DK200001669A - Nye carboxysubstituerede acycliske carboxamidderivater - Google Patents

Nye carboxysubstituerede acycliske carboxamidderivater Download PDF

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DK200001669A
DK200001669A DK200001669A DKPA200001669A DK200001669A DK 200001669 A DK200001669 A DK 200001669A DK 200001669 A DK200001669 A DK 200001669A DK PA200001669 A DKPA200001669 A DK PA200001669A DK 200001669 A DK200001669 A DK 200001669A
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carboxamide derivatives
hydrogen
substituted acyclic
group
acyclic carboxamide
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DK200001669A
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Timothy P Burkholder
George L Maynard
Elizabeth M Kudlacz
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Aventis Pharma Inc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61P11/14—Antitussive 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/64—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having an aryl radical as the second substituent in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • C07D211/66—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
    • 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
    • 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
    • C07D213/60—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 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
    • C07D213/61—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • 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
    • 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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Description

PATENTKRAV: 1. Forbindelse med formlen
Figure DK200001669AD00031
hvori Ri betyder fra 1 til 3 substituenter, som hver især uafhængigt er valgt blandt hydrogen, halogen, C(1-6)alkyl og C(1-6)alkoxy, R2 betyder hydrogen eller en gruppe valgt blandt
Figure DK200001669AD00032
hvori R3 er valgt blandt hydrogen, C(1-4)alkyl og -CF3, Ari er en gruppe valgt blandt
Figure DK200001669AD00033
hvori R4 betyder fra 1 til 3 substituenter, som hver især uafhængigt er valgt blandt hydrogen, halogen, hydroxy, -CF3, C(1-6)alkyl og C(1-6)alkoxy, R5 betyder fra 1 til 2 substituenter, som hver især uafhængigt er valgt blandt hydrogen, halogen, C(1-6)alkyl og C(1-6)alkoxy,
Ar2 er en gruppe valgt blandt
Figure DK200001669AD00041
og
Figure DK200001669AD00042
hvori R6 betyder fra 1 til 3 substituenter, som hver især uafhængigt er valgt blandt hydrogen, halogen, -CF3, C(1-6)alkyl og C(1-6)alkoxy, R7 betyder fra 1 til 2 substituenter, som hver især uafhængigt er valgt blandt hydrogen, halogen, C(1-6)alkyl og C(1-6)alkoxy, X betyder en gruppe valgt blandt
Figure DK200001669AD00043
hvori Y betyder -O- eller -CH2-, p betyder et helt tal fra 1 til 4, R10 er valgt blandt hydrogen og C(1-6)alkyl, og stereoisomerer og farmaceutisk acceptable salte deraf. 2. Forbindelse ifølge krav 1, hvori Ri betyder 3,4,5-trimethoxy. 3. Forbindelse ifølge krav 1, hvori R2 betyder gruppen
Figure DK200001669AD00051
hvori R3 betyder hydrogen. 4. Forbindelse ifølge krav 1, hvori Ri betyder 2-methoxy, og R2 er i 5-stilling og betyder gruppen
Figure DK200001669AD00052
hvori R3 betyder hydrogen. 5. Forbindelse ifølge krav 1, hvori An betyder gruppen
Figure DK200001669AD00053
hvori R4 er som defineret i krav 1. 6. Forbindelse ifølge krav 1, hvori An er valgt blandt phenyl, 3,4-dichlorphenyl og 4-fluorphenyl. 7. Forbindelse ifølge krav 1, hvori Ar2 betyder phenyl. 8. Forbindelse ifølge krav 1, hvori X betyder gruppen
Figure DK200001669AD00061
hvori p og R10 er som defineret i krav 1. 9. Forbindelse ifølge krav 8, hvori p betyder 1. 10. Forbindelse ifølge krav 8, hvori p betyder 2. 11. Forbindelse ifølge krav 9 eller 10, hvori Rio betyder hydrogen. 12. Forbindelse ifølge krav 9 eller 10, hvori Rio betyder ethyl. 13. Forbindelse ifølge ethvert af kravene 2, 3, 4, 5, 6 eller 7, hvori X betyder gruppen
Figure DK200001669AD00062
hvori p betyder 1 eller 2, og Ri0 er valgt blandt hydrogen og ethyl. 14. Forbindelse ifølge krav 1, hvori Ri betyder 3,4,5-trimethoxy, Ari betyder gruppen
Figure DK200001669AD00063
hvori R4 er som defineret i krav 1, Ar2 betyder phenyl, og X betyder gruppen
Figure DK200001669AD00071
hvori p betyder 1 eller 2, og Rio er valgt blandt hydrogen og ethyl. 15. Forbindelse ifølge krav 1, hvori R2 betyder gruppen
Figure DK200001669AD00072
hvori R3 betyder hydrogen, Ari betyder gruppen
Figure DK200001669AD00073
hvori R4 er som defineret i krav 1, Ar2 betyder phenyl, og X betyder gruppen
Figure DK200001669AD00074
hvori p betyder 1 eller 2, og R10 er valgt blandt hydrogen og ethyl. 16. Forbindelse ifølge krav 1, hvori Ri betyder 2-methoxy, og R2 er i 5-stilling og betyder gruppen
Figure DK200001669AD00081
hvori R3 betyder hydrogen, An er valgt blandt phenyl, 3,4-dichlorphenyl og 4-fluorphenyl, Ar2 betyder phenyl, og X betyder gruppen
Figure DK200001669AD00082
hvori p og R10 er som defineret i krav 1. 17. Forbindelse ifølge krav 16, hvori p betyder 1 eller 2, og R10 betyder hydrogen. 18. Forbindelse ifølge krav 16, hvori p betyder 1 eller 2, og R10 betyder ethyl. 19. Forbindelse ifølge krav 1, hvor forbindelsen er (R)- eller (S)-N-methyl-N-(4-(4-phenyl-4-((4-carboethoxymethylpiperazin-1-yl)carboxamido)piperidin-1-yl)-2-(3,4-di-chlorphenyl)butyl)-2-methoxy-5-(1H-tetrazol-1-yl)benzamid eller en blanding deraf. 20. Farmaceutisk præparat indeholdende en forbindelse ifølge krav 1 og en farmaceutisk acceptabel bærer. 21. Metode til behandling af astma hos en patient med behov derfor, omfattende indgivelse til patienten af en terapeutisk effektiv mængde af en forbindelse ifølge krav 1.
DK200001669A 1998-05-15 2000-11-09 Nye carboxysubstituerede acycliske carboxamidderivater DK200001669A (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US7961098A 1998-05-15 1998-05-15
PCT/US1999/009450 WO1999059972A1 (en) 1998-05-15 1999-04-30 Carboxy substituted carboxamide derivatives as tachykinin receptor antagonists

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JP (1) JP4132671B2 (da)
KR (1) KR20010043598A (da)
CN (1) CN1136191C (da)
AR (1) AR015298A1 (da)
AT (1) ATE286882T1 (da)
AU (1) AU743487B2 (da)
DE (1) DE69923173T2 (da)
DK (1) DK200001669A (da)
ES (1) ES2233042T3 (da)
HU (1) HUP0102531A3 (da)
IL (1) IL139262A (da)
MX (1) MXPA00011204A (da)
NO (1) NO319766B1 (da)
NZ (1) NZ507432A (da)
PT (1) PT1077942E (da)
SI (1) SI1077942T1 (da)
TW (1) TWI228122B (da)
WO (1) WO1999059972A1 (da)
ZA (1) ZA200006606B (da)

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AU2001290743A1 (en) * 2000-09-14 2002-03-26 Ortho-Mcneil Pharmaceutical, Inc. Solid salt forms of n-(2-(4-(2-(1-methylethoxy)phenyl)-1-piperazinyl)ethyl)-2-oxo-1-piperidineacetamide
WO2004005256A2 (en) * 2002-07-03 2004-01-15 Glaxo Group Limited Substituted 4-phenyl-piperidin-amides as tachykinin antagonists and serotonin reptake inhibitors
US8093268B2 (en) 2007-01-24 2012-01-10 Glaxo Group Limited Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-)

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GB9502644D0 (en) * 1995-02-10 1995-03-29 Zeneca Ltd Heterocyclic derivatives
FR2738245B1 (fr) * 1995-08-28 1997-11-21 Sanofi Sa Nouveaux derives de piperidine, procede pour leur obtention et compositions pharmaceutiques les contenant

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SI1077942T1 (en) 2005-06-30
IL139262A0 (en) 2001-11-25
TWI228122B (en) 2005-02-21
CN1301253A (zh) 2001-06-27
EP1077942A1 (en) 2001-02-28
DE69923173T2 (de) 2006-01-05
ES2233042T3 (es) 2005-06-01
EP1077942B1 (en) 2005-01-12
KR20010043598A (ko) 2001-05-25
NO20005756L (no) 2001-01-12
JP2002515487A (ja) 2002-05-28
AU743487B2 (en) 2002-01-24
MXPA00011204A (es) 2003-04-22
ZA200006606B (en) 2002-02-14
DE69923173D1 (en) 2005-02-17
NZ507432A (en) 2003-08-29
AU3775699A (en) 1999-12-06
NO319766B1 (no) 2005-09-12
WO1999059972A1 (en) 1999-11-25
PT1077942E (pt) 2005-03-31
AR015298A1 (es) 2001-04-18
HUP0102531A2 (hu) 2001-11-28
HUP0102531A3 (en) 2003-01-28
NO20005756D0 (no) 2000-11-14
ATE286882T1 (de) 2005-01-15
JP4132671B2 (ja) 2008-08-13
CN1136191C (zh) 2004-01-28

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