EA200601418A1 - ПРОИЗВОДНЫЕ 1Н-ТИЕНО [2,3-с] ПИРАЗОЛА, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ИСПОЛЬЗОВАНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ - Google Patents

ПРОИЗВОДНЫЕ 1Н-ТИЕНО [2,3-с] ПИРАЗОЛА, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ИСПОЛЬЗОВАНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ

Info

Publication number
EA200601418A1
EA200601418A1 EA200601418A EA200601418A EA200601418A1 EA 200601418 A1 EA200601418 A1 EA 200601418A1 EA 200601418 A EA200601418 A EA 200601418A EA 200601418 A EA200601418 A EA 200601418A EA 200601418 A1 EA200601418 A1 EA 200601418A1
Authority
EA
Eurasian Patent Office
Prior art keywords
thieno
derivatives
pyrazoles
intended
kinase inhibitors
Prior art date
Application number
EA200601418A
Other languages
English (en)
Other versions
EA011032B1 (ru
Inventor
Даниеле Фанчелли
Симона Бинди
Марио Варази
Паола Вианелло
Серджо Виольо
Даниа Тезеи
Original Assignee
Пфайзер Италия С.Р.Л.
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 Пфайзер Италия С.Р.Л. filed Critical Пфайзер Италия С.Р.Л.
Publication of EA200601418A1 publication Critical patent/EA200601418A1/ru
Publication of EA011032B1 publication Critical patent/EA011032B1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • 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
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pulmonology (AREA)
  • Vascular Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

В заявке раскрыты производные тиено[2,3-с]пиразола формулы (I) и их фармацевтические приемлемые соли, как определено в описании, способ получения и фармацевтические композиции, включающие их; соединения по изобретению можно использовать в терапии при лечении заболеваний, связанных с нарушением регуляции активности киназы, подобных раку.
EA200601418A 2004-02-03 2005-02-02 ПРОИЗВОДНЫЕ 1H-ТИЕНО[2,3-c]ПИРАЗОЛА, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ИСПОЛЬЗОВАНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ EA011032B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US54145204P 2004-02-03 2004-02-03
PCT/EP2005/001021 WO2005074922A1 (en) 2004-02-03 2005-02-02 1H-THIENO[2,3-c]PYRAZOLE DERIVATIVES USEFUL AS KINASE INHIBITORS

Publications (2)

Publication Number Publication Date
EA200601418A1 true EA200601418A1 (ru) 2006-12-29
EA011032B1 EA011032B1 (ru) 2008-12-30

Family

ID=34837492

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200601418A EA011032B1 (ru) 2004-02-03 2005-02-02 ПРОИЗВОДНЫЕ 1H-ТИЕНО[2,3-c]ПИРАЗОЛА, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ИСПОЛЬЗОВАНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗЫ

Country Status (38)

Country Link
US (2) US8138217B2 (ru)
EP (1) EP1711177B1 (ru)
JP (1) JP4908233B2 (ru)
KR (1) KR20060124734A (ru)
CN (1) CN1946395B (ru)
AP (1) AP2006003701A0 (ru)
AR (1) AR047531A1 (ru)
AT (1) ATE396724T1 (ru)
AU (1) AU2005210114B2 (ru)
BR (1) BRPI0507375A (ru)
CA (1) CA2555262C (ru)
CR (1) CR8546A (ru)
CY (1) CY1108246T1 (ru)
DE (1) DE602005007181D1 (ru)
DK (1) DK1711177T3 (ru)
DO (1) DOP2005000014A (ru)
EA (1) EA011032B1 (ru)
EC (1) ECSP066767A (ru)
ES (1) ES2307144T3 (ru)
GE (1) GEP20094633B (ru)
GT (1) GT200500020A (ru)
HK (1) HK1101343A1 (ru)
IL (1) IL177141A0 (ru)
MA (1) MA28429B1 (ru)
MX (1) MXPA06008787A (ru)
NO (1) NO20063768L (ru)
NZ (1) NZ548896A (ru)
PA (1) PA8622801A1 (ru)
PE (1) PE20051095A1 (ru)
PL (1) PL1711177T3 (ru)
PT (1) PT1711177E (ru)
SI (1) SI1711177T1 (ru)
TN (1) TNSN06244A1 (ru)
TW (1) TW200526204A (ru)
UA (1) UA86223C2 (ru)
UY (1) UY28738A1 (ru)
WO (1) WO2005074922A1 (ru)
ZA (1) ZA200606179B (ru)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR0312961A (pt) * 2002-07-25 2005-06-14 Pharmacia Italia Spa Derivados condensados heterociclicos de pirazol como inibidores de cinase
EP1904503B1 (en) * 2005-07-19 2013-11-06 Nerviano Medical Sciences S.R.L. 1h-thieno[2,3-c]-pyrazole compounds useful as kinase inhibitors
WO2007039773A1 (en) * 2005-10-06 2007-04-12 Merck Sharp & Dohme Limited Use of fused pyrrole carboxylic acids for the treatment of neurodegenerative and psychiatric diseases as d-amino acid oxidase inhibitors
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
EP2007380B1 (en) * 2006-03-30 2011-09-14 Nerviano Medical Sciences S.r.l. Use of a kinase inhibitor for the treatment of particular resistant tumors
US8119641B2 (en) 2006-05-31 2012-02-21 Nerviano Medical Sciences S.R.L. 1H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
FR2904626B1 (fr) * 2006-08-03 2008-09-19 Sanofi Aventis Derives de pyrazolo[4,3]thiazole, leur preparation et leur application en therapeutique
JP2010505962A (ja) 2006-10-09 2010-02-25 武田薬品工業株式会社 キナーゼ阻害剤
KR100923540B1 (ko) 2007-11-23 2009-10-27 한국과학기술연구원 5-아실하이드라진카르보닐-3,4-디치환 피라졸 유도체 및이의 제조방법
AR071780A1 (es) * 2008-05-15 2010-07-14 Nerviano Medical Sciences Srl Derivados de carbamoilo de carbonilamino-pirazoles biciclicos como profarmacos
JP2012521429A (ja) * 2009-03-23 2012-09-13 メルク・シャープ・エンド・ドーム・コーポレイション 疼痛治療用のｐ２ｘ３受容体アンタゴニスト
US9255072B2 (en) 2011-03-04 2016-02-09 National Health Rsearch Institutes Pyrazole compounds and thiazole compounds as protein kinases inhibitors
EP2836494B1 (en) * 2012-04-05 2019-08-21 Nerviano Medical Sciences S.r.l. New alkylating agents
EP3663299B1 (en) * 2017-08-01 2023-03-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Bicyclic compound acting as ror gamma inhibitor
BR112020010905A2 (pt) * 2017-11-30 2020-11-17 Hanmi Pharm. Co., Ltd. compostos, composição farmacêutica e uso de um composto ou da composiçao farmacêutica
CN113072562B (zh) * 2021-04-06 2022-01-14 山东大学 一种GSK-3β抑制剂及其制备方法与应用

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3763409D1 (de) 1986-02-19 1990-08-02 Duphar Int Res Thio-verbindungen und ihre wirkung als fungizide.
GB9911053D0 (en) 1999-05-12 1999-07-14 Pharmacia & Upjohn Spa 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents
US6387900B1 (en) 1999-08-12 2002-05-14 Pharmacia & Upjohn S.P.A. 3(5)-ureido-pyrazole derivatives process for their preparation and their use as antitumor agents
BR0013143A (pt) 1999-08-12 2002-06-11 Pharmacia Italia Spa Derivados de 3 (5) amino pirazol, processo para sua preparação e uso dos mesmos como agentes antitumorais
ZA200301813B (en) * 2000-08-10 2004-06-22 Pharmacia Italia Spa Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them.
JP2004517840A (ja) 2000-11-27 2004-06-17 フアルマシア・イタリア・エツセ・ピー・アー フェニルアセトアミド−ピラゾール誘導体およびそれの抗腫瘍薬としての使用
NZ527767A (en) 2001-01-26 2004-11-26 Pharmacia Italia S Chromane derivatives, process for their preparation and their use as antitumor agents
MXPA04001114A (es) 2001-09-26 2004-05-20 Pharmacia Italia Spa Derivados de aminoindazol activos como inhibidores de cinasa, procedimientos para su preparacion y composiciones farmaceuticas que los contienen.
ES2411655T3 (es) * 2002-05-17 2013-07-08 Pfizer Italia S.R.L. Derivados de aminoindazol activos como inhibidores de quinasas, procedimiento para su preparación y composiciones farmacéuticas que los comprenden
ES2304531T3 (es) * 2002-07-17 2008-10-16 Pfizer Italia S.R.L. Derivados heterobiciclicos de pirazol como inhibidores de quinasa.
BR0312961A (pt) * 2002-07-25 2005-06-14 Pharmacia Italia Spa Derivados condensados heterociclicos de pirazol como inibidores de cinase
US20050026984A1 (en) * 2003-07-29 2005-02-03 Aventis Pharma S.A. Substituted thieno [2,3-c] pyrazoles and their use as medicinal products

Also Published As

Publication number Publication date
MXPA06008787A (es) 2007-01-19
TNSN06244A1 (fr) 2007-12-03
AU2005210114A1 (en) 2005-08-18
US20120165311A1 (en) 2012-06-28
IL177141A0 (en) 2006-12-10
WO2005074922A1 (en) 2005-08-18
UA86223C2 (ru) 2009-04-10
US20050187209A1 (en) 2005-08-25
BRPI0507375A (pt) 2007-07-10
PT1711177E (pt) 2008-09-04
DOP2005000014A (es) 2006-08-15
CA2555262A1 (en) 2005-08-18
GEP20094633B (en) 2009-03-10
NO20063768L (no) 2006-11-02
CA2555262C (en) 2014-10-14
JP4908233B2 (ja) 2012-04-04
NZ548896A (en) 2010-05-28
CN1946395B (zh) 2014-04-02
AR047531A1 (es) 2006-01-25
HK1101343A1 (en) 2007-10-18
EP1711177B1 (en) 2008-05-28
PE20051095A1 (es) 2005-12-31
SI1711177T1 (sl) 2008-10-31
KR20060124734A (ko) 2006-12-05
JP2007520513A (ja) 2007-07-26
CY1108246T1 (el) 2014-02-12
EA011032B1 (ru) 2008-12-30
DE602005007181D1 (de) 2008-07-10
PA8622801A1 (es) 2005-11-25
US8481584B2 (en) 2013-07-09
AP2006003701A0 (en) 2006-08-31
ES2307144T3 (es) 2008-11-16
US8138217B2 (en) 2012-03-20
ATE396724T1 (de) 2008-06-15
PL1711177T3 (pl) 2008-11-28
MA28429B1 (fr) 2007-02-01
CR8546A (es) 2007-05-30
UY28738A1 (es) 2005-09-30
ECSP066767A (es) 2006-11-24
EP1711177A1 (en) 2006-10-18
AU2005210114B2 (en) 2011-07-14
DK1711177T3 (da) 2008-09-29
ZA200606179B (en) 2008-02-27
GT200500020A (es) 2005-09-06
TW200526204A (en) 2005-08-16
CN1946395A (zh) 2007-04-11

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