ATE386035T1 - Medizinische verwendung von zwitterion- verbindungen als modulatoren des cftr -kanals - Google Patents
Medizinische verwendung von zwitterion- verbindungen als modulatoren des cftr -kanalsInfo
- Publication number
- ATE386035T1 ATE386035T1 AT04805771T AT04805771T ATE386035T1 AT E386035 T1 ATE386035 T1 AT E386035T1 AT 04805771 T AT04805771 T AT 04805771T AT 04805771 T AT04805771 T AT 04805771T AT E386035 T1 ATE386035 T1 AT E386035T1
- Authority
- AT
- Austria
- Prior art keywords
- formula
- compound
- zwitterion
- derivatives
- cftr
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- OLXZPDWKRNYJJZ-UHFFFAOYSA-N 5-(6-aminopurin-9-yl)-2-(hydroxymethyl)oxolan-3-ol Chemical compound C1=NC=2C(N)=NC=NC=2N1C1CC(O)C(CO)O1 OLXZPDWKRNYJJZ-UHFFFAOYSA-N 0.000 abstract 4
- AIJULSRZWUXGPQ-UHFFFAOYSA-N Methylglyoxal Chemical compound CC(=O)C=O AIJULSRZWUXGPQ-UHFFFAOYSA-N 0.000 abstract 4
- 102000012605 Cystic Fibrosis Transmembrane Conductance Regulator Human genes 0.000 abstract 3
- 108010079245 Cystic Fibrosis Transmembrane Conductance Regulator Proteins 0.000 abstract 3
- ICSNLGPSRYBMBD-UHFFFAOYSA-N 2-aminopyridine Chemical compound NC1=CC=CC=N1 ICSNLGPSRYBMBD-UHFFFAOYSA-N 0.000 abstract 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 abstract 2
- 150000001409 amidines Chemical class 0.000 abstract 2
- OPTASPLRGRRNAP-UHFFFAOYSA-N cytosine Chemical compound NC=1C=CNC(=O)N=1 OPTASPLRGRRNAP-UHFFFAOYSA-N 0.000 abstract 2
- QTULKOMMYIUZQD-UHFFFAOYSA-N 9-propylpurin-6-amine Chemical compound N1=CN=C2N(CCC)C=NC2=C1N QTULKOMMYIUZQD-UHFFFAOYSA-N 0.000 abstract 1
- GFFGJBXGBJISGV-UHFFFAOYSA-N Adenine Chemical compound NC1=NC=NC2=C1N=CN2 GFFGJBXGBJISGV-UHFFFAOYSA-N 0.000 abstract 1
- 229930024421 Adenine Natural products 0.000 abstract 1
- 239000004475 Arginine Substances 0.000 abstract 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 abstract 1
- 108091006146 Channels Proteins 0.000 abstract 1
- ASDYPWDJDTZPTF-UHFFFAOYSA-N OC1NC=NC(C1O)C(=O)O Chemical class OC1NC=NC(C1O)C(=O)O ASDYPWDJDTZPTF-UHFFFAOYSA-N 0.000 abstract 1
- 108091034057 RNA (poly(A)) Proteins 0.000 abstract 1
- 230000004913 activation Effects 0.000 abstract 1
- 229960000643 adenine Drugs 0.000 abstract 1
- 229960005305 adenosine Drugs 0.000 abstract 1
- LEQAOMBKQFMDFZ-UHFFFAOYSA-N alpha-ketodiacetal Natural products O=CC=O LEQAOMBKQFMDFZ-UHFFFAOYSA-N 0.000 abstract 1
- 230000001088 anti-asthma Effects 0.000 abstract 1
- 239000000924 antiasthmatic agent Substances 0.000 abstract 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 abstract 1
- 210000004978 chinese hamster ovary cell Anatomy 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 229940104302 cytosine Drugs 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 229940015043 glyoxal Drugs 0.000 abstract 1
- -1 glyoxal compound Chemical class 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 230000010534 mechanism of action Effects 0.000 abstract 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
-
- 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
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61K31/52—Purines, e.g. adenine
- A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- 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
- A61P1/12—Antidiarrhoeals
-
- 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
- A61P11/06—Antiasthmatics
-
- 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
- A61P11/08—Bronchodilators
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Digital Transmission Methods That Use Modulated Carrier Waves (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0312417A FR2861304B1 (fr) | 2003-10-23 | 2003-10-23 | Modulateurs des canaux cftr |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE386035T1 true ATE386035T1 (de) | 2008-03-15 |
Family
ID=34400730
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT04805771T ATE386035T1 (de) | 2003-10-23 | 2004-10-21 | Medizinische verwendung von zwitterion- verbindungen als modulatoren des cftr -kanals |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7772198B2 (de) |
| EP (1) | EP1678175B1 (de) |
| AT (1) | ATE386035T1 (de) |
| DE (1) | DE602004011805T9 (de) |
| FR (1) | FR2861304B1 (de) |
| WO (1) | WO2005039589A2 (de) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2404919E (pt) | 2005-11-08 | 2013-10-22 | Vertex Pharma | Composto heterocíclico útil como um modulador de transportadores de cassete de ligação a atp |
| EP2164840A2 (de) | 2007-05-09 | 2010-03-24 | Vertex Pharmaceuticals Incorporated | Modulatoren von cftr |
| HUE049642T2 (hu) | 2007-12-07 | 2020-09-28 | Vertex Pharma | 3-(6-(1-(2,2-Difluorbenzo[d][1,3]dioxol-5-il)-ciklopropánkarboxamido)-3-metilpiridin-2-il)-benzoesav szilárd formái |
| CA2989620C (en) * | 2007-12-07 | 2022-05-03 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
| CA2716109C (en) | 2008-02-28 | 2016-07-19 | Vertex Pharmaceuticals Incorporated | Heteroaryl derivatives as cftr modulators |
| EP2464354B1 (de) * | 2009-08-10 | 2015-04-01 | The Regents of The University of California | Pyrimido-pyrrolo-chinoxalindionhemmer des regulatorproteins für die transmembranen-leitfähigkeit zystischer fibrose und verwendungen davon |
| ES2900353T3 (es) | 2010-04-07 | 2022-03-16 | Vertex Pharma | Composiciones farmacéuticas de ácido 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il)ciclopropanocarboxamido)-3-metilpiriidin-2-il)benzoico y administración de las mismas |
| USRE48842E1 (en) | 2011-05-27 | 2021-12-07 | The Regents Of The University Of California | Pyrimido-pyrrolo-oxazine-dione compound inhibitors of the cystic fibrosis transmembrane conductance regulator protein and uses therefor |
| NZ727015A (en) | 2012-01-25 | 2017-12-22 | Vertex Pharma | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
| CA2930199C (en) | 2013-11-12 | 2022-10-25 | Vertex Pharmaceuticals Incorporated | Process of preparing pharmaceutical compositions for the treatment of cftr mediated diseases |
| HUE055423T2 (hu) | 2014-11-18 | 2021-11-29 | Vertex Pharma | Eljárás nagy áteresztõképességû tesztelõ nagy teljesítményû folyadék-kromatográfia elvégzésére |
| AU2016333855A1 (en) * | 2015-10-09 | 2018-04-26 | AbbVie S.à.r.l. | Substituted pyrazolo[3,4-b]pyridin-6-carboxylic acids and their use |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5397786A (en) * | 1993-01-08 | 1995-03-14 | Simone; Charles B. | Rehydration drink |
| US5434171A (en) * | 1993-12-08 | 1995-07-18 | Eli Lilly And Company | Preparation of 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates and intermediates |
| US5516798A (en) * | 1994-10-11 | 1996-05-14 | North Carolina State University | Method for treating diarrhea and a composition therefor |
| CZ20012038A3 (cs) * | 1998-12-23 | 2001-09-12 | Idea Ag | Zdokonalený přípravek pro topické, neinvazivní použití in vivo |
| WO2001076577A2 (en) * | 2000-04-07 | 2001-10-18 | The Board Of Regents Of The University Of Texas System | Unique compositions of zwitterionic phospholipids and bisphosphonates and use of the compositions as bisphosphate delivery systems with reduced gi toxicity |
| DE10109798A1 (de) * | 2001-03-01 | 2002-09-12 | Aventis Pharma Gmbh | Gesundheitsfördernde Zusammensetzung von Verbindungen |
| EP1214893A1 (de) * | 2000-12-16 | 2002-06-19 | Aventis Pharma Deutschland GmbH | Zusammensetzungen zur Verbesserung der Gesundheit |
| US20030068391A1 (en) * | 2001-10-04 | 2003-04-10 | Harris Dennis H. | Ingestible nerve and circulatory nutritional formulation |
| AU2004227852B2 (en) * | 2003-03-31 | 2010-01-14 | The Brigham And Women's Hospital, Inc. | Zwitterionic immunomodulators for the treatment of asthma and allergy |
| EP1957451B1 (de) * | 2005-11-10 | 2011-10-19 | Nicholas S. Bodor | Weiche anticholinerge zwitterionen |
| CA2682032A1 (en) * | 2007-04-24 | 2008-11-06 | Theravance, Inc. | Quaternary ammonium compounds useful as muscarinic receptor antagonists |
-
2003
- 2003-10-23 FR FR0312417A patent/FR2861304B1/fr not_active Expired - Fee Related
-
2004
- 2004-10-21 DE DE602004011805T patent/DE602004011805T9/de active Active
- 2004-10-21 WO PCT/FR2004/050528 patent/WO2005039589A2/fr not_active Ceased
- 2004-10-21 AT AT04805771T patent/ATE386035T1/de not_active IP Right Cessation
- 2004-10-21 EP EP04805771A patent/EP1678175B1/de not_active Expired - Lifetime
-
2006
- 2006-04-21 US US11/408,911 patent/US7772198B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| DE602004011805T2 (de) | 2009-02-05 |
| WO2005039589A2 (fr) | 2005-05-06 |
| US7772198B2 (en) | 2010-08-10 |
| DE602004011805T9 (de) | 2009-06-04 |
| FR2861304A1 (fr) | 2005-04-29 |
| DE602004011805D1 (de) | 2008-03-27 |
| US20060258612A1 (en) | 2006-11-16 |
| EP1678175B1 (de) | 2008-02-13 |
| WO2005039589A3 (fr) | 2005-06-30 |
| FR2861304B1 (fr) | 2008-07-18 |
| EP1678175A2 (de) | 2006-07-12 |
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