DK200001151A - Ny krystallinsk form af 6-hydorxy-3-(-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]tihiophen hydrochlorid - Google Patents
Ny krystallinsk form af 6-hydorxy-3-(-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]tihiophen hydrochlorid Download PDFInfo
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- DK200001151A DK200001151A DK200001151A DKPA200001151A DK200001151A DK 200001151 A DK200001151 A DK 200001151A DK 200001151 A DK200001151 A DK 200001151A DK PA200001151 A DKPA200001151 A DK PA200001151A DK 200001151 A DK200001151 A DK 200001151A
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- piperidin
- benzo
- phenoxy
- ethoxy
- hydroxy
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
- C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
- C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
- C07D333/64—Oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/435—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
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
- A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
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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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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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
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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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
- A61P25/28—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
- A61P3/00—Drugs for disorders of the metabolism
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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
- A61P3/06—Antihyperlipidemics
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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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
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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
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/30—Oestrogens
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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
- A61P5/32—Antioestrogens
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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
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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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Biomedical Technology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Reproductive Health (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Description
Patentkrav : 1. Krystallinsk 6-hydroxy-3-(4-[2-(piperidin-l-yl)-ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen hy-drochlorid hydrat (F-I), der har et røntgenstrålediffraktionsmønster, som omfatter de følgende toppe: 7,9 +_0,2, 10,7 +0,2, 14,9 +0,2, 15,9 +0,2, 18,3 +0,2 og 20,6 +0,2° i 2Θ, når det er opnået fra en kobberbestrålingskilde. 2. Lægemiddelformulering omfattende den krystallinske forbindelse ifølge krav 1, en eller flere lægemiddelbærere, fortyndingsmidler eller excipiens, og eventuelt østrogen, eventuelt progestin, eventuelt en aromatasein-hibitor, eventuelt en LHRH-analog og eventuelt en acetyl-cholinesterase(AChE)inhibitor. 3. Formulering ifølge krav 2, som omfatter den krystallinske forbindelse ifølge krav 1, en eller flere lægemiddelbærere, fortyndingsmidler eller excipiens, og østrogen . 4. Formulering ifølge krav 3, hvori østrogenet er Prema-rin®. 5. Formulering ifølge krav 2, som omfatter den krystallinske forbindelse ifølge krav 1, en eller flere lægemiddelbærere, fortyndingsmidler eller excipiens og progestin . 6. Formulering ifølge krav 5, hvori progestinet er valgt blandt gruppen bestående af norethylnodrel og norethin-dron. 7. Formulering ifølge krav 2, som omfatter den krystallinske forbindelse ifølge krav 1, en eller flere lægemiddelbærere, fortyndingsmidler eller excipiens og en AChE-inhibitor. 8. Formulering ifølge krav 7, hvori AChE-inhibitoren er valgt blandt gruppen bestående af physostigminsalicylat, tacrin hydrochlorid og donepezil hydrochlorid. 9. Formulering ifølge krav 2, som omfatter den krystallinske forbindelse ifølge krav 1, en eller flere lægemiddelbærere, fortyndingsmidler eller excipiens, østrogen og progestin. 10. Forbindelsen ifølge krav 1 til undertrykkelse af patologiske tilstande valgt blandt gruppen bestående af livmoderfibrosis, endometriosis, aortal glatmuskelcelle-formering, restenosis, brystcancer, livmodercancer, pro-statacancer, godartet prostata-hyperplasia, bentab, osteoporosis, hjerte/karsygdomme, hyperlipidomia, CNS-forstyrrelser og Alzheimers syge. 11. Forbindelsen ifølge krav 10 til undertrykkelse af brystcancer. 12. Forbindelsen ifølge krav 11, hvori undertrykkelsesmåden er profylaktisk. 13. Forbindelsen ifølge krav 10 til undertrykkelse af ovariecancer. 14. Forbindelsen ifølge krav 10 til undertrykkelse af en-dometrial cancer. 15. Forbindelsen ifølge krav 1 til opregulering af cho-lin-acetyltransferase (ChAT) i pattedyr. 16. Fremgangsmåde til fremstilling af forbindelse ifølge krav 1, som omfatter krystallisering af 6-hydroxy-3-(4-[2-(piperidin-l-yl)ethoxyjphenoxy)-2-(4-methoxy-phenyl)-benzo[b]thiophen hydrochlorid fra tetrahydrofuran.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14628699P | 1999-07-29 | 1999-07-29 | |
US14757099P | 1999-08-06 | 1999-08-06 | |
US14977399P | 1999-08-19 | 1999-08-19 |
Publications (1)
Publication Number | Publication Date |
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DK200001151A true DK200001151A (da) | 2001-01-30 |
Family
ID=27386379
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK200001151A DK200001151A (da) | 1999-07-29 | 2000-07-28 | Ny krystallinsk form af 6-hydorxy-3-(-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]tihiophen hydrochlorid |
Country Status (45)
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE251151T1 (de) * | 1999-07-29 | 2003-10-15 | Lilly Co Eli | Eine kristalline form von 6-hydroxy-3-(4-(2- (piperidin-1-yl)ethoxy)phenoxy)-2-(4- methoxyphenyl)benzo(b)thiophen-hydrochlorid |
US7122203B2 (en) | 2000-05-08 | 2006-10-17 | Eli Lilly And Company | Stabilized formulations of 6-hydroxy-3-(-4-[2-(piperidin-1-yl) ethoxy]phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene and salts thereof |
BR0110620A (pt) * | 2000-05-08 | 2003-04-01 | Lilly Co Eli | Formulações estabilizadas de 6-hidróxi-3-(4-[2-(piperidin-1-il)etóxi]fenóxi)-2-(4-metoxi fenil)benzo[b]tiofeno e de sais do mesmo |
EP1757291A3 (en) * | 2000-05-08 | 2009-07-15 | Eli Lilly & Company | Stabilized formulations of 6-hydroxy-3-(4-[2-(piperidin-1-YL)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene and salts thereof |
EP1157996A1 (de) * | 2000-05-23 | 2001-11-28 | JENAPHARM GmbH | Neue Festkörperformen des Mesoprogestins 11Beta-[4E-(Hydroxyiminomethyl)-phenyl]-17Alpha-methoxymethyl-17Beta-methoxy-estra-4,9-dien-3-on |
KR20030037690A (ko) * | 2000-10-20 | 2003-05-14 | 일라이 릴리 앤드 캄파니 | 6-히드록시-3-(4-[2-(피페리딘-1-일)에톡시]페녹시)-2-(4-메톡시페닐)벤조[b]티오펜 히드로클로라이드의 신규 결정형 |
US6921827B2 (en) | 2000-11-27 | 2005-07-26 | Eli Lilly And Company | Process for preparing 3-aryl-benzo{b} thiophenes |
CA2393720C (en) * | 2002-07-12 | 2010-09-14 | Eli Lilly And Company | Crystalline 2,5-dione-3-(1-methyl-1h-indol-3-yl)-4-[1-(pyridin-2-ylmethyl)piperidin-4-yl]-1h-indol-3-yl]-1h-pyrrole mono-hydrochloride |
PL1773811T3 (pl) * | 2004-07-22 | 2011-02-28 | Lilly Co Eli | Krystaliczny zmienny hydrat soli hemibursztynianowej (s)-6-(4-(2-((3(9h-karbazol-4-iloksy)-2-hydroksypropylo)amino)-2-metylopropylo)fenoksy)-3-pirydynokarboksy amidu |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PE44597A1 (es) * | 1995-02-28 | 1997-10-13 | Lilly Co Eli | Compuestos de benzotiofeno, productos intermedios, composiciones y procedimientos |
US5510357A (en) | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
ZA9710262B (en) * | 1996-11-19 | 1999-05-13 | Lilly Co Eli | Process for the synthesis of benzothiophenes |
ZA982877B (en) * | 1997-04-09 | 1999-10-04 | Lilly Co Eli | Treatment of central nervous system disorders with selective estrogen receptor modulators. |
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2000
- 2000-07-17 WO PCT/US2000/016333 patent/WO2001009116A2/en not_active Application Discontinuation
- 2000-07-17 AU AU63356/00A patent/AU6335600A/en not_active Abandoned
- 2000-07-17 EP EP00950223A patent/EP1204656A2/en not_active Ceased
- 2000-07-18 LV LVP-00-94A patent/LV12623B/en unknown
- 2000-07-21 RO ROA200000736A patent/RO121851B1/ro unknown
- 2000-07-24 ID IDP20000629D patent/ID27078A/id unknown
- 2000-07-24 CZ CZ20002716A patent/CZ299311B6/cs not_active IP Right Cessation
- 2000-07-25 HR HR20000503A patent/HRP20000503B1/xx not_active IP Right Cessation
- 2000-07-27 NL NL1015821A patent/NL1015821C2/nl not_active IP Right Cessation
- 2000-07-27 TR TR2000/02206A patent/TR200002206A2/xx unknown
- 2000-07-27 IL IL13755300A patent/IL137553A/xx not_active IP Right Cessation
- 2000-07-27 CO CO00056521A patent/CO5180570A1/es active IP Right Grant
- 2000-07-28 DE DE10036854A patent/DE10036854A1/de not_active Withdrawn
- 2000-07-28 FI FI20001722A patent/FI20001722A/fi unknown
- 2000-07-28 SV SV2000000132A patent/SV2002000132A/es unknown
- 2000-07-28 AR ARP000103928A patent/AR031073A1/es unknown
- 2000-07-28 KR KR1020000043651A patent/KR100697177B1/ko not_active IP Right Cessation
- 2000-07-28 MY MYPI20003453A patent/MY128764A/en unknown
- 2000-07-28 HU HU0003001A patent/HUP0003001A2/hu unknown
- 2000-07-28 MX MXPA00007461A patent/MXPA00007461A/es active IP Right Grant
- 2000-07-28 PT PT102502A patent/PT102502A/pt not_active IP Right Cessation
- 2000-07-28 IT IT2000MI001759A patent/IT1318660B1/it active
- 2000-07-28 DK DK200001151A patent/DK200001151A/da not_active Application Discontinuation
- 2000-07-28 SE SE0002792A patent/SE0002792L/xx unknown
- 2000-07-28 LT LT2000076A patent/LT4790B/lt not_active IP Right Cessation
- 2000-07-28 SI SI200000172A patent/SI20426A/sl not_active IP Right Cessation
- 2000-07-28 BE BE2000/0478A patent/BE1013411A3/fr not_active IP Right Cessation
- 2000-07-28 NO NO20003879A patent/NO20003879L/no not_active Application Discontinuation
- 2000-07-28 LU LU90617A patent/LU90617B1/fr active
- 2000-07-28 CA CA002314682A patent/CA2314682A1/en not_active Abandoned
- 2000-07-28 UA UA2000074563A patent/UA72885C2/uk unknown
- 2000-07-28 GR GR20000100265A patent/GR1004084B/el unknown
- 2000-07-28 FR FR0009969A patent/FR2796944B1/fr not_active Expired - Fee Related
- 2000-07-28 GB GB0018641A patent/GB2352717A/en not_active Withdrawn
- 2000-07-28 CN CNB001222376A patent/CN1138770C/zh not_active Expired - Fee Related
- 2000-07-28 PL PL00341749A patent/PL341749A1/xx not_active Application Discontinuation
- 2000-07-28 TW TW089115154A patent/TWI276437B/zh not_active IP Right Cessation
- 2000-07-28 SG SG200004288A patent/SG91296A1/en unknown
- 2000-07-28 JP JP2000228939A patent/JP2001064277A/ja active Pending
- 2000-07-28 AT AT0132400A patent/AT502318A1/de not_active Application Discontinuation
- 2000-07-28 MD MDA20000162A patent/MD2336G2/ro not_active IP Right Cessation
- 2000-07-28 BR BR0003209-3A patent/BR0003209A/pt not_active Application Discontinuation
- 2000-07-29 DZ DZ000126A patent/DZ3060A1/xx active
- 2000-07-31 PE PE2000000757A patent/PE20010385A1/es not_active Application Discontinuation
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2001
- 2001-09-03 HK HK01106204A patent/HK1035370A1/xx not_active IP Right Cessation
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