PE20040944A1 - NUEVA MODIFICACION CRISTALINA DE LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA - Google Patents

NUEVA MODIFICACION CRISTALINA DE LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA

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Publication number
PE20040944A1
PE20040944A1 PE2004000110A PE2004000110A PE20040944A1 PE 20040944 A1 PE20040944 A1 PE 20040944A1 PE 2004000110 A PE2004000110 A PE 2004000110A PE 2004000110 A PE2004000110 A PE 2004000110A PE 20040944 A1 PE20040944 A1 PE 20040944A1
Authority
PE
Peru
Prior art keywords
phenyl
methyl
trifluormethyl
isobutyramide
fluor
Prior art date
Application number
PE2004000110A
Other languages
English (en)
Inventor
Torsten Hoffmann
Fabienne Hoffmann-Emery
Sonia Nick
Pius Waldmeier
Urs Schwitter
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 PE20040944A1 publication Critical patent/PE20040944A1/es

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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
    • C07D213/60—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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic 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
    • 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
    • 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
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • 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
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Detergent Compositions (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

SE REFIERE A UNA FORMA CRISTALINA DE 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-(1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA QUE PRESENTA UN MODELO DE DIFRACCION DE RAYOS X OBTENIDO CON UNA RADIACION Cuka A 2q IGUAL A 4,5, 6,4, 7,5, 7,7, 8,0, 8,2, 10,0, 10,2, 10,9, 11,1, 12,9, 13,4, 14,0, 14,5, 15,1, 15,6, 16,2, 16,5, 17,3, 17,5, 18,0, 18,9, 19,3, 19,5, 19,9, 20,1, 20,6, 21,0, 21,4, 22,7, 23,1 Y 23,6 Y UN ESPECTRO INFRARROJO CON BANDAS AGUDAS A 2925, 2854, 1637, 1604, 1484, 1395, 1375, 1285, 1230, 1172, 1125, 1082, 999, 943, 893, 868, 860, 782, 705, 684 cm-1, Y EN DONDE EL PUNTO DE FUSION EXTRAPOLADO (DSC) ES DE 137,2°C. LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-(1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA ES ACTIVA SOBRE EL RECEPTOR NK1 Y ES UTIL PARA EL TRATAMIENTO DE MIGRANNA, ARTRITIS REUMATOIDE, ASMA
PE2004000110A 2003-01-31 2004-01-28 NUEVA MODIFICACION CRISTALINA DE LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA PE20040944A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03002134 2003-01-31

Publications (1)

Publication Number Publication Date
PE20040944A1 true PE20040944A1 (es) 2004-12-14

Family

ID=32798734

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000110A PE20040944A1 (es) 2003-01-31 2004-01-28 NUEVA MODIFICACION CRISTALINA DE LA 2-(3,5-BIS-TRIFLUORMETIL-FENIL)-N-[6-1,1-DIOXO-1l6-TIOMORFOLIN-4-IL)-4-(4-FLUOR-2-METIL-FENIL)-PIRIDIN-3-IL]-N-METIL-ISOBUTIRAMIDA

Country Status (28)

Country Link
US (1) US7160881B2 (es)
EP (1) EP1592428B1 (es)
JP (1) JP5026702B2 (es)
KR (1) KR100700421B1 (es)
CN (1) CN100562320C (es)
AR (1) AR042980A1 (es)
AT (1) ATE366576T1 (es)
AU (1) AU2004208483B8 (es)
BR (1) BRPI0406702A (es)
CA (1) CA2514037C (es)
CL (1) CL2004000150A1 (es)
CO (1) CO5580750A2 (es)
DE (1) DE602004007486T2 (es)
ES (1) ES2290666T3 (es)
GT (1) GT200400009A (es)
HR (1) HRP20050664A2 (es)
IL (1) IL169600A (es)
MX (1) MXPA05008171A (es)
MY (1) MY135785A (es)
NO (1) NO20053431L (es)
NZ (1) NZ541243A (es)
PA (1) PA8594601A1 (es)
PE (1) PE20040944A1 (es)
PL (1) PL378404A1 (es)
RU (1) RU2330022C2 (es)
TW (1) TWI293294B (es)
WO (1) WO2004067007A1 (es)
ZA (1) ZA200505567B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4580426B2 (ja) 2004-07-06 2010-11-10 エフ．ホフマン−ラ ロシュ アーゲー Ｎｋ−１受容体拮抗薬の合成において中間体として使用されるカルボキサミド誘導体の製造方法
KR20070094666A (ko) 2005-02-25 2007-09-20 에프. 호프만-라 로슈 아게 약제 물질 분산성이 향상된 정제
MX2012002369A (es) * 2009-08-27 2012-03-29 Glaxosmithkline Llc Formas de anhidrato de un derivado de piridina.
CN103755592A (zh) * 2013-12-30 2014-04-30 镇江圣安医药有限公司 (2z)-氰基-3-羟基-n-[4-(三氟甲基)苯基]-2-丁烯酰胺的衍生物及其应用

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL111960A (en) 1993-12-17 1999-12-22 Merck & Co Inc Morpholines and thiomorpholines their preparation and pharmaceutical compositions containing them
CA2178219C (en) 1993-12-29 2005-03-22 Raymond Baker Substituted morpholine derivatives and their use as therapeutic agents
IL112778A0 (en) 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
US5972938A (en) * 1997-12-01 1999-10-26 Merck & Co., Inc. Method for treating or preventing psychoimmunological disorders
SE1035115T5 (sv) 1999-02-24 2015-08-04 Hoffmann La Roche 4-fenylpyridin-derivat och deras anvaendning som NK-1 receptor-antagonister
AU2002250876B2 (en) * 2001-04-23 2005-03-03 F. Hoffmann-La Roche Ag Use of NK-1 receptor antagonists against benign prostatic hyperplasia
US6849624B2 (en) * 2001-07-31 2005-02-01 Hoffmann-La Roche Inc. Aromatic and heteroaromatic substituted amides

Also Published As

Publication number Publication date
DE602004007486T2 (de) 2008-04-30
AU2004208483B2 (en) 2008-03-06
NO20053431L (no) 2005-10-05
PA8594601A1 (es) 2004-09-16
DE602004007486D1 (de) 2007-08-23
MXPA05008171A (es) 2005-10-05
WO2004067007A1 (en) 2004-08-12
US7160881B2 (en) 2007-01-09
NZ541243A (en) 2008-04-30
EP1592428B1 (en) 2007-07-11
CO5580750A2 (es) 2005-11-30
BRPI0406702A (pt) 2005-12-20
CN100562320C (zh) 2009-11-25
AU2004208483B8 (en) 2008-04-03
US20040186100A1 (en) 2004-09-23
CL2004000150A1 (es) 2005-01-07
CA2514037C (en) 2012-03-13
CN1744900A (zh) 2006-03-08
NO20053431D0 (no) 2005-07-14
ES2290666T3 (es) 2008-02-16
EP1592428A1 (en) 2005-11-09
TW200510358A (en) 2005-03-16
AR042980A1 (es) 2005-07-13
KR100700421B1 (ko) 2007-03-28
RU2005127216A (ru) 2006-04-10
IL169600A (en) 2010-11-30
HRP20050664A2 (en) 2006-12-31
RU2330022C2 (ru) 2008-07-27
TWI293294B (en) 2008-02-11
ZA200505567B (en) 2007-05-30
KR20050096964A (ko) 2005-10-06
PL378404A1 (pl) 2006-04-03
CA2514037A1 (en) 2004-08-12
JP5026702B2 (ja) 2012-09-19
AU2004208483A1 (en) 2004-08-12
GT200400009A (es) 2004-12-01
ATE366576T1 (de) 2007-08-15
JP2006514999A (ja) 2006-05-18
MY135785A (en) 2008-06-30

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