PE20110834A1 - DERIVADOS DE PIRROL[3,4-d]PIRIMIDINA COMO INHIBIDORES DE FOSFODIESTERASA 1 (PDE1) - Google Patents
DERIVADOS DE PIRROL[3,4-d]PIRIMIDINA COMO INHIBIDORES DE FOSFODIESTERASA 1 (PDE1)Info
- Publication number
- PE20110834A1 PE20110834A1 PE2011001168A PE2011001168A PE20110834A1 PE 20110834 A1 PE20110834 A1 PE 20110834A1 PE 2011001168 A PE2011001168 A PE 2011001168A PE 2011001168 A PE2011001168 A PE 2011001168A PE 20110834 A1 PE20110834 A1 PE 20110834A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- pyrrol
- pde1
- phosphodiesterase
- inhibitors
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines 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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/42—Amides
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/06—Antiabortive agents; Labour repressants
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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
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
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- A—HUMAN NECESSITIES
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- 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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- 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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- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q7/00—Preparations for affecting hair growth
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Physical Education & Sports Medicine (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Rheumatology (AREA)
- Cardiology (AREA)
- Gynecology & Obstetrics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Ophthalmology & Optometry (AREA)
- Heart & Thoracic Surgery (AREA)
- Birds (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Psychology (AREA)
- Pregnancy & Childbirth (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
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Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE (5- O 7-AMINO)-3,4-DIHIDRO-(OPCIONALMENTE 4-OXO, 4-TIOXO O 4-IMINO)-1H-PIRROL[3,4-d]PIRIMIDIN-2(6H)-ONA DE FORMULA (II-A) O (II-B) DONDE Q ES -C(=S)-, -C(=O)-, ENTRE OTROS; R1 ES H O ALQUILO(C1-C6); R2 ES H, ALQUILO(C1-C6) OPCIONALMENTE SUSTITUIDO CON HALO O HIDROXI, ARILALQUILO(C0-C6), ENTRE OTROS; R3 ES HETEROALQUILO, -D-E-F, ENTRE OTROS, EN DONDE D ES UN ENLACE SIMPLE, ALQUILENO(C1-C6) O ARILALQUILENO; E ES UN ENLACE SIMPLE, ALQUILENO(C1-C4), ALQUINILENO(C2-C6), ENTRE OTROS; F ES H, HALO, ALQUILO(C1-C6), ENTRE OTROS; R4 Y R5 SON CADA UNO H, ALQUILO(C1-C6), CICLOALQUILO(C3-C8), ENTRE OTROS; R6 ES H, ALQUILO(C1-C6), ALCOXI(C1-C6), ARILOXI, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-(4-(6-FLUOROPIRIDIN-2-IL)BENCIL)-1-ISOBUTIL-3-METIL-7-(FENILAMINO)-1H-PIRROL[3,4-d]PIRIMIDINA-2,4(3H,6H)-DIONA; 6-(4-(6-FLUOROPIRIDIN-2-IL)BENCIL)-3-METIL-1-NEOPENTIL-7-(FENILAMINO)-1H-PIRROL[3,4-d]PIRIMIDINA-2,4(3H,6H)-DIONA; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE FOSFODIESTERASA 1 (PDE1) SIENDO UTILES EN EL TRATAMIENTO DE LA ENFERMEDAD DE PARKINSON, DEPRESION, NARCOLEPSIA, ESQUIZOFRENIA
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US12044308P | 2008-12-06 | 2008-12-06 | |
US23588809P | 2009-08-21 | 2009-08-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20110834A1 true PE20110834A1 (es) | 2011-12-14 |
Family
ID=42233531
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2011001168A PE20110834A1 (es) | 2008-12-06 | 2009-12-07 | DERIVADOS DE PIRROL[3,4-d]PIRIMIDINA COMO INHIBIDORES DE FOSFODIESTERASA 1 (PDE1) |
Country Status (21)
Country | Link |
---|---|
US (2) | US8927556B2 (es) |
EP (1) | EP2367428B1 (es) |
JP (1) | JP5710492B2 (es) |
KR (1) | KR20110098730A (es) |
CN (1) | CN102238873A (es) |
AU (1) | AU2009322899A1 (es) |
BR (1) | BRPI0922809A2 (es) |
CA (1) | CA2740385A1 (es) |
CO (1) | CO6390080A2 (es) |
CR (1) | CR20110311A (es) |
DO (1) | DOP2011000171A (es) |
EA (1) | EA201170768A1 (es) |
EC (1) | ECSP11011185A (es) |
ES (1) | ES2580759T3 (es) |
IL (1) | IL213316A0 (es) |
MA (1) | MA32939B1 (es) |
MX (1) | MX2011005935A (es) |
PE (1) | PE20110834A1 (es) |
TN (1) | TN2011000244A1 (es) |
WO (1) | WO2010065147A1 (es) |
ZA (1) | ZA201103630B (es) |
Families Citing this family (57)
Publication number | Priority date | Publication date | Assignee | Title |
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EP1888534B1 (en) | 2005-06-06 | 2017-07-26 | Intra-Cellular Therapies, Inc. | Organic compounds |
CA2651519A1 (en) | 2006-06-06 | 2007-12-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
EP2081431B1 (en) * | 2006-11-13 | 2013-01-16 | Intra-Cellular Therapies, Inc. | Organic compounds |
JP5837278B2 (ja) | 2006-12-05 | 2015-12-24 | イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. | 新規使用 |
KR101227738B1 (ko) | 2007-12-06 | 2013-01-29 | 다케다 야쿠힌 고교 가부시키가이샤 | 유기 화합물 |
EP2240028B1 (en) * | 2007-12-06 | 2016-07-20 | Intra-Cellular Therapies, Inc. | Pyrazolopyrimidine-4,6-dione derivatives and their use as pharmaceutical |
ES2551133T3 (es) * | 2008-12-06 | 2015-11-16 | Intra-Cellular Therapies, Inc. | Compuestos de 4,5,7,8-tetrahidro-4-oxo-2H-imidazo[1,2-a]pirrolo[3,4-e]pirimidina como inhibidores de PDE1 |
JP5813511B2 (ja) | 2008-12-06 | 2015-11-17 | イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. | 有機化合物 |
WO2010065151A1 (en) | 2008-12-06 | 2010-06-10 | Intra-Cellular Therapies, Inc. | Organic compounds |
JP5778582B2 (ja) | 2008-12-06 | 2015-09-16 | イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. | 有機化合物 |
MA32940B1 (fr) | 2008-12-06 | 2012-01-02 | Intra Cellular Therapies Inc | Composes organiques |
WO2010098839A1 (en) | 2009-02-25 | 2010-09-02 | Intra-Cellular Therapies, Inc. | Pde 1 inhibitors for ophthalmic disorders |
EP2434895A4 (en) | 2009-05-13 | 2013-08-07 | Intra Cellular Therapies Inc | ORGANIC CONNECTIONS |
WO2011043816A1 (en) | 2009-10-08 | 2011-04-14 | Intra-Cellular Therapies, Inc. | Phosphodiesterase 1-targeting tracers and methods |
TW201206937A (en) | 2010-05-31 | 2012-02-16 | Intra Cellular Therapies Inc | Organic compounds |
US9763948B2 (en) | 2010-05-31 | 2017-09-19 | Intra-Cellular Therapies, Inc. | PDE1 inhibitory compounds and methods |
US9434730B2 (en) | 2010-05-31 | 2016-09-06 | Intra-Cellular Therapies, Inc. | PDE1 inhibitor compounds |
US9371327B2 (en) | 2010-05-31 | 2016-06-21 | Intra-Cellular Therapies, Inc. | PDE1 inhibitor compounds |
WO2012171016A1 (en) | 2011-06-10 | 2012-12-13 | Intra-Cellular Therapies, Inc. | Organic compounds |
LT2782584T (lt) | 2011-11-23 | 2021-09-10 | Therapeuticsmd, Inc. | Natūralios kombinuotos pakaitinės hormonų terapijos kompozicijos ir gydymas |
US9301920B2 (en) | 2012-06-18 | 2016-04-05 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
US20150196640A1 (en) | 2012-06-18 | 2015-07-16 | Therapeuticsmd, Inc. | Progesterone formulations having a desirable pk profile |
US10806740B2 (en) | 2012-06-18 | 2020-10-20 | Therapeuticsmd, Inc. | Natural combination hormone replacement formulations and therapies |
US20130338122A1 (en) | 2012-06-18 | 2013-12-19 | Therapeuticsmd, Inc. | Transdermal hormone replacement therapies |
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- 2009-12-07 KR KR1020117013107A patent/KR20110098730A/ko not_active Application Discontinuation
- 2009-12-07 BR BRPI0922809A patent/BRPI0922809A2/pt not_active IP Right Cessation
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- 2009-12-07 JP JP2011539518A patent/JP5710492B2/ja not_active Expired - Fee Related
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AU2009322899A1 (en) | 2010-06-10 |
US8927556B2 (en) | 2015-01-06 |
US20150353556A1 (en) | 2015-12-10 |
DOP2011000171A (es) | 2011-10-31 |
TN2011000244A1 (en) | 2012-12-17 |
MA32939B1 (fr) | 2012-01-02 |
ES2580759T3 (es) | 2016-08-26 |
WO2010065147A1 (en) | 2010-06-10 |
EP2367428B1 (en) | 2016-04-06 |
BRPI0922809A2 (pt) | 2018-05-29 |
EA201170768A1 (ru) | 2012-05-30 |
IL213316A0 (en) | 2011-07-31 |
CN102238873A (zh) | 2011-11-09 |
US20120136013A1 (en) | 2012-05-31 |
KR20110098730A (ko) | 2011-09-01 |
EP2367428A1 (en) | 2011-09-28 |
CA2740385A1 (en) | 2010-06-10 |
MX2011005935A (es) | 2011-12-16 |
EP2367428A4 (en) | 2012-06-06 |
CR20110311A (es) | 2011-11-10 |
ECSP11011185A (es) | 2011-10-31 |
JP5710492B2 (ja) | 2015-04-30 |
CO6390080A2 (es) | 2012-02-29 |
JP2012510991A (ja) | 2012-05-17 |
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