AR046133A1 - Derivados de benzazepina como inhibidores de mao-b, procesos para su obtencion, composiciones farmaceuticas que los contienen y su utilizacion en la fabricacion de medicamentos para el tratamiento de trastornos neurologicos - Google Patents
Derivados de benzazepina como inhibidores de mao-b, procesos para su obtencion, composiciones farmaceuticas que los contienen y su utilizacion en la fabricacion de medicamentos para el tratamiento de trastornos neurologicosInfo
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- AR046133A1 AR046133A1 ARP040103808A ARP040103808A AR046133A1 AR 046133 A1 AR046133 A1 AR 046133A1 AR P040103808 A ARP040103808 A AR P040103808A AR P040103808 A ARP040103808 A AR P040103808A AR 046133 A1 AR046133 A1 AR 046133A1
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- alkyl
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/14—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D223/16—Benzazepines; Hydrogenated benzazepines
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
- C07D213/16—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
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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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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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
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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
- A61P25/04—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
- A61P25/06—Antimigraine agents
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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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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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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
- A61P25/22—Anxiolytics
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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
- A61P25/24—Antidepressants
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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
- A61P25/28—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Psychology (AREA)
- Addiction (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Nutrition Science (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
La presente se refiere a derivados de benzazepina como inhibidores de MAO-B., composiciones farmacéuticas que contienen a dichos derivados y a su utilización para la fabricación de medicamentos útiles para la prevención y tratamiento de enfermedades en las que desempena un papel o está implicada la inhibición selectiva de la actividad de la monoamina oxidasa B. Reivindicación 1: Un compuesto de la fórmula (1) en la que R1 es H o metilo; R2 es H, alquilo C1-3, -CH2C(O)NH2, -CH(CH3)C(O)NH2, - S(O)2CH3 o -C(O)R6; R3, R4 y R5 con independencia entre si son H, halógeno, ciano, alquilo C1-3 u -O-alquilo C1-3-; R6 es H, -CH3, -CH2OCH3, -C(O)NH2, -CH2C(O)NH2, -OCH3, -NH2 o -NHCH2CH3, X-X´es-CH2-CH2-, -CH=CH- o -CH2-C(O)-; y Y-Y´ es -CH2-CH2-; - CH=CH- o -CH2-C(O)-; o X-X´ es -CH2- e Y-Y´ es -CH2-CH2-C(O)-; en la que cuando uno de X-X´e Y-Y´es -CH2-CH2- y el otro es -CH=CH-, o cuando los dos X-X´e Y-Y´son -CH=CH-, entonces R2 es -S(O)2CH3 o -C(O)R6; o cuando X-X´e Y-Y´son -CH2-C(O)- entonces R2 es H, alquilo C1-3, -CH2C(O)NH2 o -CH(CH3)C(O)NH2; y las sales farmacéuticamente aceptables de los mismos. Reivindicación 15: Un proceso de obtención de un compuesto de la fórmula (1) según la reivindicación 1 en la que R1 es H o metilo; R2 es H, R3, R4 y R5 con independencia entre si son H, halógeno, ciano, alquilo C1-3 u -O-alquilo C1-3; X-X´es-CH2-CH2-, -CH=CH- o -CH2-C(O)-; y Y-Y´ es -CH2-CH2-; -CH=CH- o -CH2-C(O)-; o X-X´ es -CH2- e Y-Y´ es -CH2-CH2-C(O)-; en la que cuando uno de X-X´e Y-Y´es -CH2-CH2- y el otro es -CH=CH-, o cuando los dos X-X´e Y-Y´son -CH=CH-, entonces R2 es -S(O)2CH3 o -C(O)R6; o cuando X-X´e Y-Y´son -CH2-C(O)- entonces R2 es H, alquilo C1-3, -CH2C(O)NH2 o -CH(CH3)C(O)NH2; que consiste en eliminar un grupo protector de un compuesto de la fórmula (2) en la que p1 es un grupo protector, elegido entre un grupo tert-butoxicarbonilo, metoxicarbonilo y 9-fluorenil-metoxi-carbonilo. Reivindicación 16: Un proceso de obtención de un compuesto de la fórmula (1) según la reivindicación 1 en la que: R1 es H o metilo; R2 es H, alquilo C1-3, -CH2C(O)NH2, -CH(CH3)C(O)NH2, -S(O)2CH3 o -C(O)R6; R3, R4 y R5 con independencia entre si son H, halógeno, ciano, alquilo C1-3 u -O-alquilo C1- 3-; R6 es H, -CH3, -CH2OCH3, -C(O)NH2, -CH2C(O)NH2, -OCH3, -NH2 o -NHCH2CH3, X-X´es-CH2-CH2-, -CH=CH- o -CH2-C(O)-; y Y-Y´ es -CH2-CH2-; -CH=CH- o -CH2-C(O)-; o X-X´ es -CH2- e Y-Y´ es -CH2-CH2-C(O)-; en la que cuando uno de X-X´e Y-Y´es -CH2-CH2- y el otro es -CH=CH-, o cuando los dos X-X´e Y-Y´son -CH=CH-, entonces R3 es -S(O)2CH3 o -C(O)R6; o cuando X-X´e Y-Y´son -CH2-C(O)- entonces R3 es H, alquilo C1-3, -CH2C(O)NH2 o -CH(CH3)C(O)NH2; que consiste en hacer reaccionar un compuesto de la fórmula (39 con un compuesto de la fórmula (4) en las que Z es OH, o cuando R2 es -S(O)2CH3 o -C(O)R6, entonces Z puede ser halógeno o un resto ácido sulfónico.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP03024297 | 2003-10-23 |
Publications (1)
Publication Number | Publication Date |
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AR046133A1 true AR046133A1 (es) | 2005-11-23 |
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ARP040103808A AR046133A1 (es) | 2003-10-23 | 2004-10-21 | Derivados de benzazepina como inhibidores de mao-b, procesos para su obtencion, composiciones farmaceuticas que los contienen y su utilizacion en la fabricacion de medicamentos para el tratamiento de trastornos neurologicos |
Country Status (19)
Country | Link |
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US (2) | US7173023B2 (es) |
EP (1) | EP1680127B1 (es) |
JP (1) | JP2007509094A (es) |
KR (1) | KR100856141B1 (es) |
CN (1) | CN100441188C (es) |
AR (1) | AR046133A1 (es) |
AT (1) | ATE411027T1 (es) |
AU (1) | AU2004283452A1 (es) |
BR (1) | BRPI0415842A (es) |
CA (1) | CA2543287A1 (es) |
CO (1) | CO5680409A2 (es) |
DE (1) | DE602004017206D1 (es) |
IL (1) | IL174845A0 (es) |
MX (1) | MXPA06004307A (es) |
NO (1) | NO20061907L (es) |
RU (1) | RU2006117366A (es) |
TW (1) | TWI254707B (es) |
WO (1) | WO2005039591A1 (es) |
ZA (1) | ZA200603177B (es) |
Families Citing this family (7)
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RU2423353C1 (ru) | 2002-12-20 | 2011-07-10 | Глэксо Груп Лимитед | Новые производные бензазепина |
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US20070293475A1 (en) * | 2006-06-20 | 2007-12-20 | Alcon Manufacturing Ltd. | Aryl and heteroaryl tetrahydrobenzazepine derivatives and their use for treating glaucoma |
FR2932800B1 (fr) * | 2008-06-20 | 2015-02-20 | Servier Lab | Nouveau procede de synthese de la 7,8-dimethoxy-1,3-dihydro- 2h-3-benzazepin-2-one, et application a la synthese de l'ivabradine et de ses sels d'addition a un acide pharmaceutiquement acceptable |
KR101220182B1 (ko) * | 2009-02-25 | 2013-01-11 | 에스케이바이오팜 주식회사 | 치환된 아졸 유도체 화합물, 이를 포함하는 약제학적 조성물 및 이를 이용한 파킨슨씨 병 치료방법 |
JP6346658B2 (ja) | 2013-03-14 | 2018-06-20 | ダート・ニューロサイエンス・(ケイマン)・リミテッド | Mao阻害剤としての置換ナフチリジン及びキノリン化合物 |
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US6660736B2 (en) * | 2002-03-27 | 2003-12-09 | Hoffmann-La Roche Inc. | Phthalimido derivatives and a process for their preparation |
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JP4322685B2 (ja) * | 2002-04-26 | 2009-09-02 | エフ.ホフマン−ラ ロシュ アーゲー | イソキノリン誘導体 |
WO2003099763A1 (en) * | 2002-05-29 | 2003-12-04 | F. Hoffmann-La Roche Ag | N-acylaminobenzene dervatives as selective monoamine oxidase b inhibitors |
RU2423353C1 (ru) * | 2002-12-20 | 2011-07-10 | Глэксо Груп Лимитед | Новые производные бензазепина |
WO2005042491A1 (en) * | 2003-10-22 | 2005-05-12 | Arena Pharmaceuticals, Inc. | Benzazepine derivatives and methods of prophylaxis or treatment of 5ht2c receptor associated diseases |
-
2004
- 2004-10-14 EP EP04790400A patent/EP1680127B1/en active Active
- 2004-10-14 CA CA002543287A patent/CA2543287A1/en not_active Abandoned
- 2004-10-14 JP JP2006536004A patent/JP2007509094A/ja active Pending
- 2004-10-14 MX MXPA06004307A patent/MXPA06004307A/es not_active Application Discontinuation
- 2004-10-14 DE DE602004017206T patent/DE602004017206D1/de not_active Expired - Fee Related
- 2004-10-14 AT AT04790400T patent/ATE411027T1/de not_active IP Right Cessation
- 2004-10-14 AU AU2004283452A patent/AU2004283452A1/en not_active Abandoned
- 2004-10-14 WO PCT/EP2004/011541 patent/WO2005039591A1/en active Application Filing
- 2004-10-14 RU RU2006117366/04A patent/RU2006117366A/ru not_active Application Discontinuation
- 2004-10-14 KR KR1020067007779A patent/KR100856141B1/ko not_active IP Right Cessation
- 2004-10-14 BR BRPI0415842-3A patent/BRPI0415842A/pt not_active IP Right Cessation
- 2004-10-14 CN CNB2004800309236A patent/CN100441188C/zh not_active Expired - Fee Related
- 2004-10-18 US US10/967,567 patent/US7173023B2/en not_active Expired - Fee Related
- 2004-10-20 TW TW093131855A patent/TWI254707B/zh not_active IP Right Cessation
- 2004-10-21 AR ARP040103808A patent/AR046133A1/es unknown
-
2006
- 2006-04-06 IL IL174845A patent/IL174845A0/en unknown
- 2006-04-18 CO CO06036626A patent/CO5680409A2/es not_active Application Discontinuation
- 2006-04-20 ZA ZA200603177A patent/ZA200603177B/en unknown
- 2006-04-28 NO NO20061907A patent/NO20061907L/no not_active Application Discontinuation
-
2007
- 2007-01-12 US US11/652,970 patent/US20070117791A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
IL174845A0 (en) | 2006-08-20 |
EP1680127A1 (en) | 2006-07-19 |
KR20060061390A (ko) | 2006-06-07 |
CN100441188C (zh) | 2008-12-10 |
TWI254707B (en) | 2006-05-11 |
KR100856141B1 (ko) | 2008-09-03 |
US20070117791A1 (en) | 2007-05-24 |
CN1871013A (zh) | 2006-11-29 |
US7173023B2 (en) | 2007-02-06 |
MXPA06004307A (es) | 2006-06-05 |
RU2006117366A (ru) | 2007-12-10 |
NO20061907L (no) | 2006-07-12 |
BRPI0415842A (pt) | 2007-01-02 |
WO2005039591A1 (en) | 2005-05-06 |
AU2004283452A1 (en) | 2005-05-06 |
EP1680127B1 (en) | 2008-10-15 |
JP2007509094A (ja) | 2007-04-12 |
ZA200603177B (en) | 2007-09-26 |
CO5680409A2 (es) | 2006-09-29 |
CA2543287A1 (en) | 2005-05-06 |
US20050107360A1 (en) | 2005-05-19 |
TW200524875A (en) | 2005-08-01 |
ATE411027T1 (de) | 2008-10-15 |
DE602004017206D1 (de) | 2008-11-27 |
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