ZA200501856B - Pyrazolopyridines and methods of making and using the same - Google Patents
Pyrazolopyridines and methods of making and using the same Download PDFInfo
- Publication number
- ZA200501856B ZA200501856B ZA200501856A ZA200501856A ZA200501856B ZA 200501856 B ZA200501856 B ZA 200501856B ZA 200501856 A ZA200501856 A ZA 200501856A ZA 200501856 A ZA200501856 A ZA 200501856A ZA 200501856 B ZA200501856 B ZA 200501856B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- compound
- composition
- substance
- heterocycloalkyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims description 48
- 150000005229 pyrazolopyridines Chemical class 0.000 title description 2
- 125000000217 alkyl group Chemical group 0.000 claims description 127
- 150000001875 compounds Chemical class 0.000 claims description 70
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 60
- 125000001072 heteroaryl group Chemical group 0.000 claims description 47
- -1 hydroxy, amino Chemical group 0.000 claims description 45
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 36
- 125000003545 alkoxy group Chemical group 0.000 claims description 32
- 125000004414 alkyl thio group Chemical group 0.000 claims description 28
- 102000009618 Transforming Growth Factors Human genes 0.000 claims description 24
- 108010009583 Transforming Growth Factors Proteins 0.000 claims description 23
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical group NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 20
- 125000002252 acyl group Chemical group 0.000 claims description 20
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 20
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 20
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 17
- 210000004027 cell Anatomy 0.000 claims description 16
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical group NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 16
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims description 14
- 125000003118 aryl group Chemical group 0.000 claims description 14
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 13
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 13
- 238000004519 manufacturing process Methods 0.000 claims description 13
- 125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 12
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims description 12
- 125000003342 alkenyl group Chemical group 0.000 claims description 11
- 230000003176 fibrotic effect Effects 0.000 claims description 11
- 125000001188 haloalkyl group Chemical group 0.000 claims description 11
- 102000010834 Extracellular Matrix Proteins Human genes 0.000 claims description 10
- 108010037362 Extracellular Matrix Proteins Proteins 0.000 claims description 10
- 125000005196 alkyl carbonyloxy group Chemical group 0.000 claims description 10
- 208000035475 disorder Diseases 0.000 claims description 10
- 210000002744 extracellular matrix Anatomy 0.000 claims description 10
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 10
- 125000004122 cyclic group Chemical group 0.000 claims description 9
- 230000019491 signal transduction Effects 0.000 claims description 9
- 125000000304 alkynyl group Chemical group 0.000 claims description 8
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 8
- 125000003435 aroyl group Chemical group 0.000 claims description 8
- 125000004104 aryloxy group Chemical group 0.000 claims description 8
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 8
- 125000005224 heteroarylcarbonylamino group Chemical group 0.000 claims description 8
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 8
- NVBFHJWHLNUMCV-UHFFFAOYSA-N sulfamide Chemical group NS(N)(=O)=O NVBFHJWHLNUMCV-UHFFFAOYSA-N 0.000 claims description 8
- 238000009825 accumulation Methods 0.000 claims description 7
- 125000004656 alkyl sulfonylamino group Chemical group 0.000 claims description 7
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims description 7
- 125000005169 cycloalkylcarbonylamino group Chemical group 0.000 claims description 7
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 7
- 101000635938 Homo sapiens Transforming growth factor beta-1 proprotein Proteins 0.000 claims description 6
- 102100030742 Transforming growth factor beta-1 proprotein Human genes 0.000 claims description 6
- 125000005126 aryl alkyl carbonyl amino group Chemical group 0.000 claims description 6
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims description 6
- 125000004658 aryl carbonyl amino group Chemical group 0.000 claims description 6
- 239000004202 carbamide Chemical group 0.000 claims description 6
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 6
- 125000005171 cycloalkylsulfanyl group Chemical group 0.000 claims description 6
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 6
- 239000001257 hydrogen Substances 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
- 125000003396 thiol group Chemical class [H]S* 0.000 claims description 6
- 125000005163 aryl sulfanyl group Chemical group 0.000 claims description 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 5
- 230000002018 overexpression Effects 0.000 claims description 5
- 230000002265 prevention Effects 0.000 claims description 5
- 206010016654 Fibrosis Diseases 0.000 claims description 4
- 125000004181 carboxyalkyl group Chemical group 0.000 claims description 4
- 230000004761 fibrosis Effects 0.000 claims description 4
- 125000005114 heteroarylalkoxy group Chemical group 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- JNYLMODTPLSLIF-UHFFFAOYSA-N 6-(trifluoromethyl)pyridine-3-carboxylic acid Chemical group OC(=O)C1=CC=C(C(F)(F)F)N=C1 JNYLMODTPLSLIF-UHFFFAOYSA-N 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 229920002554 vinyl polymer Polymers 0.000 claims description 3
- 206010019668 Hepatic fibrosis Diseases 0.000 claims description 2
- 125000004448 alkyl carbonyl group Chemical group 0.000 claims description 2
- 125000005018 aryl alkenyl group Chemical group 0.000 claims description 2
- 125000005099 aryl alkyl carbonyl group Chemical group 0.000 claims description 2
- 125000005015 aryl alkynyl group Chemical group 0.000 claims description 2
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 claims description 2
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims description 2
- 125000005112 cycloalkylalkoxy group Chemical group 0.000 claims description 2
- 125000005419 heteroarylsulfonylamino group Chemical group 0.000 claims description 2
- 201000002793 renal fibrosis Diseases 0.000 claims description 2
- 125000006296 sulfonyl amino group Chemical group [H]N(*)S(*)(=O)=O 0.000 claims description 2
- 230000029663 wound healing Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 42
- 239000000126 substance Substances 0.000 claims 40
- 230000002401 inhibitory effect Effects 0.000 claims 16
- 125000001475 halogen functional group Chemical group 0.000 claims 10
- 206010027476 Metastases Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 230000009401 metastasis Effects 0.000 claims 4
- 210000004881 tumor cell Anatomy 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 3
- 230000037390 scarring Effects 0.000 claims 3
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- WBYIDWODCBKPKM-UHFFFAOYSA-N 2-(6-methylpyridin-2-yl)-3-(2-methylsulfanylpyrimidin-4-yl)pyrazolo[1,5-a]pyridine Chemical compound CSC1=NC=CC(C2=C3C=CC=CN3N=C2C=2N=C(C)C=CC=2)=N1 WBYIDWODCBKPKM-UHFFFAOYSA-N 0.000 claims 1
- FSMFIPLMGNQWQW-UHFFFAOYSA-N 4-[2-(6-methylpyridin-2-yl)pyrazolo[1,5-a]pyrimidin-3-yl]pyrimidin-2-amine Chemical compound CC1=CC=CC(C=2C(=C3N=CC=CN3N=2)C=2N=C(N)N=CC=2)=N1 FSMFIPLMGNQWQW-UHFFFAOYSA-N 0.000 claims 1
- VENUMYHILKBIGQ-UHFFFAOYSA-N 4-[2-(6-methylpyridin-2-yl)pyrazolo[1,5-c]pyrimidin-3-yl]pyrimidin-2-amine Chemical compound CC1=CC=CC(C=2C(=C3C=CN=CN3N=2)C=2N=C(N)N=CC=2)=N1 VENUMYHILKBIGQ-UHFFFAOYSA-N 0.000 claims 1
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 200000000007 Arterial disease Diseases 0.000 claims 1
- 208000008439 Biliary Liver Cirrhosis Diseases 0.000 claims 1
- 208000033222 Biliary cirrhosis primary Diseases 0.000 claims 1
- 206010004664 Biliary fibrosis Diseases 0.000 claims 1
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 206010008609 Cholangitis sclerosing Diseases 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000016192 Demyelinating disease Diseases 0.000 claims 1
- 206010012305 Demyelination Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 208000007659 Fibroadenoma Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 208000002260 Keloid Diseases 0.000 claims 1
- 206010023330 Keloid scar Diseases 0.000 claims 1
- 208000004852 Lung Injury Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000012654 Primary biliary cholangitis Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010069363 Traumatic lung injury Diseases 0.000 claims 1
- 206010046798 Uterine leiomyoma Diseases 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 210000003445 biliary tract Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 230000002490 cerebral effect Effects 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 208000018631 connective tissue disease Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 206010016629 fibroma Diseases 0.000 claims 1
- 210000001035 gastrointestinal tract Anatomy 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 230000002440 hepatic effect Effects 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 210000001117 keloid Anatomy 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000010260 leiomyoma Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 231100000515 lung injury Toxicity 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 210000002569 neuron Anatomy 0.000 claims 1
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- 210000000496 pancreas Anatomy 0.000 claims 1
- 201000000742 primary sclerosing cholangitis Diseases 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000004944 pyrazin-3-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 208000010157 sclerosing cholangitis Diseases 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 108010059616 Activins Proteins 0.000 description 10
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- 125000005843 halogen group Chemical group 0.000 description 9
- 125000004076 pyridyl group Chemical group 0.000 description 4
- UBWXUGDQUBIEIZ-UHFFFAOYSA-N (13-methyl-3-oxo-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-17-yl) 3-phenylpropanoate Chemical compound CC12CCC(C3CCC(=O)C=C3CC3)C3C1CCC2OC(=O)CCC1=CC=CC=C1 UBWXUGDQUBIEIZ-UHFFFAOYSA-N 0.000 description 3
- 102400000401 Latency-associated peptide Human genes 0.000 description 3
- 102100025751 Mothers against decapentaplegic homolog 2 Human genes 0.000 description 3
- 101710143123 Mothers against decapentaplegic homolog 2 Proteins 0.000 description 3
- 102100025748 Mothers against decapentaplegic homolog 3 Human genes 0.000 description 3
- 101710143111 Mothers against decapentaplegic homolog 3 Proteins 0.000 description 3
- 102000001708 Protein Isoforms Human genes 0.000 description 3
- 108010029485 Protein Isoforms Proteins 0.000 description 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 3
- 239000003102 growth factor Substances 0.000 description 3
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 description 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 3
- 125000002883 imidazolyl group Chemical group 0.000 description 3
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- 125000003226 pyrazolyl group Chemical group 0.000 description 3
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- NWGPLYYBECWONP-UHFFFAOYSA-N (carbamoylamino) hydrogen sulfate Chemical compound NC(=O)NOS(O)(=O)=O NWGPLYYBECWONP-UHFFFAOYSA-N 0.000 description 2
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- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 2
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- 125000004608 5,6,7,8-tetrahydroquinolinyl group Chemical group N1=C(C=CC=2CCCCC12)* 0.000 description 1
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 description 1
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- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 description 1
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- 102000001253 Protein Kinase Human genes 0.000 description 1
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
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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
- A61P35/04—Antineoplastic agents specific for metastasis
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
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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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- 2003-09-05 AU AU2003268447A patent/AU2003268447B2/en not_active Ceased
- 2003-09-05 MX MXPA05002443A patent/MXPA05002443A/es active IP Right Grant
- 2003-09-05 EP EP03749412A patent/EP1551398A4/en not_active Withdrawn
- 2003-09-05 JP JP2004534571A patent/JP2006502165A/ja active Pending
- 2003-09-05 BR BR0314053-9A patent/BR0314053A/pt not_active IP Right Cessation
- 2003-09-05 NZ NZ539069A patent/NZ539069A/en unknown
- 2003-09-05 EA EA200500450A patent/EA009441B1/ru not_active IP Right Cessation
- 2003-09-05 GE GEAP20038727A patent/GEP20074125B/en unknown
- 2003-09-05 CA CA002497970A patent/CA2497970A1/en not_active Abandoned
- 2003-09-05 KR KR1020057003874A patent/KR20050057235A/ko not_active Withdrawn
- 2003-09-05 WO PCT/US2003/027722 patent/WO2004022054A1/en not_active Ceased
- 2003-09-05 RS YUP-2005/0200A patent/RS20050200A/sr unknown
- 2003-09-08 AR ARP030103250A patent/AR041207A1/es unknown
-
2005
- 2005-03-03 ZA ZA200501856A patent/ZA200501856B/en unknown
- 2005-03-04 IS IS7725A patent/IS7725A/is unknown
- 2005-03-04 IS IS7726A patent/IS7726A/is unknown
- 2005-03-21 NO NO20051503A patent/NO20051503D0/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| IS7726A (is) | 2005-03-04 |
| RS20050200A (sr) | 2007-08-03 |
| EA200500450A1 (ru) | 2005-08-25 |
| EP1551398A4 (en) | 2006-06-07 |
| AU2003268447A1 (en) | 2004-03-29 |
| GEP20074125B (en) | 2007-06-11 |
| US20060106033A1 (en) | 2006-05-18 |
| NZ539069A (en) | 2007-03-30 |
| PL375699A1 (en) | 2005-12-12 |
| NO20051503L (no) | 2005-03-21 |
| CA2497970A1 (en) | 2004-03-18 |
| BR0314053A (pt) | 2005-07-19 |
| WO2004022054A1 (en) | 2004-03-18 |
| UA80295C2 (en) | 2007-09-10 |
| CN1694698A (zh) | 2005-11-09 |
| IS7725A (is) | 2005-03-04 |
| KR20050057235A (ko) | 2005-06-16 |
| US7691865B2 (en) | 2010-04-06 |
| NO20051503D0 (no) | 2005-03-21 |
| MXPA05002443A (es) | 2005-09-30 |
| AU2003268447B2 (en) | 2008-07-24 |
| EP1551398A1 (en) | 2005-07-13 |
| JP2006502165A (ja) | 2006-01-19 |
| AR041207A1 (es) | 2005-05-11 |
| EA009441B1 (ru) | 2007-12-28 |
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