CN1353717A - 四环黄体酮受体调节剂化合物及其方法 - Google Patents
四环黄体酮受体调节剂化合物及其方法 Download PDFInfo
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- CN1353717A CN1353717A CN00808438A CN00808438A CN1353717A CN 1353717 A CN1353717 A CN 1353717A CN 00808438 A CN00808438 A CN 00808438A CN 00808438 A CN00808438 A CN 00808438A CN 1353717 A CN1353717 A CN 1353717A
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- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 description 1
- 229940049953 phenylacetate Drugs 0.000 description 1
- WLJVXDMOQOGPHL-UHFFFAOYSA-N phenylacetic acid Chemical compound OC(=O)CC1=CC=CC=C1 WLJVXDMOQOGPHL-UHFFFAOYSA-N 0.000 description 1
- 150000003016 phosphoric acids Chemical class 0.000 description 1
- 229940075930 picrate Drugs 0.000 description 1
- OXNIZHLAWKMVMX-UHFFFAOYSA-M picrate anion Chemical compound [O-]C1=C([N+]([O-])=O)C=C([N+]([O-])=O)C=C1[N+]([O-])=O OXNIZHLAWKMVMX-UHFFFAOYSA-M 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 150000004885 piperazines Chemical class 0.000 description 1
- 239000002798 polar solvent Substances 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- 239000001103 potassium chloride Substances 0.000 description 1
- 235000011164 potassium chloride Nutrition 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 239000000583 progesterone congener Substances 0.000 description 1
- QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 description 1
- 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 238000004445 quantitative analysis Methods 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 238000001959 radiotherapy Methods 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 238000001525 receptor binding assay Methods 0.000 description 1
- 229940075993 receptor modulator Drugs 0.000 description 1
- 238000009256 replacement therapy Methods 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-M salicylate Chemical compound OC1=CC=CC=C1C([O-])=O YGSDEFSMJLZEOE-UHFFFAOYSA-M 0.000 description 1
- 229960001860 salicylate Drugs 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 238000011935 selective methylation Methods 0.000 description 1
- 230000008313 sensitization Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 230000014639 sexual reproduction Effects 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 229960001866 silicon dioxide Drugs 0.000 description 1
- 238000004088 simulation Methods 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 159000000000 sodium salts Chemical class 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 239000008247 solid mixture Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 101150008563 spir gene Proteins 0.000 description 1
- 229940114926 stearate Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 230000003637 steroidlike Effects 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 150000003558 thiocarbamic acid derivatives Chemical class 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 238000006257 total synthesis reaction Methods 0.000 description 1
- WBYWAXJHAXSJNI-VOTSOKGWSA-M trans-cinnamate Chemical compound [O-]C(=O)\C=C\C1=CC=CC=C1 WBYWAXJHAXSJNI-VOTSOKGWSA-M 0.000 description 1
- 238000003146 transient transfection Methods 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 238000010626 work up procedure Methods 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US30461499A | 1999-05-04 | 1999-05-04 | |
US09/304,614 | 1999-05-04 | ||
US09/552,353 US6358947B1 (en) | 1999-05-04 | 2000-04-19 | Tetracyclic progesterone receptor modulator compounds and methods |
US09/552,353 | 2000-04-19 |
Publications (1)
Publication Number | Publication Date |
---|---|
CN1353717A true CN1353717A (zh) | 2002-06-12 |
Family
ID=26974128
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN00808438A Pending CN1353717A (zh) | 1999-05-04 | 2000-05-01 | 四环黄体酮受体调节剂化合物及其方法 |
Country Status (6)
Country | Link |
---|---|
EP (1) | EP1175422A2 (fr) |
CN (1) | CN1353717A (fr) |
AU (1) | AU4501800A (fr) |
CA (1) | CA2371273A1 (fr) |
HK (1) | HK1043788A1 (fr) |
WO (1) | WO2000066590A2 (fr) |
Families Citing this family (61)
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KR100864547B1 (ko) * | 1999-08-31 | 2008-10-20 | 바이엘 쉐링 파마 악티엔게젤샤프트 | 양성 호르몬 의존성 부인과 질병의 치료 및 예방을 위한메조프로게스틴 (프로게스테론 수용체 조절물질) |
PL353994A1 (en) * | 1999-08-31 | 2003-12-15 | Jenapharm Gmbh & Co.Kgjenapharm Gmbh & Co.Kg | Mesoprogestins (progesterone receptor modulators) as a component of female contraceptives |
US8193252B1 (en) | 1999-08-31 | 2012-06-05 | Bayer Pharma AG | Mesoprogestins (progesterone receptor modulators) for the treatment and prevention of benign hormone dependent gynecological disorders |
EP1558618A1 (fr) | 2002-10-11 | 2005-08-03 | Ligand Pharmaceuticals, Inc. | 5-(1',1'-cycloalkyl/alcenyl)methylidene 1,2-dihydro- i 5h /i -chromeno 3,4- i f /i ]quinolines utilisees comme composes modulateurs du recepteur de la progesterone selectifs |
TW200410968A (en) | 2002-10-11 | 2004-07-01 | Ligand Pharm Inc | 5-cycloalkenyl 5H-chromeno[3,4-f]quinoline derivatives as selective progesterone receptor modulator compounds |
GB0316290D0 (en) | 2003-07-11 | 2003-08-13 | Glaxo Group Ltd | Novel compounds |
WO2005090282A1 (fr) | 2004-03-12 | 2005-09-29 | Ligand Pharmaceuticals Incorporated | Composes modulateurs de recepteur d'androgenes et procedes |
AR049384A1 (es) | 2004-05-24 | 2006-07-26 | Glaxo Group Ltd | Derivados de purina |
TWI307630B (en) | 2004-07-01 | 2009-03-21 | Glaxo Group Ltd | Immunoglobulins |
US7579335B2 (en) | 2005-01-10 | 2009-08-25 | Glaxo Group Limited | Androstane 17α-carbonate derivatives for use in the treatment of allergic and inflammatory conditions |
AR053450A1 (es) | 2005-03-25 | 2007-05-09 | Glaxo Group Ltd | Derivados de 3,4-dihidro-pirimido(4,5-d)pirimidin-2-(1h)-ona 1,5,7 trisustituidos como inhibidores de la quinasa p38 |
MY145281A (en) | 2005-03-25 | 2012-01-13 | Glaxo Group Ltd | Novel compounds |
DE102005030294A1 (de) * | 2005-06-24 | 2007-01-04 | Schering Ag | Nichtsteroidale Progesteronrezeptor-Modulatoren |
GB0514809D0 (en) | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
AR058109A1 (es) | 2005-12-20 | 2008-01-23 | Glaxo Group Ltd | Acido 3 - (4 - {[4 -(4 -{[3 - (3, 3 - dimetil - 1 - piperidinil)propil]oxi}fenil) - 1 - piperidinil]carbonil} - 1 - naftalenil)propanoico como antagonistas de los receptotres de histamina h1/h3, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamie |
CA2649509A1 (fr) | 2006-04-20 | 2007-11-01 | Glaxo Group Limited | Nouveaux composes |
GB0611587D0 (en) | 2006-06-12 | 2006-07-19 | Glaxo Group Ltd | Novel compounds |
MX2010012814A (es) | 2008-05-23 | 2010-12-20 | Amira Pharmaceuticals Inc | Inhibidor de proteina activadora de 5-lipoxigenasa. |
EP2280959B1 (fr) | 2008-06-05 | 2012-04-04 | Glaxo Group Limited | 4-amino-indazoles |
WO2009147187A1 (fr) | 2008-06-05 | 2009-12-10 | Glaxo Group Limited | Dérivés de 4-carboxamide indazole utiles en tant qu'inhibiteurs de p13 kinases |
WO2010094643A1 (fr) | 2009-02-17 | 2010-08-26 | Glaxo Group Limited | Dérivés de quinoline et applications associées dans la rhinite et l'urticaire |
JP5656880B2 (ja) | 2009-03-09 | 2015-01-21 | グラクソ グループ リミテッドGlaxo Group Limited | Pi3キナーゼの阻害剤としての4−オキサジアゾール−2−イル−インダゾール |
JP2012520257A (ja) | 2009-03-10 | 2012-09-06 | グラクソ グループ リミテッド | Ikk2阻害剤としてのインドール誘導体 |
WO2010106016A1 (fr) | 2009-03-17 | 2010-09-23 | Glaxo Group Limited | Dérivés de pyrimidine utilisés comme inhibiteurs de ltk |
WO2010107958A1 (fr) | 2009-03-19 | 2010-09-23 | Merck Sharp & Dohme Corp. | INHIBITION INDUITE PAR ARN INTERFÉRENCE DE L'EXPRESSION DU GÈNE TRANSDUCTEUR DE SIGNAL ET ACTIVITATEUR DE TRANSCRIPTION 6 (STAT6) AU MOYEN D'UN ACIDE NUCLÉIQUE INTERFÉRENT COURT (ANsi) |
EP2408915A2 (fr) | 2009-03-19 | 2012-01-25 | Merck Sharp&Dohme Corp. | Inhibition induite par arn interférence d'une expression génique (gata3) d'une protéine de liaison gata au moyen d'un acide nucléique interférent court |
JP2012520684A (ja) | 2009-03-19 | 2012-09-10 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸(siNA)を用いたBTBandCNCHomology1(塩基性ロイシンジッパー転写因子1)(Bach1)遺伝子発現のRNA干渉媒介性阻害 |
JP2012520683A (ja) | 2009-03-19 | 2012-09-10 | メルク・シャープ・エンド・ドーム・コーポレイション | 低分子干渉核酸(siNA)を用いた結合組織増殖因子(CTGF)遺伝子発現のRNA干渉媒介性阻害 |
WO2010111471A2 (fr) | 2009-03-27 | 2010-09-30 | Merck Sharp & Dohme Corp. | Inhibition par interférence arn de l'expression du gène du signal transducteur et activateur de la transcription 1 (stat1) au moyen d'un acide nucléique interférent court (ansi) |
EP2411516A1 (fr) | 2009-03-27 | 2012-02-01 | Merck Sharp&Dohme Corp. | Inhibition par interférence arn de l'expression du gène kinase 1 de régulation du signal d'apoptose (ask1) au moyen d'un acide nucléique interférent court (ansi) |
US20120022143A1 (en) | 2009-03-27 | 2012-01-26 | Merck Sharp & Dohme Corp | RNA Interference Mediated Inhibition of the Thymic Stromal Lymphopoietin (TSLP) Gene Expression Using Short Interfering Nucliec Acid (siNA) |
US20120004281A1 (en) | 2009-03-27 | 2012-01-05 | Merck Sharp & Dohme Corp | RNA Interference Mediated Inhibition of the Nerve Growth Factor Beta Chain (NGFB) Gene Expression Using Short Interfering Nucleic Acid (siNA) |
US8399436B2 (en) | 2009-04-24 | 2013-03-19 | Glaxo Group Limited | N-pyrazolyl carboxamides as CRAC channel inhibitors |
EP2421834A1 (fr) | 2009-04-24 | 2012-02-29 | Glaxo Group Limited | Pyrazole et triazole carboxamides en tant qu'inhibiteurs du canal crac |
PL2899191T3 (pl) | 2009-04-30 | 2018-01-31 | Glaxo Group Ltd | Indazole podstawione oksazolem jako inhibitory kinazy PI3 |
WO2011067365A1 (fr) | 2009-12-03 | 2011-06-09 | Glaxo Group Limited | Dérivés de benzpyrazole comme inhibiteurs des pi3 kinases |
EP2507231A1 (fr) | 2009-12-03 | 2012-10-10 | Glaxo Group Limited | Dérivés d'indazole comme inhibiteurs des pi3-kinases |
US20120238559A1 (en) | 2009-12-03 | 2012-09-20 | Glaxo Group Limited | Novel compounds |
EP3020393B1 (fr) | 2009-12-16 | 2020-10-07 | 3M Innovative Properties Company | Formulations et procédés de commande de distribution granulométrique mdi |
WO2011110575A1 (fr) | 2010-03-11 | 2011-09-15 | Glaxo Group Limited | Dérivés de 2-[2-(benzo- ou pyrido-)thiazolylamino]-6- aminopyridine, utiles dans le traitement de maladies respiratoires, allergiques ou inflammatoires |
GB201007203D0 (en) | 2010-04-29 | 2010-06-16 | Glaxo Group Ltd | Novel compounds |
EP2613781B1 (fr) | 2010-09-08 | 2016-08-24 | GlaxoSmithKline Intellectual Property Development Limited | Dérivés indazole à utiliser dans le traitement d'une infection par le virus de la grippe |
PL2614058T3 (pl) | 2010-09-08 | 2015-12-31 | Glaxosmithkline Ip Dev Ltd | Polimorfy i sole n-[5-[4-(5-{[(2r,6s)-2,6-dimetylo-4-morfolinylo]-metylo}-1,3-oksazol-2-ilo)-1h-indazol-6-ilo]-2-(metyloksy)-3-pirydynylo]metanosulfonamidu |
WO2012035055A1 (fr) | 2010-09-17 | 2012-03-22 | Glaxo Group Limited | Nouveaux composés |
JP2013544794A (ja) | 2010-10-21 | 2013-12-19 | グラクソ グループ リミテッド | アレルギー性障害、炎症性障害及び免疫障害に作用するピラゾール化合物 |
ES2532213T3 (es) | 2010-10-21 | 2015-03-25 | Glaxo Group Limited | Compuestos de pirazol que actúan contra afecciones alérgicas, inmunitarias e inflamatorias |
GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
JP2014507458A (ja) | 2011-03-11 | 2014-03-27 | グラクソ グループ リミテッド | Sykインヒビターとしてのピリド[3,4−B]ピラジン誘導体 |
GB201104153D0 (en) | 2011-03-11 | 2011-04-27 | Glaxo Group Ltd | Novel compounds |
SG11201600707QA (en) | 2013-09-22 | 2016-02-26 | Calitor Sciences Llc | Substituted aminopyrimidine compounds and methods of use |
CA2925064A1 (fr) | 2013-10-17 | 2015-04-23 | Glaxosmithkline Intellectual Property Development Limited | Inhibiteur de pi3k pour le traitement d'une maladie respiratoire |
JP2016537327A (ja) | 2013-10-17 | 2016-12-01 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | 呼吸器疾患の治療のためのpi3k阻害剤 |
JP6517319B2 (ja) | 2014-03-28 | 2019-05-22 | キャリター・サイエンシーズ・リミテッド・ライアビリティ・カンパニーCalitor Sciences, Llc | 置換されたヘテロアリール化合物および使用方法 |
EA201692111A1 (ru) | 2014-05-12 | 2017-08-31 | Глаксосмитклайн Интеллекчуал Проперти (№ 2) Лимитед | Фармацевтические композиции, содержащие данириксин, для лечения инфекционных заболеваний |
WO2017044434A1 (fr) | 2015-09-11 | 2017-03-16 | Sunshine Lake Pharma Co., Ltd. | Composés hétéroaryle substitués et leurs méthodes d'utilisation |
GB201602527D0 (en) | 2016-02-12 | 2016-03-30 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
EP3497100A1 (fr) | 2016-08-08 | 2019-06-19 | GlaxoSmithKline Intellectual Property Development Limited | Composés chimiques |
GB201706102D0 (en) | 2017-04-18 | 2017-05-31 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
GB201712081D0 (en) | 2017-07-27 | 2017-09-13 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
EP3710006A4 (fr) | 2017-11-19 | 2021-09-01 | Sunshine Lake Pharma Co., Ltd. | Composés hétéroaryle substitués et leurs méthodes d'utilisation |
EP4125919A1 (fr) | 2020-03-26 | 2023-02-08 | GlaxoSmithKline Intellectual Property Development Limited | Inhibiteurs de cathepsine pour la prévention ou le traitement d'infections virales |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
PT800519E (pt) * | 1994-12-22 | 2004-03-31 | Ligand Pharm Inc | Compostos moduladores de receptores de esteroides e metodos |
US5696130A (en) * | 1994-12-22 | 1997-12-09 | Ligand Pharmaceuticals Incorporated | Tricyclic steroid receptor modulator compounds and methods |
-
2000
- 2000-05-01 CA CA002371273A patent/CA2371273A1/fr not_active Abandoned
- 2000-05-01 AU AU45018/00A patent/AU4501800A/en not_active Abandoned
- 2000-05-01 EP EP00926495A patent/EP1175422A2/fr not_active Ceased
- 2000-05-01 CN CN00808438A patent/CN1353717A/zh active Pending
- 2000-05-01 WO PCT/US2000/011750 patent/WO2000066590A2/fr not_active Application Discontinuation
-
2002
- 2002-06-28 HK HK02104861.6A patent/HK1043788A1/zh unknown
Also Published As
Publication number | Publication date |
---|---|
WO2000066590A3 (fr) | 2001-02-08 |
CA2371273A1 (fr) | 2000-11-09 |
EP1175422A2 (fr) | 2002-01-30 |
WO2000066590A2 (fr) | 2000-11-09 |
AU4501800A (en) | 2000-11-17 |
HK1043788A1 (zh) | 2002-09-27 |
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