UA80131C2 - Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions - Google Patents
Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions Download PDFInfo
- Publication number
- UA80131C2 UA80131C2 UA20041209867A UA20041209867A UA80131C2 UA 80131 C2 UA80131 C2 UA 80131C2 UA 20041209867 A UA20041209867 A UA 20041209867A UA 20041209867 A UA20041209867 A UA 20041209867A UA 80131 C2 UA80131 C2 UA 80131C2
- Authority
- UA
- Ukraine
- Prior art keywords
- methyl
- sulfonyl
- thiophene
- differs
- methylsulfanyl
- Prior art date
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- 238000000034 method Methods 0.000 title claims abstract description 121
- 230000001404 mediated effect Effects 0.000 title claims abstract description 22
- 230000000295 complement effect Effects 0.000 title claims description 27
- 201000010099 disease Diseases 0.000 title claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims description 20
- 239000000203 mixture Substances 0.000 title description 92
- QSELGEUCFNFITD-UHFFFAOYSA-N thiophene-2-carboximidamide Chemical class NC(=N)C1=CC=CS1 QSELGEUCFNFITD-UHFFFAOYSA-N 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims abstract description 340
- 238000011282 treatment Methods 0.000 claims abstract description 76
- 241000124008 Mammalia Species 0.000 claims abstract description 40
- 230000024203 complement activation Effects 0.000 claims abstract description 26
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- 208000024891 symptom Diseases 0.000 claims abstract description 9
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- -1 benzylthio Chemical group 0.000 claims description 493
- 125000000217 alkyl group Chemical group 0.000 claims description 94
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 claims description 88
- 229910052739 hydrogen Inorganic materials 0.000 claims description 87
- 239000001257 hydrogen Substances 0.000 claims description 86
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 58
- 150000002431 hydrogen Chemical class 0.000 claims description 55
- 229910052736 halogen Inorganic materials 0.000 claims description 47
- 150000002367 halogens Chemical class 0.000 claims description 44
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 33
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 32
- 125000003545 alkoxy group Chemical group 0.000 claims description 28
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 27
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- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 20
- 125000003282 alkyl amino group Chemical group 0.000 claims description 19
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 19
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 19
- 210000000056 organ Anatomy 0.000 claims description 19
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- 125000003342 alkenyl group Chemical group 0.000 claims description 16
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 16
- 230000000694 effects Effects 0.000 claims description 16
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- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims description 14
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 14
- 125000002757 morpholinyl group Chemical group 0.000 claims description 14
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims description 13
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- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims description 13
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- 125000004076 pyridyl group Chemical group 0.000 claims description 12
- XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 0.000 claims description 11
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims description 11
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- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 10
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- 125000004093 cyano group Chemical group *C#N 0.000 claims description 8
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
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- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims description 6
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims description 6
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims description 6
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- 125000003373 pyrazinyl group Chemical group 0.000 claims description 6
- 125000004343 1-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C([H])([H])[H] 0.000 claims description 5
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- 238000010322 bone marrow transplantation Methods 0.000 claims description 5
- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 5
- 238000001631 haemodialysis Methods 0.000 claims description 5
- 230000000322 hemodialysis Effects 0.000 claims description 5
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims description 5
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- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims description 4
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- ZYHQGITXIJDDKC-UHFFFAOYSA-N 2-[2-(2-aminophenyl)ethyl]aniline Chemical group NC1=CC=CC=C1CCC1=CC=CC=C1N ZYHQGITXIJDDKC-UHFFFAOYSA-N 0.000 claims description 3
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Classifications
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/22—Radicals substituted by doubly bound hetero atoms, or by two hetero atoms other than halogen singly bound to the same carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
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- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
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- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
- C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
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Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
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US38313002P | 2002-05-28 | 2002-05-28 | |
PCT/US2003/016888 WO2003099805A1 (en) | 2002-05-28 | 2003-05-28 | Novel thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions |
Publications (1)
Publication Number | Publication Date |
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UA80131C2 true UA80131C2 (en) | 2007-08-27 |
Family
ID=29584510
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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UA20041209867A UA80131C2 (en) | 2002-05-28 | 2003-05-28 | Thiophene amidines, compositions thereof, and methods of treating complement-mediated diseases and conditions |
Country Status (23)
Country | Link |
---|---|
US (2) | US7138530B2 (ru) |
EP (1) | EP1549632A4 (ru) |
JP (1) | JP2005538953A (ru) |
KR (1) | KR20050009720A (ru) |
CN (1) | CN100412073C (ru) |
AR (1) | AR039891A1 (ru) |
AU (1) | AU2003251384B2 (ru) |
BR (1) | BR0311419A (ru) |
CA (1) | CA2484822A1 (ru) |
CO (1) | CO5640081A2 (ru) |
HK (1) | HK1081187A1 (ru) |
HR (1) | HRP20041220A2 (ru) |
IL (1) | IL164890A0 (ru) |
MX (1) | MX249034B (ru) |
MY (1) | MY137509A (ru) |
NO (1) | NO20045403L (ru) |
NZ (1) | NZ537346A (ru) |
PL (1) | PL372246A1 (ru) |
RU (1) | RU2359967C2 (ru) |
TW (1) | TW200406395A (ru) |
UA (1) | UA80131C2 (ru) |
WO (1) | WO2003099805A1 (ru) |
ZA (1) | ZA200408711B (ru) |
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CN100413861C (zh) * | 2002-12-10 | 2008-08-27 | 维勒凯姆制药股份有限公司 | 用于治疗或预防黄病毒感染的化合物 |
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CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
US20080146624A1 (en) * | 2006-09-19 | 2008-06-19 | Incyte Corporation | Amidines as modulators of indoleamine 2,3-dioxygenase |
EA201101492A1 (ru) * | 2006-11-15 | 2012-09-28 | Вирокем Фарма Инк. | Аналоги тиофена для лечения или предупреждения флавивирусных инфекций |
AU2008214359B2 (en) | 2007-02-05 | 2014-01-16 | Apellis Pharmaceuticals, Inc. | Local complement inhibition for treatment of complement-mediated disorders |
JO3396B1 (ar) * | 2007-06-20 | 2019-10-20 | Anacor Pharmaceuticals Inc | جزيئات صغيرة تحتوي على البورون |
EP2226320A4 (en) * | 2007-12-26 | 2012-07-11 | Eisai R&D Man Co Ltd | PROCESS FOR THE PRODUCTION OF A HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE |
HUE036813T2 (hu) | 2008-07-08 | 2018-07-30 | Incyte Holdings Corp | 1,2,5-Oxadiazolok mint indolamin-2,3-dioxigenáz inhibitorok |
WO2011090929A1 (en) | 2010-01-19 | 2011-07-28 | Theravance, Inc. | Dual-acting thiophene, pyrrole, thiazole and furan antihypertensive agents |
EP2723361B1 (en) | 2011-06-22 | 2019-10-30 | Apellis Pharmaceuticals, Inc. | Methods of treating chronic disorders with complement inhibitors |
EP2874997A4 (en) | 2012-07-19 | 2016-01-06 | Univ Drexel | NEW SIGMA RECEPTOR LIGANDS AND METHOD FOR REGULATING CELLULAR PROTEIN HOMEOSTASIS THEREWITH |
EP2900634B1 (en) | 2012-09-27 | 2017-02-22 | Bayer CropScience AG | Process for the preparation of optionally substituted phenyl and pyridyl pyrrolidines |
CA2900029C (en) | 2013-02-06 | 2021-03-02 | Bayer Cropscience Aktiengesellschaft | Halogen-substituted pyrazol derivatives as pest-control agents |
MX2015016543A (es) * | 2013-06-27 | 2017-07-27 | Lg Chemical Ltd | Derivados de biarilo como agonistas de gpr120. |
KR102370067B1 (ko) | 2013-11-08 | 2022-03-04 | 인사이트 홀딩스 코포레이션 | 인돌아민 2,3-디옥시게나제 억제제의 합성 방법 |
WO2016131098A1 (en) | 2015-02-16 | 2016-08-25 | The University Of Queensland | Sulfonylureas and related compounds and use of same |
ES2906280T3 (es) | 2017-07-07 | 2022-04-18 | Inflazome Ltd | Nuevos compuestos de sulfonamida carboxamida |
US11370776B2 (en) | 2017-07-07 | 2022-06-28 | Inflazome Limited | Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors |
EP3668843A1 (en) | 2017-08-15 | 2020-06-24 | Inflazome Limited | Sulfonylureas and sulfonylthioureas as nlrp3 inhibitors |
WO2019034697A1 (en) | 2017-08-15 | 2019-02-21 | Inflazome Limited | NOVEL CARBOXAMIDE SULFONAMIDE COMPOUNDS |
UY37847A (es) | 2017-08-15 | 2019-03-29 | Inflazome Ltd | Sulfonilureas y sulfoniltioureas útiles como inhibidores de nlrp3 |
WO2019034692A1 (en) | 2017-08-15 | 2019-02-21 | Inflazome Limited | SULFONYLURATES AND SULFONYLTHIOURES AS INHIBITORS OF NLRP3 |
KR20200041918A (ko) * | 2017-08-15 | 2020-04-22 | 인플라좀 리미티드 | 신규한 설폰아마이드 카복스아마이드 화합물 |
WO2019089902A1 (en) | 2017-11-01 | 2019-05-09 | Drexel University | Compounds, compositions, and methods for treating diseases |
MX2020004423A (es) | 2017-11-09 | 2020-08-06 | Inflazome Ltd | Nuevos compuestos de sulfonamida carboxamida. |
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CN115667925A (zh) | 2020-05-15 | 2023-01-31 | 阿雷克森制药公司 | 使用细胞外囊泡来检测补体激活的方法以及其用于评估和/或监测补体介导的疾病的治疗的用途 |
WO2022007979A1 (zh) | 2020-09-01 | 2022-01-13 | 江苏恒瑞医药股份有限公司 | 稠合咪唑类衍生物、其制备方法及其在医药上的应用 |
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AU2001288819A1 (en) * | 2000-09-11 | 2002-03-26 | Genentech, Inc. | Amidine inhibitors of serine proteases |
DE10112041A1 (de) * | 2001-03-14 | 2002-09-26 | Aventis Pharma Gmbh | p-Thienylbenzyl-Amide als Agonisten von Angiotensin-(1-7)-Rezeptoren, Verfahren zu ihrer Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
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TWI299664B (en) * | 2003-01-06 | 2008-08-11 | Osi Pharm Inc | (2-carboxamido)(3-amino)thiophene compounds |
-
2003
- 2003-05-28 AU AU2003251384A patent/AU2003251384B2/en not_active Ceased
- 2003-05-28 UA UA20041209867A patent/UA80131C2/uk unknown
- 2003-05-28 CA CA002484822A patent/CA2484822A1/en not_active Abandoned
- 2003-05-28 TW TW092114404A patent/TW200406395A/zh unknown
- 2003-05-28 WO PCT/US2003/016888 patent/WO2003099805A1/en active Application Filing
- 2003-05-28 BR BR0311419-8A patent/BR0311419A/pt not_active IP Right Cessation
- 2003-05-28 US US10/515,554 patent/US7138530B2/en not_active Expired - Fee Related
- 2003-05-28 JP JP2004507462A patent/JP2005538953A/ja active Pending
- 2003-05-28 EP EP03755527A patent/EP1549632A4/en not_active Withdrawn
- 2003-05-28 KR KR10-2004-7019227A patent/KR20050009720A/ko not_active Application Discontinuation
- 2003-05-28 ZA ZA200408711A patent/ZA200408711B/en unknown
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- 2003-05-28 MX MXPA04011671 patent/MX249034B/es active IP Right Grant
- 2003-05-28 PL PL03372246A patent/PL372246A1/xx not_active Application Discontinuation
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- 2003-05-28 NZ NZ537346A patent/NZ537346A/en not_active IP Right Cessation
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2004
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2006
- 2006-01-26 HK HK06101171.3A patent/HK1081187A1/xx not_active IP Right Cessation
Also Published As
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CN1665800A (zh) | 2005-09-07 |
AU2003251384A1 (en) | 2003-12-12 |
US20050234081A1 (en) | 2005-10-20 |
WO2003099805A1 (en) | 2003-12-04 |
CN100412073C (zh) | 2008-08-20 |
ZA200408711B (en) | 2006-10-25 |
BR0311419A (pt) | 2005-04-05 |
US7109354B2 (en) | 2006-09-19 |
PL372246A1 (en) | 2005-07-11 |
NO20045403L (no) | 2004-12-10 |
US20040009995A1 (en) | 2004-01-15 |
IL164890A0 (en) | 2005-12-18 |
US7138530B2 (en) | 2006-11-21 |
CO5640081A2 (es) | 2006-05-31 |
MX249034B (es) | 2007-09-14 |
MY137509A (en) | 2009-02-27 |
TW200406395A (en) | 2004-05-01 |
NZ537346A (en) | 2006-12-22 |
CA2484822A1 (en) | 2003-12-04 |
MXPA04011671A (es) | 2005-03-07 |
AR039891A1 (es) | 2005-03-09 |
HRP20041220A2 (hr) | 2006-04-30 |
JP2005538953A (ja) | 2005-12-22 |
EP1549632A4 (en) | 2005-11-09 |
KR20050009720A (ko) | 2005-01-25 |
HK1081187A1 (en) | 2006-05-12 |
RU2359967C2 (ru) | 2009-06-27 |
RU2004138787A (ru) | 2005-07-10 |
EP1549632A1 (en) | 2005-07-06 |
AU2003251384B2 (en) | 2009-01-29 |
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