RU2004135382A - Замещенные пирролины в качестве ингибиторов киназы - Google Patents
Замещенные пирролины в качестве ингибиторов киназы Download PDFInfo
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- RU2004135382A RU2004135382A RU2004135382/04A RU2004135382A RU2004135382A RU 2004135382 A RU2004135382 A RU 2004135382A RU 2004135382/04 A RU2004135382/04 A RU 2004135382/04A RU 2004135382 A RU2004135382 A RU 2004135382A RU 2004135382 A RU2004135382 A RU 2004135382A
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- Prior art keywords
- alkyl
- group
- aryl
- hydrogen
- compound according
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Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 80
- 150000001875 compounds Chemical class 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 26
- 239000001257 hydrogen Substances 0.000 claims 26
- 229910052736 halogen Inorganic materials 0.000 claims 22
- 150000002367 halogens Chemical class 0.000 claims 22
- 238000000034 method Methods 0.000 claims 20
- 125000001424 substituent group Chemical group 0.000 claims 20
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 16
- 229910052799 carbon Inorganic materials 0.000 claims 14
- 125000004432 carbon atom Chemical group C* 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 102000003923 Protein Kinase C Human genes 0.000 claims 7
- 108090000315 Protein Kinase C Proteins 0.000 claims 7
- 108091000080 Phosphotransferase Proteins 0.000 claims 6
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000003118 aryl group Chemical group 0.000 claims 6
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 6
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 6
- 102000020233 phosphotransferase Human genes 0.000 claims 6
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- -1 —NR 7 Chemical group 0.000 claims 5
- 108010001483 Glycogen Synthase Proteins 0.000 claims 4
- 101710092490 Protein kinase 3 Proteins 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 206010012601 diabetes mellitus Diseases 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 102000001253 Protein Kinase Human genes 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000026278 immune system disease Diseases 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 108060006633 protein kinase Proteins 0.000 claims 3
- 201000004384 Alopecia Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010061876 Obstruction Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000003676 hair loss Effects 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 2
- 208000028867 ischemia Diseases 0.000 claims 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010059245 Angiopathy Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010019280 Heart failures Diseases 0.000 claims 1
- 241000713772 Human immunodeficiency virus 1 Species 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 102000004877 Insulin Human genes 0.000 claims 1
- 108090001061 Insulin Proteins 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 208000001344 Macular Edema Diseases 0.000 claims 1
- 206010025415 Macular oedema Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010038933 Retinopathy of prematurity Diseases 0.000 claims 1
- 206010038934 Retinopathy proliferative Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 230000005907 cancer growth Effects 0.000 claims 1
- 210000003169 central nervous system Anatomy 0.000 claims 1
- 208000015114 central nervous system disease Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000003920 cognitive function Effects 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 208000024963 hair loss Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229940125396 insulin Drugs 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 201000010230 macular retinal edema Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 230000000771 oncological effect Effects 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000000750 progressive effect Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 210000001957 retinal vein Anatomy 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 230000004614 tumor growth Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 230000003313 weakening effect Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
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- A61P11/06—Antiasthmatics
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
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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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D409/14—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
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Cardiology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pulmonology (AREA)
- Virology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Transplantation (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38593502P | 2002-06-05 | 2002-06-05 | |
| US60/385,935 | 2002-06-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2004135382A true RU2004135382A (ru) | 2005-06-27 |
Family
ID=29736126
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004135382/04A RU2004135382A (ru) | 2002-06-05 | 2003-06-04 | Замещенные пирролины в качестве ингибиторов киназы |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US6987110B2 (enExample) |
| EP (1) | EP1513830A1 (enExample) |
| JP (1) | JP2005531609A (enExample) |
| KR (1) | KR20050008787A (enExample) |
| CN (1) | CN1671694A (enExample) |
| AU (1) | AU2003238874A1 (enExample) |
| BR (1) | BR0311821A (enExample) |
| CA (1) | CA2488602A1 (enExample) |
| CR (1) | CR7606A (enExample) |
| IL (1) | IL165515A0 (enExample) |
| MX (1) | MXPA04012188A (enExample) |
| NO (1) | NO20045699L (enExample) |
| RU (1) | RU2004135382A (enExample) |
| WO (1) | WO2003104222A1 (enExample) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA03005140A (es) * | 2000-12-08 | 2004-10-15 | Johnson & Johnson | Compuestos de pirrolina sustituidos con indazolilo como inhibidores de cinasa. |
| SE0200979D0 (sv) * | 2002-03-28 | 2002-03-28 | Astrazeneca Ab | New compounds |
| SE0302546D0 (sv) * | 2003-09-24 | 2003-09-24 | Astrazeneca Ab | New compounds |
| AU2003225295A1 (en) * | 2002-05-08 | 2003-11-11 | Janssen Pharmaceutica N.V. | Substituted pyrroline kinase inhibitors |
| ATE409035T1 (de) * | 2002-06-05 | 2008-10-15 | Janssen Pharmaceutica Nv | Substituierte pyrroline als kinase inhibitoren |
| CA2393720C (en) * | 2002-07-12 | 2010-09-14 | Eli Lilly And Company | Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride |
| AU2002951253A0 (en) * | 2002-09-06 | 2002-09-19 | Medvet Science Pty. Ltd. | A method of modulating cellular activity |
| EP1611132A1 (en) * | 2003-03-27 | 2006-01-04 | Janssen Pharmaceutica N.V. | Substituted pyrroline kinase inhibitors |
| EP1654255B1 (en) * | 2003-06-13 | 2008-08-27 | Janssen Pharmaceutica N.V. | Substituted indazolyl(indolyl)maleimide derivatives as kinase inhibitors |
| WO2005083105A2 (en) * | 2004-02-26 | 2005-09-09 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with glycogen synthase kinase 3 beta (gsk3b) |
| WO2005095983A1 (en) * | 2004-03-04 | 2005-10-13 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with protein kinase c, gamma (prkcg) |
| AU2005230399B2 (en) * | 2004-04-08 | 2009-07-09 | Novartis Ag | Protein kinase C inhibitors for the treatment of autoimmune diseases and of transplant rejection |
| RU2413511C2 (ru) * | 2004-04-08 | 2011-03-10 | Новартис Аг | Ингибиторы протеинкиназы с, предназначенные для лечения аутоиммунных заболеваний и отторжения трансплантата |
| CA2567377A1 (en) * | 2004-05-21 | 2006-03-09 | The Texas A & M University System | Inhibition of atherosclerosis by diindolylmethane analogs |
| EP1662259A1 (en) * | 2004-11-25 | 2006-05-31 | Cellzome Ag | Use of Eph receptor inhibitors for the treatment of neurodegenerative diseases |
| US8017395B2 (en) | 2004-12-17 | 2011-09-13 | Lifescan, Inc. | Seeding cells on porous supports |
| CN101484575B (zh) * | 2005-06-08 | 2013-10-02 | 森托科尔公司 | 用于眼变性的细胞疗法 |
| KR20080023732A (ko) * | 2005-07-11 | 2008-03-14 | 노파르티스 아게 | 인돌릴말레이미드 유도체 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CZ280738B6 (cs) | 1988-02-10 | 1996-04-17 | F. Hoffmann - La Roche And Co., Aktiengesellschaft | Substituované pyrroly, jejich použití pro výrobu léčiv a léčiva na jejich bázi |
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| US5624949A (en) | 1993-12-07 | 1997-04-29 | Eli Lilly And Company | Protein kinase C inhibitors |
| WO1995017182A1 (en) | 1993-12-23 | 1995-06-29 | Eli Lilly And Company | Protein kinase c inhibitors |
| CA2249205A1 (en) | 1996-03-20 | 1997-09-25 | Eli Lilly And Company | Synthesis of indolylmaleimides |
| SE9603283D0 (sv) * | 1996-09-10 | 1996-09-10 | Astra Ab | New compounds |
| WO1999042100A1 (en) | 1998-02-23 | 1999-08-26 | Sagami Chemical Research Center | Cell death inhibitors |
| EP1120414A1 (en) | 1998-07-30 | 2001-08-01 | Japan Tobacco Inc. | Disubstituted maleimide compounds and medicinal utilization thereof |
| ATE284387T1 (de) | 1998-10-08 | 2004-12-15 | Smithkline Beecham Plc | 3-(3-chloro-4-hydroxyphenylamino)-4-(2- nitrophenyl)-1h-pyrrol-2,5-dion als glykogen synthase kinase-3 inhibitor (gsk-3) |
| CA2417277A1 (en) | 2000-07-27 | 2002-02-07 | F. Hoffmann-La Roche Ag | 3-indolyl-4-phenyl-1h-pyrrole-2,5-dione derivatives as inhibitors of glycogen synthase kinase-3.beta. |
| EP1337527B1 (en) | 2000-11-07 | 2009-10-14 | Novartis AG | Indolylmaleimide derivatives as protein kinase c inhibitors |
-
2003
- 2003-06-04 US US10/454,069 patent/US6987110B2/en not_active Expired - Fee Related
- 2003-06-04 MX MXPA04012188A patent/MXPA04012188A/es unknown
- 2003-06-04 BR BR0311821-5A patent/BR0311821A/pt not_active IP Right Cessation
- 2003-06-04 KR KR10-2004-7019678A patent/KR20050008787A/ko not_active Withdrawn
- 2003-06-04 CN CNA038184788A patent/CN1671694A/zh active Pending
- 2003-06-04 EP EP03734389A patent/EP1513830A1/en not_active Withdrawn
- 2003-06-04 CA CA002488602A patent/CA2488602A1/en not_active Abandoned
- 2003-06-04 JP JP2004511292A patent/JP2005531609A/ja not_active Withdrawn
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- 2004-12-06 CR CR7606A patent/CR7606A/es unknown
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| BR0311821A (pt) | 2005-04-05 |
| NO20045699L (no) | 2005-01-28 |
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| US6987110B2 (en) | 2006-01-17 |
| WO2003104222A1 (en) | 2003-12-18 |
| MXPA04012188A (es) | 2005-07-25 |
| KR20050008787A (ko) | 2005-01-21 |
| CN1671694A (zh) | 2005-09-21 |
| EP1513830A1 (en) | 2005-03-16 |
| IL165515A0 (en) | 2006-01-15 |
| CA2488602A1 (en) | 2003-12-18 |
| US20040059113A1 (en) | 2004-03-25 |
| CR7606A (es) | 2009-01-16 |
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