PT1185267E - Agentes anestesicos dermicos - Google Patents
Agentes anestesicos dermicos Download PDFInfo
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- PT1185267E PT1185267E PT00941227T PT00941227T PT1185267E PT 1185267 E PT1185267 E PT 1185267E PT 00941227 T PT00941227 T PT 00941227T PT 00941227 T PT00941227 T PT 00941227T PT 1185267 E PT1185267 E PT 1185267E
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- 230000002500 effect on skin Effects 0.000 title claims abstract description 26
- 239000003193 general anesthetic agent Substances 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 94
- 239000000203 mixture Substances 0.000 claims abstract description 42
- 238000000034 method Methods 0.000 claims abstract description 21
- 241000124008 Mammalia Species 0.000 claims abstract 2
- -1 alkoxy radical Chemical class 0.000 claims description 86
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims description 49
- 239000001257 hydrogen Substances 0.000 claims description 40
- 229910052739 hydrogen Inorganic materials 0.000 claims description 40
- 150000003254 radicals Chemical class 0.000 claims description 38
- 150000003839 salts Chemical class 0.000 claims description 37
- 206010002091 Anaesthesia Diseases 0.000 claims description 23
- 230000037005 anaesthesia Effects 0.000 claims description 23
- 150000002431 hydrogen Chemical group 0.000 claims description 22
- 239000000243 solution Substances 0.000 claims description 22
- 239000003795 chemical substances by application Substances 0.000 claims description 19
- 239000012458 free base Substances 0.000 claims description 19
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 19
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 125000004202 aminomethyl group Chemical group [H]N([H])C([H])([H])* 0.000 claims description 14
- 210000005036 nerve Anatomy 0.000 claims description 14
- 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims description 13
- 239000002585 base Substances 0.000 claims description 13
- 239000002253 acid Substances 0.000 claims description 12
- 125000004432 carbon atom Chemical group C* 0.000 claims description 12
- 238000002347 injection Methods 0.000 claims description 12
- 239000007924 injection Substances 0.000 claims description 12
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 claims description 10
- 230000007062 hydrolysis Effects 0.000 claims description 9
- 238000006460 hydrolysis reaction Methods 0.000 claims description 9
- 230000008595 infiltration Effects 0.000 claims description 9
- 238000001764 infiltration Methods 0.000 claims description 9
- 125000001424 substituent group Chemical group 0.000 claims description 9
- 230000036407 pain Effects 0.000 claims description 8
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 7
- 238000002690 local anesthesia Methods 0.000 claims description 7
- 239000002674 ointment Substances 0.000 claims description 7
- 150000003053 piperidines Chemical class 0.000 claims description 7
- GAWIXWVDTYZWAW-UHFFFAOYSA-N C[CH]O Chemical group C[CH]O GAWIXWVDTYZWAW-UHFFFAOYSA-N 0.000 claims description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 238000002691 topical anesthesia Methods 0.000 claims description 6
- FIULGFJIHJJXMT-UHFFFAOYSA-N [C]1[N]C=CC=C1 Chemical compound [C]1[N]C=CC=C1 FIULGFJIHJJXMT-UHFFFAOYSA-N 0.000 claims description 5
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- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
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- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 239000013543 active substance Substances 0.000 claims description 3
- 239000006071 cream Substances 0.000 claims description 3
- 125000000623 heterocyclic group Chemical group 0.000 claims description 3
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- 230000001988 toxicity Effects 0.000 claims description 3
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- 208000003251 Pruritus Diseases 0.000 claims description 2
- 206010042496 Sunburn Diseases 0.000 claims description 2
- 125000002723 alicyclic group Chemical group 0.000 claims description 2
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- 238000001356 surgical procedure Methods 0.000 claims description 2
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- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000001131 transforming effect Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 239000003589 local anesthetic agent Substances 0.000 abstract description 10
- 229960005015 local anesthetics Drugs 0.000 abstract description 3
- XJEVHMGJSYVQBQ-UHFFFAOYSA-N 2,3-dihydro-1h-inden-1-amine Chemical class C1=CC=C2C(N)CCC2=C1 XJEVHMGJSYVQBQ-UHFFFAOYSA-N 0.000 abstract 1
- DEEUGGDCCPTQEN-UHFFFAOYSA-N C1CCNCC1.C1=CC=C2C(N)CCC2=C1 Chemical class C1CCNCC1.C1=CC=C2C(N)CCC2=C1 DEEUGGDCCPTQEN-UHFFFAOYSA-N 0.000 abstract 1
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- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 18
- 230000003444 anaesthetic effect Effects 0.000 description 18
- 238000012360 testing method Methods 0.000 description 17
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- 125000004433 nitrogen atom Chemical group N* 0.000 description 11
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- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 10
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- 230000000694 effects Effects 0.000 description 10
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- 210000001519 tissue Anatomy 0.000 description 10
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- 229910000042 hydrogen bromide Inorganic materials 0.000 description 8
- 238000000197 pyrolysis Methods 0.000 description 8
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- 238000002360 preparation method Methods 0.000 description 7
- ODZPKZBBUMBTMG-UHFFFAOYSA-N sodium amide Chemical compound [NH2-].[Na+] ODZPKZBBUMBTMG-UHFFFAOYSA-N 0.000 description 7
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P23/00—Anaesthetics
- A61P23/02—Local anaesthetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Anesthesiology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
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|---|---|---|---|
| US13835399P | 1999-06-10 | 1999-06-10 | |
| US17926700P | 2000-01-31 | 2000-01-31 |
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| PT1185267E true PT1185267E (pt) | 2006-12-29 |
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|---|---|---|---|
| PT00941227T PT1185267E (pt) | 1999-06-10 | 2000-06-06 | Agentes anestesicos dermicos |
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| EP (1) | EP1185267B1 (enExample) |
| JP (1) | JP2003501469A (enExample) |
| CN (1) | CN1355700A (enExample) |
| AT (1) | ATE335482T1 (enExample) |
| AU (1) | AU777517B2 (enExample) |
| BR (1) | BR0011028A (enExample) |
| CA (1) | CA2376819C (enExample) |
| CY (1) | CY1105721T1 (enExample) |
| DE (1) | DE60029954T2 (enExample) |
| DK (1) | DK1185267T3 (enExample) |
| ES (1) | ES2267546T3 (enExample) |
| IL (2) | IL146190A0 (enExample) |
| MX (1) | MXPA01012632A (enExample) |
| NO (1) | NO323856B1 (enExample) |
| NZ (1) | NZ515143A (enExample) |
| PT (1) | PT1185267E (enExample) |
| WO (1) | WO2000076510A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK1321139T3 (da) * | 2001-12-21 | 2007-01-02 | Chiesi Farma Spa | 2-indanylaminoderivater til behandling af kronisk, akut eller inflammatorisk smerte |
| RU2343145C2 (ru) | 2002-11-26 | 2009-01-10 | Маруиси Фармасьютикал Ко., Лтд. | Производные изоиндолина |
| WO2006037047A2 (en) * | 2004-09-27 | 2006-04-06 | Bridge Pharma, Inc. | The r-isomer of 2-{2-[n-(2-indanyl)-n-phenylamino]ethyl}piperidine and other dermal anesthetic agents |
| WO2006036936A2 (en) * | 2004-09-27 | 2006-04-06 | Bridge Pharma, Inc. | The s-isomer of 2-{2-[n-(2-indanyl)-n-phenylamino]ethyl}piperidine and other dermal anesthetic agents |
| US20090137628A1 (en) * | 2005-09-23 | 2009-05-28 | Bridge Pharma, Inc. | Formulations of Indanylamines and the Use Thereof as Local Anesthetics and as Medication for Chronic Pain |
| US20110218218A1 (en) * | 2005-09-23 | 2011-09-08 | Bridge Pharma, Inc. | Formulations Of Indanylamines And The Use Thereof As Local Anesthetics And As Medication For Chronic Pain |
| US7592458B2 (en) * | 2006-07-21 | 2009-09-22 | Wright George E | Dermal anesthetic compounds and pharmaceutical compositions for inducing local anesthesia and mitigating neuropathic pain |
| CN107661293A (zh) * | 2008-01-22 | 2018-02-06 | 得克萨斯大学体系董事会 | 用于局部麻醉和/或疼痛缓解的含有萃取溶剂的挥发性麻醉剂组合物 |
| KR102014203B1 (ko) * | 2011-02-18 | 2019-08-26 | 아사나 바이오사이언시스 엘엘씨 | 아미노인단 화합물 및 통증 치료에서 그것의 용도 |
| US8809372B2 (en) | 2011-09-30 | 2014-08-19 | Asana Biosciences, Llc | Pyridine derivatives |
| CA2853279C (en) | 2011-10-24 | 2021-03-23 | Endo Pharmaceuticals Inc. | Cyclohexylamines |
| US9044482B2 (en) | 2012-08-15 | 2015-06-02 | Asana Biosciences, Llc | Use of aminoindane compounds in treating overactive bladder and interstitial cystitis |
| US20170296484A1 (en) | 2015-11-23 | 2017-10-19 | Grace Therapeutics Llc | Topical Film-Forming Spray |
| EA202191506A1 (ru) | 2018-12-19 | 2021-10-08 | Нортик Холдингз Инк. | Терапевтическая композиция интраназального лидокаина |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE760018A (fr) * | 1969-12-19 | 1971-06-08 | Christiaens Sa A | Nouveau derives du 2-amino-indane, leur preparation et leur utilisation |
| US3923813A (en) | 1969-12-19 | 1975-12-02 | Christiaens Sa A | Derivatives of 2-aminoindanes |
| AR206505A1 (es) * | 1972-09-18 | 1976-07-30 | Christiaens Sa A | Procedimiento para obtener nuevos derivados de n-fenil-n-aminoalquil-2-aminoindano |
| ZA738419B (en) * | 1972-11-06 | 1974-09-25 | Christiaens Sa A | New derivatives of 2-aminoindane,the preparation and use thereof |
| GB1462036A (en) | 1973-02-05 | 1977-01-19 | Manuf Prod Pharma | Aminoindane derivatives |
| GB1468347A (en) * | 1973-03-02 | 1977-03-23 | Christiaens Sa A | Aminoindanes |
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2000
- 2000-06-06 CA CA002376819A patent/CA2376819C/en not_active Expired - Fee Related
- 2000-06-06 AU AU55963/00A patent/AU777517B2/en not_active Ceased
- 2000-06-06 WO PCT/US2000/015490 patent/WO2000076510A1/en not_active Ceased
- 2000-06-06 BR BR0011028-0A patent/BR0011028A/pt not_active Application Discontinuation
- 2000-06-06 PT PT00941227T patent/PT1185267E/pt unknown
- 2000-06-06 DE DE60029954T patent/DE60029954T2/de not_active Expired - Fee Related
- 2000-06-06 US US09/588,582 patent/US6413987B1/en not_active Expired - Fee Related
- 2000-06-06 DK DK00941227T patent/DK1185267T3/da active
- 2000-06-06 NZ NZ515143A patent/NZ515143A/en not_active IP Right Cessation
- 2000-06-06 CN CN00808753A patent/CN1355700A/zh active Pending
- 2000-06-06 AT AT00941227T patent/ATE335482T1/de not_active IP Right Cessation
- 2000-06-06 ES ES00941227T patent/ES2267546T3/es not_active Expired - Lifetime
- 2000-06-06 MX MXPA01012632A patent/MXPA01012632A/es active IP Right Grant
- 2000-06-06 EP EP00941227A patent/EP1185267B1/en not_active Expired - Lifetime
- 2000-06-06 IL IL14619000A patent/IL146190A0/xx unknown
- 2000-06-06 JP JP2001502843A patent/JP2003501469A/ja active Pending
-
2001
- 2001-10-25 IL IL146190A patent/IL146190A/en not_active IP Right Cessation
- 2001-12-10 NO NO20016037A patent/NO323856B1/no unknown
-
2006
- 2006-10-23 CY CY20061101516T patent/CY1105721T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL146190A0 (en) | 2002-07-25 |
| EP1185267A1 (en) | 2002-03-13 |
| WO2000076510A9 (en) | 2002-07-04 |
| DE60029954D1 (de) | 2006-09-21 |
| NO323856B1 (no) | 2007-07-16 |
| CA2376819C (en) | 2008-09-02 |
| BR0011028A (pt) | 2002-02-19 |
| NO20016037L (no) | 2002-02-11 |
| NZ515143A (en) | 2004-05-28 |
| US6413987B1 (en) | 2002-07-02 |
| WO2000076510A1 (en) | 2000-12-21 |
| AU777517B2 (en) | 2004-10-21 |
| JP2003501469A (ja) | 2003-01-14 |
| NO20016037D0 (no) | 2001-12-10 |
| EP1185267A4 (en) | 2003-09-03 |
| DK1185267T3 (da) | 2006-12-11 |
| MXPA01012632A (es) | 2004-03-19 |
| ATE335482T1 (de) | 2006-09-15 |
| CN1355700A (zh) | 2002-06-26 |
| ES2267546T3 (es) | 2007-03-16 |
| DE60029954T2 (de) | 2007-03-08 |
| CY1105721T1 (el) | 2010-12-22 |
| EP1185267B1 (en) | 2006-08-09 |
| CA2376819A1 (en) | 2000-12-21 |
| IL146190A (en) | 2008-11-03 |
| AU5596300A (en) | 2001-01-02 |
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