化合物およびそれらの使用 |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| MX369646B (es) | 2014-08-18 | 2019-11-15 | Eisai R&D Man Co Ltd | Sal de derivado de piridina monociclico y su cristal. |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| SG11201706287PA (en) | 2015-02-20 | 2017-09-28 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
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| PT2203449T (pt) | 2016-08-02 |
| WO2009047522A1 (en) | 2009-04-16 |
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| EP2203449A1 (en) | 2010-07-07 |
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| ES2585352T3 (es) | 2016-10-05 |
| US8859582B2 (en) | 2014-10-14 |
| HRP20160852T1 (hr) | 2016-09-23 |
| AU2008309342B2 (en) | 2014-04-24 |
| AU2008309342A1 (en) | 2009-04-16 |
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| US8071614B2 (en) | 2011-12-06 |
| CY1117820T1 (el) | 2017-05-17 |
| SI2203449T1 (sl) | 2016-10-28 |
| GB0720038D0 (en) | 2007-11-21 |
| JP5562858B2 (ja) | 2014-07-30 |
| CA2701868A1 (en) | 2009-04-16 |
| HUE028999T2 (en) | 2017-02-28 |
| PL2203449T3 (pl) | 2017-03-31 |
| CA2701868C (en) | 2016-07-19 |
| RS55045B1 (sr) | 2016-12-30 |
| US20120035152A1 (en) | 2012-02-09 |
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