FI68049C - Foerfarande foer framstaellning av farmakologiskt verksamma 2-cyl-aminometyl-1,4-bensodiazepinfoereningar samt vid dera s ramstaellning anvaendbara mellanprodukter - Google Patents
Foerfarande foer framstaellning av farmakologiskt verksamma 2-cyl-aminometyl-1,4-bensodiazepinfoereningar samt vid dera s ramstaellning anvaendbara mellanprodukter Download PDFInfo
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- FI68049C FI68049C FI822148A FI822148A FI68049C FI 68049 C FI68049 C FI 68049C FI 822148 A FI822148 A FI 822148A FI 822148 A FI822148 A FI 822148A FI 68049 C FI68049 C FI 68049C
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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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/44—Radicals substituted by doubly-bound oxygen, sulfur, or nitrogen atoms, or by two such atoms singly-bound to the same carbon atom
- C07D213/46—Oxygen atoms
- C07D213/50—Ketonic radicals
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
- C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
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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
- C07D401/12—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 chain containing hetero atoms as chain links
-
- 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
- C07D401/14—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 three or more hetero rings
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (5)
1. Förfarande för framställning av farmakologiskt verksam 2-acylaminometyl-lH-2,3-d ihydro-1,4-bensod iazepin-fören ing enligt formeln I samt dess optiska isomerer och syraadditions-salter isCH2-N-C-(CH2)nR3 "6 H i vilken formel är väte eller lägre alkyl R2 är väte, n är 0, 1 eller 2, R3 är nägon av följande grupper a, b, c eller d J R12 «8 abc <1 där X är kväve eller svavel, R7 är väte, lägre alkyl eller halogen, Rg är väte eller lägre alkyl, R9 är väte, RlO är väte eller klor, Rl1 är väte, lägre alkyl, lägre alkoxi, hydroxi, halogen, nitro, trifluormetyl, cyano, amino, lägre mono- eller dialkyl-amino, lägre monoalkanoylamino, eller lägre alkanoyloxi, r12 är väte, lägre alkyl, lägre alkoxi, halogen, hydroxi eller lägre alkanoyloxi, eller 56 68049 Rll och R^2 är bundna. vid bredvid varandra liggande kolatomer och bildar tillsaminans en metylendioxigrupp, R4 är nägon av de ovan angivna grupperna a, b eller c, R5 är väte, lägre alkyl, lägre alkoxi, halogen eller nitro, och Rg är väte, lägre alkyl, lägre alkoxi eller halogen, eller R5 och Rg är bundna . vid bredvid varandra liggande kolatomer och bildar tillsammans en metylendioxigrupp, kännetecknat därav att en 2-aminometyl-lH-2,3-dihydro-l,4-bensodiazepin förening enligt formeln II C!!2-IIH 'pp - i vilken formel R^, R2, R4, R5 och Rg är samma som ovan acyleras med en syra eller ett syraderivat enligt formeln III R3-(CH2)n-CO-Y III i vilken formel R3 och n är samma som ovan och Y är en hydroxigrupp eller en aminolytiskt avspaltbar grupp och man eventuellt i föreningar enligt den allmänna formeln I, där R5, R^i och/eller R^2 är lägre alkanoyloxi- eller alkanoyl-aminogrupper, hydrolyserar dessa grupper tili fr ia hydroxi-eller aminogrupper, och eventuellt separerar de racemiska blandningarna av föreningar med formeln I i sinä optiskt aktiva isomerer, och eventuellt omvandlar föreningarna enliggt formeln I tili sinä syraadditionssalter eller omvandlar syra-additionssalter tili fr ia föreningar enligt formeln I. 57 6 8049
2. Förfarande enligt patentkravet 1 för framställning av 2-acylaminometyl-lH-2,3-dihydro-1,4-bensodiazepinföreningar, kännetecknat av att R3, R2r R4, R5/ ^6 och n är samma som ovan angivits R3 är gruppen a, där X är samma som ovan angivits och R7 är väte, lägre alkyl eller dä X är svavel kan R7 vara även fluor, klor eller brom, eller R3 är gruppen b, där Rg och Rg samma som ovan angivits eller R3 är gruppen cf där R^q är väte, eller R3 är gruppen d, där R^ är väte, lägre alkyl, lägre alkoxi, halogen eller cyano och R32 är väte, lägre alkyl, lägre alkoxi eller halogen eller R-j^ och R^ är bundna vid bredvid varandra liggande kolatomer och hildar tillsammans en metylendioxigrupp.
3. Förfarande för framställning av 1-metyl-2-((4-cyanobenso-yl) -aminometvl) -5- (3 '-tiofen) -1H-2,3-d ihydro-1,4-bensod iazepinföreningar medelst förfarandet enligt patentkravet 1.
4. 2-aminometyl-lH-2,3-d ihydro-1,4-bensod iazepinföreningar enligt den allmänna formeln Ha fl li j R1 IIa *V i vilken formel R3 är väte eller lägre alkyl R2 är väte R4' är näqon av följande grupper a', b eller c. 58 68049 -0-«7 "O-'" k a· b c i vilka formler R7 är väte, lägre alkyl eller haloqen, Rg är väte eller lägre alkvl, Rg är väte, R^q är väte eller klor, R5 är väte, lägre alkyl, lägre alkoxi, halogen eller nitro, och Rg är väte, lägre alkyl, lägre alkoxi eller halogen eller R5 och Rg är bundna vid bredvid varandra liggande kolatomer och bildar tillsammans en metvlendioxigrupp, samt deras optiska isomerer och deras syraadditionssalter.
5. 2-azidometyl-lH-2, 3-dihydro-l ,4-bensod iät sepin för en ingar enligt formeln IV ?i l>“Λ Rs"pO M i vilken formel R^ är väte eller lägre alkyl R4 är en grupp enligt nägon av följande formler
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19813124013 DE3124013A1 (de) | 1981-06-19 | 1981-06-19 | 2-acylaminomethyl-1,4-benzodiazepin-verbindungen sowie verfahren und zwischenprodukte zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
DE3124013 | 1981-06-19 |
Publications (4)
Publication Number | Publication Date |
---|---|
FI822148A0 FI822148A0 (fi) | 1982-06-15 |
FI822148L FI822148L (fi) | 1982-12-20 |
FI68049B FI68049B (fi) | 1985-03-29 |
FI68049C true FI68049C (fi) | 1985-07-10 |
Family
ID=6134869
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
FI822148A FI68049C (fi) | 1981-06-19 | 1982-06-15 | Foerfarande foer framstaellning av farmakologiskt verksamma 2-cyl-aminometyl-1,4-bensodiazepinfoereningar samt vid dera s ramstaellning anvaendbara mellanprodukter |
Country Status (21)
Country | Link |
---|---|
US (2) | US4497740A (sv) |
EP (1) | EP0068240B1 (sv) |
JP (1) | JPS58968A (sv) |
AT (1) | ATE15802T1 (sv) |
AU (1) | AU547857B2 (sv) |
CA (1) | CA1188299A (sv) |
DD (1) | DD202553A5 (sv) |
DE (2) | DE3124013A1 (sv) |
DK (1) | DK274082A (sv) |
ES (1) | ES8304564A1 (sv) |
FI (1) | FI68049C (sv) |
GR (1) | GR76499B (sv) |
HU (1) | HU188178B (sv) |
IE (1) | IE53464B1 (sv) |
IL (1) | IL66076A (sv) |
NO (1) | NO157420C (sv) |
NZ (1) | NZ201007A (sv) |
PH (1) | PH17911A (sv) |
PT (1) | PT74971B (sv) |
SU (1) | SU1245259A3 (sv) |
ZA (1) | ZA823780B (sv) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4724237A (en) * | 1984-06-26 | 1988-02-09 | Merck & Co., Inc. | 2-substituted-aminomethyl-1,4-benzodiazepines |
US4899425A (en) * | 1986-11-14 | 1990-02-13 | Mahlo Gmbh & Co. Kg. | Apparatus for straightening weft yarns in fabrics |
US6458784B1 (en) | 1994-06-29 | 2002-10-01 | Smithkline Beecham Corporation | Vitronectin receptor antagonists |
US5977101A (en) * | 1995-06-29 | 1999-11-02 | Smithkline Beecham Corporation | Benzimidazoles/Imidazoles Linked to a Fibrinogen Receptor Antagonist Template Having Vitronectin Receptor Antagonist Activity |
RU2528049C2 (ru) * | 2009-09-18 | 2014-09-10 | Мицубиси Гэс Кемикал Компани, Инк. | Способ получения циклогексилалкилкетонов |
Family Cites Families (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US28315A (en) * | 1860-05-15 | Improvement in method of decomposing fats into fatty acids and glycerine | ||
NL131733C (sv) * | 1961-06-20 | |||
USRE28315E (en) | 1964-06-15 | 1975-01-21 | Cooc.hi | |
US3560482A (en) * | 1967-12-08 | 1971-02-02 | Sumitomo Chemical Co | Method for producing benzodiazepine derivatives |
US3546212A (en) * | 1968-06-12 | 1970-12-08 | Hoffmann La Roche | Oxidation of benzodiazepines with ruthenium tetroxide |
US3773765A (en) * | 1971-08-18 | 1973-11-20 | Upjohn Co | S-triazino(1,2-a)(1,4)benzodiazepine-1,3-(2h,4h and 2h,5h)diones |
US3847935A (en) * | 1972-04-12 | 1974-11-12 | Upjohn Co | 5-substituted 1-(3h,1,4-benzodiazepin-2-yl)-2-imidazolidinones |
US4244869A (en) * | 1972-05-03 | 1981-01-13 | Kali-Chemie A.G. | Benzodiazepine derivatives and process of making them |
DE2221558C2 (de) * | 1972-05-03 | 1982-12-02 | Kali-Chemie Ag, 3000 Hannover | 5-Phenyl-2,3-dihydro-1H-1,4-benzodiazepine und ihre Säureadditionssalze, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel |
DE2314993A1 (de) * | 1973-03-26 | 1974-10-03 | Kali Chemie Pharma Gmbh | Neue benzodiazepinderivate und verfahren zu deren herstellung |
DE2353187A1 (de) * | 1973-05-02 | 1974-11-14 | Kali Chemie Ag | Neue benzodiazepinderivate |
DE2353160C2 (de) * | 1973-05-02 | 1986-07-17 | Kali-Chemie Ag, 3000 Hannover | 5-Phenyl-2,3-dihydro-1H-1,4-benzodiazepine, ihre Säureadditionssalze und diese Verbindungen enthaltende Arzneimittel |
DE2353165C2 (de) * | 1973-05-03 | 1983-06-09 | Kali-Chemie Ag, 3000 Hannover | 1-Methyl-3-hydroxy-6-(2-chlorphenyl)-1,2,3,4-tetrahydro-1,5-benzodiazocinderivate |
US3925358A (en) * | 1973-07-27 | 1975-12-09 | Hoffmann La Roche | 1-Lower alkyl-2-substituted-1,4-benzodiazepines |
US4368159A (en) * | 1978-05-15 | 1983-01-11 | Hoffmann-La Roche Inc. | Intermediates to produce imidazodiazepines |
DE2952279A1 (de) * | 1979-12-24 | 1981-06-25 | Kali-Chemie Pharma Gmbh, 3000 Hannover | Neue 2-acylaminomethyl-1,4-benzodiazepine und deren salze sowie verfahren zu ihrer herstellung und diese verbindungen enthaltende arzneimittel |
HU186760B (en) * | 1981-03-12 | 1985-09-30 | Gyogyszerkutato Intezet | Process for preparing 3,4-dihydro-5h-2,3-aenzodiazepine derivatives |
-
1981
- 1981-06-19 DE DE19813124013 patent/DE3124013A1/de not_active Withdrawn
-
1982
- 1982-05-28 ZA ZA823780A patent/ZA823780B/xx unknown
- 1982-05-28 PT PT74971A patent/PT74971B/pt unknown
- 1982-06-04 ES ES512844A patent/ES8304564A1/es not_active Expired
- 1982-06-08 US US06/386,303 patent/US4497740A/en not_active Expired - Fee Related
- 1982-06-11 JP JP57099446A patent/JPS58968A/ja active Granted
- 1982-06-12 DE DE8282105139T patent/DE3266521D1/de not_active Expired
- 1982-06-12 EP EP82105139A patent/EP0068240B1/de not_active Expired
- 1982-06-12 AT AT82105139T patent/ATE15802T1/de not_active IP Right Cessation
- 1982-06-15 FI FI822148A patent/FI68049C/fi not_active IP Right Cessation
- 1982-06-15 DD DD82240747A patent/DD202553A5/de unknown
- 1982-06-17 IL IL66076A patent/IL66076A/xx unknown
- 1982-06-17 GR GR68467A patent/GR76499B/el unknown
- 1982-06-18 NO NO822037A patent/NO157420C/no unknown
- 1982-06-18 NZ NZ201007A patent/NZ201007A/en unknown
- 1982-06-18 AU AU84991/82A patent/AU547857B2/en not_active Ceased
- 1982-06-18 DK DK274082A patent/DK274082A/da not_active Application Discontinuation
- 1982-06-18 CA CA000405518A patent/CA1188299A/en not_active Expired
- 1982-06-18 HU HU821988A patent/HU188178B/hu unknown
- 1982-06-18 PH PH27446A patent/PH17911A/en unknown
- 1982-06-18 SU SU823453651A patent/SU1245259A3/ru active
- 1982-06-21 IE IE1468/82A patent/IE53464B1/en unknown
-
1986
- 1986-04-03 US US06/847,112 patent/US4649137A/en not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
JPS58968A (ja) | 1983-01-06 |
EP0068240A1 (de) | 1983-01-05 |
AU8499182A (en) | 1982-12-23 |
NO157420B (no) | 1987-12-07 |
NO157420C (no) | 1988-03-16 |
ZA823780B (en) | 1983-03-30 |
DK274082A (da) | 1982-12-20 |
US4497740A (en) | 1985-02-05 |
FI68049B (fi) | 1985-03-29 |
ES512844A0 (es) | 1983-03-01 |
FI822148A0 (fi) | 1982-06-15 |
NO822037L (no) | 1982-12-20 |
FI822148L (fi) | 1982-12-20 |
AU547857B2 (en) | 1985-11-07 |
DE3266521D1 (en) | 1985-10-31 |
IL66076A0 (en) | 1982-09-30 |
HU188178B (en) | 1986-03-28 |
PH17911A (en) | 1985-01-25 |
SU1245259A3 (ru) | 1986-07-15 |
DE3124013A1 (de) | 1982-12-30 |
GR76499B (sv) | 1984-08-10 |
CA1188299A (en) | 1985-06-04 |
EP0068240B1 (de) | 1985-09-25 |
IE821468L (en) | 1982-12-19 |
ATE15802T1 (de) | 1985-10-15 |
DD202553A5 (de) | 1983-09-21 |
PT74971A (en) | 1982-06-01 |
US4649137A (en) | 1987-03-10 |
JPH0433795B2 (sv) | 1992-06-04 |
IE53464B1 (en) | 1988-11-23 |
PT74971B (en) | 1983-12-29 |
IL66076A (en) | 1986-03-31 |
NZ201007A (en) | 1985-05-31 |
ES8304564A1 (es) | 1983-03-01 |
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