HRP20120377T1 - Alkiltiopirimidini kao antagonisti crth2 - Google Patents
Alkiltiopirimidini kao antagonisti crth2 Download PDFInfo
- Publication number
- HRP20120377T1 HRP20120377T1 HRP20120377AT HRP20120377T HRP20120377T1 HR P20120377 T1 HRP20120377 T1 HR P20120377T1 HR P20120377A T HRP20120377A T HR P20120377AT HR P20120377 T HRP20120377 T HR P20120377T HR P20120377 T1 HRP20120377 T1 HR P20120377T1
- Authority
- HR
- Croatia
- Prior art keywords
- alkyl
- trihalogen
- mono
- substituted
- optionally substituted
- Prior art date
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- -1 Alkylthio pyrimidines Chemical class 0.000 title claims abstract 24
- 239000005557 antagonist Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract 72
- 125000003118 aryl group Chemical group 0.000 claims abstract 30
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 29
- 239000001257 hydrogen Substances 0.000 claims abstract 29
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 26
- 125000004750 (C1-C6) alkylaminosulfonyl group Chemical group 0.000 claims abstract 24
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 24
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims abstract 19
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 18
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims abstract 17
- 229910052736 halogen Inorganic materials 0.000 claims abstract 16
- 150000002367 halogens Chemical class 0.000 claims abstract 16
- 150000001875 compounds Chemical class 0.000 claims abstract 15
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims abstract 14
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims abstract 12
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 claims abstract 12
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims abstract 12
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims abstract 12
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims abstract 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims abstract 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims abstract 12
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims abstract 12
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 11
- 150000003839 salts Chemical class 0.000 claims abstract 11
- 239000012453 solvate Substances 0.000 claims abstract 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims abstract 9
- 125000003545 alkoxy group Chemical group 0.000 claims abstract 8
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims abstract 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims abstract 6
- 125000005115 alkyl carbamoyl group Chemical group 0.000 claims abstract 6
- 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims abstract 6
- 125000001424 substituent group Chemical group 0.000 claims abstract 6
- 238000006467 substitution reaction Methods 0.000 claims abstract 6
- 150000002825 nitriles Chemical class 0.000 claims abstract 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims abstract 2
- 201000010099 disease Diseases 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 13
- 208000024891 symptom Diseases 0.000 claims 10
- 208000006673 asthma Diseases 0.000 claims 6
- 208000016557 Acute basophilic leukemia Diseases 0.000 claims 3
- 208000032671 Allergic granulomatous angiitis Diseases 0.000 claims 3
- 208000006344 Churg-Strauss Syndrome Diseases 0.000 claims 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims 3
- 206010010744 Conjunctivitis allergic Diseases 0.000 claims 3
- 208000011231 Crohn disease Diseases 0.000 claims 3
- 201000004624 Dermatitis Diseases 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 3
- 208000018428 Eosinophilic granulomatosis with polyangiitis Diseases 0.000 claims 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 3
- 208000019693 Lung disease Diseases 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 206010039085 Rhinitis allergic Diseases 0.000 claims 3
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 3
- 206010052568 Urticaria chronic Diseases 0.000 claims 3
- 208000002205 allergic conjunctivitis Diseases 0.000 claims 3
- 201000010105 allergic rhinitis Diseases 0.000 claims 3
- 206010003246 arthritis Diseases 0.000 claims 3
- 208000024998 atopic conjunctivitis Diseases 0.000 claims 3
- 201000008937 atopic dermatitis Diseases 0.000 claims 3
- 208000010668 atopic eczema Diseases 0.000 claims 3
- 230000001684 chronic effect Effects 0.000 claims 3
- 208000024376 chronic urticaria Diseases 0.000 claims 3
- 206010024378 leukocytosis Diseases 0.000 claims 3
- 230000000414 obstructive effect Effects 0.000 claims 3
- 201000009890 sinusitis Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 150000002431 hydrogen Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 230000037081 physical activity Effects 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 206010003557 Asthma exercise induced Diseases 0.000 claims 1
- 208000004657 Exercise-Induced Asthma Diseases 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 210000003651 basophil Anatomy 0.000 claims 1
- 125000005841 biaryl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 210000003979 eosinophil Anatomy 0.000 claims 1
- 208000024695 exercise-induced bronchoconstriction Diseases 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/38—One sulfur atom
-
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-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/58—Two sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Otolaryngology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Gynecology & Obstetrics (AREA)
- Rheumatology (AREA)
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Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US99538607P | 2007-09-25 | 2007-09-25 | |
| PCT/US2008/011053 WO2009042138A1 (en) | 2007-09-25 | 2008-09-24 | Alkylthio pyrimidines as crth2 antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20120377T1 true HRP20120377T1 (hr) | 2012-05-31 |
Family
ID=40039984
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20120377AT HRP20120377T1 (hr) | 2007-09-25 | 2012-05-03 | Alkiltiopirimidini kao antagonisti crth2 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US8324229B2 (es) |
| EP (1) | EP2205569B1 (es) |
| JP (1) | JP5524847B2 (es) |
| KR (1) | KR20100061747A (es) |
| CN (1) | CN101874023A (es) |
| AR (1) | AR068632A1 (es) |
| AT (1) | ATE547407T1 (es) |
| AU (1) | AU2008305632B2 (es) |
| BR (1) | BRPI0817319A2 (es) |
| CA (1) | CA2700524C (es) |
| CL (1) | CL2008002826A1 (es) |
| CY (1) | CY1112720T1 (es) |
| DK (1) | DK2205569T3 (es) |
| ES (1) | ES2383249T3 (es) |
| HR (1) | HRP20120377T1 (es) |
| IL (1) | IL205647A0 (es) |
| MX (1) | MX2010003182A (es) |
| NZ (1) | NZ584352A (es) |
| PL (1) | PL2205569T3 (es) |
| PT (1) | PT2205569E (es) |
| RU (1) | RU2491280C2 (es) |
| SI (1) | SI2205569T1 (es) |
| TW (1) | TW200922587A (es) |
| WO (1) | WO2009042138A1 (es) |
| ZA (1) | ZA201002173B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CL2008002827A1 (es) | 2007-09-25 | 2009-11-27 | Actimis Pharmaceuticals Inc | Compuestos derivados de 2-s-bencil pirimidina, antagonistas del receptor crth2; composicion farmaceutica que los comprende; y su uso en el tratamiento de enfermedades alergicas mediadas por eosinofilos y basofilos, tales como asma, rinitis alergica, dermatitis atopica, conjuntivitis alergica, sinusitis y psoriasis, entre otras |
| AU2008312624B2 (en) * | 2007-10-18 | 2014-07-10 | Boehringer Ingelheim International Gmbh | Preparation of dihydrothieno [3, 2-D] pyrimidines and intermediates used therein |
| US20120129820A1 (en) * | 2009-02-09 | 2012-05-24 | Boehringer Ingelheim International Gmbh | New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders |
| CN108383789A (zh) * | 2010-01-27 | 2018-08-10 | 艾克提麦斯医药品有限公司 | 作为crth2拮抗剂的吡唑化合物 |
| EP2598145A1 (en) * | 2010-07-28 | 2013-06-05 | Boehringer Ingelheim International GmbH | Pharmaceutical composition for treatment of respiratory and inflammatory diseases |
| EP2457900A1 (en) | 2010-11-25 | 2012-05-30 | Almirall, S.A. | New pyrazole derivatives having CRTh2 antagonistic behaviour |
| TWI527809B (zh) | 2011-01-24 | 2016-04-01 | 百靈佳殷格翰國際股份有限公司 | 作為ｃｒｔｈ２拮抗劑之吡唑化合物 |
| WO2012130633A1 (en) | 2011-03-25 | 2012-10-04 | Boehringer Ingelheim International Gmbh | Pyrazole compounds as crth2 antagonists |
| GB2494277A (en) | 2011-08-29 | 2013-03-06 | Univ Heriot Watt | Electro-spinning nanofibres onto a moving wire card |
| CA2856100C (en) | 2011-11-17 | 2016-09-27 | Kbp Biosciences Co., Ltd. | Nitrogen-containing fused ring compounds as crth2 antagonists |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE790679A (fr) | 1971-11-03 | 1973-04-27 | Ici Ltd | Derives de l'indole |
| GB9125842D0 (en) | 1991-12-04 | 1992-02-05 | Ici Plc | Heterocyclic derivatives |
| WO1994008975A1 (en) * | 1992-10-16 | 1994-04-28 | Nippon Soda Co., Ltd. | Pyrimidine derivative |
| GB2359078A (en) | 2000-02-11 | 2001-08-15 | Astrazeneca Uk Ltd | Pharmaceutically active pyrimidine derivatives |
| JP2001302667A (ja) | 2000-04-28 | 2001-10-31 | Bayer Ag | イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体 |
| US6878522B2 (en) | 2000-07-07 | 2005-04-12 | Baiyong Li | Methods for the identification of compounds useful for the treatment of disease states mediated by prostaglandin D2 |
| EP1413306A1 (en) | 2002-10-21 | 2004-04-28 | Warner-Lambert Company LLC | Tetrahydroquinoline derivatives as CRTH2 antagonists |
| AU2003297398B2 (en) | 2002-12-20 | 2009-09-24 | Amgen Inc. | Asthma and allergic inflammation modulators |
| EP1471057B1 (en) * | 2003-04-25 | 2006-01-18 | Actimis Pharmaceuticals, Inc. | Pyrimidinylacetic acid derivatives useful for the treatment of diseases mediated by CRTH2 |
| DK1718649T3 (da) * | 2004-01-31 | 2009-08-24 | Actimis Pharmaceuticals Inc | Imidazo[1,2-c]pyrimidinyleddikesyrederivater |
| WO2007062677A1 (en) * | 2005-11-30 | 2007-06-07 | 7Tm Pharma A/S | Thiazolyl- and pyrimidinyl-acetic acids and their use as crth2 receptor ligands |
| CL2008002827A1 (es) | 2007-09-25 | 2009-11-27 | Actimis Pharmaceuticals Inc | Compuestos derivados de 2-s-bencil pirimidina, antagonistas del receptor crth2; composicion farmaceutica que los comprende; y su uso en el tratamiento de enfermedades alergicas mediadas por eosinofilos y basofilos, tales como asma, rinitis alergica, dermatitis atopica, conjuntivitis alergica, sinusitis y psoriasis, entre otras |
-
2008
- 2008-09-24 WO PCT/US2008/011053 patent/WO2009042138A1/en active Application Filing
- 2008-09-24 CL CL2008002826A patent/CL2008002826A1/es unknown
- 2008-09-24 AT AT08833849T patent/ATE547407T1/de active
- 2008-09-24 SI SI200830609T patent/SI2205569T1/sl unknown
- 2008-09-24 CN CN200880117669A patent/CN101874023A/zh active Pending
- 2008-09-24 JP JP2010526927A patent/JP5524847B2/ja active Active
- 2008-09-24 TW TW097136691A patent/TW200922587A/zh unknown
- 2008-09-24 BR BRPI0817319 patent/BRPI0817319A2/pt not_active IP Right Cessation
- 2008-09-24 ES ES08833849T patent/ES2383249T3/es active Active
- 2008-09-24 PT PT08833849T patent/PT2205569E/pt unknown
- 2008-09-24 MX MX2010003182A patent/MX2010003182A/es active IP Right Grant
- 2008-09-24 PL PL08833849T patent/PL2205569T3/pl unknown
- 2008-09-24 AU AU2008305632A patent/AU2008305632B2/en not_active Expired - Fee Related
- 2008-09-24 DK DK08833849.6T patent/DK2205569T3/da active
- 2008-09-24 AR ARP080104146A patent/AR068632A1/es not_active Application Discontinuation
- 2008-09-24 NZ NZ584352A patent/NZ584352A/en not_active IP Right Cessation
- 2008-09-24 RU RU2010116293/04A patent/RU2491280C2/ru not_active IP Right Cessation
- 2008-09-24 EP EP08833849A patent/EP2205569B1/en not_active Not-in-force
- 2008-09-24 KR KR1020107008867A patent/KR20100061747A/ko not_active Application Discontinuation
- 2008-09-24 CA CA2700524A patent/CA2700524C/en not_active Expired - Fee Related
- 2008-09-24 US US12/679,895 patent/US8324229B2/en not_active Expired - Fee Related
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2010
- 2010-03-26 ZA ZA2010/02173A patent/ZA201002173B/en unknown
- 2010-05-09 IL IL205647A patent/IL205647A0/en unknown
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2012
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- 2012-05-07 CY CY20121100420T patent/CY1112720T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN101874023A (zh) | 2010-10-27 |
| US20100298361A1 (en) | 2010-11-25 |
| CA2700524C (en) | 2017-08-01 |
| JP5524847B2 (ja) | 2014-06-18 |
| TW200922587A (en) | 2009-06-01 |
| WO2009042138A1 (en) | 2009-04-02 |
| RU2491280C2 (ru) | 2013-08-27 |
| MX2010003182A (es) | 2010-06-02 |
| NZ584352A (en) | 2012-03-30 |
| AU2008305632A1 (en) | 2009-04-02 |
| CY1112720T1 (el) | 2016-02-10 |
| JP2010540520A (ja) | 2010-12-24 |
| ZA201002173B (en) | 2011-05-25 |
| KR20100061747A (ko) | 2010-06-08 |
| AU2008305632B2 (en) | 2014-01-30 |
| CL2008002826A1 (es) | 2009-08-07 |
| ES2383249T3 (es) | 2012-06-19 |
| PL2205569T3 (pl) | 2012-08-31 |
| US8324229B2 (en) | 2012-12-04 |
| IL205647A0 (en) | 2011-07-31 |
| RU2010116293A (ru) | 2011-11-10 |
| DK2205569T3 (da) | 2012-05-21 |
| AR068632A1 (es) | 2009-11-25 |
| EP2205569B1 (en) | 2012-02-29 |
| CA2700524A1 (en) | 2009-04-02 |
| BRPI0817319A2 (pt) | 2015-03-17 |
| PT2205569E (pt) | 2012-05-25 |
| EP2205569A1 (en) | 2010-07-14 |
| ATE547407T1 (de) | 2012-03-15 |
| WO2009042138A9 (en) | 2009-10-15 |
| SI2205569T1 (sl) | 2012-06-29 |
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