PE20001234A1 - Compuestos azabiciclicos sustituidos de heteroaril-aminoetil/benzisoxazol como antagonistas serotonergicos 5-ht1 - Google Patents
Compuestos azabiciclicos sustituidos de heteroaril-aminoetil/benzisoxazol como antagonistas serotonergicos 5-ht1Info
- Publication number
- PE20001234A1 PE20001234A1 PE1999001116A PE00111699A PE20001234A1 PE 20001234 A1 PE20001234 A1 PE 20001234A1 PE 1999001116 A PE1999001116 A PE 1999001116A PE 00111699 A PE00111699 A PE 00111699A PE 20001234 A1 PE20001234 A1 PE 20001234A1
- Authority
- PE
- Peru
- Prior art keywords
- fluoro
- compounds
- aminoethyl
- heteroaryl
- pyrid
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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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
- A61K31/495—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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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
- A61K31/495—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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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
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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
-
- 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
- A61P25/14—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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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
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Psychology (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Addiction (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hospice & Palliative Care (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Gynecology & Obstetrics (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Child & Adolescent Psychology (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)
Abstract
SE REFIERE A COMPUESTOS AZABICICLICOS HETEROARIL-AMINOETIL/BENZOISOXAZOL SUSTITUIDOS DE FORMULA I; DONDE R1, R2, R3, R4 SON H, ALQUILO C1-C4, ALCOXI C1-C4, (ALQUILO C1-C4)(ALCOXI C1-C4) OPCIONALMENTE SUSTITUIDOS CON F; X ES CH, N. SON COMPUESTOS PREFERIDOS (7R,9aS)-TRANS-[2-(5-FLUORO-BENZO[d]ISOXAZOL-3-IL)-OCTAHIDRO-PIRIDO[1,2-a]PIRAZIN-7-ILMETIL]-(5-FLUORO-PIRIMIDIN-2-IL)AMINA, (7R, 9aS)-CIS-[2-(5-FLUORO-BENZO[d]ISOXAZOL-3-IL)-OCTAHIDRO-PIRIDO[1,2-a]PIRAZIN-7-ILMETIL]PIRIMIDIN-2-IL)-AMINA, (7S,9aS)-CIS-[2-(5-FLUORO-BENZO[d]ISOXAZOL-3-IL)-OCTAHIDRO-PIRIDO[1,2-a]PIRAZIN-7-ILMETIL]-(5-FLUORO-PIRIDIN-2-IL)AMINA), ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION QUE COMPRENDE ADEMAS UN INHIBIDOR DE LA RECAPTACION DE 5-HT TAL COMO SERTRALINA. LOS COMPUESTOS I MODULAN LA NEUROTRASMISION SEROTONERGICA 5-HT1 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE HIPERTENSION, DEPRESION, TRASTORNO DE LA ANSIEDAD GENERALIZADA, FOBIAS, SINDROME DE ESTRES POST TRAUMATICO, EYACULACION PRECOZ, OBESIDAD, CEFALEA, MIGRANA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11395798P | 1998-12-28 | 1998-12-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20001234A1 true PE20001234A1 (es) | 2000-11-07 |
Family
ID=22352526
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1999001116A PE20001234A1 (es) | 1998-12-28 | 1999-11-04 | Compuestos azabiciclicos sustituidos de heteroaril-aminoetil/benzisoxazol como antagonistas serotonergicos 5-ht1 |
Country Status (43)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003065970A2 (en) * | 2001-02-20 | 2003-08-14 | Royal College Of Surgeons Ie | Treatment of fibromyalgia and related fatigue syndromes using pindolol |
| GB0203778D0 (en) * | 2002-02-18 | 2002-04-03 | Glaxo Group Ltd | Compounds |
| BRPI0408248A (pt) * | 2003-03-12 | 2006-03-01 | Pfizer Prod Inc | derivados azabicìclicos de piridiloximetila e de benzisoxazol |
| GB0316915D0 (en) * | 2003-07-18 | 2003-08-20 | Glaxo Group Ltd | Compounds |
| CA2555172A1 (en) * | 2004-01-29 | 2005-09-09 | Pfizer Products Inc. | Combinations of an atypical antipsychotic and an aminomethylpyridyloxymethyl/benzisoxazole azabicyclic derivatives for treating cns disorders |
| AR048112A1 (es) * | 2004-03-25 | 2006-03-29 | Solvay Pharm Bv | Derivados de 1-(2h-1-benzopiran-2-on-8-il)-piperazina para el tratamiento de dolor |
| AR049478A1 (es) | 2004-03-25 | 2006-08-09 | Solvay Pharm Bv | Un procedimiento para la preparacion de 3-amino-8-(1-piperazinil)-2h-1-benzopiran-2-ona. sales e hidratos y composiciones farmaceuticas. |
| US20080318926A1 (en) * | 2004-09-10 | 2008-12-25 | Pfizer Inc | Methods of Treating Mood Disorders Using Pyridyloxymethyl and Benzisoxazole Azabicyclic Derivatives |
| WO2006027692A2 (en) * | 2004-09-10 | 2006-03-16 | Pfizer Products Inc. | Methods of treating cognitive disorders using pyridyloxymethyl and benzisoxazole azabicyclic derivatives |
| DE102005026194A1 (de) * | 2005-06-06 | 2006-12-07 | Grünenthal GmbH | Substituierte N-Benzo[d]isoxazol-3-yl-amin-Derivate und deren Verwendung zur Herstellung von Arzneimitteln |
| WO2008019431A1 (en) * | 2006-08-14 | 2008-02-21 | Brc Operations Pty Limited | Method and compositions for simultaneously regulating memory and mood |
| WO2014078568A1 (en) | 2012-11-14 | 2014-05-22 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| WO2020183011A1 (en) | 2019-03-14 | 2020-09-17 | Institut Curie | Htr1d inhibitors and uses thereof in the treatment of cancer |
| WO2021127391A1 (en) * | 2019-12-20 | 2021-06-24 | The Jackson Laboratory | Molecular targets for addiction |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5157034A (en) * | 1991-02-27 | 1992-10-20 | Pfizer Inc. | Neuroleptic perhydro-1H-pyrido[1,2-a]pyrazines |
| GB9410512D0 (en) * | 1994-05-25 | 1994-07-13 | Smithkline Beecham Plc | Novel treatment |
| WO1995032967A1 (en) * | 1994-05-28 | 1995-12-07 | Smithkline Beecham Plc | Amide derivatives having 5ht1d-antagonist activity |
| CN1260781A (zh) * | 1997-04-18 | 2000-07-19 | 史密丝克莱恩比彻姆有限公司 | 具有综合的5ht1a、5ht1b和5ht1d受体拮抗剂活性的吲哚衍生物 |
| IT1293807B1 (it) * | 1997-08-01 | 1999-03-10 | Recordati Chem Pharm | Derivati 1- (n-fenilaminoalchil) piperazinici sostituiti alla posizione 2 dell'anello fenilico |
| PA8469101A1 (es) * | 1998-04-09 | 2000-09-29 | Pfizer Prod Inc | Ligandos azabiciclicos de receptores 5ht1 |
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1999
- 1999-03-11 UA UA2001064492A patent/UA62015C2/uk unknown
- 1999-04-11 AR ARP990105589A patent/AR024840A1/es unknown
- 1999-11-03 JP JP2000591039A patent/JP2002533463A/ja active Pending
- 1999-11-03 GE GEAP19995963A patent/GEP20043227B/en unknown
- 1999-11-03 OA OA1200100172A patent/OA11742A/en unknown
- 1999-11-03 HU HU0104852A patent/HUP0104852A3/hu unknown
- 1999-11-03 EE EEP200100346A patent/EE04439B1/xx not_active IP Right Cessation
- 1999-11-03 ID IDW00200101401A patent/ID30117A/id unknown
- 1999-11-03 DK DK99951040T patent/DK1140931T3/da active
- 1999-11-03 WO PCT/IB1999/001772 patent/WO2000039128A1/en active IP Right Grant
- 1999-11-03 SK SK900-2001A patent/SK9002001A3/sk unknown
- 1999-11-03 AP APAP/P/2001/002188A patent/AP2001002188A0/en unknown
- 1999-11-03 CZ CZ20012386A patent/CZ291163B6/cs not_active IP Right Cessation
- 1999-11-03 NZ NZ511964A patent/NZ511964A/en unknown
- 1999-11-03 DE DE69915113T patent/DE69915113T2/de not_active Expired - Fee Related
- 1999-11-03 IL IL14338599A patent/IL143385A0/xx unknown
- 1999-11-03 AU AU63614/99A patent/AU761711B2/en not_active Ceased
- 1999-11-03 ES ES99951040T patent/ES2214892T3/es not_active Expired - Lifetime
- 1999-11-03 PT PT99951040T patent/PT1140931E/pt unknown
- 1999-11-03 EP EP99951040A patent/EP1140931B1/en not_active Expired - Lifetime
- 1999-11-03 KR KR10-2001-7008261A patent/KR100417506B1/ko not_active IP Right Cessation
- 1999-11-03 CN CN99815202A patent/CN1332740A/zh active Pending
- 1999-11-03 CA CA002356985A patent/CA2356985C/en not_active Expired - Fee Related
- 1999-11-03 EA EA200100517A patent/EA003099B1/ru not_active IP Right Cessation
- 1999-11-03 YU YU44301A patent/YU44301A/sh unknown
- 1999-11-03 TR TR2001/01979T patent/TR200101979T2/xx unknown
- 1999-11-03 BR BR9916807-3A patent/BR9916807A/pt not_active Application Discontinuation
- 1999-11-03 AT AT99951040T patent/ATE260278T1/de not_active IP Right Cessation
- 1999-11-04 PE PE1999001116A patent/PE20001234A1/es not_active Application Discontinuation
- 1999-11-05 TW TW088119374A patent/TW523514B/zh not_active IP Right Cessation
- 1999-11-10 MA MA25844A patent/MA26706A1/fr unknown
- 1999-11-10 DZ DZ990233A patent/DZ2933A1/xx active
- 1999-11-17 TN TNTNSN99218A patent/TNSN99218A1/fr unknown
- 1999-11-18 CO CO99072703A patent/CO5150179A1/es unknown
- 1999-12-06 US US09/454,509 patent/US6525196B1/en not_active Expired - Fee Related
- 1999-12-07 PA PA19998486701A patent/PA8486701A1/es unknown
- 1999-12-23 GT GT199900224A patent/GT199900224A/es unknown
-
2001
- 2001-05-22 IS IS5951A patent/IS5951A/is unknown
- 2001-06-19 CR CR6398A patent/CR6398A/es not_active Application Discontinuation
- 2001-06-20 ZA ZA200105041A patent/ZA200105041B/en unknown
- 2001-06-27 NO NO20013215A patent/NO20013215L/no not_active Application Discontinuation
- 2001-06-28 HR HR20010488A patent/HRP20010488A2/hr not_active Application Discontinuation
- 2001-07-16 BG BG105710A patent/BG105710A/xx unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |