EA014706B1 - КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 1-БЕНЗОИЛ-4-[2-[4-МЕТОКСИ-7-(3-МЕТИЛ-1H-1,2,4-ТРИАЗОЛ-1-ИЛ)-1-[(ФОСФОНОКСИ)МЕТИЛ]-1H-ПИРРОЛО[2,3-c]ПИРИДИН-3-ИЛ]-1,2-ДИОКСОЭТИЛ]ПИПЕРАЗИНА - Google Patents
КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 1-БЕНЗОИЛ-4-[2-[4-МЕТОКСИ-7-(3-МЕТИЛ-1H-1,2,4-ТРИАЗОЛ-1-ИЛ)-1-[(ФОСФОНОКСИ)МЕТИЛ]-1H-ПИРРОЛО[2,3-c]ПИРИДИН-3-ИЛ]-1,2-ДИОКСОЭТИЛ]ПИПЕРАЗИНА Download PDFInfo
- Publication number
- EA014706B1 EA014706B1 EA200801529A EA200801529A EA014706B1 EA 014706 B1 EA014706 B1 EA 014706B1 EA 200801529 A EA200801529 A EA 200801529A EA 200801529 A EA200801529 A EA 200801529A EA 014706 B1 EA014706 B1 EA 014706B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- crystalline form
- compound
- form according
- methyl
- temperature
- Prior art date
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- 239000003921 oil Substances 0.000 description 1
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- QELSKZZBTMNZEB-UHFFFAOYSA-N p-hydroxybenzoic acid propyl ester Natural products CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 1
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- VUNXBQRNMNVUMV-UHFFFAOYSA-N phenyl(piperazin-1-yl)methanone Chemical group C=1C=CC=CC=1C(=O)N1CCNCC1 VUNXBQRNMNVUMV-UHFFFAOYSA-N 0.000 description 1
- UYWQUFXKFGHYNT-UHFFFAOYSA-N phenylmethyl ester of formic acid Natural products O=COCC1=CC=CC=C1 UYWQUFXKFGHYNT-UHFFFAOYSA-N 0.000 description 1
- 125000004592 phthalazinyl group Chemical group C1(=NN=CC2=CC=CC=C12)* 0.000 description 1
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- 230000000069 prophylactic effect Effects 0.000 description 1
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- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 description 1
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- 229960003415 propylparaben Drugs 0.000 description 1
- 238000010926 purge Methods 0.000 description 1
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- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
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- 235000019204 saccharin Nutrition 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
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- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 229960001852 saquinavir Drugs 0.000 description 1
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- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- WRIKHQLVHPKCJU-UHFFFAOYSA-N sodium bis(trimethylsilyl)amide Chemical compound C[Si](C)(C)N([Na])[Si](C)(C)C WRIKHQLVHPKCJU-UHFFFAOYSA-N 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
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- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 235000010265 sodium sulphite Nutrition 0.000 description 1
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- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical class OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 description 1
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- MSXVEPNJUHWQHW-UHFFFAOYSA-N tertiary amyl alcohol Natural products CCC(C)(C)O MSXVEPNJUHWQHW-UHFFFAOYSA-N 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- OSBSFAARYOCBHB-UHFFFAOYSA-N tetrapropylammonium Chemical compound CCC[N+](CCC)(CCC)CCC OSBSFAARYOCBHB-UHFFFAOYSA-N 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
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- 125000001425 triazolyl group Chemical group 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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Classifications
-
- 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
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/08—Esters of oxyacids of phosphorus
- C07F9/09—Esters of phosphoric acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Communicable Diseases (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
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| US75024705P | 2005-12-14 | 2005-12-14 | |
| PCT/US2006/047571 WO2007070589A2 (en) | 2005-12-14 | 2006-12-13 | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1h-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1h-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA200801529A1 EA200801529A1 (ru) | 2009-02-27 |
| EA014706B1 true EA014706B1 (ru) | 2011-02-28 |
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| EA200801529A EA014706B1 (ru) | 2005-12-14 | 2006-12-13 | КРИСТАЛЛИЧЕСКИЕ ФОРМЫ 1-БЕНЗОИЛ-4-[2-[4-МЕТОКСИ-7-(3-МЕТИЛ-1H-1,2,4-ТРИАЗОЛ-1-ИЛ)-1-[(ФОСФОНОКСИ)МЕТИЛ]-1H-ПИРРОЛО[2,3-c]ПИРИДИН-3-ИЛ]-1,2-ДИОКСОЭТИЛ]ПИПЕРАЗИНА |
Country Status (17)
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|---|---|
| US (1) | US7851476B2 (https=) |
| EP (1) | EP1963342A2 (https=) |
| JP (1) | JP5400387B2 (https=) |
| KR (1) | KR20080077010A (https=) |
| CN (1) | CN101365708B (https=) |
| AU (1) | AU2006326432B2 (https=) |
| BR (1) | BRPI0619851A2 (https=) |
| CA (1) | CA2635717A1 (https=) |
| EA (1) | EA014706B1 (https=) |
| GE (1) | GEP20125413B (https=) |
| IL (1) | IL191769A (https=) |
| MY (1) | MY144293A (https=) |
| NO (1) | NO20082477L (https=) |
| NZ (2) | NZ568776A (https=) |
| UA (1) | UA94928C2 (https=) |
| WO (1) | WO2007070589A2 (https=) |
| ZA (1) | ZA200805063B (https=) |
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| RU2663466C1 (ru) * | 2017-03-20 | 2018-08-06 | Общество с ограниченной ответственностью "МБА-групп" | Композиция для профилактики и/или лечения вич-инфекции |
| RU2778508C1 (ru) * | 2021-03-31 | 2022-08-22 | Общество с ограниченной ответственностью «29 февраля» | Кристаллическая форма моноэтаноламин 3'-[(2Z)-2-[1-(3,4-диметилфенил)-1,5-дигидро-3-метил-5-оксо-4Н-пиразол-4-илиден]гидразино]-2'-гидрокси-[1,1'-бифенил]-3-карбоновой кислоты |
| US12180185B2 (en) | 2018-11-15 | 2024-12-31 | Hk Inno.N Corporation | Compound as protein kinase inhibitor, and pharmaceutical composition comprising thereof |
| US12365665B2 (en) | 2019-04-30 | 2025-07-22 | Beijing Tide Pharmaceutical Co., Ltd. | Solid form of diaminopyrimidine compound or hydrate thereof, preparation method therefor, and application thereof |
| US12384774B2 (en) | 2019-06-06 | 2025-08-12 | Genfleet Therapeutics (Shanghai) Inc. | Polymorph of CDK9 inhibitor and preparation method for polymorph and use thereof |
| US12419877B2 (en) | 2013-11-15 | 2025-09-23 | Akebia Therapeutics, Inc. | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof |
| US12479839B2 (en) | 2019-08-06 | 2025-11-25 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Crystalline form of ATR inhibitor and use thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040110785A1 (en) * | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US7745625B2 (en) * | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| JP5433690B2 (ja) | 2008-06-25 | 2014-03-05 | ブリストル−マイヤーズ スクイブ カンパニー | 抗−ｈｉｖ薬としてのジケト縮合アゾロピペリジンおよびアゾロピペラジン |
| JP5433691B2 (ja) * | 2008-06-25 | 2014-03-05 | ブリストル−マイヤーズ スクイブ カンパニー | Ｈｉｖ結合阻害剤としてのジケトピペリジン誘導体 |
| WO2010028108A2 (en) * | 2008-09-04 | 2010-03-11 | Bristol-Myers Squibb Company | Stable pharmaceutical composition for optimized delivery of an hiv attachment inhibitor |
| WO2012075235A1 (en) | 2010-12-02 | 2012-06-07 | Bristol-Myers Squibb Company | Alkyl amides as hiv attachment inhibitors |
| WO2012106189A1 (en) * | 2011-01-31 | 2012-08-09 | Bristol-Myers Squibb Company | Methods of making hiv attachment inhibitor prodrug compound and intermediates |
| ES2636312T3 (es) | 2011-04-12 | 2017-10-05 | VIIV Healthcare UK (No.5) Limited | Derivados de tioamida, amidoxima y amidrazona como inhibidores de la fijación del VIH |
| ES2609579T3 (es) | 2011-08-29 | 2017-04-21 | VIIV Healthcare UK (No.5) Limited | Derivados espiro de diamina bicíclica como inhibidores de la unión del VIH |
| EP2751119B1 (en) | 2011-08-29 | 2016-11-23 | VIIV Healthcare UK (No.5) Limited | Fused bicyclic diamine derivatives as hiv attachment inhibitors |
| WO2013138436A1 (en) | 2012-03-14 | 2013-09-19 | Bristol-Myers Squibb Company | Cyclolic hydrazine derivatives as hiv attachment inhibitors |
| EP2895472B1 (en) | 2012-08-09 | 2016-11-23 | VIIV Healthcare UK (No.5) Limited | Tricyclic alkene derivatives as HIV attachment inhibitors |
| ES2616492T3 (es) | 2012-08-09 | 2017-06-13 | VIIV Healthcare UK (No.5) Limited | Derivados de piperidina amida como inhibidores de la fijación del VIH |
| FI3645001T3 (fi) | 2017-06-29 | 2024-09-25 | G1 Therapeutics Inc | Git38:n morfisia muotoja ja niiden valmistusmenetelmiä |
| US11548895B2 (en) | 2019-04-24 | 2023-01-10 | Elanco Us Inc. | Process for making crystalline 2-(3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(cyclopropylsulfonyl)azetidin-3-yl)acetonitrile |
| WO2021007189A1 (en) | 2019-07-08 | 2021-01-14 | Rezolute, Inc. | Crystalline forms of plasma kallikrein inhibitors |
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| US20050209246A1 (en) * | 2004-03-15 | 2005-09-22 | Yasutsugu Ueda | Prodrugs of piperazine and substituted piperidine antiviral agents |
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- 2006-12-13 BR BRPI0619851-1A patent/BRPI0619851A2/pt not_active Application Discontinuation
- 2006-12-13 EP EP06848592A patent/EP1963342A2/en not_active Withdrawn
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| RU2663466C1 (ru) * | 2017-03-20 | 2018-08-06 | Общество с ограниченной ответственностью "МБА-групп" | Композиция для профилактики и/или лечения вич-инфекции |
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| RU2843869C2 (ru) * | 2019-04-24 | 2025-07-21 | Эланко Юс Инк. | Ингибиторы jak на основе 7h-пирроло[2,3-d]пиримидина |
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| US12516036B2 (en) | 2019-05-31 | 2026-01-06 | Hyundai Pharm Co., Ltd. | Crystal form of 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative |
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| US12384774B2 (en) | 2019-06-06 | 2025-08-12 | Genfleet Therapeutics (Shanghai) Inc. | Polymorph of CDK9 inhibitor and preparation method for polymorph and use thereof |
| RU2832707C2 (ru) * | 2019-08-06 | 2024-12-27 | Уси Байосити Байофармасьютикс Ко., Лтд. | Кристаллическая форма ингибитора atr и ее применение |
| US12479839B2 (en) | 2019-08-06 | 2025-11-25 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Crystalline form of ATR inhibitor and use thereof |
| RU2847971C2 (ru) * | 2019-12-05 | 2025-10-15 | Ле Лаборатуар Сервье | Новые кристаллические формы mcl-1 ингибитора, способ их получения и содержащие их фармацевтические композиции |
| RU2829609C1 (ru) * | 2020-07-02 | 2024-11-01 | Гуанчжоу Хэлсквест Фармасьютикалс Ко., Лтд. | Кристаллы алкинилсодержащего соединения, его соли и сольвата, способ его получения и пути применения |
| RU2854496C1 (ru) * | 2020-07-24 | 2026-01-13 | Шанхай Хансох Биомедикал Ко., Лтд. | Кристаллическая форма свободного основания производного пиридазина, способ ее получения и применение |
| RU2858128C2 (ru) * | 2020-11-13 | 2026-03-12 | Шанхай Ханьсох Байомедикал Ко., Лтд. | Кристаллическая форма свободного основания ингибитора, предусматривающего производное на основе бициклического кольца, а также способ ее получения (варианты), фармацевтическая композиция, содержащая ее, и применения кристаллической формы (варианты) |
| RU2778508C1 (ru) * | 2021-03-31 | 2022-08-22 | Общество с ограниченной ответственностью «29 февраля» | Кристаллическая форма моноэтаноламин 3'-[(2Z)-2-[1-(3,4-диметилфенил)-1,5-дигидро-3-метил-5-оксо-4Н-пиразол-4-илиден]гидразино]-2'-гидрокси-[1,1'-бифенил]-3-карбоновой кислоты |
Also Published As
| Publication number | Publication date |
|---|---|
| EP1963342A2 (en) | 2008-09-03 |
| ZA200805063B (en) | 2009-10-28 |
| JP2009521414A (ja) | 2009-06-04 |
| AU2006326432A1 (en) | 2007-06-21 |
| IL191769A0 (en) | 2008-12-29 |
| US20070155702A1 (en) | 2007-07-05 |
| KR20080077010A (ko) | 2008-08-20 |
| AU2006326432B2 (en) | 2012-07-12 |
| WO2007070589A2 (en) | 2007-06-21 |
| NO20082477L (no) | 2008-09-05 |
| EA200801529A1 (ru) | 2009-02-27 |
| BRPI0619851A2 (pt) | 2011-10-25 |
| CN101365708B (zh) | 2012-12-12 |
| US7851476B2 (en) | 2010-12-14 |
| WO2007070589A3 (en) | 2007-09-27 |
| MY144293A (en) | 2011-08-29 |
| UA94928C2 (en) | 2011-06-25 |
| JP5400387B2 (ja) | 2014-01-29 |
| IL191769A (en) | 2011-08-31 |
| GEP20125413B (en) | 2012-03-12 |
| NZ568776A (en) | 2011-06-30 |
| CN101365708A (zh) | 2009-02-11 |
| NZ592684A (en) | 2012-07-27 |
| CA2635717A1 (en) | 2007-06-21 |
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