BRPI0918966A8 - composto inibidor de proteases, composição farmacêutica compreendendo dito compostos e uso terapêutico do mesmo - Google Patents
composto inibidor de proteases, composição farmacêutica compreendendo dito compostos e uso terapêutico do mesmo Download PDFInfo
- Publication number
- BRPI0918966A8 BRPI0918966A8 BRPI0918966A BRPI0918966A BRPI0918966A8 BR PI0918966 A8 BRPI0918966 A8 BR PI0918966A8 BR PI0918966 A BRPI0918966 A BR PI0918966A BR PI0918966 A BRPI0918966 A BR PI0918966A BR PI0918966 A8 BRPI0918966 A8 BR PI0918966A8
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- BR
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- Prior art keywords
- alkyl
- fluorine
- methyl
- cycloalkyl
- pharmaceutical composition
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title abstract 5
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 title abstract 2
- 239000000137 peptide hydrolase inhibitor Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 230000001225 therapeutic effect Effects 0.000 title abstract 2
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 abstract 4
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 229910052731 fluorine Inorganic materials 0.000 abstract 4
- 239000011737 fluorine Substances 0.000 abstract 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 4
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 102000005600 Cathepsins Human genes 0.000 abstract 1
- 108010084457 Cathepsins Proteins 0.000 abstract 1
- 206010027452 Metastases to bone Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 125000001475 halogen functional group Chemical group 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D277/38—Nitrogen atoms
- C07D277/40—Unsubstituted amino or imino radicals
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
-
- 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
-
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
-
- 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
-
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Immunology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
Abstract
composto inibidor de protease, composição farmacêutica compreendendo dito composto e uso terapêutico do mesmo compostos da fórmula ii: em que r1 e r2 são independentemene h, f ou ch3; ou r1 forma uma ligação etinila e r2 é h ou c3-c6 cicloalquila, o qual é opcionalmente substituído com um ou dois substituintes independentemente selecionados de metila, cf3, ome ou halo; r3 é c1-c3 alquila ou c3-c6 cicloalquila, um dos quais é opcionalmente substituído com um ou dois metila e/ou um flúor, trifluorometila ou metóxi, quando r3 é c3-c6 cicloalquila, este pode ser, alternativamente, gem substituído com flúor; r4 é metila ou flúor; m é 0,1 ou 2; e é uma ligação, ou tiazolila, opcionalmente substituído com metila ou flúor; a1 é ch ou n, a2 é cr6r7 ou nr6, desde que pelo menos um de a1 e a2 compreenda n; r6 é h, c1-c4 alquila, c1-c4 haloalquila, c1-c3 alquil-o-c1-c3 alquila, ou quando a2 é c, r6 também pode ser c1-c4 alcóxi ou f; r7 é h, c1-c4 alquila ou f, ou um sal farmaceuticamente aceitável, n-óxido ou hidrato dos mesmos, têm utilidade no tratamento de doenças caracterizadas por expressão ou ativação inadequada de catepsina k, tais como osteoporose, osteoartrite, artrite reumatóide ou metástases ósseas.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0817424.5A GB0817424D0 (en) | 2008-09-24 | 2008-09-24 | Protease inhibitors |
| GB0817424.5 | 2008-09-24 | ||
| PCT/EP2009/062406 WO2010034788A1 (en) | 2008-09-24 | 2009-09-24 | Protease inhibitors |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| BRPI0918966A2 BRPI0918966A2 (pt) | 2015-12-01 |
| BRPI0918966A8 true BRPI0918966A8 (pt) | 2020-02-18 |
| BRPI0918966B1 BRPI0918966B1 (pt) | 2020-03-03 |
| BRPI0918966B8 BRPI0918966B8 (pt) | 2021-05-25 |
Family
ID=39952074
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0918966A BRPI0918966B8 (pt) | 2008-09-24 | 2009-09-24 | composto inibidor de protease, composição farmacêutica compreendendo dito composto e uso terapêutico do mesmo |
Country Status (23)
| Country | Link |
|---|---|
| US (11) | US8242119B2 (pt) |
| EP (1) | EP2331548B1 (pt) |
| JP (1) | JP5639592B2 (pt) |
| KR (1) | KR101671177B1 (pt) |
| CN (2) | CN103992329B (pt) |
| AU (1) | AU2009295898B2 (pt) |
| BR (1) | BRPI0918966B8 (pt) |
| CA (1) | CA2738023C (pt) |
| CY (1) | CY1114833T1 (pt) |
| DK (1) | DK2331548T3 (pt) |
| EA (1) | EA020122B1 (pt) |
| ES (1) | ES2438095T3 (pt) |
| GB (1) | GB0817424D0 (pt) |
| HK (1) | HK1152522A1 (pt) |
| HR (1) | HRP20131131T1 (pt) |
| IL (1) | IL211811A (pt) |
| MY (1) | MY152969A (pt) |
| PL (1) | PL2331548T3 (pt) |
| PT (1) | PT2331548E (pt) |
| RS (1) | RS53054B (pt) |
| SI (1) | SI2331548T1 (pt) |
| WO (2) | WO2010034788A1 (pt) |
| ZA (1) | ZA201102179B (pt) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0817424D0 (en) | 2008-09-24 | 2008-10-29 | Medivir Ab | Protease inhibitors |
| GB201314503D0 (en) | 2013-08-13 | 2013-09-25 | Medivir Ab | Cysteine protease inhibitor salt |
| CN107286150B (zh) * | 2016-04-11 | 2020-07-07 | 中国科学院上海有机化学研究所 | N-杂环类化合物、其中间体、制备方法、药物组合物和应用 |
| US20220193048A1 (en) | 2019-04-05 | 2022-06-23 | Universite De Bretagne Occidentale | Protease-activated receptor-2 inhibitors for the treatment of sensory neuropathy induced by a marine neurotoxic poisoning |
| CN110563611B (zh) * | 2019-09-19 | 2021-02-02 | 中国医学科学院医药生物技术研究所 | 一种异羟肟酸类衍生物及其制备方法和应用 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR013079A1 (es) * | 1997-05-06 | 2000-12-13 | Smithkline Beecham Corp | Derivados sustituidos de tetrahidrofurano-3-onas, de tetrahidropirano-3- onas y tetrahidrotiofen-3-onas, un procedimiento para su preparacion unacomposicion farmaceutica de un medicamento util como inhibidores de proteasas e intermediarios |
| JP3102101U (ja) | 2003-12-05 | 2004-07-02 | 株式会社ライトボーイ | 投光機 |
| WO2005056529A1 (en) | 2003-12-12 | 2005-06-23 | Merck Frosst Canada Ltd. | Cathepsin cysteine protease inhibitors |
| ATE461200T1 (de) | 2004-01-08 | 2010-04-15 | Medivir Ab | Inhibitoren von cysteinprotease |
| SE0400022D0 (sv) * | 2004-01-08 | 2004-01-08 | Medivir Ab | New compounds |
| FR2889701B1 (fr) | 2005-08-12 | 2007-10-05 | Sanofi Aventis Sa | Derives de 5-pyridinyl-1-azabicyclo[3.2.1]octane, leur preparation en therapeutique. |
| GB0614042D0 (en) | 2006-07-14 | 2006-08-23 | Amura Therapeutics Ltd | Compounds |
| GB0614044D0 (en) | 2006-07-14 | 2006-08-23 | Amura Therapeutics Ltd | Compounds |
| WO2008114054A1 (en) * | 2007-03-19 | 2008-09-25 | Medivir Ab | Protease inhibitors |
| US7893067B2 (en) * | 2007-06-27 | 2011-02-22 | Medivir Ab | Cysteine protease inhibitors |
| JP5587790B2 (ja) | 2008-01-09 | 2014-09-10 | アミュラ セラピューティクス リミティド | 化合物 |
| GB0817424D0 (en) * | 2008-09-24 | 2008-10-29 | Medivir Ab | Protease inhibitors |
-
2008
- 2008-09-24 GB GBGB0817424.5A patent/GB0817424D0/en not_active Ceased
-
2009
- 2009-09-24 EP EP09783391.7A patent/EP2331548B1/en active Active
- 2009-09-24 KR KR1020117009274A patent/KR101671177B1/ko active IP Right Grant
- 2009-09-24 RS RS20130522A patent/RS53054B/en unknown
- 2009-09-24 BR BRPI0918966A patent/BRPI0918966B8/pt active IP Right Grant
- 2009-09-24 PT PT97833917T patent/PT2331548E/pt unknown
- 2009-09-24 CN CN201410205405.9A patent/CN103992329B/zh active Active
- 2009-09-24 WO PCT/EP2009/062406 patent/WO2010034788A1/en active Application Filing
- 2009-09-24 PL PL09783391T patent/PL2331548T3/pl unknown
- 2009-09-24 JP JP2011528326A patent/JP5639592B2/ja active Active
- 2009-09-24 AU AU2009295898A patent/AU2009295898B2/en active Active
- 2009-09-24 ES ES09783391.7T patent/ES2438095T3/es active Active
- 2009-09-24 EA EA201170479A patent/EA020122B1/ru not_active IP Right Cessation
- 2009-09-24 CN CN200980148042.7A patent/CN102224156B/zh active Active
- 2009-09-24 US US12/739,489 patent/US8242119B2/en active Active
- 2009-09-24 CA CA2738023A patent/CA2738023C/en active Active
- 2009-09-24 WO PCT/EP2009/062408 patent/WO2010034790A1/en active Application Filing
- 2009-09-24 MY MYPI20111288 patent/MY152969A/en unknown
- 2009-09-24 SI SI200930786T patent/SI2331548T1/sl unknown
- 2009-09-24 DK DK09783391.7T patent/DK2331548T3/da active
-
2011
- 2011-03-17 IL IL211811A patent/IL211811A/en active IP Right Grant
- 2011-03-23 ZA ZA2011/02179A patent/ZA201102179B/en unknown
- 2011-06-24 HK HK11106551.5A patent/HK1152522A1/xx unknown
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2012
- 2012-07-03 US US13/541,519 patent/US8426421B2/en active Active
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2013
- 2013-03-14 US US13/831,267 patent/US8735395B2/en active Active
- 2013-11-18 CY CY20131101021T patent/CY1114833T1/el unknown
- 2013-11-26 HR HRP20131131AT patent/HRP20131131T1/hr unknown
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2014
- 2014-04-09 US US14/249,332 patent/US9200006B2/en active Active
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2015
- 2015-11-13 US US14/940,817 patent/US9428517B2/en active Active
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2016
- 2016-08-25 US US15/247,804 patent/US20170166538A1/en not_active Abandoned
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2017
- 2017-08-02 US US15/667,292 patent/US20170334867A1/en not_active Abandoned
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2018
- 2018-03-30 US US15/941,947 patent/US10329266B2/en not_active Expired - Fee Related
-
2019
- 2019-06-24 US US16/449,850 patent/US10723709B2/en active Active
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2020
- 2020-07-27 US US16/940,067 patent/US11312693B2/en active Active
-
2022
- 2022-04-25 US US17/728,943 patent/US20220332690A1/en active Pending
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