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PE20001549A1 - Derivados de bifenilo como antagonistas del receptor de neuroquinina 1 - Google Patents

Derivados de bifenilo como antagonistas del receptor de neuroquinina 1

Info

Publication number
PE20001549A1
PE20001549A1 PE2000000177A PE0001772000A PE20001549A1 PE 20001549 A1 PE20001549 A1 PE 20001549A1 PE 2000000177 A PE2000000177 A PE 2000000177A PE 0001772000 A PE0001772000 A PE 0001772000A PE 20001549 A1 PE20001549 A1 PE 20001549A1
Authority
PE
Peru
Prior art keywords
methyl
alkyl
biphenyl
neuroquinin
trifluoromethyl
Prior art date
Application number
PE2000000177A
Other languages
English (en)
Inventor
Michael Bos
Guido Galley
Torsten Hoffmann
Walter Hunkeler
Heinz Stadler
Thierry Godel
Patrick Schnider
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE20001549A1 publication Critical patent/PE20001549A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
    • C07C217/54—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/12—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C07C233/15—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/44—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a carbon atom of an unsaturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/66—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by halogen atoms or by nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Addiction (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A DERIVADOS DE BIFENILO DE FORMULA I, DONDE: R ES H, ALQUILO, ALCOXI, HALOGENO, AMINO, -N(R6)2, TRIFLUOROMETILO; R1 ES H, ALCOXI, HALOGENO; R Y R1 JUNTOS SON -CH=CH-CH=CH-; R2 ES HALOGENO, ALQUILO, TRIFLUOROMETILO; R3 ES H, ALQUILO; R4 ES H, AMINA TERCIARIA CICLICA SUSTITUIDA CON ALQUILO; R5 ES H, NITRO, AMINO, N(R6)2, R6 ES H, ALQUILO; X ES CONR6, (CH2)nO, (CH2)nNR6, NR6CO, NR6(CH2)n; n ES 1-2. SON COMPUESTOS PREFERIDOS ACIDO 2`-METIL-BIFENIL-2-CARBOXILICO-(3,5-BIS-TRIFLUOROMETIL-BENCIL)METIL-AMIDA, ACIDO 2'-METIL-5-(4-METIL-PIPERAZIN-1-IL)-BIFENIL-2-CARBOXILICO-(3,5-BISTRIFLUOROMETILO-BENCIL)METIL-AMIDA, ACIDO 2'-CLORO-5-(4-METIL-PIPERAZIN-1-IL)-BIFENIL-2-CARBOXILICO-(3,5-BISTRIFLUOROMETIL-BENCIL)METIL-AMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE NEUROQUININA 1 (NK-1) POR LO QUE PUEDE SER UTIL PARA EL TRATAMIENTO DEL DOLOR, CEFALEA, MIGRANA, ENFERMEDAD DE ALZHEIMER, ESCLEROSIS MULTIPLE, EDEMA
PE2000000177A 1999-03-09 2000-03-03 Derivados de bifenilo como antagonistas del receptor de neuroquinina 1 PE20001549A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP99104626 1999-03-09

Publications (1)

Publication Number Publication Date
PE20001549A1 true PE20001549A1 (es) 2001-01-09

Family

ID=8237723

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000000177A PE20001549A1 (es) 1999-03-09 2000-03-03 Derivados de bifenilo como antagonistas del receptor de neuroquinina 1

Country Status (33)

Country Link
US (2) US6291465B1 (es)
EP (1) EP1171419B1 (es)
JP (1) JP3839668B2 (es)
KR (1) KR100473247B1 (es)
CN (1) CN1152006C (es)
AR (1) AR043273A1 (es)
AT (1) ATE286018T1 (es)
AU (1) AU767449B2 (es)
BR (1) BR0008862A (es)
CA (1) CA2366205C (es)
CO (1) CO5160261A1 (es)
CZ (1) CZ20013190A3 (es)
DE (1) DE60017110T2 (es)
ES (1) ES2233338T3 (es)
HK (1) HK1045684B (es)
HR (1) HRP20010629A2 (es)
HU (1) HUP0201710A3 (es)
IL (2) IL145166A0 (es)
JO (1) JO2235B1 (es)
MA (1) MA26778A1 (es)
MY (1) MY121145A (es)
NO (1) NO20014356D0 (es)
NZ (1) NZ513824A (es)
PE (1) PE20001549A1 (es)
PL (1) PL201681B1 (es)
PT (1) PT1171419E (es)
RU (1) RU2238266C2 (es)
SI (1) SI1171419T1 (es)
TR (1) TR200102585T2 (es)
UY (1) UY26051A1 (es)
WO (1) WO2000053572A1 (es)
YU (1) YU64901A (es)
ZA (1) ZA200107259B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL350427A1 (en) 1999-02-24 2002-12-16 Hoffmann La Roche Phenyl− and pyridinyl derivatives as neurokinin 1 antagonists
AUPQ514600A0 (en) 2000-01-18 2000-02-10 James Cook University Brain injury treatment
TWI287003B (en) * 2000-07-24 2007-09-21 Hoffmann La Roche 4-phenyl-pyridine derivatives
US6642226B2 (en) 2001-02-06 2003-11-04 Hoffman-La Roche Inc. Substituted phenyl-piperidine methanone compounds
US6531597B2 (en) * 2001-02-13 2003-03-11 Hoffmann-La Roche Inc. Process for preparation of 2-phenyl acetic acid derivatives
NZ535366A (en) 2002-03-13 2007-07-27 Univ Tennessee Res Foundation Substituted tetrahydroisoquinoline compounds, methods of making, and their use
EP1888549A2 (en) * 2005-05-19 2008-02-20 Vertex Pharmaceuticals, Inc. Biaryls useful as modulators of ion channels
WO2006130493A2 (en) 2005-05-31 2006-12-07 Vertex Pharmaceuticals Incorporated Heterocycles useful as modulators of ion channels
DK2729147T3 (en) 2011-07-04 2017-12-18 Irbm - Science Park S P A NK-1 RECEPTOR ANTAGONISTS FOR TREATMENT OF CORNOVA
JP6905053B2 (ja) 2016-05-23 2021-07-21 中国医学科学院薬物研究所Ｉｎｓｔｉｔｕｔｅ Ｏｆ Ｍａｔｅｒｉａ Ｍｅｄｉｃａ， Ｃｈｉｎｅｓｅ Ａｃａｄｅｍｙ Ｏｆ Ｍｅｄｉｃａｌ Ｓｃｉｅｎｃｅｓ ベンジルフェニルエーテル誘導体、その調製方法、並びにその医薬組成物及び使用
EP4371613A3 (en) 2018-02-26 2024-07-24 Ospedale San Raffaele S.r.l. Compounds for use in the treatment of ocular pain
US20230134843A1 (en) 2020-03-11 2023-05-04 Ospedale San Raffaele S.R.L. Treatment of stem cell deficiency
CN115466195B (zh) * 2022-09-15 2024-04-19 中国科学院成都生物研究所 一类联苯类酰胺化合物及其制备方法和应用

Family Cites Families (10)

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Publication number Priority date Publication date Assignee Title
US5227484A (en) * 1982-01-14 1993-07-13 Merck Patent Gmbh Anisotropic compounds having nematic phase and liquid crystal mixtures
JPH06227913A (ja) * 1993-02-03 1994-08-16 Sumitomo Chem Co Ltd 安息香酸誘導体を有効成分とする植物病害防除剤
AU1108395A (en) * 1993-12-07 1995-06-27 Smithkline Beecham Plc Heterocyclic biphenylylamides useful as 5ht1d antagonists
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
WO1995018124A1 (en) 1993-12-29 1995-07-06 Merck Sharp & Dohme Limited Substituted morpholine derivatives and their use as therapeutic agents
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
JP3839518B2 (ja) * 1996-03-27 2006-11-01 ポーラ化成工業株式会社 抗真菌剤
IL131850A0 (en) 1997-04-18 2001-03-19 Pfizer Process and intermediates for the preparation of 4'-trifluoromethyl-biphenyl-2-carboxylic acid (1, 2, 3, 4-tetrahydro-isoquinolin-6-yl)-amide
US5972938A (en) 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
ATE277905T1 (de) * 1999-02-24 2004-10-15 Hoffmann La Roche 4-phenylpyridinderivate und deren verwendung als nk-1 rezeptorantagonisten

Also Published As

Publication number Publication date
HRP20010629A2 (en) 2002-08-31
NZ513824A (en) 2004-01-30
MY121145A (en) 2005-12-30
YU64901A (sh) 2005-07-19
DE60017110T2 (de) 2006-01-26
DE60017110D1 (de) 2005-02-03
HUP0201710A2 (en) 2002-10-28
CN1152006C (zh) 2004-06-02
JO2235B1 (en) 2004-10-07
EP1171419A1 (en) 2002-01-16
IL145166A (en) 2006-10-05
HK1045684A1 (en) 2002-12-06
KR100473247B1 (ko) 2005-03-08
HK1045684B (zh) 2004-11-26
BR0008862A (pt) 2002-01-02
US6291465B1 (en) 2001-09-18
AR043273A1 (es) 2005-07-27
CO5160261A1 (es) 2002-05-30
NO20014356L (no) 2001-09-07
CN1343197A (zh) 2002-04-03
WO2000053572A1 (en) 2000-09-14
ES2233338T3 (es) 2005-06-16
ATE286018T1 (de) 2005-01-15
HUP0201710A3 (en) 2002-11-28
PT1171419E (pt) 2005-04-29
PL201681B1 (pl) 2009-04-30
AU3161200A (en) 2000-09-28
US6552088B2 (en) 2003-04-22
KR20010111271A (ko) 2001-12-17
ZA200107259B (en) 2002-12-02
AU767449B2 (en) 2003-11-13
JP2002539112A (ja) 2002-11-19
CA2366205A1 (en) 2000-09-14
MA26778A1 (fr) 2004-12-20
PL350536A1 (en) 2002-12-16
JP3839668B2 (ja) 2006-11-01
CA2366205C (en) 2008-09-09
SI1171419T1 (en) 2005-06-30
NO20014356D0 (no) 2001-09-07
CZ20013190A3 (cs) 2002-02-13
UY26051A1 (es) 2000-09-29
RU2238266C2 (ru) 2004-10-20
EP1171419B1 (en) 2004-12-29
IL145166A0 (en) 2002-06-30
US20020040060A1 (en) 2002-04-04
TR200102585T2 (tr) 2002-01-21

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