SI20637A - Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti - Google Patents
Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti Download PDFInfo
- Publication number
- SI20637A SI20637A SI9920090A SI9920090A SI20637A SI 20637 A SI20637 A SI 20637A SI 9920090 A SI9920090 A SI 9920090A SI 9920090 A SI9920090 A SI 9920090A SI 20637 A SI20637 A SI 20637A
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- SI
- Slovenia
- Prior art keywords
- alkyl
- aryl
- aralkyl
- optionally substituted
- halo
- Prior art date
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- 125000003118 aryl group Chemical group 0.000 title claims abstract description 142
- 125000000623 heterocyclic group Chemical group 0.000 title claims abstract description 17
- 239000003146 anticoagulant agent Substances 0.000 title abstract description 12
- 229940127219 anticoagulant drug Drugs 0.000 title abstract description 12
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title abstract description 4
- 150000003230 pyrimidines Chemical class 0.000 title abstract description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 255
- -1 nitro, ureido, guanidino Chemical group 0.000 claims description 224
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 160
- 125000000217 alkyl group Chemical group 0.000 claims description 148
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 84
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 83
- 125000003545 alkoxy group Chemical group 0.000 claims description 77
- 150000001412 amines Chemical class 0.000 claims description 73
- 125000001188 haloalkyl group Chemical group 0.000 claims description 73
- 125000005265 dialkylamine group Chemical group 0.000 claims description 71
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 claims description 50
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims description 43
- 239000001257 hydrogen Substances 0.000 claims description 42
- 229910052739 hydrogen Inorganic materials 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 40
- 150000002431 hydrogen Chemical class 0.000 claims description 27
- 239000000203 mixture Substances 0.000 claims description 22
- 201000010099 disease Diseases 0.000 claims description 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 15
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 11
- WKTCFPZPRJPZID-UHFFFAOYSA-N 4-hydroxy-3-[6-[3-(1-methyl-4,5-dihydroimidazol-2-yl)phenoxy]-2-phenylpyrimidin-4-yl]oxybenzenecarboximidamide Chemical compound CN1CCN=C1C1=CC=CC(OC=2N=C(N=C(OC=3C(=CC=C(C=3)C(N)=N)O)C=2)C=2C=CC=CC=2)=C1 WKTCFPZPRJPZID-UHFFFAOYSA-N 0.000 claims description 9
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 5
- 125000001118 alkylidene group Chemical group 0.000 claims description 5
- 125000004663 dialkyl amino group Chemical group 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- OOLQXIIIKBZNTF-UHFFFAOYSA-N 4-hydroxy-3-[2-[3-(1-methyl-4,5-dihydroimidazol-2-yl)phenoxy]-6-phenylpyrimidin-4-yl]oxybenzenecarboximidamide Chemical compound CN1CCN=C1C1=CC=CC(OC=2N=C(C=C(OC=3C(=CC=C(C=3)C(N)=N)O)N=2)C=2C=CC=CC=2)=C1 OOLQXIIIKBZNTF-UHFFFAOYSA-N 0.000 claims description 3
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- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 3
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- 125000001475 halogen functional group Chemical group 0.000 claims 52
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- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 33
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Classifications
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- 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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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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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- A61P31/04—Antibacterial agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- A—HUMAN NECESSITIES
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- 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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- 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
- C07D403/02—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 two hetero rings
- C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Separation Of Suspended Particles By Flocculating Agents (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/205,498 US6127376A (en) | 1998-12-04 | 1998-12-04 | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
| PCT/US1999/028537 WO2000033844A1 (en) | 1998-12-04 | 1999-12-03 | Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SI20637A true SI20637A (sl) | 2002-02-28 |
Family
ID=22762435
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9920090A SI20637A (sl) | 1998-12-04 | 1999-12-03 | Aril- in heterociklil-substituirani pirimidinski derivati kot antikoagulanti |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US6127376A (cs) |
| EP (1) | EP1135131A4 (cs) |
| JP (1) | JP2002531506A (cs) |
| KR (1) | KR20010093799A (cs) |
| CN (1) | CN1329491A (cs) |
| AU (1) | AU760370B2 (cs) |
| BG (1) | BG105557A (cs) |
| BR (1) | BR9915938A (cs) |
| CA (1) | CA2354040A1 (cs) |
| CZ (1) | CZ20011932A3 (cs) |
| EE (1) | EE200100298A (cs) |
| HR (1) | HRP20010499A2 (cs) |
| HU (1) | HUP0104508A3 (cs) |
| IL (2) | IL143347A0 (cs) |
| LT (1) | LT4912B (cs) |
| LV (1) | LV12783B (cs) |
| MX (1) | MXPA01005656A (cs) |
| NO (1) | NO20012701L (cs) |
| NZ (1) | NZ512104A (cs) |
| PL (1) | PL348034A1 (cs) |
| RO (1) | RO120971B1 (cs) |
| RU (1) | RU2001118466A (cs) |
| SI (1) | SI20637A (cs) |
| SK (1) | SK7632001A3 (cs) |
| WO (1) | WO2000033844A1 (cs) |
| ZA (1) | ZA200104235B (cs) |
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| US6350761B1 (en) | 1999-07-30 | 2002-02-26 | Berlex Laboratories, Inc. | Benzenamine derivatives as anti-coagulants |
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| US7129242B2 (en) | 2000-12-06 | 2006-10-31 | Signal Pharmaceuticals, Llc | Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto |
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| PT1569912E (pt) | 2002-12-03 | 2015-09-15 | Pharmacyclics Llc | Derivados 2-(2-hidroxibifenil-3-il)-1h-benzoimidazole-5- carboxamidina como inibidores do fator viia |
| BRPI0413018B8 (pt) | 2003-07-30 | 2021-05-25 | Rigel Pharmaceuticals Inc | composto, e, uso de um composto |
| US8455489B2 (en) * | 2003-11-10 | 2013-06-04 | Exelixis, Inc. | Substituted pyrimidine compositions and methods of use |
| WO2006068770A1 (en) * | 2004-11-24 | 2006-06-29 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
| JP4801096B2 (ja) * | 2005-01-19 | 2011-10-26 | ライジェル ファーマシューティカルズ, インコーポレイテッド | 2,4−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用 |
| US20060270694A1 (en) * | 2005-05-03 | 2006-11-30 | Rigel Pharmaceuticals, Inc. | JAK kinase inhibitors and their uses |
| ES2367820T3 (es) * | 2006-07-21 | 2011-11-08 | Novartis Ag | Derivados de la pirimidina y sus usos como pesticidas. |
| NZ589315A (en) | 2008-04-16 | 2012-11-30 | Portola Pharm Inc | 2,6-diamino-pyrimidin-5-yl-carboxamides as Spleen tryosine kinase (syk) or Janus kinase (JAK) inhibitors |
| US8138339B2 (en) | 2008-04-16 | 2012-03-20 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| WO2009143389A1 (en) | 2008-05-21 | 2009-11-26 | Ariad Pharmaceuticals, Inc. | Phosphorous derivatives as kinase inhibitors |
| US11351168B1 (en) | 2008-06-27 | 2022-06-07 | Celgene Car Llc | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| US8338439B2 (en) * | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| AU2009262068C1 (en) | 2008-06-27 | 2015-07-02 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| US8932842B2 (en) | 2009-02-11 | 2015-01-13 | Northwestern University | Aminopyridine dimer compounds, compositions and related methods for neuronal nitric oxide synthase inhibition |
| WO2010093787A2 (en) * | 2009-02-11 | 2010-08-19 | Northwestern University | Aminopyridine dimer compounds, compositions and related methods for neuronal nitric oxide synthase inhibition |
| CA2760794C (en) | 2009-05-05 | 2017-07-25 | Dana Farber Cancer Institute | Egfr inhibitors and methods of treating disorders |
| PT2603081T (pt) | 2010-08-10 | 2017-01-13 | Celgene Avilomics Res Inc | Sal de besilato de um inibidor de btk |
| ES2635713T3 (es) | 2010-11-01 | 2017-10-04 | Celgene Car Llc | Compuestos de heteroarilo y usos de los mismos |
| BR112013010564B1 (pt) | 2010-11-01 | 2021-09-21 | Celgene Car Llc | Compostos heterocíclicos e composições compreendendo os mesmos |
| EP2637502B1 (en) | 2010-11-10 | 2018-01-10 | Celgene CAR LLC | Mutant-selective egfr inhibitors and uses thereof |
| JP5999177B2 (ja) | 2011-05-04 | 2016-09-28 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
| TW201325593A (zh) | 2011-10-28 | 2013-07-01 | Celgene Avilomics Res Inc | 治療布魯頓(bruton’s)酪胺酸激酶疾病或病症之方法 |
| MX363551B (es) | 2011-11-23 | 2019-03-27 | Portola Pharmaceuticals Inc Star | Compuestos derivados de pirazina como inhibidores de cinasa. |
| CN104302178B (zh) | 2012-03-15 | 2018-07-13 | 西建卡尔有限责任公司 | 表皮生长因子受体激酶抑制剂的固体形式 |
| EP2825042B1 (en) | 2012-03-15 | 2018-08-01 | Celgene CAR LLC | Salts of an epidermal growth factor receptor kinase inhibitor |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
| WO2014100748A1 (en) | 2012-12-21 | 2014-06-26 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CA2900012A1 (en) | 2013-02-08 | 2014-08-14 | Celgene Avilomics Research, Inc. | Erk inhibitors and uses thereof |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| US9492471B2 (en) | 2013-08-27 | 2016-11-15 | Celgene Avilomics Research, Inc. | Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase |
| US9415049B2 (en) | 2013-12-20 | 2016-08-16 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
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| CN109897005B (zh) * | 2019-04-12 | 2022-07-22 | 湖南省农业生物技术研究所 | 含取代苯氧基的苯基嘧啶类似物及其制备方法和应用 |
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| EP0518818A3 (en) * | 1991-06-11 | 1993-04-28 | Ciba-Geigy Ag | Arylethers, their manufacture and use as medicament |
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-
1998
- 1998-12-04 US US09/205,498 patent/US6127376A/en not_active Expired - Fee Related
-
1999
- 1999-12-03 RU RU2001118466/14A patent/RU2001118466A/ru not_active Application Discontinuation
- 1999-12-03 AU AU31075/00A patent/AU760370B2/en not_active Ceased
- 1999-12-03 IL IL14334799A patent/IL143347A0/xx active IP Right Grant
- 1999-12-03 PL PL99348034A patent/PL348034A1/xx not_active Application Discontinuation
- 1999-12-03 WO PCT/US1999/028537 patent/WO2000033844A1/en not_active Ceased
- 1999-12-03 KR KR1020017006934A patent/KR20010093799A/ko not_active Withdrawn
- 1999-12-03 BR BR9915938-4A patent/BR9915938A/pt not_active IP Right Cessation
- 1999-12-03 EP EP99965087A patent/EP1135131A4/en not_active Withdrawn
- 1999-12-03 CN CN99814024A patent/CN1329491A/zh active Pending
- 1999-12-03 CZ CZ20011932A patent/CZ20011932A3/cs unknown
- 1999-12-03 CA CA002354040A patent/CA2354040A1/en not_active Abandoned
- 1999-12-03 HR HR20010499A patent/HRP20010499A2/hr not_active Application Discontinuation
- 1999-12-03 SI SI9920090A patent/SI20637A/sl not_active IP Right Cessation
- 1999-12-03 MX MXPA01005656A patent/MXPA01005656A/es not_active IP Right Cessation
- 1999-12-03 JP JP2000586336A patent/JP2002531506A/ja active Pending
- 1999-12-03 SK SK763-2001A patent/SK7632001A3/sk unknown
- 1999-12-03 NZ NZ512104A patent/NZ512104A/en unknown
- 1999-12-03 EE EEP200100298A patent/EE200100298A/xx unknown
- 1999-12-03 RO ROA200100606A patent/RO120971B1/ro unknown
- 1999-12-03 HU HU0104508A patent/HUP0104508A3/hu unknown
-
2000
- 2000-03-30 US US09/539,812 patent/US6372751B1/en not_active Expired - Fee Related
-
2001
- 2001-05-23 ZA ZA200104235A patent/ZA200104235B/en unknown
- 2001-05-24 IL IL143347A patent/IL143347A/en not_active IP Right Cessation
- 2001-06-01 NO NO20012701A patent/NO20012701L/no not_active Application Discontinuation
- 2001-06-01 BG BG105557A patent/BG105557A/xx unknown
- 2001-06-12 LT LT2001061A patent/LT4912B/lt not_active IP Right Cessation
- 2001-07-04 LV LVP-01-100A patent/LV12783B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN1329491A (zh) | 2002-01-02 |
| BR9915938A (pt) | 2001-08-21 |
| HRP20010499A2 (en) | 2003-04-30 |
| ZA200104235B (en) | 2002-08-23 |
| LT2001061A (en) | 2001-12-27 |
| CA2354040A1 (en) | 2000-06-15 |
| SK7632001A3 (en) | 2001-12-03 |
| CZ20011932A3 (cs) | 2001-10-17 |
| JP2002531506A (ja) | 2002-09-24 |
| HUP0104508A2 (hu) | 2002-05-29 |
| KR20010093799A (ko) | 2001-10-29 |
| US6127376A (en) | 2000-10-03 |
| LV12783A (en) | 2002-01-20 |
| EE200100298A (et) | 2002-12-16 |
| WO2000033844A1 (en) | 2000-06-15 |
| IL143347A0 (en) | 2002-04-21 |
| IL143347A (en) | 2006-12-10 |
| BG105557A (en) | 2001-12-29 |
| EP1135131A4 (en) | 2002-01-02 |
| PL348034A1 (en) | 2002-05-06 |
| US6372751B1 (en) | 2002-04-16 |
| NO20012701D0 (no) | 2001-06-01 |
| LV12783B (en) | 2002-10-20 |
| LT4912B (lt) | 2002-04-25 |
| NO20012701L (no) | 2001-07-25 |
| HUP0104508A3 (en) | 2002-07-29 |
| EP1135131A1 (en) | 2001-09-26 |
| AU760370B2 (en) | 2003-05-15 |
| NZ512104A (en) | 2003-10-31 |
| MXPA01005656A (es) | 2002-04-24 |
| RU2001118466A (ru) | 2003-04-20 |
| AU3107500A (en) | 2000-06-26 |
| RO120971B1 (ro) | 2006-10-30 |
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Legal Events
| Date | Code | Title | Description |
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| IF | Valid on the event date | ||
| KO00 | Lapse of patent |
Effective date: 20050830 |