OA12920A - 4-(3,5-dicyanophenoxy)pyrazole derivatives for useas reverse transcriptase modulators in the treatment of I.A H.I.V. - Google Patents

4-(3,5-dicyanophenoxy)pyrazole derivatives for useas reverse transcriptase modulators in the treatment of I.A H.I.V. Download PDF

Info

Publication number: OA12920A
Authority: OA; OAPI
Prior art keywords: compound; formula; dérivative; pharmaceutically acceptable; pharmaceutical composition
Prior art date: 2002-09-16

Application number

OA1200500067A

Other languages

English (en)

Inventor

Charles Eric Mowbray

David Anthony Price

Matthew Duncan Selby

Paul Anthony Stupple

Original Assignee

Pfizer

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.)

2002-09-16

Filing date

2003-09-08

Publication date

2006-10-13

2003-09-08 Application filed by Pfizer filed Critical Pfizer

2006-10-13 Publication of OA12920A publication Critical patent/OA12920A/en

Links

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QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
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238000002638 palliative care Methods 0.000 description 1
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239000008024 pharmaceutical diluent Substances 0.000 description 1
229940124531 pharmaceutical excipient Drugs 0.000 description 1
239000012071 phase Substances 0.000 description 1
NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
239000010452 phosphate Substances 0.000 description 1
239000008363 phosphate buffer Substances 0.000 description 1
150000003014 phosphoric acid esters Chemical class 0.000 description 1
229960002169 plerixafor Drugs 0.000 description 1
239000001818 polyoxyethylene sorbitan monostearate Substances 0.000 description 1
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229910052700 potassium Inorganic materials 0.000 description 1
239000011591 potassium Substances 0.000 description 1
BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Substances [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 description 1
229910000027 potassium carbonate Inorganic materials 0.000 description 1
239000003755 preservative agent Substances 0.000 description 1
230000002335 preservative effect Effects 0.000 description 1
239000000651 prodrug Substances 0.000 description 1
229940002612 prodrug Drugs 0.000 description 1
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239000003380 propellant Substances 0.000 description 1
238000011321 prophylaxis Methods 0.000 description 1
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239000011541 reaction mixture Substances 0.000 description 1
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229960000311 ritonavir Drugs 0.000 description 1
NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 description 1
229920006395 saturated elastomer Polymers 0.000 description 1
HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 description 1
150000004760 silicates Chemical class 0.000 description 1
239000000377 silicon dioxide Substances 0.000 description 1
229910052708 sodium Inorganic materials 0.000 description 1
239000011734 sodium Substances 0.000 description 1
235000017557 sodium bicarbonate Nutrition 0.000 description 1
229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
239000011780 sodium chloride Substances 0.000 description 1
239000001509 sodium citrate Substances 0.000 description 1
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
229960001790 sodium citrate Drugs 0.000 description 1
235000011083 sodium citrates Nutrition 0.000 description 1
QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
229940080313 sodium starch Drugs 0.000 description 1
239000008247 solid mixture Substances 0.000 description 1
239000001587 sorbitan monostearate Substances 0.000 description 1
235000011076 sorbitan monostearate Nutrition 0.000 description 1
229940035048 sorbitan monostearate Drugs 0.000 description 1
235000019337 sorbitan trioleate Nutrition 0.000 description 1
229960000391 sorbitan trioleate Drugs 0.000 description 1
239000007858 starting material Substances 0.000 description 1
229960001203 stavudine Drugs 0.000 description 1
239000008117 stearic acid Substances 0.000 description 1
229940086735 succinate Drugs 0.000 description 1
KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 description 1
239000005720 sucrose Substances 0.000 description 1
150000003456 sulfonamides Chemical class 0.000 description 1
150000003462 sulfoxides Chemical class 0.000 description 1
YBBRCQOCSYXUOC-UHFFFAOYSA-N sulfuryl dichloride Chemical compound ClS(Cl)(=O)=O YBBRCQOCSYXUOC-UHFFFAOYSA-N 0.000 description 1
239000000829 suppository Substances 0.000 description 1
239000000375 suspending agent Substances 0.000 description 1
239000003765 sweetening agent Substances 0.000 description 1
239000000454 talc Substances 0.000 description 1
229910052623 talc Inorganic materials 0.000 description 1
VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 description 1
CQKAPARXKPTKBK-UHFFFAOYSA-N tert-butylazanium;bromide Chemical compound Br.CC(C)(C)N CQKAPARXKPTKBK-UHFFFAOYSA-N 0.000 description 1
JRMUNVKIHCOMHV-UHFFFAOYSA-M tetrabutylammonium bromide Chemical compound [Br-].CCCC[N+](CCCC)(CCCC)CCCC JRMUNVKIHCOMHV-UHFFFAOYSA-M 0.000 description 1
DPKBAXPHAYBPRL-UHFFFAOYSA-M tetrabutylazanium;iodide Chemical compound [I-].CCCC[N+](CCCC)(CCCC)CCCC DPKBAXPHAYBPRL-UHFFFAOYSA-M 0.000 description 1
CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
229960000838 tipranavir Drugs 0.000 description 1
SUJUHGSWHZTSEU-FYBSXPHGSA-N tipranavir Chemical compound C([C@@]1(CCC)OC(=O)C([C@H](CC)C=2C=C(NS(=O)(=O)C=3N=CC(=CC=3)C(F)(F)F)C=CC=2)=C(O)C1)CC1=CC=CC=C1 SUJUHGSWHZTSEU-FYBSXPHGSA-N 0.000 description 1
CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
229940029284 trichlorofluoromethane Drugs 0.000 description 1
229940111527 trizivir Drugs 0.000 description 1
229960000281 trometamol Drugs 0.000 description 1
230000003612 virological effect Effects 0.000 description 1
BCEHBSKCWLPMDN-MGPLVRAMSA-N voriconazole Chemical compound C1([C@H](C)[C@](O)(CN2N=CN=C2)C=2C(=CC(F)=CC=2)F)=NC=NC=C1F BCEHBSKCWLPMDN-MGPLVRAMSA-N 0.000 description 1
229960004740 voriconazole Drugs 0.000 description 1
238000005406 washing Methods 0.000 description 1
239000001993 wax Substances 0.000 description 1
238000005550 wet granulation Methods 0.000 description 1
239000003871 white petrolatum Substances 0.000 description 1
238000002424 x-ray crystallography Methods 0.000 description 1
229960000523 zalcitabine Drugs 0.000 description 1
229960002555 zidovudine Drugs 0.000 description 1
239000011701 zinc Substances 0.000 description 1
229910052725 zinc Inorganic materials 0.000 description 1
GTLDTDOJJJZVBW-UHFFFAOYSA-N zinc cyanide Chemical compound [Zn+2].N#[C-].N#[C-] GTLDTDOJJJZVBW-UHFFFAOYSA-N 0.000 description 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/18—One oxygen or sulfur atom
- 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
- A61K31/415—1,2-Diazoles
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
- 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
- C07C255/00—Carboxylic acid nitriles
- C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
- C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/004—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reaction with organometalhalides
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
- C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
- C07C45/63—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/29—Saturated compounds containing keto groups bound to rings
- C07C49/293—Saturated compounds containing keto groups bound to rings to a three- or four-membered ring
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
- C07C49/29—Saturated compounds containing keto groups bound to rings
- C07C49/327—Saturated compounds containing keto groups bound to rings containing halogen
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring

Landscapes

Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Health & Medical Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
Veterinary Medicine (AREA)
Pharmacology & Pharmacy (AREA)
Virology (AREA)
General Health & Medical Sciences (AREA)
General Chemical & Material Sciences (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Communicable Diseases (AREA)
Oncology (AREA)
Molecular Biology (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
AIDS & HIV (AREA)
Tropical Medicine & Parasitology (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

OA1200500067A 2002-09-16 2003-09-08 4-(3,5-dicyanophenoxy)pyrazole derivatives for useas reverse transcriptase modulators in the treatment of I.A H.I.V. OA12920A (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
GBGB0221477.3A GB0221477D0 (en)	2002-09-16	2002-09-16	Chemical compounds
GBGB0223354.2A GB0223354D0 (en)	2002-09-16	2002-10-08	Chemical compounds

Publications (1)

Publication Number	Publication Date
OA12920A true OA12920A (en)	2006-10-13

Family

ID=31995706

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200500067A OA12920A (en)	2002-09-16	2003-09-08	4-(3,5-dicyanophenoxy)pyrazole derivatives for useas reverse transcriptase modulators in the treatment of I.A H.I.V.

Country Status (20)

Country	Link
EP (1)	EP1542679B1 (es)
JP (1)	JP2006504792A (es)
KR (1)	KR20050043962A (es)
CN (1)	CN1681494A (es)
AP (1)	AP2005003248A0 (es)
AU (1)	AU2003263422A1 (es)
BR (1)	BR0314243A (es)
CA (1)	CA2496315A1 (es)
DE (1)	DE60311284T2 (es)
EA (1)	EA200500287A1 (es)
EC (1)	ECSP055673A (es)
GB (2)	GB0221477D0 (es)
HR (1)	HRP20050222A2 (es)
IS (1)	IS7705A (es)
MA (1)	MA27435A1 (es)
MX (1)	MXPA05002963A (es)
NO (1)	NO20051833L (es)
OA (1)	OA12920A (es)
PL (1)	PL375976A1 (es)
WO (1)	WO2004024147A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US20080132549A1 (en) *	2004-04-14	2008-06-05	Pfizer Inc.	Sulphur-Linked Imidazone Compounds for the Treatment of Hiv/Aids
DE102008015033A1 (de) *	2008-03-17	2009-09-24	Aicuris Gmbh & Co. Kg	Substituierte (Pyrazolyl-carbonyl)imidazolidinone und ihre Verwendung
DE102008015032A1 (de)	2008-03-17	2009-09-24	Aicuris Gmbh & Co. Kg	Substituierte Pyrazolamide und ihre Verwendung
DE102008062863A1 (de)	2008-12-17	2010-06-24	Aicuris Gmbh & Co. Kg	Substituierte (Thiophenyl-carbonyl)imidazolidinone und ihre Verwendung
DE102008062878A1 (de)	2008-12-17	2010-06-24	Aicuris Gmbh & Co. Kg	Substituierte Furancarboxamide und ihre Verwendung

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* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US3303200A (en) *	1963-11-05	1967-02-07	American Home Prod	Pyrazole-1-ethanol derivatives
GB0016787D0 (en) *	2000-07-07	2000-08-30	Pfizer Ltd	Compounds useful in therapy
EE05400B1 (et) *	2001-04-10	2011-04-15	Pfizer Inc.	Prasoolderivaadid, neid v?i nende farmatseutiliselt vastuv?etavaid sooli, solvaate v?i derivaate sisaldavad farmatseutilised kompositsioonid, nende kasutamine ning meetodid nende valmistamiseks

2002
- 2002-09-16 GB GBGB0221477.3A patent/GB0221477D0/en not_active Ceased
- 2002-10-08 GB GBGB0223354.2A patent/GB0223354D0/en not_active Ceased
2003
- 2003-09-08 OA OA1200500067A patent/OA12920A/en unknown
- 2003-09-08 DE DE60311284T patent/DE60311284T2/de not_active Expired - Fee Related
- 2003-09-08 AU AU2003263422A patent/AU2003263422A1/en not_active Abandoned
- 2003-09-08 EA EA200500287A patent/EA200500287A1/ru unknown
- 2003-09-08 HR HR20050222A patent/HRP20050222A2/hr not_active Application Discontinuation
- 2003-09-08 CN CNA038219603A patent/CN1681494A/zh active Pending
- 2003-09-08 PL PL03375976A patent/PL375976A1/xx not_active Application Discontinuation
- 2003-09-08 MX MXPA05002963A patent/MXPA05002963A/es unknown
- 2003-09-08 BR BR0314243-4A patent/BR0314243A/pt not_active IP Right Cessation
- 2003-09-08 AP AP2005003248A patent/AP2005003248A0/xx unknown
- 2003-09-08 JP JP2004571926A patent/JP2006504792A/ja not_active Withdrawn
- 2003-09-08 EP EP03795160A patent/EP1542679B1/en not_active Expired - Lifetime
- 2003-09-08 WO PCT/IB2003/003946 patent/WO2004024147A1/en not_active Ceased
- 2003-09-08 KR KR1020057004426A patent/KR20050043962A/ko not_active Ceased
- 2003-09-08 CA CA002496315A patent/CA2496315A1/en not_active Abandoned
2005
- 2005-02-21 IS IS7705A patent/IS7705A/is unknown
- 2005-03-14 EC EC2005005673A patent/ECSP055673A/es unknown
- 2005-03-16 MA MA28148A patent/MA27435A1/fr unknown
- 2005-04-15 NO NO20051833A patent/NO20051833L/no unknown

Also Published As

Publication number	Publication date
GB0221477D0 (en)	2002-10-23
EP1542679B1 (en)	2007-01-17
MA27435A1 (fr)	2005-07-01
BR0314243A (pt)	2005-07-26
DE60311284T2 (de)	2007-06-21
WO2004024147A1 (en)	2004-03-25
JP2006504792A (ja)	2006-02-09
CN1681494A (zh)	2005-10-12
PL375976A1 (en)	2005-12-12
NO20051833L (no)	2005-06-14
MXPA05002963A (es)	2005-05-27
CA2496315A1 (en)	2004-03-25
DE60311284D1 (de)	2007-03-08
IS7705A (is)	2005-02-21
EA200500287A1 (ru)	2005-10-27
AP2005003248A0 (en)	2005-03-31
KR20050043962A (ko)	2005-05-11
AU2003263422A1 (en)	2004-04-30
GB0223354D0 (en)	2002-11-13
HRP20050222A2 (en)	2005-10-31
ECSP055673A (es)	2005-07-06
EP1542679A1 (en)	2005-06-22

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