HRP20160267T1 - Inhibitori mitoze, namijenjeni povećavanju apoptoze u terapiji - Google Patents
Inhibitori mitoze, namijenjeni povećavanju apoptoze u terapiji Download PDFInfo
- Publication number
- HRP20160267T1 HRP20160267T1 HRP20160267TT HRP20160267T HRP20160267T1 HR P20160267 T1 HRP20160267 T1 HR P20160267T1 HR P20160267T T HRP20160267T T HR P20160267TT HR P20160267 T HRP20160267 T HR P20160267T HR P20160267 T1 HRP20160267 T1 HR P20160267T1
- Authority
- HR
- Croatia
- Prior art keywords
- inhibitor
- intended
- cancer
- accordance
- thiadiazole
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims 26
- 230000011278 mitosis Effects 0.000 title claims 4
- 230000006907 apoptotic process Effects 0.000 title claims 2
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 210000004027 cell Anatomy 0.000 claims 10
- 230000001717 pathogenic effect Effects 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 3
- LLXISKGBWFTGEI-UHFFFAOYSA-N 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-methoxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide Chemical compound CON(C)C(=O)N1N=C(C=2C(=CC=C(F)C=2)F)SC1(CCCN)C1=CC=CC=C1 LLXISKGBWFTGEI-UHFFFAOYSA-N 0.000 claims 2
- 206010023774 Large cell lung cancer Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 201000009546 lung large cell carcinoma Diseases 0.000 claims 2
- 210000004881 tumor cell Anatomy 0.000 claims 2
- LLXISKGBWFTGEI-HXUWFJFHSA-N (2r)-2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-methoxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide Chemical compound C1([C@@]2(CCCN)SC(=NN2C(=O)N(C)OC)C=2C(=CC=C(F)C=2)F)=CC=CC=C1 LLXISKGBWFTGEI-HXUWFJFHSA-N 0.000 claims 1
- AOQRBLALIZQSHS-UHFFFAOYSA-N 2-(3-aminopropyl)-5-(2,5-difluorophenyl)-n-hydroxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide Chemical compound CN(O)C(=O)N1N=C(C=2C(=CC=C(F)C=2)F)SC1(CCCN)C1=CC=CC=C1 AOQRBLALIZQSHS-UHFFFAOYSA-N 0.000 claims 1
- NMGQWLQAMQNKID-UHFFFAOYSA-N 2-(3-aminopropyl)-5-(3-fluorophenyl)-n-(2-methoxyethyl)-n-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide Chemical compound COCCN(C)C(=O)N1N=C(C=2C=C(F)C=CC=2)SC1(CCCN)C1=CC=CC=C1 NMGQWLQAMQNKID-UHFFFAOYSA-N 0.000 claims 1
- JVHFOAYTAUBQBW-UHFFFAOYSA-N 2-(3-aminopropyl)-5-(3-fluorophenyl)-n-methoxy-n-methyl-2-phenyl-1,3,4-thiadiazole-3-carboxamide Chemical compound CON(C)C(=O)N1N=C(C=2C=C(F)C=CC=2)SC1(CCCN)C1=CC=CC=C1 JVHFOAYTAUBQBW-UHFFFAOYSA-N 0.000 claims 1
- 241000321096 Adenoides Species 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010011732 Cyst Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010027406 Mesothelioma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000004337 Salivary Gland Neoplasms Diseases 0.000 claims 1
- 206010061934 Salivary gland cancer Diseases 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 210000002534 adenoid Anatomy 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000031513 cyst Diseases 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- LLXISKGBWFTGEI-FQEVSTJZSA-N filanesib Chemical compound C1([C@]2(CCCN)SC(=NN2C(=O)N(C)OC)C=2C(=CC=C(F)C=2)F)=CC=CC=C1 LLXISKGBWFTGEI-FQEVSTJZSA-N 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 231100000682 maximum tolerated dose Toxicity 0.000 claims 1
- 230000036456 mitotic arrest Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 210000003491 skin Anatomy 0.000 claims 1
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/433—Thidiazoles
-
- 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
-
- 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Claims (15)
1. Inhibitor ’161 KSP, namijenjen upotrebi u liječenju patogenih stanica u stanju zaustavljanja mitoze induciranog inhibitorom ’161 KSP, naznačen time što je namijenjen povećavanju apoptoze stanice, gdje se Inhibitor ’161 KSP bira između 2-(3-aminopropil)-5-(3-fluorfenil)-N-(2-metoksietil)-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamida, 2-(3-aminopropil)-5-(3-fluorfenil)-N-metoksi-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamida, 2-(3-aminopropil)-5-(2,5-difluorfenil)-N-metoksi-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamida, (S)-2-(3-aminopropil)-5-(2,5-difluorfenil)-N-metoksi-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamida, (R)-2-(3-aminopropil)-5-(2,5-difluorfenil)-N-metoksi-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamida i 2-(3-aminopropil)-5-(2,5-difluorfenil)-N-hidroksi-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamida.
2. Inhibitor namijenjen upotrebi u skladu s patentnim zahtjevom 1, naznačen time što je isti kao inhibitor koji je inducirao zaustavljanje mitoze.
3. Inhibitor namijenjen upotrebi u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je (S)-2-(3-aminopropil)-5-(2,5-difluorfenil)-N-metoksi-N-metil-2-fenil-1,3,4-tiadiazol-3(2H)-karboksamid.
4. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što su patogene stanice stanice raka.
5. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što su patogene stanice stanice hematoloških tumora.
6. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što se patogene stanice bira između stanica limfoma, leukemije i multiplog mijeloma.
7. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što su patogene stanice stanice čvrstih tumora.
8. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 4 ili 7, naznačen time što se patogene stanice bira između tumorskih stanica iz kože, dojke, mozga, karcinoma vrata maternice i karcinoma testisa.
9. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 4 ili 7, naznačen time što se patogene stanice bira između raka dojke, kolorektalnog raka, raka velikih stanica pluća, raka gušterače, raka mokraćnog mjehura, raka slinovnice (adenoidne ciste), raka jednjaka, raka mezotelioma, te miješanog raka malih i velikih stanica pluća.
10. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što je Inhibitor namijenjen primjeni u najvećoj toleriranoj dozi.
11. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 3 do 10, naznačen time što je najveća tolerirana doza 1,25 mg/m2 dnevno.
12. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 11, naznačen time što se Inhibitor ’161, namijenjen primjeni, primjenjuje 12 do 60 sati nakon inhibitora ’161 koji je inducirao zaustavljanje mitoze.
13. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 12, naznačen time što se Inhibitor ’161, namijenjen primjeni, primjenjuje 24 do 48 sati nakon inhibitora ’161 koji je inducirao zaustavljanje mitoze.
14. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 13, naznačen time što se Inhibitor ’161 primjenjuje u ciklusu od 11 do 24 dana.
15. Inhibitor namijenjen upotrebi u skladu s bilo kojim od patentnih zahtjeva 1 do 14, naznačen time što se Inhibitor ’161 primjenjuje u ciklusu od 14 do 21 dana.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10608608P | 2008-10-16 | 2008-10-16 | |
| PCT/US2009/061106 WO2010045624A1 (en) | 2008-10-16 | 2009-10-16 | Inhibitors of mitosis for increasing apoptosis in therapy |
| EP09748884.5A EP2349259B1 (en) | 2008-10-16 | 2009-10-16 | Inhibitors of mitosis for increasing apoptosis in therapy |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20160267T1 true HRP20160267T1 (hr) | 2016-04-08 |
Family
ID=41508147
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20160267TT HRP20160267T1 (hr) | 2008-10-16 | 2016-03-14 | Inhibitori mitoze, namijenjeni povećavanju apoptoze u terapiji |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP2349259B1 (hr) |
| JP (2) | JP5749170B2 (hr) |
| CN (2) | CN102256603B (hr) |
| AU (1) | AU2009305588B2 (hr) |
| BR (1) | BRPI0920878A2 (hr) |
| CA (1) | CA2741069C (hr) |
| CY (1) | CY1117281T1 (hr) |
| DK (1) | DK2349259T3 (hr) |
| ES (1) | ES2565778T3 (hr) |
| HK (1) | HK1154813A1 (hr) |
| HR (1) | HRP20160267T1 (hr) |
| HU (1) | HUE027170T2 (hr) |
| IL (1) | IL212413A (hr) |
| PL (1) | PL2349259T3 (hr) |
| RS (1) | RS54647B1 (hr) |
| RU (1) | RU2519145C2 (hr) |
| SI (1) | SI2349259T1 (hr) |
| SM (1) | SMT201600073B (hr) |
| UA (1) | UA106214C2 (hr) |
| WO (1) | WO2010045624A1 (hr) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0920878A2 (pt) * | 2008-10-16 | 2015-12-22 | Array Biopharma Inc | inbidor de ksp161 para aumentar apoptose, sua administração e seu uso. |
| TWI427054B (zh) * | 2012-01-20 | 2014-02-21 | Nat Univ Chung Hsing | A pharmaceutical composition for inhibiting and treating a lung tumor and inhibiting an inflammatory reaction and a method for preparing the same |
| NZ631362A (en) | 2012-08-13 | 2016-09-30 | Array Biopharma Inc | Arry-520 for use in treating cancer in a patient with low aag |
| AU2014227478A1 (en) | 2013-08-08 | 2015-02-26 | Array Biopharma Inc. | Filanesib combined with pomalidomide displays enhanced anti-tumor activity |
| CN115181778A (zh) * | 2015-02-04 | 2022-10-14 | 百时美施贵宝公司 | 选择治疗性分子的方法 |
| JP7340240B2 (ja) * | 2019-08-26 | 2023-09-07 | 学校法人関西医科大学 | 細胞又は組織にアポトーシスを誘導する方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4878285B2 (ja) * | 2003-06-05 | 2012-02-15 | エテルナ ツェンタリス ゲゼルシャフト ミット ベシュレンクテル ハフツング | アポトーシス誘発作用を有するインドール誘導体 |
| US7449486B2 (en) * | 2004-10-19 | 2008-11-11 | Array Biopharma Inc. | Mitotic kinesin inhibitors and methods of use thereof |
| BRPI0920878A2 (pt) * | 2008-10-16 | 2015-12-22 | Array Biopharma Inc | inbidor de ksp161 para aumentar apoptose, sua administração e seu uso. |
-
2009
- 2009-10-16 BR BRPI0920878A patent/BRPI0920878A2/pt not_active Application Discontinuation
- 2009-10-16 CN CN200980150472.2A patent/CN102256603B/zh active Active
- 2009-10-16 WO PCT/US2009/061106 patent/WO2010045624A1/en active Application Filing
- 2009-10-16 HU HUE09748884A patent/HUE027170T2/hu unknown
- 2009-10-16 JP JP2011532305A patent/JP5749170B2/ja active Active
- 2009-10-16 SI SI200931379T patent/SI2349259T1/sl unknown
- 2009-10-16 RS RS20160175A patent/RS54647B1/en unknown
- 2009-10-16 RU RU2011119427/15A patent/RU2519145C2/ru active
- 2009-10-16 UA UAA201106118A patent/UA106214C2/ru unknown
- 2009-10-16 CN CN201510222295.1A patent/CN104958292B/zh active Active
- 2009-10-16 CA CA2741069A patent/CA2741069C/en active Active
- 2009-10-16 EP EP09748884.5A patent/EP2349259B1/en active Active
- 2009-10-16 ES ES09748884.5T patent/ES2565778T3/es active Active
- 2009-10-16 AU AU2009305588A patent/AU2009305588B2/en active Active
- 2009-10-16 DK DK09748884.5T patent/DK2349259T3/en active
- 2009-10-16 PL PL09748884T patent/PL2349259T3/pl unknown
-
2011
- 2011-04-17 IL IL212413A patent/IL212413A/en active IP Right Grant
- 2011-09-01 HK HK11109252.1A patent/HK1154813A1/zh unknown
-
2014
- 2014-05-19 JP JP2014102987A patent/JP2014144979A/ja active Pending
-
2016
- 2016-03-10 CY CY20161100206T patent/CY1117281T1/el unknown
- 2016-03-14 HR HRP20160267TT patent/HRP20160267T1/hr unknown
- 2016-03-14 SM SM201600073T patent/SMT201600073B/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN102256603B (zh) | 2015-06-03 |
| IL212413A0 (en) | 2011-06-30 |
| HK1154813A1 (zh) | 2012-05-04 |
| RS54647B1 (en) | 2016-08-31 |
| RU2519145C2 (ru) | 2014-06-10 |
| CY1117281T1 (el) | 2017-04-26 |
| RU2011119427A (ru) | 2012-11-27 |
| HUE027170T2 (hu) | 2016-10-28 |
| CN104958292B (zh) | 2018-10-16 |
| CN102256603A (zh) | 2011-11-23 |
| PL2349259T3 (pl) | 2016-07-29 |
| WO2010045624A1 (en) | 2010-04-22 |
| JP2014144979A (ja) | 2014-08-14 |
| DK2349259T3 (en) | 2016-02-29 |
| EP2349259B1 (en) | 2015-12-23 |
| ES2565778T3 (es) | 2016-04-06 |
| SI2349259T1 (sl) | 2016-03-31 |
| JP5749170B2 (ja) | 2015-07-15 |
| EP2349259A1 (en) | 2011-08-03 |
| AU2009305588A1 (en) | 2010-04-22 |
| IL212413A (en) | 2015-08-31 |
| CA2741069A1 (en) | 2010-04-22 |
| SMT201600073B (it) | 2016-04-29 |
| CN104958292A (zh) | 2015-10-07 |
| AU2009305588B2 (en) | 2015-08-13 |
| UA106214C2 (ru) | 2014-08-11 |
| BRPI0920878A2 (pt) | 2015-12-22 |
| JP2012505924A (ja) | 2012-03-08 |
| CA2741069C (en) | 2017-08-22 |
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