HRP20080490T3 - 3-fluoro-piperidines as nmda/nr2b antagonists - Google Patents
3-fluoro-piperidines as nmda/nr2b antagonistsInfo
- Publication number
- HRP20080490T3 HRP20080490T3 HR20080490T HRP20080490T HRP20080490T3 HR P20080490 T3 HRP20080490 T3 HR P20080490T3 HR 20080490 T HR20080490 T HR 20080490T HR P20080490 T HRP20080490 T HR P20080490T HR P20080490 T3 HRP20080490 T3 HR P20080490T3
- Authority
- HR
- Croatia
- Prior art keywords
- aryl
- nmda
- piperidines
- fluoro
- nr2b antagonists
- Prior art date
Links
- YUKQZLBLVRAJSW-UHFFFAOYSA-N 3-fluoropiperidine Chemical class FC1CCCNC1 YUKQZLBLVRAJSW-UHFFFAOYSA-N 0.000 title 1
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 4
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 2
- 229910052801 chlorine Inorganic materials 0.000 abstract 2
- 239000000460 chlorine Substances 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 239000011737 fluorine Substances 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 abstract 1
- 229910052794 bromium Inorganic materials 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000003392 indanyl group Chemical group C1(CCC2=CC=CC=C12)* 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 239000011630 iodine Substances 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
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- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
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- A—HUMAN NECESSITIES
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
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- A61P27/16—Otologicals
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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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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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
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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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- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
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- A—HUMAN NECESSITIES
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- 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
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
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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
- A61P9/10—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
- 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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Virology (AREA)
- Addiction (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Communicable Diseases (AREA)
- Endocrinology (AREA)
- Molecular Biology (AREA)
- Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Biotechnology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- AIDS & HIV (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US47593803P | 2003-06-04 | 2003-06-04 | |
PCT/US2004/017175 WO2004108705A1 (en) | 2003-06-04 | 2004-05-28 | 3-fluoro-piperidines as nmda/nr2b antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20080490T3 true HRP20080490T3 (en) | 2008-11-30 |
Family
ID=33511734
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HR20080490T HRP20080490T3 (en) | 2003-06-04 | 2008-10-01 | 3-fluoro-piperidines as nmda/nr2b antagonists |
Country Status (30)
Country | Link |
---|---|
EP (1) | EP1648882B1 (no) |
JP (1) | JP3927228B2 (no) |
KR (1) | KR20060017839A (no) |
CN (1) | CN1798744A (no) |
AR (1) | AR044579A1 (no) |
AT (1) | ATE403651T1 (no) |
AU (1) | AU2004245522B2 (no) |
BR (1) | BRPI0410837A (no) |
CA (1) | CA2527093C (no) |
CL (1) | CL2004001365A1 (no) |
CO (1) | CO5700762A2 (no) |
DE (1) | DE602004015610D1 (no) |
DK (1) | DK1648882T3 (no) |
EC (1) | ECSP056192A (no) |
ES (1) | ES2309540T3 (no) |
HR (1) | HRP20080490T3 (no) |
IS (1) | IS8117A (no) |
MA (1) | MA27781A1 (no) |
MX (1) | MXPA05013151A (no) |
MY (1) | MY138547A (no) |
NO (1) | NO20060020L (no) |
PE (1) | PE20050245A1 (no) |
PL (1) | PL1648882T3 (no) |
PT (1) | PT1648882E (no) |
RU (1) | RU2339630C2 (no) |
SI (1) | SI1648882T1 (no) |
TW (1) | TW200510378A (no) |
UA (1) | UA81319C2 (no) |
WO (1) | WO2004108705A1 (no) |
ZA (1) | ZA200509000B (no) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2009535364A (ja) * | 2006-05-03 | 2009-10-01 | シーエヌエスバイオ ピーティーワイ リミテッド | 炎症性疼痛の治療のための方法および組成物 |
KR101506156B1 (ko) * | 2007-04-23 | 2015-03-26 | 얀센 파마슈티카 엔.브이. | 속해리성 도파민 2 수용체 길항제로서의 티아(디아)졸 |
WO2009000038A1 (en) * | 2007-06-28 | 2008-12-31 | Cnsbio Pty Ltd | Combination methods and compositions for treatment of neuropathic pain |
CN102762554A (zh) | 2010-02-16 | 2012-10-31 | 辉瑞大药厂 | 5-ht4受体的部分激动剂(r)-4-((4-((4-(四氢呋喃-3-基氧基)苯并[d]异*唑-3-基氧基)甲基)哌啶-1-基)甲基)四氢-2h-吡喃-4-醇 |
JP6042968B2 (ja) | 2012-04-20 | 2016-12-14 | ユセベ ファルマ ソシエテ アノニム | パーキンソン病の処置方法 |
CN103936663B (zh) * | 2013-01-23 | 2016-12-28 | 艾琪康医药科技(上海)有限公司 | 一种1-r1-3,3-二氟(或3-氟)-4-r2-4-氨甲基哌啶及其衍生物的制备方法 |
US9187506B2 (en) | 2014-01-09 | 2015-11-17 | Bristol-Myers Squibb Company | (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one and its prodrugs for the treatment of psychiatric disorders |
US9221796B2 (en) | 2014-01-09 | 2015-12-29 | Bristol-Myers Squibb Company | Selective NR2B antagonists |
US10030026B2 (en) | 2014-06-04 | 2018-07-24 | Rugen Holdings (Cayman) Limited | Difluoroethylpyridine derivatives as NR2B NMDA receptor antagonists |
CN106715435B (zh) | 2014-09-15 | 2019-10-01 | 卢郡控股(开曼)有限公司 | 作为nr2b nmda受体拮抗剂的吡咯并嘧啶衍生物 |
WO2016049048A1 (en) * | 2014-09-22 | 2016-03-31 | Rugen Holdings (Cayman) Limited | Treatment of anxiety disorders and autism spectrum disorders |
BR112017013593A2 (pt) * | 2014-12-23 | 2018-06-19 | Cerecor, Inc. | compostos, composições e métodos |
US10221182B2 (en) | 2015-02-04 | 2019-03-05 | Rugen Holdings (Cayman) Limited | 3,3-difluoro-piperidine derivatives as NR2B NMDA receptor antagonists |
JP6876625B2 (ja) | 2015-06-01 | 2021-05-26 | リューゲン ホールディングス (ケイマン) リミテッド | Nr2bnmdaレセプターアンタゴニストとしての3,3−ジフルオロピペリジンカルバメート複素環式化合物 |
WO2017066368A1 (en) | 2015-10-14 | 2017-04-20 | Bristol-Myers Squibb Company | Selective nr2b antagonists |
CN108137543B (zh) | 2015-10-14 | 2021-11-23 | 百时美施贵宝公司 | 选择性nr2b拮抗剂 |
AU2017319080B2 (en) | 2016-08-31 | 2020-12-17 | Eisai R&D Management Co., Ltd. | Pyrazolo[1,5-a]pyrimidine compound |
EP3544610A1 (en) | 2016-11-22 | 2019-10-02 | Rugen Holdings (Cayman) Limited | Treatment of autism spectrum disorders, obsessive-compulsive disorder and anxiety disorders |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI1379520T1 (sl) * | 2001-02-23 | 2006-08-31 | Merck & Co Inc | N-substituirani nonaril-heterociklicni NMDA/NR2B antagonisti |
-
2004
- 2004-05-28 SI SI200430845T patent/SI1648882T1/sl unknown
- 2004-05-28 KR KR1020057023218A patent/KR20060017839A/ko not_active Application Discontinuation
- 2004-05-28 RU RU2005137704/04A patent/RU2339630C2/ru not_active IP Right Cessation
- 2004-05-28 JP JP2006515051A patent/JP3927228B2/ja not_active Expired - Lifetime
- 2004-05-28 PT PT04753896T patent/PT1648882E/pt unknown
- 2004-05-28 CN CNA2004800153228A patent/CN1798744A/zh active Pending
- 2004-05-28 DK DK04753896T patent/DK1648882T3/da active
- 2004-05-28 ES ES04753896T patent/ES2309540T3/es not_active Expired - Lifetime
- 2004-05-28 EP EP04753896A patent/EP1648882B1/en not_active Expired - Lifetime
- 2004-05-28 MX MXPA05013151A patent/MXPA05013151A/es active IP Right Grant
- 2004-05-28 PL PL04753896T patent/PL1648882T3/pl unknown
- 2004-05-28 CA CA002527093A patent/CA2527093C/en not_active Expired - Lifetime
- 2004-05-28 AT AT04753896T patent/ATE403651T1/de not_active IP Right Cessation
- 2004-05-28 WO PCT/US2004/017175 patent/WO2004108705A1/en active Application Filing
- 2004-05-28 BR BRPI0410837-0A patent/BRPI0410837A/pt not_active IP Right Cessation
- 2004-05-28 AU AU2004245522A patent/AU2004245522B2/en not_active Expired
- 2004-05-28 DE DE602004015610T patent/DE602004015610D1/de not_active Expired - Lifetime
- 2004-05-28 UA UAA200511411A patent/UA81319C2/uk unknown
- 2004-05-31 AR ARP040101878A patent/AR044579A1/es unknown
- 2004-05-31 MY MYPI20042091A patent/MY138547A/en unknown
- 2004-06-01 PE PE2004000552A patent/PE20050245A1/es not_active Application Discontinuation
- 2004-06-03 CL CL200401365A patent/CL2004001365A1/es unknown
- 2004-06-03 TW TW093115972A patent/TW200510378A/zh unknown
-
2005
- 2005-11-07 ZA ZA200509000A patent/ZA200509000B/en unknown
- 2005-11-07 IS IS8117A patent/IS8117A/is unknown
- 2005-11-28 MA MA28626A patent/MA27781A1/fr unknown
- 2005-11-29 EC EC2005006192A patent/ECSP056192A/es unknown
- 2005-11-30 CO CO05121658A patent/CO5700762A2/es not_active Application Discontinuation
-
2006
- 2006-01-03 NO NO20060020A patent/NO20060020L/no not_active Application Discontinuation
-
2008
- 2008-10-01 HR HR20080490T patent/HRP20080490T3/xx unknown
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