RU2008129821A - Гетероциклические производные в качестве модуляторов ионных каналов - Google Patents
Гетероциклические производные в качестве модуляторов ионных каналов Download PDFInfo
- Publication number
- RU2008129821A RU2008129821A RU2008129821/04A RU2008129821A RU2008129821A RU 2008129821 A RU2008129821 A RU 2008129821A RU 2008129821/04 A RU2008129821/04 A RU 2008129821/04A RU 2008129821 A RU2008129821 A RU 2008129821A RU 2008129821 A RU2008129821 A RU 2008129821A
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- 125000001931 aliphatic group Chemical group 0.000 claims abstract 58
- 150000001875 compounds Chemical class 0.000 claims abstract 58
- 125000001424 substituent group Chemical group 0.000 claims abstract 47
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 19
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 14
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 13
- 125000005842 heteroatom Chemical group 0.000 claims abstract 12
- 125000001118 alkylidene group Chemical group 0.000 claims abstract 9
- 229920006395 saturated elastomer Polymers 0.000 claims abstract 7
- 125000003118 aryl group Chemical group 0.000 claims abstract 5
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims abstract 5
- 125000002619 bicyclic group Chemical group 0.000 claims abstract 3
- 125000004122 cyclic group Chemical group 0.000 claims abstract 3
- 125000002950 monocyclic group Chemical group 0.000 claims abstract 3
- 150000003839 salts Chemical class 0.000 claims abstract 2
- 229910052736 halogen Inorganic materials 0.000 claims 42
- 150000002367 halogens Chemical class 0.000 claims 42
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 15
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 208000002193 Pain Diseases 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- -1 1,2-methylenedioxy Chemical group 0.000 claims 4
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 208000004296 neuralgia Diseases 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- 208000007514 Herpes zoster Diseases 0.000 claims 2
- 208000019695 Migraine disease Diseases 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 230000001154 acute effect Effects 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 206010027599 migraine Diseases 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 1
- 206010002383 Angina Pectoris Diseases 0.000 claims 1
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- 206010019233 Headaches Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 1
- 208000019430 Motor disease Diseases 0.000 claims 1
- 206010061533 Myotonia Diseases 0.000 claims 1
- 206010028836 Neck pain Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000001294 Nociceptive Pain Diseases 0.000 claims 1
- 206010033557 Palpitations Diseases 0.000 claims 1
- 208000004550 Postoperative Pain Diseases 0.000 claims 1
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- 208000008765 Sciatica Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010046543 Urinary incontinence Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004391 aryl sulfonyl group Chemical group 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- JKJWYKGYGWOAHT-UHFFFAOYSA-N bis(prop-2-enyl) carbonate Chemical compound C=CCOC(=O)OCC=C JKJWYKGYGWOAHT-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 206010008118 cerebral infarction Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 208000018912 cluster headache syndrome Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 230000001037 epileptic effect Effects 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000004899 motility Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000015706 neuroendocrine disease Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000000037 tert-butyldiphenylsilyl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1[Si]([H])([*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- ITMCEJHCFYSIIV-UHFFFAOYSA-M triflate Chemical compound [O-]S(=O)(=O)C(F)(F)F ITMCEJHCFYSIIV-UHFFFAOYSA-M 0.000 claims 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 1
- 206010044652 trigeminal neuralgia Diseases 0.000 claims 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 208000009935 visceral pain Diseases 0.000 claims 1
Classifications
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- 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
- C07D417/12—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 linked by a chain containing hetero atoms as chain links
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- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
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| US75292605P | 2005-12-21 | 2005-12-21 | |
| US60/752,926 | 2005-12-21 | ||
| US79118106P | 2006-04-11 | 2006-04-11 | |
| US60/791,181 | 2006-04-11 | ||
| US79979706P | 2006-05-12 | 2006-05-12 | |
| US60/799,797 | 2006-05-12 | ||
| US83944406P | 2006-08-23 | 2006-08-23 | |
| US60/839,444 | 2006-08-23 | ||
| PCT/US2006/048802 WO2007075895A2 (en) | 2005-12-21 | 2006-12-21 | Heterocyclic derivatives as modulators of ion channels |
Publications (1)
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| RU2008129821A true RU2008129821A (ru) | 2010-01-27 |
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| US7615563B2 (en) * | 2003-08-08 | 2009-11-10 | Gonzalez Iii Jesus E | Compositions useful as inhibitors of voltage-gated sodium channels |
| RU2007145434A (ru) * | 2005-05-10 | 2009-06-20 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Бициклические производные в качестве модуляторов ионных каналов |
| US7745629B2 (en) * | 2005-05-16 | 2010-06-29 | Vertex Pharmaceuticals Incorporated | Bicyclic derivatives as modulators of ion channels |
| CN101300253B (zh) * | 2005-09-09 | 2012-08-22 | 沃泰克斯药物股份有限公司 | 作为电压门控离子通道调控剂的二环衍生物 |
| AU2006306367A1 (en) * | 2005-10-21 | 2007-05-03 | Vertex Pharmaceuticals Incorporated | Derivatives for modulation of ion channels |
| CA2687764A1 (en) | 2007-05-25 | 2008-12-04 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| UA101809C2 (uk) | 2007-08-22 | 2013-05-13 | Астразенека Аб | Похідні циклопропіламіду |
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| RU2010123876A (ru) * | 2007-11-13 | 2011-12-20 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Гетероциклические производные в качестве модуляторов ионных каналов |
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| CN101456860B (zh) * | 2007-12-10 | 2011-02-16 | 中国科学院上海药物研究所 | 4-[9-(6-氨基嘌呤基)]-2(s)-羟基丁酸甲酯的制备方法 |
| AU2008345573B2 (en) | 2007-12-20 | 2013-12-19 | Envivo Pharmaceuticals, Inc. | Tetrasubstituted benzenes |
| WO2009089277A2 (en) * | 2008-01-08 | 2009-07-16 | The Trustees Of The University Of Pennsylvania | Rel inhibitors and methods of use thereof |
| DE102008020785B4 (de) | 2008-04-25 | 2021-11-04 | Skw Stickstoffwerke Piesteritz Gmbh | Verwendung von einfachen Derivaten von 5-Amino-1,2,4-thiadiazol zur Hemmung bzw. Steuerung der Nitrifikation |
| WO2009133641A1 (ja) * | 2008-04-30 | 2009-11-05 | シャープ株式会社 | 照明装置、及び表示装置 |
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| EP2307412A2 (en) * | 2008-07-01 | 2011-04-13 | Vertex Pharmaceuticals Incorporated | Heterocyclic derivatives as modulators of ion channels |
| TW201039825A (en) | 2009-02-20 | 2010-11-16 | Astrazeneca Ab | Cyclopropyl amide derivatives 983 |
| KR20130002316A (ko) | 2010-02-18 | 2013-01-07 | 아스트라제네카 아베 | 시클로프로필 벤즈아미드 유도체의 신규 결정질 형태 |
| BR112014010197A2 (pt) * | 2011-10-28 | 2017-04-18 | Merck Sharp & Dohme | composto, composição farmacêutica, método de tratamento de um distúrbio |
| US9624208B2 (en) | 2012-10-26 | 2017-04-18 | Merck Sharp & Dohme Corp. | Benzoxazolinone compounds with selective activity in voltage-gated sodium channels |
| CA2922567A1 (en) * | 2013-08-26 | 2015-03-05 | Purdue Pharma L.P. | Azaspiro[4.5]decane derivatives and use thereof |
| WO2015077905A1 (en) | 2013-11-29 | 2015-06-04 | Merck Sharp & Dohme Corp. | Bicycloamine-substituted-n-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels |
| KR102412146B1 (ko) | 2015-02-11 | 2022-06-22 | 주식회사 아이엔테라퓨틱스 | 소디움 채널 차단제 |
| WO2016177340A1 (zh) * | 2015-05-05 | 2016-11-10 | 上海海雁医药科技有限公司 | 双环取代的苯磺酰胺衍生物、其制法与医药上的用途 |
| TW201718557A (zh) * | 2015-10-08 | 2017-06-01 | 歌林達有限公司 | 經吡唑基取代之四氫吡喃基碸 |
| HUE071358T2 (hu) | 2016-05-20 | 2025-08-28 | Xenon Pharmaceuticals Inc | Benzolszulfonamid vegyületek és terápiás szerként való alkalmazásuk |
| WO2018093694A1 (en) * | 2016-11-17 | 2018-05-24 | Merck Sharp & Dohme Corp. | Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| JP7022751B2 (ja) | 2016-12-09 | 2022-02-18 | ゼノン・ファーマシューティカルズ・インコーポレイテッド | ベンゼンスルホンアミド化合物および治療剤としてのそれらの使用 |
| US20200140383A1 (en) * | 2017-07-03 | 2020-05-07 | Glaxosmithkline Intellectual Property Development Limited | 2-(4-chlorophenoxy)-n-((1 -(2-(4-chlorophenoxy)ethynazetidin-3-yl)methyl)acetamide derivatives and related compounds as atf4 inhibitors for treating cancer and other diseases |
| SG11202011862PA (en) | 2018-06-13 | 2020-12-30 | Xenon Pharmaceuticals Inc | Benzenesulfonamide compounds and their use as therapeutic agents |
| GB201810092D0 (en) | 2018-06-20 | 2018-08-08 | Ctxt Pty Ltd | Compounds |
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| CN112638898B (zh) | 2018-08-31 | 2024-04-09 | 泽农医药公司 | 杂芳基取代的磺酰胺化合物及其作为钠通道抑制剂的用途 |
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| US11034669B2 (en) | 2018-11-30 | 2021-06-15 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| FI3986890T3 (fi) | 2019-06-18 | 2024-01-15 | Pfizer | Bentsisoksatsolisulfonamidijohdannaisia |
| CA3194198A1 (en) * | 2020-09-14 | 2022-03-17 | Genzyme Corporation | Compounds as modulators of bis-phosphoglycerate mutase for the treatment of sickle cell disease |
| PE20250155A1 (es) | 2021-06-14 | 2025-01-22 | Scorpion Therapeutics Inc | Derivados de la urea que pueden ser utilizados para tratar el cancer |
| WO2023028056A1 (en) * | 2021-08-24 | 2023-03-02 | Genentech, Inc. | 3-amino piperidyl sodium channel inhibitors |
| WO2023141432A2 (en) | 2022-01-18 | 2023-07-27 | Maze Therapeutics, Inc. | Apol1 inhibitors and methods of use |
| WO2024249254A2 (en) * | 2023-05-26 | 2024-12-05 | Maze Therapeutics, Inc. | Methods of using apol1 inhibitors |
| CN117326903B (zh) * | 2023-09-27 | 2025-05-02 | 常州大学 | 一种高立体选择性合成n-烷基化吲哚衍生物的方法 |
| WO2025096637A1 (en) * | 2023-10-31 | 2025-05-08 | Xenon Pharmaceuticals Inc. | Substituted aryl sulfonamides for use as sodium channel inhibitors |
| CN117384091B (zh) * | 2023-12-08 | 2024-02-20 | 四川大学华西第二医院 | 一类酰胺衍生物、合成方法及用途 |
| WO2025245351A1 (en) * | 2024-05-22 | 2025-11-27 | Xenon Pharmaceuticals Inc. | Substituted aryl sulfonamides and compositions and uses thereof |
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| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
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| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| TR200000073T2 (tr) * | 1997-07-11 | 2000-06-21 | Smithkline Beecham P.L.C. | 5-HT6 Reseptör antagonistleri olan sülfonamid türevleri ve bunların hazırlanma prosesi |
| SE0001899D0 (sv) * | 2000-05-22 | 2000-05-22 | Pharmacia & Upjohn Ab | New compounds |
| US7615563B2 (en) * | 2003-08-08 | 2009-11-10 | Gonzalez Iii Jesus E | Compositions useful as inhibitors of voltage-gated sodium channels |
| TW200524888A (en) * | 2003-08-08 | 2005-08-01 | Vertex Pharma | Compositions useful as inhibitors of voltage-gated ion channels |
| SE0302570D0 (sv) * | 2003-09-26 | 2003-09-26 | Astrazeneca Ab | Benzimidazole derivatives, compositions containing them, preparation thereof and uses thereof |
| JP4473764B2 (ja) * | 2005-03-31 | 2010-06-02 | タカラベルモント株式会社 | 椅子昇降用油圧装置 |
| RU2007145434A (ru) * | 2005-05-10 | 2009-06-20 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Бициклические производные в качестве модуляторов ионных каналов |
| US7745629B2 (en) * | 2005-05-16 | 2010-06-29 | Vertex Pharmaceuticals Incorporated | Bicyclic derivatives as modulators of ion channels |
| ZA200800191B (en) * | 2005-06-09 | 2009-04-29 | Vertex Pharmaceuicals Inc | Indane derivatives as modulators of ion channels |
| CN101300253B (zh) * | 2005-09-09 | 2012-08-22 | 沃泰克斯药物股份有限公司 | 作为电压门控离子通道调控剂的二环衍生物 |
| EP1934191B1 (en) * | 2005-10-12 | 2012-03-28 | Vertex Pharmaceuticals, Inc. | Biphenyl derivatives as modulators of voltage gated ion channels |
| AU2006306367A1 (en) * | 2005-10-21 | 2007-05-03 | Vertex Pharmaceuticals Incorporated | Derivatives for modulation of ion channels |
| US7994174B2 (en) * | 2007-09-19 | 2011-08-09 | Vertex Pharmaceuticals Incorporated | Pyridyl sulfonamides as modulators of ion channels |
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- 2006-12-21 ZA ZA200805338A patent/ZA200805338B/xx unknown
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- 2006-12-21 RU RU2008129821/04A patent/RU2008129821A/ru not_active Application Discontinuation
- 2006-12-21 EP EP06845951A patent/EP1963281A2/en not_active Withdrawn
- 2006-12-21 EP EP10186698A patent/EP2316829A1/en not_active Withdrawn
- 2006-12-21 NZ NZ569694A patent/NZ569694A/en not_active IP Right Cessation
- 2006-12-21 US US11/643,622 patent/US7799822B2/en not_active Expired - Fee Related
- 2006-12-21 KR KR1020087017835A patent/KR20080081178A/ko not_active Ceased
- 2006-12-21 CN CNA2006800525107A patent/CN101365686A/zh active Pending
- 2006-12-21 TW TW095148248A patent/TW200740803A/zh unknown
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- 2006-12-21 EP EP10186696A patent/EP2308872A1/en not_active Withdrawn
- 2006-12-21 JP JP2008547549A patent/JP2009524591A/ja active Pending
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Also Published As
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| JP2009524591A (ja) | 2009-07-02 |
| US20130035310A1 (en) | 2013-02-07 |
| AU2006331608B2 (en) | 2012-07-05 |
| EP2308872A1 (en) | 2011-04-13 |
| AU2006331608A1 (en) | 2007-07-05 |
| KR20080081178A (ko) | 2008-09-08 |
| SG181209A1 (en) | 2012-06-28 |
| NZ593074A (en) | 2012-04-27 |
| EP2316829A1 (en) | 2011-05-04 |
| US20080027067A1 (en) | 2008-01-31 |
| NZ569694A (en) | 2011-06-30 |
| US8586589B2 (en) | 2013-11-19 |
| ZA200805338B (en) | 2010-03-31 |
| WO2007075895A3 (en) | 2007-11-29 |
| US8309587B2 (en) | 2012-11-13 |
| US20110082117A1 (en) | 2011-04-07 |
| IL192184A0 (en) | 2009-02-11 |
| US20120178713A1 (en) | 2012-07-12 |
| WO2007075895A2 (en) | 2007-07-05 |
| NO20083220L (no) | 2008-09-22 |
| TW200740803A (en) | 2007-11-01 |
| US8163720B2 (en) | 2012-04-24 |
| EP1963281A2 (en) | 2008-09-03 |
| US7799822B2 (en) | 2010-09-21 |
| CA2633653A1 (en) | 2007-07-05 |
| CN101365686A (zh) | 2009-02-11 |
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| FA94 | Acknowledgement of application withdrawn (non-payment of fees) |
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