ZA200508872B - Novel pyridopyrazines and use thereof as kinase modulators - Google Patents
Novel pyridopyrazines and use thereof as kinase modulators Download PDFInfo
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- ZA200508872B ZA200508872B ZA200508872A ZA200508872A ZA200508872B ZA 200508872 B ZA200508872 B ZA 200508872B ZA 200508872 A ZA200508872 A ZA 200508872A ZA 200508872 A ZA200508872 A ZA 200508872A ZA 200508872 B ZA200508872 B ZA 200508872B
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- ZA
- South Africa
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- cycloalkyl
- heterocyclyl
- Prior art date
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- YEYHFKBVNARCNE-UHFFFAOYSA-N pyrido[2,3-b]pyrazine Chemical class N1=CC=NC2=CC=CN=C21 YEYHFKBVNARCNE-UHFFFAOYSA-N 0.000 title claims description 8
- 108091000080 Phosphotransferase Proteins 0.000 title description 16
- 102000020233 phosphotransferase Human genes 0.000 title description 16
- 125000000217 alkyl group Chemical group 0.000 claims description 128
- 125000003118 aryl group Chemical group 0.000 claims description 111
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 90
- XCUAIINAJCDIPM-XVFCMESISA-N N(4)-hydroxycytidine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=NO)C=C1 XCUAIINAJCDIPM-XVFCMESISA-N 0.000 claims description 85
- 125000001072 heteroaryl group Chemical group 0.000 claims description 84
- 125000000623 heterocyclic group Chemical group 0.000 claims description 78
- -1 alkyl radical Chemical class 0.000 claims description 71
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 41
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 31
- 229910052794 bromium Inorganic materials 0.000 claims description 29
- 229910052740 iodine Inorganic materials 0.000 claims description 29
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 28
- 229910052801 chlorine Inorganic materials 0.000 claims description 28
- 229910052731 fluorine Inorganic materials 0.000 claims description 25
- 229910052739 hydrogen Inorganic materials 0.000 claims description 23
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- 239000001257 hydrogen Substances 0.000 claims description 13
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- 229910006069 SO3H Inorganic materials 0.000 claims description 8
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- 238000000034 method Methods 0.000 claims description 8
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- 125000001424 substituent group Chemical group 0.000 claims description 8
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- 125000005213 alkyl heteroaryl group Chemical group 0.000 claims description 7
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- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
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- UDJFFSGCRRMVFH-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine Chemical compound N1=CN=CC2=CC=CN=C21 UDJFFSGCRRMVFH-UHFFFAOYSA-N 0.000 claims description 6
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- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
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- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
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- 125000004365 octenyl group Chemical group C(=CCCCCCC)* 0.000 claims description 2
- 125000005069 octynyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C#C* 0.000 claims description 2
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- 125000001484 phenothiazinyl group Chemical group C1(=CC=CC=2SC3=CC=CC=C3NC12)* 0.000 claims description 2
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- 125000003386 piperidinyl group Chemical group 0.000 claims description 2
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 claims description 2
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims description 2
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims description 2
- 208000037803 restenosis Diseases 0.000 claims description 2
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- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
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- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 2
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Classifications
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
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- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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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
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- 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
-
- 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
-
- 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
-
- 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
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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DE10323345A DE10323345A1 (de) | 2003-05-23 | 2003-05-23 | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
Publications (1)
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ZA200508872B true ZA200508872B (en) | 2006-07-26 |
Family
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Family Applications (2)
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ZA200508872A ZA200508872B (en) | 2003-05-23 | 2005-02-11 | Novel pyridopyrazines and use thereof as kinase modulators |
ZA200508633A ZA200508633B (en) | 2003-05-23 | 2005-10-25 | Novel pyridopyrazines and use thereof as kinase inhibitors |
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ZA200508633A ZA200508633B (en) | 2003-05-23 | 2005-10-25 | Novel pyridopyrazines and use thereof as kinase inhibitors |
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US (3) | US7323468B2 (no) |
EP (1) | EP1628976A1 (no) |
JP (1) | JP2007500195A (no) |
KR (1) | KR20060015283A (no) |
CN (2) | CN1795195B (no) |
AR (1) | AR045685A1 (no) |
AU (1) | AU2004240746B2 (no) |
BR (1) | BRPI0410632A (no) |
CA (1) | CA2524948A1 (no) |
DE (1) | DE10323345A1 (no) |
MX (1) | MXPA05012592A (no) |
NO (1) | NO20056030L (no) |
RS (2) | RS51906B (no) |
RU (1) | RU2005140378A (no) |
TW (1) | TW200504062A (no) |
WO (1) | WO2004104002A1 (no) |
ZA (2) | ZA200508872B (no) |
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MXPA05012645A (es) * | 2003-05-23 | 2006-02-08 | Zentaris Gmbh | Piridopirazinas novedosas y su uso como moduladores de cinasa. |
DE102004022383A1 (de) * | 2004-05-06 | 2005-12-01 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
DE10323345A1 (de) * | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
US20100132790A1 (en) * | 2005-05-09 | 2010-06-03 | Solaris Nanosciences, Inc. | Rechargeable Dye Sensitized Solar Cell |
US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
CN101356173B (zh) * | 2005-11-11 | 2012-10-31 | 阿特纳赞塔里斯有限公司 | 新的吡啶并吡嗪和它们作为激酶调节剂的用途 |
AU2006313701B2 (en) * | 2005-11-11 | 2012-05-31 | Aeterna Zentaris Gmbh | Novel pyridopyrazines and their use as modulators of kinases |
EP1790342A1 (de) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
EP1785423A1 (de) * | 2005-11-11 | 2007-05-16 | Zentaris GmbH | Neue Pyridopyrazine und deren Verwendung als Modulatoren von Kinasen |
EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
EP2508184A1 (en) * | 2011-04-06 | 2012-10-10 | Æterna Zentaris GmbH | Pyridopyrazine derivatives and their use |
WO2012167423A1 (en) * | 2011-06-08 | 2012-12-13 | Hutchison Medipharma Limited | Substituted pyridopyrazines as novel syk inhibitors |
GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
RU2715893C2 (ru) | 2014-03-26 | 2020-03-04 | Астекс Терапьютикс Лтд | Комбинации ингибитора fgfr и ингибитора igf1r |
JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
SI3353177T1 (sl) | 2015-09-23 | 2020-08-31 | Janssen Pharmaceutica Nv | Triciklični heterocikli za zdravljenje raka |
EP3353164B1 (en) | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
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KR20040048411A (ko) * | 2001-09-14 | 2004-06-09 | 메틸진, 인크. | 히스톤 데아세틸라아제의 억제제 |
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JP4394960B2 (ja) | 2002-04-08 | 2010-01-06 | メルク エンド カムパニー インコーポレーテッド | Akt活性阻害薬 |
EP1538907A4 (en) | 2002-07-02 | 2008-12-24 | Southern Res Inst | FTSZ-HEMMER AND ITS USE |
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GB0413953D0 (en) | 2004-06-22 | 2004-07-28 | Syngenta Participations Ag | Chemical compounds |
GB0413955D0 (en) | 2004-06-22 | 2004-07-28 | Syngenta Participations Ag | Chemical compounds |
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JP2006137723A (ja) | 2004-11-15 | 2006-06-01 | Kyowa Hakko Kogyo Co Ltd | スルホンアミド誘導体 |
EP1824828A2 (en) | 2004-12-03 | 2007-08-29 | Peakdale Molecular Limited | Pyridine based compounds useful as intermediates for pharmaceutical or agricultural end-products |
WO2006073938A2 (en) | 2004-12-30 | 2006-07-13 | East Carolina University | Method for the synthesis of 3-substituted indolizine and benzoindolizine compounds |
US20080085901A1 (en) | 2005-01-14 | 2008-04-10 | Neurogen Corporation | Heteroaryl Substituted Quinolin-4-Ylamine Analogues |
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CA2594998A1 (en) | 2005-01-25 | 2006-08-03 | Neurogen Corporation | Substituted pyridazinyl-and pyrimidinyl-quinolin-4-ylamine analogues |
JP2008528587A (ja) | 2005-01-25 | 2008-07-31 | グラクソ グループ リミテッド | 抗菌剤 |
US7605169B2 (en) | 2005-01-25 | 2009-10-20 | Glaxo Group Limited | Antibacterial agents |
EP1846416A4 (en) | 2005-01-25 | 2009-07-01 | Glaxo Group Ltd | ANTIBACTERIAL AGENTS |
WO2006128129A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating cancer |
WO2006128172A2 (en) | 2005-05-26 | 2006-11-30 | Synta Pharmaceuticals Corp. | Method for treating b cell regulated autoimmune disorders |
-
2003
- 2003-05-23 DE DE10323345A patent/DE10323345A1/de not_active Withdrawn
-
2004
- 2004-05-19 AU AU2004240746A patent/AU2004240746B2/en not_active Ceased
- 2004-05-19 RU RU2005140378/04A patent/RU2005140378A/ru not_active Application Discontinuation
- 2004-05-19 RS YU20050876A patent/RS51906B/sr unknown
- 2004-05-19 CN CN2004800142149A patent/CN1795195B/zh not_active Expired - Fee Related
- 2004-05-19 CA CA002524948A patent/CA2524948A1/en not_active Abandoned
- 2004-05-19 MX MXPA05012592A patent/MXPA05012592A/es active IP Right Grant
- 2004-05-19 WO PCT/EP2004/005379 patent/WO2004104002A1/de not_active Application Discontinuation
- 2004-05-19 EP EP04733782A patent/EP1628976A1/de not_active Withdrawn
- 2004-05-19 CN CNA2004800142045A patent/CN1795194A/zh active Pending
- 2004-05-19 RS YUP-2005/0864A patent/RS20050864A/sr unknown
- 2004-05-19 JP JP2006529871A patent/JP2007500195A/ja not_active Withdrawn
- 2004-05-19 KR KR1020057022237A patent/KR20060015283A/ko not_active Application Discontinuation
- 2004-05-19 BR BRPI0410632-6A patent/BRPI0410632A/pt not_active IP Right Cessation
- 2004-05-20 TW TW093114323A patent/TW200504062A/zh unknown
- 2004-05-21 AR ARP040101771A patent/AR045685A1/es not_active Application Discontinuation
- 2004-05-21 US US10/851,966 patent/US7323468B2/en not_active Expired - Fee Related
-
2005
- 2005-02-11 ZA ZA200508872A patent/ZA200508872B/en unknown
- 2005-10-25 ZA ZA200508633A patent/ZA200508633B/en unknown
- 2005-12-19 NO NO20056030A patent/NO20056030L/no unknown
-
2007
- 2007-07-05 US US11/825,200 patent/US8193186B2/en not_active Expired - Fee Related
- 2007-11-12 US US11/985,031 patent/US20080113991A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
EP1628976A1 (de) | 2006-03-01 |
ZA200508633B (en) | 2006-07-26 |
AR045685A1 (es) | 2005-11-09 |
CA2524948A1 (en) | 2004-12-02 |
KR20060015283A (ko) | 2006-02-16 |
US8193186B2 (en) | 2012-06-05 |
AU2004240746B2 (en) | 2007-05-31 |
RS51906B (sr) | 2012-02-29 |
RS20050864A (en) | 2008-04-04 |
US20080113991A1 (en) | 2008-05-15 |
TW200504062A (en) | 2005-02-01 |
RU2005140378A (ru) | 2007-06-27 |
US7323468B2 (en) | 2008-01-29 |
NO20056030L (no) | 2006-02-15 |
CN1795195A (zh) | 2006-06-28 |
CN1795194A (zh) | 2006-06-28 |
BRPI0410632A (pt) | 2006-06-13 |
JP2007500195A (ja) | 2007-01-11 |
AU2004240746A1 (en) | 2004-12-02 |
MXPA05012592A (es) | 2006-02-08 |
RS20050876A (en) | 2008-04-04 |
CN1795195B (zh) | 2010-04-21 |
US20050032803A1 (en) | 2005-02-10 |
WO2004104002A1 (de) | 2004-12-02 |
US20070275972A1 (en) | 2007-11-29 |
DE10323345A1 (de) | 2004-12-16 |
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